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 assesse