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
5 139 66 None -2 28 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2020.127511
5202 139 66 None -2 28 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2020.127511
CHEMBL39 139 66 None -2 28 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2020.127511
DB08839 139 66 None -2 28 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2020.127511
5 139 66 None -2 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5202 139 66 None -2 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
CHEMBL39 139 66 None -2 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
DB08839 139 66 None -2 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5 139 66 None -2 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5202 139 66 None -2 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
CHEMBL39 139 66 None -2 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
DB08839 139 66 None -2 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5 139 66 None -2 28 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
5202 139 66 None -2 28 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
CHEMBL39 139 66 None -2 28 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
DB08839 139 66 None -2 28 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
4376990 192397 4 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 192397 4 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 192397 4 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
4376990 192397 4 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 192397 4 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 192397 4 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
5 139 66 None -2 28 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
5202 139 66 None -2 28 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
CHEMBL39 139 66 None -2 28 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
DB08839 139 66 None -2 28 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
5 139 66 None -2 28 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
5202 139 66 None -2 28 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
CHEMBL39 139 66 None -2 28 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
DB08839 139 66 None -2 28 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
439280 119501 104 None -3 7 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
6971044 119501 104 None -3 7 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
CHEMBL350221 119501 104 None -3 7 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
5 139 66 None -2 28 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
5202 139 66 None -2 28 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
CHEMBL39 139 66 None -2 28 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
DB08839 139 66 None -2 28 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
5 139 66 None -2 28 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
5202 139 66 None -2 28 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
CHEMBL39 139 66 None -2 28 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
DB08839 139 66 None -2 28 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
439280 119501 104 None -3 7 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
6971044 119501 104 None -3 7 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
CHEMBL350221 119501 104 None -3 7 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
168293874 191571 0 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 191571 0 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
168293874 191571 0 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 191571 0 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
5 139 66 None -2 28 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5202 139 66 None -2 28 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
CHEMBL39 139 66 None -2 28 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
DB08839 139 66 None -2 28 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5 139 66 None -2 28 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5202 139 66 None -2 28 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
CHEMBL39 139 66 None -2 28 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
DB08839 139 66 None -2 28 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5 139 66 None -2 28 Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
5202 139 66 None -2 28 Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
CHEMBL39 139 66 None -2 28 Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
DB08839 139 66 None -2 28 Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
166 3295 12 None 2 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm0709034
3045227 3295 12 None 2 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm0709034
CHEMBL76781 3295 12 None 2 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm0709034
4407909 192254 1 None 1 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192254 1 None 1 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192254 1 None 1 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
44315993 172298 0 None 2 3 Human 8.0 pEC50 = 8 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 222 3 1 3 2.1 CSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
CHEMBL451543 172298 0 None 2 3 Human 8.0 pEC50 = 8 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 222 3 1 3 2.1 CSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
4407909 192254 1 None 1 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192254 1 None 1 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192254 1 None 1 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
16115269 137588 0 None -1 3 Human 7.0 pEC50 = 7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.2 C[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL376676 137588 0 None -1 3 Human 7.0 pEC50 = 7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.2 C[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
9881885 63763 0 None -19 3 Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 269 1 1 2 2.7 COc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL180815 63763 0 None -19 3 Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 269 1 1 2 2.7 COc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
17954204 63592 20 None -81 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1021/jm0709034
CHEMBL180668 63592 20 None -81 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1021/jm0709034
10465263 63986 55 None -89 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL181172 63986 55 None -89 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
11938 2369 5 None -75 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2bAgonist activity at human 5HT2b
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
146192952 2369 5 None -75 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2bAgonist activity at human 5HT2b
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4468760 2369 5 None -75 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2bAgonist activity at human 5HT2b
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
59312249 111168 0 None -8 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 282 3 2 4 2.4 CNc1nc(C(C)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL3286565 111168 0 None -8 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 282 3 2 4 2.4 CNc1nc(C(C)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
122442324 137809 0 None -12 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770174 137809 0 None -12 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771386 137809 0 None -12 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
11658860 2302 47 None -63 4 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
2941 2302 47 None -63 4 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
4374 2302 47 None -63 4 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL360328 2302 47 None -63 4 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
DB04871 2302 47 None -63 4 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
10379910 62956 0 None -6 2 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 297 2 1 2 3.3 COc1cc2c(cc1Br)C(C(C)C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL179329 62956 0 None -6 2 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 297 2 1 2 3.3 COc1cc2c(cc1Br)C(C(C)C)CNCC2 10.1016/j.bmcl.2004.12.080
17954204 63592 20 None -81 3 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL180668 63592 20 None -81 3 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2004.12.080
122442324 137809 0 None -12 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770174 137809 0 None -12 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771386 137809 0 None -12 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
11493484 88627 0 None -23 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337106 88627 0 None -23 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365079 88627 0 None -23 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
46230097 197675 0 None -6 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 217 0 2 3 0.6 O=C1NC2CCNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
CHEMBL590816 197675 0 None -6 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 217 0 2 3 0.6 O=C1NC2CCNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
122442251 137819 0 None -15 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770225 137819 0 None -15 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771396 137819 0 None -15 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
4312735 192262 1 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5183950 192262 1 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221924 192262 1 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
4312735 192262 1 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5183950 192262 1 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221924 192262 1 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
122442251 137819 0 None -15 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770225 137819 0 None -15 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771396 137819 0 None -15 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
44573155 188560 0 None 6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 280 4 2 3 1.1 O=S(=O)(NCC1CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL511044 188560 0 None 6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 280 4 2 3 1.1 O=S(=O)(NCC1CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
168282202 192272 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185430 192272 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221991 192272 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
168282202 192272 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185430 192272 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221991 192272 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
44412404 77400 5 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 206 1 1 2 1.6 Fc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209106 77400 5 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 206 1 1 2 1.6 Fc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
70693928 74121 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 253 5 1 2 3.3 NC[C@H]1C[C@@H]1c1ccccc1OCc1ccccc1 10.1021/ml200206z
CHEMBL2022192 74121 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 253 5 1 2 3.3 NC[C@H]1C[C@@H]1c1ccccc1OCc1ccccc1 10.1021/ml200206z
CHEMBL2028036 74121 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 253 5 1 2 3.3 NC[C@H]1C[C@@H]1c1ccccc1OCc1ccccc1 10.1021/ml200206z
162652937 183070 0 None -67 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4751981 183070 0 None -67 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802812 183070 0 None -67 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
5 139 66 None -2 28 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2009.07.063
5202 139 66 None -2 28 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2009.07.063
CHEMBL39 139 66 None -2 28 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2009.07.063
DB08839 139 66 None -2 28 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2009.07.063
168 3907 11 None 3 5 Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
6604042 3907 11 None 3 5 Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
CHEMBL309760 3907 11 None 3 5 Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
157 2030 5 None -4 4 Rat 7.9 pEC50 = 7.9 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
9840090 2030 5 None -4 4 Rat 7.9 pEC50 = 7.9 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
CHEMBL134519 2030 5 None -4 4 Rat 7.9 pEC50 = 7.9 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
157 2030 5 None -4 4 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1016/j.bmcl.2007.03.073
9840090 2030 5 None -4 4 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1016/j.bmcl.2007.03.073
CHEMBL134519 2030 5 None -4 4 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1016/j.bmcl.2007.03.073
10465263 63986 55 None -89 3 Human 6.0 pEC50 = 6.0 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL181172 63986 55 None -89 3 Human 6.0 pEC50 = 6.0 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1016/j.bmcl.2004.12.080
162652937 183070 0 None -67 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4751981 183070 0 None -67 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802812 183070 0 None -67 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
134265627 163450 0 None -602 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 297 2 1 3 2.5 Fc1cccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)c1 10.1021/acsmedchemlett.8b00328
CHEMBL4208452 163450 0 None -602 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 297 2 1 3 2.5 Fc1cccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)c1 10.1021/acsmedchemlett.8b00328
53324327 56541 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)ccn1 10.1016/j.bmcl.2010.11.089
CHEMBL1643857 56541 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)ccn1 10.1016/j.bmcl.2010.11.089
44572176 12438 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 2 1 1 2.8 Cc1ccc([C@H]2C[C@@H]2CN)c(Br)c1 10.1021/jm801354e
CHEMBL1186735 12438 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 2 1 1 2.8 Cc1ccc([C@H]2C[C@@H]2CN)c(Br)c1 10.1021/jm801354e
CHEMBL475641 12438 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 2 1 1 2.8 Cc1ccc([C@H]2C[C@@H]2CN)c(Br)c1 10.1021/jm801354e
44572207 12578 0 None -8 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F 10.1021/jm801354e
CHEMBL1187556 12578 0 None -8 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F 10.1021/jm801354e
CHEMBL508680 12578 0 None -8 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F 10.1021/jm801354e
11492162 71694 2 None -11 3 Human 5.9 pEC50 = 5.9 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 206 3 1 1 2.4 CN(C)CCc1c[nH]c2cccc(F)c12 10.1016/j.bmcl.2005.06.104
CHEMBL197646 71694 2 None -11 3 Human 5.9 pEC50 = 5.9 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 206 3 1 1 2.4 CN(C)CCc1c[nH]c2cccc(F)c12 10.1016/j.bmcl.2005.06.104
53317924 56542 0 None -6 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 406 4 1 7 1.7 CC(=O)N(C)c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643858 56542 0 None -6 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 406 4 1 7 1.7 CC(=O)N(C)c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
44572180 12440 1 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 175 2 1 1 2.4 Cc1ccc([C@H]2C[C@@H]2CN)cc1C 10.1021/jm801354e
CHEMBL1186737 12440 1 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 175 2 1 1 2.4 Cc1ccc([C@H]2C[C@@H]2CN)cc1C 10.1021/jm801354e
CHEMBL475643 12440 1 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 175 2 1 1 2.4 Cc1ccc([C@H]2C[C@@H]2CN)cc1C 10.1021/jm801354e
11151653 90656 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 Cc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397896 90656 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 Cc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
54587668 61115 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
CHEMBL1770378 61115 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
1355 1972 82 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.063
142 1972 82 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.063
CHEMBL478 1972 82 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.063
DB12110 1972 82 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.063
44573156 186704 0 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 254 2 1 3 0.6 CN(C)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492949 186704 0 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 254 2 1 3 0.6 CN(C)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
1355 1972 82 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
142 1972 82 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
CHEMBL478 1972 82 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
DB12110 1972 82 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
168285159 192302 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5196522 192302 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222172 192302 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
23652278 62287 16 None -83 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 C[C@@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL178365 62287 16 None -83 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 C[C@@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
11608308 63963 3 None -407 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
CHEMBL181076 63963 3 None -407 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
162658803 183100 0 None -14 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4759878 183100 0 None -14 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803107 183100 0 None -14 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
168285159 192302 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5196522 192302 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222172 192302 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
162658803 183100 0 None -14 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4759878 183100 0 None -14 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803107 183100 0 None -14 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
134265732 163244 0 None -1000 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 285 2 1 3 2.3 FC(F)(F)CCc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4206126 163244 0 None -1000 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 285 2 1 3 2.3 FC(F)(F)CCc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
134265665 164236 0 None -1047 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 231 2 1 3 1.8 CCCc1cncc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4218374 164236 0 None -1047 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 231 2 1 3 1.8 CCCc1cncc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
44572751 12378 1 None -16 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL1186509 12378 1 None -16 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL467736 12378 1 None -16 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
53321948 56495 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
CHEMBL1643677 56495 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
189 3423 31 None -1 4 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced increase in inositol1-phosphate accumulation measured after 30 mins by HTRF assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced increase in inositol1-phosphate accumulation measured after 30 mins by HTRF assay
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/acs.jmedchem.0c00424
5163 3423 31 None -1 4 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced increase in inositol1-phosphate accumulation measured after 30 mins by HTRF assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced increase in inositol1-phosphate accumulation measured after 30 mins by HTRF assay
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/acs.jmedchem.0c00424
CHEMBL297784 3423 31 None -1 4 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced increase in inositol1-phosphate accumulation measured after 30 mins by HTRF assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced increase in inositol1-phosphate accumulation measured after 30 mins by HTRF assay
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/acs.jmedchem.0c00424
44431699 87847 0 None -14 3 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 315 4 1 6 1.7 Cc1noc(Cc2c3c(c(C[C@@H](C)N)c4c2OCC4)OCC3)n1 10.1016/j.bmcl.2007.03.073
CHEMBL234837 87847 0 None -14 3 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 315 4 1 6 1.7 Cc1noc(Cc2c3c(c(C[C@@H](C)N)c4c2OCC4)OCC3)n1 10.1016/j.bmcl.2007.03.073
10015414 63140 0 None -32 3 Human 6.9 pEC50 = 6.9 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 259 1 1 2 3.0 COc1cc2c(cc1C(F)(F)F)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL179915 63140 0 None -32 3 Human 6.9 pEC50 = 6.9 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 259 1 1 2 3.0 COc1cc2c(cc1C(F)(F)F)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
16115271 78683 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 298 1 1 2 2.8 CC(C)[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL2113264 78683 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 298 1 1 2 2.8 CC(C)[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
44572168 12363 1 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/jm801354e
CHEMBL1186458 12363 1 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/jm801354e
CHEMBL464475 12363 1 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/jm801354e
10036629 64291 0 None -9 3 Human 6.9 pEC50 = 6.9 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL181787 64291 0 None -9 3 Human 6.9 pEC50 = 6.9 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
23652278 62287 16 None -83 3 Human 5.9 pEC50 = 5.9 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 C[C@@H]1CNCCc2ccc(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178365 62287 16 None -83 3 Human 5.9 pEC50 = 5.9 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 C[C@@H]1CNCCc2ccc(Cl)cc21 10.1016/j.bmcl.2004.12.080
25084025 12577 1 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1cccc(Br)c1 10.1021/jm801354e
CHEMBL1187522 12577 1 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1cccc(Br)c1 10.1021/jm801354e
CHEMBL506727 12577 1 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1cccc(Br)c1 10.1021/jm801354e
45484687 196777 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 339 3 1 5 1.9 O=c1cc2c(nn1Cc1ccccc1OC(F)(F)F)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL577410 196777 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 339 3 1 5 1.9 O=c1cc2c(nn1Cc1ccccc1OC(F)(F)F)CCNCC2 10.1016/j.bmcl.2009.07.063
53323196 56540 0 None -23 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cncc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
CHEMBL1643856 56540 0 None -23 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cncc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
118736623 118478 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 267 3 2 3 2.4 CNc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
CHEMBL3425755 118478 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 267 3 2 3 2.4 CNc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
118733808 120131 0 None -1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
CHEMBL3416056 120131 0 None -1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
CHEMBL3546908 120131 0 None -1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
44573231 186701 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 305 2 1 3 2.3 O=S(=O)(c1ccc(F)cc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492911 186701 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 305 2 1 3 2.3 O=S(=O)(c1ccc(F)cc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
216 2809 29 None 1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/jm0709034
9815618 2809 29 None 1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/jm0709034
CHEMBL253811 2809 29 None 1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/jm0709034
162653458 183074 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4753812 183074 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802839 183074 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
10331841 168627 6 None -158 3 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL440752 168627 6 None -158 3 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1016/j.bmcl.2004.12.080
44412389 77727 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 272 1 1 4 1.7 C[C@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1 10.1016/j.bmcl.2006.03.007
CHEMBL210215 77727 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 272 1 1 4 1.7 C[C@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1 10.1016/j.bmcl.2006.03.007
162653458 183074 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4753812 183074 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802839 183074 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
11447552 62184 4 None -239 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
CHEMBL178231 62184 4 None -239 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
54585653 61121 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 307 2 1 3 2.8 FC(F)(F)c1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
CHEMBL1770385 61121 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 307 2 1 3 2.8 FC(F)(F)c1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
11427139 84249 0 None -38 3 Human 5.8 pEC50 = 5.8 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 282 1 1 2 2.4 C=Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL222566 84249 0 None -38 3 Human 5.8 pEC50 = 5.8 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 282 1 1 2 2.4 C=Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
53325937 56496 0 None -53 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643678 56496 0 None -53 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
25070581 61117 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770380 61117 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
134265616 163848 0 None -1548 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4213447 163848 0 None -1548 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
122442286 137810 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 137810 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 137810 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
118733798 120124 0 None -12 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416051 120124 0 None -12 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546894 120124 0 None -12 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
44573220 186858 0 None 4 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 294 4 1 3 1.4 CN(CC1CC1)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL493951 186858 0 None 4 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 294 4 1 3 1.4 CN(CC1CC1)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
162658689 183098 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4759181 183098 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803103 183098 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
122442272 137807 0 None -54 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137807 0 None -54 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137807 0 None -54 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
44572371 12406 0 None -5 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1cccc(C#CCCCCO)c1 10.1021/jm801354e
CHEMBL1186608 12406 0 None -5 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1cccc(C#CCCCCO)c1 10.1021/jm801354e
CHEMBL472678 12406 0 None -5 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1cccc(C#CCCCCO)c1 10.1021/jm801354e
162658689 183098 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4759181 183098 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803103 183098 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
122442272 137807 0 None -54 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137807 0 None -54 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137807 0 None -54 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
16115652 83064 0 None -15 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 286 1 1 3 1.8 COc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL220211 83064 0 None -15 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 286 1 1 3 1.8 COc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
54580776 61118 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 273 2 1 3 2.4 Clc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
CHEMBL1770381 61118 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 273 2 1 3 2.4 Clc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
118736624 118479 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 281 4 2 3 2.8 CCNc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
CHEMBL3425756 118479 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 281 4 2 3 2.8 CCNc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
44573229 172097 0 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 305 2 1 3 2.3 O=S(=O)(c1ccc2c(c1)CCNCC2)c1ccccc1F 10.1016/j.bmcl.2009.02.071
CHEMBL449999 172097 0 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 305 2 1 3 2.3 O=S(=O)(c1ccc2c(c1)CCNCC2)c1ccccc1F 10.1016/j.bmcl.2009.02.071
42601405 192043 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 287 2 1 3 2.2 O=S(=O)(c1ccccc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL521805 192043 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 287 2 1 3 2.2 O=S(=O)(c1ccccc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
11221167 84243 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL222514 84243 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
162657053 183089 0 None -20 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4757214 183089 0 None -20 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803017 183089 0 None -20 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
10401602 122540 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCOc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL360968 122540 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCOc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
11447552 62184 4 None -239 3 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
CHEMBL178231 62184 4 None -239 3 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
25070907 61113 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
CHEMBL1770376 61113 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
44572369 12337 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 171 2 1 1 1.7 C#Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL1186108 12337 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 171 2 1 1 1.7 C#Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL450178 12337 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 171 2 1 1 1.7 C#Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
46228438 198292 0 None -1862 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1OC1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL595195 198292 0 None -1862 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1OC1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
45485742 196136 0 None -18 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 318 5 1 5 2.2 Clc1ccccc1CCOc1cncc(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.136
CHEMBL572228 196136 0 None -18 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 318 5 1 5 2.2 Clc1ccccc1CCOc1cncc(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.136
44412405 77413 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 255 1 1 1 3.4 FC(F)(F)c1cccc([C@H]2CC[C@H]3CNC[C@@H]23)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209155 77413 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 255 1 1 1 3.4 FC(F)(F)c1cccc([C@H]2CC[C@H]3CNC[C@@H]23)c1 10.1016/j.bmcl.2006.03.007
11777150 62261 0 None -63 3 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 255 0 2 2 2.4 CC1CNCCc2cc(O)c(Br)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178313 62261 0 None -63 3 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 255 0 2 2 2.4 CC1CNCCc2cc(O)c(Br)cc21 10.1016/j.bmcl.2004.12.080
11414184 83071 0 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)C2CNCCN12 10.1021/jm0612968
CHEMBL220274 83071 0 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)C2CNCCN12 10.1021/jm0612968
122442324 137809 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770174 137809 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771386 137809 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442324 137809 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770174 137809 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771386 137809 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
44573216 186745 0 None 4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 268 4 2 3 1.1 CCCNS(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL493151 186745 0 None 4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 268 4 2 3 1.1 CCCNS(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
44572759 12341 1 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 177 3 1 2 1.8 COc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL1186135 12341 1 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 177 3 1 2 1.8 COc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL451368 12341 1 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 177 3 1 2 1.8 COc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
24773650 154147 2 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)CCNCC2C 10.1021/jm0709034
CHEMBL399750 154147 2 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)CCNCC2C 10.1021/jm0709034
118733818 120140 0 None -181 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416061 120140 0 None -181 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546956 120140 0 None -181 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
168294162 192399 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5208129 192399 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222770 192399 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
10331841 168627 6 None -158 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1021/jm0709034
CHEMBL440752 168627 6 None -158 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1021/jm0709034
168294162 192399 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5208129 192399 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222770 192399 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
135453290 133070 23 None 1 8 Rat 8.7 pEC50 = 8.7 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL371300 133070 23 None 1 8 Rat 8.7 pEC50 = 8.7 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
166 3295 12 None 2 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmc.2007.10.100
3045227 3295 12 None 2 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmc.2007.10.100
CHEMBL76781 3295 12 None 2 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmc.2007.10.100
36906 104388 68 None 1 4 Rat 8.6 pEC50 = 8.6 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm050663x
CHEMBL31115 104388 68 None 1 4 Rat 8.6 pEC50 = 8.6 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm050663x
44572367 12421 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1ccccc1C#CCCCCO 10.1021/jm801354e
CHEMBL1186673 12421 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1ccccc1C#CCCCCO 10.1021/jm801354e
CHEMBL474230 12421 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1ccccc1C#CCCCCO 10.1021/jm801354e
168291130 192364 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201835 192364 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222548 192364 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
168291130 192364 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201835 192364 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222548 192364 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
11290492 137461 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 218 1 1 3 0.8 COc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL376456 137461 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 218 1 1 3 0.8 COc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
11499800 88664 0 None -10 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337503 88664 0 None -10 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365465 88664 0 None -10 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
122442254 137804 0 None -26 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770963 137804 0 None -26 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771381 137804 0 None -26 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442254 137804 0 None -26 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770963 137804 0 None -26 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771381 137804 0 None -26 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
44572810 12531 2 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
CHEMBL1187196 12531 2 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
CHEMBL493130 12531 2 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
150 2463 18 None -2 11 Human 7.7 pEC50 = 7.7 Functional
Agonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assayAgonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
1764 2463 18 None -2 11 Human 7.7 pEC50 = 7.7 Functional
Agonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assayAgonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
8226 2463 18 None -2 11 Human 7.7 pEC50 = 7.7 Functional
Agonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assayAgonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
CHEMBL1201356 2463 18 None -2 11 Human 7.7 pEC50 = 7.7 Functional
Agonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assayAgonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
DB00353 2463 18 None -2 11 Human 7.7 pEC50 = 7.7 Functional
Agonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assayAgonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
134265663 163116 0 None -19 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 243 1 1 3 2.1 c1cc(C2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4204710 163116 0 None -19 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 243 1 1 3 2.1 c1cc(C2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
53317923 56537 0 None -5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 365 4 1 7 1.7 COc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
CHEMBL1643853 56537 0 None -5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 365 4 1 7 1.7 COc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
53325936 56493 0 None -12 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 335 3 1 6 1.7 c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643675 56493 0 None -12 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 335 3 1 6 1.7 c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
122442293 137801 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3770599 137801 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3771378 137801 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
122442293 137801 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3770599 137801 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3771378 137801 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
11658860 2302 47 None -63 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
2941 2302 47 None -63 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
4374 2302 47 None -63 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
CHEMBL360328 2302 47 None -63 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
DB04871 2302 47 None -63 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
16115381 83016 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.2 C[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
CHEMBL219837 83016 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.2 C[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
44572166 12339 0 None -7 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
CHEMBL1186133 12339 0 None -7 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
CHEMBL451232 12339 0 None -7 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
118736626 118480 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 307 5 2 3 3.2 c1ccc(Cc2cc3c(c(NCC4CC4)n2)CCNCC3)cc1 10.1021/ml500507v
CHEMBL3425758 118480 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 307 5 2 3 3.2 c1ccc(Cc2cc3c(c(NCC4CC4)n2)CCNCC3)cc1 10.1021/ml500507v
18735305 203215 0 None 2 3 Human 7.7 pEC50 = 7.7 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 320 2 1 2 2.1 C[C@H](N)CN1CCc2cc(F)c(I)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL76301 203215 0 None 2 3 Human 7.7 pEC50 = 7.7 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 320 2 1 2 2.1 C[C@H](N)CN1CCc2cc(F)c(I)cc21 10.1016/j.bmcl.2003.05.001
54583742 61112 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
CHEMBL1770375 61112 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
44389645 63835 0 None -72 3 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 269 1 1 2 2.7 COc1cc2c(cc1Br)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL180867 63835 0 None -72 3 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 269 1 1 2 2.7 COc1cc2c(cc1Br)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
118733790 120146 0 None -36 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416047 120146 0 None -36 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546973 120146 0 None -36 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
44572753 12579 3 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@@H]1C[C@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL1187565 12579 3 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@@H]1C[C@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL509418 12579 3 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@@H]1C[C@H]1c1ccccc1Br 10.1021/jm801354e
53321947 56489 0 None -2 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 257 1 1 5 1.0 c1cc2nc3c(c(N4CCCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
CHEMBL1643671 56489 0 None -2 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 257 1 1 5 1.0 c1cc2nc3c(c(N4CCCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
44431701 87702 0 None -8 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 311 4 1 6 3.4 Cc1noc(Cc2c3ccoc3c(C[C@@H](C)N)c3ccoc23)n1 10.1016/j.bmcl.2007.03.073
CHEMBL234682 87702 0 None -8 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 311 4 1 6 3.4 Cc1noc(Cc2c3ccoc3c(C[C@@H](C)N)c3ccoc23)n1 10.1016/j.bmcl.2007.03.073
44409290 74287 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Efficacy against human recombinant 5HT2B receptor induced intracellular calcium mobilization in CHO cells by FLIPREfficacy against human recombinant 5HT2B receptor induced intracellular calcium mobilization in CHO cells by FLIPR
ChEMBL 273 4 1 4 1.7 C[C@@H]1CNC[C@H]2Cc3ccc(COCC4CC4)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL203013 74287 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Efficacy against human recombinant 5HT2B receptor induced intracellular calcium mobilization in CHO cells by FLIPREfficacy against human recombinant 5HT2B receptor induced intracellular calcium mobilization in CHO cells by FLIPR
ChEMBL 273 4 1 4 1.7 C[C@@H]1CNC[C@H]2Cc3ccc(COCC4CC4)nc3N12 10.1016/j.bmcl.2005.11.083
10017556 161318 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 297 2 1 2 3.5 CC(C)Oc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL415029 161318 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 297 2 1 2 3.5 CC(C)Oc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
118733760 120113 1 None -3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416032 120113 1 None -3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546869 120113 1 None -3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
11630623 88656 0 None -213 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337499 88656 0 None -213 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365399 88656 0 None -213 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
58911653 90671 0 None -25 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 244 1 1 2 1.5 CCc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397911 90671 0 None -25 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 244 1 1 2 1.5 CCc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
168291896 192373 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201903 192373 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222595 192373 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
145 140 48 None -134 12 Rat 6.6 pEC50 = 6.6 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
1832 140 48 None -134 12 Rat 6.6 pEC50 = 6.6 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
CHEMBL7257 140 48 None -134 12 Rat 6.6 pEC50 = 6.6 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
DB14010 140 48 None -134 12 Rat 6.6 pEC50 = 6.6 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
25070911 111167 0 None -7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 324 3 1 5 1.6 c1ccc(Cc2nc3c(c(N4CCOCC4)n2)CCNCC3)cc1 10.1021/jm5003292
CHEMBL3286564 111167 0 None -7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 324 3 1 5 1.6 c1ccc(Cc2nc3c(c(N4CCOCC4)n2)CCNCC3)cc1 10.1021/jm5003292
168291564 192371 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5201470 192371 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222574 192371 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
168291896 192373 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201903 192373 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222595 192373 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
122442250 137803 0 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770689 137803 0 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771380 137803 0 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
5 139 66 None -2 28 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
5202 139 66 None -2 28 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
CHEMBL39 139 66 None -2 28 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
DB08839 139 66 None -2 28 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
168291564 192371 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5201470 192371 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222574 192371 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
122442250 137803 0 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770689 137803 0 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771380 137803 0 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
24773816 94402 0 None -31 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
CHEMBL253805 94402 0 None -31 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
24773814 94405 1 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 209 1 1 1 3.0 CC[C@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL253809 94405 1 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 209 1 1 1 3.0 CC[C@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
11264345 129864 5 None -120 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 213 0 1 1 2.7 CC1CNCCc2ccc(Cl)c(F)c21 10.1021/jm0709034
CHEMBL368016 129864 5 None -120 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 213 0 1 1 2.7 CC1CNCCc2ccc(Cl)c(F)c21 10.1021/jm0709034
122442300 137808 0 None -8 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769421 137808 0 None -8 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771385 137808 0 None -8 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
122442300 137808 0 None -8 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769421 137808 0 None -8 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771385 137808 0 None -8 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
146025684 183043 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4743977 183043 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802486 183043 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
162652983 183071 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4752412 183071 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802814 183071 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
146025684 183043 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4743977 183043 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802486 183043 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
162652983 183071 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4752412 183071 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802814 183071 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
45484673 197270 0 None -8 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 289 2 1 4 1.6 O=c1cc2c(nn1Cc1ccc(Cl)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL585012 197270 0 None -8 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 289 2 1 4 1.6 O=c1cc2c(nn1Cc1ccc(Cl)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
11595191 88617 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337488 88617 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2364960 88617 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
162658153 183093 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4758641 183093 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803076 183093 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
162658153 183093 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4758641 183093 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803076 183093 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
118736627 118481 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 295 5 2 3 3.2 CCCNc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
CHEMBL3425759 118481 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 295 5 2 3 3.2 CCCNc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
118736631 118484 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 238 2 1 2 2.4 c1ccc(Cc2cc3c(cn2)CCNCC3)cc1 10.1021/ml500507v
CHEMBL3425763 118484 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 238 2 1 2 2.4 c1ccc(Cc2cc3c(cn2)CCNCC3)cc1 10.1021/ml500507v
122442270 137805 1 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770753 137805 1 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771382 137805 1 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442270 137805 1 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770753 137805 1 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771382 137805 1 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
11952353 198168 0 None -1905 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 345 4 1 4 3.0 Fc1ccc(F)c(CO[C@H]2CCc3ccc(N4CCNCC4)nc32)c1 10.1016/j.bmcl.2009.10.112
CHEMBL594469 198168 0 None -1905 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 345 4 1 4 3.0 Fc1ccc(F)c(CO[C@H]2CCc3ccc(N4CCNCC4)nc32)c1 10.1016/j.bmcl.2009.10.112
11171955 90648 0 None -4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.2 C[C@@H]1c2ccccc2C(=O)N2CCNC[C@@H]12 10.1016/j.bmcl.2013.04.061
CHEMBL2397888 90648 0 None -4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.2 C[C@@H]1c2ccccc2C(=O)N2CCNC[C@@H]12 10.1016/j.bmcl.2013.04.061
44573002 12562 1 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Br)cc1 10.1021/jm801354e
CHEMBL1187408 12562 1 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Br)cc1 10.1021/jm801354e
CHEMBL501854 12562 1 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Br)cc1 10.1021/jm801354e
16115511 84399 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 250 1 1 2 2.0 CCc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL223466 84399 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 250 1 1 2 2.0 CCc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
162643473 183023 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4777303 183023 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802306 183023 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
162643473 183023 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4777303 183023 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802306 183023 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
11300712 141142 0 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 252 1 1 3 1.4 COc1c(Cl)ccc2c1C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL385577 141142 0 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 252 1 1 3 1.4 COc1c(Cl)ccc2c1C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
44573018 12520 1 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)c(F)c1 10.1021/jm801354e
CHEMBL1187169 12520 1 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)c(F)c1 10.1021/jm801354e
CHEMBL492306 12520 1 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)c(F)c1 10.1021/jm801354e
24826869 90657 0 None -7 3 Human 7.6 pEC50 = 7.6 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 230 1 1 2 1.2 CCc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397897 90657 0 None -7 3 Human 7.6 pEC50 = 7.6 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 230 1 1 2 1.2 CCc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
16115654 136437 0 None -46 3 Human 6.6 pEC50 = 6.6 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.1 Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374562 136437 0 None -46 3 Human 6.6 pEC50 = 6.6 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.1 Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
53324629 56490 0 None -4 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 271 1 1 5 1.4 c1cc2nc3c(c(N4CCCCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
CHEMBL1643672 56490 0 None -4 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 271 1 1 5 1.4 c1cc2nc3c(c(N4CCCCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
1355 1972 82 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
142 1972 82 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
CHEMBL478 1972 82 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
DB12110 1972 82 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
1355 1972 82 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
142 1972 82 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
CHEMBL478 1972 82 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
DB12110 1972 82 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
46937339 73846 0 None -13 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 235 5 1 2 2.7 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1021/ml200206z
CHEMBL2023357 73846 0 None -13 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 235 5 1 2 2.7 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1021/ml200206z
46937339 73846 0 None -13 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium mobilizationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium mobilization
ChEMBL 235 5 1 2 2.7 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1021/jm5019274
CHEMBL2023357 73846 0 None -13 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium mobilizationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium mobilization
ChEMBL 235 5 1 2 2.7 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1021/jm5019274
16115392 84359 0 None -5 2 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 236 0 1 2 1.7 Cc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL223292 84359 0 None -5 2 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 236 0 1 2 1.7 Cc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
16115388 136828 0 None -2 3 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 284 1 1 2 2.6 CC[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
CHEMBL375302 136828 0 None -2 3 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 284 1 1 2 2.6 CC[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
11209786 136703 0 None -208 3 Human 5.5 pEC50 = 5.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 296 1 1 2 2.7 O=C1c2c(cc(C3CC3)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL375170 136703 0 None -208 3 Human 5.5 pEC50 = 5.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 296 1 1 2 2.7 O=C1c2c(cc(C3CC3)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
9859257 203403 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 218 2 1 3 1.3 C[C@H](N)CN1CCc2ccc3c(c21)CCO3 10.1016/j.bmcl.2003.05.001
CHEMBL77880 203403 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 218 2 1 3 1.3 C[C@H](N)CN1CCc2ccc3c(c21)CCO3 10.1016/j.bmcl.2003.05.001
168268877 189367 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 189367 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
168268877 189367 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 189367 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
230 4043 18 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.10.100
3045225 4043 18 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.10.100
CHEMBL407909 4043 18 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.10.100
5 139 66 None -7 28 Rat 8.5 pEC50 = 8.5 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
5202 139 66 None -7 28 Rat 8.5 pEC50 = 8.5 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
CHEMBL39 139 66 None -7 28 Rat 8.5 pEC50 = 8.5 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
DB08839 139 66 None -7 28 Rat 8.5 pEC50 = 8.5 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
44572798 12526 2 None -1 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1cccc(F)c1 10.1021/jm801354e
CHEMBL1187187 12526 2 None -1 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1cccc(F)c1 10.1021/jm801354e
CHEMBL492926 12526 2 None -1 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1cccc(F)c1 10.1021/jm801354e
46933845 15971 0 None -18 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2B receptor assessed as 5HT-induced calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor assessed as 5HT-induced calcium mobilization by FLIPR assay
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224034 15971 0 None -18 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2B receptor assessed as 5HT-induced calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor assessed as 5HT-induced calcium mobilization by FLIPR assay
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
54583743 61119 0 None 5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 273 2 1 3 2.4 Clc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
CHEMBL1770382 61119 0 None 5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 273 2 1 3 2.4 Clc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
118736630 118483 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 281 3 1 3 2.4 CN(C)c1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
CHEMBL3425762 118483 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 281 3 1 3 2.4 CN(C)c1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
122442263 137816 0 None -30 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769454 137816 0 None -30 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771393 137816 0 None -30 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
44389646 64537 0 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 269 1 1 2 2.7 COc1cc2c(cc1Br)[C@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL182184 64537 0 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 269 1 1 2 2.7 COc1cc2c(cc1Br)[C@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
122442263 137816 0 None -30 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769454 137816 0 None -30 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771393 137816 0 None -30 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442260 137813 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769543 137813 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771390 137813 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
11949712 200466 0 None -3019 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL609306 200466 0 None -3019 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
118733764 120120 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416034 120120 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546890 120120 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
118733776 120126 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
CHEMBL3416040 120126 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
CHEMBL3546903 120126 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
70687695 74114 0 None -12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 205 5 1 2 2.5 CCCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2022186 74114 0 None -12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 205 5 1 2 2.5 CCCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2027987 74114 0 None -12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 205 5 1 2 2.5 CCCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
134265675 163804 0 None -40 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 297 2 1 3 2.5 Fc1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
CHEMBL4212834 163804 0 None -40 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 297 2 1 3 2.5 Fc1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
162645074 183032 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4740346 183032 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802388 183032 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
162645074 183032 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4740346 183032 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802388 183032 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
11400855 12333 6 None -3 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@@H]1C[C@H]1c1ccccc1 10.1021/jm801354e
CHEMBL1186092 12333 6 None -3 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@@H]1C[C@H]1c1ccccc1 10.1021/jm801354e
CHEMBL449134 12333 6 None -3 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@@H]1C[C@H]1c1ccccc1 10.1021/jm801354e
57799306 88666 0 None -12 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337493 88666 0 None -12 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365469 88666 0 None -12 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
122442260 137813 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769543 137813 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771390 137813 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
44315697 203784 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 254 4 1 3 2.6 CCSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
CHEMBL80731 203784 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 254 4 1 3 2.6 CCSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
168268736 192177 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177718 192177 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221369 192177 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
9990808 122244 0 None -51 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 213 0 1 1 2.7 CC1CNCCc2cc(F)c(Cl)cc21 10.1021/jm0709034
CHEMBL360492 122244 0 None -51 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 213 0 1 1 2.7 CC1CNCCc2cc(F)c(Cl)cc21 10.1021/jm0709034
168268736 192177 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177718 192177 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221369 192177 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
11652452 88683 0 None -9 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337492 88683 0 None -9 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365703 88683 0 None -9 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
44572749 12316 1 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccccc1Cl 10.1021/jm801354e
CHEMBL1185954 12316 1 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccccc1Cl 10.1021/jm801354e
CHEMBL443128 12316 1 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccccc1Cl 10.1021/jm801354e
44412150 77365 0 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CCC3CNCC32)n1 10.1016/j.bmcl.2006.03.007
CHEMBL208936 77365 0 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CCC3CNCC32)n1 10.1016/j.bmcl.2006.03.007
11658860 2302 47 None -63 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
2941 2302 47 None -63 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
4374 2302 47 None -63 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
CHEMBL360328 2302 47 None -63 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
DB04871 2302 47 None -63 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
122442250 137803 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770689 137803 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771380 137803 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
16115644 136424 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.4 CCc1cc2c(cc1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374436 136424 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.4 CCc1cc2c(cc1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
118736628 118482 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 295 4 2 3 3.2 CC(C)Nc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
CHEMBL3425760 118482 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 295 4 2 3 3.2 CC(C)Nc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
44573230 186700 0 None -3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 305 2 1 3 2.3 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492910 186700 0 None -3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 305 2 1 3 2.3 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
3356430 192434 2 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5208864 192434 2 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222941 192434 2 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
70683433 74094 1 None -18 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 191 4 1 2 2.1 CCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2022185 74094 1 None -18 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 191 4 1 2 2.1 CCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2027895 74094 1 None -18 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 191 4 1 2 2.1 CCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
122442250 137803 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770689 137803 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771380 137803 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442266 137802 0 None -51 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769499 137802 0 None -51 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771379 137802 0 None -51 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442266 137802 0 None -51 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769499 137802 0 None -51 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771379 137802 0 None -51 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
44573016 12546 1 None -38 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1c(F)cccc1F 10.1021/jm801354e
CHEMBL1187322 12546 1 None -38 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1c(F)cccc1F 10.1021/jm801354e
CHEMBL498863 12546 1 None -38 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1c(F)cccc1F 10.1021/jm801354e
168272608 192181 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177484 192181 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221391 192181 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
162657053 183089 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4757214 183089 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803017 183089 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
168272608 192181 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177484 192181 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221391 192181 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
3356430 192434 2 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5208864 192434 2 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222941 192434 2 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
44573222 173730 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 294 2 1 3 1.5 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCCCC1 10.1016/j.bmcl.2009.02.071
CHEMBL455039 173730 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 294 2 1 3 1.5 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCCCC1 10.1016/j.bmcl.2009.02.071
118733766 120114 0 None -33 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416035 120114 0 None -33 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546870 120114 0 None -33 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
146025686 183167 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4790992 183167 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803813 183167 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
146025686 183167 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4790992 183167 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803813 183167 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
44572757 12525 1 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1ccccc1C(F)(F)F 10.1021/jm801354e
CHEMBL1187186 12525 1 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1ccccc1C(F)(F)F 10.1021/jm801354e
CHEMBL492917 12525 1 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1ccccc1C(F)(F)F 10.1021/jm801354e
45484742 196831 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 243 3 2 3 1.7 c1ccc(COc2n[nH]c3c2CCNCC3)cc1 10.1016/j.bmcl.2009.07.063
CHEMBL577903 196831 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 243 3 2 3 1.7 c1ccc(COc2n[nH]c3c2CCNCC3)cc1 10.1016/j.bmcl.2009.07.063
122442286 137810 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 137810 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 137810 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442286 137810 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 137810 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 137810 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
44573221 192468 0 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 280 2 1 3 1.2 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCCC1 10.1016/j.bmcl.2009.02.071
CHEMBL522514 192468 0 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 280 2 1 3 1.2 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCCC1 10.1016/j.bmcl.2009.02.071
44622848 192734 0 None -11 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 255 2 1 4 1.0 O=c1cc2c(nn1Cc1ccccc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL524778 192734 0 None -11 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 255 2 1 4 1.0 O=c1cc2c(nn1Cc1ccccc1)CCNCC2 10.1016/j.bmcl.2009.07.063
9881119 203752 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 232 2 1 3 1.7 C[C@H](N)CN1CCc2ccc3c(c21)CCCO3 10.1016/j.bmcl.2003.05.001
CHEMBL80482 203752 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 232 2 1 3 1.7 C[C@H](N)CN1CCc2ccc3c(c21)CCCO3 10.1016/j.bmcl.2003.05.001
9990808 122244 0 None -51 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 213 0 1 1 2.7 CC1CNCCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL360492 122244 0 None -51 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 213 0 1 1 2.7 CC1CNCCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
44573012 12519 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1cccc(F)c1F 10.1021/jm801354e
CHEMBL1187168 12519 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1cccc(F)c1F 10.1021/jm801354e
CHEMBL492305 12519 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1cccc(F)c1F 10.1021/jm801354e
11206703 90647 0 None -12 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 C[C@@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
CHEMBL2397887 90647 0 None -12 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 C[C@@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
44572657 12346 5 None -7 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
CHEMBL1186169 12346 5 None -7 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
CHEMBL452719 12346 5 None -7 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
44573004 12399 1 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1 10.1021/jm801354e
CHEMBL1186590 12399 1 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1 10.1021/jm801354e
CHEMBL471202 12399 1 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1 10.1021/jm801354e
53325938 56497 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 365 4 1 7 1.7 COc1ccccc1OC1CN(c2c3c(nc4ccnn24)CCNCC3)C1 10.1016/j.bmcl.2010.11.089
CHEMBL1643679 56497 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 365 4 1 7 1.7 COc1ccccc1OC1CN(c2c3c(nc4ccnn24)CCNCC3)C1 10.1016/j.bmcl.2010.11.089
10105208 62155 0 None -83 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178124 62155 0 None -83 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1016/j.bmcl.2004.12.080
1355 1972 82 None -5 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0709034
142 1972 82 None -5 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0709034
CHEMBL478 1972 82 None -5 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0709034
DB12110 1972 82 None -5 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0709034
24773649 94373 0 None -10 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
CHEMBL253591 94373 0 None -10 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
24773651 154306 0 None -6 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@H](C)CNCC2 10.1021/jm0709034
CHEMBL400600 154306 0 None -6 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@H](C)CNCC2 10.1021/jm0709034
46228437 198291 0 None -39 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL595194 198291 0 None -39 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
24773895 94403 0 None -50 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@@H](C)CNCC2 10.1021/jm0709034
CHEMBL253806 94403 0 None -50 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@@H](C)CNCC2 10.1021/jm0709034
122442270 137805 1 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770753 137805 1 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771382 137805 1 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
24773979 129634 17 None -12 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1021/jm0709034
CHEMBL367796 129634 17 None -12 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1021/jm0709034
11264955 203243 0 None 1 3 Human 8.4 pEC50 = 8.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 240 3 1 3 2.3 CSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
CHEMBL76474 203243 0 None 1 3 Human 8.4 pEC50 = 8.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 240 3 1 3 2.3 CSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
152 361 18 None -2 6 Rat 8.4 pEC50 = 8.4 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
2107 361 18 None -2 6 Rat 8.4 pEC50 = 8.4 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
CHEMBL275854 361 18 None -2 6 Rat 8.4 pEC50 = 8.4 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
11708275 72352 3 None 1 3 Rat 8.4 pEC50 = 8.4 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 205 3 1 4 1.4 COc1ccc2cnn(C[C@H](C)N)c2c1 10.1021/jm050663x
CHEMBL199775 72352 3 None 1 3 Rat 8.4 pEC50 = 8.4 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 205 3 1 4 1.4 COc1ccc2cnn(C[C@H](C)N)c2c1 10.1021/jm050663x
166 3295 12 None 2 4 Human 8.4 pEC50 = 8.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
3045227 3295 12 None 2 4 Human 8.4 pEC50 = 8.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
CHEMBL76781 3295 12 None 2 4 Human 8.4 pEC50 = 8.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
5 139 66 None -2 28 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF methodAgonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2018.01.002
5202 139 66 None -2 28 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF methodAgonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2018.01.002
CHEMBL39 139 66 None -2 28 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF methodAgonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2018.01.002
DB08839 139 66 None -2 28 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF methodAgonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2018.01.002
16047544 12524 7 None -3 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL1187185 12524 7 None -3 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL492916 12524 7 None -3 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
44572172 12424 0 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 179 2 1 1 2.2 Cc1cc([C@H]2C[C@@H]2CN)ccc1F 10.1021/jm801354e
CHEMBL1186686 12424 0 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 179 2 1 1 2.2 Cc1cc([C@H]2C[C@@H]2CN)ccc1F 10.1021/jm801354e
CHEMBL474633 12424 0 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 179 2 1 1 2.2 Cc1cc([C@H]2C[C@@H]2CN)ccc1F 10.1021/jm801354e
16115267 84355 0 None -2 3 Human 7.4 pEC50 = 7.4 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.2 C[C@@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL223272 84355 0 None -2 3 Human 7.4 pEC50 = 7.4 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.2 C[C@@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
9994008 165585 0 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCC1CNCCc2cc(OC)c(Br)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL426235 165585 0 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCC1CNCCc2cc(OC)c(Br)cc21 10.1016/j.bmcl.2004.12.080
122442270 137805 1 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770753 137805 1 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771382 137805 1 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
22368315 63420 0 None -50 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 255 1 1 2 2.1 COc1cc2c(cc1Br)CCNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL180166 63420 0 None -50 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 255 1 1 2 2.1 COc1cc2c(cc1Br)CCNCC2 10.1016/j.bmcl.2004.12.080
134265618 163492 0 None -323 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNCC1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4209052 163492 0 None -323 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNCC1CC2 10.1021/acsmedchemlett.8b00328
46884138 8343 0 None -812 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at 5HT2B receptorAgonist activity at 5HT2B receptor
ChEMBL 364 7 2 4 3.2 COc1cc(OCC2CCCCC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1093699 8343 0 None -812 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at 5HT2B receptorAgonist activity at 5HT2B receptor
ChEMBL 364 7 2 4 3.2 COc1cc(OCC2CCCCC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
44572812 12393 1 None -5 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1 10.1021/jm801354e
CHEMBL1186561 12393 1 None -5 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1 10.1021/jm801354e
CHEMBL469729 12393 1 None -5 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1 10.1021/jm801354e
54587669 61116 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
CHEMBL1770379 61116 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
11609026 88684 0 None -125 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337500 88684 0 None -125 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365705 88684 0 None -125 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
44573014 12400 1 None -10 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)cc1F 10.1021/jm801354e
CHEMBL1186595 12400 1 None -10 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)cc1F 10.1021/jm801354e
CHEMBL471802 12400 1 None -10 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)cc1F 10.1021/jm801354e
3568128 192321 1 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5195443 192321 1 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222291 192321 1 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
3568128 192321 1 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5195443 192321 1 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222291 192321 1 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
44420682 137070 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 0 2 2.1 CN1CCN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2C1 10.1021/jm0612968
CHEMBL375642 137070 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 0 2 2.1 CN1CCN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2C1 10.1021/jm0612968
118733802 120128 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.4 C=C(C)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416053 120128 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.4 C=C(C)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546905 120128 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.4 C=C(C)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
168284548 192299 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 1 3 2 4.1 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5191889 192299 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 1 3 2 4.1 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222143 192299 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 1 3 2 4.1 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
168284548 192299 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 1 3 2 4.1 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5191889 192299 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 1 3 2 4.1 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222143 192299 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 1 3 2 4.1 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
118733788 120139 0 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416046 120139 0 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546955 120139 0 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
11658860 2302 47 None -63 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
2941 2302 47 None -63 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
4374 2302 47 None -63 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
CHEMBL360328 2302 47 None -63 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
DB04871 2302 47 None -63 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
146025689 183125 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4781163 183125 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803350 183125 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
11658860 2302 47 None -63 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
2941 2302 47 None -63 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
4374 2302 47 None -63 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
CHEMBL360328 2302 47 None -63 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
DB04871 2302 47 None -63 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
146025689 183125 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4781163 183125 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803350 183125 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
118733792 120147 0 None -12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416048 120147 0 None -12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546974 120147 0 None -12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
162659286 183103 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4762225 183103 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803142 183103 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
122442266 137802 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769499 137802 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771379 137802 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442266 137802 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769499 137802 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771379 137802 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
162659286 183103 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4762225 183103 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803142 183103 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
146025687 183123 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4779260 183123 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803306 183123 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
118733804 120129 0 None -4 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3416054 120129 0 None -4 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3546906 120129 0 None -4 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
162668367 183147 0 None -21 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4786831 183147 0 None -21 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803642 183147 0 None -21 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
122442309 137806 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769828 137806 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771383 137806 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
168294156 192393 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5207023 192393 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222736 192393 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
162668367 183147 0 None -21 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4786831 183147 0 None -21 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803642 183147 0 None -21 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
168294156 192393 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5207023 192393 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222736 192393 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
122442254 137804 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770963 137804 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771381 137804 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442309 137806 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769828 137806 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771383 137806 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
44572164 12559 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1F 10.1021/jm801354e
CHEMBL1187390 12559 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1F 10.1021/jm801354e
CHEMBL501526 12559 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1F 10.1021/jm801354e
146025687 183123 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4779260 183123 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803306 183123 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
46230099 197622 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 251 0 2 3 1.2 O=C1NC2CCNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
CHEMBL590483 197622 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 251 0 2 3 1.2 O=C1NC2CCNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
118733794 120148 0 None -72 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416049 120148 0 None -72 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546975 120148 0 None -72 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
122442254 137804 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770963 137804 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771381 137804 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442286 137810 0 None -34 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 137810 0 None -34 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 137810 0 None -34 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
45484682 196684 0 None -3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 323 2 1 4 2.0 O=c1cc2c(nn1Cc1ccc(C(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL576651 196684 0 None -3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 323 2 1 4 2.0 O=c1cc2c(nn1Cc1ccc(C(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
11658860 2302 47 None -63 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
2941 2302 47 None -63 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
4374 2302 47 None -63 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
CHEMBL360328 2302 47 None -63 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
DB04871 2302 47 None -63 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
44573153 186604 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 336 3 2 3 2.8 O=S(=O)(Nc1ccccc1Cl)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492348 186604 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 336 3 2 3 2.8 O=S(=O)(Nc1ccccc1Cl)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
44573157 186705 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 316 3 1 3 2.2 CN(c1ccccc1)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492950 186705 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 316 3 1 3 2.2 CN(c1ccccc1)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
134265622 164190 0 None -81 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 259 1 1 3 2.4 CC(C)(C)Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4217787 164190 0 None -81 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 259 1 1 3 2.4 CC(C)(C)Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
44412388 77805 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 272 1 1 4 1.7 C[C@@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1 10.1016/j.bmcl.2006.03.007
CHEMBL210484 77805 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 272 1 1 4 1.7 C[C@@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1 10.1016/j.bmcl.2006.03.007
145966293 163891 0 None -14 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 267 0 1 3 1.6 Brc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4213971 163891 0 None -14 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 267 0 1 3 1.6 Brc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
18735309 203712 0 None 2 3 Human 7.3 pEC50 = 7.3 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 262 2 1 2 2.6 C[C@H](N)CN1CCc2cc(F)c(C(F)(F)F)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL80246 203712 0 None 2 3 Human 7.3 pEC50 = 7.3 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 262 2 1 2 2.6 C[C@H](N)CN1CCc2cc(F)c(C(F)(F)F)cc21 10.1016/j.bmcl.2003.05.001
118733814 120133 0 None -23 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
CHEMBL3416059 120133 0 None -23 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
CHEMBL3546910 120133 0 None -23 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
44572761 12556 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1ccccc1O 10.1021/jm801354e
CHEMBL1187377 12556 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1ccccc1O 10.1021/jm801354e
CHEMBL501117 12556 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1ccccc1O 10.1021/jm801354e
11302765 83818 2 None -309 3 Human 5.3 pEC50 = 5.3 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 284 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL221113 83818 2 None -309 3 Human 5.3 pEC50 = 5.3 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 284 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
11448649 83006 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 272 1 1 3 1.7 O=C1c2c(OC(F)(F)F)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL219734 83006 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 272 1 1 3 1.7 O=C1c2c(OC(F)(F)F)cccc2C2CNCCN12 10.1021/jm0612968
50878551 90300 60 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90300 60 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
50878551 90300 60 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90300 60 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
44572808 12582 0 None -1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1cccc(O)c1 10.1021/jm801354e
CHEMBL1187585 12582 0 None -1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1cccc(O)c1 10.1021/jm801354e
CHEMBL510383 12582 0 None -1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1cccc(O)c1 10.1021/jm801354e
44431688 152196 0 None 1 3 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 307 7 1 5 1.6 COCCOCc1c2c(c(C[C@@H](C)N)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
CHEMBL397321 152196 0 None 1 3 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 307 7 1 5 1.6 COCCOCc1c2c(c(C[C@@H](C)N)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
5 139 66 None -2 28 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
5202 139 66 None -2 28 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
CHEMBL39 139 66 None -2 28 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
DB08839 139 66 None -2 28 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
135509961 135596 2 None -1 3 Rat 8.2 pEC50 = 8.2 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 225 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(Cl)c21 10.1021/jm050663x
CHEMBL373245 135596 2 None -1 3 Rat 8.2 pEC50 = 8.2 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 225 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(Cl)c21 10.1021/jm050663x
9991444 62288 0 None -15 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
CHEMBL178366 62288 0 None -15 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
154699445 176842 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Antagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assayAntagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assay
ChEMBL 319 4 0 4 4.2 CCP(=O)(OC)c1ccc2oc(-c3ccc(F)cc3)nc2c1 10.1021/acs.jmedchem.0c00807
CHEMBL4638592 176842 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Antagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assayAntagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assay
ChEMBL 319 4 0 4 4.2 CCP(=O)(OC)c1ccc2oc(-c3ccc(F)cc3)nc2c1 10.1021/acs.jmedchem.0c00807
11737032 84578 0 None -13 3 Human 6.3 pEC50 = 6.3 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 222 0 1 2 1.4 O=C1c2c(Cl)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL223896 84578 0 None -13 3 Human 6.3 pEC50 = 6.3 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 222 0 1 2 1.4 O=C1c2c(Cl)cccc2C2CNCCN12 10.1021/jm0612968
162674022 182629 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assay
ChEMBL 305 4 1 4 3.5 N#Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
CHEMBL4796102 182629 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assay
ChEMBL 305 4 1 4 3.5 N#Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
22292784 64248 12 None -17 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1021/jm0709034
CHEMBL181672 64248 12 None -17 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1021/jm0709034
24773809 94428 0 None -63 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 C[C@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
CHEMBL254009 94428 0 None -63 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 C[C@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
122442300 137808 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769421 137808 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771385 137808 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
24773900 122903 8 None -6 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 191 1 1 2 1.9 COc1ccc2c(c1)C(C)CNCC2 10.1021/jm0709034
CHEMBL361742 122903 8 None -6 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 191 1 1 2 1.9 COc1ccc2c(c1)C(C)CNCC2 10.1021/jm0709034
118733778 120135 0 None -19 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
CHEMBL3416041 120135 0 None -19 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
CHEMBL3546951 120135 0 None -19 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
50942111 56538 0 None -5 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 365 4 1 7 1.7 COc1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643854 56538 0 None -5 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 365 4 1 7 1.7 COc1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
45485725 196140 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 348 5 1 6 1.9 C[C@@H](COc1ccccc1Cl)n1nc(N2CCNCC2)ccc1=O 10.1016/j.bmcl.2009.07.136
CHEMBL572252 196140 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 348 5 1 6 1.9 C[C@@H](COc1ccccc1Cl)n1nc(N2CCNCC2)ccc1=O 10.1016/j.bmcl.2009.07.136
122442300 137808 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769421 137808 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771385 137808 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
44572698 12430 0 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 197 2 1 1 2.9 NC[C@H]1C[C@@H]1c1ccc2ccccc2c1 10.1021/jm801354e
CHEMBL1186700 12430 0 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 197 2 1 1 2.9 NC[C@H]1C[C@@H]1c1ccc2ccccc2c1 10.1021/jm801354e
CHEMBL474885 12430 0 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 197 2 1 1 2.9 NC[C@H]1C[C@@H]1c1ccc2ccccc2c1 10.1021/jm801354e
162652562 183065 0 None -4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4752604 183065 0 None -4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4802785 183065 0 None -4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
11658860 2302 47 None -63 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
2941 2302 47 None -63 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
4374 2302 47 None -63 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
CHEMBL360328 2302 47 None -63 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
DB04871 2302 47 None -63 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
11666237 88669 0 None -30 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337496 88669 0 None -30 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365472 88669 0 None -30 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
162652562 183065 0 None -4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4752604 183065 0 None -4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4802785 183065 0 None -4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
44572755 12338 1 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL1186115 12338 1 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL450599 12338 1 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
22292784 64248 12 None -17 3 Human 6.3 pEC50 = 6.3 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1016/j.bmcl.2004.12.080
CHEMBL181672 64248 12 None -17 3 Human 6.3 pEC50 = 6.3 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1016/j.bmcl.2004.12.080
118733780 120115 0 None -7 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 6 1 3 2.4 COCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416042 120115 0 None -7 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 6 1 3 2.4 COCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546871 120115 0 None -7 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 6 1 3 2.4 COCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
3572096 192286 1 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5186011 192286 1 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222066 192286 1 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
3572096 192286 1 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5186011 192286 1 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222066 192286 1 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
162670523 183158 0 None -20 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4790652 183158 0 None -20 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803766 183158 0 None -20 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
146025688 183102 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4761064 183102 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803134 183102 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
146025688 183102 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4761064 183102 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803134 183102 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
11313985 90638 0 None -18 3 Human 7.3 pEC50 = 7.3 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397878 90638 0 None -18 3 Human 7.3 pEC50 = 7.3 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
11949710 198210 0 None -50 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL594717 198210 0 None -50 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
118733772 120123 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416038 120123 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546893 120123 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
11737939 83798 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 2.1 O=C1c2c(ccc(Cl)c2Cl)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL220900 83798 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 2.1 O=C1c2c(ccc(Cl)c2Cl)[C@@H]2CNCCN12 10.1021/jm0612968
11291 3157 23 None 1 5 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1016/j.bmcl.2005.06.104
4980 3157 23 None 1 5 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1016/j.bmcl.2005.06.104
CHEMBL65547 3157 23 None 1 5 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1016/j.bmcl.2005.06.104
162670523 183158 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4790652 183158 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803766 183158 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
168283046 192280 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185474 192280 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222039 192280 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
162676809 183200 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4799299 183200 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4804137 183200 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
4240627 192322 1 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5198376 192322 1 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222297 192322 1 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
162676809 183200 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4799299 183200 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4804137 183200 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
4240627 192322 1 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5198376 192322 1 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222297 192322 1 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
44431689 86807 0 None -44 3 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 383 7 1 6 2.6 C[C@@H](N)Cc1c2c(c(COCC(=O)Oc3ccccc3)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
CHEMBL232995 86807 0 None -44 3 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 383 7 1 6 2.6 C[C@@H](N)Cc1c2c(c(COCC(=O)Oc3ccccc3)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
44572800 12529 3 None -5 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1 10.1021/jm801354e
CHEMBL1187194 12529 3 None -5 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1 10.1021/jm801354e
CHEMBL493128 12529 3 None -5 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1 10.1021/jm801354e
168283046 192280 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185474 192280 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222039 192280 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
44412403 77430 0 None 7 3 Human 7.2 pEC50 = 7.2 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 222 1 1 2 2.1 Clc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209254 77430 0 None 7 3 Human 7.2 pEC50 = 7.2 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 222 1 1 2 2.1 Clc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
135399866 71696 2 None -1 3 Rat 8.2 pEC50 = 8.2 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 209 2 2 4 1.2 C[C@H](N)Cn1ncc2ccc(O)c(F)c21 10.1021/jm050663x
CHEMBL197653 71696 2 None -1 3 Rat 8.2 pEC50 = 8.2 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 209 2 2 4 1.2 C[C@H](N)Cn1ncc2ccc(O)c(F)c21 10.1021/jm050663x
44431705 144581 0 None -1 3 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 313 2 2 4 1.7 C[C@@H](N)[C@H](O)c1c2c(c(Br)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
CHEMBL391196 144581 0 None -1 3 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 313 2 2 4 1.7 C[C@@H](N)[C@H](O)c1c2c(c(Br)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
18735313 203216 1 None 6 3 Human 8.2 pEC50 = 8.2 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 210 2 1 2 2.1 C[C@H](N)CN1CCc2ccc(Cl)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL76307 203216 1 None 6 3 Human 8.2 pEC50 = 8.2 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 210 2 1 2 2.1 C[C@H](N)CN1CCc2ccc(Cl)cc21 10.1016/j.bmcl.2003.05.001
162650400 183057 0 None -22 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@H]3C[C@@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4748110 183057 0 None -22 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@H]3C[C@@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4802669 183057 0 None -22 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@H]3C[C@@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
54581791 61120 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 273 2 1 3 2.4 Clc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770383 61120 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 273 2 1 3 2.4 Clc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
162650400 183057 0 None -22 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@H]3C[C@@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4748110 183057 0 None -22 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@H]3C[C@@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4802669 183057 0 None -22 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@H]3C[C@@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
53324165 56492 0 None -9 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 231 2 2 5 0.8 CCNc1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
CHEMBL1643674 56492 0 None -9 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 231 2 2 5 0.8 CCNc1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
122442263 137816 0 None -30 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769454 137816 0 None -30 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771393 137816 0 None -30 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442263 137816 0 None -30 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769454 137816 0 None -30 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771393 137816 0 None -30 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
118733800 120127 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.4 C=C(C)COc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416052 120127 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.4 C=C(C)COc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546904 120127 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.4 C=C(C)COc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
46230098 197639 0 None -30 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 231 0 2 3 0.9 Cc1cccc2c1C(=O)NC1CCNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590580 197639 0 None -30 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 231 0 2 3 0.9 Cc1cccc2c1C(=O)NC1CCNCCN21 10.1016/j.bmcl.2009.12.014
134265705 163528 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 189 0 1 3 0.8 c1cnc2c(c1)CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4209572 163528 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 189 0 1 3 0.8 c1cnc2c(c1)CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
54584721 61114 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770377 61114 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
118733812 120117 0 None -4 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
CHEMBL3416058 120117 0 None -4 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
CHEMBL3546873 120117 0 None -4 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
24849050 77882 2 None -2 3 Human 7.2 pEC50 = 7.2 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CC[C@H]3CNC[C@H]32)n1 10.1016/j.bmcl.2006.03.007
CHEMBL210802 77882 2 None -2 3 Human 7.2 pEC50 = 7.2 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CC[C@H]3CNC[C@H]32)n1 10.1016/j.bmcl.2006.03.007
10036629 64291 0 None -9 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)C(C)CNCC2 10.1021/jm0709034
CHEMBL181787 64291 0 None -9 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)C(C)CNCC2 10.1021/jm0709034
24773728 94406 0 None -31 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 209 1 1 1 3.0 CC[C@@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL253810 94406 0 None -31 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 209 1 1 1 3.0 CC[C@@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
118733806 120130 0 None -19 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3416055 120130 0 None -19 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3546907 120130 0 None -19 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
10064386 62972 4 None -32 3 Human 7.2 pEC50 = 7.2 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 317 1 1 2 2.5 COc1cc2c(cc1I)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL179378 62972 4 None -32 3 Human 7.2 pEC50 = 7.2 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 317 1 1 2 2.5 COc1cc2c(cc1I)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
44572802 12323 2 None -13 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL1186019 12323 2 None -13 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL445747 12323 2 None -13 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
11983273 77627 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 256 1 1 2 2.5 FC(F)(F)c1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209714 77627 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 256 1 1 2 2.5 FC(F)(F)c1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
118733796 120116 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416050 120116 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546872 120116 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
44572747 12581 2 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccccc1F 10.1021/jm801354e
CHEMBL1187580 12581 2 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccccc1F 10.1021/jm801354e
CHEMBL510308 12581 2 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccccc1F 10.1021/jm801354e
44573217 186746 0 None 10 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 302 3 2 3 2.2 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL493152 186746 0 None 10 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 302 3 2 3 2.2 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
44572174 12425 0 None -2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 2 1 1 2.7 Cc1cccc(Cl)c1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL1186687 12425 0 None -2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 2 1 1 2.7 Cc1cccc(Cl)c1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL474634 12425 0 None -2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 2 1 1 2.7 Cc1cccc(Cl)c1[C@H]1C[C@@H]1CN 10.1021/jm801354e
44316017 203731 0 None 4 3 Human 8.1 pEC50 = 8.1 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 228 2 1 2 2.2 C[C@H](N)CN1CCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL80366 203731 0 None 4 3 Human 8.1 pEC50 = 8.1 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 228 2 1 2 2.2 C[C@H](N)CN1CCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2003.05.001
11644842 88654 0 None -12 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337105 88654 0 None -12 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365394 88654 0 None -12 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
53321865 56539 0 None -19 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)nc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643855 56539 0 None -19 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)nc1 10.1016/j.bmcl.2010.11.089
122442273 137815 0 None -5 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771152 137815 0 None -5 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771392 137815 0 None -5 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
44316027 203801 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 236 4 1 3 2.5 CCSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
CHEMBL80862 203801 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 236 4 1 3 2.5 CCSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
162644827 183031 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4739937 183031 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802378 183031 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
162660358 183112 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4762722 183112 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803207 183112 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
122442273 137815 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771152 137815 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771392 137815 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
162644827 183031 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4739937 183031 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802378 183031 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
53317925 56543 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 390 3 2 7 1.2 O=C1Cc2cc(OC3CN(c4c5c(nc6ccnn46)CCNCC5)C3)ccc2N1 10.1016/j.bmcl.2010.11.089
CHEMBL1643859 56543 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 390 3 2 7 1.2 O=C1Cc2cc(OC3CN(c4c5c(nc6ccnn46)CCNCC5)C3)ccc2N1 10.1016/j.bmcl.2010.11.089
162660358 183112 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4762722 183112 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803207 183112 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
118733816 120134 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416060 120134 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546911 120134 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
10624 69942 17 None 6 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
138543650 69942 17 None 6 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL194378 69942 17 None 6 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
46228422 198343 0 None -33 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL595553 198343 0 None -33 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
44572806 12530 1 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 177 3 1 2 1.8 COc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL1187195 12530 1 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 177 3 1 2 1.8 COc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL493129 12530 1 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 177 3 1 2 1.8 COc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
44573218 192445 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 320 3 2 3 2.3 O=S(=O)(Nc1ccccc1F)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL522349 192445 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 320 3 2 3 2.3 O=S(=O)(Nc1ccccc1F)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
1534 102553 51 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 102553 51 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 102553 51 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
1534 102553 51 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 102553 51 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 102553 51 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
162659049 183101 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4761526 183101 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803123 183101 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
134265620 163843 0 None -6456 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
CHEMBL4213379 163843 0 None -6456 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
162659049 183101 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4761526 183101 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803123 183101 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
44572804 12499 1 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1 10.1021/jm801354e
CHEMBL1187088 12499 1 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1 10.1021/jm801354e
CHEMBL490064 12499 1 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1 10.1021/jm801354e
162669436 183153 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4789310 183153 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803705 183153 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
134265590 164195 0 None -2 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 189 0 1 3 0.8 c1cc2c(cn1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4217846 164195 0 None -2 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 189 0 1 3 0.8 c1cc2c(cn1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
9991444 62288 0 None -15 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178366 62288 0 None -15 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
24773900 122903 8 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 191 1 1 2 1.9 COc1ccc2c(c1)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL361742 122903 8 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 191 1 1 2 1.9 COc1ccc2c(c1)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
162669436 183153 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4789310 183153 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803705 183153 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
11658860 2302 47 None -63 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
2941 2302 47 None -63 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
4374 2302 47 None -63 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
CHEMBL360328 2302 47 None -63 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
DB04871 2302 47 None -63 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
10105208 62155 0 None -83 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
CHEMBL178124 62155 0 None -83 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
11160564 62959 4 None -40 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1021/jm0709034
CHEMBL179337 62959 4 None -40 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1021/jm0709034
23395431 94459 0 None -79 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 C[C@@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
CHEMBL254215 94459 0 None -79 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 C[C@@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
16115517 84400 0 None -5 3 Human 8.1 pEC50 = 8.1 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.4 CCc1ccc2c(c1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL223468 84400 0 None -5 3 Human 8.1 pEC50 = 8.1 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.4 CCc1ccc2c(c1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
44572178 12439 0 None -1 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 175 2 1 1 2.4 Cc1cccc([C@H]2C[C@@H]2CN)c1C 10.1021/jm801354e
CHEMBL1186736 12439 0 None -1 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 175 2 1 1 2.4 Cc1cccc([C@H]2C[C@@H]2CN)c1C 10.1021/jm801354e
CHEMBL475642 12439 0 None -1 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 175 2 1 1 2.4 Cc1cccc([C@H]2C[C@@H]2CN)c1C 10.1021/jm801354e
135520431 72249 9 None -1 3 Rat 8.1 pEC50 = 8.1 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 177 2 2 4 0.7 NCCn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL199385 72249 9 None -1 3 Rat 8.1 pEC50 = 8.1 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 177 2 2 4 0.7 NCCn1ncc2ccc(O)cc21 10.1021/jm050663x
135414348 72449 2 None -1 3 Rat 8.1 pEC50 = 8.1 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 205 2 2 4 1.4 Cc1c(O)ccc2cnn(C[C@H](C)N)c12 10.1021/jm050663x
CHEMBL200104 72449 2 None -1 3 Rat 8.1 pEC50 = 8.1 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 205 2 2 4 1.4 Cc1c(O)ccc2cnn(C[C@H](C)N)c12 10.1021/jm050663x
44573154 186605 0 None -17 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 350 4 2 3 2.5 O=S(=O)(NCc1ccccc1Cl)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492349 186605 0 None -17 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 350 4 2 3 2.5 O=S(=O)(NCc1ccccc1Cl)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
45484662 196804 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 289 2 1 4 1.6 O=c1cc2c(nn1Cc1cccc(Cl)c1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL577691 196804 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 289 2 1 4 1.6 O=c1cc2c(nn1Cc1cccc(Cl)c1)CCNCC2 10.1016/j.bmcl.2009.07.063
11231392 84456 0 None -7 3 Human 6.1 pEC50 = 6.1 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.6 CC(C)Oc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL223628 84456 0 None -7 3 Human 6.1 pEC50 = 6.1 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.6 CC(C)Oc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
71682217 90673 0 None -10 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 246 1 1 3 1.0 COc1c(C)ccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397913 90673 0 None -10 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 246 1 1 3 1.0 COc1c(C)ccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
44572170 12344 1 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1Cl 10.1021/jm801354e
CHEMBL1186164 12344 1 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1Cl 10.1021/jm801354e
CHEMBL452458 12344 1 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1Cl 10.1021/jm801354e
118733810 120132 0 None -9 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
CHEMBL3416057 120132 0 None -9 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
CHEMBL3546909 120132 0 None -9 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
162657367 183090 0 None -32 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4756903 183090 0 None -32 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803034 183090 0 None -32 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
45484700 195617 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 295 3 1 4 1.9 O=c1cc2c(nn1Cc1ccc(C3CC3)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL568692 195617 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 295 3 1 4 1.9 O=c1cc2c(nn1Cc1ccc(C3CC3)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
11160564 62959 4 None -40 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL179337 62959 4 None -40 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1016/j.bmcl.2004.12.080
53320653 56491 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 245 2 1 5 0.9 CCN(C)c1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
CHEMBL1643673 56491 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 245 2 1 5 0.9 CCN(C)c1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
135399666 168187 4 None -3 7 Rat 7.1 pEC50 = 7.1 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL437314 168187 4 None -3 7 Rat 7.1 pEC50 = 7.1 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
12370465 12550 16 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
CHEMBL1187354 12550 16 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
CHEMBL500093 12550 16 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
162657367 183090 0 None -32 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4756903 183090 0 None -32 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803034 183090 0 None -32 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
118733762 120119 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416033 120119 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546889 120119 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
11437171 83063 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 234 1 1 3 1.5 CSc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL220207 83063 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 234 1 1 3 1.5 CSc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
168286640 192316 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5194223 192316 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222252 192316 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
168294430 192395 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5205429 192395 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222746 192395 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
168294430 192395 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5205429 192395 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222746 192395 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
24826868 90637 1 None 1 3 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 236 0 1 2 1.3 O=C1c2cc(Cl)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397877 90637 1 None 1 3 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 236 0 1 2 1.3 O=C1c2cc(Cl)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
11695000 88628 0 None -7 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337490 88628 0 None -7 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365083 88628 0 None -7 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
122461343 137821 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769704 137821 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771398 137821 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
7153 97557 74 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O 10.1016/j.bmc.2007.10.100
CHEMBL272942 97557 74 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O 10.1016/j.bmc.2007.10.100
154699445 176842 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Antagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assayAntagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assay
ChEMBL 319 4 0 4 4.2 CCP(=O)(OC)c1ccc2oc(-c3ccc(F)cc3)nc2c1 10.1021/acs.jmedchem.0c00807
CHEMBL4638592 176842 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Antagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assayAntagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assay
ChEMBL 319 4 0 4 4.2 CCP(=O)(OC)c1ccc2oc(-c3ccc(F)cc3)nc2c1 10.1021/acs.jmedchem.0c00807
122461343 137821 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769704 137821 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771398 137821 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
11514226 88667 0 None -85 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337494 88667 0 None -85 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365470 88667 0 None -85 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
45484661 197193 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 289 2 1 4 1.6 O=c1cc2c(nn1Cc1ccccc1Cl)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL584210 197193 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 289 2 1 4 1.6 O=c1cc2c(nn1Cc1ccccc1Cl)CCNCC2 10.1016/j.bmcl.2009.07.063
53325935 56488 0 None -17 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 243 1 1 5 0.6 c1cc2nc3c(c(N4CCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
