Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Assay
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
134265828 181627 None 0 Human Functional pEC50 = 10.2 10.2 3162 2
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 181627 None 0 Human Functional pEC50 = 10.2 10.2 3162 2
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 None 45 Human Functional pEC50 = 10.1 10.1 -2 26
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 None 45 Human Functional pEC50 = 10.1 10.1 -2 26
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 None 45 Human Functional pEC50 = 10.1 10.1 -2 26
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 None 45 Human Functional pEC50 = 10.1 10.1 -2 26
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 None 45 Human Functional pEC50 = 10.1 10.1 -2 26
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 None 45 Human Functional pEC50 = 10.1 10.1 -2 26
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 None 45 Human Functional pEC50 = 10.1 10.1 -2 26
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 None 45 Human Functional pEC50 = 10.1 10.1 -2 26
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 202441 None 0 Human Functional pEC50 = 10 10.0 1862 3
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 202441 None 0 Human Functional pEC50 = 10 10.0 1862 3
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 204618 None 0 Human Functional pEC50 = 10 10.0 870 3
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 204618 None 0 Human Functional pEC50 = 10 10.0 870 3
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 164506 None 0 Human Functional pEC50 = 10 10.0 1548 2
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 164506 None 0 Human Functional pEC50 = 10 10.0 1548 2
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 164506 None 0 Human Functional pEC50 = 10.0 10.0 1548 2
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 164506 None 0 Human Functional pEC50 = 10.0 10.0 1548 2
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 164501 None 0 Human Functional pEC50 = 9.9 9.9 426 3
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 164501 None 0 Human Functional pEC50 = 9.9 9.9 426 3
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
5 139 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
5202 139 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
CHEMBL39 139 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
DB08839 139 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
134265620 164501 None 0 Human Functional pEC50 = 9.9 9.9 426 3
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 164501 None 0 Human Functional pEC50 = 9.9 9.9 426 3
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 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
5202 139 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
CHEMBL39 139 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
DB08839 139 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
5 139 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
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 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
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 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
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 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
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 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
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 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
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 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
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 None 45 Human Functional pEC50 = 9.9 9.9 -2 26
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 None 45 Human Functional pEC50 = 9.8 9.8 -2 26
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 None 45 Human Functional pEC50 = 9.8 9.8 -2 26
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 None 45 Human Functional pEC50 = 9.8 9.8 -2 26
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 None 45 Human Functional pEC50 = 9.8 9.8 -2 26
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 None 45 Human Functional pEC50 = 9.8 9.8 -2 26
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 None 45 Human Functional pEC50 = 9.8 9.8 -2 26
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 None 45 Human Functional pEC50 = 9.8 9.8 -2 26
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 None 45 Human Functional pEC50 = 9.8 9.8 -2 26
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 None 45 Human Functional pEC50 = 9.8 9.8 -2 26
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 None 45 Human Functional pEC50 = 9.8 9.8 -2 26
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 None 45 Human Functional pEC50 = 9.8 9.8 -2 26
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 None 45 Human Functional pEC50 = 9.8 9.8 -2 26
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 120083 None 57 Human Functional pEC50 = 9.7 9.7 9 9
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 120083 None 57 Human Functional pEC50 = 9.7 9.7 9 9
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 120083 None 57 Human Functional pEC50 = 9.7 9.7 9 9
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 164108 None 0 Human Functional pEC50 = 9.7 9.7 194 3
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 164108 None 0 Human Functional pEC50 = 9.7 9.7 194 3
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 181794 None 0 Human Functional pEC50 = 9.7 9.7 501 3
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 181794 None 0 Human Functional pEC50 = 9.7 9.7 501 3
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 149721 None 0 Human Functional pEC50 = 9.7 9.7 999 3
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 149721 None 0 Human Functional pEC50 = 9.7 9.7 999 3
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 59588 None 2 Human Functional pEC50 = 9.7 9.7 724 2
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 59588 None 2 Human Functional pEC50 = 9.7 9.7 724 2
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 None 45 Human Functional pEC50 = 9.7 9.7 -2 26
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 120083 None 57 Human Functional pEC50 = 9.7 9.7 9 9
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 120083 None 57 Human Functional pEC50 = 9.7 9.7 9 9
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 120083 None 57 Human Functional pEC50 = 9.7 9.7 9 9
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 59675 None 0 Human Functional pEC50 = 9.6 9.6 1513 2
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 59675 None 0 Human Functional pEC50 = 9.6 9.6 1513 2
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 153599 None 0 Human Functional pEC50 = 9.5 9.5 251 2
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 153599 None 0 Human Functional pEC50 = 9.5 9.5 251 2
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 None 45 Human Functional pEC50 = 9.5 9.5 -2 26
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 None 45 Human Functional pEC50 = 9.5 9.5 -2 26
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 None 45 Human Functional pEC50 = 9.5 9.5 -2 26
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 None 45 Human Functional pEC50 = 9.5 9.5 -2 26
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 None 45 Human Functional pEC50 = 9.5 9.5 -2 26
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 None 45 Human Functional pEC50 = 9.5 9.5 -2 26
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 None 45 Human Functional pEC50 = 9.5 9.5 -2 26
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 None 45 Human Functional pEC50 = 9.5 9.5 -2 26
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 192972 None 0 Human Functional pEC50 = 9.5 9.5 41 2
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 192972 None 0 Human Functional pEC50 = 9.5 9.5 41 2
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 192972 None 0 Human Functional pEC50 = 9.5 9.5 41 2
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 None 45 Human Functional pEC50 = 9.5 9.5 -2 26
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 None 45 Human Functional pEC50 = 9.5 9.5 -2 26
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 None 45 Human Functional pEC50 = 9.5 9.5 -2 26
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 None 45 Human Functional pEC50 = 9.5 9.5 -2 26
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 2502 None 21 Human Functional pEC50 = 9.4 9.4 7 7
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 2502 None 21 Human Functional pEC50 = 9.4 9.4 7 7
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 2502 None 21 Human Functional pEC50 = 9.4 9.4 7 7
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 2502 None 21 Human Functional pEC50 = 9.4 9.4 7 7
