Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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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
134265828 180929 0 None 3162 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 231 2 1 3 1.8 CCCc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4765074 180929 0 None 3162 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 231 2 1 3 1.8 CCCc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
5 139 66 None -3 28 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C 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 -3 28 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C 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 -3 28 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C 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 -3 28 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C 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
5 139 66 None -3 28 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C 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 -3 28 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C 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 -3 28 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C 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 -3 28 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C 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
46228438 198292 0 None 1862 3 Human 10.0 pEC50 = 10 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C 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 10.0 pEC50 = 10 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1OC1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
11949712 200466 0 None 870 3 Human 10.0 pEC50 = 10 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C 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 870 3 Human 10.0 pEC50 = 10 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
134265616 163848 0 None 1548 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1016/j.bmcl.2021.127872
CHEMBL4213447 163848 0 None 1548 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1016/j.bmcl.2021.127872
134265616 163848 0 None 1548 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C 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 10.0 pEC50 = 10.0 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C 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
134265620 163843 0 None 426 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
CHEMBL4213379 163843 0 None 426 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
134265620 163843 0 None 426 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1016/j.bmcl.2021.127872
CHEMBL4213379 163843 0 None 426 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1016/j.bmcl.2021.127872
5 139 66 None -3 28 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor 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 -3 28 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor 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 -3 28 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor 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 -3 28 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor 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 -3 28 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor 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 -3 28 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor 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 -3 28 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor 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 -3 28 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor 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 -3 28 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 -3 28 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 -3 28 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 -3 28 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 -3 28 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 -3 28 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 -3 28 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 -3 28 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 -3 28 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
5202 139 66 None -3 28 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
CHEMBL39 139 66 None -3 28 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
DB08839 139 66 None -3 28 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
439280 119501 104 None 3 7 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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 -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
5202 139 66 None -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
CHEMBL39 139 66 None -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
DB08839 139 66 None -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
134265627 163450 0 None 194 3 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C 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 194 3 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C 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
5 139 66 None -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
5202 139 66 None -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
CHEMBL39 139 66 None -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
DB08839 139 66 None -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
5 139 66 None -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
5202 139 66 None -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
CHEMBL39 139 66 None -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
DB08839 139 66 None -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
162643595 181096 0 None 501 3 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 230 2 1 2 2.4 CCCc1cccc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4776557 181096 0 None 501 3 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 230 2 1 2 2.4 CCCc1cccc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
134147456 149089 0 None 999 3 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 230 2 1 2 2.4 CCCc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3947276 149089 0 None 999 3 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 230 2 1 2 2.4 CCCc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
16743289 59242 3 None 724 2 Human 9.7 pEC50 = 9.7 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell line
ChEMBL 200 2 1 2 2.1 NCCc1cn2c3c(cccc13)CCC2 10.1016/s0960-894x(00)00141-4
CHEMBL171774 59242 3 None 724 2 Human 9.7 pEC50 = 9.7 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell line
ChEMBL 200 2 1 2 2.1 NCCc1cn2c3c(cccc13)CCC2 10.1016/s0960-894x(00)00141-4
5 139 66 None -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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 -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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 -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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 -3 28 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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
10332474 59328 0 None 1513 2 Human 9.6 pEC50 = 9.6 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell line
ChEMBL 252 2 1 3 2.9 NCCc1cn2c3c(cc(Cl)cc13)SCC2 10.1016/s0960-894x(00)00141-4
CHEMBL172159 59328 0 None 1513 2 Human 9.6 pEC50 = 9.6 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell line
ChEMBL 252 2 1 3 2.9 NCCc1cn2c3c(cc(Cl)cc13)SCC2 10.1016/s0960-894x(00)00141-4
134152924 152964 0 None 251 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 248 2 1 3 2.5 CCSc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3979806 152964 0 None 251 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 248 2 1 3 2.5 CCSc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
5 139 66 None -3 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 -3 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 -3 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 -3 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 -3 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 -3 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 -3 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 -3 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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
168280316 192251 0 None 41 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5187275 192251 0 None 41 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221883 192251 0 None 41 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