CHEMBL1643670 56488 0 None -17 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 243 1 1 5 0.6 c1cc2nc3c(c(N4CCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
53324630 56494 0 None -18 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1ccccc1OC1CN(c2c3c(nc4ccnn24)CCNCC3)C1 10.1016/j.bmcl.2010.11.089
CHEMBL1643676 56494 0 None -18 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1ccccc1OC1CN(c2c3c(nc4ccnn24)CCNCC3)C1 10.1016/j.bmcl.2010.11.089
11658860 2302 47 None -63 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
2941 2302 47 None -63 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
4374 2302 47 None -63 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
CHEMBL360328 2302 47 None -63 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
DB04871 2302 47 None -63 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
11658860 2302 47 None -63 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysisAgonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
2941 2302 47 None -63 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysisAgonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
4374 2302 47 None -63 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysisAgonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
CHEMBL360328 2302 47 None -63 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysisAgonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
DB04871 2302 47 None -63 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysisAgonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
122442275 137820 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770862 137820 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771397 137820 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
122442275 137820 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770862 137820 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771397 137820 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
168288743 192335 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5192627 192335 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222395 192335 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
4543677 192178 1 None -2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5179287 192178 1 None -2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221372 192178 1 None -2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
4543677 192178 1 None -2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5179287 192178 1 None -2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221372 192178 1 None -2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
168288743 192335 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5192627 192335 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222395 192335 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
118733774 120125 0 None -10 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416039 120125 0 None -10 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546902 120125 0 None -10 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
46228430 198046 0 None -8 3 Human 6.0 pEC50 = 6 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL593545 198046 0 None -8 3 Human 6.0 pEC50 = 6 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
44138039 178699 8 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 363 4 1 2 4.3 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473185 178699 8 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 363 4 1 2 4.3 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565847 179977 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 367 4 1 3 3.6 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL475407 179977 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 367 4 1 3 3.6 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565831 179845 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 345 4 1 2 4.2 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL475245 179845 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 345 4 1 2 4.2 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565608 178679 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 385 4 1 3 3.8 O=S(=O)(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472990 178679 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 385 4 1 3 3.8 O=S(=O)(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
188 3327 73 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2009.02.126
196968 3327 73 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2009.02.126
CHEMBL473186 3327 73 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2009.02.126
44565850 179143 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 349 3 1 2 4.2 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474408 179143 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 349 3 1 2 4.2 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
4366334 79984 8 None - 1 Human 8.7 pIC50 = 8.7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 379 3 0 4 4.6 CCCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL214554 79984 8 None - 1 Human 8.7 pIC50 = 8.7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 379 3 0 4 4.6 CCCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
44565638 189027 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 417 4 1 3 4.8 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL514934 189027 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 417 4 1 3 4.8 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
3743171 79709 13 None - 1 Human 7.0 pIC50 = 7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 445 1 0 4 5.1 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(Cl)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL213329 79709 13 None - 1 Human 7.0 pIC50 = 7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 445 1 0 4 5.1 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(Cl)cc3)=NN12 10.1016/j.bmcl.2006.06.068
145976085 163102 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4204576 163102 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
145972374 164111 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 388 6 3 7 1.3 COC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1N=C(c2ccccc2O)S[C@@H]1C 10.1021/acs.jnatprod.7b00317
CHEMBL4216860 164111 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 388 6 3 7 1.3 COC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1N=C(c2ccccc2O)S[C@@H]1C 10.1021/acs.jnatprod.7b00317
44565828 178609 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 395 3 0 3 5.3 Cn1c(C2CCN(C(=O)c3ccc(-c4ccccc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.02.126
CHEMBL472416 178609 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 395 3 0 3 5.3 Cn1c(C2CCN(C(=O)c3ccc(-c4ccccc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.02.126
127035063 135950 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 477 13 0 6 5.2 COc1ccccc1CCCN(CCc1ccc(OC)c(OC)c1)CCc1ccc2c(c1)OCO2 10.1039/C4MD00418C
CHEMBL3736149 135950 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 477 13 0 6 5.2 COc1ccccc1CCCN(CCc1ccc(OC)c(OC)c1)CCc1ccc2c(c1)OCO2 10.1039/C4MD00418C
127037093 135972 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 433 11 0 5 4.8 COc1ccc(CCN(CCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3736252 135972 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 433 11 0 5 4.8 COc1ccc(CCN(CCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
118464427 137793 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3771331 137793 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
752565 137748 7 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 273 2 3 6 1.7 COc1cccc(NC2=NC(N)=NC3(CCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770770 137748 7 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 273 2 3 6 1.7 COc1cccc(NC2=NC(N)=NC3(CCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
44565849 178705 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 431 5 1 3 4.9 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473235 178705 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 431 5 1 3 4.9 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565805 189032 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 387 3 1 2 5.6 O=C(c1ccc(C2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL514967 189032 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 387 3 1 2 5.6 O=C(c1ccc(C2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44416247 140914 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 393 3 0 4 4.9 CCCN1CCC2(CC1)Oc1ccc(C)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL384255 140914 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 393 3 0 4 4.9 CCCN1CCC2(CC1)Oc1ccc(C)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
44156863 7980 0 None -21 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091206 7980 0 None -21 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
44565827 178608 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2ccccc2)cn1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472415 178608 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2ccccc2)cn1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565636 178678 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 383 3 1 4 4.0 O=C(c1ccc(-c2ncccn2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472986 178678 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 383 3 1 4 4.0 O=C(c1ccc(-c2ncccn2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
16812804 170544 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 381 3 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL445809 170544 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 381 3 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565606 178651 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 411 4 1 3 5.3 COc1cc(-c2ccccc2)ccc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472789 178651 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 411 4 1 3 5.3 COc1cc(-c2ccccc2)ccc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565806 179518 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 388 3 1 3 4.6 O=C(c1ccc(N2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474839 179518 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 388 3 1 3 4.6 O=C(c1ccc(N2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
168295984 191612 0 None -8 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR methodAntagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR method
ChEMBL 431 6 0 5 5.0 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccccc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5204813 191612 0 None -8 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR methodAntagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR method
ChEMBL 431 6 0 5 5.0 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccccc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
127034715 135858 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 537 15 0 8 5.2 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735261 135858 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 537 15 0 8 5.2 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
127035064 135935 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 477 13 0 6 5.2 COc1cccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
CHEMBL3735911 135935 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 477 13 0 6 5.2 COc1cccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
127034730 135903 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 523 14 0 8 5.1 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735643 135903 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 523 14 0 8 5.1 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
46830134 8118 0 None -37 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1092241 8118 0 None -37 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
3781561 138056 6 None - 1 Human 5.9 pIC50 = 5.9 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 441 2 0 5 4.4 COc1cccc2c1OC1(CCN(C)CC1)N1N=C(c3ccc(Br)cc3)CC21 10.1016/j.bmcl.2006.06.068
CHEMBL377562 138056 6 None - 1 Human 5.9 pIC50 = 5.9 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 441 2 0 5 4.4 COc1cccc2c1OC1(CCN(C)CC1)N1N=C(c3ccc(Br)cc3)CC21 10.1016/j.bmcl.2006.06.068
10449757 3426 26 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10.1016/j.bmcl.2009.02.126
190 3426 26 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10.1016/j.bmcl.2009.02.126
CHEMBL2110371 3426 26 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10.1016/j.bmcl.2009.02.126
71528206 86529 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection methodAntagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection method
ChEMBL 314 3 0 4 2.8 COC(OC)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323581 86529 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection methodAntagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection method
ChEMBL 314 3 0 4 2.8 COC(OC)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
3830738 141102 7 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 395 2 0 4 5.1 CC(C)N1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(Cl)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL385346 141102 7 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 395 2 0 4 5.1 CC(C)N1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(Cl)cc3)=NN12 10.1016/j.bmcl.2006.06.068
44565831 179845 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 345 4 1 2 4.2 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL475245 179845 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 345 4 1 2 4.2 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
145988313 166671 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs by fluorescence assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs by fluorescence assay
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
CHEMBL4292326 166671 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs by fluorescence assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs by fluorescence assay
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
4203621 138446 14 None - 1 Human 5.8 pIC50 = 5.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 397 2 0 5 4.3 COc1cccc2c1OC1(CCN(C)CC1)N1N=C(c3ccc(Cl)cc3)CC21 10.1016/j.bmcl.2006.06.068
CHEMBL378541 138446 14 None - 1 Human 5.8 pIC50 = 5.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 397 2 0 5 4.3 COc1cccc2c1OC1(CCN(C)CC1)N1N=C(c3ccc(Cl)cc3)CC21 10.1016/j.bmcl.2006.06.068
3898525 139036 8 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 362 3 0 5 3.8 CCCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL379734 139036 8 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 362 3 0 5 3.8 CCCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
44565635 178677 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2ccccn2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472985 178677 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2ccccn2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565641 178728 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 353 3 1 2 4.5 O=C(c1ccc(-c2ccccc2)cc1)N1CC(c2nc3ccccc3[nH]2)C1 10.1016/j.bmcl.2009.02.126
CHEMBL473391 178728 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 353 3 1 2 4.5 O=C(c1ccc(-c2ccccc2)cc1)N1CC(c2nc3ccccc3[nH]2)C1 10.1016/j.bmcl.2009.02.126
44565829 178629 2 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 0 3 5.5 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3o2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472589 178629 2 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 0 3 5.5 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3o2)CC1 10.1016/j.bmcl.2009.02.126
53327611 69396 0 None -154 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5HT2B receptorAntagonist activity at 5HT2B receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69396 0 None -154 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5HT2B receptorAntagonist activity at 5HT2B receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
44416290 140840 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 424 4 0 5 4.7 c1ccc(CCN2CCC3(CC2)Oc2ccccc2C2CC(c4ccncc4)=NN23)cc1 10.1016/j.bmcl.2006.06.068
CHEMBL383860 140840 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 424 4 0 5 4.7 c1ccc(CCN2CCC3(CC2)Oc2ccccc2C2CC(c4ccncc4)=NN23)cc1 10.1016/j.bmcl.2006.06.068
44565824 178703 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 465 4 1 3 6.1 O=C(c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473214 178703 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 465 4 1 3 6.1 O=C(c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44155109 8075 3 None -21 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091919 8075 3 None -21 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
732268 137755 28 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 257 1 3 5 2.0 NC1=NC2(CCCCC2)NC(Nc2ccccc2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL3770837 137755 28 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 257 1 3 5 2.0 NC1=NC2(CCCCC2)NC(Nc2ccccc2)=N1 10.1021/acsmedchemlett.8b00300
44565635 178677 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2ccccn2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472985 178677 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2ccccn2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
3716424 80623 6 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 477 3 0 5 5.0 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(OC(F)F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL215380 80623 6 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 477 3 0 5 5.0 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(OC(F)F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
3826158 79502 11 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 469 4 0 5 5.2 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(OC)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL212506 79502 11 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 469 4 0 5 5.2 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(OC)cc3)=NN12 10.1016/j.bmcl.2006.06.068
118464428 137720 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 343 4 3 7 2.6 CCCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770512 137720 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 343 4 3 7 2.6 CCCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
145988313 166671 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs in presence of human serum albumin by fluorescence assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs in presence of human serum albumin by fluorescence assay
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
CHEMBL4292326 166671 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs in presence of human serum albumin by fluorescence assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs in presence of human serum albumin by fluorescence assay
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
136020618 163351 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4207302 163351 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
3736302 138376 7 None - 1 Human 6.7 pIC50 = 6.7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 439 2 0 4 5.2 CC(C)N1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL378357 138376 7 None - 1 Human 6.7 pIC50 = 6.7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 439 2 0 4 5.2 CC(C)N1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3)=NN12 10.1016/j.bmcl.2006.06.068
188 3327 73 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2009.02.126
196968 3327 73 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2009.02.126
CHEMBL473186 3327 73 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2009.02.126
145979048 166094 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 407 3 3 7 3.0 CCOC(=O)c1cc(Br)cc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acsmedchemlett.8b00300
CHEMBL4281546 166094 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 407 3 3 7 3.0 CCOC(=O)c1cc(Br)cc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acsmedchemlett.8b00300
44565846 179976 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 395 4 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL475406 179976 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 395 4 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
16812804 170544 9 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 381 3 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL445809 170544 9 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 381 3 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565830 179132 2 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 331 3 1 2 4.1 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474404 179132 2 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 331 3 1 2 4.1 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565605 189091 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 383 3 1 4 4.0 O=C(c1cnc(-c2ccccc2)nc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL515422 189091 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 383 3 1 4 4.0 O=C(c1cnc(-c2ccccc2)nc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44416309 140897 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 376 3 0 5 4.1 CC(C)CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL384160 140897 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 376 3 0 5 4.1 CC(C)CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
145993660 166804 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 413 1 3 5 3.6 NC1=NC2(CCCCC2)NC(Nc2cc(Br)cc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4294723 166804 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 413 1 3 5 3.6 NC1=NC2(CCCCC2)NC(Nc2cc(Br)cc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
44565637 178700 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 398 3 2 3 3.9 O=C(c1ccc(-c2ccccc2)[nH]c1=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473187 178700 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 398 3 2 3 3.9 O=C(c1ccc(-c2ccccc2)[nH]c1=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
71528204 86527 0 None -15 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection methodAntagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection method
ChEMBL 439 6 1 5 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323579 86527 0 None -15 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection methodAntagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection method
ChEMBL 439 6 1 5 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
118464429 166553 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 383 1 3 5 2.6 NC1=NC2(CCCCC2)NC(Nc2cccc(I)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4290245 166553 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 383 1 3 5 2.6 NC1=NC2(CCCCC2)NC(Nc2cccc(I)c2)=N1 10.1021/acsmedchemlett.8b00300
26694436 162350 2 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B (unknown origin)Antagonist activity at 5-HT2B (unknown origin)
ChEMBL 354 5 2 3 2.9 CC(C)NS(=O)(=O)c1cccc(C(=O)Nc2ccc(F)c(F)c2)c1 10.1021/acs.jmedchem.8b00654
CHEMBL4173963 162350 2 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B (unknown origin)Antagonist activity at 5-HT2B (unknown origin)
ChEMBL 354 5 2 3 2.9 CC(C)NS(=O)(=O)c1cccc(C(=O)Nc2ccc(F)c(F)c2)c1 10.1021/acs.jmedchem.8b00654
44565807 179520 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 390 3 1 4 3.4 O=C(c1ccc(N2CCOCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474840 179520 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 390 3 1 4 3.4 O=C(c1ccc(N2CCOCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44416259 137662 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 397 3 0 4 4.7 CCCN1CCC2(CC1)Oc1ccc(F)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL376978 137662 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 397 3 0 4 4.7 CCCN1CCC2(CC1)Oc1ccc(F)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
3649661 137678 6 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770106 137678 6 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
11502243 188906 39 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 401 4 1 6 4.4 N#Cc1cc(CN2CCC(Nc3ncnc4sc(Cl)cc34)CC2)ccc1F 10.1016/j.bmcl.2009.02.126
CHEMBL513994 188906 39 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 401 4 1 6 4.4 N#Cc1cc(CN2CCC(Nc3ncnc4sc(Cl)cc34)CC2)ccc1F 10.1016/j.bmcl.2009.02.126
11949710 198210 0 None -50 3 Human 7.6 pIC50 = 7.6 Functional
Agonist activity against human 5HT2B receptor by FLIPR assay relative to 5HTAgonist activity against human 5HT2B receptor by FLIPR assay relative to 5HT
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL594717 198210 0 None -50 3 Human 7.6 pIC50 = 7.6 Functional
Agonist activity against human 5HT2B receptor by FLIPR assay relative to 5HTAgonist activity against human 5HT2B receptor by FLIPR assay relative to 5HT
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
5093797 80646 6 None - 1 Human 6.6 pIC50 = 6.6 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 367 1 0 4 4.3 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(Cl)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL215461 80646 6 None - 1 Human 6.6 pIC50 = 6.6 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 367 1 0 4 4.3 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(Cl)cc3)=NN12 10.1016/j.bmcl.2006.06.068
895660 32162 8 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 287 2 3 6 2.0 COc1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL1411080 32162 8 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 287 2 3 6 2.0 COc1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
118464425 137768 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770981 137768 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
5113614 79636 7 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 457 3 0 4 5.3 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL213005 79636 7 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 457 3 0 4 5.3 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
44565808 180319 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 411 4 1 3 5.3 COc1ccc(-c2ccc(C(=O)N3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
CHEMBL475778 180319 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 411 4 1 3 5.3 COc1ccc(-c2ccc(C(=O)N3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
11502243 188906 39 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 401 4 1 6 4.4 N#Cc1cc(CN2CCC(Nc3ncnc4sc(Cl)cc34)CC2)ccc1F 10.1016/j.bmcl.2009.02.126
CHEMBL513994 188906 39 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 401 4 1 6 4.4 N#Cc1cc(CN2CCC(Nc3ncnc4sc(Cl)cc34)CC2)ccc1F 10.1016/j.bmcl.2009.02.126
11957541 1425 38 None 1 5 Human 8.5 pIC50 = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
1229 1425 38 None 1 5 Human 8.5 pIC50 = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
147 1425 38 None 1 5 Human 8.5 pIC50 = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
170617 1425 38 None 1 5 Human 8.5 pIC50 = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
CHEMBL6616 1425 38 None 1 5 Human 8.5 pIC50 = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
3723094 79539 10 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 429 1 0 4 4.6 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL212656 79539 10 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 429 1 0 4 4.6 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
44565608 178679 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 385 4 1 3 3.8 O=S(=O)(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472990 178679 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 385 4 1 3 3.8 O=S(=O)(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565846 179976 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 395 4 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL475406 179976 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 395 4 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
168284710 190987 0 None -18 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR methodAntagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR method
ChEMBL 509 6 0 5 5.8 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccc(Br)cc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5195241 190987 0 None -18 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR methodAntagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR method
ChEMBL 509 6 0 5 5.8 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccc(Br)cc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
136020617 57010 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL1651095 57010 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/acs.jnatprod.7b00317
44565805 189032 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 387 3 1 2 5.6 O=C(c1ccc(C2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL514967 189032 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 387 3 1 2 5.6 O=C(c1ccc(C2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44416260 79566 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 413 3 0 4 5.2 CCCN1CCC2(CC1)Oc1ccc(Cl)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL212755 79566 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 413 3 0 4 5.2 CCCN1CCC2(CC1)Oc1ccc(Cl)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
44565847 179977 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 367 4 1 3 3.6 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL475407 179977 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 367 4 1 3 3.6 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565808 180319 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 411 4 1 3 5.3 COc1ccc(-c2ccc(C(=O)N3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
CHEMBL475778 180319 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 411 4 1 3 5.3 COc1ccc(-c2ccc(C(=O)N3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
11248240 2616 2 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 462 5 4 8 1.8 CNC(=O)[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.6b01183
5601 2616 2 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 462 5 4 8 1.8 CNC(=O)[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.6b01183
CHEMBL175543 2616 2 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 462 5 4 8 1.8 CNC(=O)[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.6b01183
752521 197050 7 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
CHEMBL582877 197050 7 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
118464420 137704 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
CHEMBL3770342 137704 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
44565634 178652 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2cccnc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472791 178652 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2cccnc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565850 179143 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 349 3 1 2 4.2 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474408 179143 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 349 3 1 2 4.2 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
118464420 137704 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL3770342 137704 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
118464426 137705 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 327 4 3 6 3.0 CCCC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770351 137705 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 327 4 3 6 3.0 CCCC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
3751272 80169 13 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 443 3 0 4 5.9 Clc1ccc(C2=NN3C(C2)c2ccccc2OC32CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2006.06.068
CHEMBL215024 80169 13 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 443 3 0 4 5.9 Clc1ccc(C2=NN3C(C2)c2ccccc2OC32CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2006.06.068
71528205 86528 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection methodAntagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection method
ChEMBL 368 5 1 4 2.2 CN(C)CCCNC(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323580 86528 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection methodAntagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection method
ChEMBL 368 5 1 4 2.2 CN(C)CCCNC(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
145963830 163560 0 None 3 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
CHEMBL4209942 163560 0 None 3 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
127035065 135964 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 477 13 0 6 5.2 COc1ccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1 10.1039/C4MD00418C
CHEMBL3736207 135964 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 477 13 0 6 5.2 COc1ccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1 10.1039/C4MD00418C
44565606 178651 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 411 4 1 3 5.3 COc1cc(-c2ccccc2)ccc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472789 178651 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 411 4 1 3 5.3 COc1cc(-c2ccccc2)ccc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
73389570 161441 33 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at 5-HT2B (unknown origin)Antagonist activity at 5-HT2B (unknown origin)
ChEMBL 378 5 2 4 2.5 Cc1cc(NC(=O)c2cccc(S(=O)(=O)N[C@H]3CCOC3)c2)ccc1F 10.1021/acs.jmedchem.8b00654
CHEMBL4159471 161441 33 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at 5-HT2B (unknown origin)Antagonist activity at 5-HT2B (unknown origin)
ChEMBL 378 5 2 4 2.5 Cc1cc(NC(=O)c2cccc(S(=O)(=O)N[C@H]3CCOC3)c2)ccc1F 10.1021/acs.jmedchem.8b00654
2884131 166344 7 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 275 1 3 5 2.2 NC1=NC2(CCCCC2)NC(Nc2cccc(F)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4286420 166344 7 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 275 1 3 5 2.2 NC1=NC2(CCCCC2)NC(Nc2cccc(F)c2)=N1 10.1021/acsmedchemlett.8b00300
44155107 7981 3 None -60 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091207 7981 3 None -60 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
4297073 80875 7 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 348 2 0 5 3.4 CCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL215883 80875 7 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 348 2 0 5 3.4 CCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
46933845 15971 0 None -18 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT2B receptor assessed as inhibition of 10633-induced calcium mobilization by FLIPR assayAntagonist activity at human 5HT2B receptor assessed as inhibition of 10633-induced calcium mobilization by FLIPR assay
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224034 15971 0 None -18 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT2B receptor assessed as inhibition of 10633-induced calcium mobilization by FLIPR assayAntagonist activity at human 5HT2B receptor assessed as inhibition of 10633-induced calcium mobilization by FLIPR assay
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
135753059 190114 5 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 351 4 2 5 2.7 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2ccc(C)c(C)c2)n1 10.1021/acs.jmedchem.1c01759
CHEMBL5182403 190114 5 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 351 4 2 5 2.7 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2ccc(C)c(C)c2)n1 10.1021/acs.jmedchem.1c01759
135753074 190504 7 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 341 4 2 5 2.2 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2ccccc2F)n1 10.1021/acs.jmedchem.1c01759
CHEMBL5187824 190504 7 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 341 4 2 5 2.2 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2ccccc2F)n1 10.1021/acs.jmedchem.1c01759
135753056 190571 1 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 337 4 2 5 2.4 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2cccc(C)c2)n1 10.1021/acs.jmedchem.1c01759
CHEMBL5188949 190571 1 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 337 4 2 5 2.4 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2cccc(C)c2)n1 10.1021/acs.jmedchem.1c01759
156208582 191425 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 351 5 2 5 2.6 CCc1cccc(C(=O)Nc2cc(C)nn2-c2nc(CC)cc(=O)[nH]2)c1 10.1021/acs.jmedchem.1c01759
CHEMBL5202029 191425 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 351 5 2 5 2.6 CCc1cccc(C(=O)Nc2cc(C)nn2-c2nc(CC)cc(=O)[nH]2)c1 10.1021/acs.jmedchem.1c01759
3765560 141001 9 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 411 1 0 4 4.4 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(Br)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL384745 141001 9 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 411 1 0 4 4.4 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(Br)cc3)=NN12 10.1016/j.bmcl.2006.06.068
4518239 80630 6 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 477 3 0 5 5.0 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3OC(F)F)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL215404 80630 6 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 477 3 0 5 5.0 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3OC(F)F)=NN12 10.1016/j.bmcl.2006.06.068
879244 27973 7 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 271 1 3 5 2.3 Cc1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acsmedchemlett.8b00300
CHEMBL1373650 27973 7 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 271 1 3 5 2.3 Cc1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acsmedchemlett.8b00300
4322819 79998 18 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 381 2 0 5 3.8 COc1cccc2c1OC1(CCN(C)CC1)N1N=C(c3ccc(F)cc3)CC21 10.1016/j.bmcl.2006.06.068
CHEMBL214594 79998 18 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 381 2 0 5 3.8 COc1cccc2c1OC1(CCN(C)CC1)N1N=C(c3ccc(F)cc3)CC21 10.1016/j.bmcl.2006.06.068
118464421 166728 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 291 1 3 5 2.7 NC1=NC2(CCCCC2)NC(Nc2cccc(Cl)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4293638 166728 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 291 1 3 5 2.7 NC1=NC2(CCCCC2)NC(Nc2cccc(Cl)c2)=N1 10.1021/acsmedchemlett.8b00300
44247568 81748 51 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human 5HT2B receptorAntagonist activity at human 5HT2B receptor
ChEMBL 337 5 0 5 3.0 Cc1cc(OCCN2CCOCC2)nn1-c1ccc2ccccc2c1 10.1021/jm3007323
CHEMBL2170062 81748 51 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human 5HT2B receptorAntagonist activity at human 5HT2B receptor
ChEMBL 337 5 0 5 3.0 Cc1cc(OCCN2CCOCC2)nn1-c1ccc2ccccc2c1 10.1021/jm3007323
44565806 179518 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 388 3 1 3 4.6 O=C(c1ccc(N2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474839 179518 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 388 3 1 3 4.6 O=C(c1ccc(N2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
2267399 137800 8 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 271 1 3 5 2.3 Cc1ccc(NC2=NC(N)=NC3(CCCCC3)N2)cc1 10.1021/acs.jmedchem.5b01631
CHEMBL3771373 137800 8 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 271 1 3 5 2.3 Cc1ccc(NC2=NC(N)=NC3(CCCCC3)N2)cc1 10.1021/acs.jmedchem.5b01631
136928971 137688 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 343 3 3 7 2.5 CCOC(=O)c1cccc(NC2=NC(NC)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770185 137688 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 343 3 3 7 2.5 CCOC(=O)c1cccc(NC2=NC(NC)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
5128094 79432 18 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 333 1 0 4 3.7 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccccc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL212228 79432 18 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 333 1 0 4 3.7 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccccc3)=NN12 10.1016/j.bmcl.2006.06.068
5167627 79637 7 None - 1 Human 6.3 pIC50 = 6.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 395 3 0 4 5.1 CCCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccccc3Cl)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL213006 79637 7 None - 1 Human 6.3 pIC50 = 6.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 395 3 0 4 5.1 CCCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccccc3Cl)=NN12 10.1016/j.bmcl.2006.06.068
44416351 79710 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 279 1 0 4 3.4 CC1(C)Oc2ccccc2C2CC(c3ccncc3)=NN21 10.1016/j.bmcl.2006.06.068
CHEMBL213332 79710 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 279 1 0 4 3.4 CC1(C)Oc2ccccc2C2CC(c3ccncc3)=NN21 10.1016/j.bmcl.2006.06.068
3802375 79892 7 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 453 3 0 4 5.5 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(C)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL214184 79892 7 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 453 3 0 4 5.5 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(C)cc3)=NN12 10.1016/j.bmcl.2006.06.068
4657811 80092 8 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 461 1 0 4 5.6 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc4ccccc4c3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL214802 80092 8 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 461 1 0 4 5.6 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc4ccccc4c3)=NN12 10.1016/j.bmcl.2006.06.068
5165122 80624 20 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 441 2 0 5 4.4 COc1ccc(C2=NN3C(C2)c2cc(Br)ccc2OC32CCN(C)CC2)cc1 10.1016/j.bmcl.2006.06.068
CHEMBL215386 80624 20 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 441 2 0 5 4.4 COc1ccc(C2=NN3C(C2)c2cc(Br)ccc2OC32CCN(C)CC2)cc1 10.1016/j.bmcl.2006.06.068
3757038 81047 11 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 401 1 0 5 4.0 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccco3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL215991 81047 11 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 401 1 0 5 4.0 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccco3)=NN12 10.1016/j.bmcl.2006.06.068
3773677 138443 6 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 441 2 0 5 4.4 COc1ccccc1C1=NN2C(C1)c1cc(Br)ccc1OC21CCN(C)CC1 10.1016/j.bmcl.2006.06.068
CHEMBL378540 138443 6 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 441 2 0 5 4.4 COc1ccccc1C1=NN2C(C1)c1cc(Br)ccc1OC21CCN(C)CC1 10.1016/j.bmcl.2006.06.068
3410378 140918 7 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 417 1 0 5 4.5 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3cccs3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL384270 140918 7 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 417 1 0 5 4.5 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3cccs3)=NN12 10.1016/j.bmcl.2006.06.068
4679720 165413 6 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 471 3 0 6 4.4 COc1ccc(C2=NN3C(C2)c2cc(Br)ccc2OC32CCN(C)CC2)cc1OC 10.1016/j.bmcl.2006.06.068
CHEMBL425260 165413 6 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 471 3 0 6 4.4 COc1ccc(C2=NN3C(C2)c2cc(Br)ccc2OC32CCN(C)CC2)cc1OC 10.1016/j.bmcl.2006.06.068
4148445 137760 9 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 291 1 3 5 2.7 NC1=NC2(CCCCC2)NC(Nc2ccc(Cl)cc2)=N1 10.1021/acs.jmedchem.5b01631
CHEMBL3770873 137760 9 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 291 1 3 5 2.7 NC1=NC2(CCCCC2)NC(Nc2ccc(Cl)cc2)=N1 10.1021/acs.jmedchem.5b01631
3391669 141297 7 None - 1 Human 6.3 pIC50 = 6.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 479 1 0 4 5.7 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(Cl)c(Cl)c3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL386459 141297 7 None - 1 Human 6.3 pIC50 = 6.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 479 1 0 4 5.7 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(Cl)c(Cl)c3)=NN12 10.1016/j.bmcl.2006.06.068
44565607 188964 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 427 5 1 5 4.4 CCOc1nc(-c2ccccc2)ncc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL514453 188964 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 427 5 1 5 4.4 CCOc1nc(-c2ccccc2)ncc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565848 178704 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 381 5 1 3 3.7 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473234 178704 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 381 5 1 3 3.7 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565826 178607 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 387 3 1 2 5.2 O=C(C1CCC(c2ccccc2)CC1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472414 178607 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 387 3 1 2 5.2 O=C(C1CCC(c2ccccc2)CC1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44476436 81921 5 None -7413 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alphamethyl5HT-induced intracellular calcium mobilization by Fluo4-based staining methodAntagonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alphamethyl5HT-induced intracellular calcium mobilization by Fluo4-based staining method
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172186 81921 5 None -7413 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alphamethyl5HT-induced intracellular calcium mobilization by Fluo4-based staining methodAntagonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alphamethyl5HT-induced intracellular calcium mobilization by Fluo4-based staining method
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
162674022 182629 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) assessed as inhibition of 5HT-indued response by calcium mobilization assayAntagonist activity at 5-HT2B receptor (unknown origin) assessed as inhibition of 5HT-indued response by calcium mobilization assay
ChEMBL 305 4 1 4 3.5 N#Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
CHEMBL4796102 182629 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) assessed as inhibition of 5HT-indued response by calcium mobilization assayAntagonist activity at 5-HT2B receptor (unknown origin) assessed as inhibition of 5HT-indued response by calcium mobilization assay
ChEMBL 305 4 1 4 3.5 N#Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
127037059 136001 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 445 11 0 5 5.6 COc1ccc(CCN(CC/C=C\c2ccccc2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3736516 136001 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 445 11 0 5 5.6 COc1ccc(CCN(CC/C=C\c2ccccc2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
10449757 3426 26 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10.1016/j.bmcl.2009.02.126
190 3426 26 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10.1016/j.bmcl.2009.02.126
CHEMBL2110371 3426 26 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10.1016/j.bmcl.2009.02.126
44565639 178727 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 367 4 1 2 5.6 c1ccc(-c2ccc(CN3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
CHEMBL473387 178727 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 367 4 1 2 5.6 c1ccc(-c2ccc(CN3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
44565640 188905 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.2 O=C(c1ccc(-c2ccccc2)cc1)N1CCN(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL513993 188905 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.2 O=C(c1ccc(-c2ccccc2)cc1)N1CCN(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44138039 178699 8 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 363 4 1 2 4.3 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473185 178699 8 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 363 4 1 2 4.3 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565605 189091 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 383 3 1 4 4.0 O=C(c1cnc(-c2ccccc2)nc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL515422 189091 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 383 3 1 4 4.0 O=C(c1cnc(-c2ccccc2)nc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565639 178727 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 367 4 1 2 5.6 c1ccc(-c2ccc(CN3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
CHEMBL473387 178727 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 367 4 1 2 5.6 c1ccc(-c2ccc(CN3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
145989393 166659 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 353 1 3 5 2.9 NC1=NC2(CCCCC2)NC(Nc2cc(F)cc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4292168 166659 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 353 1 3 5 2.9 NC1=NC2(CCCCC2)NC(Nc2cc(F)cc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
3473601 139586 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 367 1 0 4 4.3 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccccc3Cl)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL380167 139586 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 367 1 0 4 4.3 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccccc3Cl)=NN12 10.1016/j.bmcl.2006.06.068
44565830 179132 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 331 3 1 2 4.1 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474404 179132 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 331 3 1 2 4.1 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
57495353 124507 33 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of 5-HT2B (unknown origin) by calcium flux assayInhibition of 5-HT2B (unknown origin) by calcium flux assay
ChEMBL 450 5 1 7 2.9 CCC(=O)N1CC[C@H](Nc2ncnc3c2CN(c2cnc(OC)c(C(F)(F)F)c2)CC3)C1 10.1021/acsmedchemlett.7b00293
CHEMBL3643413 124507 33 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of 5-HT2B (unknown origin) by calcium flux assayInhibition of 5-HT2B (unknown origin) by calcium flux assay
ChEMBL 450 5 1 7 2.9 CCC(=O)N1CC[C@H](Nc2ncnc3c2CN(c2cnc(OC)c(C(F)(F)F)c2)CC3)C1 10.1021/acsmedchemlett.7b00293
3400827 79488 10 None - 1 Human 6.1 pIC50 = 6.1 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 517 3 0 4 6.0 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(Br)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL212457 79488 10 None - 1 Human 6.1 pIC50 = 6.1 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 517 3 0 4 6.0 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(Br)cc3)=NN12 10.1016/j.bmcl.2006.06.068
127035062 135915 0 None 6 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 135915 0 None 6 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
127035066 135885 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 507 14 0 7 5.2 COc1ccc(OC)c(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
CHEMBL3735434 135885 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 507 14 0 7 5.2 COc1ccc(OC)c(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
44565828 178609 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 395 3 0 3 5.3 Cn1c(C2CCN(C(=O)c3ccc(-c4ccccc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.02.126
CHEMBL472416 178609 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 395 3 0 3 5.3 Cn1c(C2CCN(C(=O)c3ccc(-c4ccccc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.02.126
145964159 163766 0 None 8 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 273 3 2 4 2.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4212435 163766 0 None 8 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 273 3 2 4 2.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
44565638 189027 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 417 4 1 3 4.8 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL514934 189027 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 417 4 1 3 4.8 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
3499360 140976 7 None - 1 Human 6.1 pIC50 = 6.1 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 445 1 0 4 5.1 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3Cl)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL384579 140976 7 None - 1 Human 6.1 pIC50 = 6.1 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 445 1 0 4 5.1 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3Cl)=NN12 10.1016/j.bmcl.2006.06.068
104697662 144860 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 293 3 2 4 3.3 Clc1cccc(CNc2nc(Cl)nc3[nH]cnc23)c1 10.1021/acs.jmedchem.6b01183
CHEMBL3914002 144860 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 293 3 2 4 3.3 Clc1cccc(CNc2nc(Cl)nc3[nH]cnc23)c1 10.1021/acs.jmedchem.6b01183
11536299 182694 6 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilizationAntagonist activity at 5-HT2B receptor (unknown origin) expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization
ChEMBL 266 3 1 3 3.3 O=c1cc(CCc2ccccc2)oc2cccc(O)c12 10.1016/j.bmcl.2014.02.029
CHEMBL479683 182694 6 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilizationAntagonist activity at 5-HT2B receptor (unknown origin) expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization
ChEMBL 266 3 1 3 3.3 O=c1cc(CCc2ccccc2)oc2cccc(O)c12 10.1016/j.bmcl.2014.02.029
109052212 161985 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5-HT2B (unknown origin)Antagonist activity at 5-HT2B (unknown origin)
ChEMBL 340 4 2 2 4.1 O=C(Nc1ccc(F)cc1)c1cccc(C(=O)NC2CCCCC2)c1 10.1021/acs.jmedchem.8b00654
CHEMBL4168125 161985 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5-HT2B (unknown origin)Antagonist activity at 5-HT2B (unknown origin)
ChEMBL 340 4 2 2 4.1 O=C(Nc1ccc(F)cc1)c1cccc(C(=O)NC2CCCCC2)c1 10.1021/acs.jmedchem.8b00654
44565607 188964 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 427 5 1 5 4.4 CCOc1nc(-c2ccccc2)ncc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL514453 188964 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 427 5 1 5 4.4 CCOc1nc(-c2ccccc2)ncc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
3442850 168983 20 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 411 1 0 4 4.4 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL443570 168983 20 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 411 1 0 4 4.4 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3)=NN12 10.1016/j.bmcl.2006.06.068
4895014 79575 7 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 334 1 0 5 3.0 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL212780 79575 7 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 334 1 0 5 3.0 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
44565824 178703 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 465 4 1 3 6.1 O=C(c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473214 178703 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 465 4 1 3 6.1 O=C(c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565848 178704 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 381 5 1 3 3.7 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473234 178704 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 381 5 1 3 3.7 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
12611598 60101 3 None - 0 Rat 7.0 pKd = 7 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 181 3 2 3 1.3 COc1ccc(O)c(CC(C)N)c1 10.1021/jm00183a006
CHEMBL175205 60101 3 None - 0 Rat 7.0 pKd = 7 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 181 3 2 3 1.3 COc1ccc(O)c(CC(C)N)c1 10.1021/jm00183a006
221 3422 63 None - 3 Rat 8.0 pKd = 8.0 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C 10.1021/jm00006a001
3277600 3422 63 None - 3 Rat 8.0 pKd = 8.0 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C 10.1021/jm00006a001
CHEMBL323356 3422 63 None - 3 Rat 8.0 pKd = 8.0 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C 10.1021/jm00006a001
44385952 61864 5 None - 0 Rat 7.9 pKd = 7.9 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 195 3 2 3 1.6 COc1cc(C)c(O)cc1CC(C)N 10.1021/jm00183a006
CHEMBL177800 61864 5 None - 0 Rat 7.9 pKd = 7.9 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 195 3 2 3 1.6 COc1cc(C)c(O)cc1CC(C)N 10.1021/jm00183a006
135398737 942 89 None - 37 Rat 6.9 pKd = 6.9 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
38 942 89 None - 37 Rat 6.9 pKd = 6.9 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
722 942 89 None - 37 Rat 6.9 pKd = 6.9 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
CHEMBL42 942 89 None - 37 Rat 6.9 pKd = 6.9 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
DB00363 942 89 None - 37 Rat 6.9 pKd = 6.9 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
10022745 119451 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 381 5 1 4 3.5 CCc1c(C)[nH]c2c1C(=O)CC(CN1CCN(c3ccccc3OC)CC1)C2 10.1021/jm011014y
CHEMBL349832 119451 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 381 5 1 4 3.5 CCc1c(C)[nH]c2c1C(=O)CC(CN1CCN(c3ccccc3OC)CC1)C2 10.1021/jm011014y
44327167 9273 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 371 4 0 4 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2sccc21 10.1021/jm011014y
CHEMBL111393 9273 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 371 4 0 4 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2sccc21 10.1021/jm011014y
CHEMBL544319 9273 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 371 4 0 4 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2sccc21 10.1021/jm011014y
12611606 60044 7 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 181 3 2 3 1.3 COc1ccc(CC(C)N)cc1O 10.1021/jm00183a006
CHEMBL174723 60044 7 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 181 3 2 3 1.3 COc1ccc(CC(C)N)cc1O 10.1021/jm00183a006
12611609 60100 3 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 167 3 2 3 0.9 COc1ccc(O)c(CCN)c1 10.1021/jm00183a006
CHEMBL175204 60100 3 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 167 3 2 3 0.9 COc1ccc(O)c(CCN)c1 10.1021/jm00183a006
12611617 60021 3 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 195 4 1 3 1.5 COc1ccc(O)c(CCN(C)C)c1 10.1021/jm00183a006
CHEMBL174563 60021 3 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 195 4 1 3 1.5 COc1ccc(O)c(CCN(C)C)c1 10.1021/jm00183a006
12611598 60101 3 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1ccc(O)c(CC(C)N)c1 10.1021/jm00183a006
CHEMBL175205 60101 3 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1ccc(O)c(CC(C)N)c1 10.1021/jm00183a006
10356829 59364 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 289 2 2 4 4.3 Cc1cc(NC(=O)Nc2ccc3sccc3c2)sn1 10.1021/jm00006a001
CHEMBL172269 59364 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 289 2 2 4 4.3 Cc1cc(NC(=O)Nc2ccc3sccc3c2)sn1 10.1021/jm00006a001
10693836 9232 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 428 8 0 5 4.3 O=C(CCCN1CCN(CCC2CCc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL111189 9232 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 428 8 0 5 4.3 O=C(CCCN1CCN(CCC2CCc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL545488 9232 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 428 8 0 5 4.3 O=C(CCCN1CCN(CCC2CCc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
10715378 15328 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 389 4 1 4 3.7 COc1ccccc1N1CCN(CC2CC(=O)c3c([nH]c4ccccc34)C2)CC1 10.1021/jm011014y
CHEMBL121744 15328 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 389 4 1 4 3.7 COc1ccccc1N1CCN(CC2CC(=O)c3c([nH]c4ccccc34)C2)CC1 10.1021/jm011014y
9979654 206172 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 422 8 0 4 4.2 O=C(CCCN1CCN(CCC2CCc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL96781 206172 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 422 8 0 4 4.2 O=C(CCCN1CCN(CCC2CCc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
12611613 60123 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 209 4 1 3 1.9 COc1ccc(O)c(CC(C)N(C)C)c1 10.1021/jm00183a006
CHEMBL175328 60123 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 209 4 1 3 1.9 COc1ccc(O)c(CC(C)N(C)C)c1 10.1021/jm00183a006
10473483 8548 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 356 4 0 5 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccsc3C2)CC1 10.1021/jm011014y
CHEMBL109528 8548 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 356 4 0 5 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccsc3C2)CC1 10.1021/jm011014y
CHEMBL544318 8548 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 356 4 0 5 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccsc3C2)CC1 10.1021/jm011014y
135398737 942 89 None - 37 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm011014y
38 942 89 None - 37 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm011014y
722 942 89 None - 37 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm011014y
CHEMBL42 942 89 None - 37 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm011014y
DB00363 942 89 None - 37 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm011014y
10710246 120601 0 None - 0 Rat 5.7 pKd = 5.7 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 312 3 0 6 1.6 O=C1CC(CN2CCN(c3ncccn3)CC2)Cc2occc21 10.1021/jm0009890
CHEMBL357517 120601 0 None - 0 Rat 5.7 pKd = 5.7 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 312 3 0 6 1.6 O=C1CC(CN2CCN(c3ncccn3)CC2)Cc2occc21 10.1021/jm0009890
10338282 34449 1 None - 0 Rat 6.7 pKd = 6.7 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B) receptor
ChEMBL 355 4 0 4 3.8 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2occc21 10.1021/jm0009890
CHEMBL143022 34449 1 None - 0 Rat 6.7 pKd = 6.7 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B) receptor
ChEMBL 355 4 0 4 3.8 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2occc21 10.1021/jm0009890
10338282 34449 1 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 355 4 0 4 3.8 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2occc21 10.1021/jm011014y
CHEMBL143022 34449 1 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 355 4 0 4 3.8 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2occc21 10.1021/jm011014y
11760018 53069 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 354 5 0 5 3.2 COc1ccccc1N1CCN(CCC2CCc3occc3C2=O)CC1 10.1021/jm011014y
CHEMBL160019 53069 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 354 5 0 5 3.2 COc1ccccc1N1CCN(CCC2CCc3occc3C2=O)CC1 10.1021/jm011014y
44326982 8556 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 351 4 0 3 4.1 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm011014y
CHEMBL109548 8556 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 351 4 0 3 4.1 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm011014y
CHEMBL545727 8556 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 351 4 0 3 4.1 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm011014y
10090486 52976 0 None - 0 Rat 6.6 pKd = 6.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 369 5 0 4 4.1 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3occc3C2=O)CC1 10.1021/jm011014y
CHEMBL159929 52976 0 None - 0 Rat 6.6 pKd = 6.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 369 5 0 4 4.1 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3occc3C2=O)CC1 10.1021/jm011014y
10090424 34459 1 None - 0 Rat 6.6 pKd = 6.6 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 368 3 0 5 4.2 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2occc21 10.1021/jm0009890
CHEMBL143027 34459 1 None - 0 Rat 6.6 pKd = 6.6 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 368 3 0 5 4.2 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2occc21 10.1021/jm0009890
10090424 34459 1 None - 0 Rat 6.6 pKd = 6.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 368 3 0 5 4.2 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2occc21 10.1021/jm011014y
CHEMBL143027 34459 1 None - 0 Rat 6.6 pKd = 6.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 368 3 0 5 4.2 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2occc21 10.1021/jm011014y
12611604 60111 3 None - 0 Rat 5.6 pKd = 5.6 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1ccc(CC(C)N)c(O)c1 10.1021/jm00183a006
CHEMBL175272 60111 3 None - 0 Rat 5.6 pKd = 5.6 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1ccc(CC(C)N)c(O)c1 10.1021/jm00183a006
10645469 110055 0 None - 0 Rat 5.6 pKd = 5.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 414 7 0 5 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccsc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL325253 110055 0 None - 0 Rat 5.6 pKd = 5.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 414 7 0 5 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccsc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL542428 110055 0 None - 0 Rat 5.6 pKd = 5.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 414 7 0 5 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccsc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
12611615 60001 1 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 285 7 0 3 3.4 COc1ccc(OCc2ccccc2)c(CCN(C)C)c1 10.1021/jm00183a006
CHEMBL174449 60001 1 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 285 7 0 3 3.4 COc1ccc(OCc2ccccc2)c(CCN(C)C)c1 10.1021/jm00183a006
12611617 60021 3 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 195 4 1 3 1.5 COc1ccc(O)c(CCN(C)C)c1 10.1021/jm00183a006
CHEMBL174563 60021 3 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 195 4 1 3 1.5 COc1ccc(O)c(CCN(C)C)c1 10.1021/jm00183a006
10024430 205869 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 408 8 0 4 3.9 O=C(CCCN1CCN(CCC2Cc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL95098 205869 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 408 8 0 4 3.9 O=C(CCCN1CCN(CCC2Cc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
12611613 60123 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 209 4 1 3 1.9 COc1ccc(O)c(CC(C)N(C)C)c1 10.1021/jm00183a006
CHEMBL175328 60123 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 209 4 1 3 1.9 COc1ccc(O)c(CC(C)N(C)C)c1 10.1021/jm00183a006
44327153 108710 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic activity on 5-hydroxytryptamine 2B receptor of Rat stomach fundus;ND is not determinedAntagonistic activity on 5-hydroxytryptamine 2B receptor of Rat stomach fundus;ND is not determined
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccsc3C2=O)CC1 10.1021/jm011014y
CHEMBL321682 108710 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic activity on 5-hydroxytryptamine 2B receptor of Rat stomach fundus;ND is not determinedAntagonistic activity on 5-hydroxytryptamine 2B receptor of Rat stomach fundus;ND is not determined
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccsc3C2=O)CC1 10.1021/jm011014y
CHEMBL558817 108710 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic activity on 5-hydroxytryptamine 2B receptor of Rat stomach fundus;ND is not determinedAntagonistic activity on 5-hydroxytryptamine 2B receptor of Rat stomach fundus;ND is not determined
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccsc3C2=O)CC1 10.1021/jm011014y
10804995 35338 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 311 3 0 5 2.2 O=C1CC(CN2CCN(c3ccccn3)CC2)Cc2occc21 10.1021/jm0009890
CHEMBL143937 35338 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 311 3 0 5 2.2 O=C1CC(CN2CCN(c3ccccn3)CC2)Cc2occc21 10.1021/jm0009890
10804995 35338 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 311 3 0 5 2.2 O=C1CC(CN2CCN(c3ccccn3)CC2)Cc2occc21 10.1021/jm011014y
CHEMBL143937 35338 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 311 3 0 5 2.2 O=C1CC(CN2CCN(c3ccccn3)CC2)Cc2occc21 10.1021/jm011014y
197139 24853 20 None - 0 Rat 5.5 pKd = 5.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1cc(CC(C)N)ccc1O 10.1021/jm00183a006
CHEMBL1347 24853 20 None - 0 Rat 5.5 pKd = 5.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1cc(CC(C)N)ccc1O 10.1021/jm00183a006
12611606 60044 7 None - 0 Rat 5.5 pKd = 5.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1ccc(CC(C)N)cc1O 10.1021/jm00183a006
CHEMBL174723 60044 7 None - 0 Rat 5.5 pKd = 5.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1ccc(CC(C)N)cc1O 10.1021/jm00183a006
12611596 59970 6 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 195 3 2 3 1.6 COc1cc(CC(C)N)c(O)cc1C 10.1021/jm00183a006
CHEMBL174380 59970 6 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 195 3 2 3 1.6 COc1cc(CC(C)N)c(O)cc1C 10.1021/jm00183a006
12611615 60001 1 None - 0 Rat 5.4 pKd = 5.4 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 285 7 0 3 3.4 COc1ccc(OCc2ccccc2)c(CCN(C)C)c1 10.1021/jm00183a006
CHEMBL174449 60001 1 None - 0 Rat 5.4 pKd = 5.4 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 285 7 0 3 3.4 COc1ccc(OCc2ccccc2)c(CCN(C)C)c1 10.1021/jm00183a006
9951008 204661 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 365 5 0 3 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3ccccc3C2=O)CC1 10.1021/jm011014y
CHEMBL87717 204661 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 365 5 0 3 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3ccccc3C2=O)CC1 10.1021/jm011014y
126769 204313 35 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1021/jm00006a001
CHEMBL536255 204313 35 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1021/jm00006a001
CHEMBL85194 204313 35 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1021/jm00006a001
9930475 204557 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 393 5 0 3 4.9 O=C(c1ccc(F)cc1)C1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1021/jm011014y
CHEMBL87026 204557 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 393 5 0 3 4.9 O=C(c1ccc(F)cc1)C1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1021/jm011014y
10597019 34029 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 398 7 0 5 3.4 O=C(CCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm0009890
CHEMBL142668 34029 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 398 7 0 5 3.4 O=C(CCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm0009890
10597019 34029 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 398 7 0 5 3.4 O=C(CCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL142668 34029 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 398 7 0 5 3.4 O=C(CCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
10249506 8702 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm011014y
CHEMBL109673 8702 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm011014y
CHEMBL544091 8702 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm011014y
11141324 52798 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 307 3 0 4 2.6 O=C1CC(CN2CCN(c3ccccn3)CC2)c2ccccc21 10.1021/jm011014y
CHEMBL159771 52798 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 307 3 0 4 2.6 O=C1CC(CN2CCN(c3ccccn3)CC2)c2ccccc21 10.1021/jm011014y
9866660 113910 2 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 417 3 1 4 5.1 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2[nH]c3ccccc3c21 10.1021/jm011014y
CHEMBL333174 113910 2 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 417 3 1 4 5.1 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2[nH]c3ccccc3c21 10.1021/jm011014y
10061837 120215 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 273 2 2 4 3.8 Cc1cc(NC(=O)Nc2ccc3sccc3c2)on1 10.1021/jm00006a001
CHEMBL354951 120215 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 273 2 2 4 3.8 Cc1cc(NC(=O)Nc2ccc3sccc3c2)on1 10.1021/jm00006a001
10022781 56744 0 None - 0 Rat 6.3 pKd = 6.3 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 382 4 0 5 4.6 O=C1c2ccoc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm011014y
CHEMBL164471 56744 0 None - 0 Rat 6.3 pKd = 6.3 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 382 4 0 5 4.6 O=C1c2ccoc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm011014y
44326751 108115 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 384 3 0 5 4.7 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2sccc21 10.1021/jm011014y
CHEMBL320572 108115 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 384 3 0 5 4.7 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2sccc21 10.1021/jm011014y
CHEMBL539544 108115 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 384 3 0 5 4.7 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2sccc21 10.1021/jm011014y
10693017 33600 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 412 8 0 5 3.8 O=C(CCCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm0009890
CHEMBL142316 33600 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 412 8 0 5 3.8 O=C(CCCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm0009890
10367486 9189 1 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 398 4 0 5 5.0 O=C1c2ccsc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm011014y
CHEMBL110948 9189 1 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 398 4 0 5 5.0 O=C1c2ccsc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm011014y
CHEMBL543613 9189 1 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 398 4 0 5 5.0 O=C1c2ccsc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm011014y
10693017 33600 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 412 8 0 5 3.8 O=C(CCCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL142316 33600 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 412 8 0 5 3.8 O=C(CCCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
10069784 14799 1 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 404 4 1 3 4.6 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2[nH]c3ccccc3c21 10.1021/jm011014y
CHEMBL120903 14799 1 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 404 4 1 3 4.6 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2[nH]c3ccccc3c21 10.1021/jm011014y
15021876 102922 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 365 4 0 3 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2ccccc21 10.1021/jm011014y
CHEMBL308480 102922 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 365 4 0 3 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2ccccc21 10.1021/jm011014y
10809188 9170 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 370 5 0 5 3.7 COc1ccccc1N1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm011014y
CHEMBL110847 9170 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 370 5 0 5 3.7 COc1ccccc1N1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm011014y
CHEMBL540822 9170 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 370 5 0 5 3.7 COc1ccccc1N1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm011014y
10497359 121210 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 340 4 0 5 2.9 COc1ccccc1N1CCN(CC2CC(=O)c3ccoc3C2)CC1 10.1021/jm0009890
CHEMBL358895 121210 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 340 4 0 5 2.9 COc1ccccc1N1CCN(CC2CC(=O)c3ccoc3C2)CC1 10.1021/jm0009890
10497359 121210 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 340 4 0 5 2.9 COc1ccccc1N1CCN(CC2CC(=O)c3ccoc3C2)CC1 10.1021/jm011014y
CHEMBL358895 121210 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 340 4 0 5 2.9 COc1ccccc1N1CCN(CC2CC(=O)c3ccoc3C2)CC1 10.1021/jm011014y
197139 24853 20 None - 0 Rat 5.2 pKd = 5.2 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 181 3 2 3 1.3 COc1cc(CC(C)N)ccc1O 10.1021/jm00183a006
CHEMBL1347 24853 20 None - 0 Rat 5.2 pKd = 5.2 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 181 3 2 3 1.3 COc1cc(CC(C)N)ccc1O 10.1021/jm00183a006
11023903 52460 0 None - 0 Rat 5.2 pKd = 5.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 327 3 0 5 2.7 O=C1CC(CN2CCN(c3ccccn3)CC2)Cc2sccc21 10.1021/jm011014y
CHEMBL159466 52460 0 None - 0 Rat 5.2 pKd = 5.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 327 3 0 5 2.7 O=C1CC(CN2CCN(c3ccccn3)CC2)Cc2sccc21 10.1021/jm011014y
10015954 164676 2 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 270 2 2 4 3.1 Cc1cc(NC(=O)Nc2ccc3c(ccn3C)c2)on1 10.1021/jm00006a001
CHEMBL422923 164676 2 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 270 2 2 4 3.1 Cc1cc(NC(=O)Nc2ccc3c(ccn3C)c2)on1 10.1021/jm00006a001
9886130 204694 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 379 5 0 3 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm011014y
CHEMBL87943 204694 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 379 5 0 3 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm011014y
10622347 54104 0 None - 0 Rat 5.1 pKd = 5.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 426 8 0 4 4.0 O=C(CCCN1CCN(CCC2Cc3cc(F)ccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL160907 54104 0 None - 0 Rat 5.1 pKd = 5.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 426 8 0 4 4.0 O=C(CCCN1CCN(CCC2Cc3cc(F)ccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
10044334 205382 13 None - 0 Rat 7.1 pKd = 7.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 364 5 0 4 3.7 COc1ccccc1N1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm011014y
CHEMBL92145 205382 13 None - 0 Rat 7.1 pKd = 7.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 364 5 0 4 3.7 COc1ccccc1N1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm011014y
12611596 59970 6 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 195 3 2 3 1.6 COc1cc(CC(C)N)c(O)cc1C 10.1021/jm00183a006
CHEMBL174380 59970 6 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 195 3 2 3 1.6 COc1cc(CC(C)N)c(O)cc1C 10.1021/jm00183a006
44385952 61864 5 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 195 3 2 3 1.6 COc1cc(C)c(O)cc1CC(C)N 10.1021/jm00183a006
CHEMBL177800 61864 5 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 195 3 2 3 1.6 COc1cc(C)c(O)cc1CC(C)N 10.1021/jm00183a006
9951964 204625 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 383 5 0 3 4.3 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3cc(F)ccc3C2=O)CC1 10.1021/jm011014y
CHEMBL87458 204625 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 383 5 0 3 4.3 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3cc(F)ccc3C2=O)CC1 10.1021/jm011014y
12611609 60100 3 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 167 3 2 3 0.9 COc1ccc(O)c(CCN)c1 10.1021/jm00183a006
CHEMBL175204 60100 3 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 167 3 2 3 0.9 COc1ccc(O)c(CCN)c1 10.1021/jm00183a006
2148 3815 109 None - 4 Rat 5.1 pKd = 5.1 Functional
Antagonistic activity of corresponding methoxy compound against serotonin 5-HT receptorAntagonistic activity of corresponding methoxy compound against serotonin 5-HT receptor
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1021/jm00183a006
2150 3815 109 None - 4 Rat 5.1 pKd = 5.1 Functional
Antagonistic activity of corresponding methoxy compound against serotonin 5-HT receptorAntagonistic activity of corresponding methoxy compound against serotonin 5-HT receptor
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1021/jm00183a006
2784 3815 109 None - 4 Rat 5.1 pKd = 5.1 Functional
Antagonistic activity of corresponding methoxy compound against serotonin 5-HT receptorAntagonistic activity of corresponding methoxy compound against serotonin 5-HT receptor
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1021/jm00183a006
5610 3815 109 None - 4 Rat 5.1 pKd = 5.1 Functional
Antagonistic activity of corresponding methoxy compound against serotonin 5-HT receptorAntagonistic activity of corresponding methoxy compound against serotonin 5-HT receptor
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1021/jm00183a006
CHEMBL11608 3815 109 None - 4 Rat 5.1 pKd = 5.1 Functional
Antagonistic activity of corresponding methoxy compound against serotonin 5-HT receptorAntagonistic activity of corresponding methoxy compound against serotonin 5-HT receptor
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1021/jm00183a006
DB08841 3815 109 None - 4 Rat 5.1 pKd = 5.1 Functional
Antagonistic activity of corresponding methoxy compound against serotonin 5-HT receptorAntagonistic activity of corresponding methoxy compound against serotonin 5-HT receptor
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1021/jm00183a006
10022123 53020 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 371 5 0 4 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3sccc3C2=O)CC1 10.1021/jm011014y
CHEMBL159969 53020 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 371 5 0 4 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3sccc3C2=O)CC1 10.1021/jm011014y
CHEMBL92673 53020 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 371 5 0 4 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3sccc3C2=O)CC1 10.1021/jm011014y
10544858 169450 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 336 4 0 4 3.2 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc32)CC1 10.1021/jm011014y
CHEMBL444269 169450 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 336 4 0 4 3.2 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc32)CC1 10.1021/jm011014y
CHEMBL542181 169450 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 336 4 0 4 3.2 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc32)CC1 10.1021/jm011014y
11121409 56093 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 341 4 0 5 3.1 O=C1c2ccsc2CCC1CCN1CCN(c2ccccn2)CC1 10.1021/jm011014y
CHEMBL163180 56093 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 341 4 0 5 3.1 O=C1c2ccsc2CCC1CCN1CCN(c2ccccn2)CC1 10.1021/jm011014y
10710246 120601 0 None - 0 Rat 6.0 pKd = 6.0 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 312 3 0 6 1.6 O=C1CC(CN2CCN(c3ncccn3)CC2)Cc2occc21 10.1021/jm011014y
CHEMBL357517 120601 0 None - 0 Rat 6.0 pKd = 6.0 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 312 3 0 6 1.6 O=C1CC(CN2CCN(c3ncccn3)CC2)Cc2occc21 10.1021/jm011014y
10017554 4260 25 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligandAntagonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligand
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm960199j
CHEMBL101008 4260 25 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligandAntagonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligand
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm960199j
10017554 4260 25 None - 1 Human 8.8 pKi = 8.8 Functional
Agonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]-5-HT as radioligandAgonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]-5-HT as radioligand
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm960199j
CHEMBL101008 4260 25 None - 1 Human 8.8 pKi = 8.8 Functional
Agonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]-5-HT as radioligandAgonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]-5-HT as radioligand
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm960199j
134143752 150104 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 447 7 3 9 1.9 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3955519 150104 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 447 7 3 9 1.9 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
49836525 18604 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 CC1(C(=O)O)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1278202 18604 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 CC1(C(=O)O)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836524 18603 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 361 2 1 2 4.0 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1278201 18603 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 361 2 1 2 4.0 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
46933091 15572 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 400 4 1 5 3.1 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(Cl)nc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222695 15572 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 400 4 1 5 3.1 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(Cl)nc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
49836526 18446 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 3 1 2 4.4 O=C(O)CC1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1276859 18446 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 3 1 2 4.4 O=C(O)CC1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836411 18523 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 389 3 1 2 4.8 O=C(O)CC1CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277585 18523 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 389 3 1 2 4.8 O=C(O)CC1CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
44516817 57343 4 None -1023 2 Human 6.0 pKi = 6.0 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilizationAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668584 57343 4 None -1023 2 Human 6.0 pKi = 6.0 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilizationAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
185 3931 54 None - 1 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10.1021/jm100856p
5311271 3931 54 None - 1 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10.1021/jm100856p
CHEMBL74355 3931 54 None - 1 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10.1021/jm100856p
DB16351 3931 54 None - 1 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10.1021/jm100856p
49836412 18522 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 O=C(O)[C@@H]1CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277584 18522 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 O=C(O)[C@@H]1CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836294 18577 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 387 2 0 3 4.4 COC(=O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1278020 18577 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 387 2 0 3 4.4 COC(=O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836522 18592 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 376 2 2 3 3.0 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CCN1 10.1021/jm100856p
CHEMBL1278113 18592 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 376 2 2 3 3.0 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CCN1 10.1021/jm100856p
52944115 18595 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 291 1 0 1 4.2 CN(C)C1CC[C@]2(Cc3ccccc3Cc3ccccc32)C1 10.1021/jm100856p
CHEMBL1278116 18595 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 291 1 0 1 4.2 CN(C)C1CC[C@]2(Cc3ccccc3Cc3ccccc32)C1 10.1021/jm100856p
49833883 15570 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 394 4 1 5 3.1 Cc1nc2n(c1C)Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1 10.1016/j.bmcl.2010.07.029
CHEMBL1222693 15570 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 394 4 1 5 3.1 Cc1nc2n(c1C)Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1 10.1016/j.bmcl.2010.07.029
44156754 6417 3 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082763 6417 3 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
49836299 18542 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277770 18542 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
49833886 15587 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 396 5 1 6 2.5 COc1cnc2n1Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1 10.1016/j.bmcl.2010.07.029
CHEMBL1222764 15587 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 396 5 1 6 2.5 COc1cnc2n1Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1 10.1016/j.bmcl.2010.07.029
49836639 18482 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 377 2 1 3 4.6 O=C(O)C1CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277216 18482 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 377 2 1 3 4.6 O=C(O)C1CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1 10.1021/jm100856p
46933089 15542 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 366 4 1 5 2.5 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222554 15542 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 366 4 1 5 2.5 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
46867519 6415 3 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082761 6415 3 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
44156752 6487 3 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083075 6487 3 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
10609802 106695 2 None - 2 Human 6.7 pKi = 6.7 Functional
Antagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine radioligandAntagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine radioligand
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2 10.1021/jm970219x
CHEMBL316527 106695 2 None - 2 Human 6.7 pKi = 6.7 Functional
Antagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine radioligandAntagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine radioligand
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2 10.1021/jm970219x
155531067 171043 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 369 7 3 6 3.3 Nc1nc(NCCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
CHEMBL4465512 171043 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 369 7 3 6 3.3 Nc1nc(NCCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
134141831 146142 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 405 6 4 8 1.4 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3923870 146142 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 405 6 4 8 1.4 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
49833882 15569 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 392 3 1 5 3.0 O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1 10.1016/j.bmcl.2010.07.029
CHEMBL1222692 15569 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 392 3 1 5 3.0 O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1 10.1016/j.bmcl.2010.07.029
46933090 15585 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 400 4 1 5 3.1 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3c(Cl)cnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222762 15585 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 400 4 1 5 3.1 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3c(Cl)cnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
49836635 18465 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 359 2 1 2 4.0 O=C(O)C=C1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277035 18465 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 359 2 1 2 4.0 O=C(O)C=C1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836409 18534 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 391 2 2 3 3.5 O=C(O)C1(O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277679 18534 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 391 2 2 3 3.5 O=C(O)C1(O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
49836300 18541 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 389 2 1 2 4.8 CC1(C(=O)O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277769 18541 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 389 2 1 2 4.8 CC1(C(=O)O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
134154065 151817 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 433 6 3 9 1.5 COC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3970041 151817 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 433 6 3 9 1.5 COC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
11957541 1425 38 None 1 5 Human 8.5 pKi = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
1229 1425 38 None 1 5 Human 8.5 pKi = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
147 1425 38 None 1 5 Human 8.5 pKi = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
170617 1425 38 None 1 5 Human 8.5 pKi = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
CHEMBL6616 1425 38 None 1 5 Human 8.5 pKi = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
10609802 106695 2 None - 2 Human 6.5 pKi = 6.5 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2 10.1021/jm970219x
CHEMBL316527 106695 2 None - 2 Human 6.5 pKi = 6.5 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2 10.1021/jm970219x
1530 2142 44 None -3 21 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
3827 2142 44 None -3 21 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
7206 2142 44 None -3 21 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
CHEMBL534 2142 44 None -3 21 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
DB00920 2142 44 None -3 21 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
10440 2632 15 None - 3 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
139030523 2632 15 None - 3 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
CHEMBL4449712 2632 15 None - 3 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
10751567 4456 2 None - 2 Human 6.5 pKi = 6.5 Functional
Antagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine radioligandAntagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine radioligand
ChEMBL 223 4 1 4 1.1 COc1cc(CCN)c2c(c1OC)OCC2 10.1021/jm970219x
CHEMBL102347 4456 2 None - 2 Human 6.5 pKi = 6.5 Functional
Antagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine radioligandAntagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine radioligand
ChEMBL 223 4 1 4 1.1 COc1cc(CCN)c2c(c1OC)OCC2 10.1021/jm970219x
49864841 15540 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 266 1 1 4 1.6 C1=C(N2CCNCC2)c2nccn2Cc2ccccc21 10.1016/j.bmcl.2010.07.029
CHEMBL1222552 15540 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 266 1 1 4 1.6 C1=C(N2CCNCC2)c2nccn2Cc2ccccc21 10.1016/j.bmcl.2010.07.029
49834053 15586 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 384 4 1 5 2.6 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(F)nc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222763 15586 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 384 4 1 5 2.6 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(F)nc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
49836634 18464 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 361 3 1 2 4.0 O=C(O)CC1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277034 18464 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 361 3 1 2 4.0 O=C(O)CC1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49833882 15569 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 392 3 1 5 3.0 O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1 10.1016/j.bmcl.2010.07.029
CHEMBL1222692 15569 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 392 3 1 5 3.0 O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1 10.1016/j.bmcl.2010.07.029
25110703 189118 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at 5HT2B receptorAntagonist activity at 5HT2B receptor
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL515624 189118 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at 5HT2B receptorAntagonist activity at 5HT2B receptor
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
49836528 18456 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 373 2 1 2 4.0 O=C(O)[C@]12C[C@H]1CN(C1CC[C@]3(Cc4ccccc4Cc4ccccc43)C1)C2 10.1021/jm100856p
CHEMBL1276947 18456 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 373 2 1 2 4.0 O=C(O)[C@]12C[C@H]1CN(C1CC[C@]3(Cc4ccccc4Cc4ccccc43)C1)C2 10.1021/jm100856p
134152052 152537 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 432 6 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3976121 152537 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 432 6 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
44156628 6621 3 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083654 6621 3 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
10751567 4456 2 None - 2 Human 6.3 pKi = 6.3 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 223 4 1 4 1.1 COc1cc(CCN)c2c(c1OC)OCC2 10.1021/jm970219x
CHEMBL102347 4456 2 None - 2 Human 6.3 pKi = 6.3 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 223 4 1 4 1.1 COc1cc(CCN)c2c(c1OC)OCC2 10.1021/jm970219x
38240 107500 18 None - 2 Human 6.3 pKi = 6.3 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 225 6 1 4 1.6 CCOc1c(OC)cc(CCN)cc1OC 10.1021/jm970219x
CHEMBL319415 107500 18 None - 2 Human 6.3 pKi = 6.3 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 225 6 1 4 1.6 CCOc1c(OC)cc(CCN)cc1OC 10.1021/jm970219x
49833884 15571 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 380 4 1 5 2.8 Cc1cn2c(n1)C(N1CCN(CC(C)(C)C(=O)O)CC1)=Cc1ccccc1C2 10.1016/j.bmcl.2010.07.029
CHEMBL1222694 15571 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 380 4 1 5 2.8 Cc1cn2c(n1)C(N1CCN(CC(C)(C)C(=O)O)CC1)=Cc1ccccc1C2 10.1016/j.bmcl.2010.07.029
49864886 15554 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 366 4 1 5 2.6 CC1CN(C2=Cc3ccccc3Cn3ccnc32)CC(C)N1CCC(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222624 15554 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 366 4 1 5 2.6 CC1CN(C2=Cc3ccccc3Cn3ccnc32)CC(C)N1CCC(=O)O 10.1016/j.bmcl.2010.07.029
155558626 174179 0 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 355 6 3 6 2.9 Nc1nc(NCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
CHEMBL4561016 174179 0 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 355 6 3 6 2.9 Nc1nc(NCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
49836633 18457 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 347 2 1 2 3.6 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1276948 18457 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 347 2 1 2 3.6 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
25184832 18493 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 349 2 1 3 3.8 O=C(O)C1CN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277312 18493 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 349 2 1 3 3.8 O=C(O)C1CN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1 10.1021/jm100856p
4076 96572 23 None - 2 Human 6.1 pKi = 6.1 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 211 5 1 4 1.2 COc1cc(CCN)cc(OC)c1OC 10.1021/jm970219x
CHEMBL26687 96572 23 None - 2 Human 6.1 pKi = 6.1 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 211 5 1 4 1.2 COc1cc(CCN)cc(OC)c1OC 10.1021/jm970219x
2995 202690 49 None -2 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 202690 49 None -2 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 202690 49 None -2 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
1225 1438 24 None -3 11 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1438 24 None -3 11 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1438 24 None -3 11 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1438 24 None -3 11 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1438 24 None -3 11 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
2105 2993 34 None -5 19 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 2993 34 None -5 19 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 2993 34 None -5 19 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 2993 34 None -5 19 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 2993 34 None -5 19 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
439280 119501 104 None -3 7 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
Drug Central 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O None
6971044 119501 104 None -3 7 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
Drug Central 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O None
CHEMBL350221 119501 104 None -3 7 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
Drug Central 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O None
11658860 2302 47 None -63 4 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
2941 2302 47 None -63 4 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
4374 2302 47 None -63 4 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
CHEMBL360328 2302 47 None -63 4 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
DB04871 2302 47 None -63 4 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
30699 215959 0 None -1 14 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 423 7 2 8 0.5 CC(=O)OCC1=C(N2[C@H](SC1)[C@H](NC(=O)CSC1=CC=NC=C1)C2=O)C(O)=O None
5215 168390 100 None 1 3 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 250 3 2 5 0.9 Nc1ccc(S(=O)(=O)Nc2ncccn2)cc1 None
CHEMBL439 168390 100 None 1 3 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 250 3 2 5 0.9 Nc1ccc(S(=O)(=O)Nc2ncccn2)cc1 None
4421 215979 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 232 2 1 4 1.4 CCN1C=C(C(O)=O)C(=O)C2=CC=C(C)N=C12 None
14052 215969 0 None 1 3 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 204 9 4 4 -0.3 CC[C@@H](CO)NCCN[C@@H](CC)CO None
33613 215949 0 None -1 3 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 365 4 4 6 0.0 CC1(C)S[C@@H]2[C@H](NC(=O)[C@H](N)C3=CC=C(O)C=C3)C(=O)N2[C@H]1C(O)=O None
2337 3193 72 None -5 22 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3193 72 None -5 22 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3193 72 None -5 22 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3193 72 None -5 22 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3193 72 None -5 22 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 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
10198431 73542 0 None -7 3 Human 9.0 pEC50 = 9.0 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201930 73542 0 None -7 3 Human 9.0 pEC50 = 9.0 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
5 139 66 None -13 55 Human 8.8 pEC50 = 8.8 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
5202 139 66 None -13 55 Human 8.8 pEC50 = 8.8 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
CHEMBL39 139 66 None -13 55 Human 8.8 pEC50 = 8.8 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
DB08839 139 66 None -13 55 Human 8.8 pEC50 = 8.8 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
44407335 72732 0 None -7 3 Human 6.9 pEC50 = 6.9 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 321 5 1 3 4.7 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCC1CCCCC1 10.1016/j.bmcl.2005.10.029
CHEMBL201117 72732 0 None -7 3 Human 6.9 pEC50 = 6.9 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 321 5 1 3 4.7 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCC1CCCCC1 10.1016/j.bmcl.2005.10.029
44407440 138763 0 None -4 3 Human 6.9 pEC50 = 6.9 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 329 5 1 3 4.7 Cc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL379223 138763 0 None -4 3 Human 6.9 pEC50 = 6.9 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 329 5 1 3 4.7 Cc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
18715554 74060 0 None -10 3 Human 6.8 pEC50 = 6.8 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cnccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL202656 74060 0 None -10 3 Human 6.8 pEC50 = 6.8 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cnccc3c21 10.1016/j.bmcl.2005.10.029
18715564 73018 0 None -7 3 Human 8.7 pEC50 = 8.7 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 259 2 1 3 3.2 C[C@H](N)Cn1ccc2cc(Cl)c3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201454 73018 0 None -7 3 Human 8.7 pEC50 = 8.7 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 259 2 1 3 3.2 C[C@H](N)Cn1ccc2cc(Cl)c3ncccc3c21 10.1016/j.bmcl.2005.10.029
18715555 74011 0 None -8 3 Human 7.7 pEC50 = 7.7 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 359 5 1 5 4.1 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2005.10.029
CHEMBL202458 74011 0 None -8 3 Human 7.7 pEC50 = 7.7 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 359 5 1 5 4.1 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2005.10.029
135398737 942 89 None -2 92 Human 7.7 pEC50 = 7.7 Binding
Inverse agonist activity at human 5HT2B receptor by R-SAT assayInverse agonist activity at human 5HT2B receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 942 89 None -2 92 Human 7.7 pEC50 = 7.7 Binding
Inverse agonist activity at human 5HT2B receptor by R-SAT assayInverse agonist activity at human 5HT2B receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 942 89 None -2 92 Human 7.7 pEC50 = 7.7 Binding
Inverse agonist activity at human 5HT2B receptor by R-SAT assayInverse agonist activity at human 5HT2B receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 942 89 None -2 92 Human 7.7 pEC50 = 7.7 Binding
Inverse agonist activity at human 5HT2B receptor by R-SAT assayInverse agonist activity at human 5HT2B receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 942 89 None -2 92 Human 7.7 pEC50 = 7.7 Binding
Inverse agonist activity at human 5HT2B receptor by R-SAT assayInverse agonist activity at human 5HT2B receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
44407398 74054 0 None -8 3 Human 7.6 pEC50 = 7.6 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 365 5 1 3 5.5 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2ccccc2c1 10.1016/j.bmcl.2005.10.029
CHEMBL202616 74054 0 None -8 3 Human 7.6 pEC50 = 7.6 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 365 5 1 3 5.5 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2ccccc2c1 10.1016/j.bmcl.2005.10.029
5 139 66 None -29 55 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secsAgonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secs
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2015.08.051
5202 139 66 None -29 55 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secsAgonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secs
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2015.08.051
CHEMBL39 139 66 None -29 55 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secsAgonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secs
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2015.08.051
DB08839 139 66 None -29 55 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secsAgonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secs
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2015.08.051
166 3295 12 None 1 3 Human 8.4 pEC50 = 8.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
3045227 3295 12 None 1 3 Human 8.4 pEC50 = 8.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
CHEMBL76781 3295 12 None 1 3 Human 8.4 pEC50 = 8.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
44407453 74039 0 None -9 3 Human 7.4 pEC50 = 7.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 349 5 1 3 5.0 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1Cl 10.1016/j.bmcl.2005.10.029
CHEMBL202538 74039 0 None -9 3 Human 7.4 pEC50 = 7.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 349 5 1 3 5.0 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1Cl 10.1016/j.bmcl.2005.10.029
18715561 72682 0 None -4 3 Human 7.4 pEC50 = 7.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cccnc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201062 72682 0 None -4 3 Human 7.4 pEC50 = 7.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cccnc3c21 10.1016/j.bmcl.2005.10.029
44407327 140703 0 None -5 3 Human 6.3 pEC50 = 6.3 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 345 6 1 4 4.4 COc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL383042 140703 0 None -5 3 Human 6.3 pEC50 = 6.3 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 345 6 1 4 4.4 COc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
18715558 73519 0 None -5 3 Human 7.2 pEC50 = 7.2 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ccncc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201897 73519 0 None -5 3 Human 7.2 pEC50 = 7.2 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ccncc3c21 10.1016/j.bmcl.2005.10.029
9901086 187038 28 None - 2 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at 5HT2B receptor (unknown origin) relative to controlAgonist activity at 5HT2B receptor (unknown origin) relative to control
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm5019274
CHEMBL494947 187038 28 None - 2 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at 5HT2B receptor (unknown origin) relative to controlAgonist activity at 5HT2B receptor (unknown origin) relative to control
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm5019274
44407337 73841 0 None -5 3 Human 7.0 pEC50 = 7.0 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 265 5 1 3 3.4 C=CCN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL202324 73841 0 None -5 3 Human 7.0 pEC50 = 7.0 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 265 5 1 3 3.4 C=CCN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
44407460 139807 0 None -6 3 Human 7.0 pEC50 = 7.0 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 315 5 1 3 4.4 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1 10.1016/j.bmcl.2005.10.029
CHEMBL380763 139807 0 None -6 3 Human 7.0 pEC50 = 7.0 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 315 5 1 3 4.4 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1 10.1016/j.bmcl.2005.10.029
CHEMBL5081637 212975 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL None None None CN(CCc1cn(C)c2cccc(O)c12)CC1CC1 10.1021/acsmedchemlett.1c00578
133 2450 48 None -2 43 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2450 48 None -2 43 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2450 48 None -2 43 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2450 48 None -2 43 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2450 48 None -2 43 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
134 2468 19 None -2 68 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 2468 19 None -2 68 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 2468 19 None -2 68 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 2468 19 None -2 68 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 2468 19 None -2 68 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
11291 3157 23 None - 5 Human 9.0 pIC50 = 9.0 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.1c00578
4980 3157 23 None - 5 Human 9.0 pIC50 = 9.0 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.1c00578
CHEMBL65547 3157 23 None - 5 Human 9.0 pIC50 = 9.0 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.1c00578
150 2463 18 None 1 16 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 2463 18 None 1 16 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 2463 18 None 1 16 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 2463 18 None 1 16 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 2463 18 None 1 16 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
191 399 92 None -5 29 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 399 92 None -5 29 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 399 92 None -5 29 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 399 92 None -5 29 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 399 92 None -5 29 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2099 9202 49 None - 1 Human 7.0 pIC50 = 7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O nan
CHEMBL1110 9202 49 None - 1 Human 7.0 pIC50 = 7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O nan
11518143 88623 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of 5-HT2B (unknown origin)Inhibition of 5-HT2B (unknown origin)
ChEMBL 454 12 1 5 4.0 COCCCOc1cc(C(=O)N(C[C@@H]2CNC[C@H]2Cc2ccccc2)C(C)C)ccc1OC 10.1021/jm3017078
CHEMBL2322611 88623 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of 5-HT2B (unknown origin)Inhibition of 5-HT2B (unknown origin)
ChEMBL 454 12 1 5 4.0 COCCCOc1cc(C(=O)N(C[C@@H]2CNC[C@H]2Cc2ccccc2)C(C)C)ccc1OC 10.1021/jm3017078
CHEMBL2365004 88623 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of 5-HT2B (unknown origin)Inhibition of 5-HT2B (unknown origin)
ChEMBL 454 12 1 5 4.0 COCCCOc1cc(C(=O)N(C[C@@H]2CNC[C@H]2Cc2ccccc2)C(C)C)ccc1OC 10.1021/jm3017078
2274 3112 53 None -10 32 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3112 53 None -10 32 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3112 53 None -10 32 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3112 53 None -10 32 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3112 53 None -10 32 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
25060119 103824 0 None -9332 7 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
CHEMBL3099899 103824 0 None -9332 7 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
3033538 1287 36 None -12 9 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
7155 1287 36 None -12 9 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
781 1287 36 None -12 9 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
CHEMBL1201216 1287 36 None -12 9 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
DB00298 1287 36 None -12 9 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
213 3780 50 None -5 44 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 3780 50 None -5 44 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 3780 50 None -5 44 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 3780 50 None -5 44 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 3780 50 None -5 44 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
12488 1619 51 None -11 23 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1619 51 None -11 23 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1619 51 None -11 23 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1619 51 None -11 23 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
135398737 942 89 None -2 92 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 942 89 None -2 92 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 942 89 None -2 92 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 942 89 None -2 92 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 942 89 None -2 92 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
73453 29388 22 None -9 17 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29388 22 None -9 17 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
25070577 111162 3 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 304 3 2 4 2.3 CNc1nc(C(F)(F)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL3286557 111162 3 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 304 3 2 4 2.3 CNc1nc(C(F)(F)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
240 929 39 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
2769 929 39 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
44279790 929 39 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
660 929 39 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL1729 929 39 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL560739 929 39 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
DB00604 929 39 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
146159245 187856 27 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
451415 187856 27 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
86289437 187856 27 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
CHEMBL502620 187856 27 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
1224 1399 79 None -6 13 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1399 79 None -6 13 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1399 79 None -6 13 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1399 79 None -6 13 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1399 79 None -6 13 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1399 79 None -6 13 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
4178 194120 58 None - 1 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N nan
CHEMBL558 194120 58 None - 1 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N nan
44190762 176296 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from 5HT2B receptorDisplacement of radioligand from 5HT2B 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 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from 5HT2B receptorDisplacement of radioligand from 5HT2B 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
222757 98904 70 None -1 3 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O nan
CHEMBL282575 98904 70 None -1 3 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O nan
2812 4696 96 None -40 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4696 96 None -40 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
2247 502 77 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
23027035 196860 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
CHEMBL578170 196860 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
54764239 68509 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 272 2 1 3 2.7 CC/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL1922537 68509 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 272 2 1 3 2.7 CC/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
2726 904 64 None -19 73 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 904 64 None -19 73 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 904 64 None -19 73 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 904 64 None -19 73 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 904 64 None -19 73 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
76072441 153401 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 391 7 0 4 3.4 C=CCN1CC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)OC1=O nan
CHEMBL3983539 153401 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 391 7 0 4 3.4 C=CCN1CC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)OC1=O nan
100 3733 52 None -11 56 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3733 52 None -11 56 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3733 52 None -11 56 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3733 52 None -11 56 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3733 52 None -11 56 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
134551 355 25 None -6 21 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 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)C(C)C)O)C nan
271 355 25 None -6 21 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 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)C(C)C)O)C nan
885 355 25 None -6 21 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 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)C(C)C)O)C nan
CHEMBL1403281 355 25 None -6 21 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 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)C(C)C)O)C nan
23027211 195564 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568400 195564 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
100951644 169056 11 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 411 7 2 9 2.3 CO[C@H](C(=O)Nc1nnc(N[C@@H]2CCN(c3cccnn3)C2)s1)c1ccccc1 10.1021/acs.jmedchem.9b00260
CHEMBL4437106 169056 11 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 411 7 2 9 2.3 CO[C@H](C(=O)Nc1nnc(N[C@@H]2CCN(c3cccnn3)C2)s1)c1ccccc1 10.1021/acs.jmedchem.9b00260
3042 1381 31 None -39 15 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1381 31 None -39 15 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1381 31 None -39 15 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1381 31 None -39 15 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1381 31 None -39 15 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
5591 156977 84 None 1 2 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 nan
CHEMBL408 156977 84 None 1 2 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 nan
3168 9157 84 None -107 22 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9157 84 None -107 22 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
127048333 140136 0 None 38 3 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human 5-HT2B receptor by PDSP assayAntagonist activity at human 5-HT2B receptor by PDSP assay
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2ccccc2F)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3815112 140136 0 None 38 3 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human 5-HT2B receptor by PDSP assayAntagonist activity at human 5-HT2B receptor by PDSP assay
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2ccccc2F)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
4543 169972 36 None -4 30 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL1201156 169972 36 None -4 30 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL445 169972 36 None -4 30 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
1548953 205935 24 None -4 17 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 205935 24 None -4 17 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
5870 31430 85 None - 1 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 270 0 1 2 3.8 C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O nan
CHEMBL1405 31430 85 None - 1 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 270 0 1 2 3.8 C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O nan
6319 23257 90 None - 1 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 4 2 2 5.2 c1ccc(Nc2ccc(Nc3ccccc3)cc2)cc1 nan
CHEMBL1333512 23257 90 None - 1 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 4 2 2 5.2 c1ccc(Nc2ccc(Nc3ccccc3)cc2)cc1 nan
1305 508 10 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
9934033 508 10 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL182150 508 10 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
121318543 176983 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5-HT2B (unknown origin)Inhibition of 5-HT2B (unknown origin)
ChEMBL 560 6 0 6 4.7 COc1c(S(C)(=O)=O)ccc(O[C@@H](C)C(F)(F)F)c1C(=O)N1CC(c2ncc(C(F)(F)F)cc2Cl)C1 10.1016/j.bmcl.2020.127214
CHEMBL4640428 176983 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5-HT2B (unknown origin)Inhibition of 5-HT2B (unknown origin)
ChEMBL 560 6 0 6 4.7 COc1c(S(C)(=O)=O)ccc(O[C@@H](C)C(F)(F)F)c1C(=O)N1CC(c2ncc(C(F)(F)F)cc2Cl)C1 10.1016/j.bmcl.2020.127214
16665072 98073 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT2BInhibition of 5HT2B
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL276393 98073 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT2BInhibition of 5HT2B
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
155558726 174226 0 None -19 4 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 835 11 0 13 6.7 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CC[C@H]3O[C@H](Cn4cc(nn4)COC[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12)[C@@H]1OC(C)(C)O[C@@H]1[C@H]3OCCC(C)C 10.1016/j.ejmech.2019.04.064
CHEMBL4562303 174226 0 None -19 4 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 835 11 0 13 6.7 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CC[C@H]3O[C@H](Cn4cc(nn4)COC[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12)[C@@H]1OC(C)(C)O[C@@H]1[C@H]3OCCC(C)C 10.1016/j.ejmech.2019.04.064
667590 67437 12 None - 1 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 3 0 1 4.4 O=C(c1ccccc1Cl)N1CCC(Cc2ccccc2)CC1 nan
CHEMBL1909048 67437 12 None - 1 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 3 0 1 4.4 O=C(c1ccccc1Cl)N1CCC(Cc2ccccc2)CC1 nan
44112 120764 41 None -11 7 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
CHEMBL357995 120764 41 None -11 7 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
17683252 67439 3 None - 1 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 347 3 0 1 4.8 O=C(c1ccccc1C(F)(F)F)N1CCC(Cc2ccccc2)CC1 nan
CHEMBL1909051 67439 3 None - 1 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 347 3 0 1 4.8 O=C(c1ccccc1C(F)(F)F)N1CCC(Cc2ccccc2)CC1 nan
155565189 174982 0 None -6 4 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 634 7 0 9 6.2 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CCCCCCOCc3cn(nn3)C[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12 10.1016/j.ejmech.2019.04.064
CHEMBL4579120 174982 0 None -6 4 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 634 7 0 9 6.2 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CCCCCCOCc3cn(nn3)C[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12 10.1016/j.ejmech.2019.04.064
3525815 73783 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT2BInhibition of 5HT2B
ChEMBL 271 2 0 3 4.1 c1ccc(-n2cc(-c3ccnc4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2022867 73783 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT2BInhibition of 5HT2B
ChEMBL 271 2 0 3 4.1 c1ccc(-n2cc(-c3ccnc4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
2520 202301 65 None -4 12 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL1280 202301 65 None -4 12 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL6966 202301 65 None -4 12 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
23027245 195442 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL567791 195442 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
10660 14283 55 None -29 12 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
CHEMBL1200406 14283 55 None -29 12 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
2333 141791 91 None 1 2 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 nan
CHEMBL388590 141791 91 None 1 2 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 nan
2771 193337 67 None 1 27 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL1200781 193337 67 None 1 27 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL549 193337 67 None 1 27 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
104903 56035 14 None -4 6 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
CHEMBL1630578 56035 14 None -4 6 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
2723 153500 104 None - 1 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl nan
CHEMBL398440 153500 104 None - 1 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl nan
1379258 67438 13 None - 1 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 3 0 1 4.1 Cc1ccccc1C(=O)N1CCC(Cc2ccccc2)CC1 nan
CHEMBL1909050 67438 13 None - 1 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 3 0 1 4.1 Cc1ccccc1C(=O)N1CCC(Cc2ccccc2)CC1 nan
76072442 145843 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 407 5 0 4 4.0 CC(C)(C)N1CC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)OC1=O nan
CHEMBL3921628 145843 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 407 5 0 4 4.0 CC(C)(C)N1CC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)OC1=O nan
11277147 105847 0 None 9 2 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysisAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092759 105847 0 None 9 2 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysisAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3139188 105847 0 None 9 2 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysisAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
76072471 152991 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 405 6 0 4 3.8 O=C1OC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)CN1C1CCC1 nan
CHEMBL3980023 152991 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 405 6 0 4 3.8 O=C1OC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)CN1C1CCC1 nan
11452268 81147 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of 5HT2BInhibition of 5HT2B
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL216228 81147 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of 5HT2BInhibition of 5HT2B
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
11957541 1425 38 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cellsDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.03.006
1229 1425 38 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cellsDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.03.006
147 1425 38 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cellsDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.03.006
170617 1425 38 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cellsDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.03.006
CHEMBL6616 1425 38 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cellsDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.03.006