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 181891 None 0 Human Functional pEC50 = 9.4 9.4 794 2
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 181891 None 0 Human Functional pEC50 = 9.4 9.4 794 2
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 85340 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 85340 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 193118 None 4 Human Functional pEC50 = 9.3 9.3 1 3
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 193118 None 4 Human Functional pEC50 = 9.3 9.3 1 3
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 193118 None 4 Human Functional pEC50 = 9.3 9.3 1 3
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 193118 None 4 Human Functional pEC50 = 9.3 9.3 1 3
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 193118 None 4 Human Functional pEC50 = 9.3 9.3 1 3
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 193118 None 4 Human Functional pEC50 = 9.3 9.3 1 3
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 183821 None 0 Human Functional pEC50 = 9.2 9.2 12 3
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 183821 None 0 Human Functional pEC50 = 9.2 9.2 12 3
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 183821 None 0 Human Functional pEC50 = 9.2 9.2 12 3
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 183821 None 0 Human Functional pEC50 = 9.2 9.2 12 3
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 183821 None 0 Human Functional pEC50 = 9.2 9.2 12 3
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 183821 None 0 Human Functional pEC50 = 9.2 9.2 12 3
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 181955 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 181955 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 16169 None 0 Human Functional pEC50 = 9.1 9.1 18 2
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 16169 None 0 Human Functional pEC50 = 9.1 9.1 18 2
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 12503 None 0 Human Functional pEC50 = 9.1 9.1 16 3
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 12503 None 0 Human Functional pEC50 = 9.1 9.1 16 3
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 12503 None 0 Human Functional pEC50 = 9.1 9.1 16 3
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 191902 None 0 Human Functional pEC50 = 9.1 9.1 -1 2
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 191902 None 0 Human Functional pEC50 = 9.1 9.1 -1 2
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 151243 None 0 Human Functional pEC50 = 9.1 9.1 100 3
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 151243 None 0 Human Functional pEC50 = 9.1 9.1 100 3
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 152118 None 0 Human Functional pEC50 = 9.1 9.1 39 2
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 152118 None 0 Human Functional pEC50 = 9.1 9.1 39 2
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 191902 None 0 Human Functional pEC50 = 9.1 9.1 -1 2
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 191902 None 0 Human Functional pEC50 = 9.1 9.1 -1 2
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 None 45 Human Functional pEC50 = 9.1 9.1 -2 26
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 None 45 Human Functional pEC50 = 9.1 9.1 -2 26
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 None 45 Human Functional pEC50 = 9.1 9.1 -2 26
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 None 45 Human Functional pEC50 = 9.1 9.1 -2 26
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 None 45 Human Functional pEC50 = 9.1 9.1 -2 26
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 None 45 Human Functional pEC50 = 9.1 9.1 -2 26
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 None 45 Human Functional pEC50 = 9.1 9.1 -2 26
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 None 45 Human Functional pEC50 = 9.1 9.1 -2 26
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 138444 None 0 Human Functional pEC50 = 9.0 9.0 15 3
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 138444 None 0 Human Functional pEC50 = 9.0 9.0 15 3
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 138444 None 0 Human Functional pEC50 = 9.0 9.0 15 3
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 202511 None 0 Human Functional pEC50 = 9 9.0 1445 2
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 202511 None 0 Human Functional pEC50 = 9 9.0 1445 2
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 89105 None 0 Human Functional pEC50 = 9 9.0 7 3
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 89105 None 0 Human Functional pEC50 = 9 9.0 7 3
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 89105 None 0 Human Functional pEC50 = 9 9.0 7 3
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 8064 None 1 Human Functional pEC50 = 9 9.0 128 2
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 8064 None 1 Human Functional pEC50 = 9 9.0 128 2
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 4119 None 22 Human Functional pEC50 = 9 9.0 3 3
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 4119 None 22 Human Functional pEC50 = 9 9.0 3 3
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 4119 None 22 Human Functional pEC50 = 9 9.0 3 3
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 150841 None 0 Human Functional pEC50 = 9 9.0 100 3
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 150841 None 0 Human Functional pEC50 = 9 9.0 100 3
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 192288 None 0 Human Functional pEC50 = 9.0 9.0 1 3
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 192288 None 0 Human Functional pEC50 = 9.0 9.0 1 3
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 192288 None 0 Human Functional pEC50 = 9.0 9.0 1 3
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 192288 None 0 Human Functional pEC50 = 9.0 9.0 1 3
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 138444 None 0 Human Functional pEC50 = 9.0 9.0 15 3
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 138444 None 0 Human Functional pEC50 = 9.0 9.0 15 3
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 138444 None 0 Human Functional pEC50 = 9.0 9.0 15 3
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 89144 None 0 Human Functional pEC50 = 9.0 9.0 85 3
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 89144 None 0 Human Functional pEC50 = 9.0 9.0 85 3
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 89144 None 0 Human Functional pEC50 = 9.0 9.0 85 3
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 163774 None 0 Human Functional pEC50 = 8.9 8.9 19 3
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 163774 None 0 Human Functional pEC50 = 8.9 8.9 19 3
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 164894 None 0 Human Functional pEC50 = 8.9 8.9 1047 2
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 164894 None 0 Human Functional pEC50 = 8.9 8.9 1047 2
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 183821 None 0 Human Functional pEC50 = 8.9 8.9 12 3
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 183821 None 0 Human Functional pEC50 = 8.9 8.9 12 3
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 183821 None 0 Human Functional pEC50 = 8.9 8.9 12 3
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 183821 None 0 Human Functional pEC50 = 8.9 8.9 12 3
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 183821 None 0 Human Functional pEC50 = 8.9 8.9 12 3
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 183821 None 0 Human Functional pEC50 = 8.9 8.9 12 3
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 163902 None 0 Human Functional pEC50 = 8.9 8.9 776 3
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 163902 None 0 Human Functional pEC50 = 8.9 8.9 776 3
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 164894 None 0 Human Functional pEC50 = 8.9 8.9 1047 2
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 164894 None 0 Human Functional pEC50 = 8.9 8.9 1047 2
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 12652 None 5 Human Functional pEC50 = 8.9 8.9 3 3
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 12652 None 5 Human Functional pEC50 = 8.9 8.9 3 3
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 12652 None 5 Human Functional pEC50 = 8.9 8.9 3 3
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 163902 None 0 Human Functional pEC50 = 8.9 8.9 776 3
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 163902 None 0 Human Functional pEC50 = 8.9 8.9 776 3
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 84872 None 0 Human Functional pEC50 = 8.9 8.9 5 3
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 84872 None 0 Human Functional pEC50 = 8.9 8.9 5 3
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 202316 None 0 Human Functional pEC50 = 8.9 8.9 1071 3
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 202316 None 0 Human Functional pEC50 = 8.9 8.9 1071 3