5 139 66 None -3 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C 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 -3 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C 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 -3 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C 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 -3 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C 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
4106 2456 16 None 7 7 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2013.02.020
5358812 2456 16 None 7 7 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2013.02.020
89 2456 16 None 7 7 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2013.02.020
CHEMBL93240 2456 16 None 7 7 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2013.02.020
134265727 181193 0 None 794 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 245 2 1 3 2.0 CC(C)Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4777852 181193 0 None 794 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 245 2 1 3 2.0 CC(C)Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
76333762 84868 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at Homo sapiens (human) 5-HT2C receptor assessed as calcium mobilization by cell based assayAgonist activity at Homo sapiens (human) 5-HT2C receptor assessed as calcium mobilization by cell based assay
ChEMBL 248 0 1 2 3.6 Cc1c2n(c3c(C)c(Cl)ccc13)C(C)NCC2 10.1007/s00044-011-9615-3
CHEMBL2260569 84868 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at Homo sapiens (human) 5-HT2C receptor assessed as calcium mobilization by cell based assayAgonist activity at Homo sapiens (human) 5-HT2C receptor assessed as calcium mobilization by cell based assay
ChEMBL 248 0 1 2 3.6 Cc1c2n(c3c(C)c(Cl)ccc13)C(C)NCC2 10.1007/s00044-011-9615-3
5 139 66 None -3 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C 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 -3 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C 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 -3 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C 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 -3 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C 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 -3 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assayAgonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b01835
5202 139 66 None -3 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assayAgonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b01835
CHEMBL39 139 66 None -3 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assayAgonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b01835
DB08839 139 66 None -3 28 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assayAgonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b01835
4376990 192397 4 None 1 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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
146025687 183123 0 None 12 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4779260 183123 0 None 12 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803306 183123 0 None 12 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
146025687 183123 0 None 12 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4779260 183123 0 None 12 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803306 183123 0 None 12 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
134265735 181257 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2cncc3c2CC[C@@H]2CNCCN32)cc1 10.1016/j.bmcl.2021.127872
CHEMBL4778570 181257 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2cncc3c2CC[C@@H]2CNCCN32)cc1 10.1016/j.bmcl.2021.127872
46933845 15971 0 None 18 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor assessed as 5HT-induced calcium mobilization by FLIPR assayAgonist activity at human 5HT2C 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 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor assessed as 5HT-induced calcium mobilization by FLIPR assayAgonist activity at human 5HT2C 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
44572751 12378 1 None 16 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C 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 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C 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 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C 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
168289382 191187 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 2 4 4 2.8 COc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5198213 191187 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 2 4 4 2.8 COc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
134155852 150610 0 None 100 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 284 2 1 3 3.1 c1csc(Cc2cccc3c2CCC2CNCCN32)c1 10.1016/j.bmcl.2016.11.016
CHEMBL3959570 150610 0 None 100 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 284 2 1 3 3.1 c1csc(Cc2cccc3c2CCC2CNCCN32)c1 10.1016/j.bmcl.2016.11.016
18520432 151485 0 None 39 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 206 0 1 2 1.6 Fc1ccc2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3967107 151485 0 None 39 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 206 0 1 2 1.6 Fc1ccc2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
168289382 191187 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 2 4 4 2.8 COc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5198213 191187 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 2 4 4 2.8 COc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
5 139 66 None -3 28 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5202 139 66 None -3 28 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
CHEMBL39 139 66 None -3 28 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
DB08839 139 66 None -3 28 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5 139 66 None -3 28 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5202 139 66 None -3 28 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
CHEMBL39 139 66 None -3 28 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
DB08839 139 66 None -3 28 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
122442263 137816 0 None 15 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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 15 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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 15 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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
11949706 198362 0 None 1445 2 Human 9.0 pEC50 = 9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 359 4 1 4 3.4 C[C@@H]1CNCCN1c1ccc2c(n1)[C@@H](OCc1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.10.112
CHEMBL595645 198362 0 None 1445 2 Human 9.0 pEC50 = 9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 359 4 1 4 3.4 C[C@@H]1CNCCN1c1ccc2c(n1)[C@@H](OCc1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.10.112
11695000 88628 0 None 7 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337490 88628 0 None 7 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365083 88628 0 None 7 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
46884102 7964 0 None 128 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 366 5 2 3 3.7 CC1(C)CCC(Oc2cc(F)c(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
CHEMBL1091106 7964 0 None 128 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 366 5 2 3 3.7 CC1(C)CCC(Oc2cc(F)c(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
230 4043 18 None 3 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2C receptor expressed in CHO 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 9.0 pEC50 = 9 Functional
Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2C receptor expressed in CHO 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 9.0 pEC50 = 9 Functional
Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2C receptor expressed in CHO 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
134143977 150208 0 None 100 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 296 2 1 2 3.1 Fc1ccc2c(c1Cc1ccccc1)CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3956394 150208 0 None 100 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 296 2 1 2 3.1 Fc1ccc2c(c1Cc1ccccc1)CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
168293874 191571 0 None 1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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