11957541 1425 38 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.11.014
1229 1425 38 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.11.014
147 1425 38 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.11.014
170617 1425 38 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.11.014
CHEMBL6616 1425 38 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.11.014
9881053 119727 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [3H]5-HT from 5-hydroxytryptamine 2B receptorAbility to displace [3H]5-HT from 5-hydroxytryptamine 2B receptor
ChEMBL 339 5 1 4 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
CHEMBL35226 119727 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [3H]5-HT from 5-hydroxytryptamine 2B receptorAbility to displace [3H]5-HT from 5-hydroxytryptamine 2B receptor
ChEMBL 339 5 1 4 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
1201549 590 22 None -26 20 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 590 22 None -26 20 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 590 22 None -26 20 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 590 22 None -26 20 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 590 22 None -26 20 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 590 22 None -26 20 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
5510 204127 97 None - 1 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 2 4.9 Cc1cccc(N(C)C(=S)Oc2ccc3ccccc3c2)c1 nan
CHEMBL83668 204127 97 None - 1 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 2 4.9 Cc1cccc(N(C)C(=S)Oc2ccc3ccccc3c2)c1 nan
44393396 126762 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3cccc(Cl)c3Cl)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL365882 126762 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3cccc(Cl)c3Cl)cc12 10.1016/j.bmcl.2004.05.051
4122 205881 102 None -3 3 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 301 3 2 5 3.0 COC(=O)Nc1nc2ccc(C(=O)c3cccs3)cc2[nH]1 nan
CHEMBL9514 205881 102 None -3 3 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 301 3 2 5 3.0 COC(=O)Nc1nc2ccc(C(=O)c3cccs3)cc2[nH]1 nan
1353 1872 85 None -295 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1872 85 None -295 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1872 85 None -295 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1872 85 None -295 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1872 85 None -295 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
1016 3678 75 None -17 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3678 75 None -17 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3678 75 None -17 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3678 75 None -17 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3678 75 None -17 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3678 75 None -17 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL1909069 207322 0 None -1 3 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL None None None None nan
1343 1850 55 None -14 9 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
3519 1850 55 None -14 9 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
522 1850 55 None -14 9 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
CHEMBL862 1850 55 None -14 9 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
DB01018 1850 55 None -14 9 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
2337 3193 72 None -15 63 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3193 72 None -15 63 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3193 72 None -15 63 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3193 72 None -15 63 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3193 72 None -15 63 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
122196341 123741 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human 5HT2bAntagonist activity at human 5HT2b
ChEMBL 422 5 1 3 6.0 O=c1ccc(-c2ccc(OCc3ccc4ccccc4n3)cc2)c(-c2ccc(F)cc2)[nH]1 10.1021/acs.jmedchem.5b01240
CHEMBL3634745 123741 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human 5HT2bAntagonist activity at human 5HT2b
ChEMBL 422 5 1 3 6.0 O=c1ccc(-c2ccc(OCc3ccc4ccccc4n3)cc2)c(-c2ccc(F)cc2)[nH]1 10.1021/acs.jmedchem.5b01240
2585 788 100 None -18 22 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 788 100 None -18 22 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 788 100 None -18 22 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 788 100 None -18 22 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 788 100 None -18 22 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
2389 3267 114 None -79 68 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3267 114 None -79 68 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3267 114 None -79 68 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3267 114 None -79 68 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3267 114 None -79 68 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
2801 161313 56 None -3 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL1200710 161313 56 None -3 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL415 161313 56 None -3 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
1605 2300 110 None -1 4 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
3957 2300 110 None -1 4 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
7216 2300 110 None -1 4 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
CHEMBL998 2300 110 None -1 4 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
DB00455 2300 110 None -1 4 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
45482789 197237 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B 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 5.6 pIC50 = 5.6 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B 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
122185011 122036 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 339 3 0 3 5.0 COc1ccc2c([C@H]3CCc4ccc(Cl)cc43)nccc2c1OC 10.1039/C4MD00113C
CHEMBL3601563 122036 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 339 3 0 3 5.0 COc1ccc2c([C@H]3CCc4ccc(Cl)cc43)nccc2c1OC 10.1039/C4MD00113C
11080 28857 74 None -6 6 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 28857 74 None -6 6 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
3151 1429 93 None -125 27 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
945 1429 93 None -125 27 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
965 1429 93 None -125 27 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
CHEMBL219916 1429 93 None -125 27 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
DB01184 1429 93 None -125 27 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
5818 3722 42 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 394 8 1 5 3.8 COc1cc(/C=C/C(=O)NCCn2c(C)cc3c2cccc3)cc(c1OC)OC 10.1021/jm401431x
5886965 3722 42 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 394 8 1 5 3.8 COc1cc(/C=C/C(=O)NCCn2c(C)cc3c2cccc3)cc(c1OC)OC 10.1021/jm401431x
CHEMBL1368005 3722 42 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 394 8 1 5 3.8 COc1cc(/C=C/C(=O)NCCn2c(C)cc3c2cccc3)cc(c1OC)OC 10.1021/jm401431x
76072440 148806 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 393 6 0 4 3.6 CC(C)N1CC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)OC1=O nan
CHEMBL3945224 148806 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 393 6 0 4 3.6 CC(C)N1CC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)OC1=O nan
1227 2444 35 None -112 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
2331 2444 35 None -112 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
3957 2444 35 None -112 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
4992 2444 35 None -112 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
CHEMBL511 2444 35 None -112 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
DB06691 2444 35 None -112 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
42636941 178361 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptorDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL470432 178361 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptorDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
1524 2141 89 None -234 52 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
197 2141 89 None -234 52 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
3822 2141 89 None -234 52 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
88 2141 89 None -234 52 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
CHEMBL51 2141 89 None -234 52 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
DB12465 2141 89 None -234 52 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
119584 2547 99 None 1 6 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
1848 2547 99 None 1 6 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
242 2547 99 None 1 6 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
CHEMBL60889 2547 99 None 1 6 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
DB11675 2547 99 None 1 6 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
76072443 151034 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 391 6 0 4 3.4 O=C1OC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)CN1C1CC1 nan
CHEMBL3963333 151034 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 391 6 0 4 3.4 O=C1OC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)CN1C1CC1 nan
11957541 1425 38 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2013.03.016
1229 1425 38 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2013.03.016
147 1425 38 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2013.03.016
170617 1425 38 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2013.03.016
CHEMBL6616 1425 38 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2013.03.016
11957541 1425 38 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
1229 1425 38 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
147 1425 38 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
170617 1425 38 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
CHEMBL6616 1425 38 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
72548703 161007 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]+/-DOI from human recombinant 5-HT2B receptor after 60 mins by scintillation counting analysisDisplacement of [125I]+/-DOI from human recombinant 5-HT2B receptor 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 8.5 pIC50 = 8.5 Binding
Displacement of [125I]+/-DOI from human recombinant 5-HT2B receptor after 60 mins by scintillation counting analysisDisplacement of [125I]+/-DOI from human recombinant 5-HT2B receptor 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
1043 1545 13 None -22 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -22 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -22 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -22 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -22 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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
23027527 195107 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL565551 195107 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
23027411 196833 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577912 196833 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
5318 15385 44 None -1 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 15385 44 None -1 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 15385 44 None -1 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
1531 2226 64 None -16 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
3869 2226 64 None -16 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
7207 2226 64 None -16 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
CHEMBL429 2226 64 None -16 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
DB00598 2226 64 None -16 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
124 2921 44 None -181 33 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2921 44 None -181 33 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2921 44 None -181 33 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2921 44 None -181 33 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2921 44 None -181 33 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
45485062 195482 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL567993 195482 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
44404883 71703 26 None -2 5 Human 7.5 pIC50 = 7.5 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1021/acsmedchemlett.1c00578
CHEMBL197664 71703 26 None -2 5 Human 7.5 pIC50 = 7.5 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1021/acsmedchemlett.1c00578
15987265 195202 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL566075 195202 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
3191 102372 93 None -7 25 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102372 93 None -7 25 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
448537 159691 86 None -21 25 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 159691 86 None -21 25 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
5897 104719 71 None -1 3 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 223 1 1 1 3.2 CC(=O)Nc1ccc2c(c1)Cc1ccccc1-2 nan
CHEMBL311469 104719 71 None -1 3 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 223 1 1 1 3.2 CC(=O)Nc1ccc2c(c1)Cc1ccccc1-2 nan
72197486 102017 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-lysergic acid from human recombinant 5HT-2B receptorDisplacement of [3H]-lysergic acid from human recombinant 5HT-2B receptor
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393245 102017 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-lysergic acid from human recombinant 5HT-2B receptorDisplacement of [3H]-lysergic acid from human recombinant 5HT-2B receptor
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040361 102017 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-lysergic acid from human recombinant 5HT-2B receptorDisplacement of [3H]-lysergic acid from human recombinant 5HT-2B receptor
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
45484995 196832 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577904 196832 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
127048335 140049 0 None 15 3 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human 5-HT2B receptor by PDSP assayAntagonist activity at human 5-HT2B receptor by PDSP assay
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2ccccc2Br)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3813726 140049 0 None 15 3 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human 5-HT2B receptor by PDSP assayAntagonist activity at human 5-HT2B receptor by PDSP assay
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2ccccc2Br)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
196129 67441 12 None -26 15 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67441 12 None -26 15 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
4011 81982 43 None -20 24 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 81982 43 None -20 24 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
4601 205010 29 None -4 17 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 205010 29 None -4 17 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 205010 29 None -4 17 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
68617 203806 60 None -15 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL1709 203806 60 None -15 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 203806 60 None -15 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
165193 3126 60 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3126 60 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3126 60 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3126 60 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3126 60 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3126 60 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3126 60 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3126 60 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3126 60 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3126 60 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3126 60 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2353 100630 75 None -7 5 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL12089 100630 75 None -7 5 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL295124 100630 75 None -7 5 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
3117 206096 100 None -8 16 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 206096 100 None -8 16 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
2284 3121 27 None -16 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3121 27 None -16 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3121 27 None -16 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3121 27 None -16 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3121 27 None -16 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
11304816 65932 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL184717 65932 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2004.05.051
11536844 114611 0 None 1 2 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343672 114611 0 None 1 2 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
2351 3222 60 None -7 21 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 3222 60 None -7 21 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 3222 60 None -7 21 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 3222 60 None -7 21 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 3222 60 None -7 21 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
444795 139456 102 None 3 2 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 nan
CHEMBL38 139456 102 None 3 2 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 nan
26987 934 29 None -47 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 934 29 None -47 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 934 29 None -47 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 934 29 None -47 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 934 29 None -47 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
72734860 103467 0 None 6 5 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysisAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092753 103467 0 None 6 5 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysisAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
3973 206429 104 None -44 3 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 4 3.3 O=c1cc(N2CCOCC2)oc2c(-c3ccccc3)cccc12 nan
CHEMBL98350 206429 104 None -44 3 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 4 3.3 O=c1cc(N2CCOCC2)oc2c(-c3ccccc3)cccc12 nan
3157 1437 69 None -37 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
7170 1437 69 None -37 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
954 1437 69 None -37 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
CHEMBL707 1437 69 None -37 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
DB00590 1437 69 None -37 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
58438464 3004 28 None - 3 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
9060 3004 28 None - 3 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
CHEMBL3287218 3004 28 None - 3 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
DB14870 3004 28 None - 3 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
6726 1249 46 None -7 13 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 1249 46 None -7 13 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 1249 46 None -7 13 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 1249 46 None -7 13 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 1249 46 None -7 13 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
118112300 155441 12 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at 5HT2B (unknown origin)Antagonist activity at 5HT2B (unknown origin)
ChEMBL 430 6 2 6 3.8 O=S(=O)(Nc1nccs1)c1cc(Cl)c(NCC23CCCN2CCC3)cc1F 10.1016/j.bmcl.2017.03.085
CHEMBL4061793 155441 12 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at 5HT2B (unknown origin)Antagonist activity at 5HT2B (unknown origin)
ChEMBL 430 6 2 6 3.8 O=S(=O)(Nc1nccs1)c1cc(Cl)c(NCC23CCCN2CCC3)cc1F 10.1016/j.bmcl.2017.03.085
2142 3035 54 None -43 37 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
4920903 3035 54 None -43 37 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
502 3035 54 None -43 37 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
5775 3035 54 None -43 37 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
CHEMBL597 3035 54 None -43 37 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
DB00692 3035 54 None -43 37 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
1212 1624 45 None -27 66 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1624 45 None -27 66 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1624 45 None -27 66 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1624 45 None -27 66 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1624 45 None -27 66 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
11957541 1425 38 None -2 16 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
1229 1425 38 None -2 16 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
147 1425 38 None -2 16 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
170617 1425 38 None -2 16 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
CHEMBL6616 1425 38 None -2 16 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
1042 1544 20 None -7 17 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 1544 20 None -7 17 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 1544 20 None -7 17 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 1544 20 None -7 17 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 1544 20 None -7 17 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
44393215 66315 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 417 6 2 4 5.4 Cc1cc(NC(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL185376 66315 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 417 6 2 4 5.4 Cc1cc(NC(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
74538762 142997 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 419 6 0 4 4.2 O=C1OC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)CN1C1CCCC1 nan
CHEMBL3898995 142997 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 419 6 0 4 4.2 O=C1OC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)CN1C1CCCC1 nan
1599 2299 47 None -144 16 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
3955 2299 47 None -144 16 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
7215 2299 47 None -144 16 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
CHEMBL841 2299 47 None -144 16 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
DB00836 2299 47 None -144 16 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
165193 3126 60 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3126 60 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3126 60 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3126 60 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3126 60 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3126 60 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3126 60 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3126 60 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3126 60 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3126 60 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3126 60 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4209 3102 71 None -758 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
4893 3102 71 None -758 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
503 3102 71 None -758 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
5385 3102 71 None -758 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
CHEMBL2 3102 71 None -758 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
DB00457 3102 71 None -758 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
CHEMBL5079070 212822 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL None None None CC(C)N(C)CCc1cn(C)c2cccc(O)c12 10.1021/acsmedchemlett.1c00578
124087 1357 106 None -5 15 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1357 106 None -5 15 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1357 106 None -5 15 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1357 106 None -5 15 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1357 106 None -5 15 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
72198754 90435 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 443 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3ccc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
CHEMBL2392349 90435 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 443 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3ccc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
58438475 91827 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml500414n
CHEMBL2426677 91827 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml500414n
21138 97986 34 None -6 7 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
CHEMBL275742 97986 34 None -6 7 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
10389430 125417 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 458 5 1 5 4.3 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL364863 125417 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 458 5 1 5 4.3 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
1530 2142 44 None -19 21 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2142 44 None -19 21 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2142 44 None -19 21 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2142 44 None -19 21 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2142 44 None -19 21 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
5353853 17788 41 None -23 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 17788 41 None -23 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 17788 41 None -23 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
2600 3708 73 None -1 13 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3708 73 None -1 13 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3708 73 None -1 13 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3708 73 None -1 13 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3708 73 None -1 13 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
4211 57502 81 None -2 4 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
CHEMBL1670 57502 81 None -2 4 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
6761 67442 17 None -7 18 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67442 17 None -7 18 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
1588 2284 24 None -8 44 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -8 44 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -8 44 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -8 44 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -8 44 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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
206 2447 10 None -1 25 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/j.ejmech.2019.04.064
68848 2447 10 None -1 25 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/j.ejmech.2019.04.064
CHEMBL12314 2447 10 None -1 25 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/j.ejmech.2019.04.064
44516817 57343 4 None -4365 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT2B receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT2B receptor
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668584 57343 4 None -4365 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT2B receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT2B receptor
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
6075 149563 36 None -8 16 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 149563 36 None -8 16 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
5624 32459 12 None 5 10 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL1203324 32459 12 None 5 10 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL141343 32459 12 None 5 10 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
11694810 120015 0 None 1 3 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human 5-HT2B receptor expressed in HEK293-EBNA cells assessed as [3H]PI metabolism by by liquid scintillation countingInhibition of human 5-HT2B receptor expressed in HEK293-EBNA cells assessed as [3H]PI metabolism by by liquid scintillation counting
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3310123 120015 0 None 1 3 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human 5-HT2B receptor expressed in HEK293-EBNA cells assessed as [3H]PI metabolism by by liquid scintillation countingInhibition of human 5-HT2B receptor expressed in HEK293-EBNA cells assessed as [3H]PI metabolism by by liquid scintillation counting
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3545474 120015 0 None 1 3 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human 5-HT2B receptor expressed in HEK293-EBNA cells assessed as [3H]PI metabolism by by liquid scintillation countingInhibition of human 5-HT2B receptor expressed in HEK293-EBNA cells assessed as [3H]PI metabolism by by liquid scintillation counting
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
44592109 178499 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptorDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor
ChEMBL 343 6 0 5 4.4 CCCCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL471663 178499 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptorDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor
ChEMBL 343 6 0 5 4.4 CCCCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
169713 79736 17 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 309 3 2 2 2.6 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2NC1 10.1016/j.bmcl.2009.09.002
CHEMBL21343 79736 17 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 309 3 2 2 2.6 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2NC1 10.1016/j.bmcl.2009.09.002
4943 192804 100 None 1 2 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 178 2 1 1 3.6 CC(C)c1cccc(C(C)C)c1O nan
CHEMBL526 192804 100 None 1 2 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 178 2 1 1 3.6 CC(C)c1cccc(C(C)C)c1O nan
11500509 120057 0 None -3 3 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343670 120057 0 None -3 3 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3545812 120057 0 None -3 3 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
4189 205185 91 None -26 34 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205185 91 None -26 34 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205185 91 None -26 34 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
2683 102402 24 None -501 16 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102402 24 None -501 16 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102402 24 None -501 16 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
3598 187228 73 None -2 7 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
CHEMBL496 187228 73 None -2 7 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
135398745 2858 108 None -5 66 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2858 108 None -5 66 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2858 108 None -5 66 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2858 108 None -5 66 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
107715 199250 18 None -14 20 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 199250 18 None -14 20 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 199250 18 None -14 20 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
122196341 123741 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human 5HT2bBinding affinity to human 5HT2b
ChEMBL 422 5 1 3 6.0 O=c1ccc(-c2ccc(OCc3ccc4ccccc4n3)cc2)c(-c2ccc(F)cc2)[nH]1 10.1021/acs.jmedchem.5b01240
CHEMBL3634745 123741 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human 5HT2bBinding affinity to human 5HT2b
ChEMBL 422 5 1 3 6.0 O=c1ccc(-c2ccc(OCc3ccc4ccccc4n3)cc2)c(-c2ccc(F)cc2)[nH]1 10.1021/acs.jmedchem.5b01240
10531 1387 18 None -15 24 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 1387 18 None -15 24 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 1387 18 None -15 24 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 1387 18 None -15 24 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 1387 18 None -15 24 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
1836 2544 56 None -69 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 2544 56 None -69 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 2544 56 None -69 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 2544 56 None -69 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 2544 56 None -69 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
14049689 196756 8 None 20 2 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 1541 28 21 42 -12.4 CC(O)COC[C@H]1O[C@@H]2O[C@@H]3[C@@H](COCC(C)O)O[C@H](O[C@@H]4[C@@H](COCC(C)O)O[C@H](O[C@@H]5[C@@H](COCC(C)O)O[C@H](O[C@@H]6[C@@H](COCC(C)O)O[C@H](O[C@@H]7[C@@H](COCC(C)O)O[C@H](O[C@@H]8[C@@H](COCC(C)O)O[C@H](O[C@H]1[C@H](O)[C@H]2O)[C@H](O)[C@H]8O)[C@H](O)[C@H]7O)[C@H](O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)[C@H]4O)[C@H](O)[C@H]3O nan
CHEMBL577294 196756 8 None 20 2 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 1541 28 21 42 -12.4 CC(O)COC[C@H]1O[C@@H]2O[C@@H]3[C@@H](COCC(C)O)O[C@H](O[C@@H]4[C@@H](COCC(C)O)O[C@H](O[C@@H]5[C@@H](COCC(C)O)O[C@H](O[C@@H]6[C@@H](COCC(C)O)O[C@H](O[C@@H]7[C@@H](COCC(C)O)O[C@H](O[C@@H]8[C@@H](COCC(C)O)O[C@H](O[C@H]1[C@H](O)[C@H]2O)[C@H](O)[C@H]8O)[C@H](O)[C@H]7O)[C@H](O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)[C@H]4O)[C@H](O)[C@H]3O nan
72198756 90437 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 478 8 0 5 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3c(Cl)nc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
CHEMBL2392351 90437 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 478 8 0 5 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3c(Cl)nc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
1782 2472 81 None -3 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
241 2472 81 None -3 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
4168 2472 81 None -3 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
CHEMBL86 2472 81 None -3 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
DB01233 2472 81 None -3 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
72713752 103255 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 396 5 2 7 3.0 Cc1csc(C(C)(O)c2nnc(NC(=O)Cc3c(F)cccc3F)s2)n1 10.1021/jm4012033
CHEMBL3088176 103255 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 396 5 2 7 3.0 Cc1csc(C(C)(O)c2nnc(NC(=O)Cc3c(F)cccc3F)s2)n1 10.1021/jm4012033
90644511 111161 13 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 282 3 2 4 2.4 CNc1nc(Cc2ccccc2)nc2c1CCNC[C@@H]2C 10.1021/jm5003292
CHEMBL3286556 111161 13 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 282 3 2 4 2.4 CNc1nc(Cc2ccccc2)nc2c1CCNC[C@@H]2C 10.1021/jm5003292
2406 99925 84 None -27 12 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
CHEMBL290106 99925 84 None -27 12 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
2286 3122 48 None -5 30 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3122 48 None -5 30 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3122 48 None -5 30 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3122 48 None -5 30 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3122 48 None -5 30 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
3198 203792 73 None -30 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203792 73 None -30 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203792 73 None -30 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
135 2486 38 None -3 58 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2486 38 None -3 58 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2486 38 None -3 58 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2486 38 None -3 58 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2486 38 None -3 58 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
180 397 50 None -35 39 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 397 50 None -35 39 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 397 50 None -35 39 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 397 50 None -35 39 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 397 50 None -35 39 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
4595 176131 102 None 2 15 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O nan
CHEMBL46 176131 102 None 2 15 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O nan
11536843 114612 0 None 1 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343673 114612 0 None 1 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
1547484 925 70 None -8 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 925 70 None -8 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 925 70 None -8 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 925 70 None -8 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 925 70 None -8 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
102 4051 44 None -93 50 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
3659 4051 44 None -93 50 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
8969 4051 44 None -93 50 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
CHEMBL15245 4051 44 None -93 50 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
DB01392 4051 44 None -93 50 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
2477 732 54 None -13 29 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
36 732 54 None -13 29 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
437 732 54 None -13 29 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
CHEMBL49 732 54 None -13 29 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
DB00490 732 54 None -13 29 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
71499384 110648 36 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 448 8 1 5 4.5 COc1cc(/C=C/C(=O)NCCn2c(C(F)(F)F)cc3ccccc32)cc(OC)c1OC 10.1021/jm401431x
CHEMBL3264204 110648 36 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 448 8 1 5 4.5 COc1cc(/C=C/C(=O)NCCn2c(C(F)(F)F)cc3ccccc32)cc(OC)c1OC 10.1021/jm401431x
2105 2993 34 None -28 33 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 2993 34 None -28 33 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 2993 34 None -28 33 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 2993 34 None -28 33 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 2993 34 None -28 33 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
67406727 116677 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 525 6 1 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
CHEMBL3394201 116677 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 525 6 1 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
11957735 198328 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 350 4 1 5 4.0 CN(C)Cc1nc(-c2ccc(C(C)(C)C)cc2)n(-c2cccc(O)c2)n1 10.1016/j.bmc.2009.07.007
CHEMBL595449 198328 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 350 4 1 5 4.0 CN(C)Cc1nc(-c2ccc(C(C)(C)C)cc2)n(-c2cccc(O)c2)n1 10.1016/j.bmc.2009.07.007
2028 2919 77 None -40 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
359 2919 77 None -40 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634 2919 77 None -40 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
CHEMBL1231 2919 77 None -40 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
DB01062 2919 77 None -40 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
31101 719 39 None -26 36 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -26 36 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -26 36 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -26 36 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -26 36 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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
161 741 3 None 2 6 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
4284720 741 3 None 2 6 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
CHEMBL1255834 741 3 None 2 6 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
54764240 68511 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 242 1 1 2 2.7 CC/C=C1\C[C@H]2CNc3ccccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL1922539 68511 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 242 1 1 2 2.7 CC/C=C1\C[C@H]2CNc3ccccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL5085055 213163 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL None None None CCN(C)CCc1cn(C)c2cccc(O)c12 10.1021/acsmedchemlett.1c00578
4098 32274 24 None -14 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1255739 32274 24 None -14 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1411979 32274 24 None -14 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
54764241 68510 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 258 1 1 3 2.3 C/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL1922538 68510 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 258 1 1 3 2.3 C/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
5282379 193304 64 None 1 3 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C\C(=O)O)C(C)(C)CCC1 nan
CHEMBL547 193304 64 None 1 3 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C\C(=O)O)C(C)(C)CCC1 nan
146420029 184169 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 379 3 1 3 4.2 CN1CCC(=C(F)c2cccc(NC(=O)c3c(F)cc(F)cc3F)n2)CC1 10.1016/j.ejmech.2021.113782
CHEMBL4851044 184169 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 379 3 1 3 4.2 CN1CCC(=C(F)c2cccc(NC(=O)c3c(F)cc(F)cc3F)n2)CC1 10.1016/j.ejmech.2021.113782
3158 55959 21 None -389 20 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 55959 21 None -389 20 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
72197484 102008 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-lysergic acid from human recombinant 5HT-2B receptorDisplacement of [3H]-lysergic acid from human recombinant 5HT-2B receptor
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL2393243 102008 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-lysergic acid from human recombinant 5HT-2B receptorDisplacement of [3H]-lysergic acid from human recombinant 5HT-2B receptor
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL3040324 102008 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-lysergic acid from human recombinant 5HT-2B receptorDisplacement of [3H]-lysergic acid from human recombinant 5HT-2B receptor
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
277 1269 55 None -5 46 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1269 55 None -5 46 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1269 55 None -5 46 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1269 55 None -5 46 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1269 55 None -5 46 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
1305 508 10 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]LSD from human 5HT2B receptorDisplacement of [125I]LSD from human 5HT2B receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
9934033 508 10 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]LSD from human 5HT2B receptorDisplacement of [125I]LSD from human 5HT2B receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL182150 508 10 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]LSD from human 5HT2B receptorDisplacement of [125I]LSD from human 5HT2B receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
9861687 188600 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptorDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor
ChEMBL 315 4 0 5 3.7 CCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL511312 188600 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptorDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor
ChEMBL 315 4 0 5 3.7 CCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
2291 3123 52 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3123 52 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3123 52 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3123 52 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3123 52 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
176 394 63 None -1 31 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -1 31 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -1 31 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -1 31 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -1 31 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
657255 197396 29 None -9 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 197396 29 None -9 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
3952 1849 33 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5353646 1849 33 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5443 1849 33 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5702063 1849 33 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL1331786 1849 33 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL420 1849 33 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
24360 201644 101 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 348 1 1 6 2.1 CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3ccccc3nc2-1 nan
CHEMBL65 201644 101 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 348 1 1 6 2.1 CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3ccccc3nc2-1 nan
127048334 140057 0 None 13 3 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human 5-HT2B receptor by PDSP assayAntagonist activity at human 5-HT2B receptor by PDSP assay
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2ccccc2Cl)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3813796 140057 0 None 13 3 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human 5-HT2B receptor by PDSP assayAntagonist activity at human 5-HT2B receptor by PDSP assay
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2ccccc2Cl)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
10851262 40303 0 None 1 3 Rat 8.9 pKd = 8.9 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 293 1 1 3 3.7 Cc1coc2cc3c(cc12)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
CHEMBL148346 40303 0 None 1 3 Rat 8.9 pKd = 8.9 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 293 1 1 3 3.7 Cc1coc2cc3c(cc12)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
9972439 40355 0 None -1 3 Rat 8.0 pKd = 8 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 306 2 1 3 3.7 CCn1ccc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
CHEMBL148385 40355 0 None -1 3 Rat 8.0 pKd = 8 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 306 2 1 3 3.7 CCn1ccc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
10851406 118746 1 None -1 3 Rat 8.0 pKd = 8 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 295 1 1 3 3.9 O=C(Nc1cccnc1)N1CCc2cc3sccc3cc21 10.1021/jm960571v
CHEMBL343666 118746 1 None -1 3 Rat 8.0 pKd = 8 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 295 1 1 3 3.9 O=C(Nc1cccnc1)N1CCc2cc3sccc3cc21 10.1021/jm960571v
141 1394 32 None -11 22 Rat 6.0 pKd = 6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm00343a013
6089 1394 32 None -11 22 Rat 6.0 pKd = 6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm00343a013
CHEMBL12420 1394 32 None -11 22 Rat 6.0 pKd = 6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm00343a013
DB01488 1394 32 None -11 22 Rat 6.0 pKd = 6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm00343a013
12281266 31601 4 None - 1 Rat 7.0 pKd = 7.0 Binding
Compound was tested for serotonin receptor affinity by the displacement of [3H]- -5-HT binding to rat fundus membranes.Compound was tested for serotonin receptor affinity by the displacement of [3H]- -5-HT binding to rat fundus membranes.
ChEMBL 187 3 0 1 3.7 CC(C)CCn1ccc2ccccc21 10.1021/jm00367a008
CHEMBL140663 31601 4 None - 1 Rat 7.0 pKd = 7.0 Binding
Compound was tested for serotonin receptor affinity by the displacement of [3H]- -5-HT binding to rat fundus membranes.Compound was tested for serotonin receptor affinity by the displacement of [3H]- -5-HT binding to rat fundus membranes.
ChEMBL 187 3 0 1 3.7 CC(C)CCn1ccc2ccccc21 10.1021/jm00367a008
6088 119324 54 None - 1 Rat 6.0 pKd = 6.0 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 174 3 2 1 1.9 CNCCc1c[nH]c2ccccc12 10.1021/jm00343a013
CHEMBL348588 119324 54 None - 1 Rat 6.0 pKd = 6.0 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 174 3 2 1 1.9 CNCCc1c[nH]c2ccccc12 10.1021/jm00343a013
10637557 36027 0 None 5 3 Rat 7.9 pKd = 7.9 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 294 1 1 3 2.7 CN1CCc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
CHEMBL144567 36027 0 None 5 3 Rat 7.9 pKd = 7.9 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 294 1 1 3 2.7 CN1CCc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
152234 55717 20 None - 1 Rat 5.9 pKd = 5.9 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 165 3 1 2 1.6 COc1cccc(CC(C)N)c1 10.1021/jm00144a009
CHEMBL16247 55717 20 None - 1 Rat 5.9 pKd = 5.9 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 165 3 1 2 1.6 COc1cccc(CC(C)N)c1 10.1021/jm00144a009
44359526 116118 1 None - 1 Rat 6.9 pKd = 6.9 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 217 4 0 2 3.7 COc1ccc2c(ccn2CCC(C)C)c1 10.1021/jm00367a008
CHEMBL336928 116118 1 None - 1 Rat 6.9 pKd = 6.9 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 217 4 0 2 3.7 COc1ccc2c(ccn2CCC(C)C)c1 10.1021/jm00367a008
44359525 28643 1 None - 1 Rat 6.9 pKd = 6.9 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 201 3 0 1 4.0 Cc1ccc2ccn(CCC(C)C)c2c1 10.1021/jm00367a008
CHEMBL137933 28643 1 None - 1 Rat 6.9 pKd = 6.9 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 201 3 0 1 4.0 Cc1ccc2ccn(CCC(C)C)c2c1 10.1021/jm00367a008
805647 30580 11 None - 1 Rat 6.9 pKd = 6.9 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 189 3 0 3 1.6 CN(C)CCn1cnc2ccccc21 10.1021/jm00367a008
CHEMBL139655 30580 11 None - 1 Rat 6.9 pKd = 6.9 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 189 3 0 3 1.6 CN(C)CCn1cnc2ccccc21 10.1021/jm00367a008
143435 99220 4 None - 1 Rat 5.9 pKd = 5.9 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(CC(C)N)cc1OC 10.1021/jm00144a009
CHEMBL284589 99220 4 None - 1 Rat 5.9 pKd = 5.9 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(CC(C)N)cc1OC 10.1021/jm00144a009
62787 204457 17 None -3 10 Rat 6.8 pKd = 6.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 10.1021/jm00144a009
CHEMBL8642 204457 17 None -3 10 Rat 6.8 pKd = 6.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 10.1021/jm00144a009
9904139 106497 0 None 1 5 Rat 7.8 pKd = 7.8 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 292 1 1 3 3.2 Cn1ccc2c3c(ccc21)N(C(=O)Nc1cccnc1)CC3 10.1021/jm960571v
CHEMBL315223 106497 0 None 1 5 Rat 7.8 pKd = 7.8 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 292 1 1 3 3.2 Cn1ccc2c3c(ccc21)N(C(=O)Nc1cccnc1)CC3 10.1021/jm960571v
31014 204165 16 None 2 4 Rat 6.8 pKd = 6.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1cc(OC)c(OC)cc1CC(C)N 10.1021/jm00144a009
CHEMBL8389 204165 16 None 2 4 Rat 6.8 pKd = 6.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1cc(OC)c(OC)cc1CC(C)N 10.1021/jm00144a009
144891 106890 8 None - 1 Rat 5.8 pKd = 5.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 241 5 1 4 2.3 COc1cc(OC)c(SC)cc1CC(C)N 10.1021/jm00144a009
CHEMBL31787 106890 8 None - 1 Rat 5.8 pKd = 5.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 241 5 1 4 2.3 COc1cc(OC)c(SC)cc1CC(C)N 10.1021/jm00144a009
9904139 106497 0 None 1 5 Rat 7.8 pKd = 7.8 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 292 1 1 3 3.2 Cn1ccc2c3c(ccc21)N(C(=O)Nc1cccnc1)CC3 10.1021/jm00014a004
CHEMBL315223 106497 0 None 1 5 Rat 7.8 pKd = 7.8 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 292 1 1 3 3.2 Cn1ccc2c3c(ccc21)N(C(=O)Nc1cccnc1)CC3 10.1021/jm00014a004
141685 106552 4 None - 1 Rat 5.8 pKd = 5.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(CC(C)N)cc1OC 10.1021/jm00144a009
CHEMBL31557 106552 4 None - 1 Rat 5.8 pKd = 5.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(CC(C)N)cc1OC 10.1021/jm00144a009
11806221 119704 1 None - 1 Rat 6.7 pKd = 6.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 220 4 1 3 2.2 COc1ccc2c(c1)C(CCN(C)C)CN2 10.1021/jm00343a013
CHEMBL352140 119704 1 None - 1 Rat 6.7 pKd = 6.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 220 4 1 3 2.2 COc1ccc2c(c1)C(CCN(C)C)CN2 10.1021/jm00343a013
10757038 118716 0 None 1 3 Rat 7.7 pKd = 7.7 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 306 1 1 3 3.5 Cc1cc2cc3c(cc2n1C)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
CHEMBL343455 118716 0 None 1 3 Rat 7.7 pKd = 7.7 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 306 1 1 3 3.5 Cc1cc2cc3c(cc2n1C)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
10690384 120430 0 None -3 2 Rat 6.7 pKd = 6.7 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 368 3 1 3 4.7 O=C(Nc1cccnc1)N1CCc2cc3c(ccn3Cc3ccccc3)cc21 10.1021/jm960571v
CHEMBL356146 120430 0 None -3 2 Rat 6.7 pKd = 6.7 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 368 3 1 3 4.7 O=C(Nc1cccnc1)N1CCc2cc3c(ccn3Cc3ccccc3)cc21 10.1021/jm960571v
44359444 28901 0 None - 1 Rat 7.7 pKd = 7.7 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 217 4 0 2 3.7 COc1ccc2ccn(CCC(C)C)c2c1 10.1021/jm00367a008
CHEMBL138144 28901 0 None - 1 Rat 7.7 pKd = 7.7 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 217 4 0 2 3.7 COc1ccc2ccn(CCC(C)C)c2c1 10.1021/jm00367a008
12655251 118791 52 None - 1 Rat 5.7 pKd = 5.7 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 162 2 2 2 1.5 NCCC1CNc2ccccc21 10.1021/jm00367a008
CHEMBL344028 118791 52 None - 1 Rat 5.7 pKd = 5.7 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 162 2 2 2 1.5 NCCC1CNc2ccccc21 10.1021/jm00367a008
11074217 52512 4 None - 1 Rat 5.7 pKd = 5.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 190 3 1 2 2.1 CN(C)CCC1CNc2ccccc21 10.1021/jm00343a013
CHEMBL159503 52512 4 None - 1 Rat 5.7 pKd = 5.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 190 3 1 2 2.1 CN(C)CCC1CNc2ccccc21 10.1021/jm00343a013
547452 54491 2 None - 1 Rat 5.7 pKd = 5.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 187 3 0 1 2.6 CN(C)CCC1=CCc2ccccc21 10.1021/jm00343a013
CHEMBL161241 54491 2 None - 1 Rat 5.7 pKd = 5.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 187 3 0 1 2.6 CN(C)CCC1=CCc2ccccc21 10.1021/jm00343a013
12451869 54883 5 None - 1 Rat 5.7 pKd = 5.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 175 3 1 1 2.3 CNCCC1CCc2ccccc21 10.1021/jm00343a013
CHEMBL161751 54883 5 None - 1 Rat 5.7 pKd = 5.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 175 3 1 1 2.3 CNCCC1CCc2ccccc21 10.1021/jm00343a013
144889 98852 6 None - 1 Rat 5.6 pKd = 5.6 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(OC)c(CC(C)N)cc1C 10.1021/jm00144a009
CHEMBL282183 98852 6 None - 1 Rat 5.6 pKd = 5.6 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(OC)c(CC(C)N)cc1C 10.1021/jm00144a009
34677 101736 79 None - 1 Rat 5.6 pKd = 5.6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 147 0 1 1 1.5 NC1CCc2ccccc2C1 10.1021/jm00343a013
CHEMBL30294 101736 79 None - 1 Rat 5.6 pKd = 5.6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 147 0 1 1 1.5 NC1CCc2ccccc2C1 10.1021/jm00343a013
141047 98934 15 None 1 3 Rat 5.6 pKd = 5.6 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1ccc(CC(C)N)c(OC)c1 10.1021/jm00144a009
CHEMBL282734 98934 15 None 1 3 Rat 5.6 pKd = 5.6 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1ccc(CC(C)N)c(OC)c1 10.1021/jm00144a009
31016 101804 12 None -11 5 Rat 5.6 pKd = 5.6 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1cc(CC(C)N)cc(OC)c1OC 10.1021/jm00144a009
CHEMBL30336 101804 12 None -11 5 Rat 5.6 pKd = 5.6 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1cc(CC(C)N)cc(OC)c1OC 10.1021/jm00144a009
15011362 52351 20 None - 1 Rat 5.6 pKd = 5.6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 161 2 1 1 2.1 NCCC1CCc2ccccc21 10.1021/jm00343a013
CHEMBL159346 52351 20 None - 1 Rat 5.6 pKd = 5.6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 161 2 1 1 2.1 NCCC1CCc2ccccc21 10.1021/jm00343a013
744368 164366 17 None - 1 Rat 6.6 pKd = 6.6 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 190 3 0 2 1.6 CN(C)CCN1CCc2ccccc21 10.1021/jm00367a008
CHEMBL422471 164366 17 None - 1 Rat 6.6 pKd = 6.6 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 190 3 0 2 1.6 CN(C)CCN1CCc2ccccc21 10.1021/jm00367a008
159755 56785 57 None - 1 Rat 5.5 pKd = 5.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 165 3 1 2 1.6 COc1ccccc1CC(C)N 10.1021/jm00144a009
CHEMBL16451 56785 57 None - 1 Rat 5.5 pKd = 5.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 165 3 1 2 1.6 COc1ccccc1CC(C)N 10.1021/jm00144a009
91255 98641 9 None 1 2 Rat 5.5 pKd = 5.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1cccc(CC(C)N)c1OC 10.1021/jm00144a009
CHEMBL280855 98641 9 None 1 2 Rat 5.5 pKd = 5.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1cccc(CC(C)N)c1OC 10.1021/jm00144a009
189 3423 31 None 2 18 Rat 8.5 pKd = 8.5 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm960571v
5163 3423 31 None 2 18 Rat 8.5 pKd = 8.5 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm960571v
CHEMBL297784 3423 31 None 2 18 Rat 8.5 pKd = 8.5 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm960571v
189 3423 31 None 2 18 Rat 8.5 pKd = 8.5 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm00014a004
5163 3423 31 None 2 18 Rat 8.5 pKd = 8.5 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm00014a004
CHEMBL297784 3423 31 None 2 18 Rat 8.5 pKd = 8.5 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm00014a004
10683987 120752 1 None 3 3 Rat 7.5 pKd = 7.5 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 278 1 2 2 3.2 O=C(Nc1cccnc1)N1CCc2cc3[nH]ccc3cc21 10.1021/jm960571v
CHEMBL357870 120752 1 None 3 3 Rat 7.5 pKd = 7.5 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 278 1 2 2 3.2 O=C(Nc1cccnc1)N1CCc2cc3[nH]ccc3cc21 10.1021/jm960571v
1614 201951 22 None -2 10 Rat 6.5 pKd = 6.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 10.1021/jm00144a009
CHEMBL6731 201951 22 None -2 10 Rat 6.5 pKd = 6.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 10.1021/jm00144a009
8423 98223 26 None - 1 Rat 5.5 pKd = 5.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1ccc(CC(C)N)cc1OC 10.1021/jm00144a009
CHEMBL277540 98223 26 None - 1 Rat 5.5 pKd = 5.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1ccc(CC(C)N)cc1OC 10.1021/jm00144a009
126769 204313 35 None -1 5 Rat 7.4 pKd = 7.4 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1021/jm00014a004
CHEMBL536255 204313 35 None -1 5 Rat 7.4 pKd = 7.4 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1021/jm00014a004
CHEMBL85194 204313 35 None -1 5 Rat 7.4 pKd = 7.4 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1021/jm00014a004
12451869 54883 5 None - 1 Rat 5.4 pKd = 5.4 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 175 3 1 1 2.3 CNCCC1CCc2ccccc21 10.1021/jm00343a013
CHEMBL161751 54883 5 None - 1 Rat 5.4 pKd = 5.4 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 175 3 1 1 2.3 CNCCC1CCc2ccccc21 10.1021/jm00343a013
155 718 20 None -10 13 Rat 7.4 pKd = 7.4 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 10.1021/jm00144a009
163 718 20 None -10 13 Rat 7.4 pKd = 7.4 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 10.1021/jm00144a009
62065 718 20 None -10 13 Rat 7.4 pKd = 7.4 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 10.1021/jm00144a009
CHEMBL6607 718 20 None -10 13 Rat 7.4 pKd = 7.4 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 10.1021/jm00144a009
DB01484 718 20 None -10 13 Rat 7.4 pKd = 7.4 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 10.1021/jm00144a009
44375004 52711 1 None - 1 Rat 5.3 pKd = 5.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 189 3 0 1 2.7 CN(C)CCC1CCc2ccccc21 10.1021/jm00343a013
CHEMBL159689 52711 1 None - 1 Rat 5.3 pKd = 5.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 189 3 0 1 2.7 CN(C)CCC1CCc2ccccc21 10.1021/jm00343a013
44359477 115921 0 None - 1 Rat 7.3 pKd = 7.3 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 201 3 0 1 4.0 Cc1cccc2ccn(CCC(C)C)c12 10.1021/jm00367a008
CHEMBL336042 115921 0 None - 1 Rat 7.3 pKd = 7.3 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 201 3 0 1 4.0 Cc1cccc2ccn(CCC(C)C)c12 10.1021/jm00367a008
77042 187763 52 None - 1 Rat 5.3 pKd = 5.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 177 4 0 2 1.8 CN(C)CCC(=O)c1ccccc1 10.1021/jm00343a013
CHEMBL50115 187763 52 None - 1 Rat 5.3 pKd = 5.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 177 4 0 2 1.8 CN(C)CCC(=O)c1ccccc1 10.1021/jm00343a013
31015 117898 12 None - 1 Rat 6.3 pKd = 6.3 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1cc(OC)c(CC(C)N)c(OC)c1 10.1021/jm00144a009
CHEMBL34108 117898 12 None - 1 Rat 6.3 pKd = 6.3 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1cc(OC)c(CC(C)N)c(OC)c1 10.1021/jm00144a009
10335310 204275 0 None 75 2 Rat 7.3 pKd = 7.3 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 306 1 1 3 3.6 Cn1ccc2cc3c(cc21)CCCN3C(=O)Nc1cccnc1 10.1021/jm00014a004
CHEMBL84888 204275 0 None 75 2 Rat 7.3 pKd = 7.3 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 306 1 1 3 3.6 Cn1ccc2cc3c(cc21)CCCN3C(=O)Nc1cccnc1 10.1021/jm00014a004
33984 29413 37 None - 1 Rat 6.3 pKd = 6.3 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 192 5 0 2 2.1 CCN(CCN(C)C)c1ccccc1 10.1021/jm00367a008
CHEMBL138604 29413 37 None - 1 Rat 6.3 pKd = 6.3 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 192 5 0 2 2.1 CCN(CCN(C)C)c1ccccc1 10.1021/jm00367a008
1150 3805 116 None -8 25 Rat 6.3 pKd = 6.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm00343a013
125 3805 116 None -8 25 Rat 6.3 pKd = 6.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm00343a013
CHEMBL6640 3805 116 None -8 25 Rat 6.3 pKd = 6.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm00343a013
DB08653 3805 116 None -8 25 Rat 6.3 pKd = 6.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm00343a013
3007 155132 25 None -1 6 Rat 5.3 pKd = 5.3 Binding
Affinity against serotonergic receptor in the isolated rat stomach fundusAffinity against serotonergic receptor in the isolated rat stomach fundus
ChEMBL 135 2 1 1 1.6 CC(N)Cc1ccccc1 10.1021/jm00144a009
CHEMBL405 155132 25 None -1 6 Rat 5.3 pKd = 5.3 Binding
Affinity against serotonergic receptor in the isolated rat stomach fundusAffinity against serotonergic receptor in the isolated rat stomach fundus
ChEMBL 135 2 1 1 1.6 CC(N)Cc1ccccc1 10.1021/jm00144a009
127035062 135915 0 None -4 19 Human 6.3 pKd = 6.3 Binding
Non-competitive antagonist activity at human recombinant 5-HT2B receptor stably expressed in HEK cell membrane by schild plot methodNon-competitive antagonist activity at human recombinant 5-HT2B receptor stably expressed in HEK cell membrane by schild plot method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 135915 0 None -4 19 Human 6.3 pKd = 6.3 Binding
Non-competitive antagonist activity at human recombinant 5-HT2B receptor stably expressed in HEK cell membrane by schild plot methodNon-competitive antagonist activity at human recombinant 5-HT2B receptor stably expressed in HEK cell membrane by schild plot method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
10591799 39695 0 None 1 3 Rat 8.2 pKd = 8.2 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 320 2 1 3 4.2 CC(C)n1ccc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
CHEMBL147820 39695 0 None 1 3 Rat 8.2 pKd = 8.2 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 320 2 1 3 4.2 CC(C)n1ccc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
44363813 40304 0 None 19 3 Rat 8.2 pKd = 8.2 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 305 1 1 2 4.1 Cc1cn(C)c2cc3c(cc12)N(C(=O)Nc1ccccc1)CC3 10.1021/jm960571v
CHEMBL148347 40304 0 None 19 3 Rat 8.2 pKd = 8.2 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 305 1 1 2 4.1 Cc1cn(C)c2cc3c(cc12)N(C(=O)Nc1ccccc1)CC3 10.1021/jm960571v
10335309 204316 0 None - 1 Rat 7.2 pKd = 7.2 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 306 1 1 3 3.6 Cn1ccc2c3c(ccc21)N(C(=O)Nc1cccnc1)CCC3 10.1021/jm00014a004
CHEMBL85247 204316 0 None - 1 Rat 7.2 pKd = 7.2 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 306 1 1 3 3.6 Cn1ccc2c3c(ccc21)N(C(=O)Nc1cccnc1)CCC3 10.1021/jm00014a004
31721 98353 37 None - 1 Rat 5.2 pKd = 5.2 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 165 3 1 2 1.6 COc1ccc(CC(C)N)cc1 10.1021/jm00144a009
CHEMBL278663 98353 37 None - 1 Rat 5.2 pKd = 5.2 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 165 3 1 2 1.6 COc1ccc(CC(C)N)cc1 10.1021/jm00144a009
10495940 78433 0 None 1 3 Rat 8.1 pKd = 8.1 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 320 3 1 3 4.0 CCCn1ccc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
CHEMBL2112859 78433 0 None 1 3 Rat 8.1 pKd = 8.1 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 320 3 1 3 4.0 CCCn1ccc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
44359524 28641 1 None - 1 Rat 7.1 pKd = 7.1 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 201 3 0 1 4.0 Cc1cccc2c1ccn2CCC(C)C 10.1021/jm00367a008
CHEMBL137932 28641 1 None - 1 Rat 7.1 pKd = 7.1 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 201 3 0 1 4.0 Cc1cccc2c1ccn2CCC(C)C 10.1021/jm00367a008
164 1427 17 None -3 10 Rat 7.1 pKd = 7.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00144a009
85875 1427 17 None -3 10 Rat 7.1 pKd = 7.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00144a009
CHEMBL8600 1427 17 None -3 10 Rat 7.1 pKd = 7.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00144a009
DB01528 1427 17 None -3 10 Rat 7.1 pKd = 7.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00144a009
141048 102383 6 None - 1 Rat 5.1 pKd = 5.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1cccc(OC)c1CC(C)N 10.1021/jm00144a009
CHEMBL30577 102383 6 None - 1 Rat 5.1 pKd = 5.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1cccc(OC)c1CC(C)N 10.1021/jm00144a009
25187 99822 25 None - 1 Rat 5.1 pKd = 5.1 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 163 4 0 1 2.2 CN(C)CCCc1ccccc1 10.1021/jm00343a013
CHEMBL289199 99822 25 None - 1 Rat 5.1 pKd = 5.1 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 163 4 0 1 2.2 CN(C)CCCc1ccccc1 10.1021/jm00343a013
44359556 118910 0 None - 1 Rat 7.1 pKd = 7.1 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 220 4 1 3 2.2 COc1ccc2c(c1)NCC2CCN(C)C 10.1021/jm00367a008
CHEMBL344878 118910 0 None - 1 Rat 7.1 pKd = 7.1 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 220 4 1 3 2.2 COc1ccc2c(c1)NCC2CCN(C)C 10.1021/jm00367a008
145 140 48 None -16 30 Rat 7.1 pKd = 7.1 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00343a013
1832 140 48 None -16 30 Rat 7.1 pKd = 7.1 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00343a013
CHEMBL7257 140 48 None -16 30 Rat 7.1 pKd = 7.1 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00343a013
DB14010 140 48 None -16 30 Rat 7.1 pKd = 7.1 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00343a013
31012 102630 15 None - 1 Rat 5.1 pKd = 5.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1ccc(CC(C)N)c(OC)c1OC 10.1021/jm00144a009
CHEMBL30777 102630 15 None - 1 Rat 5.1 pKd = 5.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1ccc(CC(C)N)c(OC)c1OC 10.1021/jm00144a009
81206 29422 32 None - 1 Rat 6.0 pKd = 6.0 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 164 4 1 2 1.7 CN(C)CCNc1ccccc1 10.1021/jm00367a008
CHEMBL138614 29422 32 None - 1 Rat 6.0 pKd = 6.0 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 164 4 1 2 1.7 CN(C)CCNc1ccccc1 10.1021/jm00367a008
81206 29422 32 None - 1 Rat 6.0 pKd = 6.0 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 164 4 1 2 1.7 CN(C)CCNc1ccccc1 10.1021/jm00343a013
CHEMBL138614 29422 32 None - 1 Rat 6.0 pKd = 6.0 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 164 4 1 2 1.7 CN(C)CCNc1ccccc1 10.1021/jm00343a013
11666595 120008 0 None 301 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1c(Cl)cccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310115 120008 0 None 301 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1c(Cl)cccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545467 120008 0 None 301 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1c(Cl)cccc1-2 10.1016/j.bmc.2014.05.027
9839057 41138 3 None -9 4 Human 9.7 pKi = 9.7 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 293 2 1 3 3.8 CC(N)Cc1c2ccoc2c(Br)c2ccoc12 10.1021/jm9803525
CHEMBL149024 41138 3 None -9 4 Human 9.7 pKi = 9.7 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 293 2 1 3 3.8 CC(N)Cc1c2ccoc2c(Br)c2ccoc12 10.1021/jm9803525
9953185 205875 2 None 97 3 Human 9.7 pKi = 9.7 Binding
Binding affinity to human 5-HT2B assessed as inhibition constantBinding affinity to human 5-HT2B assessed as inhibition constant
ChEMBL 370 4 2 3 4.6 COc1ccc(CC2NCCc3c2[nH]c2ccc(C)cc32)c(Cl)c1OC 10.1021/acs.jmedchem.2c00633
CHEMBL95121 205875 2 None 97 3 Human 9.7 pKi = 9.7 Binding
Binding affinity to human 5-HT2B assessed as inhibition constantBinding affinity to human 5-HT2B assessed as inhibition constant
ChEMBL 370 4 2 3 4.6 COc1ccc(CC2NCCc3c2[nH]c2ccc(C)cc32)c(Cl)c1OC 10.1021/acs.jmedchem.2c00633
133 2450 48 None -2 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2450 48 None -2 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2450 48 None -2 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2450 48 None -2 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2450 48 None -2 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
188 3327 73 None -1 6 Human 9.5 pKi = 9.5 Binding
Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2B (unknown origin) assessed as inhibition constant
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1021/acs.jmedchem.2c00633
196968 3327 73 None -1 6 Human 9.5 pKi = 9.5 Binding
Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2B (unknown origin) assessed as inhibition constant
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1021/acs.jmedchem.2c00633
CHEMBL473186 3327 73 None -1 6 Human 9.5 pKi = 9.5 Binding
Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2B (unknown origin) assessed as inhibition constant
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1021/acs.jmedchem.2c00633
70772974 190883 6 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human 5-HT2B assessed as inhibition constant in microplate beta scintillation counter analysisBinding affinity to human 5-HT2B assessed as inhibition constant in microplate beta scintillation counter analysis
ChEMBL 369 3 2 3 3.8 Cc1c(C(=O)N2CCC(c3ncc[nH]3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c00633
CHEMBL5193649 190883 6 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human 5-HT2B assessed as inhibition constant in microplate beta scintillation counter analysisBinding affinity to human 5-HT2B assessed as inhibition constant in microplate beta scintillation counter analysis
ChEMBL 369 3 2 3 3.8 Cc1c(C(=O)N2CCC(c3ncc[nH]3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c00633
134 2468 19 None -2 68 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 2468 19 None -2 68 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 2468 19 None -2 68 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 2468 19 None -2 68 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 2468 19 None -2 68 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
242 467 117 None -1 52 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
34 467 117 None -1 52 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
60795 467 117 None -1 52 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
CHEMBL1112 467 117 None -1 52 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
DB01238 467 117 None -1 52 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
11393666 192374 0 None 1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 192374 0 None 1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 192374 0 None 1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
11978813 712 72 None -2 24 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1016/j.ejmech.2019.111736
5014 712 72 None -2 24 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1016/j.ejmech.2019.111736
7672 712 72 None -2 24 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1016/j.ejmech.2019.111736
CHEMBL2105760 712 72 None -2 24 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1016/j.ejmech.2019.111736
DB09128 712 72 None -2 24 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1016/j.ejmech.2019.111736
11465618 101913 18 None -1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 101913 18 None -1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL5191141 101913 18 None -1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
23151734 103468 0 None 467 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 265 1 2 2 1.3 NC(N)=NC(=O)c1ccc2c(c1)C(=O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092758 103468 0 None 467 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 265 1 2 2 1.3 NC(N)=NC(=O)c1ccc2c(c1)C(=O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
11687730 120061 0 None 9 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 277 1 2 1 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343668 120061 0 None 9 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 277 1 2 1 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3545816 120061 0 None 9 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 277 1 2 1 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
71528206 86529 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 314 3 0 4 2.8 COC(OC)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323581 86529 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 314 3 0 4 2.8 COC(OC)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
56597938 3865 1 None 2 9 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
7651 3865 1 None 2 9 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
CHEMBL2165126 3865 1 None 2 9 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
56597090 81557 0 None -1 5 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 434 7 0 4 6.6 Clc1cccc(C2CCN(CCCCOc3ccc4scnc4c3)CC2)c1Cl 10.1021/jm300603y
CHEMBL2165137 81557 0 None -1 5 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 434 7 0 4 6.6 Clc1cccc(C2CCN(CCCCOc3ccc4scnc4c3)CC2)c1Cl 10.1021/jm300603y
56597938 3865 1 None 2 9 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7651 3865 1 None 2 9 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165126 3865 1 None 2 9 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
118706290 120009 0 None 128 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.5 Cc1cccc2c1C(O)c1cc(C(=O)N=C(N)N)ccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310116 120009 0 None 128 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.5 Cc1cccc2c1C(O)c1cc(C(=O)N=C(N)N)ccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545468 120009 0 None 128 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.5 Cc1cccc2c1C(O)c1cc(C(=O)N=C(N)N)ccc1-2 10.1016/j.bmc.2014.05.027
118706734 120002 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 309 2 3 2 1.9 CCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2(C)O 10.1016/j.bmc.2014.05.027
CHEMBL3310714 120002 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 309 2 3 2 1.9 CCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2(C)O 10.1016/j.bmc.2014.05.027
CHEMBL3545444 120002 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 309 2 3 2 1.9 CCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2(C)O 10.1016/j.bmc.2014.05.027
150 2463 18 None 1 16 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
1764 2463 18 None 1 16 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
8226 2463 18 None 1 16 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
CHEMBL1201356 2463 18 None 1 16 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
DB00353 2463 18 None 1 16 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
118706282 120006 0 None 17 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.5 Cc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
CHEMBL3310111 120006 0 None 17 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.5 Cc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
CHEMBL3545465 120006 0 None 17 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.5 Cc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
118706299 120013 0 None 64 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 269 1 3 2 2.3 N=C(N)NC(=O)c1ccc2c(c1)C(F)c1ccccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310121 120013 0 None 64 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 269 1 3 2 2.3 N=C(N)NC(=O)c1ccc2c(c1)C(F)c1ccccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545472 120013 0 None 64 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 269 1 3 2 2.3 N=C(N)NC(=O)c1ccc2c(c1)C(F)c1ccccc1-2 10.1016/j.bmc.2014.05.027
118706284 120000 0 None 31 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 285 1 3 2 1.3 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(F)c1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310112 120000 0 None 31 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 285 1 3 2 1.3 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(F)c1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545440 120000 0 None 31 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 285 1 3 2 1.3 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(F)c1-2 10.1016/j.bmc.2014.05.027
150 2463 18 None 1 16 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 2463 18 None 1 16 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 2463 18 None 1 16 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 2463 18 None 1 16 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 2463 18 None 1 16 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
71528205 86528 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 368 5 1 4 2.2 CN(C)CCCNC(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323580 86528 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 368 5 1 4 2.2 CN(C)CCCNC(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
71528204 86527 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 439 6 1 5 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323579 86527 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 439 6 1 5 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
11358099 179815 0 None 3 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 285 3 1 4 2.8 COc1ccc(-c2c3c(nn2C(C)C)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4752099 179815 0 None 3 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 285 3 1 4 2.8 COc1ccc(-c2c3c(nn2C(C)C)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
11460460 181770 0 None -1 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 289 2 1 3 3.5 CC(C)n1nc2c(c1-c1ccc(Cl)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4784845 181770 0 None -1 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 289 2 1 3 3.5 CC(C)n1nc2c(c1-c1ccc(Cl)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
9954003 71341 18 None -1 9 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 422 5 2 4 3.8 C[C@H]1Oc2c(cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)NC1=O 10.1021/jm070516u
CHEMBL196514 71341 18 None -1 9 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 422 5 2 4 3.8 C[C@H]1Oc2c(cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)NC1=O 10.1021/jm070516u
16062782 97371 0 None 2 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 307 2 1 3 3.8 Cc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL272082 97371 0 None 2 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 307 2 1 3 3.8 Cc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
59757163 105848 0 None 218 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1cccc2c1Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092760 105848 0 None 218 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1cccc2c1Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3139189 105848 0 None 218 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1cccc2c1Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
118706732 120003 0 None 3 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 295 1 3 2 1.6 Cc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2(C)O 10.1016/j.bmc.2014.05.027
CHEMBL3310713 120003 0 None 3 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 295 1 3 2 1.6 Cc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2(C)O 10.1016/j.bmc.2014.05.027
CHEMBL3545445 120003 0 None 3 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 295 1 3 2 1.6 Cc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2(C)O 10.1016/j.bmc.2014.05.027
56593482 3866 1 None 1 9 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7650 3866 1 None 1 9 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165119 3866 1 None 1 9 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
10568771 102303 2 None -5 6 Human 8.9 pKi = 8.9 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligand
ChEMBL 297 2 1 3 2.2 C[C@@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm980076u
CHEMBL305275 102303 2 None -5 6 Human 8.9 pKi = 8.9 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligand
ChEMBL 297 2 1 3 2.2 C[C@@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm980076u
CHEMBL6710 102303 2 None -5 6 Human 8.9 pKi = 8.9 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligand
ChEMBL 297 2 1 3 2.2 C[C@@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm980076u
242 467 117 None -1 52 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
34 467 117 None -1 52 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
60795 467 117 None -1 52 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
CHEMBL1112 467 117 None -1 52 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
DB01238 467 117 None -1 52 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
11658860 2302 47 None -1 3 Human 8.9 pKi = 8.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2012.10.091
2941 2302 47 None -1 3 Human 8.9 pKi = 8.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2012.10.091
4374 2302 47 None -1 3 Human 8.9 pKi = 8.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2012.10.091
CHEMBL360328 2302 47 None -1 3 Human 8.9 pKi = 8.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2012.10.091
DB04871 2302 47 None -1 3 Human 8.9 pKi = 8.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2012.10.091
37 764 56 None 1 17 Human 8.9 pKi = 8.9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1021/ml3003814
460 764 56 None 1 17 Human 8.9 pKi = 8.9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1021/ml3003814
54746 764 56 None 1 17 Human 8.9 pKi = 8.9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1021/ml3003814
CHEMBL1201087 764 56 None 1 17 Human 8.9 pKi = 8.9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1021/ml3003814
DB00248 764 56 None 1 17 Human 8.9 pKi = 8.9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1021/ml3003814
242 467 117 None -1 52 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
34 467 117 None -1 52 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
60795 467 117 None -1 52 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL1112 467 117 None -1 52 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
DB01238 467 117 None -1 52 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
118706278 119999 0 None 26 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(Cl)c1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310109 119999 0 None 26 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(Cl)c1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545439 119999 0 None 26 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(Cl)c1-2 10.1016/j.bmc.2014.05.027
2865 4064 67 None -12 54 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
59 4064 67 None -12 54 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
60854 4064 67 None -12 54 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
CHEMBL708 4064 67 None -12 54 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
DB00246 4064 67 None -12 54 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
9888211 21201 9 None -1 10 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
CHEMBL131495 21201 9 None -1 10 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
10568771 102303 2 None -5 6 Human 8.8 pKi = 8.8 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 297 2 1 3 2.2 C[C@@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm980076u
CHEMBL305275 102303 2 None -5 6 Human 8.8 pKi = 8.8 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 297 2 1 3 2.2 C[C@@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm980076u
CHEMBL6710 102303 2 None -5 6 Human 8.8 pKi = 8.8 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 297 2 1 3 2.2 C[C@@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm980076u
10017554 4260 25 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm9803525
CHEMBL101008 4260 25 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm9803525
11957541 1425 38 None -2 16 Human 8.8 pKi = 8.8 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
1229 1425 38 None -2 16 Human 8.8 pKi = 8.8 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
147 1425 38 None -2 16 Human 8.8 pKi = 8.8 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
170617 1425 38 None -2 16 Human 8.8 pKi = 8.8 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
CHEMBL6616 1425 38 None -2 16 Human 8.8 pKi = 8.8 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
118706285 112376 0 None 2 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 295 2 3 2 1.7 CCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
CHEMBL3310113 112376 0 None 2 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 295 2 3 2 1.7 CCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
135399866 71696 2 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 209 2 2 4 1.2 C[C@H](N)Cn1ncc2ccc(O)c(F)c21 10.1021/jm050663x
CHEMBL197653 71696 2 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 209 2 2 4 1.2 C[C@H](N)Cn1ncc2ccc(O)c(F)c21 10.1021/jm050663x
118464429 166553 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 383 1 3 5 2.6 NC1=NC2(CCCCC2)NC(Nc2cccc(I)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4290245 166553 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 383 1 3 5 2.6 NC1=NC2(CCCCC2)NC(Nc2cccc(I)c2)=N1 10.1021/acsmedchemlett.8b00300
127048333 140136 0 None 38 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2ccccc2F)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3815112 140136 0 None 38 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2ccccc2F)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
118706280 120005 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cc(Cl)ccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310110 120005 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cc(Cl)ccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545464 120005 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cc(Cl)ccc1-2 10.1016/j.bmc.2014.05.027
118717220 120056 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 305 1 2 1 2.9 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343669 120056 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 305 1 2 1 2.9 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3545811 120056 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 305 1 2 1 2.9 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
72734860 103467 0 None 6 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092753 103467 0 None 6 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
11277147 105847 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092759 105847 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3139188 105847 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
11277147 105847 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3092759 105847 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3139188 105847 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2014.05.027
134 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.ejmech.2019.111736
1775 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.ejmech.2019.111736
9681 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.ejmech.2019.111736
CHEMBL1065 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.ejmech.2019.111736
DB00247 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.ejmech.2019.111736
206 2447 10 None -1 25 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/S0960-894X(96)00503-3
68848 2447 10 None -1 25 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/S0960-894X(96)00503-3
CHEMBL12314 2447 10 None -1 25 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/S0960-894X(96)00503-3
192 3433 46 None -10 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10.1021/jm990388c
443390 3433 46 None -10 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10.1021/jm990388c
CHEMBL14276 3433 46 None -10 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10.1021/jm990388c
10573762 98314 0 None 1 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(-c3cccnc3)cc1)CC2 10.1021/jm990388c
CHEMBL278267 98314 0 None 1 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(-c3cccnc3)cc1)CC2 10.1021/jm990388c
10670813 162029 0 None -15 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 441 4 1 3 5.9 CCc1cc(NC(=O)N2CCc3cc(OC)c(C(F)(F)F)cc32)cc(-c2cccnc2)c1 10.1021/jm990388c
CHEMBL416896 162029 0 None -15 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 441 4 1 3 5.9 CCc1cc(NC(=O)N2CCc3cc(OC)c(C(F)(F)F)cc32)cc(-c2cccnc2)c1 10.1021/jm990388c
44397929 66830 0 None -6 3 Human 8.0 pKi = 8 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 222 0 1 2 2.0 Cc1c(Cl)ccc2c1N1CCNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL187739 66830 0 None -6 3 Human 8.0 pKi = 8 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 222 0 1 2 2.0 Cc1c(Cl)ccc2c1N1CCNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
10808965 99854 0 None -3 3 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 367 3 1 3 4.8 CCSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
CHEMBL289436 99854 0 None -3 3 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 367 3 1 3 4.8 CCSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
46230098 197639 0 None -3 3 Human 8.0 pKi = 8 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 231 0 2 3 0.9 Cc1cccc2c1C(=O)NC1CCNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590580 197639 0 None -3 3 Human 8.0 pKi = 8 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 231 0 2 3 0.9 Cc1cccc2c1C(=O)NC1CCNCCN21 10.1016/j.bmcl.2009.12.014
18931422 205650 0 None -50 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 435 8 2 5 3.4 COc1ccc(-c2ccccc2)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
CHEMBL93862 205650 0 None -50 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 435 8 2 5 3.4 COc1ccc(-c2ccccc2)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
10740494 34898 0 None -12 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 414 3 1 4 4.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL14345 34898 0 None -12 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 414 3 1 4 4.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3cccnc3)c1)CC2 10.1021/jm990388c
10764263 40630 0 None -15 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 414 3 1 4 4.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3ccncc3)c1)CC2 10.1021/jm990388c
CHEMBL14863 40630 0 None -15 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 414 3 1 4 4.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3ccncc3)c1)CC2 10.1021/jm990388c
10740495 98163 0 None -1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 414 3 1 4 4.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(-c3cccnc3)nc1)CC2 10.1021/jm990388c
CHEMBL277111 98163 0 None -1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 414 3 1 4 4.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(-c3cccnc3)nc1)CC2 10.1021/jm990388c
122178705 120844 0 None 2 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 7 0 5 5.0 CCCC(C)Oc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581250 120844 0 None 2 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 7 0 5 5.0 CCCC(C)Oc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
59395105 105846 1 None 4 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 252 1 3 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)[nH]c1ccccc12 10.1016/j.bmc.2013.10.010
CHEMBL3092755 105846 1 None 4 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 252 1 3 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)[nH]c1ccccc12 10.1016/j.bmc.2013.10.010
CHEMBL3139187 105846 1 None 4 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 252 1 3 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)[nH]c1ccccc12 10.1016/j.bmc.2013.10.010
118729272 120185 0 None 3 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 5.0 CN(C)[C@@H]1Cc2ccccc2[C@@H](C2CCCCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402680 120185 0 None 3 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 5.0 CN(C)[C@@H]1Cc2ccccc2[C@@H](C2CCCCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547158 120185 0 None 3 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 5.0 CN(C)[C@@H]1Cc2ccccc2[C@@H](C2CCCCCCC2)C1 10.1016/j.bmc.2015.01.060
44214724 193306 0 None -19 3 Human 8.0 pKi = 8 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 429 4 1 5 4.4 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3cnccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL54707 193306 0 None -19 3 Human 8.0 pKi = 8 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 429 4 1 5 4.4 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3cnccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
5 139 66 None -13 55 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00726
5202 139 66 None -13 55 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00726
CHEMBL39 139 66 None -13 55 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00726
DB08839 139 66 None -13 55 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00726
24841480 183307 0 None -50 20 Human 7.0 pKi = 7 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 183307 0 None -50 20 Human 7.0 pKi = 7 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
193 3437 38 None -707 5 Human 7.0 pKi = 7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm990388c
3644637 3437 38 None -707 5 Human 7.0 pKi = 7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm990388c
CHEMBL14563 3437 38 None -707 5 Human 7.0 pKi = 7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm990388c
194 3438 25 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm990388c
443391 3438 25 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm990388c
CHEMBL14460 3438 25 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm990388c
193 3437 38 None -707 5 Human 7.0 pKi = 7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2005.08.004
3644637 3437 38 None -707 5 Human 7.0 pKi = 7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2005.08.004
CHEMBL14563 3437 38 None -707 5 Human 7.0 pKi = 7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2005.08.004
194 3438 25 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2005.08.004
443391 3438 25 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2005.08.004
CHEMBL14460 3438 25 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2005.08.004
193 3437 38 None -707 5 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1016/s0960-894x(00)00364-4
3644637 3437 38 None -707 5 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1016/s0960-894x(00)00364-4
CHEMBL14563 3437 38 None -707 5 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1016/s0960-894x(00)00364-4
194 3438 25 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/s0960-894x(00)00364-4
443391 3438 25 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/s0960-894x(00)00364-4
CHEMBL14460 3438 25 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/s0960-894x(00)00364-4
44298230 192990 0 None -79 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 492 3 1 4 6.0 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Br)c(C(F)(F)F)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL53152 192990 0 None -79 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 492 3 1 4 6.0 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Br)c(C(F)(F)F)cc32)cn1 10.1016/s0960-894x(00)00364-4
44298022 193875 0 None -63 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 422 5 1 4 5.8 CCCc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(C)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL55472 193875 0 None -63 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 422 5 1 4 5.8 CCCc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(C)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
18931133 167457 0 None -10 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 465 9 2 6 3.4 COc1cc(OC)c(-c2ccccc2)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
CHEMBL432217 167457 0 None -10 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 465 9 2 6 3.4 COc1cc(OC)c(-c2ccccc2)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
145977338 163154 0 None 19 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 259 3 2 4 2.2 Oc1ccccc1C1=NC(Cc2c[nH]cn2)CS1 10.1021/acs.jnatprod.7b00317
CHEMBL4205064 163154 0 None 19 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 259 3 2 4 2.2 Oc1ccccc1C1=NC(Cc2c[nH]cn2)CS1 10.1021/acs.jnatprod.7b00317
145963830 163560 0 None 7 7 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
CHEMBL4209942 163560 0 None 7 7 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
193 3437 38 None -707 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm970424c
3644637 3437 38 None -707 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm970424c
CHEMBL14563 3437 38 None -707 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm970424c
11419526 87614 0 None -100 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3ccc(Cl)c(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234533 87614 0 None -100 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3ccc(Cl)c(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
16215237 87733 0 None -39 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.6 COc1ccc(N2Cc3cc(Cl)c(Cl)c(C)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234738 87733 0 None -39 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.6 COc1ccc(N2Cc3cc(Cl)c(Cl)c(C)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
10503674 98356 0 None -3 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 449 3 1 3 5.6 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3c(F)cccc3F)c1)CC2 10.1021/jm990388c
CHEMBL278685 98356 0 None -3 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 449 3 1 3 5.6 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3c(F)cccc3F)c1)CC2 10.1021/jm990388c
9813197 96075 5 None -11 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 215 0 1 1 2.7 Clc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL262862 96075 5 None -11 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 215 0 1 1 2.7 Clc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
25122651 198555 0 None -23 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL597002 198555 0 None -23 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
67268994 163405 2 None -3 7 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4207884 163405 2 None -3 7 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
44298108 100444 0 None -39 2 Human 7.0 pKi = 7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 394 4 1 4 4.6 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL293937 100444 0 None -39 2 Human 7.0 pKi = 7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 394 4 1 4 4.6 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
44298092 101486 0 None -19 2 Human 7.0 pKi = 7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 400 4 1 5 4.7 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3nccs3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL301409 101486 0 None -19 2 Human 7.0 pKi = 7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 400 4 1 5 4.7 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3nccs3)nc1)CC2 10.1016/s0960-894x(00)00365-6
162663486 181407 0 None - 1 Human 6.0 pKi = 6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 348 4 1 3 4.7 O=c1cc(CCCc2cccc(C(F)(F)F)c2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
CHEMBL4780527 181407 0 None - 1 Human 6.0 pKi = 6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 348 4 1 3 4.7 O=c1cc(CCCc2cccc(C(F)(F)F)c2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
162672422 182589 0 None -1 2 Human 6.0 pKi = 6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 310 5 1 4 3.7 COc1ccc(CCCc2cc(=O)c3c(O)cccc3o2)cc1 10.1016/j.bmcl.2020.127511
CHEMBL4795598 182589 0 None -1 2 Human 6.0 pKi = 6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 310 5 1 4 3.7 COc1ccc(CCCc2cc(=O)c3c(O)cccc3o2)cc1 10.1016/j.bmcl.2020.127511
24888181 79699 0 None -158 3 Human 6.0 pKi = 6 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 410 7 0 4 4.1 COc1ccc(N2CC=C(c3ccc(F)cc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL213272 79699 0 None -158 3 Human 6.0 pKi = 6 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 410 7 0 4 4.1 COc1ccc(N2CC=C(c3ccc(F)cc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
24887525 79944 0 None -199 3 Human 6.0 pKi = 6 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 476 7 0 4 5.6 COc1ccc(N2CCC(C)(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL214398 79944 0 None -199 3 Human 6.0 pKi = 6 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 476 7 0 4 5.6 COc1ccc(N2CCC(C)(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
9888494 97706 0 None -446 13 Human 6.0 pKi = 6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor was determinedBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL273921 97706 0 None -446 13 Human 6.0 pKi = 6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor was determinedBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
11168182 3465 18 None -158 13 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
264 3465 18 None -158 13 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
CHEMBL1181770 3465 18 None -158 13 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
6918648 101076 1 None -1621 14 Human 6.0 pKi = 6 Binding
Compound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HTCompound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HT
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL29846 101076 1 None -1621 14 Human 6.0 pKi = 6 Binding
Compound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HTCompound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HT
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
145972374 164111 0 None -3 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 388 6 3 7 1.3 COC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1N=C(c2ccccc2O)S[C@@H]1C 10.1021/acs.jnatprod.7b00317
CHEMBL4216860 164111 0 None -3 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 388 6 3 7 1.3 COC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1N=C(c2ccccc2O)S[C@@H]1C 10.1021/acs.jnatprod.7b00317
136054961 57006 4 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 220 2 2 4 1.6 NC(=O)c1csc(-c2ccccc2O)n1 10.1021/acs.jnatprod.7b00317
CHEMBL1651091 57006 4 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 220 2 2 4 1.6 NC(=O)c1csc(-c2ccccc2O)n1 10.1021/acs.jnatprod.7b00317
153287535 174318 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 0 1 3 2.0 CN1CC[C@H]2c3ccc(O)cc3OC[C@]21C 10.1021/acsmedchemlett.9b00225
CHEMBL4564308 174318 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 0 1 3 2.0 CN1CC[C@H]2c3ccc(O)cc3OC[C@]21C 10.1021/acsmedchemlett.9b00225
23462894 156677 3 None -15 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 240 1 0 3 2.3 CN1CCc2ccc([N+](=O)[O-])c(Cl)c2CC1 10.1016/j.bmc.2007.12.009
CHEMBL407636 156677 3 None -15 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 240 1 0 3 2.3 CN1CCc2ccc([N+](=O)[O-])c(Cl)c2CC1 10.1016/j.bmc.2007.12.009
9934284 89851 0 None -2511 10 Human 6.0 pKi = 6 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
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 -2511 10 Human 6.0 pKi = 6 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
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
76325517 105239 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 272 3 1 4 3.3 O=c1cc(CCc2cccs2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
CHEMBL3126302 105239 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 272 3 1 4 3.3 O=c1cc(CCc2cccs2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
118278480 121484 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 282 3 2 4 3.0 O=c1cc(CCc2ccc(O)cc2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
CHEMBL3593950 121484 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 282 3 2 4 3.0 O=c1cc(CCc2ccc(O)cc2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
44453877 155064 0 None -19 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 305 2 1 3 3.6 Fc1ccc(-c2nc(-c3ccccc3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL404582 155064 0 None -19 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 305 2 1 3 3.6 Fc1ccc(-c2nc(-c3ccccc3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
44298151 100385 0 None -31 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 380 4 1 4 4.3 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2cc(Cl)ccc21 10.1016/s0960-894x(00)00365-6
CHEMBL293597 100385 0 None -31 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 380 4 1 4 4.3 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2cc(Cl)ccc21 10.1016/s0960-894x(00)00365-6
44298158 192896 0 None -12 3 Human 6.0 pKi = 6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 380 4 1 4 4.3 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2c(Cl)cccc21 10.1016/s0960-894x(00)00365-6
CHEMBL52783 192896 0 None -12 3 Human 6.0 pKi = 6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 380 4 1 4 4.3 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2c(Cl)cccc21 10.1016/s0960-894x(00)00365-6
6918648 101076 1 None -1621 14 Human 6.0 pKi = 6 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
CHEMBL29846 101076 1 None -1621 14 Human 6.0 pKi = 6 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
3233 3443 40 None -165 12 Human 5.0 pKi = 5 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
3247 3443 40 None -165 12 Human 5.0 pKi = 5 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
6604889 3443 40 None -165 12 Human 5.0 pKi = 5 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
CHEMBL282199 3443 40 None -165 12 Human 5.0 pKi = 5 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
DB13988 3443 40 None -165 12 Human 5.0 pKi = 5 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
16063047 94926 0 None -77 3 Human 5.0 pKi = 5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 333 3 1 3 3.9 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CNCCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL256811 94926 0 None -77 3 Human 5.0 pKi = 5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 333 3 1 3 3.9 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CNCCC3)cc1 10.1016/j.bmcl.2008.01.090
122483292 137570 0 None -3 7 Human 7.0 pKi = 7 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764335 137570 0 None -3 7 Human 7.0 pKi = 7 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765876 137570 0 None -3 7 Human 7.0 pKi = 7 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
141 1394 32 None -1 22 Human 7.0 pKi = 7 Binding
Compound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptor
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm980692q
6089 1394 32 None -1 22 Human 7.0 pKi = 7 Binding
Compound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptor
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm980692q
CHEMBL12420 1394 32 None -1 22 Human 7.0 pKi = 7 Binding
Compound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptor
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm980692q
DB01488 1394 32 None -1 22 Human 7.0 pKi = 7 Binding
Compound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptor
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm980692q
136054961 57006 4 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 220 2 2 4 1.6 NC(=O)c1csc(-c2ccccc2O)n1 10.1021/np100588c
CHEMBL1651091 57006 4 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 220 2 2 4 1.6 NC(=O)c1csc(-c2ccccc2O)n1 10.1021/np100588c
73213196 103968 1 None 1 13 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptor (unknown origin)Binding affinity to 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2014.05.016
CHEMBL3104093 103968 1 None 1 13 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptor (unknown origin)Binding affinity to 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2014.05.016
73213196 103968 1 None 1 13 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 103968 1 None 1 13 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
73213196 103968 1 None 1 13 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 103968 1 None 1 13 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
142601343 185011 0 None -36 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4863868 185011 0 None -36 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
71455083 81404 0 None -173 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164354 81404 0 None -173 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
2520 202301 65 None -4 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL1280 202301 65 None -4 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL6966 202301 65 None -4 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
118055295 177488 0 None -17 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 242 0 1 2 2.2 FC(F)(F)c1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4647417 177488 0 None -17 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 242 0 1 2 2.2 FC(F)(F)c1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
11324968 90640 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397880 90640 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
168285382 190914 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 9 0 5 5.4 CCCCCCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5194057 190914 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 9 0 5 5.4 CCCCCCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
44582707 186405 0 None -8 5 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 430 10 0 6 4.1 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490634 186405 0 None -8 5 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 430 10 0 6 4.1 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmc.2009.03.021
13091359 113027 0 None -1479 10 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321790 113027 0 None -1479 10 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
53251189 130359 3 None - 1 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000704a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000704a HTR2B
ChEMBL 452 5 3 7 5.1 Cc1cc(Nc2nccc(C)n2)cc(-c2cnc([C@@]3(O)CC[C@H](C(=O)O)C(C)(C)C3)s2)c1 nan
CHEMBL3685796 130359 3 None - 1 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000704a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000704a HTR2B
ChEMBL 452 5 3 7 5.1 Cc1cc(Nc2nccc(C)n2)cc(-c2cnc([C@@]3(O)CC[C@H](C(=O)O)C(C)(C)C3)s2)c1 nan
135367405 163633 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4210782 163633 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
122179556 120961 0 None 2 2 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR2B
ChEMBL 303 2 0 3 4.5 FC(F)(F)c1ccc2c(c1)nc(-c1cccnc1)n2C1CC1 nan
CHEMBL3582461 120961 0 None 2 2 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR2B
ChEMBL 303 2 0 3 4.5 FC(F)(F)c1ccc2c(c1)nc(-c1cccnc1)n2C1CC1 nan
15560577 184749 6 None 1 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 398 5 1 5 3.8 CC[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
CHEMBL4859858 184749 6 None 1 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 398 5 1 5 3.8 CC[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
123683 3060 58 None -12302 13 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B receptor (unknown origin) by PDSP screeningBinding affinity to 5HT2B receptor (unknown origin) by PDSP screening
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm501021n
422 3060 58 None -12302 13 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B receptor (unknown origin) by PDSP screeningBinding affinity to 5HT2B receptor (unknown origin) by PDSP screening
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm501021n
CHEMBL119709 3060 58 None -12302 13 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B receptor (unknown origin) by PDSP screeningBinding affinity to 5HT2B receptor (unknown origin) by PDSP screening
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm501021n
DB05511 3060 58 None -12302 13 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B receptor (unknown origin) by PDSP screeningBinding affinity to 5HT2B receptor (unknown origin) by PDSP screening
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm501021n
123683 3060 58 None -12302 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
422 3060 58 None -12302 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
CHEMBL119709 3060 58 None -12302 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
DB05511 3060 58 None -12302 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
16115652 83064 0 None -27 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 286 1 1 3 1.8 COc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL220211 83064 0 None -27 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 286 1 1 3 1.8 COc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
71061724 145007 0 None 1 5 Mouse 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
CHEMBL3915107 145007 0 None 1 5 Mouse 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
10660 14283 55 None -29 12 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
CHEMBL1200406 14283 55 None -29 12 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
134138168 147146 0 None 1 10 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL3931889 147146 0 None 1 10 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
44397832 122580 0 None -7 3 Human 8.0 pKi = 8.0 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 256 0 1 2 2.4 C[C@@H]1CNC[C@H]2Cc3ccc(C(F)(F)F)cc3N12 10.1016/j.bmcl.2005.05.074
CHEMBL361079 122580 0 None -7 3 Human 8.0 pKi = 8.0 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 256 0 1 2 2.4 C[C@@H]1CNC[C@H]2Cc3ccc(C(F)(F)F)cc3N12 10.1016/j.bmcl.2005.05.074
118706287 120007 0 None 14 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccc(Cl)cc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310114 120007 0 None 14 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccc(Cl)cc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545466 120007 0 None 14 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccc(Cl)cc1-2 10.1016/j.bmc.2014.05.027
10131066 21388 0 None -54 4 Human 8.0 pKi = 8.0 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 244 2 1 3 2.4 CC(N)Cc1cn(C)c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL131736 21388 0 None -54 4 Human 8.0 pKi = 8.0 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 244 2 1 3 2.4 CC(N)Cc1cn(C)c2ccc3c(c12)CCCO3 10.1021/jm030205t
134141831 146142 0 None 2 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 405 6 4 8 1.4 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3923870 146142 0 None 2 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 405 6 4 8 1.4 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
45486902 195261 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 449 5 2 4 4.6 O=c1[nH]c2cccc(OCC3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 10.1016/j.bmcl.2009.08.050
CHEMBL566396 195261 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 449 5 2 4 4.6 O=c1[nH]c2cccc(OCC3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 10.1016/j.bmcl.2009.08.050
118729270 120177 0 None -1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402678 120177 0 None -1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547139 120177 0 None -1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(F)c2)C1 10.1016/j.bmc.2015.01.060
145965628 163484 0 None -4 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 333 4 1 3 4.6 C[C@@H]1SC(c2ccc(-c3ccccc3)cc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4208914 163484 0 None -4 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 333 4 1 3 4.6 C[C@@H]1SC(c2ccc(-c3ccccc3)cc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
146025727 171109 0 None -40 27 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK 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 -40 27 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK 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
132060743 161674 0 None -4 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4163428 161674 0 None -4 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
10541003 102631 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 283 1 1 3 2.2 COc1cc(Br)c2c3c1C[C@H](N)C[C@H]3CO2 10.1021/jm980076u
CHEMBL307770 102631 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 283 1 1 3 2.2 COc1cc(Br)c2c3c1C[C@H](N)C[C@H]3CO2 10.1021/jm980076u
136118640 75950 0 None 3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058700 75950 0 None 3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
21044391 76263 0 None -21 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 219 1 2 4 0.3 C[C@@H]1CNC[C@H]2Cc3ccc(CO)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL206386 76263 0 None -21 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 219 1 2 4 0.3 C[C@@H]1CNC[C@H]2Cc3ccc(CO)nc3N12 10.1016/j.bmcl.2005.11.083
2333 141791 91 None 1 2 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 nan
CHEMBL388590 141791 91 None 1 2 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 nan
11313985 90638 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397878 90638 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
18715561 72682 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cccnc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201062 72682 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cccnc3c21 10.1016/j.bmcl.2005.10.029
46914774 15253 0 None 21 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 364 7 0 4 4.5 CCCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
CHEMBL1215037 15253 0 None 21 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 364 7 0 4 4.5 CCCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
16115269 137588 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL376676 137588 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
21786603 134327 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 259 3 2 3 1.7 CN1CCN(CCc2c[nH]c3cccc(O)c23)CC1 10.1016/j.bmcl.2005.06.104
CHEMBL371899 134327 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 259 3 2 3 1.7 CN1CCN(CCc2c[nH]c3cccc(O)c23)CC1 10.1016/j.bmcl.2005.06.104
127051592 140334 0 None -51 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818710 140334 0 None -51 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819742 140334 0 None -51 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
2771 193337 67 None 1 27 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL1200781 193337 67 None 1 27 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL549 193337 67 None 1 27 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
127051592 140334 0 None -51 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818710 140334 0 None -51 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819742 140334 0 None -51 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
104903 56035 14 None -4 6 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
CHEMBL1630578 56035 14 None -4 6 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
58911534 90664 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397904 90664 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
2723 153500 104 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl nan
CHEMBL398440 153500 104 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl nan
1379258 67438 13 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 3 0 1 4.1 Cc1ccccc1C(=O)N1CCC(Cc2ccccc2)CC1 nan
CHEMBL1909050 67438 13 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 3 0 1 4.1 Cc1ccccc1C(=O)N1CCC(Cc2ccccc2)CC1 nan
16754 85134 43 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 355 4 0 5 3.5 COc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL228082 85134 43 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 355 4 0 5 3.5 COc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
5 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
5202 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
CHEMBL39 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
DB08839 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
CHEMBL5081379 212964 0 None -1 9 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
58405183 110195 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 339 6 1 3 3.9 FC(F)(COc1ccc(Cl)cc1OC1CNC1)c1ccccc1 10.1021/ml500082j
CHEMBL3260336 110195 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 339 6 1 3 3.9 FC(F)(COc1ccc(Cl)cc1OC1CNC1)c1ccccc1 10.1021/ml500082j
11380477 179092 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 280 2 1 4 2.7 CC(C)n1nc2c(c1-c1ccc(C#N)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4743582 179092 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 280 2 1 4 2.7 CC(C)n1nc2c(c1-c1ccc(C#N)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
5 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
5202 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
CHEMBL39 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
DB08839 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
10198431 73542 0 None -7 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201930 73542 0 None -7 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
189 3423 31 None -5 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1016/j.bmcl.2013.12.024
5163 3423 31 None -5 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1016/j.bmcl.2013.12.024
CHEMBL297784 3423 31 None -5 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1016/j.bmcl.2013.12.024
11625624 112576 0 None -17 7 Human 7.9 pKi = 7.9 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 406 4 4 8 0.9 CNC(=O)[C@]12C[C@@H]1[C@@H](n1cnc3c(NC4CCCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL331291 112576 0 None -17 7 Human 7.9 pKi = 7.9 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 406 4 4 8 0.9 CNC(=O)[C@]12C[C@@H]1[C@@H](n1cnc3c(NC4CCCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
189 3423 31 None -5 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1016/j.bmcl.2013.12.024
5163 3423 31 None -5 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1016/j.bmcl.2013.12.024
CHEMBL297784 3423 31 None -5 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1016/j.bmcl.2013.12.024
10741816 97725 0 None -5 3 Human 7.9 pKi = 7.9 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 441 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3c(C)ccnc3C)c1)CC2 10.1021/jm990388c
CHEMBL274066 97725 0 None -5 3 Human 7.9 pKi = 7.9 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 441 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3c(C)ccnc3C)c1)CC2 10.1021/jm990388c
10549658 97818 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(-c3ccncc3)cc1)CC2 10.1021/jm990388c
CHEMBL274692 97818 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(-c3ccncc3)cc1)CC2 10.1021/jm990388c
18475509 101464 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 318 2 2 3 3.9 CN1CCc2cc(NC(=O)Nc3ccnc4ccccc34)ccc21 10.1016/s0960-894x(01)00343-2
CHEMBL301209 101464 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 318 2 2 3 3.9 CN1CCc2cc(NC(=O)Nc3ccnc4ccccc34)ccc21 10.1016/s0960-894x(01)00343-2
191 3429 47 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 10.1021/jm970741j
443389 3429 47 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 10.1021/jm970741j
CHEMBL276140 3429 47 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 10.1021/jm970741j
44298172 101288 0 None -6 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 429 3 1 5 4.9 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cncnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL299938 101288 0 None -6 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 429 3 1 5 4.9 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cncnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
44298163 193720 0 None -25 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cnccc3Cl)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL55207 193720 0 None -25 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cnccc3Cl)nc1)CC2 10.1016/s0960-894x(00)00364-4
191 3429 47 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 10.1021/jm970424c
443389 3429 47 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 10.1021/jm970424c
CHEMBL276140 3429 47 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 10.1021/jm970424c
9887537 83913 38 None -15 10 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
CHEMBL221692 83913 38 None -15 10 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
CHEMBL4751170 83913 38 None -15 10 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
44298246 193926 0 None -2 3 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 397 4 1 5 4.0 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3nccn3C)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL55597 193926 0 None -2 3 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 397 4 1 5 4.0 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3nccn3C)nc1)CC2 10.1016/s0960-894x(00)00365-6
56658155 65317 0 None 13 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 350 6 0 4 3.8 COc1ccccc1CCN1CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmcl.2011.08.029
CHEMBL1834252 65317 0 None 13 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 350 6 0 4 3.8 COc1ccccc1CCN1CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmcl.2011.08.029
145972796 164033 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 236 3 2 4 2.0 CNc1ccccc1C1=N[C@@H](CO)[C@H](C)S1 10.1021/acs.jnatprod.7b00317
CHEMBL4215741 164033 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 236 3 2 4 2.0 CNc1ccccc1C1=N[C@@H](CO)[C@H](C)S1 10.1021/acs.jnatprod.7b00317
71212556 143018 0 None -24 6 Human 6.9 pKi = 6.9 Binding
Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.