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 146240 None 0 Human Functional pEC50 = 8.8 8.8 79 3
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 146240 None 0 Human Functional pEC50 = 8.8 8.8 79 3
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 183768 None 0 Human Functional pEC50 = 8.8 8.8 22 3
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 183768 None 0 Human Functional pEC50 = 8.8 8.8 22 3
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 183768 None 0 Human Functional pEC50 = 8.8 8.8 22 3
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 183768 None 0 Human Functional pEC50 = 8.8 8.8 22 3
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 183768 None 0 Human Functional pEC50 = 8.8 8.8 22 3
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 183768 None 0 Human Functional pEC50 = 8.8 8.8 22 3
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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
152 364 None 24 Rat Functional pEC50 = 8.7 8.7 1 5
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 364 None 24 Rat Functional pEC50 = 8.7 8.7 1 5
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 364 None 24 Rat Functional pEC50 = 8.7 8.7 1 5
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 201768 None 0 Human Functional pEC50 = 8.7 8.7 25 3
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 201768 None 0 Human Functional pEC50 = 8.7 8.7 25 3
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 2344 None 24 Human Functional pEC50 = 8.7 8.7 1 11
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 2344 None 24 Human Functional pEC50 = 8.7 8.7 1 11
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 2344 None 24 Human Functional pEC50 = 8.7 8.7 1 11
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 2344 None 24 Human Functional pEC50 = 8.7 8.7 1 11
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 2344 None 24 Human Functional pEC50 = 8.7 8.7 1 11
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 187737 None 28 Human Functional pEC50 = 8.7 8.7 54 6
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
CHEMBL4743049 187737 None 28 Human Functional pEC50 = 8.7 8.7 54 6
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 187737 None 28 Human Functional pEC50 = 8.7 8.7 54 6
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 192015 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 192015 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 187737 None 28 Human Functional pEC50 = 8.7 8.7 54 6
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
CHEMBL4743049 187737 None 28 Human Functional pEC50 = 8.7 8.7 54 6
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 187737 None 28 Human Functional pEC50 = 8.7 8.7 54 6
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 192015 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 192015 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 180124 None 0 Human Functional pEC50 = 8.7 8.7 19 2
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 180124 None 0 Human Functional pEC50 = 8.7 8.7 19 2
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 147538 None 0 Human Functional pEC50 = 8.7 8.7 15 2
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 147538 None 0 Human Functional pEC50 = 8.7 8.7 15 2
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 79139 None 0 Human Functional pEC50 = 8 8.0 1 3
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 79139 None 0 Human Functional pEC50 = 8 8.0 1 3
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 202440 None 1 Human Functional pEC50 = 8 8.0 6 3
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 202440 None 1 Human Functional pEC50 = 8 8.0 6 3
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 91116 None 1 Human Functional pEC50 = 8 8.0 -1 3
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 91116 None 1 Human Functional pEC50 = 8 8.0 -1 3
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 183833 None 0 Human Functional pEC50 = 8 8.0 38 2
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 183833 None 0 Human Functional pEC50 = 8 8.0 38 2
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 183833 None 0 Human Functional pEC50 = 8 8.0 38 2
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 12657 None 2 Human Functional pEC50 = 8 8.0 5 3
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 12657 None 2 Human Functional pEC50 = 8 8.0 5 3
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 12657 None 2 Human Functional pEC50 = 8 8.0 5 3
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 94966 None 0 Human Functional pEC50 = 8 8.0 10 3
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 94966 None 0 Human Functional pEC50 = 8 8.0 10 3
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 169307 None 5 Human Functional pEC50 = 8 8.0 46 3
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 169307 None 5 Human Functional pEC50 = 8 8.0 46 3
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 193080 None 0 Human Functional pEC50 = 8 8.0 5 2
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 193080 None 0 Human Functional pEC50 = 8 8.0 5 2
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 193080 None 0 Human Functional pEC50 = 8 8.0 5 2
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 200279 None 0 Human Functional pEC50 = 8 8.0 18 3
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 200279 None 0 Human Functional pEC50 = 8 8.0 18 3
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 111728 None 17 Human Functional pEC50 = 8 8.0 6 5
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 111728 None 17 Human Functional pEC50 = 8 8.0 6 5
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 149260 None 0 Human Functional pEC50 = 8 8.0 - 1
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 149260 None 0 Human Functional pEC50 = 8 8.0 - 1
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 193080 None 0 Human Functional pEC50 = 8 8.0 5 2
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 193080 None 0 Human Functional pEC50 = 8 8.0 5 2
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 193080 None 0 Human Functional pEC50 = 8 8.0 5 2
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 183833 None 0 Human Functional pEC50 = 8.0 8.0 38 2
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 183833 None 0 Human Functional pEC50 = 8.0 8.0 38 2
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 183833 None 0 Human Functional pEC50 = 8.0 8.0 38 2
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 61474 None 27 Dog Functional pEC50 = 8.0 8.0 2 9
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 61474 None 27 Dog Functional pEC50 = 8.0 8.0 2 9
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 183741 None 0 Human Functional pEC50 = 8.0 8.0 6 3
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 183741 None 0 Human Functional pEC50 = 8.0 8.0 6 3
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 183741 None 0 Human Functional pEC50 = 8.0 8.0 6 3
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 183800 None 0 Human Functional pEC50 = 8.0 8.0 20 3
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 183800 None 0 Human Functional pEC50 = 8.0 8.0 20 3
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 183800 None 0 Human Functional pEC50 = 8.0 8.0 20 3
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 164186 None 0 Human Functional pEC50 = 7 7.0 -1 3
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 164186 None 0 Human Functional pEC50 = 7 7.0 -1 3
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 183898 None 0 Human Functional pEC50 = 7 7.0 5 2
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 183898 None 0 Human Functional pEC50 = 7 7.0 5 2
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 183898 None 0 Human Functional pEC50 = 7 7.0 5 2
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 61481 None 0 Human Functional pEC50 = 7 7.0 1 2
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 61481 None 0 Human Functional pEC50 = 7 7.0 1 2
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 87341 None 0 Human Functional pEC50 = 7 7.0 3 2
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 87341 None 0 Human Functional pEC50 = 7 7.0 3 2
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 150807 None 0 Human Functional pEC50 = 7 7.0 63 2
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 150807 None 0 Human Functional pEC50 = 7 7.0 63 2
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 107570 None 0 Rat Functional pEC50 = 7 7.0 - 1
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 107570 None 0 Rat Functional pEC50 = 7 7.0 - 1
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
172460286 196116 None 0 Human Functional pEC50 = 7 7.0 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 251 1 1 2 3.1 COc1ccc2c3c1-c1ccccc1CC3NCC2 10.1021/acsmedchemlett.3c00454
CHEMBL5417234 196116 None 0 Human Functional pEC50 = 7 7.0 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 251 1 1 2 3.1 COc1ccc2c3c1-c1ccccc1CC3NCC2 10.1021/acsmedchemlett.3c00454