122442263 137816 0 None 15 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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 15 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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 15 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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
11514226 88667 0 None 85 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337494 88667 0 None 85 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365470 88667 0 None 85 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
134265663 163116 0 None 19 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C 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 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C 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
134265665 164236 0 None 1047 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C 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 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C 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
146025687 183123 0 None 12 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4779260 183123 0 None 12 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803306 183123 0 None 12 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
146025687 183123 0 None 12 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4779260 183123 0 None 12 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803306 183123 0 None 12 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5-HT2C INI receptor 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-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
134265732 163244 0 None 776 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 285 2 1 3 2.3 FC(F)(F)CCc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4206126 163244 0 None 776 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 285 2 1 3 2.3 FC(F)(F)CCc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
134265665 164236 0 None 1047 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 231 2 1 3 1.8 CCCc1cncc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4218374 164236 0 None 1047 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 231 2 1 3 1.8 CCCc1cncc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
16047544 12524 7 None 3 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL1187185 12524 7 None 3 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL492916 12524 7 None 3 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
134265732 163244 0 None 776 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C 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 776 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C 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
16115517 84400 0 None 5 3 Human 8.9 pEC50 = 8.9 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.4 CCc1ccc2c(c1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL223468 84400 0 None 5 3 Human 8.9 pEC50 = 8.9 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.4 CCc1ccc2c(c1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
11952353 198168 0 None 1071 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C 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 1071 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C 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
134139964 145607 0 None 79 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 278 2 1 2 3.0 c1ccc(Cc2cccc3c2CCC2CNCCN32)cc1 10.1016/j.bmcl.2016.11.016
CHEMBL3919795 145607 0 None 79 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 278 2 1 2 3.0 c1ccc(Cc2cccc3c2CCC2CNCCN32)cc1 10.1016/j.bmcl.2016.11.016
162652937 183070 0 None 22 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 22 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 22 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
162652937 183070 0 None 22 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 22 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 22 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 -3 28 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2012.01.122
5202 139 66 None -3 28 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2012.01.122
CHEMBL39 139 66 None -3 28 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2012.01.122
DB08839 139 66 None -3 28 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2012.01.122
5 139 66 None -3 28 Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2C 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 -3 28 Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2C 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 -3 28 Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2C 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 -3 28 Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2C 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
152 361 18 None 1 6 Rat 8.7 pEC50 = 8.7 Functional
Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cellsActivity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
2107 361 18 None 1 6 Rat 8.7 pEC50 = 8.7 Functional
Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cellsActivity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
CHEMBL275854 361 18 None 1 6 Rat 8.7 pEC50 = 8.7 Functional
Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cellsActivity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
46230099 197622 0 None 25 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 251 0 2 3 1.2 O=C1NC2CCNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
CHEMBL590483 197622 0 None 25 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 251 0 2 3 1.2 O=C1NC2CCNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
11658860 2302 47 None 2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
2941 2302 47 None 2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
4374 2302 47 None 2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
CHEMBL360328 2302 47 None 2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
DB04871 2302 47 None 2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
9901086 187038 28 None 54 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
CHEMBL494947 187038 28 None 54 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
168291775 191299 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 314 1 4 3 3.5 Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5200026 191299 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 314 1 4 3 3.5 Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
9901086 187038 28 None 54 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
CHEMBL494947 187038 28 None 54 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
168291775 191299 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 314 1 4 3 3.5 Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5200026 191299 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 314 1 4 3 3.5 Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
134265831 179428 0 None 19 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 203 0 1 3 1.1 Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4747291 179428 0 None 19 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 203 0 1 3 1.1 Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
112713234 146905 1 None 15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 202 0 1 2 1.7 Cc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3930174 146905 1 None 15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 202 0 1 2 1.7 Cc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
16115271 78683 0 None 1 3 Human 8.0 pEC50 = 8 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C 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 8.0 pEC50 = 8 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C 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
46228437 198291 0 None 6 3 Human 8.0 pEC50 = 8 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL595194 198291 0 None 6 3 Human 8.0 pEC50 = 8 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
24826868 90637 1 None -1 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 236 0 1 2 1.3 O=C1c2cc(Cl)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397877 90637 1 None -1 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 236 0 1 2 1.3 O=C1c2cc(Cl)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
162665030 183135 0 None 38 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4782824 183135 0 None 38 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803449 183135 0 None 38 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