ChEMBL 433 3 1 6 4.6 Cc1ccc2c(c1)Oc1sc(Cl)cc1C(N1CCN(CC(C)(C)C(=O)O)CC1)=N2 nan
CHEMBL3899169 143018 0 None -24 6 Human 6.9 pKi = 6.9 Binding
Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.
ChEMBL 433 3 1 6 4.6 Cc1ccc2c(c1)Oc1sc(Cl)cc1C(N1CCN(CC(C)(C)C(=O)O)CC1)=N2 nan
155561439 175083 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assay
ChEMBL 411 4 4 7 3.5 Oc1ccc(CCNc2nc(C#Cc3ccc(Cl)s3)nc3[nH]cnc23)cc1O 10.1039/C8MD00317C
CHEMBL4581568 175083 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assay
ChEMBL 411 4 4 7 3.5 Oc1ccc(CCNc2nc(C#Cc3ccc(Cl)s3)nc3[nH]cnc23)cc1O 10.1039/C8MD00317C
44404899 70074 2 None -70 5 Human 5.9 pKi = 5.9 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 190 2 2 2 1.9 CN(C)Cc1c[nH]c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL194588 70074 2 None -70 5 Human 5.9 pKi = 5.9 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 190 2 2 2 1.9 CN(C)Cc1c[nH]c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
44404904 132477 1 None -11 3 Human 5.9 pKi = 5.9 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 204 2 1 3 1.9 CN(C)Cc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL370221 132477 1 None -11 3 Human 5.9 pKi = 5.9 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 204 2 1 3 1.9 CN(C)Cc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
127050699 140328 0 None -14 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819082 140328 0 None -14 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819726 140328 0 None -14 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
117209918 185818 1 None -3 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4876036 185818 1 None -3 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
135508617 136016503 10515 0 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL1170237 10515 0 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
9869628 71684 0 None -199 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 440 7 0 4 4.8 COc1cc2c(cc1OCCN1CCCCC1)N(C(=O)/C=C/c1ccccc1Cl)CC2 10.1016/j.bmcl.2005.08.004
CHEMBL197630 71684 0 None -199 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 440 7 0 4 4.8 COc1cc2c(cc1OCCN1CCCCC1)N(C(=O)/C=C/c1ccccc1Cl)CC2 10.1016/j.bmcl.2005.08.004
10127968 71860 0 None -15 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 479 7 0 5 4.2 COc1ccc(N2CCN(c3ccc(C)c(C(F)(F)F)c3)C2=O)cc1OCCN1CCOCC1 10.1016/j.bmcl.2005.08.004
CHEMBL198109 71860 0 None -15 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 479 7 0 5 4.2 COc1ccc(N2CCN(c3ccc(C)c(C(F)(F)F)c3)C2=O)cc1OCCN1CCOCC1 10.1016/j.bmcl.2005.08.004
10479409 77694 0 None -25 3 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 460 7 0 4 5.3 COc1ccc(C2=CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL210007 77694 0 None -25 3 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 460 7 0 4 5.3 COc1ccc(C2=CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
49850874 56153 0 None -398 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 450 6 1 4 5.2 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632210 56153 0 None -398 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 450 6 1 4 5.2 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
44298243 100182 0 None -100 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 Cc1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(Oc2cccnc2C)nc1 10.1016/s0960-894x(00)00364-4
CHEMBL292228 100182 0 None -100 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 Cc1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(Oc2cccnc2C)nc1 10.1016/s0960-894x(00)00364-4
44298254 192930 0 None -50 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 442 4 1 4 5.8 CCc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL52919 192930 0 None -50 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 442 4 1 4 5.8 CCc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
22619858 197386 0 None -39 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 429 3 1 5 4.9 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nn1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL58765 197386 0 None -39 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 429 3 1 5 4.9 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nn1)CC2 10.1016/s0960-894x(00)00364-4
18931348 104249 0 None -39 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 389 8 2 6 1.7 COc1ccc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)c1 10.1016/S0960-894X(96)00503-3
CHEMBL310656 104249 0 None -39 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 389 8 2 6 1.7 COc1ccc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)c1 10.1016/S0960-894X(96)00503-3
44324011 111108 0 None -12 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 562 11 3 8 2.7 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(F)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL328375 111108 0 None -12 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 562 11 3 8 2.7 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(F)cc1 10.1016/S0960-894X(96)00503-3
148302367 172939 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 267 2 1 2 4.0 CC[C@H]1c2cc(-c3ccccc3)ccc2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4530979 172939 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 267 2 1 2 4.0 CC[C@H]1c2cc(-c3ccccc3)ccc2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
149396365 175421 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 295 3 1 3 3.5 C[C@@]12COc3cc(OCc4ccccc4)ccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4589450 175421 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 295 3 1 3 3.5 C[C@@]12COc3cc(OCc4ccccc4)ccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
44430976 87599 0 None -50 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCCC(C)C1 10.1016/j.bmcl.2006.10.029
CHEMBL234492 87599 0 None -50 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCCC(C)C1 10.1016/j.bmcl.2006.10.029
11236301 87612 0 None -63 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 450 6 0 4 4.9 COc1ccc(N2Cc3c(F)c(F)cc(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234531 87612 0 None -63 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 450 6 0 4 4.9 COc1ccc(N2Cc3c(F)c(F)cc(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
11475519 151531 0 None -79 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 414 6 0 4 4.6 COc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL396747 151531 0 None -79 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 414 6 0 4 4.6 COc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
44430979 152646 0 None -19 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.8 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1[C@@H](C)CCC[C@H]1C 10.1016/j.bmcl.2006.10.029
CHEMBL397709 152646 0 None -19 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.8 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1[C@@H](C)CCC[C@H]1C 10.1016/j.bmcl.2006.10.029
162654275 180088 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 310 5 1 4 3.7 COc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
CHEMBL4755344 180088 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 310 5 1 4 3.7 COc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
10287730 3467 36 None -1584 12 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor Binding affinity for human 5-hydroxytryptamine 2B receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
77 3467 36 None -1584 12 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor Binding affinity for human 5-hydroxytryptamine 2B receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
CHEMBL425190 3467 36 None -1584 12 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor Binding affinity for human 5-hydroxytryptamine 2B receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
10217208 71854 0 None -125 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 463 7 0 4 5.3 COc1ccc(N2CCN(c3cccc(Cl)c3Cl)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
CHEMBL198097 71854 0 None -125 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 463 7 0 4 5.3 COc1ccc(N2CCN(c3cccc(Cl)c3Cl)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
44404608 71893 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 346 6 1 4 2.7 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCO 10.1016/j.bmcl.2005.08.004
CHEMBL198192 71893 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 346 6 1 4 2.7 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCO 10.1016/j.bmcl.2005.08.004
10309622 140830 0 None -1000 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 395 7 0 4 4.0 COc1ccc(N2CCN(c3ccccc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
CHEMBL383800 140830 0 None -1000 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 395 7 0 4 4.0 COc1ccc(N2CCN(c3ccccc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
44414209 80810 0 None -398 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 424 7 0 4 4.4 COc1ccc(N2CC=C(c3ccc(F)cc3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
CHEMBL215864 80810 0 None -398 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 424 7 0 4 4.4 COc1ccc(N2CC=C(c3ccc(F)cc3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
9891002 106911 0 None -1258 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5-HT2B receptor in HEK 293 cells using [3H]- -5-HT as radioligandBinding affinity to human cloned 5-HT2B receptor in HEK 293 cells using [3H]- -5-HT as radioligand
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL318018 106911 0 None -1258 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5-HT2B receptor in HEK 293 cells using [3H]- -5-HT as radioligandBinding affinity to human cloned 5-HT2B receptor in HEK 293 cells using [3H]- -5-HT as radioligand
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
11304596 56087 0 None -7943 9 Human 5.9 pKi = 5.9 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 416 5 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc(N5CCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631542 56087 0 None -7943 9 Human 5.9 pKi = 5.9 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 416 5 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc(N5CCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
9827938 11651 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181680 11651 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL188486 11651 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
2470 3583 46 None -14125 60 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/S0960-894X(96)00503-3
3300 3583 46 None -14125 60 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/S0960-894X(96)00503-3
5265 3583 46 None -14125 60 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/S0960-894X(96)00503-3
99 3583 46 None -14125 60 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/S0960-894X(96)00503-3
CHEMBL267930 3583 46 None -14125 60 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/S0960-894X(96)00503-3
10008294 205090 0 None -63 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 574 12 3 9 2.5 COc1ccc(S(=O)(=O)Nc2cc(C(=O)CCCCN3CCC4(CC3)NC(=O)NC4=O)c(OC)cc2OC)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL90467 205090 0 None -63 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 574 12 3 9 2.5 COc1ccc(S(=O)(=O)Nc2cc(C(=O)CCCCN3CCC4(CC3)NC(=O)NC4=O)c(OC)cc2OC)cc1 10.1016/S0960-894X(96)00503-3
10371119 205269 0 None -794 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 586 12 3 8 3.7 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C(C)C)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL91454 205269 0 None -794 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 586 12 3 8 3.7 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C(C)C)cc1 10.1016/S0960-894X(96)00503-3
127050699 140328 0 None -14 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819082 140328 0 None -14 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819726 140328 0 None -14 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
122182283 121483 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 282 3 2 4 3.0 O=c1cc(CCc2cccc(O)c2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
CHEMBL3593949 121483 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 282 3 2 4 3.0 O=c1cc(CCc2cccc(O)c2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
9935387 98970 0 None -1584 14 Human 5.9 pKi = 5.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL282971 98970 0 None -1584 14 Human 5.9 pKi = 5.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
9913554 100510 0 None -1584 14 Human 5.9 pKi = 5.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29433 100510 0 None -1584 14 Human 5.9 pKi = 5.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
136030693 57007 1 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 222 2 2 4 0.7 NC(=O)C1CSC(c2ccccc2O)=N1 10.1021/np100588c
CHEMBL1651092 57007 1 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 222 2 2 4 0.7 NC(=O)C1CSC(c2ccccc2O)=N1 10.1021/np100588c
3034396 101155 33 None -20 17 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 398 5 1 5 3.8 CC[C@@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
CHEMBL299031 101155 33 None -20 17 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 398 5 1 5 3.8 CC[C@@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
1201549 590 22 None -26 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 590 22 None -26 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 590 22 None -26 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 590 22 None -26 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 590 22 None -26 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 590 22 None -26 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
118055293 176661 0 None -17 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 252 0 1 2 1.9 Brc1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4635854 176661 0 None -17 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 252 0 1 2 1.9 Brc1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
58911604 90661 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 236 0 1 2 1.3 O=C1c2ccc(Cl)cc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397901 90661 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 236 0 1 2 1.3 O=C1c2ccc(Cl)cc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
135846982 92609 0 None 7 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3cc(Br)ccc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2442268 92609 0 None 7 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3cc(Br)ccc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
5510 204127 97 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 2 4.9 Cc1cccc(N(C)C(=S)Oc2ccc3ccccc3c2)c1 nan
CHEMBL83668 204127 97 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 2 4.9 Cc1cccc(N(C)C(=S)Oc2ccc3ccccc3c2)c1 nan
135846955 188883 4 None 7 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 240 1 3 2 1.5 CN1C(=N)N/C(=C/c2c[nH]c3ccccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL513803 188883 4 None 7 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 240 1 3 2 1.5 CN1C(=N)N/C(=C/c2c[nH]c3ccccc23)C1=O 10.1016/j.bmc.2013.09.011
4122 205881 102 None -3 3 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 301 3 2 5 3.0 COC(=O)Nc1nc2ccc(C(=O)c3cccs3)cc2[nH]1 nan
CHEMBL9514 205881 102 None -3 3 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 301 3 2 5 3.0 COC(=O)Nc1nc2ccc(C(=O)c3cccs3)cc2[nH]1 nan
71682216 90669 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 260 3 1 3 1.4 CCCOc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397909 90669 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 260 3 1 3 1.4 CCCOc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL4754103 212270 0 None - 1 Human 5.9 pKi = 5.9 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000328a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000328a HTR2B
ChEMBL None None None CNC(=O)Nc1ccc2c(c1)CC[C@]21OC(=O)N(CC(=O)N(Cc2ccc(F)cc2)[C@@H](C)C(F)(F)F)C1=O nan
92042876 150792 0 None -2 10 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL3961059 150792 0 None -2 10 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
9920815 66898 0 None -7 3 Human 7.9 pKi = 7.9 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 216 0 1 2 2.0 Cc1ccc2c(c1C)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL188033 66898 0 None -7 3 Human 7.9 pKi = 7.9 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 216 0 1 2 2.0 Cc1ccc2c(c1C)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
5 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
5202 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
CHEMBL39 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
DB08839 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
152 361 18 None 1 19 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
2107 361 18 None 1 19 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
CHEMBL275854 361 18 None 1 19 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
24826790 90649 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397889 90649 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
46230095 197601 0 None 11 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 271 0 2 3 1.2 O=C1NC2CNCCN2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2009.12.014
CHEMBL590333 197601 0 None 11 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 271 0 2 3 1.2 O=C1NC2CNCCN2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2009.12.014
127048336 140062 0 None 5 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 573 12 0 5 5.8 COc1ccc(CCN(CCCc2ccccc2I)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3813855 140062 0 None 5 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 573 12 0 5 5.8 COc1ccc(CCN(CCCc2ccccc2I)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
5 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030205t
5202 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030205t
CHEMBL39 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030205t
DB08839 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030205t
152 361 18 None 1 19 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm030205t
2107 361 18 None 1 19 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm030205t
CHEMBL275854 361 18 None 1 19 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm030205t
9856041 23895 2 None -42 9 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 CC(N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL133868 23895 2 None -42 9 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 CC(N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
5 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2014.02.029
5202 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2014.02.029
CHEMBL39 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2014.02.029
DB08839 139 66 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2014.02.029
156013985 176591 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from recombinant human 5HT2B receptor expressed in CHO cells measured after 120 mins by scintillation counter methodDisplacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from recombinant human 5HT2B receptor expressed in CHO cells measured after 120 mins by scintillation counter method
ChEMBL 230 0 1 2 1.8 C1=CC2CNCCN3C[C@@H]4CCC[C@@H]4C(=C1)C23 10.1016/j.bmcl.2019.126929
CHEMBL4634785 176591 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from recombinant human 5HT2B receptor expressed in CHO cells measured after 120 mins by scintillation counter methodDisplacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from recombinant human 5HT2B receptor expressed in CHO cells measured after 120 mins by scintillation counter method
ChEMBL 230 0 1 2 1.8 C1=CC2CNCCN3C[C@@H]4CCC[C@@H]4C(=C1)C23 10.1016/j.bmcl.2019.126929
45486824 195691 0 None -14 3 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 421 4 3 4 3.3 O=C1Cc2c(ccc3c2OC[C@H](CNCC2CCc4[nH]c5ccc(F)cc5c4C2)O3)N1 10.1016/j.bmcl.2009.08.050
CHEMBL569251 195691 0 None -14 3 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 421 4 3 4 3.3 O=C1Cc2c(ccc3c2OC[C@H](CNCC2CCc4[nH]c5ccc(F)cc5c4C2)O3)N1 10.1016/j.bmcl.2009.08.050
CHEMBL5094234 213787 0 None -61 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096019 213787 0 None -61 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5090884 213791 0 None -1 7 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096072 213791 0 None -1 7 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
24771120 183508 0 None -56 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5HT2b receptorBinding affinity to 5HT2b receptor
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
CHEMBL482562 183508 0 None -56 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5HT2b receptorBinding affinity to 5HT2b receptor
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
136020618 163351 0 None 12 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4207302 163351 0 None 12 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
135753074 190504 7 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assay
ChEMBL 341 4 2 5 2.2 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2ccccc2F)n1 10.1021/acs.jmedchem.1c01759
CHEMBL5187824 190504 7 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assay
ChEMBL 341 4 2 5 2.2 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2ccccc2F)n1 10.1021/acs.jmedchem.1c01759
136030693 57007 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 222 2 2 4 0.7 NC(=O)C1CSC(c2ccccc2O)=N1 10.1021/acs.jnatprod.7b00317
CHEMBL1651092 57007 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 222 2 2 4 0.7 NC(=O)C1CSC(c2ccccc2O)=N1 10.1021/acs.jnatprod.7b00317
11739217 136503 0 None -8 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 300 2 1 3 2.2 CCOc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374660 136503 0 None -8 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 300 2 1 3 2.2 CCOc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
16063039 155063 0 None -147 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 333 3 1 3 3.9 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CCCNC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL404581 155063 0 None -147 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 333 3 1 3 3.9 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CCCNC3)cc1 10.1016/j.bmcl.2008.01.090
1353 1872 85 None -295 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1872 85 None -295 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1872 85 None -295 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1872 85 None -295 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1872 85 None -295 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL4537673 212226 24 None - 1 Human 5.9 pKi = 5.9 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000305b HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000305b HTR2B
ChEMBL None None None C[C@H](c1ccnc(Nc2nc3ccc(-c4cc(N(C)C)ncn4)cc3[nH]2)c1)N1CCN(C(=O)CC(F)(F)F)CC1 nan
44409332 76362 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 261 3 1 4 1.9 CCO[C@H](C)c1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL206618 76362 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 261 3 1 4 1.9 CCO[C@H](C)c1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
162661262 181260 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 432 6 4 7 2.7 OC[C@@]12C[C@@H]1[C@@H](n1ccc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1016/j.bmcl.2020.127599
CHEMBL4778636 181260 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 432 6 4 7 2.7 OC[C@@]12C[C@@H]1[C@@H](n1ccc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1016/j.bmcl.2020.127599
1016 3678 75 None -17 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3678 75 None -17 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3678 75 None -17 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3678 75 None -17 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3678 75 None -17 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3678 75 None -17 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
71061585 159938 0 None 3 2 Mouse 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 367 6 0 5 2.8 Cc1ccnc(C)c1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL4112090 159938 0 None 3 2 Mouse 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 367 6 0 5 2.8 Cc1ccnc(C)c1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL1909069 207322 0 None -1 3 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL None None None None nan
117209971 185893 1 None -26 5 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4877051 185893 1 None -26 5 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
1343 1850 55 None -14 9 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
3519 1850 55 None -14 9 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
522 1850 55 None -14 9 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
CHEMBL862 1850 55 None -14 9 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
DB01018 1850 55 None -14 9 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
CHEMBL4780458 212277 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000540a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000540a HTR2B
ChEMBL None None None O=C(Nc1cccnn1)N1CC(C/C=C/c2cncc(Oc3ccc(C(F)(F)F)cn3)n2)C1 nan
58911681 90540 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@@H]1CN2C(=O)c3ccccc3C[C@@H]2CN1 10.1016/j.bmcl.2013.04.061
CHEMBL2396668 90540 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@@H]1CN2C(=O)c3ccccc3C[C@@H]2CN1 10.1016/j.bmcl.2013.04.061
136118639 75949 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058699 75949 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
2337 3193 72 None -15 63 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3193 72 None -15 63 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3193 72 None -15 63 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3193 72 None -15 63 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3193 72 None -15 63 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
71455625 82537 0 None -3388 6 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1021/jm300943r
CHEMBL2181170 82537 0 None -3388 6 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1021/jm300943r
44407398 74054 0 None -8 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 365 5 1 3 5.5 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2ccccc2c1 10.1016/j.bmcl.2005.10.029
CHEMBL202616 74054 0 None -8 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 365 5 1 3 5.5 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2ccccc2c1 10.1016/j.bmcl.2005.10.029
136030596 57005 1 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 209 2 2 4 1.2 OC[C@@H]1CSC(c2ccccc2O)=N1 10.1021/np100588c
CHEMBL1651090 57005 1 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 209 2 2 4 1.2 OC[C@@H]1CSC(c2ccccc2O)=N1 10.1021/np100588c
168277287 189547 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assayDisplacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assay
ChEMBL 426 7 2 3 7.8 CCCC(CCC)c1nc2c(Nc3ccc(Cl)c(Cl)c3)nc3ccccc3c2[nH]1 10.1021/acs.jmedchem.2c01170
CHEMBL5173661 189547 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assayDisplacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assay
ChEMBL 426 7 2 3 7.8 CCCC(CCC)c1nc2c(Nc3ccc(Cl)c(Cl)c3)nc3ccccc3c2[nH]1 10.1021/acs.jmedchem.2c01170
25123011 199498 0 None -74 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
CHEMBL603483 199498 0 None -74 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
46230046 197557 0 None 14 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 203 0 2 3 0.2 O=C1NC2CNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
CHEMBL590077 197557 0 None 14 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 203 0 2 3 0.2 O=C1NC2CNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
135846958 75877 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2cc(Br)ccc12 10.1016/j.bmc.2013.09.011
CHEMBL2058408 75877 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2cc(Br)ccc12 10.1016/j.bmc.2013.09.011
18715555 74011 0 None -8 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 359 5 1 5 4.1 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2005.10.029
CHEMBL202458 74011 0 None -8 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 359 5 1 5 4.1 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2005.10.029
168286940 191673 0 None -691 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor at 25 uM incubated for 1 hr by microbeta2 beta-counter analysisDisplacement of [3H]-LSD from human 5-HT2B receptor at 25 uM incubated for 1 hr by microbeta2 beta-counter analysis
ChEMBL 454 7 1 4 4.0 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCC(F)(F)F)cc2)CC1 10.1016/j.ejmech.2022.114246
CHEMBL5205903 191673 0 None -691 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor at 25 uM incubated for 1 hr by microbeta2 beta-counter analysisDisplacement of [3H]-LSD from human 5-HT2B receptor at 25 uM incubated for 1 hr by microbeta2 beta-counter analysis
ChEMBL 454 7 1 4 4.0 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCC(F)(F)F)cc2)CC1 10.1016/j.ejmech.2022.114246
76518514 113025 0 None -147 9 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321788 113025 0 None -147 9 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
58911582 90654 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397894 90654 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
59012632 87296 0 None 91 2 Human 7.9 pKi = 7.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 388 2 1 3 4.6 COc1ccc(-c2cc3c4c(c2)[C@@H]2CNCC[C@@H]2N4CCC3)c(C(F)(F)F)c1 10.1016/j.bmcl.2012.10.091
CHEMBL2337102 87296 0 None 91 2 Human 7.9 pKi = 7.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 388 2 1 3 4.6 COc1ccc(-c2cc3c4c(c2)[C@@H]2CNCC[C@@H]2N4CCC3)c(C(F)(F)F)c1 10.1016/j.bmcl.2012.10.091
127051482 140110 0 None 8 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2ccc(F)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3814737 140110 0 None 8 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2ccc(F)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
127050282 140129 0 None 7 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2cccc(Br)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3815066 140129 0 None 7 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2cccc(Br)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
10353268 97308 1 None -23 5 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 216 2 2 2 2.0 NCCc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL27173 97308 1 None -23 5 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 216 2 2 2 2.0 NCCc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
24893978 993 5 None -35 8 Human 6.9 pKi = 6.9 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
8872 993 5 None -35 8 Human 6.9 pKi = 6.9 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
CHEMBL495075 993 5 None -35 8 Human 6.9 pKi = 6.9 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
10176869 165463 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 222 0 1 2 2.0 Cc1c(Cl)ccc2c1N1CCNC[C@@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL425545 165463 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 222 0 1 2 2.0 Cc1c(Cl)ccc2c1N1CCNC[C@@H]1C2 10.1016/j.bmcl.2005.05.074
11595191 88617 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337488 88617 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2364960 88617 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
145978819 163318 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2cccs2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4206939 163318 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2cccs2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
145975226 163370 0 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 388 6 3 7 1.3 COC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1N=C(c2ccccc2O)S[C@@H]1C 10.1021/acs.jnatprod.7b00317
CHEMBL4207529 163370 0 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 388 6 3 7 1.3 COC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1N=C(c2ccccc2O)S[C@@H]1C 10.1021/acs.jnatprod.7b00317
145976983 163443 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 333 4 1 3 4.6 C[C@H]1SC(c2ccc(-c3ccccc3)cc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4208376 163443 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 333 4 1 3 4.6 C[C@H]1SC(c2ccc(-c3ccccc3)cc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
136030596 57005 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 209 2 2 4 1.2 OC[C@@H]1CSC(c2ccccc2O)=N1 10.1021/acs.jnatprod.7b00317
CHEMBL1651090 57005 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 209 2 2 4 1.2 OC[C@@H]1CSC(c2ccccc2O)=N1 10.1021/acs.jnatprod.7b00317
44537940 18572 0 None -18 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1278001 18572 0 None -18 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
16115513 135866 0 None -23 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL373531 135866 0 None -23 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
136118732 75878 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2c(Br)cccc12 10.1016/j.bmc.2013.09.011
CHEMBL2058409 75878 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2c(Br)cccc12 10.1016/j.bmc.2013.09.011
122187383 122501 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 455 5 0 5 5.6 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(CC1CC1)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609148 122501 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 455 5 0 5 5.6 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(CC1CC1)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
72549033 110191 0 None -660 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-R-O-DOI from human 5-HT2B receptor expressed in CHO-K1 cells by by liquid scintillation spectrometryDisplacement of [125I]-R-O-DOI from human 5-HT2B receptor expressed in CHO-K1 cells by by liquid scintillation spectrometry
ChEMBL 367 3 0 5 3.3 CN1CCC(c2cccc3cc(S(=O)(=O)c4ccccn4)cnc23)CC1 10.1021/ml500045k
CHEMBL3260311 110191 0 None -660 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-R-O-DOI from human 5-HT2B receptor expressed in CHO-K1 cells by by liquid scintillation spectrometryDisplacement of [125I]-R-O-DOI from human 5-HT2B receptor expressed in CHO-K1 cells by by liquid scintillation spectrometry
ChEMBL 367 3 0 5 3.3 CN1CCC(c2cccc3cc(S(=O)(=O)c4ccccn4)cnc23)CC1 10.1021/ml500045k
155536080 171538 0 None 2 10 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4472703 171538 0 None 2 10 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
142601333 185171 0 None -63 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4866412 185171 0 None -63 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
71062646 148999 0 None -2398 13 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
CHEMBL3946661 148999 0 None -2398 13 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
56675412 65320 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 334 6 0 3 4.2 c1ccc(CCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
CHEMBL1834255 65320 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 334 6 0 3 4.2 c1ccc(CCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
134141050 146759 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 419 6 4 8 1.4 O=C(O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3928983 146759 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 419 6 4 8 1.4 O=C(O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
21302483 87297 0 None 10 2 Human 7.8 pKi = 7.8 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 246 0 1 3 2.4 c1cc2c3c(c1)[C@@H]1CNCC[C@@H]1N3CCCS2 10.1016/j.bmcl.2012.10.091
CHEMBL2337103 87297 0 None 10 2 Human 7.8 pKi = 7.8 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 246 0 1 3 2.4 c1cc2c3c(c1)[C@@H]1CNCC[C@@H]1N3CCCS2 10.1016/j.bmcl.2012.10.091
CHEMBL5094680 213724 0 None 3 8 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
46914487 15221 0 None 144 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 336 5 0 4 3.8 COc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
CHEMBL1214830 15221 0 None 144 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 336 5 0 4 3.8 COc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
71461603 78114 1 None -7 3 Human 7.8 pKi = 7.8 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@@H]1CNC[C@H]2Cc3ccccc3N12 10.1016/j.bmcl.2005.05.074
CHEMBL2112055 78114 1 None -7 3 Human 7.8 pKi = 7.8 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@@H]1CNC[C@H]2Cc3ccccc3N12 10.1016/j.bmcl.2005.05.074
2585 788 100 None -18 22 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 788 100 None -18 22 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 788 100 None -18 22 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 788 100 None -18 22 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 788 100 None -18 22 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
2389 3267 114 None -79 68 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3267 114 None -79 68 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3267 114 None -79 68 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3267 114 None -79 68 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3267 114 None -79 68 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
135520431 72249 9 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 177 2 2 4 0.7 NCCn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL199385 72249 9 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 177 2 2 4 0.7 NCCn1ncc2ccc(O)cc21 10.1021/jm050663x
24873257 179666 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 289 2 1 3 3.2 c1ccc(-c2c3c(nn2-c2ccccc2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4750414 179666 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 289 2 1 3 3.2 c1ccc(-c2c3c(nn2-c2ccccc2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
168274008 189592 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 7 0 5 4.6 CCCCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5174366 189592 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 7 0 5 4.6 CCCCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
134143752 150104 0 None 3 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 447 7 3 9 1.9 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3955519 150104 0 None 3 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 447 7 3 9 1.9 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
134143752 150104 0 None 3 5 Human 7.8 pKi = 7.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 447 7 3 9 1.9 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL3955519 150104 0 None 3 5 Human 7.8 pKi = 7.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 447 7 3 9 1.9 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
10550406 31722 0 None -3 3 Human 7.8 pKi = 7.8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 427 3 1 3 5.7 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3C)c1)CC2 10.1021/jm990388c
CHEMBL14076 31722 0 None -3 3 Human 7.8 pKi = 7.8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 427 3 1 3 5.7 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3C)c1)CC2 10.1021/jm990388c
10718089 98091 0 None -31 3 Human 7.8 pKi = 7.8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 443 4 1 4 5.4 COc1ccc(NC(=O)N2CCc3cc(OC)c(C(F)(F)F)cc32)cc1-c1cccnc1 10.1021/jm990388c
CHEMBL276571 98091 0 None -31 3 Human 7.8 pKi = 7.8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 443 4 1 4 5.4 COc1ccc(NC(=O)N2CCc3cc(OC)c(C(F)(F)F)cc32)cc1-c1cccnc1 10.1021/jm990388c
10767350 98572 0 None -6 3 Human 7.8 pKi = 7.8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 489 4 1 3 7.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(-c3ccccc3)cc(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL280297 98572 0 None -6 3 Human 7.8 pKi = 7.8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 489 4 1 3 7.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(-c3ccccc3)cc(-c3cccnc3)c1)CC2 10.1021/jm990388c
18475610 195111 0 None 3 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 327 3 2 3 4.5 COc1ccc(NC(=O)Nc2ccnc3ccccc23)cc1Cl 10.1016/s0960-894x(01)00343-2
CHEMBL56557 195111 0 None 3 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 327 3 2 3 4.5 COc1ccc(NC(=O)Nc2ccnc3ccccc23)cc1Cl 10.1016/s0960-894x(01)00343-2
10714852 162588 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 381 4 1 3 5.2 CCCSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
CHEMBL41792 162588 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 381 4 1 3 5.2 CCCSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
44298082 193284 0 None -3 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 4 1 4 5.3 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ncccc3C)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL54484 193284 0 None -3 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 4 1 4 5.3 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ncccc3C)nc1)CC2 10.1016/s0960-894x(00)00365-6
118055289 177315 0 None -19 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 236 0 1 2 2.7 Cc1cc2c3c(c1Cl)C(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4644872 177315 0 None -19 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 236 0 1 2 2.7 Cc1cc2c3c(c1Cl)C(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
10421236 188137 1 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation counting
ChEMBL 226 1 3 4 1.9 Nc1nccc(-c2c[nH]c3cccc(O)c23)n1 10.1016/j.bmc.2011.08.033
CHEMBL50498 188137 1 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation counting
ChEMBL 226 1 3 4 1.9 Nc1nccc(-c2c[nH]c3cccc(O)c23)n1 10.1016/j.bmc.2011.08.033
135367857 164041 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4215875 164041 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
145967795 164260 0 None 5 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2ccsc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4218679 164260 0 None 5 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2ccsc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
136259032 164077 16 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 205 2 1 4 2.3 O=Cc1csc(-c2ccccc2O)n1 10.1021/acs.jnatprod.7b00317
CHEMBL4216337 164077 16 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 205 2 1 4 2.3 O=Cc1csc(-c2ccccc2O)n1 10.1021/acs.jnatprod.7b00317
732268 137755 28 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 257 1 3 5 2.0 NC1=NC2(CCCCC2)NC(Nc2ccccc2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL3770837 137755 28 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 257 1 3 5 2.0 NC1=NC2(CCCCC2)NC(Nc2ccccc2)=N1 10.1021/acsmedchemlett.8b00300
127051843 140207 0 None -6 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818200 140207 0 None -6 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
1222 1626 44 None -52 33 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm100600y
3396 1626 44 None -52 33 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm100600y
85 1626 44 None -52 33 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm100600y
CHEMBL46516 1626 44 None -52 33 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm100600y
DB04842 1626 44 None -52 33 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm100600y
2801 161313 56 None -3 29 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL1200710 161313 56 None -3 29 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL415 161313 56 None -3 29 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
127051843 140207 0 None -6 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818200 140207 0 None -6 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
155543832 172630 0 None -134 7 Human 5.8 pKi = 5.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 451 6 3 7 3.4 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CCl)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL4522864 172630 0 None -134 7 Human 5.8 pKi = 5.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 451 6 3 7 3.4 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CCl)[C@H]1O 10.1021/acs.jmedchem.8b01662
11952353 198168 0 None -10 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]DOI from human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from human 5HT2B receptor expressed in CHO cells
ChEMBL 345 4 1 4 3.0 Fc1ccc(F)c(CO[C@H]2CCc3ccc(N4CCNCC4)nc32)c1 10.1016/j.bmcl.2009.10.112
CHEMBL594469 198168 0 None -10 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]DOI from human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from human 5HT2B receptor expressed in CHO cells
ChEMBL 345 4 1 4 3.0 Fc1ccc(F)c(CO[C@H]2CCc3ccc(N4CCNCC4)nc32)c1 10.1016/j.bmcl.2009.10.112
168274751 190034 0 None 2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 369 5 0 5 3.9 CCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5181312 190034 0 None 2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 369 5 0 5 3.9 CCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
11302765 83818 2 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 284 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL221113 83818 2 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 284 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
10235 2626 1 None -61 6 Human 6.8 pKi = 6.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 433 6 4 8 2.1 OC[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC(C1CCC1)C1CCC1 10.1021/acs.jmedchem.8b01662
137553161 2626 1 None -61 6 Human 6.8 pKi = 6.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 433 6 4 8 2.1 OC[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC(C1CCC1)C1CCC1 10.1021/acs.jmedchem.8b01662
CHEMBL4470080 2626 1 None -61 6 Human 6.8 pKi = 6.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 433 6 4 8 2.1 OC[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC(C1CCC1)C1CCC1 10.1021/acs.jmedchem.8b01662
CHEMBL4545807 212231 0 None - 1 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000748a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000748a HTR2B
ChEMBL None None None Cn1c(-c2csc(C3CCN(CC4=NC5N=CC=CC5N4)CC3)n2)nc2ccccc21 nan
56645363 120963 7 None -2 4 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000313b HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000313b HTR2B
ChEMBL 311 3 1 4 3.8 CC(C)(O)c1cncc(-c2nc3ccc(F)cc3n2C2CC2)c1 nan
CHEMBL3582478 120963 7 None -2 4 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000313b HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000313b HTR2B
ChEMBL 311 3 1 4 3.8 CC(C)(O)c1cncc(-c2nc3ccc(F)cc3n2C2CC2)c1 nan
136118650 75955 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058705 75955 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
44581972 175017 0 None -5 10 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458001 175017 0 None -5 10 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
136020620 57011 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 219 2 1 4 2.6 Cc1sc(-c2ccccc2O)nc1C=O 10.1021/np100588c
CHEMBL1651096 57011 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 219 2 1 4 2.6 Cc1sc(-c2ccccc2O)nc1C=O 10.1021/np100588c
142601325 185277 0 None -3 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 242 2 2 3 1.9 c1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4868035 185277 0 None -3 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 242 2 2 3 1.9 c1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
16117151 59756 0 None -154 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642882 59756 0 None -154 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739102 59756 0 None -154 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
25263297 183745 0 None -19 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2b receptorBinding affinity to 5HT2b receptor
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
CHEMBL484345 183745 0 None -19 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2b receptorBinding affinity to 5HT2b receptor
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
53483975 65268 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 364 7 0 4 4.2 COc1ccc(CCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
CHEMBL1833977 65268 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 364 7 0 4 4.2 COc1ccc(CCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
1605 2300 110 None -1 4 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
3957 2300 110 None -1 4 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
7216 2300 110 None -1 4 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
CHEMBL998 2300 110 None -1 4 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
DB00455 2300 110 None -1 4 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
168282554 190262 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 383 5 0 5 4.3 COc1cc2c(cc1OC)-c1c(OC)c(OC(C)C)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5184659 190262 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 383 5 0 5 4.3 COc1cc2c(cc1OC)-c1c(OC)c(OC(C)C)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
155530292 170918 0 None -3548 7 Human 5.8 pKi = 5.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 458 5 4 8 1.6 O=C(NC1CC1)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H]4C[C@H]5CC[C@@H]4C5)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL4463802 170918 0 None -3548 7 Human 5.8 pKi = 5.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 458 5 4 8 1.6 O=C(NC1CC1)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H]4C[C@H]5CC[C@@H]4C5)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
10151289 133047 0 None -6 3 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 434 6 0 4 4.7 O=C1N(c2ccc(OCCN3CCCCC3)nc2)CCN1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.08.004
CHEMBL371211 133047 0 None -6 3 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 434 6 0 4 4.7 O=C1N(c2ccc(OCCN3CCCCC3)nc2)CCN1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.08.004
49850872 56149 0 None -630 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 388 5 1 4 3.9 CC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1632206 56149 0 None -630 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 388 5 1 4 3.9 CC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
10830245 100941 0 None -7 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 329 1 1 2 4.6 CC(C)(C)c1cc2c(cc1Cl)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
CHEMBL297445 100941 0 None -7 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 329 1 1 2 4.6 CC(C)(C)c1cc2c(cc1Cl)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
10408409 192550 0 None -79 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 395 3 1 5 4.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cccnc3C)nn1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL52308 192550 0 None -79 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 395 3 1 5 4.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cccnc3C)nn1)CC2 10.1016/s0960-894x(00)00364-4
44298226 194801 0 None -100 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 378 3 1 4 4.6 Cc1cc2c(cc1F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL56336 194801 0 None -100 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 378 3 1 4 4.6 Cc1cc2c(cc1F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
153287542 168956 0 None -6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 265 1 1 2 3.6 C[C@@]12COc3c(-c4ccccc4)cccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4435237 168956 0 None -6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 265 1 1 2 3.6 C[C@@]12COc3c(-c4ccccc4)cccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
11237290 87515 0 None -199 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 458 6 0 4 4.7 COc1ccc(N2Cc3cccc(Br)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234109 87515 0 None -199 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 458 6 0 4 4.7 COc1ccc(N2Cc3cccc(Br)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
10413268 152123 0 None -31 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 453 6 0 5 4.9 COc1ccc(N2Cc3c(c4ccc(Cl)cc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
CHEMBL397259 152123 0 None -31 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 453 6 0 5 4.9 COc1ccc(N2Cc3c(c4ccc(Cl)cc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
44420682 137070 0 None -3 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 0 2 2.1 CN1CCN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2C1 10.1021/jm0612968
CHEMBL375642 137070 0 None -3 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 0 2 2.1 CN1CCN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2C1 10.1021/jm0612968
162647275 178972 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 294 4 1 3 4.0 Cc1ccc(CCCc2cc(=O)c3c(O)cccc3o2)cc1 10.1016/j.bmcl.2020.127511
CHEMBL4741776 178972 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 294 4 1 3 4.0 Cc1ccc(CCCc2cc(=O)c3c(O)cccc3o2)cc1 10.1016/j.bmcl.2020.127511
10150393 71550 0 None -398 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 373 7 0 4 3.2 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCN(C)C 10.1016/j.bmcl.2005.08.004
CHEMBL197170 71550 0 None -398 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 373 7 0 4 3.2 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCN(C)C 10.1016/j.bmcl.2005.08.004
10479309 79322 0 None -79 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 458 8 0 5 4.7 COc1ccc(N2CCC(c3ccc(OC)c(OCCN4CCCCC4)c3)C2=O)cc1Cl 10.1016/j.bmcl.2006.05.034
CHEMBL211719 79322 0 None -79 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 458 8 0 5 4.7 COc1ccc(N2CCC(c3ccc(OC)c(OCCN4CCCCC4)c3)C2=O)cc1Cl 10.1016/j.bmcl.2006.05.034
44414217 79718 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 516 7 0 4 6.3 O=C1C(c2ccc(Cl)c(Cl)c2)CCN1c1ccc(OC(F)(F)F)c(OCCN2CCCCC2)c1 10.1016/j.bmcl.2006.05.034
CHEMBL213368 79718 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 516 7 0 4 6.3 O=C1C(c2ccc(Cl)c(Cl)c2)CCN1c1ccc(OC(F)(F)F)c(OCCN2CCCCC2)c1 10.1016/j.bmcl.2006.05.034
24887284 141202 0 None -125 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 462 7 0 4 5.4 COc1ccc(N2CCC(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL385921 141202 0 None -125 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 462 7 0 4 5.4 COc1ccc(N2CCC(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
24888183 141275 0 None -1000 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 420 7 0 4 4.5 COc1ccc(N2CC=C(c3ccc(C)cc3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
CHEMBL386332 141275 0 None -1000 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 420 7 0 4 4.5 COc1ccc(N2CC=C(c3ccc(C)cc3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
10296414 3462 11 None -1258 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
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 -1258 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
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 -1258 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2006.11.031
11248705 89850 0 None -630 10 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
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 -630 10 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
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
91826739 121486 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 282 4 1 4 3.2 O=c1cc(COCc2ccccc2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
CHEMBL3593952 121486 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 282 4 1 4 3.2 O=c1cc(COCc2ccccc2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
168271856 189957 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 381 6 0 5 4.0 C=CCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5180016 189957 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 381 6 0 5 4.0 C=CCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
44572166 12339 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
CHEMBL1186133 12339 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
CHEMBL451232 12339 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
44572751 12378 1 None 4 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL1186509 12378 1 None 4 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL467736 12378 1 None 4 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
127026052 137015 0 None 4 19 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754496 137015 0 None 4 19 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
145989551 166574 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 297 3 0 2 4.1 CN(C)CC/C=C1\c2ccc(F)cc2COc2ccccc21 10.1021/acsmedchemlett.8b00300
CHEMBL4290607 166574 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 297 3 0 2 4.1 CN(C)CC/C=C1\c2ccc(F)cc2COc2ccccc21 10.1021/acsmedchemlett.8b00300
70687202 77609 0 None -10 3 Human 6.8 pKi = 6.8 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@@H]1CNC[C@@H]2Cc3ccccc3N21 10.1016/j.bmcl.2005.05.074
CHEMBL2096809 77609 0 None -10 3 Human 6.8 pKi = 6.8 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@@H]1CNC[C@@H]2Cc3ccccc3N21 10.1016/j.bmcl.2005.05.074
11231392 84456 0 None -13 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 246 2 1 3 1.6 CC(C)Oc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL223628 84456 0 None -13 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 246 2 1 3 1.6 CC(C)Oc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
11080 28857 74 None -6 6 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 28857 74 None -6 6 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
59652086 114081 0 None -85 2 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000726a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000726a HTR2B
ChEMBL 448 8 2 6 3.6 COc1cccc(CNC(=O)c2nc3scc(CN(C)Cc4ccccc4)c3c(=O)[nH]2)c1 nan
CHEMBL3337895 114081 0 None -85 2 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000726a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000726a HTR2B
ChEMBL 448 8 2 6 3.6 COc1cccc(CNC(=O)c2nc3scc(CN(C)Cc4ccccc4)c3c(=O)[nH]2)c1 nan
49865833 15973 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 296 1 1 3 3.2 O=C(Nc1ccccc1)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224036 15973 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 296 1 1 3 3.2 O=C(Nc1ccccc1)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
14702424 18362 61 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 176 2 2 2 1.6 COc1ccc2[nH]cc(CN)c2c1 10.1021/jm100600y
CHEMBL1276050 18362 61 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 176 2 2 2 1.6 COc1ccc2[nH]cc(CN)c2c1 10.1021/jm100600y
71462776 82536 0 None -134 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181169 82536 0 None -134 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
136118659 75887 0 None 1 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058427 75887 0 None 1 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
21527771 69798 0 None -645 10 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940404 69798 0 None -645 10 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
134135745 143834 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 407 6 4 8 1.6 CC(C)[C@@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
CHEMBL3905850 143834 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 407 6 4 8 1.6 CC(C)[C@@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
134156506 153517 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 407 6 4 8 1.6 CC(C)[C@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
CHEMBL3984645 153517 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 407 6 4 8 1.6 CC(C)[C@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
58911666 90646 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
CHEMBL2397886 90646 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
25120700 80813 0 None 5 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
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 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
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
45486820 195249 0 None -12 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 432 3 2 4 3.8 O=c1[nH]c2cccc(N3C[C@H]4C[C@@H]3CN4CC3CCc4[nH]c5ccc(F)cc5c4C3)c2o1 10.1016/j.bmcl.2009.08.050
CHEMBL1237149 195249 0 None -12 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 432 3 2 4 3.8 O=c1[nH]c2cccc(N3C[C@H]4C[C@@H]3CN4CC3CCc4[nH]c5ccc(F)cc5c4C3)c2o1 10.1016/j.bmcl.2009.08.050
CHEMBL566356 195249 0 None -12 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 432 3 2 4 3.8 O=c1[nH]c2cccc(N3C[C@H]4C[C@@H]3CN4CC3CCc4[nH]c5ccc(F)cc5c4C3)c2o1 10.1016/j.bmcl.2009.08.050
71062768 143192 0 None -4 4 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
CHEMBL3900699 143192 0 None -4 4 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
3151 1429 93 None -125 27 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
945 1429 93 None -125 27 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
965 1429 93 None -125 27 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
CHEMBL219916 1429 93 None -125 27 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
DB01184 1429 93 None -125 27 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
44409317 140814 0 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 267 0 1 3 1.6 C[C@@H]1CNC[C@@H]2Cc3ccc(Br)nc3N21 10.1016/j.bmcl.2005.11.083
CHEMBL383694 140814 0 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 267 0 1 3 1.6 C[C@@H]1CNC[C@@H]2Cc3ccc(Br)nc3N21 10.1016/j.bmcl.2005.11.083
46884102 7964 0 None -912 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 366 5 2 3 3.7 CC1(C)CCC(Oc2cc(F)c(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
CHEMBL1091106 7964 0 None -912 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 366 5 2 3 3.7 CC1(C)CCC(Oc2cc(F)c(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
135501716 75945 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2ccc(Br)cc12 10.1016/j.bmc.2013.09.011
CHEMBL2058695 75945 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2ccc(Br)cc12 10.1016/j.bmc.2013.09.011
49783419 17552 0 None -501 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258671 17552 0 None -501 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
118055288 176452 0 None -58 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 256 0 1 2 3.0 CC1CN2CCNCc3cc(Cl)c(Cl)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4632473 176452 0 None -58 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 256 0 1 2 3.0 CC1CN2CCNCc3cc(Cl)c(Cl)c1c32 10.1016/j.bmcl.2019.126929
25209356 179195 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 544 7 2 8 4.0 COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCNCC5)c(Cl)c4=O)c3C)cc2)cn1 10.1021/jm800962k
CHEMBL474473 179195 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 544 7 2 8 4.0 COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCNCC5)c(Cl)c4=O)c3C)cc2)cn1 10.1021/jm800962k
127051015 140330 0 None -63 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818128 140330 0 None -63 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819731 140330 0 None -63 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
24826957 90672 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 246 1 1 3 1.0 COc1ccc(C)c2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397912 90672 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 246 1 1 3 1.0 COc1ccc(C)c2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
127049983 140118 0 None 7 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2cccc(Cl)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3814821 140118 0 None 7 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2cccc(Cl)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
127037093 135972 0 None 40 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 433 11 0 5 4.8 COc1ccc(CCN(CCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3736252 135972 0 None 40 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 433 11 0 5 4.8 COc1ccc(CCN(CCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
44435193 90780 0 None 1 7 Human 6.8 pKi = 6.8 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 331 2 0 2 5.6 CC(C(=O)N1c2ccccc2Sc2ccccc21)c1ccccc1 10.1016/j.bmcl.2013.04.082
CHEMBL240045 90780 0 None 1 7 Human 6.8 pKi = 6.8 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 331 2 0 2 5.6 CC(C(=O)N1c2ccccc2Sc2ccccc21)c1ccccc1 10.1016/j.bmcl.2013.04.082
CHEMBL5083607 213091 0 None -14 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCN(C)C2)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL5093342 213778 0 None -19 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095971 213778 0 None -19 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
162647063 179058 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 499 6 4 8 1.6 CC(C)[C@@H](Nc1nc(I)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1016/j.bmcl.2020.127599
CHEMBL4743059 179058 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 499 6 4 8 1.6 CC(C)[C@@H](Nc1nc(I)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1016/j.bmcl.2020.127599
162646751 179152 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 419 7 4 9 1.7 CSc1nc(N[C@H](C(C)C)C2CC2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@]4(CO)C[C@H]34)c2n1 10.1016/j.bmcl.2020.127599
CHEMBL4744176 179152 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 419 7 4 9 1.7 CSc1nc(N[C@H](C(C)C)C2CC2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@]4(CO)C[C@H]34)c2n1 10.1016/j.bmcl.2020.127599
90469115 185250 2 None -56 17 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B 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 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
67978437 120152 0 None -85 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 257 2 0 1 4.2 CN(C)[C@H]1Cc2ccccc2[C@H](C2CCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402657 120152 0 None -85 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 257 2 0 1 4.2 CN(C)[C@H]1Cc2ccccc2[C@H](C2CCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547010 120152 0 None -85 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 257 2 0 1 4.2 CN(C)[C@H]1Cc2ccccc2[C@H](C2CCCCC2)C1 10.1016/j.bmc.2015.01.060
44404887 133893 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 340 8 2 4 3.0 CCCCn1cc(CCN(C)C)c2c(OP(=O)(O)O)cccc21 10.1016/j.bmcl.2005.06.104
CHEMBL371753 133893 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 340 8 2 4 3.0 CCCCn1cc(CCN(C)C)c2c(OP(=O)(O)O)cccc21 10.1016/j.bmcl.2005.06.104
127051015 140330 0 None -63 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818128 140330 0 None -63 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819731 140330 0 None -63 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
11652359 88685 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 264 1 1 2 2.0 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1N(C)C2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337502 88685 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 264 1 1 2 2.0 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1N(C)C2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365706 88685 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 264 1 1 2 2.0 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1N(C)C2=O 10.1016/j.bmcl.2012.10.091
45279963 80482 48 None 21 2 Human 6.8 pKi = 6.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000717a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000717a HTR2B
ChEMBL 425 6 3 5 3.8 O=C1c2ccc(Nc3ccc(F)cc3F)cc2CCc2ccc(OC[C@H](O)CO)cc21 nan
CHEMBL2152944 80482 48 None 21 2 Human 6.8 pKi = 6.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000717a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000717a HTR2B
ChEMBL 425 6 3 5 3.8 O=C1c2ccc(Nc3ccc(F)cc3F)cc2CCc2ccc(OC[C@H](O)CO)cc21 nan
46884101 7962 0 None -87 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 310 6 2 3 2.6 O=C(NCc1ccc(OCc2ccccc2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1091104 7962 0 None -87 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 310 6 2 3 2.6 O=C(NCc1ccc(OCc2ccccc2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
25263302 191377 0 None -134 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2b receptorBinding affinity to 5HT2b receptor
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
CHEMBL520129 191377 0 None -134 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2b receptorBinding affinity to 5HT2b receptor
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
44409290 74287 0 None -45 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 273 4 1 4 1.7 C[C@@H]1CNC[C@H]2Cc3ccc(COCC4CC4)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL203013 74287 0 None -45 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 273 4 1 4 1.7 C[C@@H]1CNC[C@H]2Cc3ccc(COCC4CC4)nc3N12 10.1016/j.bmcl.2005.11.083
16117279 59805 0 None -1778 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642886 59805 0 None -1778 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739606 59805 0 None -1778 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
57799326 88665 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 242 1 2 2 1.7 Cc1cc(C2CC2)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337104 88665 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 242 1 2 2 1.7 Cc1cc(C2CC2)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365468 88665 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 242 1 2 2 1.7 Cc1cc(C2CC2)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
145988693 166602 0 None -7 17 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4291048 166602 0 None -7 17 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
153287572 172840 0 None 11 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 205 1 1 2 2.6 CC[C@H]1c2cc(C)ccc2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4528651 172840 0 None 11 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 205 1 1 2 2.6 CC[C@H]1c2cc(C)ccc2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
49865887 15990 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 302 1 1 3 3.0 O=C(NC1CCCCC1)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224103 15990 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 302 1 1 3 3.0 O=C(NC1CCCCC1)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
1227 2444 35 None -112 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
2331 2444 35 None -112 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
3957 2444 35 None -112 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
4992 2444 35 None -112 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
CHEMBL511 2444 35 None -112 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
DB06691 2444 35 None -112 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
118055202 176610 0 None -12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 236 0 1 2 2.5 CC1(C)CN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4635105 176610 0 None -12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 236 0 1 2 2.5 CC1(C)CN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
118055282 177430 0 None -22 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 334 1 1 2 3.4 FC(F)(F)CC1CN2CCNCc3ccc(Br)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4646572 177430 0 None -22 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 334 1 1 2 3.4 FC(F)(F)CC1CN2CCNCc3ccc(Br)c1c32 10.1016/j.bmcl.2019.126929
157 2030 5 None -134 5 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
9840090 2030 5 None -134 5 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
CHEMBL134519 2030 5 None -134 5 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
46230049 199850 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 237 0 2 3 0.8 O=C1NC2CNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
CHEMBL605402 199850 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 237 0 2 3 0.8 O=C1NC2CNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
18715564 73018 0 None -7 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 259 2 1 3 3.2 C[C@H](N)Cn1ccc2cc(Cl)c3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201454 73018 0 None -7 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 259 2 1 3 3.2 C[C@H](N)Cn1ccc2cc(Cl)c3ncccc3c21 10.1016/j.bmcl.2005.10.029
127053028 140098 0 None 8 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 573 12 0 5 5.8 COc1ccc(CCN(CCCc2cccc(I)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3814559 140098 0 None 8 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 573 12 0 5 5.8 COc1ccc(CCN(CCCc2cccc(I)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
127049982 140122 0 None 9 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2cccc(F)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3815000 140122 0 None 9 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2cccc(F)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
16115517 84400 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 246 2 1 3 1.4 CCc1ccc2c(c1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL223468 84400 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 246 2 1 3 1.4 CCc1ccc2c(c1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
23151712 120012 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 266 1 3 2 1.1 NC(N)=NC(=O)c1ccc2c(c1)C(N)c1ccccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310120 120012 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 266 1 3 2 1.1 NC(N)=NC(=O)c1ccc2c(c1)C(N)c1ccccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545471 120012 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 266 1 3 2 1.1 NC(N)=NC(=O)c1ccc2c(c1)C(N)c1ccccc1-2 10.1016/j.bmc.2014.05.027
157 2030 5 None -134 5 Human 7.8 pKi = 7.8 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm030205t
9840090 2030 5 None -134 5 Human 7.8 pKi = 7.8 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm030205t
CHEMBL134519 2030 5 None -134 5 Human 7.8 pKi = 7.8 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm030205t
49862237 14823 0 None -11 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 395 6 0 5 4.3 COc1ccc(OC)c(C2CCN(Cc3cnn(-c4ccccc4F)c3C)C2)c1 10.1016/j.bmcl.2010.06.033
CHEMBL1209157 14823 0 None -11 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 395 6 0 5 4.3 COc1ccc(OC)c(C2CCN(Cc3cnn(-c4ccccc4F)c3C)C2)c1 10.1016/j.bmcl.2010.06.033
1524 2141 89 None -234 52 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
197 2141 89 None -234 52 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
3822 2141 89 None -234 52 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
88 2141 89 None -234 52 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
CHEMBL51 2141 89 None -234 52 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
DB12465 2141 89 None -234 52 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
118055199 177371 0 None -33 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 202 0 1 2 1.9 CC1(C)CN2CCNCc3cccc1c32 10.1016/j.bmcl.2019.126929
CHEMBL4645774 177371 0 None -33 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 202 0 1 2 1.9 CC1(C)CN2CCNCc3cccc1c32 10.1016/j.bmcl.2019.126929
44409124 74105 0 None -30 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 214 0 1 4 0.7 C[C@@H]1CNC[C@H]2Cc3ccc(C#N)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL202795 74105 0 None -30 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 214 0 1 4 0.7 C[C@@H]1CNC[C@H]2Cc3ccc(C#N)nc3N12 10.1016/j.bmcl.2005.11.083
46914777 15254 0 None 18 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 382 8 0 4 4.5 FCCCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
CHEMBL1215038 15254 0 None 18 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 382 8 0 4 4.5 FCCCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
33630 178369 94 None -6 28 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 178369 94 None -6 28 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
44582677 180981 0 None -70 4 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 432 10 1 6 3.9 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476838 180981 0 None -70 4 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 432 10 1 6 3.9 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmc.2009.03.021
71061729 160384 0 None -1 4 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4115493 160384 0 None -1 4 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
25117679 198910 0 None -8 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599263 198910 0 None -8 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
142601318 184953 0 None -12 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 272 3 2 4 1.9 COc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4863036 184953 0 None -12 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 272 3 2 4 1.9 COc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
134138183 147266 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 393 6 4 8 1.4 CC[C@@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
CHEMBL3932820 147266 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 393 6 4 8 1.4 CC[C@@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
155567457 175366 0 None -158 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assay
ChEMBL 359 2 3 6 2.8 O[C@H]1CCC[C@@H]1Nc1nc(C#Cc2ccc(Cl)s2)nc2[nH]cnc12 10.1039/C8MD00317C
CHEMBL4587951 175366 0 None -158 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assay
ChEMBL 359 2 3 6 2.8 O[C@H]1CCC[C@@H]1Nc1nc(C#Cc2ccc(Cl)s2)nc2[nH]cnc12 10.1039/C8MD00317C
46914926 15242 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 382 8 0 4 4.5 FCCCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
CHEMBL1214960 15242 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 382 8 0 4 4.5 FCCCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
11579853 88642 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337504 88642 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365200 88642 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
119584 2547 99 None 1 6 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
1848 2547 99 None 1 6 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
242 2547 99 None 1 6 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
CHEMBL60889 2547 99 None 1 6 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
DB11675 2547 99 None 1 6 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
CHEMBL4750687 212268 0 None - 1 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000312b HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000312b HTR2B
ChEMBL None None None Cc1ncc(-c2cc(Cl)ccc2F)cc1-n1c(=O)n(CC(N)=O)c2cnccc21 nan
CHEMBL4741904 212266 0 None - 1 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000710a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000710a HTR2B
ChEMBL None None None Cc1ncc(-c2cc(Cl)ccc2F)cc1-n1c(=O)n(CC(N)=O)c2ccccc21 nan
44316027 203801 0 None -12 3 Human 6.7 pKi = 6.7 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 236 4 1 3 2.5 CCSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
CHEMBL80862 203801 0 None -12 3 Human 6.7 pKi = 6.7 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 236 4 1 3 2.5 CCSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
11658860 2302 47 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
2941 2302 47 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
4374 2302 47 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
CHEMBL360328 2302 47 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
DB04871 2302 47 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
CHEMBL5074880 212558 0 None -1 9 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
9899500 67532 0 None -14 3 Human 7.7 pKi = 7.7 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](CNC[C@H]1C)C2 10.1016/j.bmcl.2005.05.074
CHEMBL191054 67532 0 None -14 3 Human 7.7 pKi = 7.7 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](CNC[C@H]1C)C2 10.1016/j.bmcl.2005.05.074
11391654 179933 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 273 2 1 3 3.0 CC(C)n1nc2c(c1-c1ccc(F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4753511 179933 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 273 2 1 3 3.0 CC(C)n1nc2c(c1-c1ccc(F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
24873384 182009 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 255 2 1 3 2.8 CC(C)n1nc2c(c1-c1ccccc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4788223 182009 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 255 2 1 3 2.8 CC(C)n1nc2c(c1-c1ccccc1)CCNCC2 10.1016/j.bmcl.2020.127669
134154065 151817 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 433 6 3 9 1.5 COC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3970041 151817 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 433 6 3 9 1.5 COC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
11020695 25295 1 None -38 4 Human 7.7 pKi = 7.7 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL135076 25295 1 None -38 4 Human 7.7 pKi = 7.7 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
879244 27973 7 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 271 1 3 5 2.3 Cc1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acsmedchemlett.8b00300
CHEMBL1373650 27973 7 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 271 1 3 5 2.3 Cc1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acsmedchemlett.8b00300
10791286 35076 0 None -9 2 Human 7.7 pKi = 7.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 491 3 1 3 6.1 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(Br)cc(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL14368 35076 0 None -9 2 Human 7.7 pKi = 7.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 491 3 1 3 6.1 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(Br)cc(-c3cccnc3)c1)CC2 10.1021/jm990388c
10526616 39254 0 None -15 3 Human 7.7 pKi = 7.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 430 4 1 5 4.9 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3)nc1)CC2 10.1021/jm990388c
CHEMBL14726 39254 0 None -15 3 Human 7.7 pKi = 7.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 430 4 1 5 4.9 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3)nc1)CC2 10.1021/jm990388c
44298229 101441 0 None -31 3 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.8 Cc1cc2c(cc1Cl)N(C(=O)Nc1cnc(Oc3cccnc3C)c(Cl)c1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL301012 101441 0 None -31 3 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.8 Cc1cc2c(cc1Cl)N(C(=O)Nc1cnc(Oc3cccnc3C)c(Cl)c1)CC2 10.1016/s0960-894x(00)00364-4
147653864 170985 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 267 0 1 2 2.7 C[C@@]12COc3c(Br)cccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4464697 170985 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 267 0 1 2 2.7 C[C@@]12COc3c(Br)cccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
153061504 172231 0 None 15 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2c(ccc3ccccc23)OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4513930 172231 0 None 15 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2c(ccc3ccccc23)OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
2389 3267 114 None -79 68 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
5073 3267 114 None -79 68 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
96 3267 114 None -79 68 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
CHEMBL85 3267 114 None -79 68 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
DB00734 3267 114 None -79 68 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
2267 553 64 None -10 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
271 553 64 None -10 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
7121 553 64 None -10 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
CHEMBL639 553 64 None -10 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
DB00972 553 64 None -10 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
44298118 192798 0 None -1 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 5 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL52592 192798 0 None -1 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 5 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
12017599 194101 0 None -6 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 426 4 1 3 5.2 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(CCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL55784 194101 0 None -6 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 426 4 1 3 5.2 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(CCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
72698088 103499 0 None -954 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT2BBinding affinity to human 5HT2B
ChEMBL 421 6 0 4 5.4 Fc1cccc2c1nc(OCC1CCN(CCCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
CHEMBL3093187 103499 0 None -954 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT2BBinding affinity to human 5HT2B
ChEMBL 421 6 0 4 5.4 Fc1cccc2c1nc(OCC1CCN(CCCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
11175045 136005 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 298 1 1 2 2.9 CC(C)c1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL373695 136005 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 298 1 1 2 2.9 CC(C)c1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
135474338 188672 0 None 10 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL511879 188672 0 None 10 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
54761054 137540 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Positive allosteric modulation of 5-HT2B receptor (unknown origin)Positive allosteric modulation of 5-HT2B receptor (unknown origin)
ChEMBL 367 3 1 5 4.0 Cc1ccc(C(C)(C)O)cc1-c1ccc2c(n1)n(C)c(=O)n2CC(C)(C)C 10.1016/j.bmcl.2016.01.021
CHEMBL3765778 137540 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Positive allosteric modulation of 5-HT2B receptor (unknown origin)Positive allosteric modulation of 5-HT2B receptor (unknown origin)
ChEMBL 367 3 1 5 4.0 Cc1ccc(C(C)(C)O)cc1-c1ccc2c(n1)n(C)c(=O)n2CC(C)(C)C 10.1016/j.bmcl.2016.01.021
134149168 147702 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 297 2 0 2 3.6 CN1CC[C@H]2CC(=O)[C@H](Cc3ccccc3)[C@H]3CCC[C@@H]1[C@H]23 10.1016/j.bmcl.2016.10.065
CHEMBL3936289 147702 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 297 2 0 2 3.6 CN1CC[C@H]2CC(=O)[C@H](Cc3ccccc3)[C@H]3CCC[C@@H]1[C@H]23 10.1016/j.bmcl.2016.10.065
11499800 88664 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337503 88664 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365465 88664 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
25117680 198941 0 None -13 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599466 198941 0 None -13 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
155536619 171625 0 None -75 4 Human 5.7 pKi = 5.7 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 254 3 4 7 -2.3 NC(=O)c1ncn([C@H]2[C@H](O)[C@H](O)[C@]3(CO)C[C@H]23)n1 10.1021/acs.jmedchem.8b01662
CHEMBL4473739 171625 0 None -75 4 Human 5.7 pKi = 5.7 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 254 3 4 7 -2.3 NC(=O)c1ncn([C@H]2[C@H](O)[C@H](O)[C@]3(CO)C[C@H]23)n1 10.1021/acs.jmedchem.8b01662
122178710 120849 0 None -8 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 431 6 0 5 5.0 COc1cc2c(cc1OCc1ccccc1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
CHEMBL3581255 120849 0 None -8 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 431 6 0 5 5.0 COc1cc2c(cc1OCc1ccccc1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
11290492 137461 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 218 1 1 3 0.8 COc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL376456 137461 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 218 1 1 3 0.8 COc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
5318 15385 44 None -1 13 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 15385 44 None -1 13 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 15385 44 None -1 13 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
1531 2226 64 None -16 15 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
3869 2226 64 None -16 15 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
7207 2226 64 None -16 15 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
CHEMBL429 2226 64 None -16 15 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
DB00598 2226 64 None -16 15 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
124 2921 44 None -181 33 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2921 44 None -181 33 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2921 44 None -181 33 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2921 44 None -181 33 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2921 44 None -181 33 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
11416698 90662 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397902 90662 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
73349359 92097 0 None -2 8 Human 5.7 pKi = 5.7 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 341 6 1 4 2.9 COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432051 92097 0 None -2 8 Human 5.7 pKi = 5.7 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 341 6 1 4 2.9 COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
44582708 186246 0 None -12 6 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 415 10 0 5 4.2 COc1ccc(CCN2CCC(C(=O)c3cccc(OCCF)c3OC)CC2)cc1 10.1016/j.bmc.2009.03.021
CHEMBL489408 186246 0 None -12 6 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 415 10 0 5 4.2 COc1ccc(CCN2CCC(C(=O)c3cccc(OCCF)c3OC)CC2)cc1 10.1016/j.bmc.2009.03.021
3191 102372 93 None -7 25 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102372 93 None -7 25 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
44414251 77704 0 None -158 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 470 7 0 4 4.8 COc1ccc(N2CC=C(c3ccc(Br)cc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL210053 77704 0 None -158 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 470 7 0 4 4.8 COc1ccc(N2CC=C(c3ccc(Br)cc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
44414070 79495 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 474 7 0 4 5.7 COc1ccc(C2=C(C)CN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL212482 79495 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 474 7 0 4 5.7 COc1ccc(C2=C(C)CN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
49850672 56077 0 None -794 9 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 404 5 1 5 4.1 COC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1631532 56077 0 None -794 9 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 404 5 1 5 4.1 COC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
44298021 193081 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 422 4 1 4 5.9 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cccnc3C(C)C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL53793 193081 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 422 4 1 4 5.9 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cccnc3C(C)C)nc1)CC2 10.1016/s0960-894x(00)00364-4
18931377 204739 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 578 11 3 8 3.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1cccc(Cl)c1 10.1016/S0960-894X(96)00503-3
CHEMBL88193 204739 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 578 11 3 8 3.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1cccc(Cl)c1 10.1016/S0960-894X(96)00503-3
18931150 205091 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 393 7 2 5 2.4 COc1cc(Cl)ccc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
CHEMBL90470 205091 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 393 7 2 5 2.4 COc1cc(Cl)ccc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
153287566 170604 0 None -74 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 278 1 0 2 4.0 CN1CC[C@H]2c3ccccc3N(c3ccccc3)C[C@]21C 10.1021/acsmedchemlett.9b00225
CHEMBL4459009 170604 0 None -74 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 278 1 0 2 4.0 CN1CC[C@H]2c3ccccc3N(c3ccccc3)C[C@]21C 10.1021/acsmedchemlett.9b00225
11292350 87499 0 None -79 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 394 6 0 4 4.3 COc1ccc(N2Cc3cccc(C)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234006 87499 0 None -79 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 394 6 0 4 4.3 COc1ccc(N2Cc3cccc(C)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
11775262 87613 0 None -125 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234532 87613 0 None -125 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
11430311 149503 0 None -158 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 428 6 0 4 5.2 COc1ccc(N2C(=O)c3c(Cl)cccc3C2C)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL395059 149503 0 None -158 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 428 6 0 4 5.2 COc1ccc(N2C(=O)c3c(Cl)cccc3C2C)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
11453704 149522 0 None -79 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.4 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCCCCC1 10.1016/j.bmcl.2006.10.029
CHEMBL395072 149522 0 None -79 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.4 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCCCCC1 10.1016/j.bmcl.2006.10.029
11282335 149778 0 None -39 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3cc(Cl)c(Cl)cc3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL395297 149778 0 None -39 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3cc(Cl)c(Cl)cc3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
11753782 12682 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 419 6 0 5 4.2 COc1ccc(N2Cc3c(c4ccccc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
CHEMBL1188213 12682 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 419 6 0 5 4.2 COc1ccc(N2Cc3c(c4ccccc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
CHEMBL535626 12682 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 419 6 0 5 4.2 COc1ccc(N2Cc3c(c4ccccc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
10458785 86321 0 None -50 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 467 6 0 5 5.1 COc1ccc(N2Cc3c(c4ccc(Cl)cc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
CHEMBL232045 86321 0 None -50 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 467 6 0 5 5.1 COc1ccc(N2Cc3c(c4ccc(Cl)cc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
10346749 87965 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 487 6 0 5 5.5 COc1ccc(N2Cc3c(c4cc(Cl)c(Cl)cc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
CHEMBL234947 87965 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 487 6 0 5 5.5 COc1ccc(N2Cc3c(c4cc(Cl)c(Cl)cc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
10390089 141817 0 None -125 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 436 6 0 5 5.2 COc1ccc(N2Cc3sc4ccccc4c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
CHEMBL388882 141817 0 None -125 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 436 6 0 5 5.2 COc1ccc(N2Cc3sc4ccccc4c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
44298138 193819 0 None -39 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 428 4 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(COc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL55344 193819 0 None -39 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 428 4 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(COc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
162660908 180828 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 294 4 1 3 4.0 Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
CHEMBL4763861 180828 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 294 4 1 3 4.0 Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
162669225 182172 0 None - 1 Human 5.7 pKi = 5.7 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 314 4 1 3 4.3 O=c1cc(CCCc2cccc(Cl)c2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
CHEMBL4790230 182172 0 None - 1 Human 5.7 pKi = 5.7 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 314 4 1 3 4.3 O=c1cc(CCCc2cccc(Cl)c2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
10812577 98575 0 None 1 3 Human 5.7 pKi = 5.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 431 3 1 3 5.5 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(-c3cccnc3)ccc1F)CC2 10.1021/jm990388c
CHEMBL280322 98575 0 None 1 3 Human 5.7 pKi = 5.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 431 3 1 3 5.5 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(-c3cccnc3)ccc1F)CC2 10.1021/jm990388c
10249573 205849 0 None -199 11 Human 5.7 pKi = 5.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
CHEMBL94984 205849 0 None -199 11 Human 5.7 pKi = 5.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
10237852 72044 0 None -316 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 411 7 0 6 3.6 COc1ccc(-n2ccn(-c3cccc(F)c3)c2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
CHEMBL198712 72044 0 None -316 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 411 7 0 6 3.6 COc1ccc(-n2ccn(-c3cccc(F)c3)c2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
24887517 168462 0 None -158 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 476 7 0 4 5.6 COc1ccc(N2CCC(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
CHEMBL439504 168462 0 None -158 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 476 7 0 4 5.6 COc1ccc(N2CCC(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
11191906 11647 0 None -39 12 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181665 11647 0 None -39 12 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL187928 11647 0 None -39 12 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
44298079 194639 0 None -19 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 346 3 1 4 4.2 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3ccccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL56232 194639 0 None -19 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 346 3 1 4 4.2 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3ccccc32)cn1 10.1016/s0960-894x(00)00364-4
44298193 197687 0 None -316 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 380 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Cl)ccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL59097 197687 0 None -316 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 380 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Cl)ccc32)cn1 10.1016/s0960-894x(00)00364-4
10433930 50801 0 None -999 5 Human 5.7 pKi = 5.7 Binding
Compound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligandCompound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligand
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157910 50801 0 None -999 5 Human 5.7 pKi = 5.7 Binding
Compound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligandCompound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligand
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
118278424 121485 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 256 3 1 4 2.9 O=c1cc(CCc2ccco2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
CHEMBL3593951 121485 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 256 3 1 4 2.9 O=c1cc(CCc2ccco2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
24865725 187491 0 None -3981 12 Human 5.7 pKi = 5.7 Binding
Displacement of radioligand from human cloned 5HT2B receptorDisplacement of radioligand from human cloned 5HT2B receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL497963 187491 0 None -3981 12 Human 5.7 pKi = 5.7 Binding
Displacement of radioligand from human cloned 5HT2B receptorDisplacement of radioligand from human cloned 5HT2B receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
9892409 100470 0 None -398 9 Human 5.7 pKi = 5.7 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 505 5 1 6 5.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCCCC2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29410 100470 0 None -398 9 Human 5.7 pKi = 5.7 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 505 5 1 6 5.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCCCC2C1 10.1016/s0960-894x(02)00172-5
448537 159691 86 None -21 25 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 159691 86 None -21 25 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
11957541 1425 38 None -2 16 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
1229 1425 38 None -2 16 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
147 1425 38 None -2 16 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
170617 1425 38 None -2 16 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
CHEMBL6616 1425 38 None -2 16 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
11957541 1425 38 None -2 16 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)-DOI from human 5HT2B receptorDisplacement of [125I](+/-)-DOI from human 5HT2B receptor
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm2006782
1229 1425 38 None -2 16 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)-DOI from human 5HT2B receptorDisplacement of [125I](+/-)-DOI from human 5HT2B receptor
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm2006782
147 1425 38 None -2 16 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)-DOI from human 5HT2B receptorDisplacement of [125I](+/-)-DOI from human 5HT2B receptor
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm2006782
170617 1425 38 None -2 16 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)-DOI from human 5HT2B receptorDisplacement of [125I](+/-)-DOI from human 5HT2B receptor
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm2006782
CHEMBL6616 1425 38 None -2 16 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)-DOI from human 5HT2B receptorDisplacement of [125I](+/-)-DOI from human 5HT2B receptor
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm2006782
24826867 90650 0 None 3 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397890 90650 0 None 3 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
11323169 179377 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 269 2 1 3 3.1 Cc1ccc(-c2c3c(nn2C(C)C)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4746737 179377 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 269 2 1 3 3.1 Cc1ccc(-c2c3c(nn2C(C)C)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
2220 3073 78 None -1 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1016/j.bmc.2013.10.010
27400 3073 78 None -1 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1016/j.bmc.2013.10.010
93 3073 78 None -1 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1016/j.bmc.2013.10.010
CHEMBL294951 3073 78 None -1 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1016/j.bmc.2013.10.010
DB06153 3073 78 None -1 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1016/j.bmc.2013.10.010
118717217 120052 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 325 4 2 3 1.6 COCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343667 120052 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 325 4 2 3 1.6 COCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545762 120052 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 325 4 2 3 1.6 COCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
72734862 105812 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 253 1 2 2 2.0 NC(N)=NC(=O)c1ccc2c(c1)oc1ccccc12 10.1016/j.bmc.2013.10.010
CHEMBL3092754 105812 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 253 1 2 2 2.0 NC(N)=NC(=O)c1ccc2c(c1)oc1ccccc12 10.1016/j.bmc.2013.10.010
CHEMBL3139079 105812 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 253 1 2 2 2.0 NC(N)=NC(=O)c1ccc2c(c1)oc1ccccc12 10.1016/j.bmc.2013.10.010
44269058 31136 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 425 6 2 4 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL14022 31136 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 425 6 2 4 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/ml3003814
157 2030 5 None -134 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/acs.jmedchem.1c00726
9840090 2030 5 None -134 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/acs.jmedchem.1c00726
CHEMBL134519 2030 5 None -134 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/acs.jmedchem.1c00726
1043 1545 13 None -22 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -22 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -22 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -22 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -22 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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
10251906 67426 14 None -186 8 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constant by liquid scintillation counter analysisBinding affinity to 5-HT2B (unknown origin) assessed as inhibition constant by liquid scintillation counter analysis
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1021/acs.jmedchem.2c00633
CHEMBL1908863 67426 14 None -186 8 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constant by liquid scintillation counter analysisBinding affinity to 5-HT2B (unknown origin) assessed as inhibition constant by liquid scintillation counter analysis
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1021/acs.jmedchem.2c00633
CHEMBL482496 67426 14 None -186 8 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constant by liquid scintillation counter analysisBinding affinity to 5-HT2B (unknown origin) assessed as inhibition constant by liquid scintillation counter analysis
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1021/acs.jmedchem.2c00633
72734867 105872 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 268 1 3 3 2.0 NC(N)=NC(=O)c1ccc2c(c1)Oc1ccccc1N2 10.1016/j.bmc.2013.10.010
CHEMBL3092757 105872 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 268 1 3 3 2.0 NC(N)=NC(=O)c1ccc2c(c1)Oc1ccccc1N2 10.1016/j.bmc.2013.10.010
CHEMBL3139241 105872 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 268 1 3 3 2.0 NC(N)=NC(=O)c1ccc2c(c1)Oc1ccccc1N2 10.1016/j.bmc.2013.10.010
230 4043 18 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.12.009
3045225 4043 18 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.12.009
CHEMBL407909 4043 18 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.12.009
67781610 166390 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 0 2 4.7 CN(C)CC/C=C1\c2ccc(Br)cc2COc2ccccc21 10.1021/acsmedchemlett.8b00300
CHEMBL4287193 166390 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 0 2 4.7 CN(C)CC/C=C1\c2ccc(Br)cc2COc2ccccc21 10.1021/acsmedchemlett.8b00300
16062910 96965 0 None -6 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 329 3 1 3 3.7 Cc1ccc(-c2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL269974 96965 0 None -6 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 329 3 1 3 3.7 Cc1ccc(-c2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
9839920 101225 0 None 10 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 316 2 2 3 4.4 Cn1ccc2cc(NC(=O)Nc3ccnc4ccccc34)ccc21 10.1016/s0960-894x(01)00343-2
CHEMBL299498 101225 0 None 10 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 316 2 2 3 4.4 Cn1ccc2cc(NC(=O)Nc3ccnc4ccccc34)ccc21 10.1016/s0960-894x(01)00343-2
146709966 175196 0 None 338 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2ccc3ccccc3c2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4583909 175196 0 None 338 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2ccc3ccccc3c2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
1042 1544 20 None -7 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 1544 20 None -7 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 1544 20 None -7 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 1544 20 None -7 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 1544 20 None -7 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
11536844 114611 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343672 114611 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
206 2447 10 None -1 25 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/j.ejmech.2019.04.064
68848 2447 10 None -1 25 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/j.ejmech.2019.04.064
CHEMBL12314 2447 10 None -1 25 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/j.ejmech.2019.04.064
4376990 192397 4 None -1 11 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B 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 -1 11 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B 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 -1 11 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B 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
153061504 172231 0 None 15 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2c(ccc3ccccc23)OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4513930 172231 0 None 15 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2c(ccc3ccccc23)OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
59752538 180560 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 339 3 1 4 3.7 CC(C)n1nc2c(c1-c1ccc(OC(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4760784 180560 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 339 3 1 4 3.7 CC(C)n1nc2c(c1-c1ccc(OC(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
11414582 180746 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 271 2 1 3 2.7 Fc1ccc(-c2c3c(nn2C2CC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4762886 180746 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 271 2 1 3 2.7 Fc1ccc(-c2c3c(nn2C2CC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
59752638 181805 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 253 2 1 3 2.6 c1ccc(-c2c3c(nn2C2CC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4785470 181805 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 253 2 1 3 2.6 c1ccc(-c2c3c(nn2C2CC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
189 3423 31 None -5 18 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/acs.jnatprod.2c00365
5163 3423 31 None -5 18 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/acs.jnatprod.2c00365
CHEMBL297784 3423 31 None -5 18 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/acs.jnatprod.2c00365
3037629 183979 13 None 1 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 396 5 1 5 3.6 C=C[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
CHEMBL4848517 183979 13 None 1 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 396 5 1 5 3.6 C=C[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
66647021 120151 0 None -9 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 257 2 0 1 4.2 CN(C)[C@@H]1Cc2ccccc2[C@@H](C2CCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402656 120151 0 None -9 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 257 2 0 1 4.2 CN(C)[C@@H]1Cc2ccccc2[C@@H](C2CCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547009 120151 0 None -9 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 257 2 0 1 4.2 CN(C)[C@@H]1Cc2ccccc2[C@@H](C2CCCCC2)C1 10.1016/j.bmc.2015.01.060
118729256 120184 0 None 6 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc([N+](=O)[O-])c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402670 120184 0 None 6 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc([N+](=O)[O-])c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547156 120184 0 None 6 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc([N+](=O)[O-])c2)C1 10.1016/j.bmc.2015.01.060
16062785 94665 0 None -5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 2 1 3 3.1 CC(C)c1nc2c(c(-c3ccc(F)cc3)n1)CCNCC2 10.1016/j.bmcl.2008.01.090
CHEMBL255543 94665 0 None -5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 2 1 3 3.1 CC(C)c1nc2c(c(-c3ccc(F)cc3)n1)CCNCC2 10.1016/j.bmcl.2008.01.090
16062784 94711 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 318 2 1 4 3.4 N#Cc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL255802 94711 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 318 2 1 4 3.4 N#Cc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
752521 197050 7 None 12 9 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
CHEMBL582877 197050 7 None 12 9 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
118729260 120163 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402672 120163 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547044 120163 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmc.2015.01.060
118729274 120186 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 327 3 0 1 5.4 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402681 120186 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 327 3 0 1 5.4 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547175 120186 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 327 3 0 1 5.4 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmc.2015.01.060
44435219 91346 0 None -6 4 Human 5.7 pKi = 5.7 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 367 2 0 2 6.2 O=C(Cc1ccc2ccccc2c1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL241115 91346 0 None -6 4 Human 5.7 pKi = 5.7 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 367 2 0 2 6.2 O=C(Cc1ccc2ccccc2c1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