3288856 192922 None 0 Human Functional pEC50 = 6 6.0 -3 2
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 192922 None 0 Human Functional pEC50 = 6 6.0 -3 2
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 192922 None 0 Human Functional pEC50 = 6 6.0 -3 2
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 149746 None 0 Human Functional pEC50 = 6 6.0 -2 2
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 149746 None 0 Human Functional pEC50 = 6 6.0 -2 2
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 107248 None 1 Rat Functional pEC50 = 6 6.0 - 1
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 107248 None 1 Rat Functional pEC50 = 6 6.0 - 1
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
172445778 195053 None 0 Human Functional pEC50 = 6 6.0 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.3 C[C@@H]1CC2(C=Cc3ccc(Cl)cc3O2)CCN1 10.1021/acsmedchemlett.3c00454
CHEMBL5395596 195053 None 0 Human Functional pEC50 = 6 6.0 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.3 C[C@@H]1CC2(C=Cc3ccc(Cl)cc3O2)CCN1 10.1021/acsmedchemlett.3c00454
10560133 107393 None 0 Rat Functional pEC50 = 5 5.0 - 1
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 107393 None 0 Rat Functional pEC50 = 5 5.0 - 1
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 192922 None 0 Human Functional pEC50 = 6 6.0 -3 2
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 192922 None 0 Human Functional pEC50 = 6 6.0 -3 2
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 192922 None 0 Human Functional pEC50 = 6 6.0 -3 2
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 183853 None 0 Human Functional pEC50 = 7 7.0 - 1
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 183853 None 0 Human Functional pEC50 = 7 7.0 - 1
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 183853 None 0 Human Functional pEC50 = 7 7.0 - 1
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 199792 None 0 Human Functional pEC50 = 7 7.0 - 1
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 199792 None 0 Human Functional pEC50 = 7 7.0 - 1
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 183853 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 183853 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 183853 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 161241 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
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 161241 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
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 161241 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
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 87341 None 0 Human Functional pEC50 = 7.0 7.0 3 2
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 87341 None 0 Human Functional pEC50 = 7.0 7.0 3 2
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 200216 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 200216 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 120703 None 0 Human Functional pEC50 = 7.0 7.0 33 2
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 120703 None 0 Human Functional pEC50 = 7.0 7.0 33 2
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 120703 None 0 Human Functional pEC50 = 7.0 7.0 33 2
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 161241 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
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 161241 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
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 161241 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
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 199709 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 199709 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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
172460286 196116 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at recombinant human 5-HT2C stably expressed in human T-REx-293 cells measured after 60 mins by FLIPR assayAgonist activity at recombinant human 5-HT2C stably expressed in human T-REx-293 cells measured after 60 mins by FLIPR assay
ChEMBL 251 1 1 2 3.1 COc1ccc2c3c1-c1ccccc1CC3NCC2 10.1016/j.ejmech.2023.115414
CHEMBL5417234 196116 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at recombinant human 5-HT2C stably expressed in human T-REx-293 cells measured after 60 mins by FLIPR assayAgonist activity at recombinant human 5-HT2C stably expressed in human T-REx-293 cells measured after 60 mins by FLIPR assay
ChEMBL 251 1 1 2 3.1 COc1ccc2c3c1-c1ccccc1CC3NCC2 10.1016/j.ejmech.2023.115414
11983273 78025 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
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 78025 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
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
172460286 196116 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 251 1 1 2 3.1 COc1ccc2c3c1-c1ccccc1CC3NCC2 10.1021/acsmedchemlett.3c00454
CHEMBL5417234 196116 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 251 1 1 2 3.1 COc1ccc2c3c1-c1ccccc1CC3NCC2 10.1021/acsmedchemlett.3c00454
137655846 158782 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 158782 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 138449 None 0 Human Functional pEC50 = 7.0 7.0 9 2
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 138449 None 0 Human Functional pEC50 = 7.0 7.0 9 2
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 138449 None 0 Human Functional pEC50 = 7.0 7.0 9 2
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 216550 None 1 Human Functional pEC50 = 7.0 7.0 -1 2
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 216550 None 1 Human Functional pEC50 = 7.0 7.0 -1 2
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 138449 None 0 Human Functional pEC50 = 7.0 7.0 9 2
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 138449 None 0 Human Functional pEC50 = 7.0 7.0 9 2
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 138449 None 0 Human Functional pEC50 = 7.0 7.0 9 2
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 155913 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 155913 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 216550 None 1 Human Functional pEC50 = 7.0 7.0 -1 2
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 216550 None 1 Human Functional pEC50 = 7.0 7.0 -1 2
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 193074 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 193074 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 193074 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 192946 None 0 Human Functional pEC50 = 6.0 6.0 1 2
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 192946 None 0 Human Functional pEC50 = 6.0 6.0 1 2
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 192946 None 0 Human Functional pEC50 = 6.0 6.0 1 2
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 176654 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 176654 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 176654 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 84928 None 0 Human Functional pEC50 = 7.0 7.0 4 3
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 84928 None 0 Human Functional pEC50 = 7.0 7.0 4 3
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 200920 None 0 Human Functional pEC50 = 7.0 7.0 1 2
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 200920 None 0 Human Functional pEC50 = 7.0 7.0 1 2
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 103095 None 23 Human Functional pEC50 = 7.0 7.0 -5 3
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 103095 None 23 Human Functional pEC50 = 7.0 7.0 -5 3
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 103095 None 23 Human Functional pEC50 = 7.0 7.0 -5 3
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 103095 None 23 Human Functional pEC50 = 7.0 7.0 -5 3
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 103095 None 23 Human Functional pEC50 = 7.0 7.0 -5 3
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 103095 None 23 Human Functional pEC50 = 7.0 7.0 -5 3
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 138446 None 0 Human Functional pEC50 = 7.0 7.0 3 2
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 138446 None 0 Human Functional pEC50 = 7.0 7.0 3 2
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 138446 None 0 Human Functional pEC50 = 7.0 7.0 3 2
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 192946 None 0 Human Functional pEC50 = 6.0 6.0 1 2
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 192946 None 0 Human Functional pEC50 = 6.0 6.0 1 2
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 192946 None 0 Human Functional pEC50 = 6.0 6.0 1 2