44572800 12529 3 None 5 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1 10.1021/jm801354e
CHEMBL1187194 12529 3 None 5 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1 10.1021/jm801354e
CHEMBL493128 12529 3 None 5 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1 10.1021/jm801354e
23395431 94459 0 None 10 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 C[C@@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
CHEMBL254215 94459 0 None 10 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 C[C@@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
10331841 168627 6 None 46 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C 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 46 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1021/jm0709034
157292621 192359 0 None 5 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 268 1 2 3 2.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5199923 192359 0 None 5 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 268 1 2 3 2.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222513 192359 0 None 5 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 268 1 2 3 2.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
45485742 196136 0 None 18 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 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 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 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
90644511 111161 13 None 6 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 282 3 2 4 2.4 CNc1nc(Cc2ccccc2)nc2c1CCNC[C@@H]2C 10.1021/jm5003292
CHEMBL3286556 111161 13 None 6 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 282 3 2 4 2.4 CNc1nc(Cc2ccccc2)nc2c1CCNC[C@@H]2C 10.1021/jm5003292
134146228 148628 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 300 1 1 3 3.1 COc1cc2c(c(Cl)c1Cl)N1CCCNC[C@H]1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3943620 148628 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 300 1 1 3 3.1 COc1cc2c(c(Cl)c1Cl)N1CCCNC[C@H]1CC2 10.1016/j.bmcl.2016.11.016
157292621 192359 0 None 5 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 268 1 2 3 2.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5199923 192359 0 None 5 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 268 1 2 3 2.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222513 192359 0 None 5 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 268 1 2 3 2.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
162665030 183135 0 None 38 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4782824 183135 0 None 38 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803449 183135 0 None 38 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
25070582 61110 21 None 2 9 Dog 8.0 pEC50 = 8.0 Functional
Agonist activity at dog 5HT2C receptorAgonist activity at dog 5HT2C receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 61110 21 None 2 9 Dog 8.0 pEC50 = 8.0 Functional
Agonist activity at dog 5HT2C receptorAgonist activity at dog 5HT2C receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
146025684 183043 0 None 6 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
146025688 183102 0 None 20 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4761064 183102 0 None 20 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803134 183102 0 None 20 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
134265705 163528 0 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 189 0 1 3 0.8 c1cnc2c(c1)CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4209572 163528 0 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 189 0 1 3 0.8 c1cnc2c(c1)CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
162676809 183200 0 None 5 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4799299 183200 0 None 5 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4804137 183200 0 None 5 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
25070581 61117 0 None 1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C 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 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C 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
71562661 86865 0 None 3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
CHEMBL2331794 86865 0 None 3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
134144277 150174 0 None 63 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 280 2 1 3 3.2 c1ccc(Oc2cccc3c2CCC2CNCCN32)cc1 10.1016/j.bmcl.2016.11.016
CHEMBL3956136 150174 0 None 63 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 280 2 1 3 3.2 c1ccc(Oc2cccc3c2CCC2CNCCN32)cc1 10.1016/j.bmcl.2016.11.016
19036360 107015 0 None - 1 Rat 7.0 pEC50 = 7 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 270 3 1 3 3.2 COc1ccc2c(c1)-c1c(ccn1CC(C)N)C2(C)C 10.1021/jm970030l
CHEMBL318639 107015 0 None - 1 Rat 7.0 pEC50 = 7 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 270 3 1 3 3.2 COc1ccc2c(c1)-c1c(ccn1CC(C)N)C2(C)C 10.1021/jm970030l
3288856 192201 2 None -3 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 284 1 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5176057 192201 2 None -3 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 284 1 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5221496 192201 2 None -3 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 284 1 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
132820208 149114 0 None -2 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 232 1 1 3 1.8 COc1cccc2c1CC[C@@H]1CNCCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3947432 149114 0 None -2 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 232 1 1 3 1.8 COc1cccc2c1CC[C@@H]1CNCCCN21 10.1016/j.bmcl.2016.11.016
10609802 106695 2 None 1 2 Rat 6.0 pEC50 = 6 Functional
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptor
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2 10.1021/jm970219x
CHEMBL316527 106695 2 None 1 2 Rat 6.0 pEC50 = 6 Functional
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptor
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2 10.1021/jm970219x
10560133 106840 0 None - 1 Rat 5.0 pEC50 = 5 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 204 3 1 3 2.0 COc1ccc2c(ccn2CC(C)N)c1 10.1021/jm970030l
CHEMBL317564 106840 0 None - 1 Rat 5.0 pEC50 = 5 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 204 3 1 3 2.0 COc1ccc2c(ccn2CC(C)N)c1 10.1021/jm970030l
3288856 192201 2 None -3 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 284 1 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5176057 192201 2 None -3 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 284 1 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5221496 192201 2 None -3 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 284 1 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
162669817 183155 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@@H]3C[C@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4789175 183155 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@@H]3C[C@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803726 183155 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@@H]3C[C@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
45485787 195650 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 378 5 1 6 1.5 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1Br 10.1016/j.bmcl.2009.07.136
CHEMBL568897 195650 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 378 5 1 6 1.5 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1Br 10.1016/j.bmcl.2009.07.136
162669817 183155 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@@H]3C[C@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4789175 183155 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@@H]3C[C@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803726 183155 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@@H]3C[C@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
137631035 160588 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4101194 160588 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4117313 160588 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
71562661 86865 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
CHEMBL2331794 86865 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
45484785 196073 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assay
ChEMBL 328 6 1 6 1.4 Cc1cc(=O)n(CCCOc2ccccc2)c(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.133
CHEMBL571733 196073 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assay