155556618 173895 0 None -1905 5 Human 5.7 pKi = 5.7 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 417 6 3 7 2.7 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)ncnc32)[C@H]2C[C@@]2(CCl)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL4554295 173895 0 None -1905 5 Human 5.7 pKi = 5.7 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 417 6 3 7 2.7 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)ncnc32)[C@H]2C[C@@]2(CCl)[C@H]1O 10.1021/acs.jmedchem.8b01662
5897 104719 71 None -1 3 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 223 1 1 1 3.2 CC(=O)Nc1ccc2c(c1)Cc1ccccc1-2 nan
CHEMBL311469 104719 71 None -1 3 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 223 1 1 1 3.2 CC(=O)Nc1ccc2c(c1)Cc1ccccc1-2 nan
9926401 140331 0 None -4 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819556 140331 0 None -4 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819732 140331 0 None -4 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
71459553 83268 5 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysis
ChEMBL 406 7 0 4 5.3 COc1ccc2c(C)c(C(=O)N(CCCN3CCCCC3)c3ccccc3)oc2c1 10.1016/j.bmc.2012.09.044
CHEMBL2205360 83268 5 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysis
ChEMBL 406 7 0 4 5.3 COc1ccc2c(C)c(C(=O)N(CCCN3CCCCC3)c3ccccc3)oc2c1 10.1016/j.bmc.2012.09.044
9926401 140331 0 None -4 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819556 140331 0 None -4 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819732 140331 0 None -4 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
155554410 173812 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 331 2 2 5 0.6 Cc1cccc(C)c1N1C(=O)[C@H](CO)NC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4552298 173812 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 331 2 2 5 0.6 Cc1cccc(C)c1N1C(=O)[C@H](CO)NC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
11615459 197558 0 None 10 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1cccc2c1C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590078 197558 0 None 10 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1cccc2c1C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
122186881 122453 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 429 4 0 5 5.2 CCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3608451 122453 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 429 4 0 5 5.2 CCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
11209786 136703 0 None -6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 296 1 1 2 2.7 O=C1c2c(cc(C3CC3)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL375170 136703 0 None -6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 296 1 1 2 2.7 O=C1c2c(cc(C3CC3)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
155558626 174179 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 355 6 3 6 2.9 Nc1nc(NCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
CHEMBL4561016 174179 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 355 6 3 6 2.9 Nc1nc(NCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
11336079 83049 0 None -6 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 280 0 1 2 1.8 C#Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL220115 83049 0 None -6 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 280 0 1 2 1.8 C#Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
11264955 203243 0 None -6 3 Human 7.7 pKi = 7.7 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 240 3 1 3 2.3 CSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
CHEMBL76474 203243 0 None -6 3 Human 7.7 pKi = 7.7 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 240 3 1 3 2.3 CSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
20824945 67231 0 None -16 3 Human 7.7 pKi = 7.7 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 202 0 1 2 1.7 Cc1ccc2c(c1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL190124 67231 0 None -16 3 Human 7.7 pKi = 7.7 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 202 0 1 2 1.7 Cc1ccc2c(c1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
196129 67441 12 None -26 15 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67441 12 None -26 15 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
118055334 176886 0 None -34 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 266 0 1 2 2.5 CC1CN2CCNCc3ccc(Br)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4639090 176886 0 None -34 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 266 0 1 2 2.5 CC1CN2CCNCc3ccc(Br)c1c32 10.1016/j.bmcl.2019.126929
24826963 90670 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 0 1 2 1.3 Cc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397910 90670 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 0 1 2 1.3 Cc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
71681897 90674 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 258 0 1 3 1.0 O=C1c2ccc3c(c2C[C@@H]2CNCCN12)OCCC3 10.1016/j.bmcl.2013.04.061
CHEMBL2397914 90674 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 258 0 1 3 1.0 O=C1c2ccc3c(c2C[C@@H]2CNCCN12)OCCC3 10.1016/j.bmcl.2013.04.061
25123014 198737 0 None -6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598229 198737 0 None -6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
126769 204313 35 None 1 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1016/j.bmcl.2016.05.079
CHEMBL536255 204313 35 None 1 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1016/j.bmcl.2016.05.079
CHEMBL85194 204313 35 None 1 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1016/j.bmcl.2016.05.079
189 3423 31 None -5 18 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1039/C4MD00418C
5163 3423 31 None -5 18 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1039/C4MD00418C
CHEMBL297784 3423 31 None -5 18 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1039/C4MD00418C
127037059 136001 0 None 10 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 445 11 0 5 5.6 COc1ccc(CCN(CC/C=C\c2ccccc2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3736516 136001 0 None 10 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 445 11 0 5 5.6 COc1ccc(CCN(CC/C=C\c2ccccc2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL4777443 212276 0 None 11 14 Human 7.7 pKi = 7.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HTR2B
ChEMBL None None None CC(C)(C)OC(=O)N1CCCC1CN[C@H]1CC[C@@](c2cc(F)ccc2F)(S(=O)(=O)c2ccc(Cl)cc2)CC1 nan
70687202 77609 0 None -10 3 Human 6.7 pKi = 6.7 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@@H]1CNC[C@@H]2Cc3ccccc3N21 10.1016/j.bmcl.2005.05.074
CHEMBL2096809 77609 0 None -10 3 Human 6.7 pKi = 6.7 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@@H]1CNC[C@@H]2Cc3ccccc3N21 10.1016/j.bmcl.2005.05.074
18715558 73519 0 None -5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ccncc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201897 73519 0 None -5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ccncc3c21 10.1016/j.bmcl.2005.10.029
44451390 155197 2 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 210 1 2 2 2.1 CNc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL405717 155197 2 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 210 1 2 2 2.1 CNc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
118729246 120162 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(Br)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402663 120162 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(Br)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547043 120162 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(Br)cc2)C1 10.1016/j.bmc.2015.01.060
16062143 97232 0 None -19 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 283 2 1 3 3.2 Fc1ccc(-c2nc(C3CCC3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL271318 97232 0 None -19 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 283 2 1 3 3.2 Fc1ccc(-c2nc(C3CCC3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
134146585 148365 0 None 2 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 366 3 3 8 -0.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)C)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3941738 148365 0 None 2 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 366 3 3 8 -0.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)C)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
117209911 185737 1 None -26 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4874854 185737 1 None -26 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
24826786 90641 0 None -8 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 202 0 1 2 0.7 O=C1c2ccccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397881 90641 0 None -8 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 202 0 1 2 0.7 O=C1c2ccccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
10330266 21188 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Compound was tested for the displacement of [3H]5-HT from cloned human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from cloned human 5-hydroxytryptamine 2B receptor
ChEMBL 194 3 1 2 2.3 CN(C)CCc1c[nH]c2ccsc12 10.1021/jm980692q
CHEMBL13147 21188 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Compound was tested for the displacement of [3H]5-HT from cloned human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from cloned human 5-hydroxytryptamine 2B receptor
ChEMBL 194 3 1 2 2.3 CN(C)CCc1c[nH]c2ccsc12 10.1021/jm980692q
4011 81982 43 None -20 24 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 81982 43 None -20 24 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
155512086 169043 0 None -407 5 Human 6.7 pKi = 6.7 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 399 6 4 8 1.5 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CCC4)C4CCC4)ncnc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL4436786 169043 0 None -407 5 Human 6.7 pKi = 6.7 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 399 6 4 8 1.5 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CCC4)C4CCC4)ncnc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
137645406 157348 0 None -269 13 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4084262 157348 0 None -269 13 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4526351 212221 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000703a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000703a HTR2B
ChEMBL None None None Cc1cc(NC(=O)c2cccc(S(F)(F)(F)(F)F)c2)cc(-n2ccn3nc(-c4cccnc4)cc23)c1 nan
117209857 184545 1 None -5 8 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4856702 184545 1 None -5 8 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
4601 205010 29 None -4 17 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 205010 29 None -4 17 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 205010 29 None -4 17 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
68617 203806 60 None -15 26 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL1709 203806 60 None -15 26 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 203806 60 None -15 26 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
104697662 144860 1 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 293 3 2 4 3.3 Clc1cccc(CNc2nc(Cl)nc3[nH]cnc23)c1 10.1021/acs.jmedchem.6b01183
CHEMBL3914002 144860 1 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 293 3 2 4 3.3 Clc1cccc(CNc2nc(Cl)nc3[nH]cnc23)c1 10.1021/acs.jmedchem.6b01183
71682217 90673 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 246 1 1 3 1.0 COc1c(C)ccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397913 90673 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 246 1 1 3 1.0 COc1c(C)ccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
44409032 74657 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 223 0 1 3 1.5 C[C@@H]1CNC[C@@H]2Cc3ccc(Cl)nc3N21 10.1016/j.bmcl.2005.11.083
CHEMBL203396 74657 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 223 0 1 3 1.5 C[C@@H]1CNC[C@@H]2Cc3ccc(Cl)nc3N21 10.1016/j.bmcl.2005.11.083
165193 3126 60 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3126 60 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3126 60 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3126 60 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3126 60 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3126 60 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3126 60 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3126 60 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3126 60 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3126 60 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3126 60 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2353 100630 75 None -7 5 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL12089 100630 75 None -7 5 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL295124 100630 75 None -7 5 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
10440 2632 15 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
139030523 2632 15 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
CHEMBL4449712 2632 15 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
3117 206096 100 None -8 16 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 206096 100 None -8 16 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
145992489 166413 0 None -6 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4287623 166413 0 None -6 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
118055195 177433 0 None -9 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 202 0 1 2 2.0 Cc1ccc2c3c1C(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4646618 177433 0 None -9 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 202 0 1 2 2.0 Cc1ccc2c3c1C(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
122178704 120843 0 None 1 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 6 0 5 4.6 CCC(C)Oc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581249 120843 0 None 1 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 6 0 5 4.6 CCC(C)Oc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
16047544 12524 7 None 5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL1187185 12524 7 None 5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL492916 12524 7 None 5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
16062911 97249 0 None -27 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 383 3 1 3 4.4 FC(F)(F)c1ccc(-c2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL271418 97249 0 None -27 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 383 3 1 3 4.4 FC(F)(F)c1ccc(-c2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
189 3423 31 None -5 18 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1039/C8MD00204E
5163 3423 31 None -5 18 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1039/C8MD00204E
CHEMBL297784 3423 31 None -5 18 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1039/C8MD00204E
11658860 2302 47 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
2941 2302 47 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
4374 2302 47 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
CHEMBL360328 2302 47 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
DB04871 2302 47 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
11187156 135818 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 312 3 1 2 3.1 CCCCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL373483 135818 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 312 3 1 2 3.1 CCCCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
16062270 97211 0 None -100 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 297 2 1 3 3.6 Fc1ccc(-c2nc(C3CCCC3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL271212 97211 0 None -100 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 297 2 1 3 3.6 Fc1ccc(-c2nc(C3CCCC3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
16062266 97231 0 None -169 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 337 3 1 3 3.7 Fc1ccc(Cc2nc3c(c(-c4ccc(F)cc4)n2)CNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL271317 97231 0 None -169 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 337 3 1 3 3.7 Fc1ccc(Cc2nc3c(c(-c4ccc(F)cc4)n2)CNCC3)cc1 10.1016/j.bmcl.2008.01.090
2284 3121 27 None -16 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3121 27 None -16 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3121 27 None -16 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3121 27 None -16 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3121 27 None -16 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
9837204 74329 1 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 209 0 1 3 1.1 Clc1ccc2c(n1)N1CCNCC1C2 10.1016/j.bmcl.2005.11.083
CHEMBL203025 74329 1 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 209 0 1 3 1.1 Clc1ccc2c(n1)N1CCNCC1C2 10.1016/j.bmcl.2005.11.083
49865829 15968 0 None 22 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 330 1 1 3 4.1 O=C(Nc1ccccc1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224031 15968 0 None 22 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 330 1 1 3 4.1 O=C(Nc1ccccc1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
16062139 157113 0 None -204 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 3 1 3 3.4 CCC(C)c1nc2c(c(-c3ccc(F)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
CHEMBL408154 157113 0 None -204 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 3 1 3 3.4 CCC(C)c1nc2c(c(-c3ccc(F)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
71463061 83367 0 None -3 9 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 339 5 1 4 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205813 83367 0 None -3 9 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 339 5 1 4 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC 10.1016/j.bmcl.2012.08.046
2351 3222 60 None -7 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 3222 60 None -7 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 3222 60 None -7 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 3222 60 None -7 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 3222 60 None -7 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
156012918 176864 0 None -7 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 222 0 1 2 2.2 Clc1ccc2c3c1CCCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4638807 176864 0 None -7 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 222 0 1 2 2.2 Clc1ccc2c3c1CCCN3CCNC2 10.1016/j.bmcl.2019.126929
24826870 90658 0 None -4 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397898 90658 0 None -4 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
444795 139456 102 None 3 2 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 nan
CHEMBL38 139456 102 None 3 2 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 nan
136118613 92617 0 None 5 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442275 92617 0 None 5 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
26987 934 29 None -47 21 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 934 29 None -47 21 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 934 29 None -47 21 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 934 29 None -47 21 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 934 29 None -47 21 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
46230099 197622 0 None -2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 251 0 2 3 1.2 O=C1NC2CCNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
CHEMBL590483 197622 0 None -2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 251 0 2 3 1.2 O=C1NC2CCNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
11514226 88667 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337494 88667 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365470 88667 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
15560577 184749 6 None 1 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 398 5 1 5 3.8 CC[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
CHEMBL4859858 184749 6 None 1 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 398 5 1 5 3.8 CC[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
134152052 152537 0 None 3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 432 6 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3976121 152537 0 None 3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 432 6 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
134152052 152537 0 None 3 5 Human 7.6 pKi = 7.6 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 432 6 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL3976121 152537 0 None 3 5 Human 7.6 pKi = 7.6 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 432 6 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL5094493 213713 0 None -11 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCN(CCC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
72698087 103498 0 None -2089 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT2BBinding affinity to human 5HT2B
ChEMBL 407 5 0 4 5.0 Fc1cccc2c1nc(OCC1CCN(CCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
CHEMBL3093186 103498 0 None -2089 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT2BBinding affinity to human 5HT2B
ChEMBL 407 5 0 4 5.0 Fc1cccc2c1nc(OCC1CCN(CCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
10251906 67426 14 None -186 8 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1016/j.bmc.2008.04.050
CHEMBL1908863 67426 14 None -186 8 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1016/j.bmc.2008.04.050
CHEMBL482496 67426 14 None -186 8 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1016/j.bmc.2008.04.050
155539605 172266 0 None 3 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4514672 172266 0 None 3 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
127034730 135903 0 None 9 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 523 14 0 8 5.1 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735643 135903 0 None 9 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 523 14 0 8 5.1 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
46914927 15230 0 None 14 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 382 8 0 4 4.5 FCCCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
CHEMBL1214893 15230 0 None 14 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 382 8 0 4 4.5 FCCCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
91864602 140194 0 None -66 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818047 140194 0 None -66 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
135514796 92612 0 None -2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 226 1 4 2 1.2 N=C1NC(=O)/C(=C\c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442270 92612 0 None -2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 226 1 4 2 1.2 N=C1NC(=O)/C(=C\c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
142601323 185249 0 None -9 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 272 3 2 4 1.9 COc1ccccc1-c1n[nH]cc1N1CCCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4867560 185249 0 None -9 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 272 3 2 4 1.9 COc1ccccc1-c1n[nH]cc1N1CCCNCC1 10.1021/acs.jmedchem.1c01093
3973 206429 104 None -44 3 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 4 3.3 O=c1cc(N2CCOCC2)oc2c(-c3ccccc3)cccc12 nan
CHEMBL98350 206429 104 None -44 3 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 4 3.3 O=c1cc(N2CCOCC2)oc2c(-c3ccccc3)cccc12 nan
3157 1437 69 None -37 12 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
7170 1437 69 None -37 12 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
954 1437 69 None -37 12 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
CHEMBL707 1437 69 None -37 12 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
DB00590 1437 69 None -37 12 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
91864602 140194 0 None -66 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818047 140194 0 None -66 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
16115388 136828 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 284 1 1 2 2.6 CC[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
CHEMBL375302 136828 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 284 1 1 2 2.6 CC[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
11185858 84354 0 None -7 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@@H]1CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
CHEMBL223271 84354 0 None -7 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@@H]1CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
71061785 159937 0 None -6 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
CHEMBL4112056 159937 0 None -6 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
10430623 18473 22 None -213 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1277105 18473 22 None -213 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
72901200 119259 21 None -162 4 Human 6.6 pKi = 6.6 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HTR2BSelectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HTR2B
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 nan
CHEMBL3480577 119259 21 None -162 4 Human 6.6 pKi = 6.6 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HTR2BSelectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HTR2B
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 nan
11587397 88613 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337489 88613 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2364893 88613 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
6726 1249 46 None -7 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 1249 46 None -7 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 1249 46 None -7 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 1249 46 None -7 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 1249 46 None -7 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
44579715 192639 0 None -2238 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 405 4 3 7 2.7 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCc3cccc(Cl)c3)nc(Cl)nc21 10.1021/acs.jmedchem.6b01183
CHEMBL523797 192639 0 None -2238 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 405 4 3 7 2.7 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCc3cccc(Cl)c3)nc(Cl)nc21 10.1021/acs.jmedchem.6b01183
46230048 197600 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1cccc2c1N1CCNCC1NC2=O 10.1016/j.bmcl.2009.12.014
CHEMBL590332 197600 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1cccc2c1N1CCNCC1NC2=O 10.1016/j.bmcl.2009.12.014
118055215 176872 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 216 0 1 2 2.2 Cc1ccc2c3c1C(C)(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4638879 176872 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 216 0 1 2 2.2 Cc1ccc2c3c1C(C)(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
1355 1972 82 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
142 1972 82 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
CHEMBL478 1972 82 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
DB12110 1972 82 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
11652452 88683 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337492 88683 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365703 88683 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
162668650 182081 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 284 3 2 4 2.9 CNc1ccc(-c2c3c(nn2C(C)C)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4789085 182081 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 284 3 2 4 2.9 CNc1ccc(-c2c3c(nn2C(C)C)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
3251 3997 50 None -79 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
5684 3997 50 None -79 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
80 3997 50 None -79 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
CHEMBL31354 3997 50 None -79 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
1355 1972 82 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
142 1972 82 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
CHEMBL478 1972 82 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
DB12110 1972 82 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
16115381 83016 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
CHEMBL219837 83016 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
10015055 2063 4 None -120 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
1212 2063 4 None -120 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
CHEMBL3402679 2063 4 None -120 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
46884100 7920 0 None -104 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 314 5 2 3 3.0 O=C(NCc1ccc(Oc2cccc(F)c2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1090757 7920 0 None -104 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 314 5 2 3 3.0 O=C(NCc1ccc(Oc2cccc(F)c2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
145978665 162954 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 246 2 2 3 2.4 C[C@@H]1SC(c2c[nH]c3ccccc23)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4202582 162954 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 246 2 2 3 2.4 C[C@@H]1SC(c2c[nH]c3ccccc23)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
2142 3035 54 None -43 37 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
4920903 3035 54 None -43 37 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
502 3035 54 None -43 37 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
5775 3035 54 None -43 37 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
CHEMBL597 3035 54 None -43 37 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
DB00692 3035 54 None -43 37 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
56678761 65322 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 364 7 0 4 4.2 COc1cccc(CCCN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1016/j.bmcl.2011.08.029
CHEMBL1834257 65322 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 364 7 0 4 4.2 COc1cccc(CCCN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1016/j.bmcl.2011.08.029
46914773 15240 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 368 7 0 4 4.1 FCCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
CHEMBL1214958 15240 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 368 7 0 4 4.1 FCCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
9921064 126644 18 None -8 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT2B receptor (unknown origin)Binding affinity to 5-HT2B receptor (unknown origin)
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
CHEMBL365751 126644 18 None -8 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT2B receptor (unknown origin)Binding affinity to 5-HT2B receptor (unknown origin)
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
22254068 65624 24 None -173 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 423 5 2 6 4.0 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836317 65624 24 None -173 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 423 5 2 6 4.0 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
11536299 182694 6 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 266 3 1 3 3.3 O=c1cc(CCc2ccccc2)oc2cccc(O)c12 10.1016/j.bmcl.2014.02.029
CHEMBL479683 182694 6 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 266 3 1 3 3.3 O=c1cc(CCc2ccccc2)oc2cccc(O)c12 10.1016/j.bmcl.2014.02.029
145990586 166279 0 None -19 11 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to 5-HT2B 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 -19 11 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to 5-HT2B 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
136118660 75888 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058428 75888 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
135367816 164272 0 None -3 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218801 164272 0 None -3 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
11483068 84374 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 250 1 1 2 2.0 CCc1cc(Cl)c2c(c1)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL223440 84374 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 250 1 1 2 2.0 CCc1cc(Cl)c2c(c1)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
11414184 83071 0 None -13 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)C2CNCCN12 10.1021/jm0612968
CHEMBL220274 83071 0 None -13 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)C2CNCCN12 10.1021/jm0612968
43922 114254 9 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 250 4 2 2 2.0 COc1cc2c(CCNC(C)=O)c[nH]c2cc1F 10.1021/jm100600y
CHEMBL333886 114254 9 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 250 4 2 2 2.0 COc1cc2c(CCNC(C)=O)c[nH]c2cc1F 10.1021/jm100600y
1212 1624 45 None -27 66 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1624 45 None -27 66 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1624 45 None -27 66 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1624 45 None -27 66 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1624 45 None -27 66 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
9856509 95508 4 None -10 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 259 0 1 1 2.8 Clc1c(Br)ccc2c1CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL259480 95508 4 None -10 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 259 0 1 1 2.8 Clc1c(Br)ccc2c1CCNCC2 10.1016/j.bmc.2007.12.009
168293016 191502 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 7 0 5 5.0 CCCC(C)Oc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5203303 191502 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 7 0 5 5.0 CCCC(C)Oc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
10599545 36157 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 447 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Cl)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL14469 36157 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 447 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Cl)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
10436045 3447 3 None -7 13 Human 7.6 pKi = 7.6 Binding
Binding affinity for 5-hydroxytryptamine 2B receptor was determinedBinding affinity for 5-hydroxytryptamine 2B receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
782 3447 3 None -7 13 Human 7.6 pKi = 7.6 Binding
Binding affinity for 5-hydroxytryptamine 2B receptor was determinedBinding affinity for 5-hydroxytryptamine 2B receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
CHEMBL432713 3447 3 None -7 13 Human 7.6 pKi = 7.6 Binding
Binding affinity for 5-hydroxytryptamine 2B receptor was determinedBinding affinity for 5-hydroxytryptamine 2B receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
189 3423 31 None -5 18 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm970741j
5163 3423 31 None -5 18 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm970741j
CHEMBL297784 3423 31 None -5 18 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm970741j
11391654 179933 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 273 2 1 3 3.0 CC(C)n1nc2c(c1-c1ccc(F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4753511 179933 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 273 2 1 3 3.0 CC(C)n1nc2c(c1-c1ccc(F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
189 3423 31 None -5 18 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm970424c
5163 3423 31 None -5 18 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm970424c
CHEMBL297784 3423 31 None -5 18 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm970424c
10835537 38376 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3ccccc3)c1)CC2 10.1021/jm990388c
CHEMBL14652 38376 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3ccccc3)c1)CC2 10.1021/jm990388c
10574607 40388 0 None -7 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 429 3 1 3 6.1 CSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3ccncc3)c1)CC2 10.1021/jm990388c
CHEMBL14841 40388 0 None -7 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 429 3 1 3 6.1 CSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3ccncc3)c1)CC2 10.1021/jm990388c
44298249 192976 0 None 1 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 394 4 1 4 4.6 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3cccnc3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL53063 192976 0 None 1 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 394 4 1 4 4.6 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3cccnc3)nc1)CC2 10.1016/s0960-894x(00)00365-6
44298121 193150 0 None -3 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 4 1 4 5.3 Cc1cccc(COc2ccc(NC(=O)N3CCc4cc(C)c(C(F)(F)F)cc43)cn2)n1 10.1016/s0960-894x(00)00365-6
CHEMBL53939 193150 0 None -3 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 4 1 4 5.3 Cc1cccc(COc2ccc(NC(=O)N3CCc4cc(C)c(C(F)(F)F)cc43)cn2)n1 10.1016/s0960-894x(00)00365-6
44214723 193812 0 None -10 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 427 4 1 3 5.6 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)cc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL55335 193812 0 None -10 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 427 4 1 3 5.6 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)cc1)CC2 10.1016/s0960-894x(00)00365-6
1225 1438 24 None -89 22 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acsmedchemlett.8b00300
3958 1438 24 None -89 22 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acsmedchemlett.8b00300
667477 1438 24 None -89 22 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acsmedchemlett.8b00300
CHEMBL860 1438 24 None -89 22 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acsmedchemlett.8b00300
DB01142 1438 24 None -89 22 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acsmedchemlett.8b00300
20824946 123113 0 None -7 3 Human 6.6 pKi = 6.6 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 218 1 2 3 0.9 C[C@@H]1CNC[C@H]2Cc3ccc(CO)cc3N12 10.1016/j.bmcl.2005.05.074
CHEMBL361929 123113 0 None -7 3 Human 6.6 pKi = 6.6 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 218 1 2 3 0.9 C[C@@H]1CNC[C@H]2Cc3ccc(CO)cc3N12 10.1016/j.bmcl.2005.05.074
118729244 120161 0 None -1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402662 120161 0 None -1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547029 120161 0 None -1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmc.2015.01.060
122188579 122655 0 None -1479 4 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 471 4 4 8 2.0 CCNc1cc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acsmedchemlett.5b00150
CHEMBL3612940 122655 0 None -1479 4 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 471 4 4 8 2.0 CCNc1cc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acsmedchemlett.5b00150
16062137 97250 0 None -125 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 319 3 1 3 3.5 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL271419 97250 0 None -125 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 319 3 1 3 3.5 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
44298186 101228 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 458 4 1 5 5.5 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(Oc3cccnc3C)cc1C)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL299506 101228 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 458 4 1 5 5.5 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(Oc3cccnc3C)cc1C)CC2 10.1016/s0960-894x(00)00364-4
44298120 193320 0 None -158 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 438 3 1 4 5.2 Cc1ccc2c(c1Br)CCN2C(=O)Nc1ccc(Oc2cccnc2C)nc1 10.1016/s0960-894x(00)00364-4
CHEMBL54775 193320 0 None -158 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 438 3 1 4 5.2 Cc1ccc2c(c1Br)CCN2C(=O)Nc1ccc(Oc2cccnc2C)nc1 10.1016/s0960-894x(00)00364-4
44323840 204836 0 None -6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 586 12 3 9 2.7 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C(C)=O)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL88809 204836 0 None -6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 586 12 3 9 2.7 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C(C)=O)cc1 10.1016/S0960-894X(96)00503-3
155519891 169814 0 None 2 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 249 2 1 4 1.9 COc1cc(OC)c2c(c1)OC[C@@]1(C)NCC[C@@H]21 10.1021/acsmedchemlett.9b00225
CHEMBL4447975 169814 0 None 2 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 249 2 1 4 1.9 COc1cc(OC)c2c(c1)OC[C@@]1(C)NCC[C@@H]21 10.1021/acsmedchemlett.9b00225
155526977 170545 0 None 10 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 221 2 1 3 2.3 CC[C@H]1c2cc(OC)ccc2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4458099 170545 0 None 10 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 221 2 1 3 2.3 CC[C@H]1c2cc(OC)ccc2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
153287541 171619 0 None -12 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 279 1 0 2 3.9 CN1CC[C@H]2c3cccc(-c4ccccc4)c3OC[C@]21C 10.1021/acsmedchemlett.9b00225
CHEMBL4473697 171619 0 None -12 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 279 1 0 2 3.9 CN1CC[C@H]2c3cccc(-c4ccccc4)c3OC[C@]21C 10.1021/acsmedchemlett.9b00225
153287539 175490 0 None 3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 265 1 1 2 3.6 C[C@@]12COc3ccc(-c4ccccc4)cc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4591008 175490 0 None 3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 265 1 1 2 3.6 C[C@@]12COc3ccc(-c4ccccc4)cc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
11465413 87601 0 None -125 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.7 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCC(C)(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234494 87601 0 None -125 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.7 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCC(C)(C)CC1 10.1016/j.bmcl.2006.10.029
11305844 87734 0 None -630 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 466 6 0 4 5.1 COc1ccc(N2Cc3cc(F)cc(C(F)(F)F)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234739 87734 0 None -630 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 466 6 0 4 5.1 COc1ccc(N2Cc3cc(F)cc(C(F)(F)F)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
10368204 86323 0 None -15 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 451 6 0 5 4.6 COc1ccc(N2Cc3c(c4ccc(F)cc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
CHEMBL232047 86323 0 None -15 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 451 6 0 5 4.6 COc1ccc(N2Cc3c(c4ccc(F)cc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
2337 3193 72 None -15 63 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
50 3193 72 None -15 63 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
5002 3193 72 None -15 63 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
CHEMBL716 3193 72 None -15 63 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
DB01224 3193 72 None -15 63 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
76325516 105238 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 280 4 1 3 3.7 O=c1cc(CCCc2ccccc2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
CHEMBL3126299 105238 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 280 4 1 3 3.7 O=c1cc(CCCc2ccccc2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
18357724 194912 0 None -31 3 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 414 4 1 4 4.7 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2ccc(C(F)(F)F)cc21 10.1016/s0960-894x(00)00365-6
CHEMBL56405 194912 0 None -31 3 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 414 4 1 4 4.7 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2ccc(C(F)(F)F)cc21 10.1016/s0960-894x(00)00365-6
162645563 179100 0 None - 1 Human 5.6 pKi = 5.6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 348 4 1 3 4.7 O=c1cc(CCCc2ccc(C(F)(F)F)cc2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
CHEMBL4743625 179100 0 None - 1 Human 5.6 pKi = 5.6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 348 4 1 3 4.7 O=c1cc(CCCc2ccc(C(F)(F)F)cc2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
162648564 179331 0 None - 1 Human 5.6 pKi = 5.6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 314 4 1 3 4.3 O=c1cc(CCCc2ccc(Cl)cc2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
CHEMBL4746138 179331 0 None - 1 Human 5.6 pKi = 5.6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 314 4 1 3 4.3 O=c1cc(CCCc2ccc(Cl)cc2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
162666438 181678 0 None - 1 Human 5.6 pKi = 5.6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 298 4 1 3 3.8 O=c1cc(CCCc2cccc(F)c2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
CHEMBL4783824 181678 0 None - 1 Human 5.6 pKi = 5.6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 298 4 1 3 3.8 O=c1cc(CCCc2cccc(F)c2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
44298126 101111 0 None -158 2 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 380 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c(Cl)cccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL298696 101111 0 None -158 2 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 380 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c(Cl)cccc32)cn1 10.1016/s0960-894x(00)00364-4
10085260 170050 0 None -66 6 Human 6.6 pKi = 6.6 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine as radioligand
ChEMBL 283 1 1 3 2.2 COc1cc(Br)c2c3c1C[C@H](N)C[C@@H]3CO2 10.1021/jm980076u
CHEMBL445106 170050 0 None -66 6 Human 6.6 pKi = 6.6 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine as radioligand
ChEMBL 283 1 1 3 2.2 COc1cc(Br)c2c3c1C[C@H](N)C[C@@H]3CO2 10.1021/jm980076u
71086303 160251 0 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4114493 160251 0 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
117209965 184655 1 None -10 6 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4858338 184655 1 None -10 6 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
46914775 15241 0 None 3 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 364 7 0 4 4.5 CCCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
CHEMBL1214959 15241 0 None 3 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 364 7 0 4 4.5 CCCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
127035062 135915 0 None -4 19 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3735756 135915 0 None -4 19 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
127035062 135915 0 None -4 19 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane 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 -4 19 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
15011385 160992 3 None -6 5 Human 7.6 pKi = 7.6 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 244 3 1 2 2.6 CN(C)CCc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL412876 160992 3 None -6 5 Human 7.6 pKi = 7.6 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 244 3 1 2 2.6 CN(C)CCc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
45378936 197815 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL591940 197815 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
70695555 77592 1 None -14 3 Human 5.6 pKi = 5.6 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@H]1CNC[C@@H]2Cc3ccccc3N12 10.1016/j.bmcl.2005.05.074
CHEMBL2096711 77592 1 None -14 3 Human 5.6 pKi = 5.6 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@H]1CNC[C@@H]2Cc3ccccc3N12 10.1016/j.bmcl.2005.05.074
168286277 191009 0 None -3 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assayDisplacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assay
ChEMBL 468 3 2 3 6.5 Ic1ccc(Nc2nc3ccccc3c3[nH]c(C4CCCCC4)nc23)cc1 10.1021/acs.jmedchem.2c01170
CHEMBL5195535 191009 0 None -3 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assayDisplacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assay
ChEMBL 468 3 2 3 6.5 Ic1ccc(Nc2nc3ccccc3c3[nH]c(C4CCCCC4)nc23)cc1 10.1021/acs.jmedchem.2c01170
1599 2299 47 None -144 16 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
3955 2299 47 None -144 16 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
7215 2299 47 None -144 16 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
CHEMBL841 2299 47 None -144 16 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
DB00836 2299 47 None -144 16 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
46914771 15222 0 None 12 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 350 6 0 4 4.1 CCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
CHEMBL1214831 15222 0 None 12 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 350 6 0 4 4.1 CCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
165193 3126 60 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3126 60 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3126 60 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3126 60 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3126 60 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3126 60 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3126 60 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3126 60 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3126 60 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3126 60 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3126 60 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4209 3102 71 None -758 34 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
4893 3102 71 None -758 34 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
503 3102 71 None -758 34 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
5385 3102 71 None -758 34 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
CHEMBL2 3102 71 None -758 34 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
DB00457 3102 71 None -758 34 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
10085260 170050 0 None -66 6 Human 6.6 pKi = 6.6 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 283 1 1 3 2.2 COc1cc(Br)c2c3c1C[C@H](N)C[C@@H]3CO2 10.1021/jm980076u
CHEMBL445106 170050 0 None -66 6 Human 6.6 pKi = 6.6 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 283 1 1 3 2.2 COc1cc(Br)c2c3c1C[C@H](N)C[C@@H]3CO2 10.1021/jm980076u
135433933 176454 1 None -2 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL463249 176454 1 None -2 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
136118728 92615 0 None -1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442273 92615 0 None -1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
90181059 159672 0 None -1 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
CHEMBL4109801 159672 0 None -1 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
10472143 118759 0 None -60 17 Human 7.6 pKi = 7.6 Binding
Binding affinities towards 5-hydroxytryptamine 2B receptorBinding affinities towards 5-hydroxytryptamine 2B 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 -60 17 Human 7.6 pKi = 7.6 Binding
Binding affinities towards 5-hydroxytryptamine 2B receptorBinding affinities towards 5-hydroxytryptamine 2B 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
59757153 105849 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1cccc2c1-c1ccccc1C2 10.1016/j.bmc.2013.10.010
CHEMBL3092762 105849 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1cccc2c1-c1ccccc1C2 10.1016/j.bmc.2013.10.010
CHEMBL3139190 105849 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1cccc2c1-c1ccccc1C2 10.1016/j.bmc.2013.10.010
118464427 137793 0 None 15 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3771331 137793 0 None 15 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
118709750 113028 0 None -24 9 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1cccc(F)c1 10.1016/j.bmcl.2014.07.018
CHEMBL3321791 113028 0 None -24 9 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1cccc(F)c1 10.1016/j.bmcl.2014.07.018
44453652 154905 0 None 4 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 273 1 1 3 2.8 Cc1nc2c(c(-c3ccc(Cl)cc3)n1)CCNCC2 10.1016/j.bmcl.2008.01.090
CHEMBL403902 154905 0 None 4 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 273 1 1 3 2.8 Cc1nc2c(c(-c3ccc(Cl)cc3)n1)CCNCC2 10.1016/j.bmcl.2008.01.090
73349361 92102 0 None -3 7 Human 5.6 pKi = 5.6 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 279 4 0 1 3.3 CN(CCc1ccccc1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL2432058 92102 0 None -3 7 Human 5.6 pKi = 5.6 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 279 4 0 1 3.3 CN(CCc1ccccc1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
136118636 75946 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2cc(Br)ccc12 10.1016/j.bmc.2013.09.011
CHEMBL2058696 75946 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2cc(Br)ccc12 10.1016/j.bmc.2013.09.011
43229249 140273 1 None -70 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 279 5 0 2 3.7 O=C(CCCN1CCc2ccccc2C1)c1ccccc1 10.1016/j.bmc.2016.05.053
CHEMBL3818989 140273 1 None -70 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 279 5 0 2 3.7 O=C(CCCN1CCc2ccccc2C1)c1ccccc1 10.1016/j.bmc.2016.05.053
25067564 199605 0 None -61 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL604102 199605 0 None -61 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
56658157 65323 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 348 7 0 3 4.6 c1ccc(CCCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
CHEMBL1834258 65323 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 348 7 0 3 4.6 c1ccc(CCCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
43229249 140273 1 None -70 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 279 5 0 2 3.7 O=C(CCCN1CCc2ccccc2C1)c1ccccc1 10.1016/j.bmc.2016.05.053
CHEMBL3818989 140273 1 None -70 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 279 5 0 2 3.7 O=C(CCCN1CCc2ccccc2C1)c1ccccc1 10.1016/j.bmc.2016.05.053
44582706 186404 0 None -46 2 Human 5.6 pKi = 5.6 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 417 10 1 5 4.0 COc1ccc(CCN2CCC(C(O)c3cccc(OCCF)c3OC)CC2)cc1 10.1016/j.bmc.2009.03.021
CHEMBL490633 186404 0 None -46 2 Human 5.6 pKi = 5.6 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 417 10 1 5 4.0 COc1ccc(CCN2CCC(C(O)c3cccc(OCCF)c3OC)CC2)cc1 10.1016/j.bmc.2009.03.021
3035850 936 65 None -15135 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
457 936 65 None -15135 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
CHEMBL431733 936 65 None -15135 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
DB12885 936 65 None -15135 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
145973771 164156 0 None -3 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4217398 164156 0 None -3 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
21138 97986 34 None -6 7 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
CHEMBL275742 97986 34 None -6 7 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
46914486 15231 0 None 13 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 336 5 0 4 3.8 COc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
CHEMBL1214894 15231 0 None 13 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 336 5 0 4 3.8 COc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
124087 1357 106 None -5 15 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1357 106 None -5 15 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1357 106 None -5 15 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1357 106 None -5 15 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1357 106 None -5 15 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
118055191 176731 0 None -31 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 280 0 1 2 2.7 CC1(C)CN2CCNCc3ccc(Br)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4636977 176731 0 None -31 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 280 0 1 2 2.7 CC1(C)CN2CCNCc3ccc(Br)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL5074190 212533 0 None -112 9 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(CCN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
11701315 197599 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1ccc2c(c1)N1CCNCC1NC2=O 10.1016/j.bmcl.2009.12.014
CHEMBL590331 197599 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1ccc2c(c1)N1CCNCC1NC2=O 10.1016/j.bmcl.2009.12.014
44554393 18346 0 None -61 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1275630 18346 0 None -61 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
49783415 17481 0 None -3890 13 Human 5.5 pKi = 5.5 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258452 17481 0 None -3890 13 Human 5.5 pKi = 5.5 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
136118647 75952 0 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 240 1 3 2 1.2 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058702 75952 0 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 240 1 3 2 1.2 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
1530 2142 44 None -19 21 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2142 44 None -19 21 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2142 44 None -19 21 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2142 44 None -19 21 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2142 44 None -19 21 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
122178707 120846 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 395 6 0 5 4.3 COc1cc2c(cc1OCC1CC1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
CHEMBL3581252 120846 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 395 6 0 5 4.3 COc1cc2c(cc1OCC1CC1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
11233293 83733 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 310 1 1 2 2.9 CC1(c2cc3c(c(C(F)(F)F)c2)C(=O)N2CCNC[C@@H]32)CC1 10.1021/jm0612968
CHEMBL220833 83733 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 310 1 1 2 2.9 CC1(c2cc3c(c(C(F)(F)F)c2)C(=O)N2CCNC[C@@H]32)CC1 10.1021/jm0612968
16115267 84355 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL223272 84355 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
71461049 82548 0 None -1 6 Human 7.5 pKi = 7.5 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3c(OC)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181187 82548 0 None -1 6 Human 7.5 pKi = 7.5 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3c(OC)cccc3c3ccccc23)CC1 10.1021/jm300943r
56665074 65318 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 350 6 0 4 3.8 COc1cccc(CCN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1016/j.bmcl.2011.08.029
CHEMBL1834253 65318 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 350 6 0 4 3.8 COc1cccc(CCN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1016/j.bmcl.2011.08.029
155534799 175928 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor after 60 mins by radiometric scintillation analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor after 60 mins by radiometric scintillation analysis
ChEMBL 416 7 1 6 2.7 O=c1c2cc(Cl)ccc2oc2ccc(CN3CCN(CCOCCO)CC3)cc12 10.1016/j.bmcl.2019.126679
CHEMBL4471059 175928 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor after 60 mins by radiometric scintillation analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor after 60 mins by radiometric scintillation analysis
ChEMBL 416 7 1 6 2.7 O=c1c2cc(Cl)ccc2oc2ccc(CN3CCN(CCOCCO)CC3)cc12 10.1016/j.bmcl.2019.126679
CHEMBL4596904 175928 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor after 60 mins by radiometric scintillation analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor after 60 mins by radiometric scintillation analysis
ChEMBL 416 7 1 6 2.7 O=c1c2cc(Cl)ccc2oc2ccc(CN3CCN(CCOCCO)CC3)cc12 10.1016/j.bmcl.2019.126679
155535203 171465 0 None -7 6 Human 5.5 pKi = 5.5 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 403 5 3 7 2.8 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CCC3)C3CCC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
CHEMBL4471712 171465 0 None -7 6 Human 5.5 pKi = 5.5 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 403 5 3 7 2.8 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CCC3)C3CCC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
5353853 17788 41 None -23 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 17788 41 None -23 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 17788 41 None -23 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
44409327 76264 0 None -128 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 261 3 1 4 1.9 CCO[C@@H](C)c1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL206394 76264 0 None -128 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 261 3 1 4 1.9 CCO[C@@H](C)c1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
155531067 171043 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 369 7 3 6 3.3 Nc1nc(NCCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
CHEMBL4465512 171043 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 369 7 3 6 3.3 Nc1nc(NCCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
71459604 83365 0 None -5 14 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 83365 0 None -5 14 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
122187378 122497 0 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 455 5 0 5 5.6 COc1cc2c3c(c1OCC1CC1)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609143 122497 0 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 455 5 0 5 5.6 COc1cc2c3c(c1OCC1CC1)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
44455426 154598 0 None -33 13 Human 6.5 pKi = 6.5 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 154598 0 None -33 13 Human 6.5 pKi = 6.5 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
11288612 182019 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 267 2 1 3 3.0 c1ccc(-c2c3c(nn2C2CCC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4788327 182019 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 267 2 1 3 3.0 c1ccc(-c2c3c(nn2C2CCC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
145981805 166146 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 313 3 0 2 4.6 CN(C)CC/C=C1\c2ccc(Cl)cc2COc2ccccc21 10.1021/acsmedchemlett.8b00300
CHEMBL4282729 166146 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 313 3 0 2 4.6 CN(C)CC/C=C1\c2ccc(Cl)cc2COc2ccccc21 10.1021/acsmedchemlett.8b00300
127048334 140057 0 None 13 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2ccccc2Cl)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3813796 140057 0 None 13 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2ccccc2Cl)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
135398737 942 89 None -2 92 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
38 942 89 None -2 92 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
722 942 89 None -2 92 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
CHEMBL42 942 89 None -2 92 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
DB00363 942 89 None -2 92 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
29943048 67306 0 None -10 3 Human 8.5 pKi = 8.5 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL190699 67306 0 None -10 3 Human 8.5 pKi = 8.5 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
29943048 67306 0 None -10 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL190699 67306 0 None -10 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
1588 2284 24 None -8 44 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -8 44 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -8 44 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -8 44 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -8 44 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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
11637931 120059 0 None -2 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 295 2 2 2 2.0 COC1(C)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343665 120059 0 None -2 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 295 2 2 2 2.0 COC1(C)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545814 120059 0 None -2 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 295 2 2 2 2.0 COC1(C)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
145993540 166769 0 None -1 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEKT cells after 90 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEKT cells after 90 mins by scintillation counting method
ChEMBL 503 12 3 11 2.2 NCCCCNC(=O)COc1ccc(CCCn2ncc3c2nc(N)n2nc(-c4ccco4)nc32)cc1 10.1039/C7MD00247E
CHEMBL4294350 166769 0 None -1 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEKT cells after 90 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEKT cells after 90 mins by scintillation counting method
ChEMBL 503 12 3 11 2.2 NCCCCNC(=O)COc1ccc(CCCn2ncc3c2nc(N)n2nc(-c4ccco4)nc32)cc1 10.1039/C7MD00247E
127048335 140049 0 None 15 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2ccccc2Br)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3813726 140049 0 None 15 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2ccccc2Br)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
11502243 188906 39 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 401 4 1 6 4.4 N#Cc1cc(CN2CCC(Nc3ncnc4sc(Cl)cc34)CC2)ccc1F 10.1016/j.bmc.2019.02.044
CHEMBL513994 188906 39 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 401 4 1 6 4.4 N#Cc1cc(CN2CCC(Nc3ncnc4sc(Cl)cc34)CC2)ccc1F 10.1016/j.bmc.2019.02.044
146709966 175196 0 None 338 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2ccc3ccccc3c2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4583909 175196 0 None 338 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2ccc3ccccc3c2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
72734865 105821 0 None 39 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 268 1 3 3 2.0 NC(N)=NC(=O)c1ccc2c(c1)Nc1ccccc1O2 10.1016/j.bmc.2013.10.010
CHEMBL3092756 105821 0 None 39 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 268 1 3 3 2.0 NC(N)=NC(=O)c1ccc2c(c1)Nc1ccccc1O2 10.1016/j.bmc.2013.10.010
CHEMBL3139103 105821 0 None 39 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 268 1 3 3 2.0 NC(N)=NC(=O)c1ccc2c(c1)Nc1ccccc1O2 10.1016/j.bmc.2013.10.010
135509961 135596 2 None -3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(Cl)c21 10.1021/jm050663x
CHEMBL373245 135596 2 None -3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(Cl)c21 10.1021/jm050663x
10623020 32169 0 None -12 2 Human 8.4 pKi = 8.4 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 441 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(C)c(-c3cnccc3C)c1)CC2 10.1021/jm990388c
CHEMBL14111 32169 0 None -12 2 Human 8.4 pKi = 8.4 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 441 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(C)c(-c3cnccc3C)c1)CC2 10.1021/jm990388c
18475630 101413 0 None 19 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 330 2 2 3 4.7 Cc1cc2cc(NC(=O)Nc3ccnc4ccccc34)ccc2n1C 10.1016/s0960-894x(01)00343-2
CHEMBL300835 101413 0 None 19 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 330 2 2 3 4.7 Cc1cc2cc(NC(=O)Nc3ccnc4ccccc34)ccc2n1C 10.1016/s0960-894x(01)00343-2
10690185 161193 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 365 3 1 3 4.5 CC(C)Oc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
CHEMBL41389 161193 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 365 3 1 3 4.5 CC(C)Oc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
1621 2386 16 None -19 45 Human 7.5 pKi = 7.5 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
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 -19 45 Human 7.5 pKi = 7.5 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
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 -19 45 Human 7.5 pKi = 7.5 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
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 -19 45 Human 7.5 pKi = 7.5 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
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 -19 45 Human 7.5 pKi = 7.5 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
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
2600 3708 73 None -1 13 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3708 73 None -1 13 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3708 73 None -1 13 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3708 73 None -1 13 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3708 73 None -1 13 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
118729264 120174 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(Cl)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402675 120174 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(Cl)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547136 120174 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(Cl)c2)C1 10.1016/j.bmc.2015.01.060
118729248 120178 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(Br)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402664 120178 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(Br)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547150 120178 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(Br)cc2)C1 10.1016/j.bmc.2015.01.060
16062788 97011 0 None -50 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 333 3 1 3 3.6 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL270188 97011 0 None -50 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 333 3 1 3 3.6 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
16062781 154628 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 311 2 1 3 3.6 Fc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL402357 154628 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 311 2 1 3 3.6 Fc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
127036932 136811 0 None 1 22 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752900 136811 0 None 1 22 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
44581973 175018 0 None -14 10 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458002 175018 0 None -14 10 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
73346042 91388 3 None -3019 17 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 91388 3 None -3019 17 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
44451429 155214 3 None -21 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 226 1 1 3 1.9 O=[N+]([O-])c1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL405829 155214 3 None -21 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 226 1 1 3 1.9 O=[N+]([O-])c1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
89901929 120179 0 None -38 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402665 120179 0 None -38 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547151 120179 0 None -38 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.01.060
89901938 120188 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccccc2Cl)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402684 120188 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccccc2Cl)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547177 120188 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccccc2Cl)C1 10.1016/j.bmc.2015.01.060
145978113 163274 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 207 2 1 3 1.9 C[C@@H]1SC(c2ccccc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4206418 163274 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 207 2 1 3 1.9 C[C@@H]1SC(c2ccccc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
11312820 135798 0 None -8 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@H]1CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
CHEMBL373402 135798 0 None -8 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@H]1CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
46914621 15232 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 350 6 0 4 4.1 CCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
CHEMBL1214895 15232 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 350 6 0 4 4.1 CCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
122187375 122494 0 None 5 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 443 5 0 5 5.6 CCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609140 122494 0 None 5 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 443 5 0 5 5.6 CCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
4211 57502 81 None -2 4 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
CHEMBL1670 57502 81 None -2 4 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
11737032 84578 0 None -10 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 222 0 1 2 1.4 O=C1c2c(Cl)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL223896 84578 0 None -10 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 222 0 1 2 1.4 O=C1c2c(Cl)cccc2C2CNCCN12 10.1021/jm0612968
44316017 203731 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 228 2 1 2 2.2 C[C@H](N)CN1CCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL80366 203731 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 228 2 1 2 2.2 C[C@H](N)CN1CCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2003.05.001
6761 67442 17 None -7 18 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67442 17 None -7 18 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
59752584 180903 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 323 2 1 3 4.1 CC(C)n1nc2c(c1-c1ccc(Cl)c(Cl)c1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4764808 180903 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 323 2 1 3 4.1 CC(C)n1nc2c(c1-c1ccc(Cl)c(Cl)c1)CCNCC2 10.1016/j.bmcl.2020.127669
118717213 120055 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 323 4 3 2 2.5 CCCCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343664 120055 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 323 4 3 2 2.5 CCCCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545802 120055 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 323 4 3 2 2.5 CCCCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
10244831 193208 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 309 3 2 3 4.6 CSc1ccc(NC(=O)Nc2ccnc3ccccc23)cc1 10.1016/s0960-894x(01)00343-2
CHEMBL54062 193208 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 309 3 2 3 4.6 CSc1ccc(NC(=O)Nc2ccnc3ccccc23)cc1 10.1016/s0960-894x(01)00343-2
9888804 193311 2 None -63 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 428 4 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)nc1)CC2 10.1016/j.bmcl.2005.08.004
CHEMBL54719 193311 2 None -63 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 428 4 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)nc1)CC2 10.1016/j.bmcl.2005.08.004
10811153 168542 0 None -7 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 403 3 1 3 5.1 CSc1cc2c(cc1C(F)(F)C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
CHEMBL44015 168542 0 None -7 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 403 3 1 3 5.1 CSc1cc2c(cc1C(F)(F)C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
44298173 193811 0 None -31 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cnccc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL55331 193811 0 None -31 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cnccc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
44298236 194278 0 None -19 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 408 3 1 4 5.4 Cc1cc2c(cc1Cl)N(C(=O)Nc1cnc(Oc3cccnc3C)c(C)c1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL55964 194278 0 None -19 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 408 3 1 4 5.4 Cc1cc2c(cc1Cl)N(C(=O)Nc1cnc(Oc3cccnc3C)c(C)c1)CC2 10.1016/s0960-894x(00)00364-4
10435572 149555 0 None -12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 451 6 0 5 4.6 COc1ccc(N2Cc3c(c4cccc(F)c4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
CHEMBL395098 149555 0 None -12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 451 6 0 5 4.6 COc1ccc(N2Cc3c(c4cccc(F)c4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
50878551 90300 60 None -1 18 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90300 60 None -1 18 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
9888804 193311 2 None -63 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 428 4 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL54719 193311 2 None -63 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 428 4 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
11121216 29910 0 None -154 15 Human 6.5 pKi = 6.5 Binding
Binding affinities towards 5-hydroxytryptamine 2B receptorBinding affinities towards 5-hydroxytryptamine 2B 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
CHEMBL138989 29910 0 None -154 15 Human 6.5 pKi = 6.5 Binding
Binding affinities towards 5-hydroxytryptamine 2B receptorBinding affinities towards 5-hydroxytryptamine 2B 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
3845148 65316 1 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 320 5 0 3 3.8 c1ccc(CCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
CHEMBL1834251 65316 1 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 320 5 0 3 3.8 c1ccc(CCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
16063181 154882 0 None -34 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 319 3 1 3 3.5 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CCNC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL403764 154882 0 None -34 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 319 3 1 3 3.5 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CCNC3)cc1 10.1016/j.bmcl.2008.01.090
142601337 185378 0 None -97 5 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4869695 185378 0 None -97 5 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
145990659 166361 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 273 1 4 6 1.7 NC1=NC2(CCCCC2)NC(Nc2cccc(O)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4286819 166361 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 273 1 4 6 1.7 NC1=NC2(CCCCC2)NC(Nc2cccc(O)c2)=N1 10.1021/acsmedchemlett.8b00300
9906447 193894 1 None -4365 13 Human 5.5 pKi = 5.5 Binding
Binding affinity to human recombinant 5HT2B receptorBinding affinity to human recombinant 5HT2B receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL2031738 193894 1 None -4365 13 Human 5.5 pKi = 5.5 Binding
Binding affinity to human recombinant 5HT2B receptorBinding affinity to human recombinant 5HT2B receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL555146 193894 1 None -4365 13 Human 5.5 pKi = 5.5 Binding
Binding affinity to human recombinant 5HT2B receptorBinding affinity to human recombinant 5HT2B receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
9909089 186375 0 None -2511 7 Human 6.5 pKi = 6.5 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL490417 186375 0 None -2511 7 Human 6.5 pKi = 6.5 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
10217207 71753 0 None -398 3 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 463 7 0 4 5.3 COc1ccc(N2CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
CHEMBL197807 71753 0 None -398 3 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 463 7 0 4 5.3 COc1ccc(N2CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
10288601 71825 0 None -100 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 465 7 0 5 4.2 COc1ccc(N2CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCOCC1 10.1016/j.bmcl.2005.08.004
CHEMBL198007 71825 0 None -100 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 465 7 0 5 4.2 COc1ccc(N2CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCOCC1 10.1016/j.bmcl.2005.08.004
50898777 56131 0 None -2951 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 441 9 1 6 3.6 COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632158 56131 0 None -2951 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 441 9 1 6 3.6 COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
44414105 137644 0 None -79 2 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 488 7 0 4 5.9 COc1ccc(N2CC=C(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCC(C)(C)CC1 10.1016/j.bmcl.2006.05.034
CHEMBL376962 137644 0 None -79 2 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 488 7 0 4 5.9 COc1ccc(N2CC=C(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCC(C)(C)CC1 10.1016/j.bmcl.2006.05.034
19356259 101546 0 None -158 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Cl)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL301784 101546 0 None -158 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Cl)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
44298192 167576 0 None -100 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 472 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(I)ccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL433060 167576 0 None -100 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 472 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(I)ccc32)cn1 10.1016/s0960-894x(00)00364-4
187 3324 15 None -288 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 10.1016/S0960-894X(96)00503-3
3693566 3324 15 None -288 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 10.1016/S0960-894X(96)00503-3
CHEMBL88402 3324 15 None -288 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 10.1016/S0960-894X(96)00503-3
11766873 205005 0 None -31 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 558 11 3 8 2.8 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL89967 205005 0 None -31 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 558 11 3 8 2.8 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C)cc1 10.1016/S0960-894X(96)00503-3
18931123 205489 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 601 12 4 9 2.5 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(NC(C)=O)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL92809 205489 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 601 12 4 9 2.5 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(NC(C)=O)cc1 10.1016/S0960-894X(96)00503-3
153287567 171808 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 292 1 1 2 4.3 Cc1ccc(N2C[C@@]3(C)NCC[C@H]3c3cc(C)ccc32)cc1 10.1021/acsmedchemlett.9b00225
CHEMBL4476396 171808 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 292 1 1 2 4.3 Cc1ccc(N2C[C@@]3(C)NCC[C@H]3c3cc(C)ccc32)cc1 10.1021/acsmedchemlett.9b00225
153287557 175495 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 420 1 1 2 5.2 C[C@@]12CN(c3ccc(Br)cc3)c3ccc(Br)cc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4591108 175495 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 420 1 1 2 5.2 C[C@@]12CN(c3ccc(Br)cc3)c3ccc(Br)cc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
11463745 151244 0 None -79 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 400 6 0 4 4.4 COc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.029
CHEMBL396505 151244 0 None -79 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 400 6 0 4 4.4 COc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.029
11750162 151269 0 None -100 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 408 6 0 4 4.6 COc1ccc(N2Cc3cc(C)cc(C)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL396527 151269 0 None -100 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 408 6 0 4 4.6 COc1ccc(N2Cc3cc(C)cc(C)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
179 396 107 None -17 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1021/jm070516u
2159 396 107 None -17 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1021/jm070516u
963 396 107 None -17 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1021/jm070516u
CHEMBL243712 396 107 None -17 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1021/jm070516u
DB06288 396 107 None -17 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1021/jm070516u
10440 2632 15 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
139030523 2632 15 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
CHEMBL4449712 2632 15 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
155531067 171043 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 369 7 3 6 3.3 Nc1nc(NCCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
CHEMBL4465512 171043 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 369 7 3 6 3.3 Nc1nc(NCCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
155558626 174179 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 355 6 3 6 2.9 Nc1nc(NCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
CHEMBL4561016 174179 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 355 6 3 6 2.9 Nc1nc(NCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
44243470 88655 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 431 5 1 6 5.5 CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334981 88655 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 431 5 1 6 5.5 CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2365395 88655 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 431 5 1 6 5.5 CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
18931217 205053 0 None -39 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 623 12 4 10 1.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(S(N)(=O)=O)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL90267 205053 0 None -39 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 623 12 4 10 1.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(S(N)(=O)=O)cc1 10.1016/S0960-894X(96)00503-3
44439167 90112 0 None -316 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
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 -316 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
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
71062790 159494 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ncccc1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL4108274 159494 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ncccc1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
44420683 83704 0 None -2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 284 0 1 2 2.6 CC1(C)CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
CHEMBL220789 83704 0 None -2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 284 0 1 2 2.6 CC1(C)CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
1355 1972 82 None -1 16 Human 7.5 pKi = 7.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
142 1972 82 None -1 16 Human 7.5 pKi = 7.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
CHEMBL478 1972 82 None -1 16 Human 7.5 pKi = 7.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
DB12110 1972 82 None -1 16 Human 7.5 pKi = 7.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
11151653 90656 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397896 90656 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
1355 1972 82 None -1 16 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2005.10.029
142 1972 82 None -1 16 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2005.10.029
CHEMBL478 1972 82 None -1 16 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2005.10.029
DB12110 1972 82 None -1 16 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2005.10.029
CHEMBL5084249 213123 0 None -38 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCN(CC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
1704 3453 76 None -10 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 356 3 2 3 4.5 O=C(Nc1cc(C)nc2c1cc(F)cc2F)Nc1ccc(cc1)N(C)C 10.1016/j.bmcl.2013.06.057
4331799 3453 76 None -10 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 356 3 2 3 4.5 O=C(Nc1cc(C)nc2c1cc(F)cc2F)Nc1ccc(cc1)N(C)C 10.1016/j.bmcl.2013.06.057
CHEMBL1334465 3453 76 None -10 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 356 3 2 3 4.5 O=C(Nc1cc(C)nc2c1cc(F)cc2F)Nc1ccc(cc1)N(C)C 10.1016/j.bmcl.2013.06.057
118055337 176787 0 None -28 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 220 0 1 2 2.0 CC1(C)CN2CCNCc3ccc(F)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4637882 176787 0 None -28 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 220 0 1 2 2.0 CC1(C)CN2CCNCc3ccc(F)c1c32 10.1016/j.bmcl.2019.126929
44582675 189099 0 None -436 16 Human 6.5 pKi = 6.5 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 189099 0 None -436 16 Human 6.5 pKi = 6.5 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
3336 94547 27 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1021/jm100600y
CHEMBL1405922 94547 27 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1021/jm100600y
CHEMBL254832 94547 27 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1021/jm100600y
16573 177035 30 None -16 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
CHEMBL464099 177035 30 None -16 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
168273532 189582 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assayDisplacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assay
ChEMBL 450 3 2 3 7.8 Clc1ccc(Nc2nc3ccccc3c3[nH]c([C@@H]4C[C@@H]5CCC[C@@H](C5)C4)nc23)cc1Cl 10.1021/acs.jmedchem.2c01170
CHEMBL5174205 189582 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assayDisplacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assay
ChEMBL 450 3 2 3 7.8 Clc1ccc(Nc2nc3ccccc3c3[nH]c([C@@H]4C[C@@H]5CCC[C@@H](C5)C4)nc23)cc1Cl 10.1021/acs.jmedchem.2c01170
23290944 81400 0 None -213 7 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164350 81400 0 None -213 7 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
6075 149563 36 None -8 16 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 149563 36 None -8 16 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
44247568 81748 51 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 337 5 0 5 3.0 Cc1cc(OCCN2CCOCC2)nn1-c1ccc2ccccc2c1 10.1021/jm3007323
CHEMBL2170062 81748 51 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 337 5 0 5 3.0 Cc1cc(OCCN2CCOCC2)nn1-c1ccc2ccccc2c1 10.1021/jm3007323
16118923 59815 0 None -30 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1642866 59815 0 None -30 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1739656 59815 0 None -30 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
11695000 88628 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337490 88628 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365083 88628 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
122178706 120845 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 8 0 5 5.4 CCCCC(C)Oc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581251 120845 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 8 0 5 5.4 CCCCC(C)Oc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
3038495 699 30 None -22 19 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm100600y
7625 699 30 None -22 19 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm100600y
CHEMBL25236 699 30 None -22 19 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm100600y
11948707 165603 0 None -83 13 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
CHEMBL426317 165603 0 None -83 13 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
5624 32459 12 None 5 10 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL1203324 32459 12 None 5 10 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL141343 32459 12 None 5 10 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
56675413 65324 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 378 8 0 4 4.6 COc1ccccc1CCCCN1CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmcl.2011.08.029
CHEMBL1834259 65324 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 378 8 0 4 4.6 COc1ccccc1CCCCN1CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmcl.2011.08.029
134143302 144771 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 503 9 5 9 0.6 CC(=O)NCCNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3913293 144771 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 503 9 5 9 0.6 CC(=O)NCCNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
90181065 160253 0 None 5 2 Mouse 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@@H](COc2cccc(Cl)c2)C1 nan
CHEMBL4114519 160253 0 None 5 2 Mouse 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@@H](COc2cccc(Cl)c2)C1 nan
155566272 175205 0 None 4 5 Human 6.5 pKi = 6.5 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 543 8 3 8 5.1 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CSc2ccccc2F)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL4584140 175205 0 None 4 5 Human 6.5 pKi = 6.5 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 543 8 3 8 5.1 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CSc2ccccc2F)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL5089613 213432 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL None None None C=C[C@H]1CN2CCc3c([nH]c4cccc(O)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
16115654 136437 0 None -38 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.1 Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374562 136437 0 None -38 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.1 Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
44451373 95875 1 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 187 0 1 2 2.1 c1cc2ccc3c(c2o1)CCNCC3 10.1016/j.bmc.2007.12.009
CHEMBL261490 95875 1 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 187 0 1 2 2.1 c1cc2ccc3c(c2o1)CCNCC3 10.1016/j.bmc.2007.12.009
50878551 90300 60 None -1 18 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90300 60 None -1 18 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
118706296 120001 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 308 2 3 2 1.3 CC(=O)NC1c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3310119 120001 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 308 2 3 2 1.3 CC(=O)NC1c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3545441 120001 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 308 2 3 2 1.3 CC(=O)NC1c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
134143536 144972 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 419 6 4 8 1.7 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H](C4CCC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3914843 144972 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 419 6 4 8 1.7 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H](C4CCC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
71459269 82533 0 None -1479 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
CHEMBL2181166 82533 0 None -1479 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
58911532 90659 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 244 2 1 2 1.6 CCCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397899 90659 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 244 2 1 2 1.6 CCCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
11176570 90675 0 None -8 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2cc(C(F)(F)F)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397915 90675 0 None -8 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2cc(C(F)(F)F)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
56661666 65325 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 378 8 0 4 4.6 COc1cccc(CCCCN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1016/j.bmcl.2011.08.029
CHEMBL1834260 65325 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 378 8 0 4 4.6 COc1cccc(CCCCN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1016/j.bmcl.2011.08.029
11150514 84439 0 None -3 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@H]2CNCCN12 10.1021/jm0612968
CHEMBL223584 84439 0 None -3 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@H]2CNCCN12 10.1021/jm0612968
16071847 59814 0 None -229 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642865 59814 0 None -229 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739655 59814 0 None -229 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
11195293 90643 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@@]12CNCCN1C(=O)c1ccccc1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397883 90643 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@@]12CNCCN1C(=O)c1ccccc1C2 10.1016/j.bmcl.2013.04.061
90181070 159978 0 None 1 3 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 381 5 0 5 2.4 Cc1ccnc(OC[C@H]2CN(CC(=O)N3c4ccccc4CC3C)CCO2)c1 nan
CHEMBL4112412 159978 0 None 1 3 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 381 5 0 5 2.4 Cc1ccnc(OC[C@H]2CN(CC(=O)N3c4ccccc4CC3C)CCO2)c1 nan
136118621 75885 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2058420 75885 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
4943 192804 100 None 1 2 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 178 2 1 1 3.6 CC(C)c1cccc(C(C)C)c1O nan
CHEMBL526 192804 100 None 1 2 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 178 2 1 1 3.6 CC(C)c1cccc(C(C)C)c1O nan
135399666 168187 4 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL437314 168187 4 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
46884034 7832 0 None -870 2 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 347 3 2 2 3.3 O=C(NCc1ccc(-c2ccc(Cl)cc2)cc1F)N1CCNCC1 10.1016/j.bmcl.2010.01.107
CHEMBL1090397 7832 0 None -870 2 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 347 3 2 2 3.3 O=C(NCc1ccc(-c2ccc(Cl)cc2)cc1F)N1CCNCC1 10.1016/j.bmcl.2010.01.107
118055294 176890 0 None -24 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 204 1 1 3 1.2 COc1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4639115 176890 0 None -24 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 204 1 1 3 1.2 COc1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
56682068 65326 0 None 16 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 378 8 0 4 4.6 COc1ccc(CCCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
CHEMBL1834261 65326 0 None 16 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 378 8 0 4 4.6 COc1ccc(CCCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
4189 205185 91 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205185 91 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205185 91 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
136118651 75956 0 None 1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058706 75956 0 None 1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
127052458 140196 0 None -35 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818056 140196 0 None -35 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
9881119 203752 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 232 2 1 3 1.7 C[C@H](N)CN1CCc2ccc3c(c21)CCCO3 10.1016/j.bmcl.2003.05.001
CHEMBL80482 203752 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 232 2 1 3 1.7 C[C@H](N)CN1CCc2ccc3c(c21)CCCO3 10.1016/j.bmcl.2003.05.001
117209864 185442 1 None -1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4870675 185442 1 None -1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
127052458 140196 0 None -35 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818056 140196 0 None -35 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
168284710 190987 0 None -17 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 509 6 0 5 5.8 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccc(Br)cc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5195241 190987 0 None -17 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 509 6 0 5 5.8 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccc(Br)cc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
135398745 2858 108 None -5 66 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2858 108 None -5 66 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2858 108 None -5 66 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2858 108 None -5 66 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
127035066 135885 0 None 7 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 507 14 0 7 5.2 COc1ccc(OC)c(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
CHEMBL3735434 135885 0 None 7 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 507 14 0 7 5.2 COc1ccc(OC)c(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
156021327 177549 0 None -33 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 224 0 1 3 1.6 Clc1ccc2c3c1OCCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4648457 177549 0 None -33 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 224 0 1 3 1.6 Clc1ccc2c3c1OCCN3CCNC2 10.1016/j.bmcl.2019.126929
132075278 162082 0 None -6 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
CHEMBL4169752 162082 0 None -6 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
2683 102402 24 None -501 16 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102402 24 None -501 16 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102402 24 None -501 16 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
3598 187228 73 None -2 7 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
CHEMBL496 187228 73 None -2 7 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
136118635 75944 0 None 5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2cccc(Br)c12 10.1016/j.bmc.2013.09.011
CHEMBL2058694 75944 0 None 5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2cccc(Br)c12 10.1016/j.bmc.2013.09.011
16115148 84401 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 206 0 1 2 0.9 O=C1c2c(F)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL223469 84401 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 206 0 1 2 0.9 O=C1c2c(F)cccc2C2CNCCN12 10.1021/jm0612968
156014235 176594 0 None -20 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 240 0 1 3 2.4 Clc1ccc2c3c1SCCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4634836 176594 0 None -20 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 240 0 1 3 2.4 Clc1ccc2c3c1SCCN3CCNC2 10.1016/j.bmcl.2019.126929
53324045 56761 0 None -9 16 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644980 56761 0 None -9 16 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
11253485 141434 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 204 0 2 3 0.5 O=C1c2c(O)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL387344 141434 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 204 0 2 3 0.5 O=C1c2c(O)cccc2C2CNCCN12 10.1021/jm0612968
44409101 140706 0 None -23 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 233 2 1 4 1.0 COCc1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL383051 140706 0 None -23 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 233 2 1 4 1.0 COCc1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
18735305 203215 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 320 2 1 2 2.1 C[C@H](N)CN1CCc2cc(F)c(I)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL76301 203215 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 320 2 1 2 2.1 C[C@H](N)CN1CCc2cc(F)c(I)cc21 10.1016/j.bmcl.2003.05.001
44404883 71703 26 None -2 5 Human 7.4 pKi = 7.4 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL197664 71703 26 None -2 5 Human 7.4 pKi = 7.4 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
44364215 39375 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 202 2 2 2 2.0 COc1ccc2[nH]cc(C3CC3N)c2c1 10.1021/jm980318q
CHEMBL147434 39375 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 202 2 2 2 2.0 COc1ccc2[nH]cc(C3CC3N)c2c1 10.1021/jm980318q
118464425 137768 0 None 3 9 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770981 137768 0 None 3 9 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
145976085 163102 0 None 2 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4204576 163102 0 None 2 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
44407453 74039 0 None -9 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 349 5 1 3 5.0 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1Cl 10.1016/j.bmcl.2005.10.029
CHEMBL202538 74039 0 None -9 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 349 5 1 3 5.0 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1Cl 10.1016/j.bmcl.2005.10.029
11163458 136032 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 298 2 1 2 2.8 CCCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL373905 136032 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 298 2 1 2 2.8 CCCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
49865831 15970 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 296 2 1 3 3.0 CCCNC(=O)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224033 15970 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 296 2 1 3 3.0 CCCNC(=O)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
132060720 161927 0 None 2 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4167315 161927 0 None 2 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
11206703 90647 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
CHEMBL2397887 90647 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
10528314 171305 0 None -12 3 Human 7.4 pKi = 7.4 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 469 3 1 3 6.7 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(C(C)(C)C)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL446942 171305 0 None -12 3 Human 7.4 pKi = 7.4 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 469 3 1 3 6.7 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(C(C)(C)C)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
240 929 39 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
2769 929 39 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
44279790 929 39 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
660 929 39 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL1729 929 39 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL560739 929 39 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
DB00604 929 39 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
18005120 193288 0 None -100 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 460 4 1 5 5.9 CSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL54560 193288 0 None -100 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 460 4 1 5 5.9 CSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
44298086 193539 0 None -39 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c2cc(Cl)c(C)c3Cl)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL55079 193539 0 None -39 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c2cc(Cl)c(C)c3Cl)cn1 10.1016/s0960-894x(00)00364-4
44298234 195050 0 None -25 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 462 3 1 4 6.2 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(Oc3cccnc3C)c(Cl)c1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL56508 195050 0 None -25 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 462 3 1 4 6.2 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(Oc3cccnc3C)c(Cl)c1)CC2 10.1016/s0960-894x(00)00364-4
10255548 86322 0 None -12 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 467 6 0 5 5.1 COc1ccc(N2Cc3c(c4cc(Cl)ccc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
CHEMBL232046 86322 0 None -12 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 467 6 0 5 5.1 COc1ccc(N2Cc3c(c4cc(Cl)ccc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
2726 904 64 None -19 73 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
621 904 64 None -19 73 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
83 904 64 None -19 73 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
CHEMBL71 904 64 None -19 73 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
DB00477 904 64 None -19 73 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
25235287 177132 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 302 0 1 2 4.5 Cc1nccc2c1C(C)(C)Nc1cc(Br)ccc1-2 10.1021/acs.jnatprod.9b01107
CHEMBL4642292 177132 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 302 0 1 2 4.5 Cc1nccc2c1C(C)(C)Nc1cc(Br)ccc1-2 10.1021/acs.jnatprod.9b01107
136188797 57009 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@H]1SC[C@](C)(C(=O)O)N1C 10.1021/acs.jnatprod.7b00317
CHEMBL1651094 57009 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@H]1SC[C@](C)(C(=O)O)N1C 10.1021/acs.jnatprod.7b00317
136030744 57008 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@@H]1SC[C@](C)(C(=O)O)N1C 10.1021/np100588c
CHEMBL1651093 57008 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@@H]1SC[C@](C)(C(=O)O)N1C 10.1021/np100588c
11288140 84331 0 None -12 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 213 0 1 3 0.7 N#Cc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL223090 84331 0 None -12 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 213 0 1 3 0.7 N#Cc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
46830177 7963 29 None -4365 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 378 6 2 4 3.6 COc1cc(OC2CCC(C)(C)CC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1091105 7963 29 None -4365 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 378 6 2 4 3.6 COc1cc(OC2CCC(C)(C)CC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
118055319 176942 0 None -20 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 256 1 1 2 2.6 FC(F)(F)CC1CN2CCNCc3cccc1c32 10.1016/j.bmcl.2019.126929
CHEMBL4639970 176942 0 None -20 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 256 1 1 2 2.6 FC(F)(F)CC1CN2CCNCc3cccc1c32 10.1016/j.bmcl.2019.126929
10050022 165792 0 None -39 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 462 7 0 4 5.4 COc1ccc(C2CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL427398 165792 0 None -39 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 462 7 0 4 5.4 COc1ccc(C2CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
49850870 56080 0 None -3162 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 424 6 1 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631535 56080 0 None -3162 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 424 6 1 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm100714c
49850570 56163 0 None -2511 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 417 6 2 4 4.0 CCNC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1632220 56163 0 None -2511 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 417 6 2 4 4.0 CCNC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
44298140 100080 0 None -79 3 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.2 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3ccc(C(F)(F)F)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL291510 100080 0 None -79 3 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.2 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3ccc(C(F)(F)F)cc32)cn1 10.1016/s0960-894x(00)00364-4
18931172 105680 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 578 11 3 8 3.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccccc1Cl 10.1016/S0960-894X(96)00503-3
CHEMBL313745 105680 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 578 11 3 8 3.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccccc1Cl 10.1016/S0960-894X(96)00503-3
18931163 205038 0 None -50 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 569 11 3 9 2.4 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C#N)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL90175 205038 0 None -50 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 569 11 3 9 2.4 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C#N)cc1 10.1016/S0960-894X(96)00503-3
18931420 205109 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 628 12 3 9 3.4 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(OC(F)(F)F)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL90565 205109 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 628 12 3 9 3.4 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(OC(F)(F)F)cc1 10.1016/S0960-894X(96)00503-3
127052465 140187 0 None -10 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 340 5 0 3 3.6 O=C1c2ccccc2C(=O)N1CCCCN1CCC2CCCCC2C1 10.1016/j.bmc.2016.05.053
CHEMBL3817911 140187 0 None -10 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 340 5 0 3 3.6 O=C1c2ccccc2C(=O)N1CCCCN1CCC2CCCCC2C1 10.1016/j.bmc.2016.05.053
10835585 101378 0 None -63 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 414 4 1 4 4.7 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2cc(C(F)(F)F)ccc21 10.1016/s0960-894x(00)00365-6
CHEMBL300618 101378 0 None -63 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 414 4 1 4 4.7 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2cc(C(F)(F)F)ccc21 10.1016/s0960-894x(00)00365-6
1836 2544 56 None -69 15 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 2544 56 None -69 15 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 2544 56 None -69 15 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 2544 56 None -69 15 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 2544 56 None -69 15 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
10597140 62701 0 None -251 6 Human 5.4 pKi = 5.4 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 400 5 0 3 4.5 CC1CCN(CC[C@H]2CCCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
CHEMBL1788231 62701 0 None -251 6 Human 5.4 pKi = 5.4 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 400 5 0 3 4.5 CC1CCN(CC[C@H]2CCCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
1703 3450 90 None -158 6 Human 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 319 2 2 5 3.7 O=C(Nc1ccnc2c1nccc2)Nc1ccc2c(c1)oc(n2)C 10.1016/s0960-894x(01)00343-2
6604926 3450 90 None -158 6 Human 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 319 2 2 5 3.7 O=C(Nc1ccnc2c1nccc2)Nc1ccc2c(c1)oc(n2)C 10.1016/s0960-894x(01)00343-2
CHEMBL291536 3450 90 None -158 6 Human 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 319 2 2 5 3.7 O=C(Nc1ccnc2c1nccc2)Nc1ccc2c(c1)oc(n2)C 10.1016/s0960-894x(01)00343-2
44343212 9730 0 None -100 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor (human cloned receptor) in HEK 293 cells using [3H]5-HT as radioligand.Binding affinity towards 5-hydroxytryptamine 2B receptor (human cloned receptor) in HEK 293 cells using [3H]5-HT as radioligand.