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 193074 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 193074 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 193074 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 176654 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 176654 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 176654 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 91138 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 91138 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 138446 None 0 Human Functional pEC50 = 7.0 7.0 3 2
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 138446 None 0 Human Functional pEC50 = 7.0 7.0 3 2
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 138446 None 0 Human Functional pEC50 = 7.0 7.0 3 2
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 120715 None 0 Human Functional pEC50 = 6.0 6.0 2 2
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 120715 None 0 Human Functional pEC50 = 6.0 6.0 2 2
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 120715 None 0 Human Functional pEC50 = 6.0 6.0 2 2
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 83524 None 0 Human Functional pEC50 = 8.0 8.0 15 3
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 83524 None 0 Human Functional pEC50 = 8.0 8.0 15 3
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 89133 None 0 Human Functional pEC50 = 8.0 8.0 151 3
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 89133 None 0 Human Functional pEC50 = 8.0 8.0 151 3
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 89133 None 0 Human Functional pEC50 = 8.0 8.0 151 3
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 120729 None 0 Human Functional pEC50 = 8.0 8.0 93 3
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 120729 None 0 Human Functional pEC50 = 8.0 8.0 93 3
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 120729 None 0 Human Functional pEC50 = 8.0 8.0 93 3
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 183741 None 0 Human Functional pEC50 = 8.0 8.0 6 3
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 183741 None 0 Human Functional pEC50 = 8.0 8.0 6 3
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 183741 None 0 Human Functional pEC50 = 8.0 8.0 6 3
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 183800 None 0 Human Functional pEC50 = 8.0 8.0 20 3
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 183800 None 0 Human Functional pEC50 = 8.0 8.0 20 3
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 183800 None 0 Human Functional pEC50 = 8.0 8.0 20 3
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 12488 None 0 Human Functional pEC50 = 8.0 8.0 1 3
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 12488 None 0 Human Functional pEC50 = 8.0 8.0 1 3
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 12488 None 0 Human Functional pEC50 = 8.0 8.0 1 3
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 200008 None 0 Human Functional pEC50 = 8.0 8.0 1 2
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 200008 None 0 Human Functional pEC50 = 8.0 8.0 1 2
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 2344 None 24 Human Functional pEC50 = 8.0 8.0 1 11
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 2344 None 24 Human Functional pEC50 = 8.0 8.0 1 11
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 2344 None 24 Human Functional pEC50 = 8.0 8.0 1 11
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 2344 None 24 Human Functional pEC50 = 8.0 8.0 1 11
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 2344 None 24 Human Functional pEC50 = 8.0 8.0 1 11
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 64353 None 37 Human Functional pEC50 = 8.0 8.0 19 3
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 64353 None 37 Human Functional pEC50 = 8.0 8.0 19 3
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 64658 None 0 Human Functional pEC50 = 8.0 8.0 7 3
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 64658 None 0 Human Functional pEC50 = 8.0 8.0 7 3
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 166244 None 0 Human Functional pEC50 = 8.0 8.0 3 3
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 166244 None 0 Human Functional pEC50 = 8.0 8.0 3 3
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 78458 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 78458 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 61475 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 61475 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 201767 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 201767 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 169786 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 169786 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 200787 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 200787 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 111735 None 0 Human Functional pEC50 = 7.0 7.0 8 2
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 111735 None 0 Human Functional pEC50 = 7.0 7.0 8 2
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 183763 None 0 Human Functional pEC50 = 7.0 7.0 4 2
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 183763 None 0 Human Functional pEC50 = 7.0 7.0 4 2
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 183763 None 0 Human Functional pEC50 = 7.0 7.0 4 2
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 193097 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 193097 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 193097 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 120718 None 0 Human Functional pEC50 = 6.0 6.0 4 2
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 120718 None 0 Human Functional pEC50 = 6.0 6.0 4 2
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 120718 None 0 Human Functional pEC50 = 6.0 6.0 4 2
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 183763 None 0 Human Functional pEC50 = 7.0 7.0 4 2
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 183763 None 0 Human Functional pEC50 = 7.0 7.0 4 2
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 183763 None 0 Human Functional pEC50 = 7.0 7.0 4 2
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 193097 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 193097 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 193097 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 200284 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 200284 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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
22241625 196520 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 205 3 2 3 1.4 CN(C)CCc1n[nH]c2ccc(O)cc12 10.1021/acsmedchemlett.3c00566
CHEMBL5425772 196520 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 205 3 2 3 1.4 CN(C)CCc1n[nH]c2ccc(O)cc12 10.1021/acsmedchemlett.3c00566
162659576 183803 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 183803 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 183803 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 138435 None 0 Human Functional pEC50 = 6.9 6.9 19 3
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 138435 None 0 Human Functional pEC50 = 6.9 6.9 19 3
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 138435 None 0 Human Functional pEC50 = 6.9 6.9 19 3
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 138440 None 0 Human Functional pEC50 = 6.9 6.9 7 2
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 138440 None 0 Human Functional pEC50 = 6.9 6.9 7 2
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 138440 None 0 Human Functional pEC50 = 6.9 6.9 7 2
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
22241625 196520 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 205 3 2 3 1.4 CN(C)CCc1n[nH]c2ccc(O)cc12 10.1021/acsmedchemlett.3c00566
CHEMBL5425772 196520 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 205 3 2 3 1.4 CN(C)CCc1n[nH]c2ccc(O)cc12 10.1021/acsmedchemlett.3c00566
162659576 183803 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 183803 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 183803 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 193282 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 193282 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 138435 None 0 Human Functional pEC50 = 6.9 6.9 19 3
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 138435 None 0 Human Functional pEC50 = 6.9 6.9 19 3
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 138435 None 0 Human Functional pEC50 = 6.9 6.9 19 3
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 138440 None 0 Human Functional pEC50 = 6.9 6.9 7 2
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 138440 None 0 Human Functional pEC50 = 6.9 6.9 7 2
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 138440 None 0 Human Functional pEC50 = 6.9 6.9 7 2
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 192316 None 0 Human Functional pEC50 = 5.9 5.9 6 2
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 192316 None 0 Human Functional pEC50 = 5.9 5.9 6 2