ChEMBL 328 6 1 6 1.4 Cc1cc(=O)n(CCCOc2ccccc2)c(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.133
118733766 120114 0 None 33 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416035 120114 0 None 33 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546870 120114 0 None 33 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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
137631035 160588 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4101194 160588 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4117313 160588 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
45484866 195567 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assay
ChEMBL 366 5 1 6 2.0 CCn1c(COc2cc(F)ccc2Cl)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
CHEMBL568437 195567 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assay
ChEMBL 366 5 1 6 2.0 CCn1c(COc2cc(F)ccc2Cl)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
11983273 77627 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Induction of 5HT2C receptor mediated increase in intracellular calcium concentration in HEK293 cellsInduction of 5HT2C receptor mediated increase in intracellular calcium concentration in HEK293 cells
ChEMBL 256 1 1 2 2.5 FC(F)(F)c1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209714 77627 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Induction of 5HT2C receptor mediated increase in intracellular calcium concentration in HEK293 cellsInduction of 5HT2C receptor mediated increase in intracellular calcium concentration in HEK293 cells
ChEMBL 256 1 1 2 2.5 FC(F)(F)c1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
137655846 158132 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 349 3 1 3 4.3 Cc1cc(-c2cccc3ccccc23)oc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4093102 158132 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 349 3 1 3 4.3 Cc1cc(-c2cccc3ccccc23)oc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
122461343 137821 0 None 9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769704 137821 0 None 9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771398 137821 0 None 9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL4742882 212282 2 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 None None None Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL4802403 212282 2 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 None None None Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
122461343 137821 0 None 9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769704 137821 0 None 9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771398 137821 0 None 9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
137635172 155270 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 337 2 1 4 3.3 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCNCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4059943 155270 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 337 2 1 4 3.3 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCNCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4742882 212282 2 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 None None None Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL4802403 212282 2 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 None None None Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
168290156 192353 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 301 1 2 2 3.6 Fc1ncccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5194324 192353 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 301 1 2 2 3.6 Fc1ncccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222484 192353 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 301 1 2 2 3.6 Fc1ncccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
168277051 192225 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5178562 192225 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221669 192225 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
155553235 175965 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@@H]1C[C@@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4544700 175965 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@@H]1C[C@@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4597226 175965 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@@H]1C[C@@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
11231392 84456 0 None 4 3 Human 7.0 pEC50 = 7.0 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.6 CC(C)Oc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL223628 84456 0 None 4 3 Human 7.0 pEC50 = 7.0 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.6 CC(C)Oc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
45484687 196777 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells 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 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells 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
1534 102553 51 None -5 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 102553 51 None -5 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 102553 51 None -5 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
1534 102553 51 None -5 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 102553 51 None -5 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 102553 51 None -5 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
122461993 137818 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769581 137818 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771395 137818 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
168277051 192225 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5178562 192225 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221669 192225 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
168290156 192353 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 301 1 2 2 3.6 Fc1ncccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5194324 192353 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 301 1 2 2 3.6 Fc1ncccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222484 192353 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 301 1 2 2 3.6 Fc1ncccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
155553235 175965 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@@H]1C[C@@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4544700 175965 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@@H]1C[C@@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4597226 175965 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@@H]1C[C@@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
58911532 90659 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 244 2 1 2 1.6 CCCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397899 90659 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 244 2 1 2 1.6 CCCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
122461993 137818 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769581 137818 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771395 137818 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
118733776 120126 0 None 2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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
16115652 83064 0 None 15 3 Human 8.0 pEC50 = 8.0 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C 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 8.0 pEC50 = 8.0 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C 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
11630623 88656 0 None 151 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C 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 151 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C 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 151 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C 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
118733818 120140 0 None 93 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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 93 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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 93 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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
146025684 183043 0 None 6 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
146025688 183102 0 None 20 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4761064 183102 0 None 20 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803134 183102 0 None 20 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