ChEMBL 400 5 0 3 4.5 CC1CCN(CCC2CCCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
CHEMBL114012 9730 0 None -100 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor (human cloned receptor) in HEK 293 cells using [3H]5-HT as radioligand.Binding affinity towards 5-hydroxytryptamine 2B receptor (human cloned receptor) in HEK 293 cells using [3H]5-HT as radioligand.
ChEMBL 400 5 0 3 4.5 CC1CCN(CCC2CCCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
49865890 15991 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 310 1 1 3 3.5 Cc1ccccc1NC(=O)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224106 15991 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 310 1 1 3 3.5 Cc1ccccc1NC(=O)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
57799324 88649 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 236 0 2 2 1.4 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337501 88649 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 236 0 2 2 1.4 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365359 88649 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 236 0 2 2 1.4 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
11312173 181519 0 None -3 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 285 2 1 3 3.1 Fc1ccc(-c2c3c(nn2C2CCC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4782005 181519 0 None -3 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 285 2 1 3 3.1 Fc1ccc(-c2c3c(nn2C2CCC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
127034715 135858 0 None 35 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 537 15 0 8 5.2 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735261 135858 0 None 35 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 537 15 0 8 5.2 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
107715 199250 18 None -14 20 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 199250 18 None -14 20 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 199250 18 None -14 20 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
189 3423 31 None -5 18 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm100600y
5163 3423 31 None -5 18 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm100600y
CHEMBL297784 3423 31 None -5 18 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm100600y
11694810 120015 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3310123 120015 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3545474 120015 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
11694810 120015 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3310123 120015 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545474 120015 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
10531 1387 18 None -15 24 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 1387 18 None -15 24 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 1387 18 None -15 24 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 1387 18 None -15 24 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 1387 18 None -15 24 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
118706301 120014 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 265 1 2 1 2.2 CC1c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3310122 120014 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 265 1 2 1 2.2 CC1c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3545473 120014 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 265 1 2 1 2.2 CC1c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
168293874 191571 0 None 5 11 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 191571 0 None 5 11 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
145988313 166671 0 None 104 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
CHEMBL4292326 166671 0 None 104 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
168268877 189367 0 None 1 12 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 189367 0 None 1 12 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
127035064 135935 0 None 23 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 477 13 0 6 5.2 COc1cccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
CHEMBL3735911 135935 0 None 23 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 477 13 0 6 5.2 COc1cccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
135 2486 38 None -3 58 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2486 38 None -3 58 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2486 38 None -3 58 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2486 38 None -3 58 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2486 38 None -3 58 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
11681111 120060 0 None -7 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 309 3 2 2 2.4 CCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343666 120060 0 None -7 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 309 3 2 2 2.4 CCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545815 120060 0 None -7 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 309 3 2 2 2.4 CCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
16062783 154471 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 323 3 1 4 3.5 COc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL401509 154471 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 323 3 1 4 3.5 COc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
14049689 196756 8 None 20 2 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 1541 28 21 42 -12.4 CC(O)COC[C@H]1O[C@@H]2O[C@@H]3[C@@H](COCC(C)O)O[C@H](O[C@@H]4[C@@H](COCC(C)O)O[C@H](O[C@@H]5[C@@H](COCC(C)O)O[C@H](O[C@@H]6[C@@H](COCC(C)O)O[C@H](O[C@@H]7[C@@H](COCC(C)O)O[C@H](O[C@@H]8[C@@H](COCC(C)O)O[C@H](O[C@H]1[C@H](O)[C@H]2O)[C@H](O)[C@H]8O)[C@H](O)[C@H]7O)[C@H](O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)[C@H]4O)[C@H](O)[C@H]3O nan
CHEMBL577294 196756 8 None 20 2 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 1541 28 21 42 -12.4 CC(O)COC[C@H]1O[C@@H]2O[C@@H]3[C@@H](COCC(C)O)O[C@H](O[C@@H]4[C@@H](COCC(C)O)O[C@H](O[C@@H]5[C@@H](COCC(C)O)O[C@H](O[C@@H]6[C@@H](COCC(C)O)O[C@H](O[C@@H]7[C@@H](COCC(C)O)O[C@H](O[C@@H]8[C@@H](COCC(C)O)O[C@H](O[C@H]1[C@H](O)[C@H]2O)[C@H](O)[C@H]8O)[C@H](O)[C@H]7O)[C@H](O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)[C@H]4O)[C@H](O)[C@H]3O nan
58911653 90671 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 244 1 1 2 1.5 CCc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397911 90671 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 244 1 1 2 1.5 CCc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
57799306 88666 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337493 88666 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365469 88666 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
9899500 67532 0 None -14 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](CNC[C@H]1C)C2 10.1016/j.bmcl.2005.11.083
CHEMBL191054 67532 0 None -14 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](CNC[C@H]1C)C2 10.1016/j.bmcl.2005.11.083
168281367 190297 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 395 6 0 5 4.3 COc1cc2c(cc1OC)-c1c(OC)c(OCC3CC3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5185086 190297 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 395 6 0 5 4.3 COc1cc2c(cc1OC)-c1c(OC)c(OCC3CC3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
118729232 120150 0 None 9 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 5.0 CN(C)[C@H]1Cc2ccccc2[C@H](C2CCCCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402655 120150 0 None 9 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 5.0 CN(C)[C@H]1Cc2ccccc2[C@H](C2CCCCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547008 120150 0 None 9 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 5.0 CN(C)[C@H]1Cc2ccccc2[C@H](C2CCCCCCC2)C1 10.1016/j.bmc.2015.01.060
90188146 120173 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(Br)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402674 120173 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(Br)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547135 120173 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(Br)c2)C1 10.1016/j.bmc.2015.01.060
16062912 154601 0 None -56 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 351 3 1 3 3.7 Fc1ccc(Cc2nc3c(c(-c4ccc(F)cc4)n2)CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL402164 154601 0 None -56 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 351 3 1 3 3.7 Fc1ccc(Cc2nc3c(c(-c4ccc(F)cc4)n2)CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
71461050 82550 0 None -13 5 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181189 82550 0 None -13 5 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1021/jm300943r
45486891 195255 0 None -83 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 449 6 3 4 4.1 O=C1Cc2c(ccc3c2OC[C@H](CNCCCC2CCc4c([nH]c5ccc(F)cc45)C2)O3)N1 10.1016/j.bmcl.2009.08.050
CHEMBL566379 195255 0 None -83 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 449 6 3 4 4.1 O=C1Cc2c(ccc3c2OC[C@H](CNCCCC2CCc4c([nH]c5ccc(F)cc45)C2)O3)N1 10.1016/j.bmcl.2009.08.050
145974750 164192 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 223 2 2 4 1.6 C[C@H]1SC(c2ccccc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4217810 164192 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 223 2 2 4 1.6 C[C@H]1SC(c2ccccc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
127052465 140187 0 None -10 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 340 5 0 3 3.6 O=C1c2ccccc2C(=O)N1CCCCN1CCC2CCCCC2C1 10.1016/j.bmc.2016.05.053
CHEMBL3817911 140187 0 None -10 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 340 5 0 3 3.6 O=C1c2ccccc2C(=O)N1CCCCN1CCC2CCCCC2C1 10.1016/j.bmc.2016.05.053
89901924 120181 0 None -100 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402667 120181 0 None -100 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547153 120181 0 None -100 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(F)cc2)C1 10.1016/j.bmc.2015.01.060
16062651 95188 0 None -13 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 3 1 3 3.1 CC(C)Cc1nc2c(c(-c3ccc(F)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
CHEMBL257944 95188 0 None -13 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 3 1 3 3.1 CC(C)Cc1nc2c(c(-c3ccc(F)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
132007291 148401 0 None -33 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 395 3 2 4 4.3 Fc1ccc(C#Cc2nc(NCc3cccc(Cl)c3)c3nc[nH]c3n2)cc1F 10.1021/acs.jmedchem.6b01183
CHEMBL3941980 148401 0 None -33 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 395 3 2 4 4.3 Fc1ccc(C#Cc2nc(NCc3cccc(Cl)c3)c3nc[nH]c3n2)cc1F 10.1021/acs.jmedchem.6b01183
1782 2472 81 None -3 23 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
241 2472 81 None -3 23 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
4168 2472 81 None -3 23 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
CHEMBL86 2472 81 None -3 23 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
DB01233 2472 81 None -3 23 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
11171955 90648 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.2 C[C@@H]1c2ccccc2C(=O)N2CCNC[C@@H]12 10.1016/j.bmcl.2013.04.061
CHEMBL2397888 90648 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.2 C[C@@H]1c2ccccc2C(=O)N2CCNC[C@@H]12 10.1016/j.bmcl.2013.04.061
16115515 137058 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 290 0 1 2 2.5 O=C1c2c(C(F)(F)F)ccc(Cl)c2[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL375575 137058 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 290 0 1 2 2.5 O=C1c2c(C(F)(F)F)ccc(Cl)c2[C@@H]2CNCCN12 10.1021/jm0612968
2775690 92565 47 None -15 6 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT2B receptor (unknown origin)Binding affinity to 5-HT2B receptor (unknown origin)
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
CHEMBL2441619 92565 47 None -15 6 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT2B receptor (unknown origin)Binding affinity to 5-HT2B receptor (unknown origin)
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
11848624 88702 0 None 2 6 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL236587 88702 0 None 2 6 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
46230100 197629 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 231 0 2 3 0.9 Cc1ccc2c(c1)N1CCNCCC1NC2=O 10.1016/j.bmcl.2009.12.014
CHEMBL590531 197629 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 231 0 2 3 0.9 Cc1ccc2c(c1)N1CCNCCC1NC2=O 10.1016/j.bmcl.2009.12.014
118717211 120054 0 None -33 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 295 2 3 2 1.7 CCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343663 120054 0 None -33 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 295 2 3 2 1.7 CCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545801 120054 0 None -33 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 295 2 3 2 1.7 CCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
44451422 166860 2 None -9 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 199 0 1 1 2.2 Fc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL429689 166860 2 None -9 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 199 0 1 1 2.2 Fc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
75201901 165861 14 None -301 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK 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 -301 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK 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
118729238 120154 0 None -52 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccccc2Br)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402659 120154 0 None -52 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccccc2Br)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547012 120154 0 None -52 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccccc2Br)C1 10.1016/j.bmc.2015.01.060
118729240 120155 0 None -6 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc([N+](=O)[O-])cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402660 120155 0 None -6 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc([N+](=O)[O-])cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547013 120155 0 None -6 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc([N+](=O)[O-])cc2)C1 10.1016/j.bmc.2015.01.060
46884098 8088 0 None -954 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 286 4 2 2 3.1 O=C(NCc1ccc(C2CCCCC2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1092029 8088 0 None -954 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 286 4 2 2 3.1 O=C(NCc1ccc(C2CCCCC2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
142601329 185925 3 None -63 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4877603 185925 3 None -63 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
122187379 122498 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 441 5 0 5 5.3 C=CCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609144 122498 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 441 5 0 5 5.3 C=CCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
122483223 137568 0 None -5 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 455 8 0 5 5.8 COc1ccccc1N1CCN(CCCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3764650 137568 0 None -5 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 455 8 0 5 5.8 COc1ccccc1N1CCN(CCCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3765874 137568 0 None -5 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 455 8 0 5 5.8 COc1ccccc1N1CCN(CCCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
122187382 122500 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 429 4 0 5 5.2 CCN1CC(c2ccccc2)c2cc(OC)c(OC)c3c2C1Cc1cc2c(cc1-3)OCO2 10.1016/j.bmcl.2015.07.012
CHEMBL3609147 122500 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 429 4 0 5 5.2 CCN1CC(c2ccccc2)c2cc(OC)c(OC)c3c2C1Cc1cc2c(cc1-3)OCO2 10.1016/j.bmcl.2015.07.012
137646281 157252 0 None -95 17 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 157252 0 None -95 17 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
122178711 120850 0 None 1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 509 6 0 5 5.8 COc1cc2c(cc1OCc1ccc(Br)cc1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
CHEMBL3581256 120850 0 None 1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 509 6 0 5 5.8 COc1cc2c(cc1OCc1ccc(Br)cc1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
46933845 15971 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224034 15971 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
11957541 1425 38 None -2 16 Human 7.4 pKi = 7.4 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm9803525
1229 1425 38 None -2 16 Human 7.4 pKi = 7.4 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm9803525
147 1425 38 None -2 16 Human 7.4 pKi = 7.4 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm9803525
170617 1425 38 None -2 16 Human 7.4 pKi = 7.4 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm9803525
CHEMBL6616 1425 38 None -2 16 Human 7.4 pKi = 7.4 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm9803525
25117676 198765 0 None -831 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598444 198765 0 None -831 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
53325242 56760 0 None -2 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644978 56760 0 None -2 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
21854226 124071 4 None -1 3 Human 6.4 pKi = 6.4 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 230 3 2 2 2.5 Oc1cccc2[nH]cc(CCN3CCCC3)c12 10.1016/j.bmcl.2005.06.104
CHEMBL364061 124071 4 None -1 3 Human 6.4 pKi = 6.4 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 230 3 2 2 2.5 Oc1cccc2[nH]cc(CCN3CCCC3)c12 10.1016/j.bmcl.2005.06.104
2286 3122 48 None -5 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3122 48 None -5 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3122 48 None -5 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3122 48 None -5 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3122 48 None -5 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
59752589 179236 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 323 2 1 3 4.1 CC(C)n1nc2c(c1-c1ccc(Cl)cc1Cl)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4745055 179236 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 323 2 1 3 4.1 CC(C)n1nc2c(c1-c1ccc(Cl)cc1Cl)CCNCC2 10.1016/j.bmcl.2020.127669
11425677 181743 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 269 1 1 3 3.0 CC(C)(C)n1nc2c(c1-c1ccccc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4784424 181743 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 269 1 1 3 3.0 CC(C)(C)n1nc2c(c1-c1ccccc1)CCNCC2 10.1016/j.bmcl.2020.127669
145975946 163357 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
CHEMBL4207355 163357 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
2406 99925 84 None -27 12 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
CHEMBL290106 99925 84 None -27 12 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
3198 203792 73 None -30 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203792 73 None -30 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203792 73 None -30 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
118055192 176449 0 None -46 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 188 0 1 2 1.7 CC1CN2CCNCc3cccc1c32 10.1016/j.bmcl.2019.126929
CHEMBL4632419 176449 0 None -46 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 188 0 1 2 1.7 CC1CN2CCNCc3cccc1c32 10.1016/j.bmcl.2019.126929
10947658 28475 0 None -39 17 Human 7.4 pKi = 7.4 Binding
Binding affinities against 5-hydroxytryptamine 2B receptorBinding affinities against 5-hydroxytryptamine 2B 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 -39 17 Human 7.4 pKi = 7.4 Binding
Binding affinities against 5-hydroxytryptamine 2B receptorBinding affinities against 5-hydroxytryptamine 2B 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
44409095 75662 0 None -4 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 219 1 1 4 0.8 COc1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL205671 75662 0 None -4 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 219 1 1 4 0.8 COc1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
71618702 142838 0 None 1 4 Mouse 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@H](COc2cccc(Cl)c2)C1 nan
CHEMBL3897835 142838 0 None 1 4 Mouse 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@H](COc2cccc(Cl)c2)C1 nan
156014421 176621 0 None -12 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 256 0 1 3 1.4 [O-][S+]1CCN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4635293 176621 0 None -12 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 256 0 1 3 1.4 [O-][S+]1CCN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
25122654 198834 0 None -54 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
CHEMBL598851 198834 0 None -54 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
135476741 154973 9 None -7 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.8 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL404232 154973 9 None -7 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.8 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccccc23)C1=O 10.1016/j.bmc.2013.09.011
117209962 184276 1 None -16 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4852622 184276 1 None -16 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
136118716 92613 0 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442271 92613 0 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
180 397 50 None -35 39 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 397 50 None -35 39 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 397 50 None -35 39 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 397 50 None -35 39 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 397 50 None -35 39 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
122178703 120842 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 383 5 0 5 4.3 COc1cc2c(cc1OC(C)C)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
CHEMBL3581248 120842 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 383 5 0 5 4.3 COc1cc2c(cc1OC(C)C)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
127049980 140090 0 None 4 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2ccc(Br)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3814485 140090 0 None 4 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2ccc(Br)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
134144970 150228 0 None 4 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 461 8 3 9 2.3 CCCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3956531 150228 0 None 4 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 461 8 3 9 2.3 CCCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
12901777 137458 26 None -7 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 188 0 1 2 0.8 O=C1c2ccccc2C2CNCCN12 10.1021/jm0612968
CHEMBL376455 137458 26 None -7 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 188 0 1 2 0.8 O=C1c2ccccc2C2CNCCN12 10.1021/jm0612968
44407337 73841 0 None -5 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 265 5 1 3 3.4 C=CCN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL202324 73841 0 None -5 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 265 5 1 3 3.4 C=CCN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
45378934 199951 0 None -8 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL605971 199951 0 None -8 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
135449090 188715 3 None -2 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 268 1 1 2 1.9 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL512332 188715 3 None -2 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 268 1 1 2 1.9 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccccc23)N1C 10.1016/j.bmc.2013.09.011
4595 176131 102 None 2 15 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O nan
CHEMBL46 176131 102 None 2 15 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O nan
136118729 92616 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442274 92616 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
10150497 3999 41 None -223 4 Human 6.3 pKi = 6.3 Binding
Inhibition of human 5HT2B receptor expressed in CHO cellsInhibition of human 5HT2B receptor expressed in CHO cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
3240 3999 41 None -223 4 Human 6.3 pKi = 6.3 Binding
Inhibition of human 5HT2B receptor expressed in CHO cellsInhibition of human 5HT2B receptor expressed in CHO cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
CHEMBL392760 3999 41 None -223 4 Human 6.3 pKi = 6.3 Binding
Inhibition of human 5HT2B receptor expressed in CHO cellsInhibition of human 5HT2B receptor expressed in CHO cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
168 3907 11 None -3 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
6604042 3907 11 None -3 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
CHEMBL309760 3907 11 None -3 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
10430183 203906 0 None -457 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5-HT2B receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human 5-HT2B receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
CHEMBL81728 203906 0 None -457 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5-HT2B receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human 5-HT2B receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
118055338 176601 0 None -57 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 222 0 1 2 2.4 CC1CN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4634942 176601 0 None -57 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 222 0 1 2 2.4 CC1CN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
56852956 111538 1 None -12 10 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by PDSP assayDisplacement of [3H]LSD from human 5-HT2B receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 111538 1 None -12 10 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by PDSP assayDisplacement of [3H]LSD from human 5-HT2B receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
71618636 148341 0 None -7 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 381 5 0 5 2.4 Cc1ncccc1OC[C@@H]1CN(CC(=O)N2c3ccccc3CC2C)CCO1 nan
CHEMBL3941579 148341 0 None -7 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 381 5 0 5 2.4 Cc1ncccc1OC[C@@H]1CN(CC(=O)N2c3ccccc3CC2C)CCO1 nan
56665075 65319 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 350 6 0 4 3.8 COc1ccc(CCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
CHEMBL1834254 65319 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 350 6 0 4 3.8 COc1ccc(CCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
1547484 925 70 None -8 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 925 70 None -8 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 925 70 None -8 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 925 70 None -8 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 925 70 None -8 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
44582678 180982 0 None -257 11 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476839 180982 0 None -257 11 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
136188797 57009 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@H]1SC[C@](C)(C(=O)O)N1C 10.1021/np100588c
CHEMBL1651094 57009 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@H]1SC[C@](C)(C(=O)O)N1C 10.1021/np100588c
102 4051 44 None -93 50 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
3659 4051 44 None -93 50 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
8969 4051 44 None -93 50 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
CHEMBL15245 4051 44 None -93 50 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
DB01392 4051 44 None -93 50 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
24826787 90652 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2c(cccc2C(F)(F)F)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397892 90652 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2c(cccc2C(F)(F)F)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
24826869 90657 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397897 90657 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
145964159 163766 0 None 3 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 273 3 2 4 2.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4212435 163766 0 None 3 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 273 3 2 4 2.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
168281307 190202 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 8 0 5 5.0 CCCCCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5183799 190202 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 8 0 5 5.0 CCCCCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
56852956 111538 1 None -12 10 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by PDSP assayDisplacement of [3H]LSD from human 5-HT2B receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 111538 1 None -12 10 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by PDSP assayDisplacement of [3H]LSD from human 5-HT2B receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
11347858 136500 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 286 1 2 3 1.3 O=C1c2c(cc(CO)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL374659 136500 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 286 1 2 3 1.3 O=C1c2c(cc(CO)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
136030744 57008 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@@H]1SC[C@](C)(C(=O)O)N1C 10.1021/acs.jnatprod.7b00317
CHEMBL1651093 57008 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@@H]1SC[C@](C)(C(=O)O)N1C 10.1021/acs.jnatprod.7b00317
134149008 147917 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 353 3 3 8 -0.1 CN(C)c1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)O)C[C@H]12 10.1021/acs.jmedchem.6b01183
CHEMBL3938006 147917 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 353 3 3 8 -0.1 CN(C)c1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)O)C[C@H]12 10.1021/acs.jmedchem.6b01183
16115521 84228 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1cc2c(cc1Cl)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL222466 84228 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1cc2c(cc1Cl)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
155566338 175328 0 None -446 6 Human 6.3 pKi = 6.3 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 405 4 4 8 1.4 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H]4C[C@H]5CC[C@@H]4C5)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL4587144 175328 0 None -446 6 Human 6.3 pKi = 6.3 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 405 4 4 8 1.4 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H]4C[C@H]5CC[C@@H]4C5)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
134134668 143709 0 None -4 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 381 6 4 8 1.4 CCC(CC)Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12 10.1021/acs.jmedchem.6b01183
CHEMBL3904817 143709 0 None -4 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 381 6 4 8 1.4 CCC(CC)Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12 10.1021/acs.jmedchem.6b01183
2477 732 54 None -13 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
36 732 54 None -13 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
437 732 54 None -13 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
CHEMBL49 732 54 None -13 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
DB00490 732 54 None -13 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
11666237 88669 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337496 88669 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365472 88669 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
11609026 88684 0 None -3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337500 88684 0 None -3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365705 88684 0 None -3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
44409031 74592 0 None -30 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 223 0 1 3 1.5 C[C@@H]1CNC[C@H]2Cc3ccc(Cl)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL203230 74592 0 None -30 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 223 0 1 3 1.5 C[C@@H]1CNC[C@H]2Cc3ccc(Cl)nc3N12 10.1016/j.bmcl.2005.11.083
122178702 120841 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 387 6 0 5 3.8 COc1cc2c(cc1OCCF)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
CHEMBL3581247 120841 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 387 6 0 5 3.8 COc1cc2c(cc1OCCF)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
168295984 191612 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 431 6 0 5 5.0 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccccc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5204813 191612 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 431 6 0 5 5.0 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccccc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
134155462 150565 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 339 3 3 8 -0.2 CN(C)c1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12 10.1021/acs.jmedchem.6b01183
CHEMBL3959210 150565 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 339 3 3 8 -0.2 CN(C)c1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12 10.1021/acs.jmedchem.6b01183
10058473 20440 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Compound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptor
ChEMBL 194 3 1 2 2.3 CN(C)CCc1c[nH]c2sccc12 10.1021/jm980692q
CHEMBL13086 20440 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Compound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptor
ChEMBL 194 3 1 2 2.3 CN(C)CCc1c[nH]c2sccc12 10.1021/jm980692q
71681898 90644 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 0 2 1.0 CN1CCN2C(=O)c3ccccc3C[C@@H]2C1 10.1016/j.bmcl.2013.04.061
CHEMBL2397884 90644 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 0 2 1.0 CN1CCN2C(=O)c3ccccc3C[C@@H]2C1 10.1016/j.bmcl.2013.04.061
49865832 15972 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 310 3 1 3 3.3 CCCCNC(=O)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224035 15972 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 310 3 1 3 3.3 CCCCNC(=O)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
136118618 75882 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058417 75882 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
9859257 203403 0 None -5 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 218 2 1 3 1.3 C[C@H](N)CN1CCc2ccc3c(c21)CCO3 10.1016/j.bmcl.2003.05.001
CHEMBL77880 203403 0 None -5 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 218 2 1 3 1.3 C[C@H](N)CN1CCc2ccc3c(c21)CCO3 10.1016/j.bmcl.2003.05.001
2105 2993 34 None -28 33 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 2993 34 None -28 33 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 2993 34 None -28 33 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 2993 34 None -28 33 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 2993 34 None -28 33 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
71028 83929 23 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 216 1 2 2 2.4 COc1ccc2[nH]c3c(c2c1)CCNC3C 10.1021/jm100600y
CHEMBL221811 83929 23 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 216 1 2 2 2.4 COc1ccc2[nH]c3c(c2c1)CCNC3C 10.1021/jm100600y
25122652 198968 0 None -134 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
CHEMBL599663 198968 0 None -134 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
11653679 180599 1 None -75 11 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned 5HT2B receptorBinding affinity to human cloned 5HT2B receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476108 180599 1 None -75 11 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned 5HT2B receptorBinding affinity to human cloned 5HT2B receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
56707820 2855 34 None - 1 Human 6.3 pKi = 6.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000354a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000354a HTR2B
ChEMBL 307 5 3 6 2.2 OCc1ccccc1c1nc(NCc2ccccc2)nc(n1)N nan
9155 2855 34 None - 1 Human 6.3 pKi = 6.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000354a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000354a HTR2B
ChEMBL 307 5 3 6 2.2 OCc1ccccc1c1nc(NCc2ccccc2)nc(n1)N nan
CHEMBL4548689 2855 34 None - 1 Human 6.3 pKi = 6.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000354a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000354a HTR2B
ChEMBL 307 5 3 6 2.2 OCc1ccccc1c1nc(NCc2ccccc2)nc(n1)N nan
5009938 15220 1 None 1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 306 4 0 3 3.8 c1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
CHEMBL1214829 15220 1 None 1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 306 4 0 3 3.8 c1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
11393128 182269 0 None -2 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 323 2 1 3 3.8 CC(C)n1nc2c(c1-c1ccc(C(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4791646 182269 0 None -2 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 323 2 1 3 3.8 CC(C)n1nc2c(c1-c1ccc(C(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
10527432 36042 0 None 1 3 Human 8.3 pKi = 8.3 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 447 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3)c1Cl)CC2 10.1021/jm990388c
CHEMBL14458 36042 0 None 1 3 Human 8.3 pKi = 8.3 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 447 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3)c1Cl)CC2 10.1021/jm990388c
10550405 37809 0 None -5 3 Human 8.3 pKi = 8.3 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 427 3 1 3 5.7 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(C)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL14606 37809 0 None -5 3 Human 8.3 pKi = 8.3 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 427 3 1 3 5.7 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(C)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
75306277 108754 0 None -2 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to serotonin 5-HT2B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 108754 0 None -2 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to serotonin 5-HT2B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
166 3295 12 None 1 3 Human 8.3 pKi = 8.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
3045227 3295 12 None 1 3 Human 8.3 pKi = 8.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
CHEMBL76781 3295 12 None 1 3 Human 8.3 pKi = 8.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
166 3295 12 None 1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
3045227 3295 12 None 1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
CHEMBL76781 3295 12 None 1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
11536843 114612 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343673 114612 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
11500509 120057 0 None -3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343670 120057 0 None -3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3545812 120057 0 None -3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
31101 719 39 None -26 36 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -26 36 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -26 36 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -26 36 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -26 36 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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
10331436 321 7 None -25 7 Human 8.3 pKi = 8.3 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
160 321 7 None -25 7 Human 8.3 pKi = 8.3 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
CHEMBL133455 321 7 None -25 7 Human 8.3 pKi = 8.3 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
242 467 117 None -1 52 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
34 467 117 None -1 52 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
60795 467 117 None -1 52 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
CHEMBL1112 467 117 None -1 52 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
DB01238 467 117 None -1 52 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
44364163 39535 1 None -3 4 Human 8.2 pKi = 8.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 190 1 2 1 2.1 NC1CC1c1c[nH]c2ccc(F)cc12 10.1021/jm980318q
CHEMBL147656 39535 1 None -3 4 Human 8.2 pKi = 8.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 190 1 2 1 2.1 NC1CC1c1c[nH]c2ccc(F)cc12 10.1021/jm980318q
118464420 137704 0 None 26 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL3770342 137704 0 None 26 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
127035063 135950 0 None 21 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 477 13 0 6 5.2 COc1ccccc1CCCN(CCc1ccc(OC)c(OC)c1)CCc1ccc2c(c1)OCO2 10.1039/C4MD00418C
CHEMBL3736149 135950 0 None 21 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 477 13 0 6 5.2 COc1ccccc1CCCN(CCc1ccc(OC)c(OC)c1)CCc1ccc2c(c1)OCO2 10.1039/C4MD00418C
44404886 71866 0 None 1 5 Human 8.2 pKi = 8.2 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 260 6 1 3 3.3 CCCCn1cc(CCN(C)C)c2c(O)cccc21 10.1016/j.bmcl.2005.06.104
CHEMBL198124 71866 0 None 1 5 Human 8.2 pKi = 8.2 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 260 6 1 3 3.3 CCCCn1cc(CCN(C)C)c2c(O)cccc21 10.1016/j.bmcl.2005.06.104
CHEMBL5077293 212710 0 None -17 9 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCNC2)ccc1Cl 10.1021/acs.jmedchem.1c00110
136118648 75953 0 None 1 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058703 75953 0 None 1 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
118729266 120175 0 None 1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(Cl)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402676 120175 0 None 1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(Cl)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547137 120175 0 None 1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(Cl)c2)C1 10.1016/j.bmc.2015.01.060
10837002 35124 0 None -79 3 Human 7.3 pKi = 7.3 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 444 4 1 5 5.2 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1021/jm990388c
CHEMBL14374 35124 0 None -79 3 Human 7.3 pKi = 7.3 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 444 4 1 5 5.2 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1021/jm990388c
18475647 196025 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 334 5 2 3 4.7 CCN(CC)c1ccc(NC(=O)Nc2ccnc3ccccc23)cc1 10.1016/s0960-894x(01)00343-2
CHEMBL57135 196025 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 334 5 2 3 4.7 CCN(CC)c1ccc(NC(=O)Nc2ccnc3ccccc23)cc1 10.1016/s0960-894x(01)00343-2
10837002 35124 0 None -79 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 444 4 1 5 5.2 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL14374 35124 0 None -79 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 444 4 1 5 5.2 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
44298175 100460 0 None -39 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cccnc3Cl)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL294030 100460 0 None -39 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cccnc3Cl)nc1)CC2 10.1016/s0960-894x(00)00364-4
11742218 194110 0 None -25 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 408 4 1 4 5.4 CCc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(C)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL55792 194110 0 None -25 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 408 4 1 4 5.4 CCc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(C)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
18931202 205066 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 393 7 2 5 2.4 COc1ccc(Cl)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
CHEMBL90346 205066 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 393 7 2 5 2.4 COc1ccc(Cl)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
73350823 102044 0 None -33 9 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptor by competitive binding assayBinding affinity to human 5HT2B receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL2424668 102044 0 None -33 9 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptor by competitive binding assayBinding affinity to human 5HT2B receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL3040578 102044 0 None -33 9 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptor by competitive binding assayBinding affinity to human 5HT2B receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
10257042 202648 0 None -12 7 Human 6.3 pKi = 6.3 Binding
Binding affinity for 5-hydroxytryptamine 2B receptor was determinedBinding affinity for 5-hydroxytryptamine 2B receptor was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL71707 202648 0 None -12 7 Human 6.3 pKi = 6.3 Binding
Binding affinity for 5-hydroxytryptamine 2B receptor was determinedBinding affinity for 5-hydroxytryptamine 2B receptor was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
9866423 71945 0 None -316 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 413 7 0 4 4.1 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
CHEMBL198330 71945 0 None -316 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 413 7 0 4 4.1 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
24887527 79601 0 None -100 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 440 7 0 4 4.9 COc1ccc(N2CC=C(c3cccc(Cl)c3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
CHEMBL212886 79601 0 None -100 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 440 7 0 4 4.9 COc1ccc(N2CC=C(c3cccc(Cl)c3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
24887290 79824 0 None -630 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 410 7 0 4 4.1 COc1ccc(N2CC=C(c3cccc(F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL213839 79824 0 None -630 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 410 7 0 4 4.1 COc1ccc(N2CC=C(c3cccc(F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
44414051 165663 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 440 7 0 4 5.0 COc1ccc(C2=C(C)CN(c3ccc(Cl)cc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL426684 165663 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 440 7 0 4 5.0 COc1ccc(C2=C(C)CN(c3ccc(Cl)cc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
10454231 168384 0 None -79 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 410 7 0 4 4.1 COc1ccc(C2=CCN(c3cccc(F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL438963 168384 0 None -79 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 410 7 0 4 4.1 COc1ccc(C2=CCN(c3cccc(F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
11292933 56085 39 None -2511 9 Human 6.3 pKi = 6.3 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 415 5 1 4 3.4 Cc1ccc2c(N3CCN(CCc4cccc(N5CCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631540 56085 39 None -2511 9 Human 6.3 pKi = 6.3 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 415 5 1 4 3.4 Cc1ccc2c(N3CCN(CCc4cccc(N5CCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
44298100 194381 0 None -158 3 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c2ccc(Cl)c3Cl)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL56050 194381 0 None -158 3 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c2ccc(Cl)c3Cl)cn1 10.1016/s0960-894x(00)00364-4
153287551 169374 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 307 1 0 2 3.8 CC(=O)N1CC[C@H]2c3cccc(-c4ccccc4)c3OC[C@]21C 10.1021/acsmedchemlett.9b00225
CHEMBL4441621 169374 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 307 1 0 2 3.8 CC(=O)N1CC[C@H]2c3cccc(-c4ccccc4)c3OC[C@]21C 10.1021/acsmedchemlett.9b00225
153287553 170528 0 None -79 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK 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 -79 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK 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
17989823 151532 0 None -316 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.0 COc1ccc(N2Cc3cccc(C(F)(F)F)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL396748 151532 0 None -316 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.0 COc1ccc(N2Cc3cccc(C(F)(F)F)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
10813396 98250 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 449 3 1 3 5.6 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3cc(F)cc(F)c3)c1)CC2 10.1021/jm990388c
CHEMBL277732 98250 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 449 3 1 3 5.6 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3cc(F)cc(F)c3)c1)CC2 10.1021/jm990388c
18357723 193838 0 None -31 3 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 424 4 1 4 4.4 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2cc(Br)ccc21 10.1016/s0960-894x(00)00365-6
CHEMBL55388 193838 0 None -31 3 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 424 4 1 4 4.4 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2cc(Br)ccc21 10.1016/s0960-894x(00)00365-6
44298129 194273 0 None -125 2 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 364 3 1 4 4.3 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(F)ccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL55958 194273 0 None -125 2 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 364 3 1 4 4.3 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(F)ccc32)cn1 10.1016/s0960-894x(00)00364-4
2028 2919 77 None -40 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
359 2919 77 None -40 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634 2919 77 None -40 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
CHEMBL1231 2919 77 None -40 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
DB01062 2919 77 None -40 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
136020617 57010 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/np100588c
CHEMBL1651095 57010 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/np100588c
132060770 162077 0 None -8 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 451 7 0 6 3.5 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4169689 162077 0 None -8 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 451 7 0 6 3.5 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
135367820 164258 0 None -9 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218672 164258 0 None -9 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
135846981 92606 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.6 C/N=C1/N/C(=C/c2c[nH]c3ccccc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2442265 92606 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.6 C/N=C1/N/C(=C/c2c[nH]c3ccccc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
CHEMBL5072247 212494 5 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL None None None CC[C@H]1CN2CCc3c([nH]c4cccc(O)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
145980271 165928 0 None 1 16 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4278465 165928 0 None 1 16 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
71452172 83091 0 None -1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by microbeta scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by microbeta scintillation counting analysis
ChEMBL 274 6 1 5 2.4 c1ccc(OCc2cc(OC[C@@H]3CCCN3)no2)cc1 10.1021/ml3002715
CHEMBL2203551 83091 0 None -1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by microbeta scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by microbeta scintillation counting analysis
ChEMBL 274 6 1 5 2.4 c1ccc(OCc2cc(OC[C@@H]3CCCN3)no2)cc1 10.1021/ml3002715
46230100 197629 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 231 0 2 3 0.9 Cc1ccc2c(c1)N1CCNCCC1NC2=O 10.1016/j.bmcl.2009.12.014
CHEMBL590531 197629 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 231 0 2 3 0.9 Cc1ccc2c(c1)N1CCNCCC1NC2=O 10.1016/j.bmcl.2009.12.014
127049981 140056 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 573 12 0 5 5.8 COc1ccc(CCN(CCCc2ccc(I)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3813789 140056 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 573 12 0 5 5.8 COc1ccc(CCN(CCCc2ccc(I)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
135464118 92614 0 None -1 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442272 92614 0 None -1 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
155556596 173841 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of human 5HT2B by radio-ligand binding displacement assayInhibition of human 5HT2B by radio-ligand binding displacement assay
ChEMBL 428 5 4 7 3.1 OC[C@@]12C[C@@H]1[C@@H](n1cc(-c3ccccc3)c3c(Nc4ccccc4)ncnc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b00689
CHEMBL4552895 173841 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of human 5HT2B by radio-ligand binding displacement assayInhibition of human 5HT2B by radio-ligand binding displacement assay
ChEMBL 428 5 4 7 3.1 OC[C@@]12C[C@@H]1[C@@H](n1cc(-c3ccccc3)c3c(Nc4ccccc4)ncnc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b00689
161 741 3 None 2 6 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
4284720 741 3 None 2 6 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
CHEMBL1255834 741 3 None 2 6 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
58911644 90655 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 227 0 1 3 0.5 N#Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397895 90655 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 227 0 1 3 0.5 N#Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
136020617 57010 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL1651095 57010 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/acs.jnatprod.7b00317
44407460 139807 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 315 5 1 3 4.4 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1 10.1016/j.bmcl.2005.10.029
CHEMBL380763 139807 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 315 5 1 3 4.4 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1 10.1016/j.bmcl.2005.10.029
90181061 160312 0 None 1 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 381 5 0 5 2.4 Cc1ncccc1OC[C@H]1CN(CC(=O)N2c3ccccc3CC2C)CCO1 nan
CHEMBL4115017 160312 0 None 1 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 381 5 0 5 2.4 Cc1ncccc1OC[C@H]1CN(CC(=O)N2c3ccccc3CC2C)CCO1 nan
145 140 48 None -87 30 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
1832 140 48 None -87 30 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
CHEMBL7257 140 48 None -87 30 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
DB14010 140 48 None -87 30 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
2726 904 64 None -19 73 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm100600y
621 904 64 None -19 73 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm100600y
83 904 64 None -19 73 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm100600y
CHEMBL71 904 64 None -19 73 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm100600y
DB00477 904 64 None -19 73 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm100600y
72735042 105816 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 293 2 3 2 1.6 NC(N)=NC(=O)/C=C/c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092763 105816 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 293 2 3 2 1.6 NC(N)=NC(=O)/C=C/c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3139089 105816 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 293 2 3 2 1.6 NC(N)=NC(=O)/C=C/c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
127036953 136977 0 None -5 22 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754166 136977 0 None -5 22 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
118709751 113029 0 None -407 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
CHEMBL3321792 113029 0 None -407 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
136118653 92608 0 None 2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3ccc(Br)cc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2442267 92608 0 None 2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3ccc(Br)cc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
54764240 68511 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 242 1 1 2 2.7 CC/C=C1\C[C@H]2CNc3ccccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL1922539 68511 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 242 1 1 2 2.7 CC/C=C1\C[C@H]2CNc3ccccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL4592872 212257 0 None -4 3 Human 5.3 pKi = 5.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000340a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000340a HTR2B
ChEMBL None None None O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@H]1c1ccc(F)cc1 nan
58405078 110194 0 None -6 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 310 5 1 5 3.0 Cc1nc(COc2ccc(Cl)cc2OC2CNC2)cs1 10.1021/ml500082j
CHEMBL3260335 110194 0 None -6 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 310 5 1 5 3.0 Cc1nc(COc2ccc(Cl)cc2OC2CNC2)cs1 10.1021/ml500082j
398712 77501 5 None -52 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 417 9 1 5 2.9 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm0508641
CHEMBL209324 77501 5 None -52 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 417 9 1 5 2.9 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm0508641
9859144 67009 1 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 208 0 1 2 1.7 Clc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2005.05.074
CHEMBL188605 67009 1 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 208 0 1 2 1.7 Clc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2005.05.074
122178701 120840 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 9 0 5 5.4 CCCCCCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581246 120840 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 9 0 5 5.4 CCCCCCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
122178708 120847 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 423 5 0 5 5.2 COc1cc2c(cc1OC1CCCCC1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
CHEMBL3581253 120847 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 423 5 0 5 5.2 COc1cc2c(cc1OC1CCCCC1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
2884131 166344 7 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 275 1 3 5 2.2 NC1=NC2(CCCCC2)NC(Nc2cccc(F)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4286420 166344 7 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 275 1 3 5 2.2 NC1=NC2(CCCCC2)NC(Nc2cccc(F)c2)=N1 10.1021/acsmedchemlett.8b00300
71655748 87383 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 359 5 1 4 4.8 CC(C)CCOc1ccc2c(c1)[C@H]1OCCC[C@H]1[C@@H](C1CCOCC1)N2 10.1021/jm400181k
CHEMBL2338343 87383 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 359 5 1 4 4.8 CC(C)CCOc1ccc2c(c1)[C@H]1OCCC[C@H]1[C@@H](C1CCOCC1)N2 10.1021/jm400181k
142601335 185829 0 None -44 7 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4876193 185829 0 None -44 7 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
134157367 153352 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 517 10 5 9 1.0 CC(=O)NCCCNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3983143 153352 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 517 10 5 9 1.0 CC(=O)NCCCNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
11644842 88654 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337105 88654 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365394 88654 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
4098 32274 24 None -14 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1255739 32274 24 None -14 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1411979 32274 24 None -14 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL4557026 212244 0 None - 1 Human 6.3 pKi = 6.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000700a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000700a HTR2B
ChEMBL None None None C[C@H](NC(=O)Nc1cc2[nH]ncc2c(CO)n1)c1ccccn1 nan
54764241 68510 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 258 1 1 3 2.3 C/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL1922538 68510 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 258 1 1 3 2.3 C/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
18735313 203216 1 None -4 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 210 2 1 2 2.1 C[C@H](N)CN1CCc2ccc(Cl)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL76307 203216 1 None -4 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 210 2 1 2 2.1 C[C@H](N)CN1CCc2ccc(Cl)cc21 10.1016/j.bmcl.2003.05.001
24826868 90637 1 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 236 0 1 2 1.3 O=C1c2cc(Cl)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397877 90637 1 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 236 0 1 2 1.3 O=C1c2cc(Cl)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
127049979 140106 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2ccc(Cl)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3814708 140106 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2ccc(Cl)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
5282379 193304 64 None 1 3 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C\C(=O)O)C(C)(C)CCC1 nan
CHEMBL547 193304 64 None 1 3 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C\C(=O)O)C(C)(C)CCC1 nan
118729242 120160 0 None -1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402661 120160 0 None -1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547028 120160 0 None -1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmc.2015.01.060
181743 177987 3 None -275 22 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL467094 177987 3 None -275 22 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2015.07.012
181743 177987 3 None -275 22 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B 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 -275 22 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
16115511 84399 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 250 1 1 2 2.0 CCc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL223466 84399 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 250 1 1 2 2.0 CCc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
122178709 120848 0 None -2 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 381 6 0 5 4.0 C=CCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581254 120848 0 None -2 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 381 6 0 5 4.0 C=CCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
4407909 192254 1 None 4 10 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B 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 4 10 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B 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 4 10 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B 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
118055233 176684 0 None -38 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 214 0 1 2 2.0 c1cc2c3c(c1)C1(CCC1)CN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4636196 176684 0 None -38 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 214 0 1 2 2.0 c1cc2c3c(c1)C1(CCC1)CN3CCNC2 10.1016/j.bmcl.2019.126929
11448649 83006 0 None -27 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 272 1 1 3 1.7 O=C1c2c(OC(F)(F)F)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL219734 83006 0 None -27 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 272 1 1 3 1.7 O=C1c2c(OC(F)(F)F)cccc2C2CNCCN12 10.1021/jm0612968
29101 71865 1 None -10 2 Human 5.3 pKi = 5.3 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 298 5 2 4 1.8 CN(C)CCc1cn(C)c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL198123 71865 1 None -10 2 Human 5.3 pKi = 5.3 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 298 5 2 4 1.8 CN(C)CCc1cn(C)c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
71061709 148983 0 None -3 12 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3946540 148983 0 None -3 12 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
11222829 90666 0 None -3 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2cccc(C(F)(F)F)c2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397906 90666 0 None -3 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2cccc(C(F)(F)F)c2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
162669941 182063 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 409 6 4 8 1.8 CC(C)C(Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C(C)C 10.1016/j.bmcl.2020.127599
CHEMBL4788883 182063 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 409 6 4 8 1.8 CC(C)C(Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C(C)C 10.1016/j.bmcl.2020.127599
44404895 170232 0 None -12 4 Human 5.3 pKi = 5.3 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 292 3 2 2 3.9 Oc1cccc2[nH]cc(CCN3CCCc4ccccc43)c12 10.1016/j.bmcl.2005.06.104
CHEMBL445331 170232 0 None -12 4 Human 5.3 pKi = 5.3 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 292 3 2 2 3.9 Oc1cccc2[nH]cc(CCN3CCCc4ccccc43)c12 10.1016/j.bmcl.2005.06.104
CHEMBL4798829 212279 4 None 6 2 Human 6.3 pKi = 6.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000752a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000752a HTR2B
ChEMBL None None None c1ccc2oc(-c3csc(C4CCN(Cc5nc6ncccc6[nH]5)CC4)n3)cc2c1 nan
44582705 186403 0 None -123 14 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 186403 0 None -123 14 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
3158 55959 21 None -389 20 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 55959 21 None -389 20 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
122178699 120839 0 None -3 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 7 0 5 4.6 CCCCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581245 120839 0 None -3 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 7 0 5 4.6 CCCCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
216239 23576 114 None 2 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1200485 23576 114 None 2 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1336 23576 114 None 2 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
73213195 103967 0 None -1 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 103967 0 None -1 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
11808247 17876 0 None -6 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL126667 17876 0 None -6 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819366 17876 0 None -6 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
11808247 17876 0 None -6 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL126667 17876 0 None -6 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819366 17876 0 None -6 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
44456400 12710 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12710 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12710 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12710 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
44456400 12710 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12710 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12710 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12710 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
49865830 15969 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 296 1 1 3 3.0 CC(C)NC(=O)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224032 15969 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 296 1 1 3 3.0 CC(C)NC(=O)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
41305446 166688 1 None 1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 398 5 1 2 4.5 O=C(NCc1ccccc1)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
CHEMBL4292719 166688 1 None 1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 398 5 1 2 4.5 O=C(NCc1ccccc1)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
46914772 15252 0 None 56 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 368 7 0 4 4.1 FCCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
CHEMBL1215036 15252 0 None 56 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 368 7 0 4 4.1 FCCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
73213195 103967 0 None -1 12 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 103967 0 None -1 12 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
122178700 120778 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 8 0 5 5.0 CCCCCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3580670 120778 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 8 0 5 5.0 CCCCCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
71681899 90642 0 None -3 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 202 0 1 2 0.7 O=C1c2ccccc2C[C@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397882 90642 0 None -3 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 202 0 1 2 0.7 O=C1c2ccccc2C[C@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
2291 3123 52 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3123 52 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3123 52 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3123 52 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3123 52 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
44364514 121172 9 None -1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 172 1 2 1 2.0 NC1CC1c1c[nH]c2ccccc12 10.1021/jm980318q
CHEMBL358810 121172 9 None -1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 172 1 2 1 2.0 NC1CC1c1c[nH]c2ccccc12 10.1021/jm980318q
10103618 120999 4 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 172 1 2 1 2.0 N[C@@H]1C[C@H]1c1c[nH]c2ccccc12 10.1021/jm980318q
CHEMBL358522 120999 4 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 172 1 2 1 2.0 N[C@@H]1C[C@H]1c1c[nH]c2ccccc12 10.1021/jm980318q
50878551 90300 60 None -1 18 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL2391541 90300 60 None -1 18 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
11492300 88668 1 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 188 0 2 2 0.5 O=C1N[C@H]2CNC[C@@H]2c2ccccc21 10.1016/j.bmcl.2012.10.091
CHEMBL2337495 88668 1 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 188 0 2 2 0.5 O=C1N[C@H]2CNC[C@@H]2c2ccccc21 10.1016/j.bmcl.2012.10.091
CHEMBL2365471 88668 1 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 188 0 2 2 0.5 O=C1N[C@H]2CNC[C@@H]2c2ccccc21 10.1016/j.bmcl.2012.10.091
68691189 90663 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 227 0 1 3 0.5 N#Cc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397903 90663 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 227 0 1 3 0.5 N#Cc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
25117677 198558 0 None -23 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL597009 198558 0 None -23 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
176 394 63 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
127051844 140303 0 None -48 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 140303 0 None -48 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
127051844 140303 0 None -48 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 140303 0 None -48 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
136118620 75884 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2058419 75884 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
44397846 67288 0 None -22 3 Human 7.2 pKi = 7.2 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 202 0 1 2 1.7 Cc1cccc2c1N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL190584 67288 0 None -22 3 Human 7.2 pKi = 7.2 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 202 0 1 2 1.7 Cc1cccc2c1N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
127034729 135829 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 463 12 0 6 5.1 COc1cccc(CCCN(CCc2ccc(OC)c(OC)c2)Cc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
CHEMBL3734894 135829 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 463 12 0 6 5.1 COc1cccc(CCCN(CCc2ccc(OC)c(OC)c2)Cc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
127036910 135929 0 None 18 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 419 10 0 5 4.7 COc1ccc(CCN(CCc2ccc3c(c2)OCO3)Cc2ccccc2)cc1OC 10.1039/C4MD00418C
CHEMBL3735862 135929 0 None 18 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 419 10 0 5 4.7 COc1ccc(CCN(CCc2ccc3c(c2)OCO3)Cc2ccccc2)cc1OC 10.1039/C4MD00418C
136118615 92619 0 None 2 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442277 92619 0 None 2 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
657255 197396 29 None -9 15 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 197396 29 None -9 15 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
45486824 195691 0 None -14 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 421 4 3 4 3.3 O=C1Cc2c(ccc3c2OC[C@H](CNCC2CCc4[nH]c5ccc(F)cc5c4C2)O3)N1 10.1016/j.bmcl.2009.08.050
CHEMBL569251 195691 0 None -14 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 421 4 3 4 3.3 O=C1Cc2c(ccc3c2OC[C@H](CNCC2CCc4[nH]c5ccc(F)cc5c4C2)O3)N1 10.1016/j.bmcl.2009.08.050
135427931 72758 2 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 317 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(I)c21 10.1021/jm050663x
CHEMBL201132 72758 2 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 317 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(I)c21 10.1021/jm050663x
58911579 90651 0 None 12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 242 1 1 2 1.5 O=C1c2c(cccc2C2CC2)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397891 90651 0 None 12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 242 1 1 2 1.5 O=C1c2c(cccc2C2CC2)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
277 1269 55 None -5 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1269 55 None -5 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1269 55 None -5 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1269 55 None -5 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1269 55 None -5 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
118464420 137704 0 None 26 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
CHEMBL3770342 137704 0 None 26 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
118464421 166728 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 291 1 3 5 2.7 NC1=NC2(CCCCC2)NC(Nc2cccc(Cl)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4293638 166728 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 291 1 3 5 2.7 NC1=NC2(CCCCC2)NC(Nc2cccc(Cl)c2)=N1 10.1021/acsmedchemlett.8b00300
118706294 120011 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 311 3 3 3 1.3 COCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
CHEMBL3310118 120011 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 311 3 3 3 1.3 COCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
CHEMBL3545470 120011 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 311 3 3 3 1.3 COCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
44324142 205218 0 None -25 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 427 7 2 5 3.0 COc1cc(Cl)c(Cl)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
CHEMBL91221 205218 0 None -25 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 427 7 2 5 3.0 COc1cc(Cl)c(Cl)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
10670191 40641 0 None -15 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 428 3 1 4 5.1 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3cnccc3C)c1)CC2 10.1021/jm990388c
CHEMBL14864 40641 0 None -15 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 428 3 1 4 5.1 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3cnccc3C)c1)CC2 10.1021/jm990388c
135398745 2858 108 None -5 66 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
47 2858 108 None -5 66 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
CHEMBL715 2858 108 None -5 66 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
DB00334 2858 108 None -5 66 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
44298080 194286 0 None -1 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 431 4 1 5 4.3 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3cncn3C)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL55969 194286 0 None -1 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 431 4 1 5 4.3 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3cncn3C)nc1)CC2 10.1016/s0960-894x(00)00365-6
191 399 92 None -5 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 399 92 None -5 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 399 92 None -5 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 399 92 None -5 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 399 92 None -5 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
118706292 120010 0 None 6 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 297 2 4 3 0.7 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(CO)c1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310117 120010 0 None 6 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 297 2 4 3 0.7 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(CO)c1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545469 120010 0 None 6 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 297 2 4 3 0.7 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(CO)c1-2 10.1016/j.bmc.2014.05.027
127035065 135964 0 None 30 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 477 13 0 6 5.2 COc1ccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1 10.1039/C4MD00418C
CHEMBL3736207 135964 0 None 30 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 477 13 0 6 5.2 COc1ccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1 10.1039/C4MD00418C
73453 29388 22 None -9 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29388 22 None -9 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
118729258 120171 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402671 120171 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547133 120171 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmc.2015.01.060
127036186 136876 0 None -1 19 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3753318 136876 0 None -1 19 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
71062829 159575 0 None 1 3 Mouse 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1ccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)nc1 nan
CHEMBL4108986 159575 0 None 1 3 Mouse 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1ccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)nc1 nan
10659364 120189 0 None -50 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 265 2 0 1 4.0 Cc1ccccc1[C@@H]1C[C@@H](N(C)C)Cc2ccccc21 10.1016/j.bmc.2015.01.060
CHEMBL3402685 120189 0 None -50 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 265 2 0 1 4.0 Cc1ccccc1[C@@H]1C[C@@H](N(C)C)Cc2ccccc21 10.1016/j.bmc.2015.01.060
CHEMBL3547178 120189 0 None -50 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 265 2 0 1 4.0 Cc1ccccc1[C@@H]1C[C@@H](N(C)C)Cc2ccccc21 10.1016/j.bmc.2015.01.060
122187376 122495 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 457 6 0 5 5.9 CCCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609141 122495 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 457 6 0 5 5.9 CCCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
9978683 18472 0 None -380 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
CHEMBL1277104 18472 0 None -380 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
53325861 56546 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL1643902 56546 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
53325861 56546 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmcl.2010.11.075
CHEMBL1643902 56546 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmcl.2010.11.075
117209858 183961 1 None -3 7 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4848305 183961 1 None -3 7 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
46230047 197560 0 None 16 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1ccc2c(c1)C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590089 197560 0 None 16 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1ccc2c(c1)C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
24839550 136778 14 None 1 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752576 136778 14 None 1 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
45486891 195255 0 None -83 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 449 6 3 4 4.1 O=C1Cc2c(ccc3c2OC[C@H](CNCCCC2CCc4c([nH]c5ccc(F)cc45)C2)O3)N1 10.1016/j.bmcl.2009.08.050
CHEMBL566379 195255 0 None -83 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 449 6 3 4 4.1 O=C1Cc2c(ccc3c2OC[C@H](CNCCCC2CCc4c([nH]c5ccc(F)cc45)C2)O3)N1 10.1016/j.bmcl.2009.08.050
27620 140274 13 None -269 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 297 5 0 2 3.8 O=C(CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818994 140274 13 None -269 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 297 5 0 2 3.8 O=C(CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
24360 201644 101 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 348 1 1 6 2.1 CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3ccccc3nc2-1 nan
CHEMBL65 201644 101 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 348 1 1 6 2.1 CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3ccccc3nc2-1 nan
44315697 203784 0 None -9 3 Human 7.2 pKi = 7.2 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 254 4 1 3 2.6 CCSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
CHEMBL80731 203784 0 None -9 3 Human 7.2 pKi = 7.2 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 254 4 1 3 2.6 CCSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
3952 1849 33 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5353646 1849 33 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5443 1849 33 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5702063 1849 33 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL1331786 1849 33 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL420 1849 33 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
145967771 164224 0 None 3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 223 2 2 4 1.6 C[C@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4218231 164224 0 None 3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 223 2 2 4 1.6 C[C@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/acs.jnatprod.7b00317
57396813 71186 0 None -891 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human 5HT2BInhibition of human 5HT2B
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71186 0 None -891 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human 5HT2BInhibition of human 5HT2B
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71186 0 None -891 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human 5HT2BInhibition of human 5HT2B
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
44407335 72732 0 None -7 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 321 5 1 3 4.7 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCC1CCCCC1 10.1016/j.bmcl.2005.10.029
CHEMBL201117 72732 0 None -7 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 321 5 1 3 4.7 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCC1CCCCC1 10.1016/j.bmcl.2005.10.029
57799321 88618 1 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@@H]2CNC[C@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337491 88618 1 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@@H]2CNC[C@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2364961 88618 1 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@@H]2CNC[C@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
71462777 82538 0 None -83 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3ncccc23)CC1 10.1021/jm300943r
CHEMBL2181171 82538 0 None -83 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3ncccc23)CC1 10.1021/jm300943r
56658156 65321 0 None 9 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 364 7 0 4 4.2 COc1ccccc1CCCN1CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmcl.2011.08.029
CHEMBL1834256 65321 0 None 9 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 364 7 0 4 4.2 COc1ccccc1CCCN1CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmcl.2011.08.029
168281486 190430 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 387 6 0 5 3.8 COc1cc2c(cc1OC)-c1c(OC)c(OCCF)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5187013 190430 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 387 6 0 5 3.8 COc1cc2c(cc1OC)-c1c(OC)c(OCCF)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
11630147 90668 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 246 2 1 3 1.1 CCOc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397908 90668 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 246 2 1 3 1.1 CCOc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
44298209 192983 0 None -19 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 395 3 1 5 4.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1cnc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL53113 192983 0 None -19 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 395 3 1 5 4.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1cnc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
44298225 193797 0 None -50 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 456 3 1 5 5.1 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c2cc(C(F)(F)F)c2c3CCO2)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL55292 193797 0 None -50 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 456 3 1 5 5.1 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c2cc(C(F)(F)F)c2c3CCO2)cn1 10.1016/s0960-894x(00)00364-4
44298244 198382 0 None -79 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 438 3 1 4 5.2 Cc1cc2c(cc1Br)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL59584 198382 0 None -79 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 438 3 1 4 5.2 Cc1cc2c(cc1Br)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
17989871 149780 0 None -50 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.6 COc1ccc(N2Cc3cc(Cl)c(C)c(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL395298 149780 0 None -50 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.6 COc1ccc(N2Cc3cc(Cl)c(C)c(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
10693974 35422 0 None -9 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 431 3 1 3 5.5 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3ccc(F)cc3)c1)CC2 10.1021/jm990388c
CHEMBL14401 35422 0 None -9 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 431 3 1 3 5.5 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3ccc(F)cc3)c1)CC2 10.1021/jm990388c
10458193 86400 0 None -25 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 451 6 0 5 4.6 COc1ccc(N2Cc3c(c4cc(F)ccc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
CHEMBL232254 86400 0 None -25 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 451 6 0 5 4.6 COc1ccc(N2Cc3c(c4cc(F)ccc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
44568347 191045 0 None -30 15 Human 6.2 pKi = 6.2 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL519609 191045 0 None -30 15 Human 6.2 pKi = 6.2 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
18475581 197908 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 318 2 2 4 4.3 Cc1nc2ccc(NC(=O)Nc3ccnc4ccccc34)cc2o1 10.1016/s0960-894x(01)00343-2
CHEMBL59266 197908 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 318 2 2 4 4.3 Cc1nc2ccc(NC(=O)Nc3ccnc4ccccc34)cc2o1 10.1016/s0960-894x(01)00343-2
24888180 79443 0 None -251 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 426 7 0 4 4.6 COc1ccc(N2CC=C(c3cccc(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL212270 79443 0 None -251 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 426 7 0 4 4.6 COc1ccc(N2CC=C(c3cccc(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
24887518 79859 0 None -794 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 460 7 0 4 5.3 COc1ccc(N2CC=C(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL213987 79859 0 None -794 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 460 7 0 4 5.3 COc1ccc(N2CC=C(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
44298091 101236 0 None -99 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 398 3 1 4 5.0 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(F)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL299530 101236 0 None -99 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 398 3 1 4 5.0 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(F)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
10476876 193296 0 None -158 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.2 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(C(F)(F)F)ccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL54610 193296 0 None -158 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.2 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(C(F)(F)F)ccc32)cn1 10.1016/s0960-894x(00)00364-4
44298182 193317 0 None -199 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 424 3 1 4 4.9 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Br)ccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL54769 193317 0 None -199 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 424 3 1 4 4.9 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Br)ccc32)cn1 10.1016/s0960-894x(00)00364-4
10413595 161280 0 None -1995 11 Human 6.2 pKi = 6.2 Binding
Compound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligandCompound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligand
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL414628 161280 0 None -1995 11 Human 6.2 pKi = 6.2 Binding
Compound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligandCompound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligand
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
6918647 100265 2 None -125 14 Human 6.2 pKi = 6.2 Binding
Compound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HTCompound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HT
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL292759 100265 2 None -125 14 Human 6.2 pKi = 6.2 Binding
Compound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HTCompound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HT
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
18931344 204798 0 None -19 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 544 11 3 8 2.5 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccccc1 10.1016/S0960-894X(96)00503-3
CHEMBL88571 204798 0 None -19 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 544 11 3 8 2.5 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccccc1 10.1016/S0960-894X(96)00503-3
155557042 173975 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 1 1 3 1.9 COc1ccc2c(c1)[C@@H]1CCN[C@]1(C)CO2 10.1021/acsmedchemlett.9b00225
CHEMBL4556297 173975 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 1 1 3 1.9 COc1ccc2c(c1)[C@@H]1CCN[C@]1(C)CO2 10.1021/acsmedchemlett.9b00225
15124 140591 6 None 1 4 Human 5.2 pKi = 5.2 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 204 3 2 2 2.0 CN(C)CCc1c[nH]c2cc(O)ccc12 10.1016/j.bmcl.2005.06.104
CHEMBL382750 140591 6 None 1 4 Human 5.2 pKi = 5.2 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 204 3 2 2 2.0 CN(C)CCc1c[nH]c2cc(O)ccc12 10.1016/j.bmcl.2005.06.104
118055308 177178 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 208 0 1 2 1.8 Clc1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4642763 177178 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 208 0 1 2 1.8 Clc1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
2099 9202 49 None - 1 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O nan
CHEMBL1110 9202 49 None - 1 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O nan
25209050 180998 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 479 6 2 6 3.9 Cc1c(Cn2ncc(N3CCNCC3)cc2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL477008 180998 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 479 6 2 6 3.9 Cc1c(Cn2ncc(N3CCNCC3)cc2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
11820166 40020 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 202 2 2 2 2.0 COc1cccc2[nH]cc(C3CC3N)c12 10.1021/jm980318q
CHEMBL148091 40020 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 202 2 2 2 2.0 COc1cccc2[nH]cc(C3CC3N)c12 10.1021/jm980318q
70695812 72922 0 None -831 8 Human 6.2 pKi = 6.2 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 375 5 3 7 2.0 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CC3)C3CC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
CHEMBL2012686 72922 0 None -831 8 Human 6.2 pKi = 6.2 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 375 5 3 7 2.0 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CC3)C3CC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
71062560 152882 0 None -1 2 Mouse 5.2 pKi = 5.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 352 5 0 4 2.4 O=C(CN1CCO[C@H](COc2ccccc2)C1)N1CCc2ccccc21 nan
CHEMBL3979116 152882 0 None -1 2 Mouse 5.2 pKi = 5.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 352 5 0 4 2.4 O=C(CN1CCO[C@H](COc2ccccc2)C1)N1CCc2ccccc21 nan
59511191 184931 3 None -8 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 228 2 2 3 1.5 c1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4862745 184931 3 None -8 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 228 2 2 3 1.5 c1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
44276349 99529 0 None -288 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 325 3 4 8 -0.2 CNc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12 10.1021/acs.jmedchem.6b01183
CHEMBL286739 99529 0 None -288 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 325 3 4 8 -0.2 CNc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12 10.1021/acs.jmedchem.6b01183
11427139 84249 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 282 1 1 2 2.4 C=Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL222566 84249 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 282 1 1 2 2.4 C=Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
2274 3112 53 None -10 32 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3112 53 None -10 32 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3112 53 None -10 32 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3112 53 None -10 32 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3112 53 None -10 32 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
132060812 161475 0 None -16 10 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4160064 161475 0 None -16 10 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
44215629 155789 1 None -12 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 206 0 1 2 1.9 N#Cc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL406585 155789 1 None -12 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 206 0 1 2 1.9 N#Cc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
118729236 120153 0 None -9 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccccc2Br)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402658 120153 0 None -9 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccccc2Br)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547011 120153 0 None -9 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccccc2Br)C1 10.1016/j.bmc.2015.01.060
CHEMBL4513786 212207 5 None -1174 8 Human 5.2 pKi = 5.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl HTR2B
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC nan
CHEMBL4796803 212207 5 None -1174 8 Human 5.2 pKi = 5.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl HTR2B
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC nan
46914776 15229 0 None 7 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 364 7 0 4 4.5 CCCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
CHEMBL1214892 15229 0 None 7 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 364 7 0 4 4.5 CCCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
71062708 153760 0 None -3 12 Mouse 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3986651 153760 0 None -3 12 Mouse 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
49865886 15989 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 262 2 1 3 2.1 CCCNC(=O)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224102 15989 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 262 2 1 3 2.1 CCCNC(=O)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
11198145 9707 2 None -2 5 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL113830 9707 2 None -2 5 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
49783209 17412 0 None -114 27 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17412 0 None -114 27 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
10539928 120182 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402668 120182 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547154 120182 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(F)cc2)C1 10.1016/j.bmc.2015.01.060
136118619 75883 0 None 2 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058418 75883 0 None 2 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
25060119 103824 0 None -9332 7 Human 6.2 pKi = 6.2 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
CHEMBL3099899 103824 0 None -9332 7 Human 6.2 pKi = 6.2 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
122187377 122496 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 485 8 0 5 6.7 CCCCCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609142 122496 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 485 8 0 5 6.7 CCCCCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL5071978 212491 0 None 1 6 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCN(CC)Cc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
44397752 124736 0 None -7 3 Human 7.2 pKi = 7.2 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 216 0 1 2 2.0 Cc1ccc2c(c1C)N1[C@H](CNC[C@H]1C)C2 10.1016/j.bmcl.2005.05.074
CHEMBL364534 124736 0 None -7 3 Human 7.2 pKi = 7.2 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 216 0 1 2 2.0 Cc1ccc2c(c1C)N1[C@H](CNC[C@H]1C)C2 10.1016/j.bmcl.2005.05.074
46230097 197675 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.6 O=C1NC2CCNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
CHEMBL590816 197675 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.6 O=C1NC2CCNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
130442480 174688 0 None -83 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK 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 -83 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK 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
134150123 151546 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 381 4 2 9 0.4 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)C)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3967613 151546 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 381 4 2 9 0.4 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)C)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
3033538 1287 36 None -12 9 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
7155 1287 36 None -12 9 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
781 1287 36 None -12 9 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
CHEMBL1201216 1287 36 None -12 9 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
DB00298 1287 36 None -12 9 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
16118795 59765 0 None -954 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642851 59765 0 None -954 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739215 59765 0 None -954 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
16117153 59808 0 None -1122 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642889 59808 0 None -1122 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739616 59808 0 None -1122 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
70695812 72922 0 None -831 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 375 5 3 7 2.0 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CC3)C3CC3)nc(Cl)nc21 10.1021/acs.jmedchem.6b01183
CHEMBL2012686 72922 0 None -831 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 375 5 3 7 2.0 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CC3)C3CC3)nc(Cl)nc21 10.1021/acs.jmedchem.6b01183
44352308 116971 0 None -83 12 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 2B receptor using [3H]5-HT as radioligandBinding affinity towards human 5-hydroxytryptamine 2B receptor using [3H]5-HT as radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
CHEMBL339980 116971 0 None -83 12 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 2B receptor using [3H]5-HT as radioligandBinding affinity towards human 5-hydroxytryptamine 2B receptor using [3H]5-HT as radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
122442272 137807 0 None -2 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT2B receptor by radioligand binding assayBinding affinity to human 5HT2B receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137807 0 None -2 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT2B receptor by radioligand binding assayBinding affinity to human 5HT2B receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137807 0 None -2 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT2B receptor by radioligand binding assayBinding affinity to human 5HT2B receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
213 3780 50 None -5 44 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 3780 50 None -5 44 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 3780 50 None -5 44 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 3780 50 None -5 44 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 3780 50 None -5 44 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
44409097 76238 0 None -4 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 257 0 1 3 1.8 C[C@@H]1CNC[C@H]2Cc3ccc(C(F)(F)F)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL206333 76238 0 None -4 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 257 0 1 3 1.8 C[C@@H]1CNC[C@H]2Cc3ccc(C(F)(F)F)nc3N12 10.1016/j.bmcl.2005.11.083
44626329 195722 0 None -20 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 420 3 2 4 3.7 O=c1[nH]c2cccc(N3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 10.1016/j.bmcl.2009.08.050
CHEMBL569513 195722 0 None -20 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 420 3 2 4 3.7 O=c1[nH]c2cccc(N3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 10.1016/j.bmcl.2009.08.050
11148641 90645 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@H]1CN2C(=O)c3ccccc3C[C@@H]2CN1 10.1016/j.bmcl.2013.04.061
CHEMBL2397885 90645 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@H]1CN2C(=O)c3ccccc3C[C@@H]2CN1 10.1016/j.bmcl.2013.04.061
CHEMBL5091373 213781 0 None -33 9 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 213781 0 None -33 9 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
2351 3222 60 None -7 21 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm100600y
2820 3222 60 None -7 21 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm100600y
5035 3222 60 None -7 21 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm100600y
CHEMBL81 3222 60 None -7 21 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm100600y
DB00481 3222 60 None -7 21 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm100600y
122442272 137807 0 None -2 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT2B receptor by radioligand binding assayBinding affinity to human 5HT2B receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137807 0 None -2 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT2B receptor by radioligand binding assayBinding affinity to human 5HT2B receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137807 0 None -2 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT2B receptor by radioligand binding assayBinding affinity to human 5HT2B receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
9909648 203851 1 None -22 12 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm100600y
CHEMBL81330 203851 1 None -22 12 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm100600y
145977799 163080 0 None 1 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4204036 163080 0 None 1 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
12488 1619 51 None -11 23 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1619 51 None -11 23 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1619 51 None -11 23 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1619 51 None -11 23 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
53324553 56545 0 None -9 10 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
CHEMBL1643900 56545 0 None -9 10 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
53324553 56545 0 None -9 10 Human 5.2 pKi = 5.2 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
CHEMBL1643900 56545 0 None -9 10 Human 5.2 pKi = 5.2 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
16115271 78683 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 298 1 1 2 2.8 CC(C)[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL2113264 78683 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 298 1 1 2 2.8 CC(C)[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
71720492 86526 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 493 8 2 5 3.0 C=CCN1C[C@H](C(=O)N(CCCN2CCOCC2)C(=O)NCC)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/ml3003814
CHEMBL2323578 86526 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 493 8 2 5 3.0 C=CCN1C[C@H](C(=O)N(CCCN2CCOCC2)C(=O)NCC)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/ml3003814
135398737 942 89 None -2 92 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 942 89 None -2 92 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 942 89 None -2 92 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 942 89 None -2 92 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 942 89 None -2 92 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
9803032 190847 0 None -12 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 435 7 0 4 4.4 COc1ccccc1N1CCN(CC[C@@H](C(=O)N2CCCCCC2)c2ccccc2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5193178 190847 0 None -12 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 435 7 0 4 4.4 COc1ccccc1N1CCN(CC[C@@H](C(=O)N2CCCCCC2)c2ccccc2)CC1 10.1021/acs.jmedchem.2c00633
3649661 137678 6 None 23 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770106 137678 6 None 23 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
2247 502 77 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
11708275 72352 3 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 205 3 1 4 1.4 COc1ccc2cnn(C[C@H](C)N)c2c1 10.1021/jm050663x
CHEMBL199775 72352 3 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 205 3 1 4 1.4 COc1ccc2cnn(C[C@H](C)N)c2c1 10.1021/jm050663x
134 2468 19 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
1775 2468 19 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
9681 2468 19 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
CHEMBL1065 2468 19 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
DB00247 2468 19 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
134 2468 19 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
1775 2468 19 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
9681 2468 19 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
CHEMBL1065 2468 19 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
DB00247 2468 19 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
11949710 198210 0 None -5 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from human 5HT2B receptor expressed in CHO cells
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL594717 198210 0 None -5 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from human 5HT2B receptor expressed in CHO cells
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
36906 104388 68 None -4 6 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm050663x
CHEMBL31115 104388 68 None -4 6 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm050663x
36906 104388 68 None -4 6 Human 8.1 pKi = 8.1 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm030205t
CHEMBL31115 104388 68 None -4 6 Human 8.1 pKi = 8.1 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm030205t
44573547 187039 0 None -11 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human recombinant 5-HT2B expressed in HEK293 cells assessed as inhibition constant by radioligand binding assayBinding affinity to human recombinant 5-HT2B expressed in HEK293 cells assessed as inhibition constant by radioligand binding assay
ChEMBL 348 5 1 5 2.6 C[C@H](Cc1cccc(F)c1)Oc1nc(N2CCNC[C@H]2C)ncc1F 10.1021/acs.jmedchem.2c00633
CHEMBL494948 187039 0 None -11 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human recombinant 5-HT2B expressed in HEK293 cells assessed as inhibition constant by radioligand binding assayBinding affinity to human recombinant 5-HT2B expressed in HEK293 cells assessed as inhibition constant by radioligand binding assay
ChEMBL 348 5 1 5 2.6 C[C@H](Cc1cccc(F)c1)Oc1nc(N2CCNC[C@H]2C)ncc1F 10.1021/acs.jmedchem.2c00633
9931534 33872 0 None -7 3 Human 8.1 pKi = 8.1 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL14255 33872 0 None -7 3 Human 8.1 pKi = 8.1 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3)c1)CC2 10.1021/jm990388c
10623205 98597 0 None -12 3 Human 8.1 pKi = 8.1 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 445 3 1 3 5.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(F)c(C)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL280465 98597 0 None -12 3 Human 8.1 pKi = 8.1 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 445 3 1 3 5.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(F)c(C)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
10837468 162146 0 None -15 3 Human 8.1 pKi = 8.1 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 455 3 1 4 5.3 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc3c(c(-c4cccnc4)c1)OCC3)CC2 10.1021/jm990388c
CHEMBL417082 162146 0 None -15 3 Human 8.1 pKi = 8.1 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 455 3 1 4 5.3 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc3c(c(-c4cccnc4)c1)OCC3)CC2 10.1021/jm990388c
10622480 166472 0 None -5 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 429 3 1 3 6.1 CSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL428879 166472 0 None -5 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 429 3 1 3 6.1 CSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3)c1)CC2 10.1021/jm990388c
44298176 100148 0 None -6 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 394 4 1 4 4.6 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3ccncc3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL291949 100148 0 None -6 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 394 4 1 4 4.6 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3ccncc3)nc1)CC2 10.1016/s0960-894x(00)00365-6
18357730 194225 0 None -19 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 4 1 4 5.3 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(OCc3ccccn3)c(C)c1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL55914 194225 0 None -19 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 4 1 4 5.3 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(OCc3ccccn3)c(C)c1)CC2 10.1016/s0960-894x(00)00365-6
44453103 97598 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 296 4 1 4 2.9 CCN(CC)c1nc2c(c(-c3ccc(C)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
CHEMBL273173 97598 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 296 4 1 4 2.9 CCN(CC)c1nc2c(c(-c3ccc(C)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
240 929 39 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
2769 929 39 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
44279790 929 39 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
660 929 39 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL1729 929 39 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL560739 929 39 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
DB00604 929 39 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
11737939 83798 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 2.1 O=C1c2c(ccc(Cl)c2Cl)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL220900 83798 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 2.1 O=C1c2c(ccc(Cl)c2Cl)[C@@H]2CNCCN12 10.1021/jm0612968
118729268 120176 0 None -22 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402677 120176 0 None -22 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547138 120176 0 None -22 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(F)c2)C1 10.1016/j.bmc.2015.01.060
118729254 120183 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc([N+](=O)[O-])c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402669 120183 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc([N+](=O)[O-])c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547155 120183 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc([N+](=O)[O-])c2)C1 10.1016/j.bmc.2015.01.060
16062136 157114 4 None -13 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 1 1 3 3.2 CC(C)(C)c1nc2c(c(-c3ccc(F)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
CHEMBL408155 157114 4 None -13 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 1 1 3 3.2 CC(C)(C)c1nc2c(c(-c3ccc(F)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
146159245 187856 27 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
451415 187856 27 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
86289437 187856 27 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
CHEMBL502620 187856 27 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
12613159 186733 7 None -2 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL493054 186733 7 None -2 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
10517285 120187 0 None -14 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccccc2Cl)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402683 120187 0 None -14 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccccc2Cl)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547176 120187 0 None -14 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccccc2Cl)C1 10.1016/j.bmc.2015.01.060
1224 1399 79 None -6 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1399 79 None -6 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1399 79 None -6 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1399 79 None -6 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1399 79 None -6 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1399 79 None -6 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
122187381 122499 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 401 2 1 5 4.5 COc1cc2c3c(c1O)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609146 122499 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 401 2 1 5 4.5 COc1cc2c3c(c1O)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
135465870 188394 7 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.6 C/N=C1\NC(=O)/C(=C\c2c[nH]c3ccccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL508657 188394 7 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.6 C/N=C1\NC(=O)/C(=C\c2c[nH]c3ccccc23)N1C 10.1016/j.bmc.2013.09.011
155565326 175002 0 None -467 7 Human 6.1 pKi = 6.1 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 462 6 5 9 0.5 O=C(NCCO)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H]4C[C@H]5CC[C@@H]4C5)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL4579650 175002 0 None -467 7 Human 6.1 pKi = 6.1 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 462 6 5 9 0.5 O=C(NCCO)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H]4C[C@H]5CC[C@@H]4C5)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
46914620 15244 0 None 6 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 350 6 0 4 4.1 CCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
CHEMBL1214962 15244 0 None 6 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 350 6 0 4 4.1 CCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
46230094 197621 0 None 5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 237 0 2 3 0.8 O=C1NC2CNCCN2c2ccc(Cl)cc21 10.1016/j.bmcl.2009.12.014
CHEMBL590482 197621 0 None 5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 237 0 2 3 0.8 O=C1NC2CNCCN2c2ccc(Cl)cc21 10.1016/j.bmcl.2009.12.014
57403525 69796 0 None -478 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940402 69796 0 None -478 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
127051845 140185 0 None -42 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3817898 140185 0 None -42 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
4178 194120 58 None - 1 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N nan
CHEMBL558 194120 58 None - 1 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N nan
127051845 140185 0 None -42 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3817898 140185 0 None -42 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
145986752 166712 0 None -1 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
CHEMBL4293307 166712 0 None -1 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
11695000 88628 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337490 88628 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365083 88628 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
118729276 120164 0 None -14 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 327 3 0 1 5.4 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402682 120164 0 None -14 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 327 3 0 1 5.4 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547045 120164 0 None -14 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 327 3 0 1 5.4 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmc.2015.01.060
134152157 152593 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 393 6 4 8 1.4 CC[C@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
CHEMBL3976579 152593 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 393 6 4 8 1.4 CC[C@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
21830793 91389 5 None -489 46 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 91389 5 None -489 46 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
16115392 84359 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 236 0 1 2 1.7 Cc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL223292 84359 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 236 0 1 2 1.7 Cc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
11665991 197654 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 251 0 2 3 1.2 O=C1NC2CNCCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
CHEMBL590721 197654 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 251 0 2 3 1.2 O=C1NC2CNCCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
222757 98904 70 None -1 3 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O nan
CHEMBL282575 98904 70 None -1 3 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O nan
2812 4696 96 None -40 34 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4696 96 None -40 34 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
44407440 138763 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 329 5 1 3 4.7 Cc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL379223 138763 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 329 5 1 3 4.7 Cc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
24740863 88714 0 None 1 6 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
CHEMBL236610 88714 0 None 1 6 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
46214153 110193 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 367 5 1 3 4.0 Clc1cccc(COc2ccc(Br)cc2OC2CNC2)c1 10.1021/ml500082j
CHEMBL3260334 110193 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 367 5 1 3 4.0 Clc1cccc(COc2ccc(Br)cc2OC2CNC2)c1 10.1021/ml500082j
11221167 84243 0 None -10 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL222514 84243 0 None -10 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL4520788 212215 6 None -3 25 Human 7.1 pKi = 7.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR2B
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 nan
155535754 171499 0 None 13 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 301 1 1 4 1.2 Cc1cccc(C)c1N1C(=O)CNC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4472251 171499 0 None 13 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 301 1 1 4 1.2 Cc1cccc(C)c1N1C(=O)CNC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
44404906 69912 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 218 3 2 2 2.4 CC(Cc1c[nH]c2cccc(O)c12)N(C)C 10.1016/j.bmcl.2005.06.104
CHEMBL194202 69912 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 218 3 2 2 2.4 CC(Cc1c[nH]c2cccc(O)c12)N(C)C 10.1016/j.bmcl.2005.06.104
24873261 182602 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 241 2 1 3 2.3 CCn1nc2c(c1-c1ccccc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4795756 182602 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 241 2 1 3 2.3 CCn1nc2c(c1-c1ccccc1)CCNCC2 10.1016/j.bmcl.2020.127669
16115644 136424 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 246 2 1 3 1.4 CCc1cc2c(cc1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374436 136424 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 246 2 1 3 1.4 CCc1cc2c(cc1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
145964150 163743 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
CHEMBL4212246 163743 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
118567543 170792 0 None -7 3 Human 6.1 pKi = 6.1 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 463 4 0 4 4.2 O=C1N(c2cccnc2C(F)(F)F)CC2(CCN(CCc3ccccc3F)CC2)OC12CC2 10.1021/acs.jmedchem.9b01256
CHEMBL4461774 170792 0 None -7 3 Human 6.1 pKi = 6.1 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 463 4 0 4 4.2 O=C1N(c2cccnc2C(F)(F)F)CC2(CCN(CCc3ccccc3F)CC2)OC12CC2 10.1021/acs.jmedchem.9b01256
88912137 110196 0 None -245 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 405 5 1 3 5.2 C[C@@H](Oc1ccc(C(F)(F)F)cc1OC1CNC1)c1cccc(C(F)(F)F)c1 10.1021/ml500082j
CHEMBL3260337 110196 0 None -245 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 405 5 1 3 5.2 C[C@@H](Oc1ccc(C(F)(F)F)cc1OC1CNC1)c1cccc(C(F)(F)F)c1 10.1021/ml500082j
122188580 122656 0 None -19 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 485 5 4 8 2.4 CCCNc1cc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acsmedchemlett.9b00637
CHEMBL3612941 122656 0 None -19 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 485 5 4 8 2.4 CCCNc1cc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acsmedchemlett.9b00637
71062889 147730 0 None -41 5 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
CHEMBL3936595 147730 0 None -41 5 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
44409096 76407 0 None -28 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 203 0 1 3 1.1 Cc1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL206845 76407 0 None -28 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 203 0 1 3 1.1 Cc1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
134138769 147126 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 419 6 4 8 1.7 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@@H](C4CCC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3931747 147126 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 419 6 4 8 1.7 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@@H](C4CCC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
132559161 172443 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT2b (unknown origin)Binding affinity to 5HT2b (unknown origin)
ChEMBL 538 7 2 7 1.8 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccoc2)N(C)C(=O)[C@H](Cc2ccoc2)NC(=O)[C@H](Cc2ccoc2)N(C)C1=O 10.1039/C9MD00050J
CHEMBL4518571 172443 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT2b (unknown origin)Binding affinity to 5HT2b (unknown origin)
ChEMBL 538 7 2 7 1.8 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccoc2)N(C)C(=O)[C@H](Cc2ccoc2)NC(=O)[C@H](Cc2ccoc2)N(C)C1=O 10.1039/C9MD00050J
90181066 159604 0 None 9 2 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 380 5 0 4 3.1 Cc1ccccc1OC[C@H]1CN(CC(=O)N2c3ccccc3CC2C)CCO1 nan
CHEMBL4109218 159604 0 None 9 2 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 380 5 0 4 3.1 Cc1ccccc1OC[C@H]1CN(CC(=O)N2c3ccccc3CC2C)CCO1 nan
136118652 92607 0 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3cccc(Br)c23)C(=O)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2442266 92607 0 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3cccc(Br)c23)C(=O)N1C 10.1016/j.bmc.2013.09.011
11673842 88645 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 264 2 2 2 2.1 CCCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337498 88645 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 264 2 2 2 2.1 CCCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365254 88645 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 264 2 2 2 2.1 CCCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
11361103 90660 1 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2ccc(C(F)(F)F)cc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397900 90660 1 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2ccc(C(F)(F)F)cc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
18715554 74060 0 None -10 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cnccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL202656 74060 0 None -10 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cnccc3c21 10.1016/j.bmcl.2005.10.029
24826871 90667 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397907 90667 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
25122653 198833 0 None -17 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL598850 198833 0 None -17 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
136118638 75948 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058698 75948 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
136118730 75876 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2cccc(Br)c12 10.1016/j.bmc.2013.09.011
CHEMBL2058407 75876 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2cccc(Br)c12 10.1016/j.bmc.2013.09.011
71062567 159856 0 None 2 2 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccnc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4111349 159856 0 None 2 2 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccnc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
54764239 68509 0 None - 1 Human 5.1 pKi = 5.1 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 272 2 1 3 2.7 CC/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL1922537 68509 0 None - 1 Human 5.1 pKi = 5.1 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 272 2 1 3 2.7 CC/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
11630623 88656 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337499 88656 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365399 88656 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
56649649 67500 0 None -93 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 480 8 0 5 4.6 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)CC3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910140 67500 0 None -93 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 480 8 0 5 4.6 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)CC3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
86221574 166123 2 None 9 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 375 5 2 2 3.4 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccccc2)CC1 10.1039/C8MD00204E
CHEMBL4282117 166123 2 None 9 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 375 5 2 2 3.4 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccccc2)CC1 10.1039/C8MD00204E
162674022 182629 0 None - 1 Human 7.1 pKi = 7.1 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 305 4 1 4 3.5 N#Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
CHEMBL4796102 182629 0 None - 1 Human 7.1 pKi = 7.1 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 305 4 1 4 3.5 N#Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
44299663 162564 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 306 3 2 3 3.9 CN(C)c1ccc(NC(=O)Nc2ccnc3ccccc23)cc1 10.1016/s0960-894x(01)00343-2