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 192316 None 0 Human Functional pEC50 = 5.9 5.9 6 2
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 192316 None 0 Human Functional pEC50 = 5.9 5.9 6 2
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 12562 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 12562 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 12562 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 156394 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 156394 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 12546 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 12546 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 12546 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 141773 None 0 Human Functional pEC50 = 7.9 7.9 2 3
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 141773 None 0 Human Functional pEC50 = 7.9 7.9 2 3
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 89119 None 0 Human Functional pEC50 = 7.9 7.9 70 2
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 89119 None 0 Human Functional pEC50 = 7.9 7.9 70 2
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 89119 None 0 Human Functional pEC50 = 7.9 7.9 70 2
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 91133 None 0 Human Functional pEC50 = 7.9 7.9 16 2
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 91133 None 0 Human Functional pEC50 = 7.9 7.9 16 2
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 91146 None 0 Human Functional pEC50 = 7.9 7.9 85 2
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 91146 None 0 Human Functional pEC50 = 7.9 7.9 85 2
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 183787 None 0 Human Functional pEC50 = 7.9 7.9 20 3
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 183787 None 0 Human Functional pEC50 = 7.9 7.9 20 3
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 183787 None 0 Human Functional pEC50 = 7.9 7.9 20 3
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 187528 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 187528 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 158102 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 158102 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 158550 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 158550 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 176567 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 176567 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 176567 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 102034 None 22 Human Functional pEC50 = 7.9 7.9 1 2
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 102034 None 22 Human Functional pEC50 = 7.9 7.9 1 2
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 72086 None 24 Human Functional pEC50 = 7.9 7.9 2 3
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 72086 None 24 Human Functional pEC50 = 7.9 7.9 2 3
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 63959 None 17 Human Functional pEC50 = 7.9 7.9 7 3
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 63959 None 17 Human Functional pEC50 = 7.9 7.9 7 3
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 169307 None 5 Human Functional pEC50 = 7.9 7.9 46 3
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 169307 None 5 Human Functional pEC50 = 7.9 7.9 46 3
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 183787 None 0 Human Functional pEC50 = 7.9 7.9 20 3
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 183787 None 0 Human Functional pEC50 = 7.9 7.9 20 3
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 183787 None 0 Human Functional pEC50 = 7.9 7.9 20 3
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 164150 None 0 Human Functional pEC50 = 7.9 7.9 204 3
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 164150 None 0 Human Functional pEC50 = 7.9 7.9 204 3
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 176567 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 176567 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 176567 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 63959 None 17 Human Functional pEC50 = 7.9 7.9 7 3
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 63959 None 17 Human Functional pEC50 = 7.9 7.9 7 3
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 64353 None 37 Human Functional pEC50 = 7.9 7.9 19 3
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 64353 None 37 Human Functional pEC50 = 7.9 7.9 19 3
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 216558 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 216558 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 2011 None 45 Human Functional pEC50 = 7.9 7.9 4 6
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 2011 None 45 Human Functional pEC50 = 7.9 7.9 4 6
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 2011 None 45 Human Functional pEC50 = 7.9 7.9 4 6
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 2011 None 45 Human Functional pEC50 = 7.9 7.9 4 6
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 88064 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
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 88064 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
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 216558 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 216558 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 161120 None 0 Human Functional pEC50 = 7.9 7.9 21 2
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 161120 None 0 Human Functional pEC50 = 7.9 7.9 21 2
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 161120 None 0 Human Functional pEC50 = 7.9 7.9 21 2
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 202194 None 0 Human Functional pEC50 = 6.9 6.9 4 3
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 202194 None 0 Human Functional pEC50 = 6.9 6.9 4 3
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 161309 None 0 Human Functional pEC50 = 6.9 6.9 3 2
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 161309 None 0 Human Functional pEC50 = 6.9 6.9 3 2
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 161309 None 0 Human Functional pEC50 = 6.9 6.9 3 2
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 205867 None 7 Human Functional pEC50 = 6.9 6.9 -1 2
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 205867 None 7 Human Functional pEC50 = 6.9 6.9 -1 2
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 74485 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 74485 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 74485 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 98073 None 55 Human Functional pEC50 = 6.9 6.9 -1 4
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 98073 None 55 Human Functional pEC50 = 6.9 6.9 -1 4
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 161084 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 161084 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 161084 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 161309 None 0 Human Functional pEC50 = 6.9 6.9 3 2
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 161309 None 0 Human Functional pEC50 = 6.9 6.9 3 2
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 161309 None 0 Human Functional pEC50 = 6.9 6.9 3 2
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 202512 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 202512 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161072 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161072 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161072 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 102545 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 102545 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 102545 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 87339 None 1 Human Functional pEC50 = 4.9 4.9 - 1
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 87339 None 1 Human Functional pEC50 = 4.9 4.9 - 1
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 161072 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161072 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161072 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 87339 None 1 Human Functional pEC50 = 4.9 4.9 - 1
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 87339 None 1 Human Functional pEC50 = 4.9 4.9 - 1
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 161084 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 161084 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 161084 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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
82045794 195280 None 3 Human Functional pEC50 = 6.9 6.9 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5399965 195280 None 3 Human Functional pEC50 = 6.9 6.9 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