44572168 12363 1 None 1 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C 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 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C 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 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C 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
44626357 195865 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 382 5 1 6 2.1 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2C(F)(F)F)n1 10.1016/j.bmcl.2009.07.136
CHEMBL570274 195865 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 382 5 1 6 2.1 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2C(F)(F)F)n1 10.1016/j.bmcl.2009.07.136
11658860 2302 47 None 2 4 Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C 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 2 4 Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C 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 2 4 Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C 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 2 4 Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C 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 2 4 Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C 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
10465263 63986 55 None 19 3 Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C 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 19 3 Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C 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
10036629 64291 0 None 7 3 Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C 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 7 3 Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C 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
9994008 165585 0 None 3 3 Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCC1CNCCc2cc(OC)c(Br)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL426235 165585 0 None 3 3 Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCC1CNCCc2cc(OC)c(Br)cc21 10.1016/j.bmcl.2004.12.080
44414290 78003 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inhibition of 5HT2C assessed as intracellular calcium concentrationInhibition of 5HT2C assessed as intracellular calcium concentration
ChEMBL 193 0 1 1 2.2 Clc1ccc2c(c1)C[C@@H]1CNC[C@H]21 10.1016/j.bmcl.2006.04.070
CHEMBL211153 78003 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inhibition of 5HT2C assessed as intracellular calcium concentrationInhibition of 5HT2C assessed as intracellular calcium concentration
ChEMBL 193 0 1 1 2.2 Clc1ccc2c(c1)C[C@@H]1CNC[C@H]21 10.1016/j.bmcl.2006.04.070
54584720 61111 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 3 1 3 2.0 c1ccc(CCc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770374 61111 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 3 1 3 2.0 c1ccc(CCc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
46230094 197621 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 237 0 2 3 0.8 O=C1NC2CNCCN2c2ccc(Cl)cc21 10.1016/j.bmcl.2009.12.014
CHEMBL590482 197621 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 237 0 2 3 0.8 O=C1NC2CNCCN2c2ccc(Cl)cc21 10.1016/j.bmcl.2009.12.014
155512645 169105 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5-HT2C receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.3 CC(c1ccccc1)c1cc2c(nn1)CCNCC2 10.1016/j.bmcl.2016.06.060
CHEMBL4437696 169105 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5-HT2C receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.3 CC(c1ccccc1)c1cc2c(nn1)CCNCC2 10.1016/j.bmcl.2016.06.060
45484865 196644 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assay
ChEMBL 339 5 1 7 1.1 CCn1c(COc2cccc(C#N)c2)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
CHEMBL576253 196644 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assay
ChEMBL 339 5 1 7 1.1 CCn1c(COc2cccc(C#N)c2)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
59312249 111168 0 None 8 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C 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 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C 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
162652562 183065 0 None 4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4752604 183065 0 None 4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4802785 183065 0 None 4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
168292007 192376 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 278 1 3 2 3.4 Cc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5200288 192376 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 278 1 3 2 3.4 Cc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222607 192376 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 278 1 3 2 3.4 Cc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
118733804 120129 0 None 4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3416054 120129 0 None 4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3546906 120129 0 None 4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
162652562 183065 0 None 4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4752604 183065 0 None 4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4802785 183065 0 None 4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
168292007 192376 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 278 1 3 2 3.4 Cc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5200288 192376 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 278 1 3 2 3.4 Cc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222607 192376 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 278 1 3 2 3.4 Cc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
45485764 196141 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 325 5 1 7 0.6 N#Cc1ccccc1OCCn1nc(N2CCNCC2)ccc1=O 10.1016/j.bmcl.2009.07.136
CHEMBL572253 196141 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 325 5 1 7 0.6 N#Cc1ccccc1OCCn1nc(N2CCNCC2)ccc1=O 10.1016/j.bmcl.2009.07.136
162659576 183105 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
CHEMBL4762960 183105 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
CHEMBL4803163 183105 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
122442272 137807 0 None 19 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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 19 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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 19 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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
122442268 137812 0 None 7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769633 137812 0 None 7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771389 137812 0 None 7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
162659576 183105 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
CHEMBL4762960 183105 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
CHEMBL4803163 183105 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
44573226 192560 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 404 4 1 4 2.7 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCC(Oc2ccccc2F)CC1 10.1016/j.bmcl.2009.02.071
CHEMBL523169 192560 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 404 4 1 4 2.7 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCC(Oc2ccccc2F)CC1 10.1016/j.bmcl.2009.02.071
122442272 137807 0 None 19 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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 19 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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 19 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI 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
122442268 137812 0 None 7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769633 137812 0 None 7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771389 137812 0 None 7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
3549735 191599 2 None 6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 300 1 2 1 4.2 Fc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5204651 191599 2 None 6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 300 1 2 1 4.2 Fc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
3549735 191599 2 None 6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 300 1 2 1 4.2 Fc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5204651 191599 2 None 6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 300 1 2 1 4.2 Fc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
44572308 12436 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 252 5 2 2 3.4 NC[C@H]1C[C@@H]1c1cccc(NCc2ccccc2)c1 10.1021/jm801354e