CHEMBL417753 162564 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 306 3 2 3 3.9 CN(C)c1ccc(NC(=O)Nc2ccnc3ccccc23)cc1 10.1016/s0960-894x(01)00343-2
10127939 71883 0 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 477 7 0 4 5.3 COc1ccc(N2CCN(c3ccc(C)c(C(F)(F)F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
CHEMBL198171 71883 0 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 477 7 0 4 5.3 COc1ccc(N2CCN(c3ccc(C)c(C(F)(F)F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
49850772 56090 0 None -501 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 397 5 0 5 4.1 Cc1ccc2c(N3CCN(CCc4cccc(-n5cccn5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631545 56090 0 None -501 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 397 5 0 5 4.1 Cc1ccc2c(N3CCN(CCc4cccc(-n5cccn5)c4)CC3)cccc2n1 10.1021/jm100714c
44298208 193009 0 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 429 3 1 5 4.9 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(Oc3cccnc3C)cn1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL53308 193009 0 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 429 3 1 5 4.9 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(Oc3cccnc3C)cn1)CC2 10.1016/s0960-894x(00)00364-4
18931357 204852 0 None -15 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 578 11 3 8 3.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL88894 204852 0 None -15 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 578 11 3 8 3.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/S0960-894X(96)00503-3
153287568 170408 0 None 15 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 217 0 1 2 2.5 Cc1cc(C)c2c(c1)OC[C@@]1(C)NCC[C@@H]21 10.1021/acsmedchemlett.9b00225
CHEMBL4456195 170408 0 None 15 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 217 0 1 2 2.5 Cc1cc(C)c2c(c1)OC[C@@]1(C)NCC[C@@H]21 10.1021/acsmedchemlett.9b00225
12017598 167543 0 None -15 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 429 4 1 5 4.4 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)nn1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL432879 167543 0 None -15 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 429 4 1 5 4.4 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)nn1)CC2 10.1016/s0960-894x(00)00365-6
21533446 69797 0 None -213 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940403 69797 0 None -213 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
117209964 185542 1 None -10 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4871980 185542 1 None -10 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
10194524 72192 0 None -63 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 415 7 0 5 3.0 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCN1CCOCC1 10.1016/j.bmcl.2005.08.004
CHEMBL199177 72192 0 None -63 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 415 7 0 5 3.0 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCN1CCOCC1 10.1016/j.bmcl.2005.08.004
49850567 56160 0 None -3981 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 452 6 1 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cnccn5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632217 56160 0 None -3981 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 452 6 1 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cnccn5)c4)CC3)cccc2n1 10.1021/jm100714c
44298142 101262 0 None -199 3 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 380 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3ccc(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL299726 101262 0 None -199 3 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 380 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3ccc(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
153287574 174665 0 None -10 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4572167 174665 0 None -10 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
10368126 86278 0 None -25 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 449 7 0 6 4.2 COc1ccc2c(c1)c1c(n2C)CN(c2ccc(OC)c(OCCN3CCCCC3)c2)C1=O 10.1016/j.bmcl.2006.10.034
CHEMBL231833 86278 0 None -25 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 449 7 0 6 4.2 COc1ccc2c(c1)c1c(n2C)CN(c2ccc(OC)c(OCCN3CCCCC3)c2)C1=O 10.1016/j.bmcl.2006.10.034
25164129 160601 0 None -1479 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 447 12 1 5 4.1 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4088036 160601 0 None -1479 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 447 12 1 5 4.1 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117406 160601 0 None -1479 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 447 12 1 5 4.1 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
25056080 65344 0 None -407 2 Human 5.1 pKi = 5.1 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
CHEMBL1834345 65344 0 None -407 2 Human 5.1 pKi = 5.1 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
24826788 90653 0 None 7 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 236 0 1 2 1.3 O=C1c2c(Cl)cccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397893 90653 0 None 7 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 236 0 1 2 1.3 O=C1c2c(Cl)cccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
71657836 120172 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(Br)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402673 120172 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(Br)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547134 120172 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(Br)c2)C1 10.1016/j.bmc.2015.01.060
135453290 133070 23 None -2 8 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL371300 133070 23 None -2 8 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
134551 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 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)C(C)C)O)C nan
271 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 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)C(C)C)O)C nan
885 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 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)C(C)C)O)C nan
CHEMBL1403281 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 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)C(C)C)O)C nan
30241 41784 14 None -8 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 204 3 2 2 2.2 COc1ccc2[nH]cc(C(C)CN)c2c1 10.1021/jm980318q
CHEMBL149564 41784 14 None -8 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 204 3 2 2 2.2 COc1ccc2[nH]cc(C(C)CN)c2c1 10.1021/jm980318q
11492162 71694 2 None 10 5 Human 8.1 pKi = 8.1 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 206 3 1 1 2.4 CN(C)CCc1c[nH]c2cccc(F)c12 10.1016/j.bmcl.2005.06.104
CHEMBL197646 71694 2 None 10 5 Human 8.1 pKi = 8.1 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 206 3 1 1 2.4 CN(C)CCc1c[nH]c2cccc(F)c12 10.1016/j.bmcl.2005.06.104
11615459 197558 0 None 10 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1cccc2c1C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590078 197558 0 None 10 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1cccc2c1C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
135414348 72449 2 None -4 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 205 2 2 4 1.4 Cc1c(O)ccc2cnn(C[C@H](C)N)c12 10.1021/jm050663x
CHEMBL200104 72449 2 None -4 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 205 2 2 4 1.4 Cc1c(O)ccc2cnn(C[C@H](C)N)c12 10.1021/jm050663x
CHEMBL5082177 213010 0 None 5 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCN(CCC)Cc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
2726 904 64 None -19 73 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 904 64 None -19 73 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 904 64 None -19 73 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 904 64 None -19 73 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 904 64 None -19 73 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
122178698 120838 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 369 5 0 5 3.9 CCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581244 120838 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 369 5 0 5 3.9 CCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
10827035 120180 0 None -13 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402666 120180 0 None -13 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547152 120180 0 None -13 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.01.060
118729281 120159 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 265 2 0 1 4.0 Cc1ccccc1[C@H]1C[C@H](N(C)C)Cc2ccccc21 10.1016/j.bmc.2015.01.060
CHEMBL3402686 120159 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 265 2 0 1 4.0 Cc1ccccc1[C@H]1C[C@H](N(C)C)Cc2ccccc21 10.1016/j.bmc.2015.01.060
CHEMBL3547018 120159 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 265 2 0 1 4.0 Cc1ccccc1[C@H]1C[C@H](N(C)C)Cc2ccccc21 10.1016/j.bmc.2015.01.060
44409316 74656 0 None -102 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 267 0 1 3 1.6 C[C@@H]1CNC[C@H]2Cc3ccc(Br)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL203393 74656 0 None -102 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 267 0 1 3 1.6 C[C@@H]1CNC[C@H]2Cc3ccc(Br)nc3N12 10.1016/j.bmcl.2005.11.083
145965940 163635 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 273 2 2 4 2.8 C[C@@H]1SC(c2cc3ccccc3cc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4210787 163635 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 273 2 2 4 2.8 C[C@@H]1SC(c2cc3ccccc3cc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
100 3733 52 None -11 56 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3733 52 None -11 56 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3733 52 None -11 56 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3733 52 None -11 56 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3733 52 None -11 56 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
168277348 189695 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 8 0 5 5.4 CCCCC(C)Oc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5175973 189695 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 8 0 5 5.4 CCCCC(C)Oc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
155558726 174226 0 None -19 4 Human 5.1 pKi = 5.1 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 835 11 0 13 6.7 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CC[C@H]3O[C@H](Cn4cc(nn4)COC[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12)[C@@H]1OC(C)(C)O[C@@H]1[C@H]3OCCC(C)C 10.1016/j.ejmech.2019.04.064
CHEMBL4562303 174226 0 None -19 4 Human 5.1 pKi = 5.1 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 835 11 0 13 6.7 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CC[C@H]3O[C@H](Cn4cc(nn4)COC[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12)[C@@H]1OC(C)(C)O[C@@H]1[C@H]3OCCC(C)C 10.1016/j.ejmech.2019.04.064
3042 1381 31 None -39 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1381 31 None -39 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1381 31 None -39 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1381 31 None -39 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1381 31 None -39 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
122483275 137569 0 None -3 8 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764133 137569 0 None -3 8 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765875 137569 0 None -3 8 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
11949706 198362 0 None -11 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]DOI from human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from human 5HT2B receptor expressed in CHO cells
ChEMBL 359 4 1 4 3.4 C[C@@H]1CNCCN1c1ccc2c(n1)[C@@H](OCc1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.10.112
CHEMBL595645 198362 0 None -11 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]DOI from human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from human 5HT2B receptor expressed in CHO cells
ChEMBL 359 4 1 4 3.4 C[C@@H]1CNCCN1c1ccc2c(n1)[C@@H](OCc1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.10.112
3037629 183979 13 None 1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 396 5 1 5 3.6 C=C[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
CHEMBL4848517 183979 13 None 1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 396 5 1 5 3.6 C=C[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
130442572 171332 0 None -17 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK 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 -17 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK 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
5591 156977 84 None 1 2 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 nan
CHEMBL408 156977 84 None 1 2 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 nan
21044398 140540 0 None -21 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 233 1 2 4 0.9 C[C@H](O)c1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL382618 140540 0 None -21 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 233 1 2 4 0.9 C[C@H](O)c1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
46945446 17565 0 None -5 2 Human 5.1 pKi = 5.1 Binding
Inhibition of 5-HT2B receptorInhibition of 5-HT2B receptor
ChEMBL 408 9 0 5 4.6 CCCCOc1ccc(-c2nn3c(C)cc(C)nc3c2CC(=O)N(CC)CC)cc1 10.1016/j.bmcl.2010.07.135
CHEMBL1258723 17565 0 None -5 2 Human 5.1 pKi = 5.1 Binding
Inhibition of 5-HT2B receptorInhibition of 5-HT2B receptor
ChEMBL 408 9 0 5 4.6 CCCCOc1ccc(-c2nn3c(C)cc(C)nc3c2CC(=O)N(CC)CC)cc1 10.1016/j.bmcl.2010.07.135
136118657 92610 0 None 12 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3c(Br)cccc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2442269 92610 0 None 12 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3c(Br)cccc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
44451393 156119 1 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 211 1 1 2 2.0 COc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL406957 156119 1 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 211 1 1 2 2.0 COc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
11437171 83063 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 234 1 1 3 1.5 CSc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL220207 83063 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 234 1 1 3 1.5 CSc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
155558968 174236 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 432 3 2 5 3.2 Cc1cccc(C)c1N1C(=O)[C@H](CC2CNc3ccccc32)NC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4562437 174236 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 432 3 2 5 3.2 Cc1cccc(C)c1N1C(=O)[C@H](CC2CNc3ccccc32)NC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
44572802 12323 2 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL1186019 12323 2 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL445747 12323 2 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
136016509 136118731 10844 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2ccc(Br)cc12 10.1016/j.bmc.2013.09.011
CHEMBL1173331 10844 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2ccc(Br)cc12 10.1016/j.bmc.2013.09.011
3168 9157 84 None -107 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9157 84 None -107 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
71450550 83379 0 None -1 16 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205836 83379 0 None -1 16 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
4543 169972 36 None -4 30 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL1201156 169972 36 None -4 30 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL445 169972 36 None -4 30 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
11300712 141142 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1c(Cl)ccc2c1C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL385577 141142 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1c(Cl)ccc2c1C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
59757162 105810 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)-c1ccccc1C2O 10.1016/j.bmc.2013.10.010
CHEMBL3092761 105810 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)-c1ccccc1C2O 10.1016/j.bmc.2013.10.010
CHEMBL3139074 105810 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)-c1ccccc1C2O 10.1016/j.bmc.2013.10.010
1548953 205935 24 None -4 17 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 205935 24 None -4 17 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
5870 31430 85 None - 1 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 270 0 1 2 3.8 C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O nan
CHEMBL1405 31430 85 None - 1 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 270 0 1 2 3.8 C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O nan
6452095 40447 17 None -9 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 174 2 2 1 2.2 CC(CN)c1c[nH]c2ccccc12 10.1021/jm980318q
CHEMBL148463 40447 17 None -9 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 174 2 2 1 2.2 CC(CN)c1c[nH]c2ccccc12 10.1021/jm980318q
11493484 88627 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337106 88627 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365079 88627 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
21509921 103966 0 None -8 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 103966 0 None -8 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
44554395 18521 0 None -54 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277565 18521 0 None -54 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
21509921 103966 0 None -8 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 103966 0 None -8 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
155565189 174982 0 None -6 4 Human 6.1 pKi = 6.1 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 634 7 0 9 6.2 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CCCCCCOCc3cn(nn3)C[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12 10.1016/j.ejmech.2019.04.064
CHEMBL4579120 174982 0 None -6 4 Human 6.1 pKi = 6.1 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 634 7 0 9 6.2 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CCCCCCOCc3cn(nn3)C[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12 10.1016/j.ejmech.2019.04.064
18735309 203712 0 None -3 3 Human 7.1 pKi = 7.1 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 262 2 1 2 2.6 C[C@H](N)CN1CCc2cc(F)c(C(F)(F)F)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL80246 203712 0 None -3 3 Human 7.1 pKi = 7.1 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 262 2 1 2 2.6 C[C@H](N)CN1CCc2cc(F)c(C(F)(F)F)cc21 10.1016/j.bmcl.2003.05.001
53381002 65119 0 None 15 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation counting
ChEMBL 240 2 2 4 2.2 COc1cccc2[nH]cc(-c3ccnc(N)n3)c12 10.1016/j.bmc.2011.08.033
CHEMBL1829959 65119 0 None 15 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation counting
ChEMBL 240 2 2 4 2.2 COc1cccc2[nH]cc(-c3ccnc(N)n3)c12 10.1016/j.bmc.2011.08.033
56649650 67501 0 None -100 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 466 8 0 5 4.2 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)C3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910141 67501 0 None -100 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 466 8 0 5 4.2 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)C3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
71062530 159533 0 None -3 2 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
CHEMBL4108620 159533 0 None -3 2 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
44407327 140703 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 345 6 1 4 4.4 COc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL383042 140703 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 345 6 1 4 4.4 COc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
136118617 75881 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058416 75881 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
44315993 172298 0 None -15 3 Human 7.1 pKi = 7.1 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 222 3 1 3 2.1 CSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
CHEMBL451543 172298 0 None -15 3 Human 7.1 pKi = 7.1 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 222 3 1 3 2.1 CSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
44572810 12531 2 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
CHEMBL1187196 12531 2 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
CHEMBL493130 12531 2 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
11346775 83054 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1cc(Cl)c2c(c1)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL220157 83054 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1cc(Cl)c2c(c1)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
132060776 161840 0 None -3 16 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4165863 161840 0 None -3 16 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
136118658 75886 0 None 2 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058426 75886 0 None 2 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
13091356 113026 0 None -218 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321789 113026 0 None -218 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
118717223 120058 0 None -7 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 321 1 2 2 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CCOCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343671 120058 0 None -7 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 321 1 2 2 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CCOCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3545813 120058 0 None -7 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 321 1 2 2 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CCOCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
46914485 15243 0 None 83 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 336 5 0 4 3.8 COc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
CHEMBL1214961 15243 0 None 83 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 336 5 0 4 3.8 COc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
44397731 66867 0 None -23 3 Human 7.1 pKi = 7.1 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 213 0 1 3 1.3 C[C@@H]1CNC[C@H]2Cc3ccc(C#N)cc3N12 10.1016/j.bmcl.2005.05.074
CHEMBL187888 66867 0 None -23 3 Human 7.1 pKi = 7.1 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 213 0 1 3 1.3 C[C@@H]1CNC[C@H]2Cc3ccc(C#N)cc3N12 10.1016/j.bmcl.2005.05.074
6319 23257 90 None - 1 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 4 2 2 5.2 c1ccc(Nc2ccc(Nc3ccccc3)cc2)cc1 nan
CHEMBL1333512 23257 90 None - 1 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 4 2 2 5.2 c1ccc(Nc2ccc(Nc3ccccc3)cc2)cc1 nan
44451369 95874 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 187 0 1 2 2.1 c1cc2c3c(ccc2o1)CCNCC3 10.1016/j.bmc.2007.12.009
CHEMBL261489 95874 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 187 0 1 2 2.1 c1cc2c3c(ccc2o1)CCNCC3 10.1016/j.bmc.2007.12.009
135753056 190571 1 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assay
ChEMBL 337 4 2 5 2.4 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2cccc(C)c2)n1 10.1021/acs.jmedchem.1c01759
CHEMBL5188949 190571 1 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assay
ChEMBL 337 4 2 5 2.4 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2cccc(C)c2)n1 10.1021/acs.jmedchem.1c01759
16062145 97196 0 None -223 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 269 2 1 3 2.8 Fc1ccc(-c2nc(C3CC3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL271111 97196 0 None -223 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 269 2 1 3 2.8 Fc1ccc(-c2nc(C3CC3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
11716185 88621 0 None -20 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 250 1 2 2 1.7 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337497 88621 0 None -20 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 250 1 2 2 1.7 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2364998 88621 0 None -20 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 250 1 2 2 1.7 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
10028436 3463 3 None -45 12 Human 7.0 pKi = 7.0 Binding
Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2B receptor in HEK 293 using [3H]ketanserin as a radioligandCompound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2B receptor in HEK 293 using [3H]ketanserin as a radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
3237 3463 3 None -45 12 Human 7.0 pKi = 7.0 Binding
Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2B receptor in HEK 293 using [3H]ketanserin as a radioligandCompound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2B receptor in HEK 293 using [3H]ketanserin as a radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
CHEMBL95104 3463 3 None -45 12 Human 7.0 pKi = 7.0 Binding
Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2B receptor in HEK 293 using [3H]ketanserin as a radioligandCompound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2B receptor in HEK 293 using [3H]ketanserin as a radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
25209705 180468 23 None -144 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 510 7 2 8 3.3 COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCNCC5)cc4=O)c3C)cc2)cn1 10.1021/jm800962k
CHEMBL475965 180468 23 None -144 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 510 7 2 8 3.3 COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCNCC5)cc4=O)c3C)cc2)cn1 10.1021/jm800962k
168294400 191872 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 423 5 0 5 5.2 COc1cc2c(cc1OC)-c1c(OC)c(OC3CCCCC3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5208882 191872 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 423 5 0 5 5.2 COc1cc2c(cc1OC)-c1c(OC)c(OC3CCCCC3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
118055296 177367 0 None -58 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 264 2 1 2 2.7 c1ccc(Cc2ccc3c4c2CCN4CCNC3)cc1 10.1016/j.bmcl.2019.126929
CHEMBL4645736 177367 0 None -58 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 264 2 1 2 2.7 c1ccc(Cc2ccc3c4c2CCN4CCNC3)cc1 10.1016/j.bmcl.2019.126929
122483281 137567 0 None -18 8 Human 7.0 pKi = 7.0 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3763779 137567 0 None -18 8 Human 7.0 pKi = 7.0 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3765873 137567 0 None -18 8 Human 7.0 pKi = 7.0 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
136118649 75954 0 None 2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058704 75954 0 None 2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
11819486 120623 0 None -4 4 Human 7.0 pKi = 7.0 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 172 1 2 1 2.0 N[C@H]1C[C@@H]1c1c[nH]c2ccccc12 10.1021/jm980318q
CHEMBL357702 120623 0 None -4 4 Human 7.0 pKi = 7.0 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 172 1 2 1 2.0 N[C@H]1C[C@@H]1c1c[nH]c2ccccc12 10.1021/jm980318q
58911668 90665 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397905 90665 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
162652711 179789 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 409 6 3 7 2.6 CC(C)[C@@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CF)C[C@H]12)C1CC1 10.1016/j.bmcl.2020.127599
CHEMBL4751718 179789 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 409 6 3 7 2.6 CC(C)[C@@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CF)C[C@H]12)C1CC1 10.1016/j.bmcl.2020.127599
71452341 83269 4 None -3 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysis
ChEMBL 376 6 0 3 5.3 Cc1c(C(=O)N(CCCN2CCCCC2)c2ccccc2)oc2ccccc12 10.1016/j.bmc.2012.09.044
CHEMBL2205361 83269 4 None -3 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysis
ChEMBL 376 6 0 3 5.3 Cc1c(C(=O)N(CCCN2CCCCC2)c2ccccc2)oc2ccccc12 10.1016/j.bmc.2012.09.044
11848625 5700 0 None 2 6 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 10.1016/j.bmcl.2009.09.024
CHEMBL1078745 5700 0 None 2 6 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 10.1016/j.bmcl.2009.09.024
136118614 92618 0 None 3 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442276 92618 0 None 3 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
10106214 2064 1 None -46 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
1207 2064 1 None -46 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
1209 2064 1 None -46 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
CHEMBL127307 2064 1 None -46 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
6604117 187254 6 None 1 6 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL2062340 187254 6 None 1 6 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL49623 187254 6 None 1 6 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
49864027 15228 0 None 25 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 400 8 0 4 4.8 FC(F)CCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
CHEMBL1214891 15228 0 None 25 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 400 8 0 4 4.8 FC(F)CCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
168279369 190529 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 6 0 5 4.6 CCC(C)Oc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5188171 190529 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 6 0 5 4.6 CCC(C)Oc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
122186880 122452 0 None 4 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3608450 122452 0 None 4 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
44554227 18548 0 None -33 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277837 18548 0 None -33 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
20824949 66845 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 245 1 2 3 1.4 CC(=O)Nc1ccc2c(c1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL187787 66845 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 245 1 2 3 1.4 CC(=O)Nc1ccc2c(c1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
667590 67437 12 None - 1 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 3 0 1 4.4 O=C(c1ccccc1Cl)N1CCC(Cc2ccccc2)CC1 nan
CHEMBL1909048 67437 12 None - 1 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 3 0 1 4.4 O=C(c1ccccc1Cl)N1CCC(Cc2ccccc2)CC1 nan
44582676 189177 0 None -295 18 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 189177 0 None -295 18 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
135511529 135555540 10871 0 None 5 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 240 1 3 2 1.5 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2ccccc12 10.1016/j.bmc.2013.09.011
CHEMBL1173525 10871 0 None 5 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 240 1 3 2 1.5 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2ccccc12 10.1016/j.bmc.2013.09.011
136118661 75889 0 None 6 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058429 75889 0 None 6 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
44112 120764 41 None -11 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
CHEMBL357995 120764 41 None -11 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
124247485 163506 7 None 1 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4209274 163506 7 None 1 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
155563428 174704 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 475 7 3 9 2.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL4572905 174704 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 475 7 3 9 2.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
44581974 175121 0 None -1 9 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 513 6 2 6 4.6 Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458220 175121 0 None -1 9 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 513 6 2 6 4.6 Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
25123013 198764 0 None -27 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598443 198764 0 None -27 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
10383646 18560 0 None -512 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277917 18560 0 None -512 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
71450247 82549 0 None -19 9 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181188 82549 0 None -19 9 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
44404905 72020 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 218 4 2 2 2.4 CN(C)CCCc1c[nH]c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL198617 72020 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 218 4 2 2 2.4 CN(C)CCCc1c[nH]c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
17683252 67439 3 None - 1 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 347 3 0 1 4.8 O=C(c1ccccc1C(F)(F)F)N1CCC(Cc2ccccc2)CC1 nan
CHEMBL1909051 67439 3 None - 1 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 347 3 0 1 4.8 O=C(c1ccccc1C(F)(F)F)N1CCC(Cc2ccccc2)CC1 nan
142601328 184410 0 None -63 5 Human 6.0 pKi = 6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4854605 184410 0 None -63 5 Human 6.0 pKi = 6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
142601341 184780 0 None -3 3 Human 6.0 pKi = 6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 272 3 2 4 1.9 COc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4860503 184780 0 None -3 3 Human 6.0 pKi = 6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 272 3 2 4 1.9 COc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
56649648 67498 0 None -301 8 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 474 8 0 5 3.0 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52CF)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910139 67498 0 None -301 8 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 474 8 0 5 3.0 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52CF)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
136118616 75880 0 None 3 6 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058415 75880 0 None 3 6 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
136118646 75951 0 None 2 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058701 75951 0 None 2 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
3007 155132 25 None -1 6 Rat 8.3 pKd = 8.3 Binding
Affinity against serotonergic receptor in the isolated rat stomach fundusAffinity against serotonergic receptor in the isolated rat stomach fundus
Drug Central 135 2 1 1 1.6 CC(N)Cc1ccccc1 None
CHEMBL405 155132 25 None -1 6 Rat 8.3 pKd = 8.3 Binding
Affinity against serotonergic receptor in the isolated rat stomach fundusAffinity against serotonergic receptor in the isolated rat stomach fundus
Drug Central 135 2 1 1 1.6 CC(N)Cc1ccccc1 None
10615 566 26 None 501 4 Human 11.6 pKd = 11.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
46200932 566 26 None 501 4 Human 11.6 pKd = 11.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
CHEMBL4297183 566 26 None 501 4 Human 11.6 pKd = 11.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
DB14823 566 26 None 501 4 Human 11.6 pKd = 11.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
136 3228 28 None -12 16 Human 8.4 pKd None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
223 3228 28 None -12 16 Human 8.4 pKd None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
643606 3228 28 None -12 16 Human 8.4 pKd None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
CHEMBL10347 3228 28 None -12 16 Human 8.4 pKd None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
134 2468 19 3H- LSD -2 68 Human 10.0 pKi = 10 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
134 2468 19 3H-LSD -2 68 Human 10.0 pKi = 10 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 3H- LSD -2 68 Human 10.0 pKi = 10 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 3H-LSD -2 68 Human 10.0 pKi = 10 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 3H- LSD -2 68 Human 10.0 pKi = 10 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 3H-LSD -2 68 Human 10.0 pKi = 10 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 3H- LSD -2 68 Human 10.0 pKi = 10 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 3H-LSD -2 68 Human 10.0 pKi = 10 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 3H- LSD -2 68 Human 10.0 pKi = 10 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 3H-LSD -2 68 Human 10.0 pKi = 10 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
188 3327 73 3H-5HT -1 6 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
196968 3327 73 3H-5HT -1 6 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
CHEMBL473186 3327 73 3H-5HT -1 6 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
242 467 117 3H-LSD -1 52 Human 9.4 pKi = 9.4 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]-LSD -1 52 Human 9.4 pKi = 9.4 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-LSD -1 52 Human 9.4 pKi = 9.4 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]-LSD -1 52 Human 9.4 pKi = 9.4 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-LSD -1 52 Human 9.4 pKi = 9.4 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]-LSD -1 52 Human 9.4 pKi = 9.4 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-LSD -1 52 Human 9.4 pKi = 9.4 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]-LSD -1 52 Human 9.4 pKi = 9.4 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-LSD -1 52 Human 9.4 pKi = 9.4 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]-LSD -1 52 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
134 2468 19 3H-5HT -2 68 Human 9.4 pKi = 9.4 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 3H-5HT -2 68 Human 9.4 pKi = 9.4 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 3H-5HT -2 68 Human 9.4 pKi = 9.4 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 3H-5HT -2 68 Human 9.4 pKi = 9.4 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 3H-5HT -2 68 Human 9.4 pKi = 9.4 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
5074 3268 75 3H-RAUWOLSCINE -3 30 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3268 75 3H-RAUWOLSCINE -3 30 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3268 75 3H-RAUWOLSCINE -3 30 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3268 75 3H-RAUWOLSCINE -3 30 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
None 214271 0 3H-5HT -2 8 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 339 4 3 3 1.9 CCC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
None 214271 0 3H-5HT -2 8 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 339 4 3 3 1.9 CCC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
107 141 116 3H-5HT -4 31 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-5HT -4 31 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-5HT -4 31 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
None 214620 0 3H-MESULERGINE 5 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 342 4 3 4 2.5 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N.C(=CC(=O)O)C(=O)O None
4106 2456 16 3H-RAUWOLSCINE -3 34 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2456 16 3H-RAUWOLSCINE -3 34 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2456 16 3H-RAUWOLSCINE -3 34 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2456 16 3H-RAUWOLSCINE -3 34 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
134 2468 19 3H-RAUWOLSCINE -2 68 Human 9.2 pKi = 9.2 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 3H-RAUWOLSCINE -2 68 Human 9.2 pKi = 9.2 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 3H-RAUWOLSCINE -2 68 Human 9.2 pKi = 9.2 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 3H-RAUWOLSCINE -2 68 Human 9.2 pKi = 9.2 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 3H-RAUWOLSCINE -2 68 Human 9.2 pKi = 9.2 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
133 2450 48 3H-MESULERGINE -2 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2450 48 3H-MESULERGINE -2 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2450 48 3H-MESULERGINE -2 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2450 48 3H-MESULERGINE -2 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2450 48 3H-MESULERGINE -2 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
133 2450 48 3H-5HT -2 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2450 48 3H-5HT -2 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2450 48 3H-5HT -2 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2450 48 3H-5HT -2 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2450 48 3H-5HT -2 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
6437377 214165 0 3H-RAUWOLSCINE 5 5 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 500 6 3 7 3.2 CC(C)N1C=C2CC3C(CC(CN3C)C(=O)OC(C)C(C)O)C4=C2C1=CC=C4.C(=CC(=O)O)C(=O)O None
5 139 66 3H-5HT -13 55 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -13 55 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -13 55 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -13 55 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
2470 3583 46 3H-KETANSERIN -23 60 Bovine 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-KETANSERIN -23 60 Bovine 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-KETANSERIN -23 60 Bovine 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-KETANSERIN -23 60 Bovine 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-KETANSERIN -23 60 Bovine 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
None 214271 0 Functional -2 8 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 339 4 3 3 1.9 CCC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
1342 36 42 3H-RAUWOLSCINE 2 19 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 42 3H-RAUWOLSCINE 2 19 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 42 3H-RAUWOLSCINE 2 19 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
None 214620 0 Functional 5 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 342 4 3 4 2.5 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N.C(=CC(=O)O)C(=O)O None
1621 2386 16 3H-5HT -19 45 Human 9.0 pKi = 9.0 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 3H-5HT -19 45 Human 9.0 pKi = 9.0 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 3H-5HT -19 45 Human 9.0 pKi = 9.0 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 3H-5HT -19 45 Human 9.0 pKi = 9.0 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 3H-5HT -19 45 Human 9.0 pKi = 9.0 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
5 139 66 Functional -13 55 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 Functional -13 55 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 Functional -13 55 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 Functional -13 55 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5074 3268 75 3H-5HT -3 30 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3268 75 3H-5HT -3 30 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3268 75 3H-5HT -3 30 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3268 75 3H-5HT -3 30 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
1588 2284 24 3H-5HT -8 44 Human 9.0 pKi = 9.0 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-5HT -8 44 Human 9.0 pKi = 9.0 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-5HT -8 44 Human 9.0 pKi = 9.0 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-5HT -8 44 Human 9.0 pKi = 9.0 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-5HT -8 44 Human 9.0 pKi = 9.0 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
188 3327 73 3H-5HT -1 6 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
196968 3327 73 3H-5HT -1 6 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
CHEMBL473186 3327 73 3H-5HT -1 6 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
None 214693 0 Functional 1 28 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
5 139 66 3H-5HT -13 55 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -13 55 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -13 55 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -13 55 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
None 214580 0 3H-MESULERGINE -1 19 Human 8.9 pKi = 8.9 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
103 4074 56 3H-LSD 1 54 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4074 56 3H-LSD 1 54 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4074 56 3H-LSD 1 54 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4074 56 3H-LSD 1 54 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4074 56 3H-LSD 1 54 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5074 3268 75 3H-MESULERGINE -3 30 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3268 75 3H-MESULERGINE -3 30 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3268 75 3H-MESULERGINE -3 30 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3268 75 3H-MESULERGINE -3 30 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
189 3423 31 UNDEFINED 2 18 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
5163 3423 31 UNDEFINED 2 18 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
CHEMBL297784 3423 31 UNDEFINED 2 18 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
11954224 214164 0 3H-5HT -66 60 Human 8.9 pKi = 8.9 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
1588 2284 24 3H-MESULERGINE -8 44 Human 8.9 pKi = 8.9 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-MESULERGINE -8 44 Human 8.9 pKi = 8.9 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-MESULERGINE -8 44 Human 8.9 pKi = 8.9 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-MESULERGINE -8 44 Human 8.9 pKi = 8.9 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-MESULERGINE -8 44 Human 8.9 pKi = 8.9 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
1588 2284 24 3H-MESULERGINE -8 44 Human 8.9 pKi = 8.9 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-MESULERGINE -8 44 Human 8.9 pKi = 8.9 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-MESULERGINE -8 44 Human 8.9 pKi = 8.9 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-MESULERGINE -8 44 Human 8.9 pKi = 8.9 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-MESULERGINE -8 44 Human 8.9 pKi = 8.9 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
2435 3520 78 3H-LSD -2 49 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3520 78 3H-LSD -2 49 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3520 78 3H-LSD -2 49 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3520 78 3H-LSD -2 49 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3520 78 3H-LSD -2 49 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
11957541 1425 38 Functional -2 16 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1425 38 Functional -2 16 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1425 38 Functional -2 16 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1425 38 Functional -2 16 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1425 38 Functional -2 16 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
206 2447 10 3H-5HT -1 25 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2447 10 3H-5HT -1 25 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2447 10 3H-5HT -1 25 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
134 2468 19 3H-5HT -2 68 Human 8.8 pKi = 8.8 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 3H-5HT -2 68 Human 8.8 pKi = 8.8 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 3H-5HT -2 68 Human 8.8 pKi = 8.8 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 3H-5HT -2 68 Human 8.8 pKi = 8.8 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 3H-5HT -2 68 Human 8.8 pKi = 8.8 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
6437377 214165 0 3H-5HT 5 5 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 500 6 3 7 3.2 CC(C)N1C=C2CC3C(CC(CN3C)C(=O)OC(C)C(C)O)C4=C2C1=CC=C4.C(=CC(=O)O)C(=O)O None
277 1269 55 3H-5HT -5 46 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1269 55 3H-5HT -5 46 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1269 55 3H-5HT -5 46 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1269 55 3H-5HT -5 46 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1269 55 3H-5HT -5 46 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
4106 2456 16 3H-5HT -3 34 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2456 16 3H-5HT -3 34 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2456 16 3H-5HT -3 34 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2456 16 3H-5HT -3 34 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
135 2486 38 3H-5HT -3 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 3H-5HT -3 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 3H-5HT -3 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 3H-5HT -3 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 3H-5HT -3 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
134 2468 19 3H-5HT -2 68 Human 8.8 pKi = 8.8 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 3H-5HT -2 68 Human 8.8 pKi = 8.8 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 3H-5HT -2 68 Human 8.8 pKi = 8.8 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 3H-5HT -2 68 Human 8.8 pKi = 8.8 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 3H-5HT -2 68 Human 8.8 pKi = 8.8 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
6437377 214165 0 3H-5HT 5 5 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 500 6 3 7 3.2 CC(C)N1C=C2CC3C(CC(CN3C)C(=O)OC(C)C(C)O)C4=C2C1=CC=C4.C(=CC(=O)O)C(=O)O None
5074 3268 75 3H-5HT -3 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3268 75 3H-5HT -3 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3268 75 3H-5HT -3 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3268 75 3H-5HT -3 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
134 2468 19 3H-5HT -2 68 Human 8.8 pKi = 8.8 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 3H-5HT -2 68 Human 8.8 pKi = 8.8 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 3H-5HT -2 68 Human 8.8 pKi = 8.8 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 3H-5HT -2 68 Human 8.8 pKi = 8.8 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 3H-5HT -2 68 Human 8.8 pKi = 8.8 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
5074 3268 75 3H-5HT -3 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3268 75 3H-5HT -3 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3268 75 3H-5HT -3 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3268 75 3H-5HT -3 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
133 2450 48 3H-5HT -2 43 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2450 48 3H-5HT -2 43 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2450 48 3H-5HT -2 43 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2450 48 3H-5HT -2 43 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2450 48 3H-5HT -2 43 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
11954224 214164 0 3H- LSD -66 60 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
11954224 214164 0 3H-LSD -66 60 Human 8.7 pKi = 8.7 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
206 2447 10 3H-RAUWOLSCINE -1 25 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2447 10 3H-RAUWOLSCINE -1 25 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2447 10 3H-RAUWOLSCINE -1 25 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
206 2447 10 3H-MESULERGINE -1 25 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2447 10 3H-MESULERGINE -1 25 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2447 10 3H-MESULERGINE -1 25 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
199 389 0 3H-5HT 1 5 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
9821951 389 0 3H-5HT 1 5 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
CHEMBL160293 389 0 3H-5HT 1 5 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
5 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
135398737 942 89 3H-5HT -2 92 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 3H-5HT -2 92 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 3H-5HT -2 92 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 3H-5HT -2 92 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 3H-5HT -2 92 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
152 361 18 3H-5HT -1 19 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 361 18 3H-5HT -1 19 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 361 18 3H-5HT -1 19 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
152 361 18 3H-5HT -1 19 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 361 18 3H-5HT -1 19 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 361 18 3H-5HT -1 19 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
7153 97557 74 3H-RAUWOLSCINE -1 34 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-RAUWOLSCINE -1 34 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
199 389 0 3H-5HT -5 5 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
9821951 389 0 3H-5HT -5 5 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
CHEMBL160293 389 0 3H-5HT -5 5 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
11957541 1425 38 3H-KETANSERIN -17 16 Bovine 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1425 38 3H-KETANSERIN -17 16 Bovine 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1425 38 3H-KETANSERIN -17 16 Bovine 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1425 38 3H-KETANSERIN -17 16 Bovine 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1425 38 3H-KETANSERIN -17 16 Bovine 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1614 201951 22 Functional 2 10 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
CHEMBL6731 201951 22 Functional 2 10 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
24840389 114701 3 3H-MESULERGINE -741 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
CHEMBL334529 114701 3 3H-MESULERGINE -741 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
1809 134 28 3H-KETANSERIN -109647 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-KETANSERIN -109647 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-KETANSERIN -109647 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1209 1620 69 3H-5HT -199 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1620 69 3H-5HT -199 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1620 69 3H-5HT -199 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1620 69 3H-5HT -199 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1620 69 3H-5HT -199 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
1357 2440 133 3H-5HT -3890 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 3H-5HT -3890 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 3H-5HT -3890 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 3H-5HT -3890 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 3H-5HT -3890 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 3H-5HT -3890 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
107992 2506 47 3H-5HT -5 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 2506 47 3H-5HT -5 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 2506 47 3H-5HT -5 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 2506 47 3H-5HT -5 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
208 2810 0 3H-5HT -69 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
4541 2810 0 3H-5HT -69 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL1494 2810 0 3H-5HT -69 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
119570 3098 90 3H-LSD -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-MESULERGINE -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-LSD -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-MESULERGINE -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-LSD -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-MESULERGINE -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-LSD -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-MESULERGINE -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-LSD -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-MESULERGINE -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 3H-5HT -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 3H-5HT -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 3H-5HT -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 3H-5HT -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 3H-5HT -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
2 3198 19 3H-MESULERGINE -363 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-MESULERGINE -363 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-MESULERGINE -363 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
128563 3395 28 3H-LSD -2398 42 Human 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 3H-LSD -2398 42 Human 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 3H-LSD -2398 42 Human 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 3H-LSD -2398 42 Human 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
2470 3583 46 3H-5HT -120226 60 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-5HT -120226 60 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-5HT -120226 60 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-5HT -120226 60 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-5HT -120226 60 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2543 3638 66 3H-5HT -2818 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2543 3638 66 3H-5HT -2818 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3638 66 3H-5HT -2818 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3638 66 3H-5HT -2818 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3638 66 3H-5HT -2818 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3638 66 3H-5HT -2818 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3638 66 3H-5HT -2818 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3638 66 3H-5HT -2818 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3638 66 3H-5HT -2818 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3638 66 3H-5HT -2818 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
46882133 5716 0 UNDEFINED -54 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC None
CHEMBL1078896 5716 0 UNDEFINED -54 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC None
46882180 5749 0 UNDEFINED -39 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F None
CHEMBL1079180 5749 0 UNDEFINED -39 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F None
2662 11264 124 3H-LSD -41 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 11264 124 3H-LSD -41 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
10836 14314 13 3H-LSD -3 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
CHEMBL1201201 14314 13 3H-LSD -3 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
5210 33104 45 3H-5HT -123 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 None
CHEMBL1200765 33104 45 3H-5HT -123 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 None
CHEMBL1419 33104 45 3H-5HT -123 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 None
156391 46522 95 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 46522 95 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 46522 95 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
4771 50244 26 3H-5HT 1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 1 2.0 CC(C)(N)Cc1ccccc1 None
CHEMBL1574 50244 26 3H-5HT 1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 1 2.0 CC(C)(N)Cc1ccccc1 None
2244 93785 96 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 93785 96 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
4076 96572 23 3H-KETANSERIN -26 8 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 5 1 4 1.2 COc1cc(CCN)cc(OC)c1OC None
CHEMBL26687 96572 23 3H-KETANSERIN -26 8 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 5 1 4 1.2 COc1cc(CCN)cc(OC)c1OC None
104870 98410 39 3H-MESULERGINE -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-MESULERGINE -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-MESULERGINE -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
43815 186327 58 3H-5HT -1995 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186327 58 3H-5HT -1995 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186327 58 3H-5HT -1995 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
54676228 192864 108 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 192864 108 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
4495 194850 87 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 194850 87 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
54677470 198857 110 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 198857 110 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 198857 110 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
5281600 201327 85 3H-LSD -275 33 Human 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 3H-LSD -275 33 Human 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
5656 201368 82 3H-5HT -79 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 201368 82 3H-5HT -79 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
4158 203620 21 3H-5HT -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 203620 21 3H-5HT -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 203620 21 3H-5HT -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
4054 203780 64 3H-LSD -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-LSD -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-LSD -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
6852400 214150 0 3H-KETANSERIN -25118 22 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 214150 0 3H-KETANSERIN -25118 22 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
3821 214539 0 3H-LSD -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(CCCCC1=O)C2=CC=CC=C2Cl None
None 214581 0 3H-MESULERGINE -1862 19 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 246 2 1 4 1.6 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N None
135269 214629 0 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 214630 0 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 214631 0 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
3672 214632 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)CC1=CC=C(C=C1)C(C)C(=O)O None
84003 214633 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
123619 214634 0 3H-LSD -1412 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 214635 0 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
5090 214636 0 3H-LSD -1348 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3 None
None 214638 0 3H-LSD -7 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
None 214694 0 3H-5HT -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 4 1 1 4.6 CC(C)CC(C1(CCC1)C2=CC=C(C=C2)Cl)N.Cl None
None 214737 0 3H-LSD -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
1150 3805 116 3H-5HT -2 25 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3805 116 3H-5HT -2 25 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3805 116 3H-5HT -2 25 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3805 116 3H-5HT -2 25 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
185 3931 54 3H-5HT -2344 38 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3931 54 3H-5HT -2344 38 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3931 54 3H-5HT -2344 38 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3931 54 3H-5HT -2344 38 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
62787 204457 17 3H-5HT -10 10 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
CHEMBL8642 204457 17 3H-5HT -10 10 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
None 214356 0 3H-LSD -1122 24 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
102 4051 44 3H-5HT -100 50 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 3H-5HT -100 50 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 3H-5HT -100 50 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 3H-5HT -100 50 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 3H-5HT -100 50 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
141 1394 32 3H-LSD -1 22 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1394 32 3H-LSD -1 22 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1394 32 3H-LSD -1 22 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1394 32 3H-LSD -1 22 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
3668 214342 0 3H-LSD -977 10 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 510 5 4 9 0.4 CNC(=O)C1C(C(C(O1)N2C=NC3=C2N=CN=C3NCC4=CC(=CC=C4)I)O)O None
146 135 80 3H-5HT -1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 None
164682 135 80 3H-5HT -1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 None
CHEMBL275628 135 80 3H-5HT -1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 None
1621 2386 16 3H-KETANSERIN -35 45 Bovine 8.0 pKi = 8.0 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 3H-KETANSERIN -35 45 Bovine 8.0 pKi = 8.0 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 3H-KETANSERIN -35 45 Bovine 8.0 pKi = 8.0 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 3H-KETANSERIN -35 45 Bovine 8.0 pKi = 8.0 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 3H-KETANSERIN -35 45 Bovine 8.0 pKi = 8.0 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
15897 2807 0 3H-LSD 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2807 0 3H-LSD 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2807 0 3H-LSD 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
15897 2807 0 3H-5-HT 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
15897 2807 0 3H-5HT 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2807 0 3H-5-HT 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2807 0 3H-5HT 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2807 0 3H-5-HT 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2807 0 3H-5HT 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
5 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
152 361 18 3H-5HT 1 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 361 18 3H-5HT 1 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 361 18 3H-5HT 1 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
135398745 2858 108 3H-5HT -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 3H-5HT -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 3H-5HT -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 3H-5HT -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
152 361 18 3H-5HT 1 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 361 18 3H-5HT 1 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 361 18 3H-5HT 1 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
45486902 195261 0 UNDEFINED -3 2 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 449 5 2 4 4.6 O=c1[nH]c2cccc(OCC3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 None
CHEMBL566396 195261 0 UNDEFINED -3 2 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 449 5 2 4 4.6 O=c1[nH]c2cccc(OCC3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 None
1150 3805 116 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3805 116 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3805 116 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3805 116 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
1150 3805 116 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3805 116 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3805 116 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3805 116 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
77590 214166 0 3H-5HT -15 6 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 124 4 0 2 0.8 COCCOCCl None
2389 3267 114 35S-GTPGammaS -79 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 35S-GTPGammaS -79 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 35S-GTPGammaS -79 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 35S-GTPGammaS -79 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 35S-GTPGammaS -79 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
542051 204370 4 3H-5HT -128 7 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 237 6 1 3 2.5 CCCc1cc(OC)c(CC(C)N)cc1OC None
CHEMBL8569 204370 4 3H-5HT -128 7 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 237 6 1 3 2.5 CCCc1cc(OC)c(CC(C)N)cc1OC None
1809 134 28 3H-5HT -999 37 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-5HT -999 37 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-5HT -999 37 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
5 139 66 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
199 389 0 3H-5HT -5 5 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
9821951 389 0 3H-5HT -5 5 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
CHEMBL160293 389 0 3H-5HT -5 5 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
135398745 2858 108 35S-GTPGammaS -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 35S-GTPGammaS -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 35S-GTPGammaS -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 35S-GTPGammaS -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135 2486 38 3H-5HT -3 58 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 3H-5HT -3 58 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 3H-5HT -3 58 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 3H-5HT -3 58 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 3H-5HT -3 58 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
7153 97557 74 3H-MESULERGINE -1 34 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-MESULERGINE -1 34 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
134 2468 19 125I-DOI -10 68 Mouse 7.9 pKi = 7.9 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-DOI -10 68 Mouse 7.9 pKi = 7.9 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-DOI -10 68 Mouse 7.9 pKi = 7.9 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-DOI -10 68 Mouse 7.9 pKi = 7.9 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-DOI -10 68 Mouse 7.9 pKi = 7.9 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
None 214693 0 Functional -1 28 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 214693 0 UNDEFINED -1 28 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 214158 0 3H-KETANSERIN -851 24 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
2202 3071 91 3H-MESULERGINE -6 21 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3071 91 3H-MESULERGINE -6 21 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3071 91 3H-MESULERGINE -6 21 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3071 91 3H-MESULERGINE -6 21 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3071 91 3H-MESULERGINE -6 21 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
221 3422 63 3H-5HT -4 14 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 3422 63 3H-5HT -4 14 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 3422 63 3H-5HT -4 14 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
5 139 66 125I-DOI -2951 55 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 125I-DOI -2951 55 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 125I-DOI -2951 55 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 125I-DOI -2951 55 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1809 134 28 3H-5HT -999 37 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-5HT -999 37 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-5HT -999 37 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
173 3199 88 3H-5HT -3 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3199 88 3H-5HT -3 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3199 88 3H-5HT -3 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
None 214451 0 3H-5HT -120 15 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 438 5 1 4 4.8 C1CC(CCC1CCN2CCC3=C(C2)C=CC(=C3)C#N)NC(=O)C4=CC=NC5=CC=CC=C45 None
179 396 107 3H-LSD -17 51 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 3H-LSD -17 51 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 3H-LSD -17 51 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 3H-LSD -17 51 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 3H-LSD -17 51 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
77379 18841 66 3H-5HT -2 2 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 194 2 2 1 2.3 NCCc1c[nH]c2ccc(Cl)cc12 None
CHEMBL1288716 18841 66 3H-5HT -2 2 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 194 2 2 1 2.3 NCCc1c[nH]c2ccc(Cl)cc12 None
102 4051 44 3H-RAUWOLSCINE -93 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 3H-RAUWOLSCINE -93 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 3H-RAUWOLSCINE -93 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 3H-RAUWOLSCINE -93 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 3H-RAUWOLSCINE -93 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
5 139 66 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
77158 18842 48 3H-5HT 2 2 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 None
CHEMBL1288717 18842 48 3H-5HT 2 2 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 None
None 215721 0 UNDEFINED -14 3 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 421 4 3 4 3.3 C1CC2=C(CC1CNCC3COC4=C(O3)C=CC5=C4CC(=O)N5)C6=C(N2)C=CC(=C6)F None
145 140 48 3H-KETANSERIN -251 30 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 48 3H-KETANSERIN -251 30 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 48 3H-KETANSERIN -251 30 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 48 3H-KETANSERIN -251 30 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1150 3805 116 3H-KETANSERIN -56 25 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3805 116 3H-KETANSERIN -56 25 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3805 116 3H-KETANSERIN -56 25 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3805 116 3H-KETANSERIN -56 25 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
173 3199 88 3H-5HT -3 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3199 88 3H-5HT -3 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3199 88 3H-5HT -3 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
25058166 214171 0 3H-MESULERGINE -66 27 Human 6.9 pKi = 6.9 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-MESULERGINE -66 27 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
2470 3583 46 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 3583 46 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
None 214158 0 3H-5HT -33 24 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
130 3431 43 3H-5HT -478 13 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3378093 3431 43 3H-5HT -478 13 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL281350 3431 43 3H-5HT -478 13 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
240 929 39 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 929 39 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 929 39 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 929 39 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 929 39 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 929 39 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 929 39 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2105 2993 34 3H-LSD -28 33 Human 7.9 pKi = 7.9 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-LSD -28 33 Human 7.9 pKi = 7.9 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-LSD -28 33 Human 7.9 pKi = 7.9 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-LSD -28 33 Human 7.9 pKi = 7.9 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-LSD -28 33 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
138107169 214163 0 3H-5HT -33 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 214163 0 3H-5HT -33 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
186 1769 47 3H-LSD -575 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1769 47 3H-LSD -575 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1769 47 3H-LSD -575 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
1353 1872 85 3H-5HT -295 86 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 3H-5HT -295 86 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 3H-5HT -295 86 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 3H-5HT -295 86 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 3H-5HT -295 86 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 214151 0 3H-5HT -2398 21 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
1809 134 28 3H-5HT -1659 37 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-5HT -1659 37 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-5HT -1659 37 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
124 2921 44 3H-5HT -181 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2921 44 3H-5HT -181 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2921 44 3H-5HT -181 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2921 44 3H-5HT -181 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2921 44 3H-5HT -181 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
15897 2807 0 3H-LSD 12 37 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2807 0 3H-LSD 12 37 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2807 0 3H-LSD 12 37 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
138107169 214163 0 3H-5HT -33 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 214163 0 3H-5HT -33 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
None 214151 0 3H-LSD -407 21 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
1809 134 28 Functional -999 37 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 Functional -999 37 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 Functional -999 37 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
221 3422 63 UNDEFINED 4 14 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 3422 63 UNDEFINED 4 14 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 3422 63 UNDEFINED 4 14 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
6446436 214696 0 3H-MESULERGINE -1 2 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 3 4 3.2 CC1=CC2=C(C=C1)C(C3=C2N(C=C3)CC(C)N)(C)C.C(=CC(=O)O)C(=O)O None
134 2468 19 Functional -2 68 Human 6.8 pKi = 6.8 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 Functional -2 68 Human 6.8 pKi = 6.8 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 Functional -2 68 Human 6.8 pKi = 6.8 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 Functional -2 68 Human 6.8 pKi = 6.8 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 Functional -2 68 Human 6.8 pKi = 6.8 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
1614 201951 22 Functional 2 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
CHEMBL6731 201951 22 Functional 2 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
1809 134 28 3H-5HT -1659 37 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-5HT -1659 37 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-5HT -1659 37 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
107992 2506 47 3H-MESULERGINE -1 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 2506 47 3H-MESULERGINE -1 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 2506 47 3H-MESULERGINE -1 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 2506 47 3H-MESULERGINE -1 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
28 3427 37 3H-5HT -954 10 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3292447 3427 37 3H-5HT -954 10 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL20963 3427 37 3H-5HT -954 10 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
2470 3583 46 3H-5HT -14125 60 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-5HT -14125 60 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-5HT -14125 60 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-5HT -14125 60 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-5HT -14125 60 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2389 3267 114 3H-LSD -79 68 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 3H-LSD -79 68 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 3H-LSD -79 68 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 3H-LSD -79 68 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 3H-LSD -79 68 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
107 141 116 3H-5HT -4 31 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-5HT -4 31 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-5HT -4 31 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
None 214158 0 3H-5HT -12 24 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
None 215723 0 UNDEFINED -12 3 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 432 3 2 4 3.8 C1CC2=C(CC1CN3CC4CC3CN4C5=CC=CC6=C5OC(=O)N6)C7=C(N2)C=CC(=C7)F None
105432 214244 0 3H-5HT -30 4 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 240 5 1 5 1.5 CC(CC1=CC(=C(C=C1OC)[N+](=O)[O-])OC)N None
18971832 2375 0 3H-5HT -263 13 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
21 2375 0 3H-5HT -263 13 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
CHEMBL3186179 2375 0 3H-5HT -263 13 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
37459 733 10 3H-KETANSERIN -39 25 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 733 10 3H-KETANSERIN -39 25 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 733 10 3H-KETANSERIN -39 25 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
None 214158 0 3H-5HT -12 24 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
5268 3586 34 3H-RAUWOLSCINE -1047 18 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3586 34 3H-RAUWOLSCINE -1047 18 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3586 34 3H-RAUWOLSCINE -1047 18 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
173 3199 88 Functional 1 23 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3199 88 Functional 1 23 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3199 88 Functional 1 23 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
1353 1872 85 3H-5HT -295 86 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 3H-5HT -295 86 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 3H-5HT -295 86 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 3H-5HT -295 86 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 3H-5HT -295 86 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
119607 214637 0 3H-LSD 97 28 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 CC1=C(C(=NO1)C2=CC=CC=C2)C3=CC=C(C=C3)S(=O)(=O)N None
1809 134 28 3H-5HT -999 37 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-5HT -999 37 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-5HT -999 37 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
31016 101804 12 3H-5HT -11 5 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 225 5 1 4 1.6 COc1cc(CC(C)N)cc(OC)c1OC None
CHEMBL30336 101804 12 3H-5HT -11 5 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 225 5 1 4 1.6 COc1cc(CC(C)N)cc(OC)c1OC None
213 3780 50 3H-LSD -5 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3780 50 3H-LSD -5 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3780 50 3H-LSD -5 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3780 50 3H-LSD -5 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3780 50 3H-LSD -5 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5 139 66 3H-5HT -13 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -13 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -13 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -13 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
134 2468 19 3H-LSD -2 68 Human 7.7 pKi = 7.7 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 3H-LSD -2 68 Human 7.7 pKi = 7.7 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 3H-LSD -2 68 Human 7.7 pKi = 7.7 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 3H-LSD -2 68 Human 7.7 pKi = 7.7 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 3H-LSD -2 68 Human 7.7 pKi = 7.7 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
11957541 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
7153 97557 74 3H-LSD -1 34 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-LSD -1 34 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
135 2486 38 3H-5HT -3 58 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 3H-5HT -3 58 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 3H-5HT -3 58 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 3H-5HT -3 58 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 3H-5HT -3 58 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
3652 4022 72 3H-5HT -2 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4022 72 3H-5HT -2 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4022 72 3H-5HT -2 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4022 72 3H-5HT -2 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4022 72 3H-5HT -2 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
5268 3586 34 3H-5HT -616 18 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3586 34 3H-5HT -616 18 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3586 34 3H-5HT -616 18 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
1574 81 52 3H-5HT -2 21 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 52 3H-5HT -2 21 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 52 3H-5HT -2 21 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
135 2486 38 3H-5HT -37 58 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 3H-5HT -37 58 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 3H-5HT -37 58 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 3H-5HT -37 58 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 3H-5HT -37 58 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1150 3805 116 125I-DOI -8 25 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
1150 3805 116 3H-5HT -8 25 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3805 116 125I-DOI -8 25 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3805 116 3H-5HT -8 25 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3805 116 125I-DOI -8 25 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3805 116 3H-5HT -8 25 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3805 116 125I-DOI -8 25 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3805 116 3H-5HT -8 25 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
152 361 18 Functional 1 19 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 361 18 Functional 1 19 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 361 18 Functional 1 19 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
5 139 66 Functional -13 55 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 Functional -13 55 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 Functional -13 55 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 Functional -13 55 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
4106 2456 16 3H-5HT -3 34 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2456 16 3H-5HT -3 34 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2456 16 3H-5HT -3 34 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2456 16 3H-5HT -3 34 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5074 3268 75 3H-5HT -3 30 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3268 75 3H-5HT -3 30 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3268 75 3H-5HT -3 30 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3268 75 3H-5HT -3 30 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
None 214271 0 3H-LSD -2 8 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 339 4 3 3 1.9 CCC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
133 2450 48 3H-KETANSERIN -4 43 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2450 48 3H-KETANSERIN -4 43 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2450 48 3H-KETANSERIN -4 43 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2450 48 3H-KETANSERIN -4 43 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2450 48 3H-KETANSERIN -4 43 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1524 2141 89 3H-KETANSERIN -1 52 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-KETANSERIN -1 52 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-KETANSERIN -1 52 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-KETANSERIN -1 52 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-KETANSERIN -1 52 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-KETANSERIN -1 52 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
None 214620 0 3H-5HT 5 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 342 4 3 4 2.5 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N.C(=CC(=O)O)C(=O)O None
191 3429 47 3H-5HT -1 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 None
443389 3429 47 3H-5HT -1 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 None
CHEMBL276140 3429 47 3H-5HT -1 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 None
None 214619 0 3H-5HT -2 11 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 243 3 1 4 2.7 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N None
135409468 1996 63 3H-LSD 1 40 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 1996 63 3H-LSD 1 40 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 1996 63 3H-LSD 1 40 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
5 139 66 3H-MESULERGINE -13 55 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-MESULERGINE -13 55 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-MESULERGINE -13 55 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-MESULERGINE -13 55 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
155 718 20 Functional -5 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
163 718 20 Functional -5 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
62065 718 20 Functional -5 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
CHEMBL6607 718 20 Functional -5 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
DB01484 718 20 Functional -5 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
1588 2284 24 3H-LSD -8 44 Human 8.5 pKi = 8.5 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-LSD -8 44 Human 8.5 pKi = 8.5 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-LSD -8 44 Human 8.5 pKi = 8.5 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-LSD -8 44 Human 8.5 pKi = 8.5 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-LSD -8 44 Human 8.5 pKi = 8.5 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
None 214516 0 3H-LSD -32 12 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 426 6 0 6 3.4 C1CCC2C(C1)C(=O)N(C2=O)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54 None
11957541 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
11957541 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1425 38 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1615 167217 22 Functional -2 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167217 22 Functional -2 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
2389 3267 114 3H-5HT -660 68 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 3H-5HT -660 68 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 3H-5HT -660 68 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 3H-5HT -660 68 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 3H-5HT -660 68 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1524 2141 89 125I-DOI -158 52 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 125I-DOI -158 52 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 125I-DOI -158 52 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 125I-DOI -158 52 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 125I-DOI -158 52 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 125I-DOI -158 52 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
189 3423 31 3H-LSD -5 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
5163 3423 31 3H-LSD -5 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
CHEMBL297784 3423 31 3H-LSD -5 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
155 718 20 3H-5HT -10 13 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
163 718 20 3H-5HT -10 13 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
62065 718 20 3H-5HT -10 13 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
CHEMBL6607 718 20 3H-5HT -10 13 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
DB01484 718 20 3H-5HT -10 13 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
202 1475 0 3H-5HT -1 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1475 0 3H-5HT -1 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1475 0 3H-5HT -1 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1475 0 3H-5HT -1 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1475 0 3H-5HT -1 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
2477 732 54 3H-5HT -13 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 732 54 3H-5HT -13 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 732 54 3H-5HT -13 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 732 54 3H-5HT -13 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 732 54 3H-5HT -13 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
1524 2141 89 3H-RAUWOLSCINE -234 52 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-RAUWOLSCINE -234 52 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-RAUWOLSCINE -234 52 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-RAUWOLSCINE -234 52 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-RAUWOLSCINE -234 52 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-RAUWOLSCINE -234 52 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2176 3065 66 3H-5HT -933 27 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3065 66 3H-5HT -933 27 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3065 66 3H-5HT -933 27 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3065 66 3H-5HT -933 27 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3065 66 3H-5HT -933 27 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
277 1269 55 125I-DOI -26 46 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1269 55 125I-DOI -26 46 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1269 55 125I-DOI -26 46 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1269 55 125I-DOI -26 46 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1269 55 125I-DOI -26 46 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
189 3423 31 3H-5HT -5 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
5163 3423 31 3H-5HT -5 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
CHEMBL297784 3423 31 3H-5HT -5 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
1220 186 46 3H-5HT -1905 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 186 46 3H-5HT -1905 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 186 46 3H-5HT -1905 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 186 46 3H-5HT -1905 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
6917970 3622 54 3H-LSD -51 34 Human 6.7 pKi = 6.7 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 3H-LSD -51 34 Human 6.7 pKi = 6.7 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 3H-LSD -51 34 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
1524 2141 89 3H-MESULERGINE -234 52 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-MESULERGINE -234 52 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-MESULERGINE -234 52 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-MESULERGINE -234 52 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-MESULERGINE -234 52 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-MESULERGINE -234 52 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
104911 214239 0 3H-LSD -99 38 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
105432 214244 0 3H-5HT -44 4 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 240 5 1 5 1.5 CC(CC1=CC(=C(C=C1OC)[N+](=O)[O-])OC)N None
1150 3805 116 3H-5HT -2 25 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3805 116 3H-5HT -2 25 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3805 116 3H-5HT -2 25 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3805 116 3H-5HT -2 25 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
7153 97557 74 3H-5HT -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-5HT -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
7153 97557 74 UNDEFINED -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 UNDEFINED -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
None 214693 0 UNDEFINED -1 28 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
198 310 120 3H-MESULERGINE -346 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
82148 310 120 3H-MESULERGINE -346 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
99 310 120 3H-MESULERGINE -346 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
CHEMBL10878 310 120 3H-MESULERGINE -346 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
DB06594 310 120 3H-MESULERGINE -346 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
None 214158 0 Functional -33 24 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
11957541 1425 38 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1425 38 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1425 38 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1425 38 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1425 38 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
7153 97557 74 3H-5HT -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-5HT -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
6166 214243 0 3H-5HT -7 4 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 330 2 1 3 3.7 C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2C(=O)CO)CCC4=CC(=O)CC[C@]34C None
155 718 20 3H-5HT -5 13 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
163 718 20 3H-5HT -5 13 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
62065 718 20 3H-5HT -5 13 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
CHEMBL6607 718 20 3H-5HT -5 13 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
DB01484 718 20 3H-5HT -5 13 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
7153 97557 74 3H-5HT -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-5HT -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
57174031 214153 0 3H-KETANSERIN -457 20 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
185 3931 54 3H-LSD -2344 38 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3931 54 3H-LSD -2344 38 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3931 54 3H-LSD -2344 38 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3931 54 3H-LSD -2344 38 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
3294 1967 106 3H-LSD -38 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1967 106 3H-LSD -38 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1967 106 3H-LSD -38 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1967 106 3H-LSD -38 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1967 106 3H-LSD -38 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
3337 214431 0 3H-LSD -75 41 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 3H-LSD -75 41 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 3H-LSD -75 41 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 3H-LSD -75 41 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
2865 4064 67 3H-5HT -12 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4064 67 3H-5HT -12 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4064 67 3H-5HT -12 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4064 67 3H-5HT -12 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4064 67 3H-5HT -12 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
11957541 1425 38 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1425 38 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1425 38 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1425 38 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1425 38 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
5 139 66 3H-5HT -29 55 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -29 55 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -29 55 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -29 55 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
11957541 1425 38 3H-5HT -2 16 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1425 38 3H-5HT -2 16 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1425 38 3H-5HT -2 16 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1425 38 3H-5HT -2 16 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1425 38 3H-5HT -2 16 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
7153 97557 74 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
7153 97557 74 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
138107169 214163 0 3H-5HT -33 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 214163 0 3H-5HT -33 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
1574 81 52 3H-5HT -3 21 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 52 3H-5HT -3 21 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 52 3H-5HT -3 21 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
1574 81 52 3H-5HT -3 21 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 52 3H-5HT -3 21 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 52 3H-5HT -3 21 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
115 3720 78 Functional -1 27 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3720 78 Functional -1 27 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3720 78 Functional -1 27 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
2389 3267 114 3H-5HT -79 68 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 3H-5HT -79 68 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 3H-5HT -79 68 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 3H-5HT -79 68 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 3H-5HT -79 68 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1150 3805 116 Functional -2 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3805 116 Functional -2 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3805 116 Functional -2 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3805 116 Functional -2 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
107992 2506 47 Functional -1 10 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 2506 47 Functional -1 10 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 2506 47 Functional -1 10 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 2506 47 Functional -1 10 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
11954224 214164 0 3H-5HT -66 60 Human 8.5 pKi = 8.5 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
None 214693 0 3H-MESULERGINE 1 28 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
7153 97557 74 3H-5HT -1 34 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-5HT -1 34 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1342 36 42 3H-5HT 2 19 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 42 3H-5HT 2 19 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 42 3H-5HT 2 19 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
206 2447 10 3H-5HT -1 25 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2447 10 3H-5HT -1 25 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2447 10 3H-5HT -1 25 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
135398737 942 89 3H-RAUWOLSCINE -2 92 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 3H-RAUWOLSCINE -2 92 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 3H-RAUWOLSCINE -2 92 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 3H-RAUWOLSCINE -2 92 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 3H-RAUWOLSCINE -2 92 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
206 2447 10 3H-5HT -1 25 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2447 10 3H-5HT -1 25 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2447 10 3H-5HT -1 25 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
242 467 117 3H-LSD -1 52 Human 8.5 pKi = 8.5 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-LSD -1 52 Human 8.5 pKi = 8.5 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-LSD -1 52 Human 8.5 pKi = 8.5 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-LSD -1 52 Human 8.5 pKi = 8.5 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-LSD -1 52 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
11954224 214164 0 3H-5HT -66 60 Human 8.5 pKi = 8.5 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
206 2447 10 3H-5HT -1 25 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2447 10 3H-5HT -1 25 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2447 10 3H-5HT -1 25 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
5074 3268 75 125I-DOI -6 30 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3268 75 125I-DOI -6 30 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3268 75 125I-DOI -6 30 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3268 75 125I-DOI -6 30 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
1342 36 42 3H-5HT 2 19 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 42 3H-5HT 2 19 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 42 3H-5HT 2 19 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1621 2386 16 3H-LSD -19 45 Human 8.4 pKi = 8.4 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 3H-LSD -19 45 Human 8.4 pKi = 8.4 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 3H-LSD -19 45 Human 8.4 pKi = 8.4 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 3H-LSD -19 45 Human 8.4 pKi = 8.4 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 3H-LSD -19 45 Human 8.4 pKi = 8.4 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
1342 36 42 3H-5HT 2 19 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 42 3H-5HT 2 19 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 42 3H-5HT 2 19 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1621 2386 16 3H-LSD -39 45 Rat 7.5 pKi = 7.5 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 3H-LSD -39 45 Rat 7.5 pKi = 7.5 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 3H-LSD -39 45 Rat 7.5 pKi = 7.5 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 3H-LSD -39 45 Rat 7.5 pKi = 7.5 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 3H-LSD -39 45 Rat 7.5 pKi = 7.5 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
None 214151 0 Functional -407 21 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
6971132 214225 0 3H-LSD -7 14 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
219050 3309 21 3H-MESULERGINE -194 21 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
52 3309 21 3H-MESULERGINE -194 21 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
CHEMBL431367 3309 21 3H-MESULERGINE -194 21 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
2470 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2 3198 19 3H-5HT -363 29 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3198 19 3H-5HT -363 29 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3198 19 3H-5HT -363 29 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
186 1769 47 3H-5HT -575 17 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1769 47 3H-5HT -575 17 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1769 47 3H-5HT -575 17 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
31016 101804 12 3H-5HT -5 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 225 5 1 4 1.6 COc1cc(CC(C)N)cc(OC)c1OC None
CHEMBL30336 101804 12 3H-5HT -5 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 225 5 1 4 1.6 COc1cc(CC(C)N)cc(OC)c1OC None
135398737 942 89 3H-5HT -36 92 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 3H-5HT -36 92 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 3H-5HT -36 92 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 3H-5HT -36 92 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 3H-5HT -36 92 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
102 4051 44 3H-5HT -93 50 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 3H-5HT -93 50 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 3H-5HT -93 50 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 3H-5HT -93 50 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 3H-5HT -93 50 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
7153 97557 74 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
None 214158 0 3H-5HT -33 24 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
6166 214243 0 3H-5HT -4 4 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 330 2 1 3 3.7 C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2C(=O)CO)CCC4=CC(=O)CC[C@]34C None
1574 81 52 3H-5HT -3 21 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 52 3H-5HT -3 21 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 52 3H-5HT -3 21 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
130 3431 43 35S-GTPGammaS -478 13 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3378093 3431 43 35S-GTPGammaS -478 13 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL281350 3431 43 35S-GTPGammaS -478 13 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
2470 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1524 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2470 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 3583 46 3H-RAUWOLSCINE -14125 60 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-RAUWOLSCINE -14125 60 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-RAUWOLSCINE -14125 60 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-RAUWOLSCINE -14125 60 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-RAUWOLSCINE -14125 60 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
7153 97557 74 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1524 2141 89 3H-5HT -234 52 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-5HT -234 52 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-5HT -234 52 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-5HT -234 52 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-5HT -234 52 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-5HT -234 52 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2470 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
15760 112567 55 3H-5HT -5 2 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 174 2 2 1 2.0 Cc1ccc2[nH]cc(CCN)c2c1 None
CHEMBL331241 112567 55 3H-5HT -5 2 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 174 2 2 1 2.0 Cc1ccc2[nH]cc(CCN)c2c1 None
None 214151 0 3H-LSD -407 21 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
186 1769 47 3H-5HT -575 17 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1769 47 3H-5HT -575 17 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1769 47 3H-5HT -575 17 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
2470 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
138107169 214163 0 3H-5HT -117 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 214163 0 3H-5HT -117 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
138107169 214163 0 3H-5HT -117 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 214163 0 3H-5HT -117 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
206 2447 10 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2447 10 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2447 10 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
1524 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-5HT -2754 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
206 2447 10 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2447 10 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2447 10 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
7153 97557 74 3H-5HT -1 34 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-5HT -1 34 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1353 1872 85 3H-5HT -295 86 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 3H-5HT -295 86 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 3H-5HT -295 86 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 3H-5HT -295 86 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 3H-5HT -295 86 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1524 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2141 89 3H-KETANSERIN -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-KETANSERIN -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-KETANSERIN -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-KETANSERIN -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-KETANSERIN -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-KETANSERIN -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2220 3073 78 3H-5HT -10 14 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
27400 3073 78 3H-5HT -10 14 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
93 3073 78 3H-5HT -10 14 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
CHEMBL294951 3073 78 3H-5HT -10 14 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
DB06153 3073 78 3H-5HT -10 14 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
77158 18842 48 3H-5HT -2 2 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 None
CHEMBL1288717 18842 48 3H-5HT -2 2 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 None
2402 3306 58 3H-MESULERGINE -9 25 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3306 58 3H-MESULERGINE -9 25 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3306 58 3H-MESULERGINE -9 25 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3306 58 3H-MESULERGINE -9 25 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3306 58 3H-MESULERGINE -9 25 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
145 140 48 3H-LSD -87 30 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 48 3H-LSD -87 30 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 48 3H-LSD -87 30 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 48 3H-LSD -87 30 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
77158 18842 48 3H-5HT -2 2 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 None
CHEMBL1288717 18842 48 3H-5HT -2 2 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 None
206 2447 10 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2447 10 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2447 10 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
138107169 214163 0 3H-5HT -117 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 214163 0 3H-5HT -117 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
115 3720 78 3H-5HT -1 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3720 78 3H-5HT -1 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3720 78 3H-5HT -1 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
3337 214431 0 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
1524 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-5HT -234 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
102 4051 44 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
102 4051 44 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
1524 2141 89 3H-5HT -2754 52 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-5HT -2754 52 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-5HT -2754 52 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-5HT -2754 52 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-5HT -2754 52 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-5HT -2754 52 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
5 139 66 3H-5HT -13 55 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -13 55 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -13 55 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -13 55 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
135398737 942 89 3H-LSD -2 92 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 3H-LSD -2 92 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 3H-LSD -2 92 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 3H-LSD -2 92 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 3H-LSD -2 92 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
138107169 214163 0 3H-RAUWOLSCINE -33 23 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 214163 0 3H-RAUWOLSCINE -33 23 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
135 2486 38 3H-5HT -3 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 3H-5HT -3 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 3H-5HT -3 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 3H-5HT -3 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 3H-5HT -3 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2865 4064 67 3H-LSD -12 54 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4064 67 3H-LSD -12 54 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4064 67 3H-LSD -12 54 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4064 67 3H-LSD -12 54 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4064 67 3H-LSD -12 54 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1342 36 42 3H-5HT -4 19 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 42 3H-5HT -4 19 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 42 3H-5HT -4 19 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3117 206096 100 None -8 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 206096 100 None -8 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
104903 56035 14 None -4 6 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 None
CHEMBL1630578 56035 14 None -4 6 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 None
7153 97557 74 3H-5HT -1 34 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-5HT -1 34 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
102 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
7153 97557 74 3H-5HT -1 34 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-5HT -1 34 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
164 1427 17 3H-KETANSERIN -17 10 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
85875 1427 17 3H-KETANSERIN -17 10 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
CHEMBL8600 1427 17 3H-KETANSERIN -17 10 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
DB01528 1427 17 3H-KETANSERIN -17 10 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
3337 214431 0 Functional -75 41 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 Functional -75 41 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 Functional -75 41 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 Functional -75 41 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
None 215720 0 UNDEFINED -83 3 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 449 6 3 4 4.1 C1CC2=C(CC1CCCNCC3COC4=C(O3)C=CC5=C4CC(=O)N5)NC6=C2C=C(C=C6)F None
107992 2506 47 3H-5HT -5 10 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 2506 47 3H-5HT -5 10 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 2506 47 3H-5HT -5 10 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 2506 47 3H-5HT -5 10 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
1220 186 46 3H-5HT -1905 45 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 186 46 3H-5HT -1905 45 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 186 46 3H-5HT -1905 45 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 186 46 3H-5HT -1905 45 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
11848624 88702 0 UNDEFINED 2 6 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
CHEMBL236587 88702 0 UNDEFINED 2 6 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
2389 3267 114 3H-LSD -79 68 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 3H-LSD -79 68 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 3H-LSD -79 68 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 3H-LSD -79 68 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 3H-LSD -79 68 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1220 186 46 3H-5HT -3235 45 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 186 46 3H-5HT -3235 45 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 186 46 3H-5HT -3235 45 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 186 46 3H-5HT -3235 45 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
3337 214431 0 3H-5HT -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
3337 214431 0 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 3H-5HT -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 3H-5HT -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 3H-5HT -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
1210 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1213 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2725 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
33036 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4411 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
616 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6976 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
716121 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
90475904 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 903 45 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
102 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
155 718 20 3H-5HT -5 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
163 718 20 3H-5HT -5 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
62065 718 20 3H-5HT -5 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
CHEMBL6607 718 20 3H-5HT -5 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
DB01484 718 20 3H-5HT -5 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
102 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
11954224 214164 0 3H-LSD -66 60 Human 7.4 pKi = 7.4 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
11291 3157 23 3H-KETANSERIN -44 5 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C None
4980 3157 23 3H-KETANSERIN -44 5 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C None
CHEMBL65547 3157 23 3H-KETANSERIN -44 5 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C None
None 214693 0 3H-5HT 1 28 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
173 3199 88 3H-KETANSERIN -5 23 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3199 88 3H-KETANSERIN -5 23 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3199 88 3H-KETANSERIN -5 23 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
2181 3067 0 3H-5HT -15 35 Human 7.3 pKi = 7.3 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 3H-5HT -15 35 Human 7.3 pKi = 7.3 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 3H-5HT -15 35 Human 7.3 pKi = 7.3 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 3H-5HT -15 35 Human 7.3 pKi = 7.3 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 3H-5HT -15 35 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
15897 2807 0 3H-5-HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
15897 2807 0 3H-5HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2807 0 3H-5-HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2807 0 3H-5HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2807 0 3H-5-HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2807 0 3H-5HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
186 1769 47 3H-5HT -1047 17 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1769 47 3H-5HT -1047 17 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1769 47 3H-5HT -1047 17 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
5268 3586 34 3H-5HT -1047 18 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3586 34 3H-5HT -1047 18 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3586 34 3H-5HT -1047 18 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
15897 2807 0 3H-LSD 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2807 0 3H-LSD 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2807 0 3H-LSD 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
173 3199 88 3H-5HT 1 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3199 88 3H-5HT 1 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3199 88 3H-5HT 1 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
11653679 180599 1 UNDEFINED -75 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476108 180599 1 UNDEFINED -75 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
10836 14314 13 None -3 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
CHEMBL1201201 14314 13 None -3 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
5475158 66862 20 3H-KETANSERIN -1 14 Bovine 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
CHEMBL18786 66862 20 3H-KETANSERIN -1 14 Bovine 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
5074 3268 75 3H-5HT -3 30 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
5074 3268 75 3H-5HT -9 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3268 75 3H-5HT -3 30 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3268 75 3H-5HT -9 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3268 75 3H-5HT -3 30 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3268 75 3H-5HT -9 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3268 75 3H-5HT -3 30 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3268 75 3H-5HT -9 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
5870 31430 85 None - 1 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 270 0 1 2 3.8 C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O None
CHEMBL1405 31430 85 None - 1 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 270 0 1 2 3.8 C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O None
None 214620 0 3H-5HT 5 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 342 4 3 4 2.5 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N.C(=CC(=O)O)C(=O)O None
5074 3268 75 3H-5HT -9 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3268 75 3H-5HT -9 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3268 75 3H-5HT -9 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3268 75 3H-5HT -9 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
2812 4696 96 None -40 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4696 96 None -40 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
222757 98904 70 None -1 3 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O None
CHEMBL282575 98904 70 None -1 3 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O None
1210 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1213 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2725 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
33036 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4411 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
616 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6976 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
716121 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
90475904 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 903 45 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
5074 3268 75 3H-5HT -9 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3268 75 3H-5HT -9 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3268 75 3H-5HT -9 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3268 75 3H-5HT -9 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
1357 2440 133 None -3890 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 None -3890 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 None -3890 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 None -3890 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 None -3890 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 None -3890 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1342 36 42 3H-5HT -4 19 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 42 3H-5HT -4 19 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 42 3H-5HT -4 19 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1209 1620 69 None -199 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 -199 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 -199 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 -199 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 -199 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
3198 203792 73 None -30 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 203792 73 None -30 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 203792 73 None -30 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
2406 99925 84 None -27 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O None
CHEMBL290106 99925 84 None -27 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O None
None 214620 0 3H-5HT 5 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 342 4 3 4 2.5 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N.C(=CC(=O)O)C(=O)O None
66265 93566 12 None -1 19 Human 8.3 pKi = 8.3 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 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
1836 2544 56 None -69 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
3340 2544 56 None -69 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
5281040 2544 56 None -69 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
CHEMBL787 2544 56 None -69 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
DB00471 2544 56 None -69 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