70681346 74489 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 74489 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 74489 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 120709 None 0 Human Functional pEC50 = 5.9 5.9 2 2
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 120709 None 0 Human Functional pEC50 = 5.9 5.9 2 2
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 120709 None 0 Human Functional pEC50 = 5.9 5.9 2 2
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 193155 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
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 193155 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
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 193155 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
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 205867 None 7 Human Functional pEC50 = 6.9 6.9 -1 2
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 205867 None 7 Human Functional pEC50 = 6.9 6.9 -1 2
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 193155 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
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 193155 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
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 193155 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
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 61477 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 61477 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 200827 None 0 Human Functional pEC50 = 6.9 6.9 3 2
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 200827 None 0 Human Functional pEC50 = 6.9 6.9 3 2
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 142731 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 142731 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 142743 None 0 Human Functional pEC50 = 6.9 6.9 7 2
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 142743 None 0 Human Functional pEC50 = 6.9 6.9 7 2
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 143682 None 0 Human Functional pEC50 = 6.9 6.9 19 2
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 143682 None 0 Human Functional pEC50 = 6.9 6.9 19 2
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 79706 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
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 79706 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
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
82045794 195280 None 3 Human Functional pEC50 = 6.9 6.9 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5399965 195280 None 3 Human Functional pEC50 = 6.9 6.9 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
46228441 202321 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 202321 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 120706 None 0 Human Functional pEC50 = 5.9 5.9 4 2
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 120706 None 0 Human Functional pEC50 = 5.9 5.9 4 2
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 120706 None 0 Human Functional pEC50 = 5.9 5.9 4 2
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 64446 None 1 Human Functional pEC50 = 5.9 5.9 - 1
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 64446 None 1 Human Functional pEC50 = 5.9 5.9 - 1
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 193032 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 193032 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 193032 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 152883 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 152883 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 209651 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
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
CHEMBL92565 209651 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
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
10774565 210247 None 0 Rat Functional pEC50 = 4.9 4.9 - 1
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 COc1cccc2c1ccn2CC(C)N 10.1021/jm970030l
CHEMBL96095 210247 None 0 Rat Functional pEC50 = 4.9 4.9 - 1
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 COc1cccc2c1ccn2CC(C)N 10.1021/jm970030l
168286082 193032 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 193032 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 193032 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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
11736340 74011 None 39 Human Functional pEC50 = 5.9 5.9 - 1
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 229 1 1 1 3.2 FC(F)(F)c1cccc(C2CCNCC2)c1 10.1016/j.bmcl.2012.01.122
CHEMBL2011553 74011 None 39 Human Functional pEC50 = 5.9 5.9 - 1
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 229 1 1 1 3.2 FC(F)(F)c1cccc(C2CCNCC2)c1 10.1016/j.bmcl.2012.01.122
CHEMBL2021656 74011 None 39 Human Functional pEC50 = 5.9 5.9 - 1
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 229 1 1 1 3.2 FC(F)(F)c1cccc(C2CCNCC2)c1 10.1016/j.bmcl.2012.01.122
137636435 156150 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 326 2 0 4 3.1 O=C(c1csc(-c2cccc(Cl)c2F)n1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4062613 156150 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 326 2 0 4 3.1 O=C(c1csc(-c2cccc(Cl)c2F)n1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
702235 53228 None 50 Human Functional pEC50 = 6.9 6.9 - 1
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 200 1 2 1 2.6 c1ccc2c(C3CCNCC3)c[nH]c2c1 10.1016/j.bmcl.2012.01.122
CHEMBL15988 53228 None 50 Human Functional pEC50 = 6.9 6.9 - 1
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 200 1 2 1 2.6 c1ccc2c(C3CCNCC3)c[nH]c2c1 10.1016/j.bmcl.2012.01.122
CHEMBL2011564 53228 None 50 Human Functional pEC50 = 6.9 6.9 - 1
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 200 1 2 1 2.6 c1ccc2c(C3CCNCC3)c[nH]c2c1 10.1016/j.bmcl.2012.01.122
44572164 12687 None 0 Human Functional pEC50 = 6.9 6.9 3 3
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 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1F 10.1021/jm801354e
CHEMBL1187390 12687 None 0 Human Functional pEC50 = 6.9 6.9 3 3
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 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1F 10.1021/jm801354e
CHEMBL501526 12687 None 0 Human Functional pEC50 = 6.9 6.9 3 3
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 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1F 10.1021/jm801354e
168268773 192901 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 282 1 3 2 3.2 Oc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177208 192901 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 282 1 3 2 3.2 Oc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221390 192901 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 282 1 3 2 3.2 Oc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
137647246 157920 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 354 2 0 4 3.7 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CC2CC1CO2 10.1021/acs.jmedchem.7b00385
CHEMBL4083432 157920 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 354 2 0 4 3.7 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CC2CC1CO2 10.1021/acs.jmedchem.7b00385
118733762 120708 None 0 Human Functional pEC50 = 7.9 7.9 6 3
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 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416033 120708 None 0 Human Functional pEC50 = 7.9 7.9 6 3
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 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546889 120708 None 0 Human Functional pEC50 = 7.9 7.9 6 3
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 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
137629964 161120 None 0 Human Functional pEC50 = 7.9 7.9 21 2
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 161120 None 0 Human Functional pEC50 = 7.9 7.9 21 2
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 161120 None 0 Human Functional pEC50 = 7.9 7.9 21 2
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
12370465 12678 None 15 Human Functional pEC50 = 7.9 7.9 6 3
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 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
CHEMBL1187354 12678 None 15 Human Functional pEC50 = 7.9 7.9 6 3
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 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
CHEMBL500093 12678 None 15 Human Functional pEC50 = 7.9 7.9 6 3
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 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
44572207 12706 None 0 Human Functional pEC50 = 7.9 7.9 8 3
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 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F 10.1021/jm801354e
CHEMBL1187556 12706 None 0 Human Functional pEC50 = 7.9 7.9 8 3
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 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F 10.1021/jm801354e
CHEMBL508680 12706 None 0 Human Functional pEC50 = 7.9 7.9 8 3