CHEMBL1186720 12436 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 252 5 2 2 3.4 NC[C@H]1C[C@@H]1c1cccc(NCc2ccccc2)c1 10.1021/jm801354e
CHEMBL475384 12436 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 252 5 2 2 3.4 NC[C@H]1C[C@@H]1c1cccc(NCc2ccccc2)c1 10.1021/jm801354e
137632218 155750 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 342 2 0 4 3.6 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4065444 155750 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 342 2 0 4 3.6 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
44572306 12420 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 3.0 NC[C@H]1C[C@@H]1c1ccc(-c2ccco2)cc1 10.1021/jm801354e
CHEMBL1186669 12420 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 3.0 NC[C@H]1C[C@@H]1c1ccc(-c2ccco2)cc1 10.1021/jm801354e
CHEMBL474206 12420 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 3.0 NC[C@H]1C[C@@H]1c1ccc(-c2ccco2)cc1 10.1021/jm801354e
11300712 141142 0 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C 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 7.9 pEC50 = 7.9 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C 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
11579853 88642 0 None 70 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337504 88642 0 None 70 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365200 88642 0 None 70 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
58911582 90654 0 None 16 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397894 90654 0 None 16 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
24826871 90667 0 None 85 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397907 90667 0 None 85 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
162657053 183089 0 None 20 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
44573160 186829 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 392 4 1 4 2.5 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CC(Oc2cccc(Cl)c2)C1 10.1016/j.bmcl.2009.02.071
CHEMBL493757 186829 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 392 4 1 4 2.5 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CC(Oc2cccc(Cl)c2)C1 10.1016/j.bmcl.2009.02.071
137645674 157454 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 348 3 2 2 4.0 Cc1[nH]c(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4085497 157454 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 348 3 2 2 4.0 Cc1[nH]c(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
137642857 157900 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 373 4 0 4 4.9 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)Cc1cccnc1 10.1021/acs.jmedchem.7b00385
CHEMBL4090637 157900 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 373 4 0 4 4.9 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)Cc1cccnc1 10.1021/acs.jmedchem.7b00385
155540515 175878 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4516935 175878 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4596490 175878 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
3906894 101496 17 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity for 5-HT2c (5-HT2C) by measuring [3H]inositol monophosphate fromation in CHO cells in which the human 5-HT2C receptor subtype was stably expressedAgonistic activity for 5-HT2c (5-HT2C) by measuring [3H]inositol monophosphate fromation in CHO cells in which the human 5-HT2C receptor subtype was stably expressed
ChEMBL 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1016/s0960-894x(00)00400-5
CHEMBL301466 101496 17 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity for 5-HT2c (5-HT2C) by measuring [3H]inositol monophosphate fromation in CHO cells in which the human 5-HT2C receptor subtype was stably expressedAgonistic activity for 5-HT2c (5-HT2C) by measuring [3H]inositol monophosphate fromation in CHO cells in which the human 5-HT2C receptor subtype was stably expressed
ChEMBL 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1016/s0960-894x(00)00400-5
44404883 71703 26 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2C receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2C receptor determined by phosphoinositide hydrolysis assay
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL197664 71703 26 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2C receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2C receptor determined by phosphoinositide hydrolysis assay
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
17954204 63592 20 None 7 3 Human 7.9 pEC50 = 7.9 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C 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 7 3 Human 7.9 pEC50 = 7.9 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C 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
10331841 168627 6 None 46 3 Human 7.9 pEC50 = 7.9 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C 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 46 3 Human 7.9 pEC50 = 7.9 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C 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
162657053 183089 0 None 20 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor 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-HT2C receptor 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
134265618 163492 0 None 204 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNCC1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4209052 163492 0 None 204 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNCC1CC2 10.1021/acsmedchemlett.8b00328
155540515 175878 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4516935 175878 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4596490 175878 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
17954204 63592 20 None 7 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C 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 7 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C 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 19 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C 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 19 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL4790446 212290 2 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL4803723 212290 2 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
1355 1972 82 None 4 6 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2016.11.016
142 1972 82 None 4 6 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2016.11.016
CHEMBL478 1972 82 None 4 6 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2016.11.016
DB12110 1972 82 None 4 6 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2016.11.016
16747713 87588 0 None -6 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2C receptor expressed in rat SR3T3 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2C receptor expressed in rat SR3T3 cells assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 263 4 1 4 1.6 COCc1c2c(c(C[C@@H](C)N)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
CHEMBL234464 87588 0 None -6 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2C receptor expressed in rat SR3T3 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2C receptor expressed in rat SR3T3 cells assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 263 4 1 4 1.6 COCc1c2c(c(C[C@@H](C)N)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
CHEMBL4790446 212290 2 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL4803723 212290 2 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
137629964 160467 0 None 21 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 6 1 2 2.7 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CNC 10.1021/acs.jmedchem.7b00584
CHEMBL4098721 160467 0 None 21 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 6 1 2 2.7 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CNC 10.1021/acs.jmedchem.7b00584
CHEMBL4116380 160467 0 None 21 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 6 1 2 2.7 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CNC 10.1021/acs.jmedchem.7b00584
46228430 198046 0 None 4 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL593545 198046 0 None 4 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
137646604 160656 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 291 6 1 3 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1cccs1 10.1021/acs.jmedchem.7b00584
CHEMBL4085380 160656 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 291 6 1 3 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1cccs1 10.1021/acs.jmedchem.7b00584