2402 3306 58 None -9 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3306 58 None -9 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3306 58 None -9 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3306 58 None -9 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3306 58 None -9 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
3598 187228 73 None -2 7 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl None
CHEMBL496 187228 73 None -2 7 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl None
135 2486 38 3H-RAUWOLSCINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 3H-RAUWOLSCINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 3H-RAUWOLSCINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 3H-RAUWOLSCINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 3H-RAUWOLSCINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4189 205185 91 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 205185 91 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 205185 91 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
4943 192804 100 None 1 2 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 178 2 1 1 3.6 CC(C)c1cccc(C(C)C)c1O None
CHEMBL526 192804 100 None 1 2 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 178 2 1 1 3.6 CC(C)c1cccc(C(C)C)c1O None
3336 94547 27 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 None
CHEMBL1405922 94547 27 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 None
CHEMBL254832 94547 27 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 None
135 2486 38 3H-MESULERGINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 3H-MESULERGINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 3H-MESULERGINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 3H-MESULERGINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 3H-MESULERGINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
189 3423 31 3H-MESULERGINE -5 18 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
5163 3423 31 3H-MESULERGINE -5 18 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
CHEMBL297784 3423 31 3H-MESULERGINE -5 18 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
4211 57502 81 None -2 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 None
CHEMBL1670 57502 81 None -2 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 None
5353853 17788 41 None -23 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
9556529 17788 41 None -23 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1262 17788 41 None -23 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
1599 2299 47 None -144 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
3955 2299 47 None -144 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
7215 2299 47 None -144 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
CHEMBL841 2299 47 None -144 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
DB00836 2299 47 None -144 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
4209 3102 71 None -758 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3102 71 None -758 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3102 71 None -758 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3102 71 None -758 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3102 71 None -758 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3102 71 None -758 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
2142 3035 54 None -43 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3035 54 None -43 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3035 54 None -43 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3035 54 None -43 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3035 54 None -43 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3035 54 None -43 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
146 135 80 3H-5HT 1 3 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 None
164682 135 80 3H-5HT 1 3 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 None
CHEMBL275628 135 80 3H-5HT 1 3 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 None
68617 203806 60 None -15 26 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 203806 60 None -15 26 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 203806 60 None -15 26 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
4601 205010 29 None -4 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 205010 29 None -4 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 205010 29 None -4 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
448537 159691 86 None -21 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
CHEMBL411 159691 86 None -21 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
2176 3065 66 None -933 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3065 66 None -933 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3065 66 None -933 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3065 66 None -933 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3065 66 None -933 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
1531 2226 64 None -16 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
3869 2226 64 None -16 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
7207 2226 64 None -16 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
CHEMBL429 2226 64 None -16 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
DB00598 2226 64 None -16 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
5318 15385 44 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1200348 15385 44 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1221 15385 44 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
119607 214637 0 None 97 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 3 1 4 3.0 CC1=C(C(=NO1)C2=CC=CC=C2)C3=CC=C(C=C3)S(=O)(=O)N None
1227 2444 35 None -112 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2444 35 None -112 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2444 35 None -112 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2444 35 None -112 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2444 35 None -112 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2444 35 None -112 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3151 1429 93 None -125 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
945 1429 93 None -125 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
965 1429 93 None -125 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
CHEMBL219916 1429 93 None -125 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
DB01184 1429 93 None -125 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
1343 1850 55 None -14 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
3519 1850 55 None -14 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
522 1850 55 None -14 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
CHEMBL862 1850 55 None -14 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
DB01018 1850 55 None -14 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
1016 3678 75 None -17 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3678 75 None -17 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3678 75 None -17 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3678 75 None -17 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3678 75 None -17 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3678 75 None -17 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5510 204127 97 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 2 0 2 4.9 Cc1cccc(N(C)C(=S)Oc2ccc3ccccc3c2)c1 None
CHEMBL83668 204127 97 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 2 0 2 4.9 Cc1cccc(N(C)C(=S)Oc2ccc3ccccc3c2)c1 None
2202 3071 91 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3071 91 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3071 91 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3071 91 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3071 91 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
2723 153500 104 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl None
CHEMBL398440 153500 104 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl None
2771 193337 67 None 1 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 193337 67 None 1 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 193337 67 None 1 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
2333 141791 91 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 None
CHEMBL388590 141791 91 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 None
135 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2470 3583 46 125I-DOI -1513 60 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 125I-DOI -1513 60 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 125I-DOI -1513 60 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 125I-DOI -1513 60 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 125I-DOI -1513 60 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
102 4051 44 3H-5HT -93 50 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
102 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 3H-5HT -93 50 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 3H-5HT -93 50 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 3H-5HT -93 50 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 3H-5HT -93 50 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
135 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
221 3422 63 UNDEFINED 4 14 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 3422 63 UNDEFINED 4 14 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 3422 63 UNDEFINED 4 14 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
102 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
1615 167217 22 3H-LSD -2 45 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167217 22 3H-LSD -2 45 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
122 1404 9 3H-5HT -100 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
156314 1404 9 3H-5HT -100 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL1332062 1404 9 3H-5HT -100 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
1209 1620 69 3H-5HT -199 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1620 69 3H-5HT -199 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1620 69 3H-5HT -199 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1620 69 3H-5HT -199 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1620 69 3H-5HT -199 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
5268 3586 34 3H-5HT -1047 18 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3586 34 3H-5HT -1047 18 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3586 34 3H-5HT -1047 18 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
208 2810 0 3H-5HT -69 13 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
4541 2810 0 3H-5HT -69 13 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL1494 2810 0 3H-5HT -69 13 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3337 214431 0 3H-5-HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
3337 214431 0 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 3H-5-HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 3H-5-HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 3H-5-HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
221 3422 63 3H-MESULERGINE -4 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 3422 63 3H-MESULERGINE -4 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 3422 63 3H-MESULERGINE -4 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3337 214431 0 3H-LSD -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 3H-LSD -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 3H-LSD -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 3H-LSD -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
108182 4055 18 3H-5HT -1 17 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 4055 18 3H-5HT -1 17 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 4055 18 3H-5HT -1 17 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
15897 2807 0 3H-LSD 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2807 0 3H-LSD 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2807 0 3H-LSD 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
15897 2807 0 3H-5HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2807 0 3H-5HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2807 0 3H-5HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
135 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
135 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
None 214245 0 3H-5HT -5 4 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2105 2993 34 Functional -28 33 Human 7.3 pKi = 7.3 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 Functional -28 33 Human 7.3 pKi = 7.3 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 Functional -28 33 Human 7.3 pKi = 7.3 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 Functional -28 33 Human 7.3 pKi = 7.3 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 Functional -28 33 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
102 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
135398745 2858 108 3H-5HT -27 66 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 3H-5HT -27 66 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 3H-5HT -27 66 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 3H-5HT -27 66 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
11957541 1425 38 3H-5HT -2 16 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1425 38 3H-5HT -2 16 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1425 38 3H-5HT -2 16 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1425 38 3H-5HT -2 16 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1425 38 3H-5HT -2 16 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
102 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
542051 204370 4 3H-5HT -61 7 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 237 6 1 3 2.5 CCCc1cc(OC)c(CC(C)N)cc1OC None
CHEMBL8569 204370 4 3H-5HT -61 7 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 237 6 1 3 2.5 CCCc1cc(OC)c(CC(C)N)cc1OC None
1220 186 46 3H-KETANSERIN -4265 45 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 186 46 3H-KETANSERIN -4265 45 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 186 46 3H-KETANSERIN -4265 45 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 186 46 3H-KETANSERIN -4265 45 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
3337 214431 0 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
11957541 1425 38 3H-KETANSERIN -17 16 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1425 38 3H-KETANSERIN -17 16 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1425 38 3H-KETANSERIN -17 16 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1425 38 3H-KETANSERIN -17 16 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1425 38 3H-KETANSERIN -17 16 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
141 1394 32 3H-KETANSERIN -6 22 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1394 32 3H-KETANSERIN -6 22 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1394 32 3H-KETANSERIN -6 22 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1394 32 3H-KETANSERIN -6 22 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
31101 719 39 3H-MESULERGINE -26 36 Human 7.3 pKi = 7.3 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-MESULERGINE -26 36 Human 7.3 pKi = 7.3 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-MESULERGINE -26 36 Human 7.3 pKi = 7.3 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-MESULERGINE -26 36 Human 7.3 pKi = 7.3 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-MESULERGINE -26 36 Human 7.3 pKi = 7.3 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
2181 3067 0 3H-5HT -478 35 Rat 6.2 pKi = 6.2 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 3H-5HT -478 35 Rat 6.2 pKi = 6.2 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 3H-5HT -478 35 Rat 6.2 pKi = 6.2 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 3H-5HT -478 35 Rat 6.2 pKi = 6.2 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 3H-5HT -478 35 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
3337 214431 0 3H-5-HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
3337 214431 0 3H-5HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
3337 214431 0 3H-LSD -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 3H-5-HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 3H-5HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 3H-LSD -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 3H-5-HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 3H-5HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 3H-LSD -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 3H-5-HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 3H-5HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 3H-LSD -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
1357 2440 133 3H-MESULERGINE -3890 9 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 3H-MESULERGINE -3890 9 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 3H-MESULERGINE -3890 9 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 3H-MESULERGINE -3890 9 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 3H-MESULERGINE -3890 9 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 3H-MESULERGINE -3890 9 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
115 3720 78 3H-5HT -1 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3720 78 3H-5HT -1 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3720 78 3H-5HT -1 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
138107169 214163 0 3H-5HT -117 23 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 214163 0 3H-5HT -117 23 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
2470 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
283 3069 47 3H-5HT -562 12 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
4847 3069 47 3H-5HT -562 12 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
CHEMBL18331 3069 47 3H-5HT -562 12 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
2726 904 64 3H-KETANSERIN -3 73 Bovine 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 904 64 3H-KETANSERIN -3 73 Bovine 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 904 64 3H-KETANSERIN -3 73 Bovine 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 904 64 3H-KETANSERIN -3 73 Bovine 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 904 64 3H-KETANSERIN -3 73 Bovine 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
None 215721 0 UNDEFINED -14 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 421 4 3 4 3.3 C1CC2=C(CC1CNCC3COC4=C(O3)C=CC5=C4CC(=O)N5)C6=C(N2)C=CC(=C6)F None
44112 120764 41 None -11 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -11 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 None
1548955 88139 17 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2800 88139 17 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
CHEMBL2355051 88139 17 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
3168 9157 84 None -107 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 9157 84 None -107 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
3042 1381 31 None -39 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 1381 31 None -39 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 1381 31 None -39 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 1381 31 None -39 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 1381 31 None -39 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
5591 156977 84 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 None
CHEMBL408 156977 84 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 None
1353 1872 85 None -295 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 None -295 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 None -295 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 None -295 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 None -295 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
4452 2711 18 3H-LSD -208 19 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 2711 18 3H-LSD -208 19 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 2711 18 3H-LSD -208 19 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
4178 194120 58 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N None
CHEMBL558 194120 58 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N None
1224 1399 79 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1399 79 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1399 79 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1399 79 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1399 79 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1399 79 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
146159245 187856 27 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC None
451415 187856 27 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC None
86289437 187856 27 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC None
CHEMBL502620 187856 27 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC None
12488 1619 51 None -11 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
941361 1619 51 None -11 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
CHEMBL30008 1619 51 None -11 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
DB04841 1619 51 None -11 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
3033538 1287 36 None -12 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
7155 1287 36 None -12 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
781 1287 36 None -12 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
CHEMBL1201216 1287 36 None -12 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
DB00298 1287 36 None -12 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
77379 18841 66 3H-5HT 2 2 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 194 2 2 1 2.3 NCCc1c[nH]c2ccc(Cl)cc12 None
CHEMBL1288716 18841 66 3H-5HT 2 2 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 194 2 2 1 2.3 NCCc1c[nH]c2ccc(Cl)cc12 None
657255 197396 29 None -9 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
CHEMBL588119 197396 29 None -9 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
176 394 63 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
4098 32274 24 None -14 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1255739 32274 24 None -14 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1411979 32274 24 None -14 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
5282379 193304 64 None 1 3 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C\C(=O)O)C(C)(C)CCC1 None
CHEMBL547 193304 64 None 1 3 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C\C(=O)O)C(C)(C)CCC1 None
134 2468 19 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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
2028 2919 77 None -40 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
359 2919 77 None -40 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634 2919 77 None -40 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
CHEMBL1231 2919 77 None -40 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
DB01062 2919 77 None -40 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
134 2468 19 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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
134 2468 19 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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 3H-5HT -12 68 Rat 8.2 pKi = 8.2 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
6437377 214165 0 3H-5HT -5 5 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 500 6 3 7 3.2 CC(C)N1C=C2CC3C(CC(CN3C)C(=O)OC(C)C(C)O)C4=C2C1=CC=C4.C(=CC(=O)O)C(=O)O None
1547484 925 70 None -8 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
654 925 70 None -8 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
9072 925 70 None -8 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL43064 925 70 None -8 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB00568 925 70 None -8 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
4595 176131 102 None 2 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL46 176131 102 None 2 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
1782 2472 81 None -3 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 2472 81 None -3 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 2472 81 None -3 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 2472 81 None -3 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 2472 81 None -3 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
2477 732 54 None -13 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 732 54 None -13 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 732 54 None -13 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 732 54 None -13 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 732 54 None -13 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
5074 3268 75 3H-5HT -3 30 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3268 75 3H-5HT -3 30 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3268 75 3H-5HT -3 30 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3268 75 3H-5HT -3 30 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
6075 149563 36 None -8 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
CHEMBL395110 149563 36 None -8 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
2470 3583 46 None -14125 60 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 None -14125 60 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 None -14125 60 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 None -14125 60 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 None -14125 60 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
198 310 120 None -346 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
82148 310 120 None -346 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
99 310 120 None -346 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
CHEMBL10878 310 120 None -346 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
DB06594 310 120 None -346 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
210 3408 0 None -7 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C None
2423 3408 0 None -7 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C None
5160 3408 0 None -7 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C None
CHEMBL52939 3408 0 None -7 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C None
DB12163 3408 0 None -7 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C None
133 2450 48 3H-5HT -12 43 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2450 48 3H-5HT -12 43 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2450 48 3H-5HT -12 43 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2450 48 3H-5HT -12 43 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2450 48 3H-5HT -12 43 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
6726 1249 46 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
7151 1249 46 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
749 1249 46 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL648 1249 46 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB01176 1249 46 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
3157 1437 69 None -37 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
7170 1437 69 None -37 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
954 1437 69 None -37 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
CHEMBL707 1437 69 None -37 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
DB00590 1437 69 None -37 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
444795 139456 102 None 3 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 None
CHEMBL38 139456 102 None 3 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 None
2284 3121 27 None -16 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3121 27 None -16 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3121 27 None -16 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3121 27 None -16 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3121 27 None -16 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
165193 3126 60 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4011 81982 43 None -20 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 81982 43 None -20 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
3191 102372 93 None -7 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102372 93 None -7 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
1524 2141 89 None -234 52 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 None -234 52 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 None -234 52 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 None -234 52 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 None -234 52 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 None -234 52 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
119584 2547 99 None 1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
1848 2547 99 None 1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
242 2547 99 None 1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
CHEMBL60889 2547 99 None 1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
DB11675 2547 99 None 1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
33630 178369 94 None -6 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178369 94 None -6 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
1605 2300 110 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
3957 2300 110 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
7216 2300 110 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
CHEMBL998 2300 110 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
DB00455 2300 110 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
2895 201889 35 None 1 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
CHEMBL669 201889 35 None 1 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
2801 161313 56 None -3 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL1200710 161313 56 None -3 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL415 161313 56 None -3 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
1222 1626 44 None -52 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1626 44 None -52 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1626 44 None -52 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1626 44 None -52 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1626 44 None -52 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
11658860 2302 47 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 None
2941 2302 47 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 None
4374 2302 47 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 None
CHEMBL360328 2302 47 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 None
DB04871 2302 47 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 None
124 2921 44 None -181 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2921 44 None -181 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2921 44 None -181 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2921 44 None -181 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2921 44 None -181 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
6437377 214165 0 3H-5HT -5 5 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 500 6 3 7 3.2 CC(C)N1C=C2CC3C(CC(CN3C)C(=O)OC(C)C(C)O)C4=C2C1=CC=C4.C(=CC(=O)O)C(=O)O None
1201549 590 22 None -26 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
333 590 22 None -26 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
7601 590 22 None -26 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL1201203 590 22 None -26 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL438151 590 22 None -26 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
DB00245 590 22 None -26 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
228 441 26 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 441 26 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 441 26 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 441 26 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 441 26 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
152 361 18 3H-5HT 1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 361 18 3H-5HT 1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 361 18 3H-5HT 1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2520 202301 65 None -4 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
CHEMBL1280 202301 65 None -4 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
CHEMBL6966 202301 65 None -4 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
15897 2807 0 Functional 12 37 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2807 0 Functional 12 37 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2807 0 Functional 12 37 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
None 214152 0 3H-KETANSERIN -19 6 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 6 2 7 2.1 CC(C1=CC=CC2=NC3=C(C=CC=C3N=C21)C(=O)O)OC(=O)C(CO)OC None
10624 69942 17 3H-KETANSERIN -46 33 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 69942 17 3H-KETANSERIN -46 33 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 69942 17 3H-KETANSERIN -46 33 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
71285 214197 0 Functional 1 2 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 209 3 2 4 1.3 CC(CC1=CC2=C(C=C1O)OCO2)NC None
283 3069 47 3H-5HT -57 12 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
4847 3069 47 3H-5HT -57 12 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
CHEMBL18331 3069 47 3H-5HT -57 12 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
115237 55281 113 3H-LSD -89 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55281 113 3H-LSD -89 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
None 215720 0 UNDEFINED -83 3 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 449 6 3 4 4.1 C1CC2=C(CC1CCCNCC3COC4=C(O3)C=CC5=C4CC(=O)N5)NC6=C2C=C(C=C6)F None
107992 2506 47 3H-5HT -1 10 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 2506 47 3H-5HT -1 10 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 2506 47 3H-5HT -1 10 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 2506 47 3H-5HT -1 10 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
240 929 39 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 929 39 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 929 39 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 929 39 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 929 39 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 929 39 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 929 39 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
7153 97557 74 Functional -1 34 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 Functional -1 34 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
None 214693 0 Functional 1 28 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
107780 1806 50 3H-5HT -676 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1806 50 3H-5HT -676 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1806 50 3H-5HT -676 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
1524 2141 89 3H-5HT -234 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-5HT -234 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-5HT -234 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-5HT -234 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-5HT -234 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-5HT -234 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2141 89 3H-5HT -234 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-5HT -234 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-5HT -234 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-5HT -234 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-5HT -234 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-5HT -234 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
173 3199 88 3H-5HT -3 23 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3199 88 3H-5HT -3 23 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3199 88 3H-5HT -3 23 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
1574 81 52 125I-DOI -70 21 Mouse 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 52 125I-DOI -70 21 Mouse 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 52 125I-DOI -70 21 Mouse 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
173 3199 88 125I-DOI -75 23 Mouse 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3199 88 125I-DOI -75 23 Mouse 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3199 88 125I-DOI -75 23 Mouse 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
1342 36 42 3H-5HT -4 19 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 42 3H-5HT -4 19 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 42 3H-5HT -4 19 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
44626329 195722 0 UNDEFINED -20 3 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 420 3 2 4 3.7 O=c1[nH]c2cccc(N3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 None
CHEMBL569513 195722 0 UNDEFINED -20 3 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 420 3 2 4 3.7 O=c1[nH]c2cccc(N3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 None
3337 214431 0 3H-LSD -75 41 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 3H-LSD -75 41 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 3H-LSD -75 41 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 3H-LSD -75 41 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
1210 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1213 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2725 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
33036 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4411 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
616 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6976 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
716121 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
90475904 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 903 45 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
62787 204457 17 3H-KETANSERIN -64 10 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
CHEMBL8642 204457 17 3H-KETANSERIN -64 10 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
2470 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
4976 201876 27 None -1 12 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
CHEMBL668 201876 27 None -1 12 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
5440 215991 0 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 399 6 0 5 5.0 CCSC1=CC=C2SC3=CC=CC=C3N(CCCN3CCN(C)CC3)C2=C1 None
5022 1613 67 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
6918248 1613 67 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
8182 1613 67 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
CHEMBL231068 1613 67 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
DB04908 1613 67 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
4543 169972 36 None -4 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL1201156 169972 36 None -4 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL445 169972 36 None -4 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
107 141 116 3H-5HT -12 31 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-5HT -12 31 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-5HT -12 31 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
213 3780 50 None -5 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3780 50 None -5 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3780 50 None -5 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3780 50 None -5 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3780 50 None -5 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
11957541 1425 38 3H-MESULERGINE -2 16 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1425 38 3H-MESULERGINE -2 16 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1425 38 3H-MESULERGINE -2 16 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1425 38 3H-MESULERGINE -2 16 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1425 38 3H-MESULERGINE -2 16 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
2105 2993 34 3H-MESULERGINE -28 33 Human 8.2 pKi = 8.2 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-MESULERGINE -28 33 Human 8.2 pKi = 8.2 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-MESULERGINE -28 33 Human 8.2 pKi = 8.2 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-MESULERGINE -28 33 Human 8.2 pKi = 8.2 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-MESULERGINE -28 33 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
2601 3709 30 3H-MESULERGINE -8 21 Human 8.2 pKi = 8.2 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-MESULERGINE -8 21 Human 8.2 pKi = 8.2 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-MESULERGINE -8 21 Human 8.2 pKi = 8.2 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-MESULERGINE -8 21 Human 8.2 pKi = 8.2 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-MESULERGINE -8 21 Human 8.2 pKi = 8.2 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
100 3733 52 None -11 56 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3733 52 None -11 56 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3733 52 None -11 56 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3733 52 None -11 56 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3733 52 None -11 56 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
240 929 39 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 929 39 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 929 39 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 929 39 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 929 39 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 929 39 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 929 39 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
135398737 942 89 3H-5HT -2 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 3H-5HT -2 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 3H-5HT -2 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 3H-5HT -2 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 3H-5HT -2 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2351 3222 60 None -7 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2820 3222 60 None -7 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
5035 3222 60 None -7 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
CHEMBL81 3222 60 None -7 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
DB00481 3222 60 None -7 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2274 3112 53 None -10 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3112 53 None -10 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3112 53 None -10 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3112 53 None -10 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3112 53 None -10 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2099 9202 49 None - 1 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL1110 9202 49 None - 1 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O None
135398745 2858 108 3H-LSD -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 3H-LSD -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 3H-LSD -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 3H-LSD -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3952 1849 33 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5353646 1849 33 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5443 1849 33 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5702063 1849 33 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL1331786 1849 33 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL420 1849 33 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
115237 55281 113 None -89 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55281 113 None -89 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
2291 3123 52 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
2561 3123 52 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
4932 3123 52 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
CHEMBL631 3123 52 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
DB01182 3123 52 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
216239 23576 114 None 2 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1200485 23576 114 None 2 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1336 23576 114 None 2 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
2726 904 64 None -19 73 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 904 64 None -19 73 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 904 64 None -19 73 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 904 64 None -19 73 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 904 64 None -19 73 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
31101 719 39 None -26 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 719 39 None -26 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 719 39 None -26 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 719 39 None -26 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 719 39 None -26 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
102 4051 44 None -100 50 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 None -100 50 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 None -100 50 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 None -100 50 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 None -100 50 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2181 3067 0 None -15 35 Human 8.1 pKi = 8.1 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 -15 35 Human 8.1 pKi = 8.1 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 -15 35 Human 8.1 pKi = 8.1 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 -15 35 Human 8.1 pKi = 8.1 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 -15 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
2286 3122 48 None -5 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3122 48 None -5 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3122 48 None -5 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3122 48 None -5 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3122 48 None -5 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
180 397 50 None -35 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 None -35 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 None -35 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 None -35 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 None -35 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2389 3267 114 None -79 68 Human 8.1 pKi = 8.1 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 -79 68 Human 8.1 pKi = 8.1 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 -79 68 Human 8.1 pKi = 8.1 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 -79 68 Human 8.1 pKi = 8.1 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 -79 68 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
114948 216007 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Biased for β-arrestin signalling.Biased for β-arrestin signalling.
Drug Central 577 5 3 6 2.5 CC(C)C[C@@H]1N2C(=O)[C@](NC(=O)[C@@H]3C[C@H]4[C@@H](CC5=CNC6=CC=CC4=C56)N(C)C3)(O[C@@]2(O)[C@@H]2CCCN2C1=O)C(C)C None
6761 67442 17 None -7 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL1909072 67442 17 None -7 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
1621 2386 16 None -19 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
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 -19 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
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 -19 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
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 -19 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
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 -19 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
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
2600 3708 73 None -1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
2608 3708 73 None -1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
5405 3708 73 None -1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
CHEMBL17157 3708 73 None -1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
DB00342 3708 73 None -1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
1530 2142 44 None -19 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 2142 44 None -19 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 2142 44 None -19 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 2142 44 None -19 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 2142 44 None -19 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
124087 1357 106 None -5 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
7157 1357 106 None -5 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
814 1357 106 None -5 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
CHEMBL1172 1357 106 None -5 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
DB00967 1357 106 None -5 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
2865 4064 67 None -12 54 Human 8.1 pKi = 8.1 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 -12 54 Human 8.1 pKi = 8.1 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 -12 54 Human 8.1 pKi = 8.1 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 -12 54 Human 8.1 pKi = 8.1 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 -12 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
135398737 942 89 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1212 1624 45 None -27 66 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1624 45 None -27 66 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1624 45 None -27 66 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1624 45 None -27 66 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1624 45 None -27 66 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
26987 934 29 None -47 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 934 29 None -47 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 934 29 None -47 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 934 29 None -47 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 934 29 None -47 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
2267 553 64 None -10 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
271 553 64 None -10 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
7121 553 64 None -10 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
CHEMBL639 553 64 None -10 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
DB00972 553 64 None -10 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
3652 4022 72 None -2 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4022 72 None -2 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4022 72 None -2 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4022 72 None -2 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4022 72 None -2 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
2585 788 100 None -18 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 788 100 None -18 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 788 100 None -18 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 788 100 None -18 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 788 100 None -18 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
102 4051 44 None -93 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 None -93 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 None -93 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 None -93 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 None -93 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
135398745 2858 108 None -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 None -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 None -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 None -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
134 2468 19 3H-5HT -2 68 Human 8.1 pKi = 8.1 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 3H-5HT -2 68 Human 8.1 pKi = 8.1 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 3H-5HT -2 68 Human 8.1 pKi = 8.1 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 3H-5HT -2 68 Human 8.1 pKi = 8.1 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 3H-5HT -2 68 Human 8.1 pKi = 8.1 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
3036864 201057 16 Functional -295 28 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201057 16 Functional -295 28 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201057 16 Functional -295 28 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201057 16 Functional -295 28 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
1615 167217 22 3H-LSD -2 45 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167217 22 3H-LSD -2 45 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
2470 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1210 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1213 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2725 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
33036 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4411 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
616 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6976 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
716121 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
90475904 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 903 45 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1150 3805 116 3H-5HT -2 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3805 116 3H-5HT -2 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3805 116 3H-5HT -2 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3805 116 3H-5HT -2 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
213 3780 50 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3780 50 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3780 50 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3780 50 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3780 50 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
21830793 91389 5 3H-8-OH-DPAT -489 46 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91389 5 3H-8-OH-DPAT -489 46 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
45266826 215944 0 [3H] LSD 2 8 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 177 3 1 2 1.8 CC1=CC=C(C=C1)C(=O)C(C)NC None
179 396 107 3H-LSD -17 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 3H-LSD -17 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 3H-LSD -17 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 3H-LSD -17 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 3H-LSD -17 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
24740863 88714 0 UNDEFINED 1 6 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl None
CHEMBL236610 88714 0 UNDEFINED 1 6 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl None
1524 2141 89 3H-5HT -234 52 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 3H-5HT -234 52 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 3H-5HT -234 52 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 3H-5HT -234 52 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 3H-5HT -234 52 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 3H-5HT -234 52 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
5 139 66 3H-KETANSERIN -1778 55 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-KETANSERIN -1778 55 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-KETANSERIN -1778 55 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-KETANSERIN -1778 55 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
77590 214166 0 3H-5HT -10 6 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 124 4 0 2 0.8 COCCOCCl None
221 3422 63 3H-5HT -4 14 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 3422 63 3H-5HT -4 14 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 3422 63 3H-5HT -4 14 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
None 214693 0 UNDEFINED 1 28 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
206 2447 10 3H-KETANSERIN -5 25 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2447 10 3H-KETANSERIN -5 25 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2447 10 3H-KETANSERIN -5 25 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
134551 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 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)C(C)C)O)C None
271 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 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)C(C)C)O)C None
885 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 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)C(C)C)O)C None
CHEMBL1403281 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 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)C(C)C)O)C None
135 2486 38 None -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 None -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 None -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 None -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 None -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2247 502 77 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 502 77 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 502 77 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 502 77 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 502 77 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
1385580 29048 73 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 None
4615 29048 73 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 None
CHEMBL13828 29048 73 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 None
191 399 92 None -5 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 None -5 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 None -5 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 None -5 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 None -5 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2601 3709 30 None -8 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3709 30 None -8 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3709 30 None -8 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3709 30 None -8 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3709 30 None -8 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
135398737 942 89 None -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 None -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 None -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 None -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 None -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
10531 1387 18 None -15 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
121 1387 18 None -15 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
888 1387 18 None -15 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL1732 1387 18 None -15 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00320 1387 18 None -15 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
107715 199250 18 None -14 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 199250 18 None -14 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 199250 18 None -14 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
135526515 215990 0 None 1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 301 7 4 3 2.8 CCCCCNC(=N)NN=CC1=CNC2=C1C=C(OC)C=C2 None
1588 2284 24 None -8 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -8 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -8 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -8 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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 -8 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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
135398737 942 89 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1042 1544 20 None -7 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
148 1544 20 None -7 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
443884 1544 20 None -7 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
CHEMBL119443 1544 20 None -7 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
DB01253 1544 20 None -7 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
2220 3073 78 None -1 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
Drug Central 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
27400 3073 78 None -1 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
Drug Central 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
93 3073 78 None -1 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
Drug Central 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
CHEMBL294951 3073 78 None -1 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
Drug Central 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
DB06153 3073 78 None -1 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
Drug Central 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
3337 214431 0 Functional -75 41 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 Functional -75 41 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 Functional -75 41 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 Functional -75 41 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
11978813 712 72 None -2 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 -2 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 -2 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 -2 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 -2 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
133 2450 48 None -2 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2450 48 None -2 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2450 48 None -2 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2450 48 None -2 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2450 48 None -2 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
277 1269 55 None -5 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1269 55 None -5 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1269 55 None -5 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1269 55 None -5 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1269 55 None -5 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
37 764 56 None 1 17 Human 8.1 pKi = 8.1 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
460 764 56 None 1 17 Human 8.1 pKi = 8.1 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
54746 764 56 None 1 17 Human 8.1 pKi = 8.1 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
CHEMBL1201087 764 56 None 1 17 Human 8.1 pKi = 8.1 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
DB00248 764 56 None 1 17 Human 8.1 pKi = 8.1 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
11954224 214164 0 None -66 60 Human 8.1 pKi = 8.1 Binding
NoneNone
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
1621 2386 16 Functional -19 45 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2386 16 Functional -19 45 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2386 16 Functional -19 45 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2386 16 Functional -19 45 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2386 16 Functional -19 45 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
135 2486 38 3H-5HT -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 3H-5HT -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 3H-5HT -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 3H-5HT -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 3H-5HT -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
None 214181 0 3H-KETANSERIN -147 2 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 5 1 3 2.6 CCC1=CC(=C(C=C1OC)CC(C)N)OC.Cl None
3036864 201057 16 3H-5HT -346 28 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201057 16 3H-5HT -346 28 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201057 16 3H-5HT -346 28 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201057 16 3H-5HT -346 28 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
213 3780 50 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3780 50 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3780 50 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3780 50 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3780 50 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
115 3720 78 3H-5HT -2 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3720 78 3H-5HT -2 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3720 78 3H-5HT -2 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
173 3199 88 3H-5HT 1 23 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3199 88 3H-5HT 1 23 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3199 88 3H-5HT 1 23 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
115 3720 78 3H-5HT -2 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3720 78 3H-5HT -2 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3720 78 3H-5HT -2 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
2337 3193 72 3H-LSD -15 63 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3193 72 3H-LSD -15 63 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3193 72 3H-LSD -15 63 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3193 72 3H-LSD -15 63 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3193 72 3H-LSD -15 63 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
134 2468 19 3H-5HT -12 68 Rat 7.1 pKi = 7.1 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 3H-5HT -12 68 Rat 7.1 pKi = 7.1 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 3H-5HT -12 68 Rat 7.1 pKi = 7.1 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 3H-5HT -12 68 Rat 7.1 pKi = 7.1 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 3H-5HT -12 68 Rat 7.1 pKi = 7.1 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
119376 1803 41 3H-5HT -4786 27 Human 6.1 pKi = 6.1 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-5HT -4786 27 Human 6.1 pKi = 6.1 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-5HT -4786 27 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
71299720 214162 0 3H-5HT -691 17 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
1220 186 46 Functional -1905 45 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 186 46 Functional -1905 45 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 186 46 Functional -1905 45 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 186 46 Functional -1905 45 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
150 2463 18 None 1 16 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
1764 2463 18 None 1 16 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
8226 2463 18 None 1 16 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
CHEMBL1201356 2463 18 None 1 16 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
DB00353 2463 18 None 1 16 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
134 2468 19 3H-5HT -2 68 Human 8.0 pKi = 8.0 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 3H-5HT -2 68 Human 8.0 pKi = 8.0 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 3H-5HT -2 68 Human 8.0 pKi = 8.0 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 3H-5HT -2 68 Human 8.0 pKi = 8.0 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 3H-5HT -2 68 Human 8.0 pKi = 8.0 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
107 141 116 3H-5HT -12 31 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-5HT -12 31 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-5HT -12 31 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
107 141 116 3H-5HT -12 31 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-5HT -12 31 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-5HT -12 31 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
11154555 786 57 None -39 12 Human 8.0 pKi = 8.0 Binding
CHO-K1 cells, [3H]LSD (1.2nM)CHO-K1 cells, [3H]LSD (1.2nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
5037 786 57 None -39 12 Human 8.0 pKi = 8.0 Binding
CHO-K1 cells, [3H]LSD (1.2nM)CHO-K1 cells, [3H]LSD (1.2nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
7671 786 57 None -39 12 Human 8.0 pKi = 8.0 Binding
CHO-K1 cells, [3H]LSD (1.2nM)CHO-K1 cells, [3H]LSD (1.2nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL2028019 786 57 None -39 12 Human 8.0 pKi = 8.0 Binding
CHO-K1 cells, [3H]LSD (1.2nM)CHO-K1 cells, [3H]LSD (1.2nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL3085826 786 57 None -39 12 Human 8.0 pKi = 8.0 Binding
CHO-K1 cells, [3H]LSD (1.2nM)CHO-K1 cells, [3H]LSD (1.2nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB06016 786 57 None -39 12 Human 8.0 pKi = 8.0 Binding
CHO-K1 cells, [3H]LSD (1.2nM)CHO-K1 cells, [3H]LSD (1.2nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
134 2468 19 None -2 68 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cellsDisplacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cells
Drug Central 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 None -2 68 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cellsDisplacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cells
Drug Central 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 None -2 68 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cellsDisplacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cells
Drug Central 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 None -2 68 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cellsDisplacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cells
Drug Central 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 None -2 68 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cellsDisplacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cells
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
242 467 117 None -1 52 Human 8.0 pKi = 8.0 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 -1 52 Human 8.0 pKi = 8.0 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 -1 52 Human 8.0 pKi = 8.0 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 -1 52 Human 8.0 pKi = 8.0 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 -1 52 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
5 139 66 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
135 2486 38 3H-5HT -3 58 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 3H-5HT -3 58 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 3H-5HT -3 58 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 3H-5HT -3 58 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 3H-5HT -3 58 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
46780481 107032 18 None -57 54 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107032 18 None -57 54 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107032 18 None -57 54 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107032 18 None -57 54 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
5 139 66 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
11848625 5700 0 UNDEFINED 2 6 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 None
CHEMBL1078745 5700 0 UNDEFINED 2 6 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 None
62787 204457 17 3H-5HT -3 10 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
CHEMBL8642 204457 17 3H-5HT -3 10 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
7153 97557 74 3H-KETANSERIN -50 34 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-KETANSERIN -50 34 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
None 214245 0 3H-5HT -10 4 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
None 214695 0 3H-5HT -43 3 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 419 6 1 4 3.4 C1CN(CCC12C(=O)NCN2C3=CC=CC=C3)CCCOC4=CC=C(C=C4)F.Cl None
10624 69942 17 3H-LSD -7 33 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 69942 17 3H-LSD -7 33 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 69942 17 3H-LSD -7 33 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
282 1386 0 None -371 7 Human 7.5 pKi = 7.5 Binding
Biased for β-arrestin signalling.Biased for β-arrestin signalling.
Guide to Pharmacology 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 23519215
522609 1386 0 None -371 7 Human 7.5 pKi = 7.5 Binding
Biased for β-arrestin signalling.Biased for β-arrestin signalling.
Guide to Pharmacology 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 23519215
1621 2386 16 None -19 45 Human 8.4 pKi = 8.4 Binding
Biased for β-arrestin sihnalling.Biased for β-arrestin sihnalling.
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 23519215
17 2386 16 None -19 45 Human 8.4 pKi = 8.4 Binding
Biased for β-arrestin sihnalling.Biased for β-arrestin sihnalling.
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 23519215
5761 2386 16 None -19 45 Human 8.4 pKi = 8.4 Binding
Biased for β-arrestin sihnalling.Biased for β-arrestin sihnalling.
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 23519215
CHEMBL263881 2386 16 None -19 45 Human 8.4 pKi = 8.4 Binding
Biased for β-arrestin sihnalling.Biased for β-arrestin sihnalling.
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 23519215
DB04829 2386 16 None -19 45 Human 8.4 pKi = 8.4 Binding
Biased for β-arrestin sihnalling.Biased for β-arrestin sihnalling.
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 23519215
10287037 619 0 None 31 2 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 3 0 4 5.1 CCOc1ccc2c(c1)Sc1c(C2=C2CCN(CC2)C)c(OC)ccc1 25666387
8424 619 0 None 31 2 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 3 0 4 5.1 CCOc1ccc2c(c1)Sc1c(C2=C2CCN(CC2)C)c(OC)ccc1 25666387
2 3198 19 None -363 29 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
2 3198 19 None -363 29 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 15322733
54562 3198 19 None -363 29 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
54562 3198 19 None -363 29 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 15322733
CHEMBL240773 3198 19 None -363 29 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
CHEMBL240773 3198 19 None -363 29 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 15322733
11658860 2302 47 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
2941 2302 47 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
4374 2302 47 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
CHEMBL360328 2302 47 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
DB04871 2302 47 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
45275554 3248 0 None -6 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 9 3 6 3.7 COc1cc(N)c(cc1C(=O)NCC1CCN(CC1)CC[C@@H](c1ccc(cc1)F)OC(=O)N)Cl 25316608
8427 3248 0 None -6 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 9 3 6 3.7 COc1cc(N)c(cc1C(=O)NCC1CCN(CC1)CC[C@@H](c1ccc(cc1)F)OC(=O)N)Cl 25316608
CHEMBL3544975 3248 0 None -6 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 9 3 6 3.7 COc1cc(N)c(cc1C(=O)NCC1CCN(CC1)CC[C@@H](c1ccc(cc1)F)OC(=O)N)Cl 25316608
DB12798 3248 0 None -6 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 9 3 6 3.7 COc1cc(N)c(cc1C(=O)NCC1CCN(CC1)CC[C@@H](c1ccc(cc1)F)OC(=O)N)Cl 25316608
11957541 1425 38 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
11957541 1425 38 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8450835
1229 1425 38 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
1229 1425 38 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8450835
147 1425 38 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
147 1425 38 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8450835
170617 1425 38 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
170617 1425 38 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8450835
CHEMBL6616 1425 38 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
CHEMBL6616 1425 38 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8450835
11957541 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 12970106
11957541 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
11957541 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 9933142
1229 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 12970106
1229 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
1229 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 9933142
147 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 12970106
147 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
147 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 9933142
170617 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 12970106
170617 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
170617 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 9933142
CHEMBL6616 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 12970106
CHEMBL6616 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
CHEMBL6616 1425 38 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 9933142
161 741 3 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 12970106
161 741 3 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 15322733
161 741 3 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 15466450
4284720 741 3 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 12970106
4284720 741 3 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 15322733
4284720 741 3 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 15466450
CHEMBL1255834 741 3 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 12970106
CHEMBL1255834 741 3 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 15322733
CHEMBL1255834 741 3 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 15466450
166 3295 12 None 1 3 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 15322733
3045227 3295 12 None 1 3 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 15322733
CHEMBL76781 3295 12 None 1 3 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 15322733
135 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10455251
135 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 15322733
135 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9459568
1796 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10455251
1796 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 15322733
1796 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9459568
4184 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10455251
4184 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 15322733
4184 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9459568
CHEMBL6437 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10455251
CHEMBL6437 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 15322733
CHEMBL6437 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9459568
DB06148 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10455251
DB06148 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 15322733
DB06148 2486 38 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9459568
134 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 11104741
134 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 15322733
134 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9459568
1775 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 11104741
1775 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 15322733
1775 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9459568
9681 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 11104741
9681 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 15322733
9681 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9459568
CHEMBL1065 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 11104741
CHEMBL1065 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 15322733
CHEMBL1065 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9459568
DB00247 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 11104741
DB00247 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 15322733
DB00247 2468 19 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9459568
176 1502 0 None 19 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 4 1 5 2.8 Nc1cc(N2CCN(CC2)Cc2ccccc2)c(cc1C)[N+](=O)[O-] 15107597
9930789 1502 0 None 19 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 4 1 5 2.8 Nc1cc(N2CCN(CC2)Cc2ccccc2)c(cc1C)[N+](=O)[O-] 15107597
CHEMBL1628720 1502 0 None 19 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 4 1 5 2.8 Nc1cc(N2CCN(CC2)Cc2ccccc2)c(cc1C)[N+](=O)[O-] 15107597
188 3327 73 None -1 6 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10455251
188 3327 73 None -1 6 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 15322733
196968 3327 73 None -1 6 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10455251
196968 3327 73 None -1 6 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 15322733
CHEMBL473186 3327 73 None -1 6 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10455251
CHEMBL473186 3327 73 None -1 6 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 15322733
3763 215974 0 None - 1 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 184 2 0 1 2.4 FC(F)OC(Cl)C(F)(F)F None
202 1475 0 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1475 0 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1475 0 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1475 0 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1475 0 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
3337 214431 0 None -75 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 -75 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 -75 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 -75 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
4450 215981 0 None -1 3 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 253 1 0 2 3.2 CN1CCOC(C2=CC=CC=C2)C2=CC=CC=C2C1 None
6166 214243 0 None -4 4 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 330 2 1 3 3.7 C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2C(=O)CO)CCC4=CC(=O)CC[C@]34C None
179 396 107 None -17 51 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 None -17 51 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 None -17 51 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 None -17 51 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 None -17 51 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
1357 2440 133 None -3890 9 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12750432
1672 2440 133 None -3890 9 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12750432
224 2440 133 None -3890 9 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12750432
896 2440 133 None -3890 9 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12750432
CHEMBL45 2440 133 None -3890 9 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12750432
DB01065 2440 133 None -3890 9 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12750432
1209 1620 69 None -199 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
203 1620 69 None -199 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
3386 1620 69 None -199 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
CHEMBL41 1620 69 None -199 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
DB00472 1620 69 None -199 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
208 2810 0 None -69 13 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
4541 2810 0 None -69 13 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
CHEMBL1494 2810 0 None -69 13 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
1220 186 46 None -1905 45 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 15322733
1220 186 46 None -3235 45 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450835
31 186 46 None -1905 45 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 15322733
31 186 46 None -3235 45 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450835
7 186 46 None -1905 45 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 15322733
7 186 46 None -3235 45 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450835
CHEMBL56 186 46 None -1905 45 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 15322733
CHEMBL56 186 46 None -3235 45 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450835
1524 2141 89 None -2754 52 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8450835
197 2141 89 None -2754 52 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8450835
3822 2141 89 None -2754 52 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8450835
88 2141 89 None -2754 52 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8450835
CHEMBL51 2141 89 None -2754 52 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8450835
DB12465 2141 89 None -2754 52 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8450835
186 1769 47 None -575 17 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 15322733
71781 1769 47 None -575 17 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 15322733
CHEMBL18972 1769 47 None -575 17 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 15322733
2470 3583 46 None -120226 60 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8450835
3300 3583 46 None -120226 60 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8450835
5265 3583 46 None -120226 60 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8450835
99 3583 46 None -120226 60 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8450835
CHEMBL267930 3583 46 None -120226 60 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8450835
2176 3065 66 None -933 27 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 15322733
4828 3065 66 None -933 27 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 15322733
91 3065 66 None -933 27 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 15322733
CHEMBL500 3065 66 None -933 27 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 15322733
DB00960 3065 66 None -933 27 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 15322733
29 778 0 None -2511 9 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
9805719 778 0 None -2511 9 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
CHEMBL2027925 778 0 None -2511 9 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
18971832 2375 0 None -263 13 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C 9395253
21 2375 0 None -263 13 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C 9395253
CHEMBL3186179 2375 0 None -263 13 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C 9395253
28 3427 37 None -954 10 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
3292447 3427 37 None -954 10 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
CHEMBL20963 3427 37 None -954 10 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
2202 3071 91 None -6 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
4850 3071 91 None -6 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
49 3071 91 None -6 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
CHEMBL1371770 3071 91 None -6 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
DB12478 3071 91 None -6 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
130 3431 43 None -478 13 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 15322733
3378093 3431 43 None -478 13 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 15322733
CHEMBL281350 3431 43 None -478 13 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 15322733
143 3446 45 None -158 7 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10945872
5311096 3446 45 None -158 7 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10945872
CHEMBL85606 3446 45 None -158 7 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10945872
175 3585 38 None -331 7 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
68186 3585 38 None -331 7 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
CHEMBL79834 3585 38 None -331 7 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
185 3931 54 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10188965
185 3931 54 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 15322733
5311271 3931 54 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10188965
5311271 3931 54 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 15322733
CHEMBL74355 3931 54 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10188965
CHEMBL74355 3931 54 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 15322733
DB16351 3931 54 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10188965
DB16351 3931 54 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 15322733
187 3324 15 None -288 5 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 15322733
187 3324 15 None -288 5 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 9225287
3693566 3324 15 None -288 5 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 15322733
3693566 3324 15 None -288 5 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 9225287
CHEMBL88402 3324 15 None -288 5 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 15322733
CHEMBL88402 3324 15 None -288 5 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 9225287
1353 1872 85 None -295 86 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 9459568
3559 1872 85 None -295 86 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 9459568
86 1872 85 None -295 86 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 9459568
CHEMBL54 1872 85 None -295 86 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 9459568
DB00502 1872 85 None -295 86 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 9459568
109 887 23 None -281 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 15322733
2689 887 23 None -281 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 15322733
CHEMBL27403 887 23 None -281 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 15322733
2470 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
2470 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8078486
2470 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 9459568
3300 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
3300 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8078486
3300 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 9459568
5265 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
5265 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8078486
5265 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 9459568
99 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
99 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8078486
99 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 9459568
CHEMBL267930 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
CHEMBL267930 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8078486
CHEMBL267930 3583 46 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 9459568
107780 1806 50 None -676 18 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
14 1806 50 None -676 18 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
CHEMBL15928 1806 50 None -676 18 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
133633 2201 46 None -87 8 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10869410
177 2201 46 None -87 8 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10869410
CHEMBL445102 2201 46 None -87 8 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10869410
177336 3059 45 None -1412 3 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 11504648
225 3059 45 None -1412 3 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 11504648
CHEMBL356359 3059 45 None -1412 3 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 11504648
DB04873 3059 45 None -1412 3 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 11504648
1524 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 12738034
1524 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 15322733
1524 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8078486
1524 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8845011
1524 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9459568
197 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 12738034
197 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 15322733
197 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8078486
197 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8845011
197 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9459568
3822 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 12738034
3822 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 15322733
3822 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8078486
3822 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8845011
3822 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9459568
88 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 12738034
88 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 15322733
88 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8078486
88 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8845011
88 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9459568
CHEMBL51 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 12738034
CHEMBL51 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 15322733
CHEMBL51 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8078486
CHEMBL51 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8845011
CHEMBL51 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9459568
DB12465 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 12738034
DB12465 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 15322733
DB12465 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8078486
DB12465 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8845011
DB12465 2141 89 None -234 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9459568
107992 2506 47 None -5 10 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 8450835
165 2506 47 None -5 10 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 8450835
CHEMBL269521 2506 47 None -5 10 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 8450835
DB12111 2506 47 None -5 10 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 8450835
107992 2506 47 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 12970106
107992 2506 47 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 15322733
165 2506 47 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 12970106
165 2506 47 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 15322733
CHEMBL269521 2506 47 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 12970106
CHEMBL269521 2506 47 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 15322733
DB12111 2506 47 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 12970106
DB12111 2506 47 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 15322733
5268 3586 34 None -1047 18 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 9459568
53 3586 34 None -1047 18 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 9459568
CHEMBL300555 3586 34 None -1047 18 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 9459568
1574 81 52 None -3 21 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 8450835
218 81 52 None -3 21 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 8450835
CHEMBL266591 81 52 None -3 21 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 8450835
198 310 120 None -346 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12750432
82148 310 120 None -346 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12750432
99 310 120 None -346 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12750432
CHEMBL10878 310 120 None -346 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12750432
DB06594 310 120 None -346 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12750432
177336 3059 45 None -1412 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 15466450
225 3059 45 None -1412 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 15466450
CHEMBL356359 3059 45 None -1412 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 15466450
DB04873 3059 45 None -1412 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 15466450
210 3408 0 None -7 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C 12738034
2423 3408 0 None -7 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C 12738034
5160 3408 0 None -7 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C 12738034
CHEMBL52939 3408 0 None -7 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C 12738034
DB12163 3408 0 None -7 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C 12738034
195 3501 5 None -25 5 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 0 0 2 2.1 CN1CC[C@H]2[C@@H](C1)c1cccc3c1N(C2)CC3 15322733
9859407 3501 5 None -25 5 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 0 0 2 2.1 CN1CC[C@H]2[C@@H](C1)c1cccc3c1N(C2)CC3 15322733
CHEMBL316069 3501 5 None -25 5 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 0 0 2 2.1 CN1CC[C@H]2[C@@H](C1)c1cccc3c1N(C2)CC3 15322733
1809 134 28 None -999 37 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 15322733
1809 134 28 None -999 37 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8078486
4 134 28 None -999 37 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 15322733
4 134 28 None -999 37 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8078486
CHEMBL18840 134 28 None -999 37 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 15322733
CHEMBL18840 134 28 None -999 37 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8078486
1809 134 28 None -1659 37 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8078486
1809 134 28 None -1659 37 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450835
4 134 28 None -1659 37 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8078486
4 134 28 None -1659 37 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450835
CHEMBL18840 134 28 None -1659 37 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8078486
CHEMBL18840 134 28 None -1659 37 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450835
129 3372 7 None -562 9 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 7 1 4 4.8 N#Cc1ccc2c(c1)[C@H]1CN(C[C@@H]1CO2)CCCCNC(=O)c1ccc(cc1)c1ccccc1 10869410
9868452 3372 7 None -562 9 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 7 1 4 4.8 N#Cc1ccc2c(c1)[C@H]1CN(C[C@@H]1CO2)CCCCNC(=O)c1ccc(cc1)c1ccccc1 10869410
CHEMBL65280 3372 7 None -562 9 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 7 1 4 4.8 N#Cc1ccc2c(c1)[C@H]1CN(C[C@@H]1CO2)CCCCNC(=O)c1ccc(cc1)c1ccccc1 10869410
193 3437 38 None -707 5 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 15322733
193 3437 38 None -707 5 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 9225286
3644637 3437 38 None -707 5 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 15322733
3644637 3437 38 None -707 5 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 9225286
CHEMBL14563 3437 38 None -707 5 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 15322733
CHEMBL14563 3437 38 None -707 5 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 9225286
228 441 26 None -5 24 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
33 441 26 None -5 24 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
6005 441 26 None -5 24 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
CHEMBL53 441 26 None -5 24 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
DB00714 441 26 None -5 24 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
173 3199 88 None -3 23 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 8450835
5011 3199 88 None -3 23 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 8450835
CHEMBL18772 3199 88 None -3 23 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 8450835
108029 3349 50 None -125 13 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 15322733
23 3349 50 None -125 13 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 15322733
CHEMBL18785 3349 50 None -125 13 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 15322733
221 3422 63 None -4 14 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C 15322733
3277600 3422 63 None -4 14 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C 15322733
CHEMBL323356 3422 63 None -4 14 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C 15322733
170 2905 0 None -6 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 1 1 3 2.2 FC(c1ccc(nc1Cl)N1CCNCC1)(F)F 15322733
9796408 2905 0 None -6 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 1 1 3 2.2 FC(c1ccc(nc1Cl)N1CCNCC1)(F)F 15322733
CHEMBL506999 2905 0 None -6 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 1 1 3 2.2 FC(c1ccc(nc1Cl)N1CCNCC1)(F)F 15322733
194 3438 25 None -100 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10737744
443391 3438 25 None -100 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10737744
CHEMBL14460 3438 25 None -100 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10737744
1150 3805 116 None -2 25 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 15322733
1150 3805 116 None -8 25 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 8450835
125 3805 116 None -2 25 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 15322733
125 3805 116 None -8 25 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 8450835
CHEMBL6640 3805 116 None -2 25 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 15322733
CHEMBL6640 3805 116 None -8 25 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 8450835
DB08653 3805 116 None -2 25 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 15322733
DB08653 3805 116 None -8 25 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 8450835
173 3199 88 None 1 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 15322733
5011 3199 88 None 1 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 15322733
CHEMBL18772 3199 88 None 1 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 15322733
115 3720 78 None -2 27 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450835
4296 3720 78 None -2 27 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450835
CHEMBL274866 3720 78 None -2 27 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450835
213 3780 50 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 11104741
213 3780 50 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 15322733
2717 3780 50 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 11104741
2717 3780 50 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 15322733
5533 3780 50 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 11104741
5533 3780 50 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 15322733
CHEMBL621 3780 50 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 11104741
CHEMBL621 3780 50 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 15322733
DB00656 3780 50 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 11104741
DB00656 3780 50 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 15322733
115 3720 78 None -1 27 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 15322733
4296 3720 78 None -1 27 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 15322733
CHEMBL274866 3720 78 None -1 27 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 15322733
31101 719 39 None -26 36 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
35 719 39 None -26 36 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
403 719 39 None -26 36 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
CHEMBL493 719 39 None -26 36 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
DB01200 719 39 None -26 36 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
135 2486 38 None -37 58 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8450835
1796 2486 38 None -37 58 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8450835
4184 2486 38 None -37 58 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8450835
CHEMBL6437 2486 38 None -37 58 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8450835
DB06148 2486 38 None -37 58 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8450835
15897 2807 0 None 12 37 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N 11104741
215 2807 0 None 12 37 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N 11104741
CHEMBL1979333 2807 0 None 12 37 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N 11104741
12895728 2808 0 None - 1 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 C[C@H](Cc1cccc(c1)C(F)(F)F)N 11104741
217 2808 0 None - 1 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 C[C@H](Cc1cccc(c1)C(F)(F)F)N 11104741
CHEMBL250881 2808 0 None - 1 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 C[C@H](Cc1cccc(c1)C(F)(F)F)N 11104741
102 4051 44 None -100 50 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
3659 4051 44 None -100 50 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
8969 4051 44 None -100 50 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
CHEMBL15245 4051 44 None -100 50 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
DB01392 4051 44 None -100 50 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
157 2030 5 None -134 5 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 15322733
157 2030 5 None -134 5 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 9857084
9840090 2030 5 None -134 5 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 15322733
9840090 2030 5 None -134 5 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 9857084
CHEMBL134519 2030 5 None -134 5 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 15322733
CHEMBL134519 2030 5 None -134 5 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 9857084
10 714 23 None -3 9 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
3654103 714 23 None -3 9 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
CHEMBL534232 714 23 None -3 9 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
206 2447 10 None -26 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 8450835
68848 2447 10 None -26 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 8450835
CHEMBL12314 2447 10 None -26 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 8450835
171 2907 0 None -5 3 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 233 3 1 3 1.9 COc1ccc2c(c1O[C@@H]1CNCC1)CCC2 15322733
9794656 2907 0 None -5 3 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 233 3 1 3 1.9 COc1ccc2c(c1O[C@@H]1CNCC1)CCC2 15322733
136 3228 28 None -85 16 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
223 3228 28 None -85 16 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
643606 3228 28 None -85 16 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
CHEMBL10347 3228 28 None -85 16 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
155 718 20 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 15322733
155 718 20 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 9933142
163 718 20 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 15322733
163 718 20 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 9933142
62065 718 20 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 15322733
62065 718 20 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 9933142
CHEMBL6607 718 20 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 15322733
CHEMBL6607 718 20 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 9933142
DB01484 718 20 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 15322733
DB01484 718 20 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 9933142
219050 3309 21 None -194 21 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
52 3309 21 None -194 21 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
CHEMBL431367 3309 21 None -194 21 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
168 3907 11 None -3 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 15322733
6604042 3907 11 None -3 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 15322733
CHEMBL309760 3907 11 None -3 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 15322733
153 1426 5 None -25 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@@H](N)C)OC 15322733
6603801 1426 5 None -25 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@@H](N)C)OC 15322733
CHEMBL1434583 1426 5 None -25 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@@H](N)C)OC 15322733
1355 1972 82 None -1 16 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 8450835
142 1972 82 None -1 16 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 8450835
CHEMBL478 1972 82 None -1 16 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 8450835
DB12110 1972 82 None -1 16 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 8450835
102 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10455251
102 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8078486
102 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
3659 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10455251
3659 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8078486
3659 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
8969 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10455251
8969 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8078486
8969 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
CHEMBL15245 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10455251
CHEMBL15245 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8078486
CHEMBL15245 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
DB01392 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10455251
DB01392 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8078486
DB01392 4051 44 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
157 2030 5 None -134 5 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 12954071
9840090 2030 5 None -134 5 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 12954071
CHEMBL134519 2030 5 None -134 5 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 12954071
3652 4022 72 None -2 18 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
57 4022 72 None -2 18 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
60809 4022 72 None -2 18 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
CHEMBL21536 4022 72 None -2 18 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
DB15357 4022 72 None -2 18 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
108029 3349 50 None -15 13 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450835
23 3349 50 None -15 13 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450835
CHEMBL18785 3349 50 None -15 13 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450835
13878025 2384 0 None -19 3 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 3 2 4 2.4 CC(C(OC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C)O 8450835
184 2384 0 None -19 3 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 3 2 4 2.4 CC(C(OC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C)O 8450835
CHEMBL52422 2384 0 None -19 3 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 3 2 4 2.4 CC(C(OC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C)O 8450835
1355 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 11104741
1355 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 12970106
1355 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 15322733
1355 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9459568
1355 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9933142
142 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 11104741
142 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 12970106
142 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 15322733
142 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9459568
142 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9933142
CHEMBL478 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 11104741
CHEMBL478 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 12970106
CHEMBL478 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 15322733
CHEMBL478 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9459568
CHEMBL478 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9933142
DB12110 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 11104741
DB12110 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 12970106
DB12110 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 15322733
DB12110 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9459568
DB12110 1972 82 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9933142
5 139 66 None -29 55 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450835
5202 139 66 None -29 55 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450835
CHEMBL39 139 66 None -29 55 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450835
DB08839 139 66 None -29 55 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450835
107 141 116 None -12 31 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8450835
1833 141 116 None -12 31 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8450835
CHEMBL8165 141 116 None -12 31 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8450835
152 361 18 None -1 19 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8450835
2107 361 18 None -1 19 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8450835
CHEMBL275854 361 18 None -1 19 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8450835
199 389 0 None -5 5 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 8450835
9821951 389 0 None -5 5 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 8450835
CHEMBL160293 389 0 None -5 5 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 8450835
216 2809 29 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 11104741
9815618 2809 29 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 11104741
CHEMBL253811 2809 29 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 11104741
189 3423 31 None -5 18 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 15322733
189 3423 31 None -5 18 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 15466450
5163 3423 31 None -5 18 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 15322733
5163 3423 31 None -5 18 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 15466450
CHEMBL297784 3423 31 None -5 18 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 15322733
CHEMBL297784 3423 31 None -5 18 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 15466450
192 3433 46 None -10 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10188965
192 3433 46 None -10 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10737744
443390 3433 46 None -10 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10188965
443390 3433 46 None -10 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10737744
CHEMBL14276 3433 46 None -10 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10188965
CHEMBL14276 3433 46 None -10 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10737744
136 3228 28 None -12 16 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
223 3228 28 None -12 16 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
643606 3228 28 None -12 16 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
CHEMBL10347 3228 28 None -12 16 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
152 361 18 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15322733
152 361 18 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15466450
152 361 18 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8078486
2107 361 18 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15322733
2107 361 18 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15466450
2107 361 18 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8078486
CHEMBL275854 361 18 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15322733
CHEMBL275854 361 18 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15466450
CHEMBL275854 361 18 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8078486
5 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11104741
5 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 12954071
5 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15322733
5 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15466450
5 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8078486
5202 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11104741
5202 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 12954071
5202 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15322733
5202 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15466450
5202 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8078486
CHEMBL39 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11104741
CHEMBL39 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 12954071
CHEMBL39 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15322733
CHEMBL39 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15466450
CHEMBL39 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8078486
DB08839 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11104741
DB08839 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 12954071
DB08839 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15322733
DB08839 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15466450
DB08839 139 66 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8078486
183 2382 0 None -5 4 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 4 1 5 3.5 CC(C(O)C)OC(=O)[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C 8450835
3034814 2382 0 None -5 4 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 4 1 5 3.5 CC(C(O)C)OC(=O)[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C 8450835
CHEMBL1356280 2382 0 None -5 4 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 4 1 5 3.5 CC(C(O)C)OC(=O)[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C 8450835
133 2450 48 None -12 43 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8450835
1723 2450 48 None -12 43 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8450835
28693 2450 48 None -12 43 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8450835
CHEMBL19215 2450 48 None -12 43 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8450835
DB13520 2450 48 None -12 43 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8450835
134 2468 19 None -12 68 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450835
1775 2468 19 None -12 68 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450835
9681 2468 19 None -12 68 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450835
CHEMBL1065 2468 19 None -12 68 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450835
DB00247 2468 19 None -12 68 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450835
2105 2993 34 None -28 33 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
47811 2993 34 None -28 33 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
48 2993 34 None -28 33 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
CHEMBL531 2993 34 None -28 33 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
DB01186 2993 34 None -28 33 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
2601 3709 30 None -8 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
443951 3709 30 None -8 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
56 3709 30 None -8 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
CHEMBL73151 3709 30 None -8 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
DB13399 3709 30 None -8 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
10331436 321 7 None -25 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 12954071
160 321 7 None -25 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 12954071
CHEMBL133455 321 7 None -25 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 12954071
1621 2386 16 None -39 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12213075
17 2386 16 None -39 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12213075
5761 2386 16 None -39 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12213075
CHEMBL263881 2386 16 None -39 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12213075
DB04829 2386 16 None -39 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12213075
5074 3268 75 None -9 30 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8450835
97 3268 75 None -9 30 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8450835
CHEMBL267777 3268 75 None -9 30 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8450835
DB12693 3268 75 None -9 30 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8450835
10449757 3426 26 None 3 3 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10188965
190 3426 26 None 3 3 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10188965
CHEMBL2110371 3426 26 None 3 3 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10188965
1342 36 42 None -4 19 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8078486
1342 36 42 None -4 19 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8450835
3 36 42 None -4 19 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8078486
3 36 42 None -4 19 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8450835
CHEMBL277120 36 42 None -4 19 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8078486
CHEMBL277120 36 42 None -4 19 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8450835
135398737 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15322733
135398737 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9459568
135398737 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
38 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15322733
38 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9459568
38 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
722 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15322733
722 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9459568
722 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
CHEMBL42 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15322733
CHEMBL42 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9459568
CHEMBL42 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
DB00363 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15322733
DB00363 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9459568
DB00363 942 89 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
167 3364 0 None -3 5 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 7 0 5 3.6 Fc1ccc(cc1)C(=O)CC1CCN(C1)CCOc1cccc2c1OCCO2 9732398
9821498 3364 0 None -3 5 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 7 0 5 3.6 Fc1ccc(cc1)C(=O)CC1CCN(C1)CCOc1cccc2c1OCCO2 9732398
135409453 3702 38 None 2 2 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 15466450
226 3702 38 None 2 2 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 15466450
CHEMBL76370 3702 38 None 2 2 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 15466450
191 3429 47 None -1 3 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 15322733
443389 3429 47 None -1 3 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 15322733
CHEMBL276140 3429 47 None -1 3 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 15322733
206 2447 10 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 15107597
206 2447 10 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 15322733
206 2447 10 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9459568
68848 2447 10 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 15107597
68848 2447 10 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 15322733
68848 2447 10 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9459568
CHEMBL12314 2447 10 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 15107597
CHEMBL12314 2447 10 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 15322733
CHEMBL12314 2447 10 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9459568
1342 36 42 None 2 19 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8078486
1342 36 42 None 2 19 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 9459568
3 36 42 None 2 19 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8078486
3 36 42 None 2 19 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 9459568
CHEMBL277120 36 42 None 2 19 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8078486
CHEMBL277120 36 42 None 2 19 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 9459568
1043 1545 13 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11104741
1043 1545 13 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15322733
149 1545 13 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11104741
149 1545 13 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15322733
8223 1545 13 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11104741
8223 1545 13 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15322733
CHEMBL442 1545 13 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11104741
CHEMBL442 1545 13 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15322733
DB00696 1545 13 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11104741
DB00696 1545 13 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15322733
133 2450 48 None -2 43 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 15322733
1723 2450 48 None -2 43 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 15322733
28693 2450 48 None -2 43 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 15322733
CHEMBL19215 2450 48 None -2 43 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 15322733
DB13520 2450 48 None -2 43 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 15322733
37 764 56 None 1 17 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
460 764 56 None 1 17 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746 764 56 None 1 17 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
CHEMBL1201087 764 56 None 1 17 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
DB00248 764 56 None 1 17 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
1588 2284 24 None -8 44 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
28864 2284 24 None -8 44 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
43 2284 24 None -8 44 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL157138 2284 24 None -8 44 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB00589 2284 24 None -8 44 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
4106 2456 16 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 15322733
4106 2456 16 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9459568
5358812 2456 16 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 15322733
5358812 2456 16 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9459568
89 2456 16 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 15322733
89 2456 16 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9459568
CHEMBL93240 2456 16 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 15322733
CHEMBL93240 2456 16 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9459568
5074 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10188965
5074 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10455251
5074 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 15322733
5074 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9459568
97 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10188965
97 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10455251
97 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 15322733
97 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9459568
CHEMBL267777 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10188965
CHEMBL267777 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10455251
CHEMBL267777 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 15322733
CHEMBL267777 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9459568
DB12693 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10188965
DB12693 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10455251
DB12693 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 15322733
DB12693 3268 75 None -3 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9459568
183 2382 0 None 2 4 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 4 1 5 3.5 CC(C(O)C)OC(=O)[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C 9459568
3034814 2382 0 None 2 4 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 4 1 5 3.5 CC(C(O)C)OC(=O)[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C 9459568
CHEMBL1356280 2382 0 None 2 4 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 4 1 5 3.5 CC(C(O)C)OC(=O)[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C 9459568
154 2317 0 None -1 4 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 15322733
638252 2317 0 None -1 4 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 15322733
150 2463 18 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 11104741
150 2463 18 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 15322733
1764 2463 18 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 11104741
1764 2463 18 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 15322733
8226 2463 18 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 11104741
8226 2463 18 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 15322733
CHEMBL1201356 2463 18 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 11104741
CHEMBL1201356 2463 18 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 15322733
DB00353 2463 18 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 11104741
DB00353 2463 18 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 15322733