CHEMBL4117915 160656 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 291 6 1 3 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1cccs1 10.1021/acs.jmedchem.7b00584
27559 201709 9 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
CHEMBL6557 201709 9 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
70693926 74095 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 217 5 1 2 2.5 NC[C@H]1C[C@@H]1c1ccccc1OCC1CC1 10.1021/ml200206z
CHEMBL2022189 74095 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 217 5 1 2 2.5 NC[C@H]1C[C@@H]1c1ccccc1OCC1CC1 10.1021/ml200206z
CHEMBL2027896 74095 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 217 5 1 2 2.5 NC[C@H]1C[C@@H]1c1ccccc1OCC1CC1 10.1021/ml200206z
7153 97557 74 None -1 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O 10.1016/j.bmc.2007.10.100
CHEMBL272942 97557 74 None -1 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O 10.1016/j.bmc.2007.10.100
137628797 160431 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4103313 160431 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116143 160431 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC 10.1021/acs.jmedchem.7b00584
137646604 160656 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 291 6 1 3 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1cccs1 10.1021/acs.jmedchem.7b00584
CHEMBL4085380 160656 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 291 6 1 3 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1cccs1 10.1021/acs.jmedchem.7b00584
CHEMBL4117915 160656 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 291 6 1 3 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1cccs1 10.1021/acs.jmedchem.7b00584
46228423 198363 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 360 4 1 6 3.3 Clc1cccc(COc2nc(N3CCNCC3)nc3sccc23)c1 10.1016/j.bmcl.2009.10.112
CHEMBL595646 198363 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 360 4 1 6 3.3 Clc1cccc(COc2nc(N3CCNCC3)nc3sccc23)c1 10.1016/j.bmcl.2009.10.112
137628895 160419 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)cc1 10.1021/acs.jmedchem.7b00584
CHEMBL4078425 160419 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)cc1 10.1021/acs.jmedchem.7b00584
CHEMBL4115999 160419 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)cc1 10.1021/acs.jmedchem.7b00584
72197308 102004 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAgonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 290 2 1 6 -0.0 CN1CCN(c2nc3c(c(N(C)C)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
CHEMBL2393233 102004 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAgonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 290 2 1 6 -0.0 CN1CCN(c2nc3c(c(N(C)C)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
CHEMBL3040291 102004 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAgonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 290 2 1 6 -0.0 CN1CCN(c2nc3c(c(N(C)C)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
14515726 86863 5 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 168 1 1 4 0.4 COc1noc2c1CCNCC2 10.1021/jm301656h
CHEMBL2331792 86863 5 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 168 1 1 4 0.4 COc1noc2c1CCNCC2 10.1021/jm301656h
137628895 160419 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)cc1 10.1021/acs.jmedchem.7b00584
CHEMBL4078425 160419 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)cc1 10.1021/acs.jmedchem.7b00584
CHEMBL4115999 160419 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)cc1 10.1021/acs.jmedchem.7b00584
14515726 86863 5 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 168 1 1 4 0.4 COc1noc2c1CCNCC2 10.1021/jm301656h
CHEMBL2331792 86863 5 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 168 1 1 4 0.4 COc1noc2c1CCNCC2 10.1021/jm301656h
137628797 160431 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4103313 160431 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116143 160431 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC 10.1021/acs.jmedchem.7b00584
70681346 74099 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 231 5 1 2 2.9 NC[C@H]1C[C@@H]1c1ccccc1OCC1CCC1 10.1021/ml200206z
CHEMBL2022190 74099 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 231 5 1 2 2.9 NC[C@H]1C[C@@H]1c1ccccc1OCC1CCC1 10.1021/ml200206z
CHEMBL2027922 74099 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 231 5 1 2 2.9 NC[C@H]1C[C@@H]1c1ccccc1OCC1CCC1 10.1021/ml200206z
118733764 120120 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C 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
3356430 192434 2 None -3 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5208864 192434 2 None -3 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222941 192434 2 None -3 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
27559 201709 9 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
CHEMBL6557 201709 9 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
3356430 192434 2 None -3 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5208864 192434 2 None -3 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222941 192434 2 None -3 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
25070907 61113 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C 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
45484682 196684 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 323 2 1 4 2.0 O=c1cc2c(nn1Cc1ccc(C(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL576651 196684 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 323 2 1 4 2.0 O=c1cc2c(nn1Cc1ccc(C(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
134136722 142100 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 270 2 1 2 3.1 c1cc(CC2CCC2)c2c(c1)N1CCCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3891704 142100 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 270 2 1 2 3.1 c1cc(CC2CCC2)c2c(c1)N1CCCNCC1CC2 10.1016/j.bmcl.2016.11.016
134136932 142112 0 None 7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 216 0 1 2 2.2 c1ccc2c(c1)CCC1CCNCCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3891802 142112 0 None 7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 216 0 1 2 2.2 c1ccc2c(c1)CCC1CCNCCCN21 10.1016/j.bmcl.2016.11.016
134133531 143051 0 None 19 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 264 1 1 2 3.1 c1ccc(-c2cccc3c2CCC2CNCCN32)cc1 10.1016/j.bmcl.2016.11.016
CHEMBL3899449 143051 0 None 19 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 264 1 1 2 3.1 c1ccc(-c2cccc3c2CCC2CNCCN32)cc1 10.1016/j.bmcl.2016.11.016
10774796 79250 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 210 2 1 2 2.3 C[C@@H](N)Cn1ccc2cc(F)c(F)cc21 10.1021/jm970030l
CHEMBL2115252 79250 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 210 2 1 2 2.3 C[C@@H](N)Cn1ccc2cc(F)c(F)cc21 10.1021/jm970030l
46228441 198173 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 246 3 1 6 0.6 CCCn1cnc2c(N3CCNCC3)ncnc21 10.1016/j.bmcl.2009.10.112
CHEMBL594489 198173 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 246 3 1 6 0.6 CCCn1cnc2c(N3CCNCC3)ncnc21 10.1016/j.bmcl.2009.10.112
118733812 120117 0 None 4 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
CHEMBL3416058 120117 0 None 4 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
CHEMBL3546873 120117 0 None 4 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
24773648 64079 2 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 191 1 1 2 1.9 COc1ccc2c(c1)CCNCC2C 10.1021/jm0709034
CHEMBL181324 64079 2 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 191 1 1 2 1.9 COc1ccc2c(c1)CCNCC2C 10.1021/jm0709034
168286082 192311 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 273 1 2 3 3.0 Fc1ccc2[nH]c3c(c2c1)CCNC3c1nccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5191954 192311 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 273 1 2 3 3.0 Fc1ccc2[nH]c3c(c2c1)CCNC3c1nccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5222230 192311 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor stably 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 5HT2C receptor stably 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 273 1 2 3 3.0 Fc1ccc2[nH]c3c(c2c1)CCNC3c1nccs1 10.1021/acsmedchemlett.1c00694
134153263 152250 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 216 0 1 2 2.1 CC1(C)CC2CNCCN2c2ccccc21 10.1016/j.bmcl.2016.11.016
CHEMBL3973690 152250 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 216 0 1 2 2.1 CC1(C)CC2CNCCN2c2ccccc21 10.1016/j.bmcl.2016.11.016
10631592 205454 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 192 2 1 2 2.1 CC(N)Cn1ccc2c(F)cccc21 10.1021/jm970030l