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 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F 10.1021/jm801354e
137638508 156923 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 376 4 0 5 4.3 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)Cc1ccn(C)n1 10.1021/acs.jmedchem.7b00385
CHEMBL4071321 156923 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 376 4 0 5 4.3 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)Cc1ccn(C)n1 10.1021/acs.jmedchem.7b00385
137647007 157945 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 301 3 0 5 3.6 CCn1nc(-c2cccc3ccncc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
CHEMBL4083752 157945 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 301 3 0 5 3.6 CCn1nc(-c2cccc3ccncc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
122442286 138438 None 0 Human Functional pEC50 = 7.9 7.9 13 3
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 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 138438 None 0 Human Functional pEC50 = 7.9 7.9 13 3
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 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 138438 None 0 Human Functional pEC50 = 7.9 7.9 13 3
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 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
168273192 190525 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 282 1 3 2 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5177900 190525 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 282 1 3 2 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
122442286 138438 None 0 Human Functional pEC50 = 7.9 7.9 13 3
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 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 138438 None 0 Human Functional pEC50 = 7.9 7.9 13 3
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 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 138438 None 0 Human Functional pEC50 = 7.9 7.9 13 3
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 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
168273192 190525 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 282 1 3 2 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5177900 190525 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 282 1 3 2 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
122442260 138441 None 0 Human Functional pEC50 = 7.9 7.9 2 3
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 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769543 138441 None 0 Human Functional pEC50 = 7.9 7.9 2 3
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 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771390 138441 None 0 Human Functional pEC50 = 7.9 7.9 2 3
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 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
168268773 192901 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 282 1 3 2 3.2 Oc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177208 192901 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 282 1 3 2 3.2 Oc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221390 192901 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 282 1 3 2 3.2 Oc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
155527636 171390 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 239 2 1 3 1.8 c1ccc(Cc2cc3c(nn2)CCNCC3)cc1 10.1016/j.bmcl.2016.06.060
CHEMBL4460600 171390 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 239 2 1 3 1.8 c1ccc(Cc2cc3c(nn2)CCNCC3)cc1 10.1016/j.bmcl.2016.06.060
134136932 142743 None 0 Human Functional pEC50 = 6.9 6.9 7 2
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 142743 None 0 Human Functional pEC50 = 6.9 6.9 7 2
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
18735309 207891 None 0 Human Functional pEC50 = 6.9 6.9 -2 3
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 262 2 1 2 2.6 C[C@H](N)CN1CCc2cc(F)c(C(F)(F)F)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL80246 207891 None 0 Human Functional pEC50 = 6.9 6.9 -2 3
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 262 2 1 2 2.6 C[C@H](N)CN1CCc2cc(F)c(C(F)(F)F)cc21 10.1016/j.bmcl.2003.05.001
168294156 193114 None 0 Human Functional pEC50 = 5.9 5.9 -2 3
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 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5207023 193114 None 0 Human Functional pEC50 = 5.9 5.9 -2 3
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 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222736 193114 None 0 Human Functional pEC50 = 5.9 5.9 -2 3
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 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
168294156 193114 None 0 Human Functional pEC50 = 5.9 5.9 -2 3
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 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5207023 193114 None 0 Human Functional pEC50 = 5.9 5.9 -2 3
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 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222736 193114 None 0 Human Functional pEC50 = 5.9 5.9 -2 3
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 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
118733798 120713 None 0 Human Functional pEC50 = 6.9 6.9 12 2
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 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416051 120713 None 0 Human Functional pEC50 = 6.9 6.9 12 2
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 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546894 120713 None 0 Human Functional pEC50 = 6.9 6.9 12 2
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 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
46230047 201706 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 217 0 2 3 0.5 Cc1ccc2c(c1)C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590089 201706 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 217 0 2 3 0.5 Cc1ccc2c(c1)C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
122442275 138448 None 0 Human Functional pEC50 = 6.9 6.9 9 3
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770862 138448 None 0 Human Functional pEC50 = 6.9 6.9 9 3
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771397 138448 None 0 Human Functional pEC50 = 6.9 6.9 9 3
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
44573004 12524 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
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 161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1 10.1021/jm801354e
CHEMBL1186590 12524 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
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 161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1 10.1021/jm801354e
CHEMBL471202 12524 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
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 161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1 10.1021/jm801354e
122442275 138448 None 0 Human Functional pEC50 = 6.9 6.9 9 3
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770862 138448 None 0 Human Functional pEC50 = 6.9 6.9 9 3
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771397 138448 None 0 Human Functional pEC50 = 6.9 6.9 9 3
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
11195293 91122 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 216 0 1 2 1.0 C[C@@]12CNCCN1C(=O)c1ccccc1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397883 91122 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 216 0 1 2 1.0 C[C@@]12CNCCN1C(=O)c1ccccc1C2 10.1016/j.bmcl.2013.04.061
11290492 138088 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 218 1 1 3 0.8 COc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL376456 138088 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 218 1 1 3 0.8 COc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
44572369 12462 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 171 2 1 1 1.7 C#Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL1186108 12462 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 171 2 1 1 1.7 C#Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL450178 12462 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 171 2 1 1 1.7 C#Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
9839494 102524 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 305 0 2 3 2.1 O=C1Nc2cc(C(F)(F)F)c(Cl)cc2N2CCNCC12 10.1016/s0960-894x(00)00400-5
CHEMBL304013 102524 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 305 0 2 3 2.1 O=C1Nc2cc(C(F)(F)F)c(Cl)cc2N2CCNCC12 10.1016/s0960-894x(00)00400-5
46228424 204652 None 1 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 281 1 1 5 0.9 Brc1cn2ccnc2c(N2CCNCC2)n1 10.1016/j.bmcl.2009.10.112
CHEMBL609595 204652 None 1 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 281 1 1 5 0.9 Brc1cn2ccnc2c(N2CCNCC2)n1 10.1016/j.bmcl.2009.10.112
46230046 201703 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 203 0 2 3 0.2 O=C1NC2CNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
CHEMBL590077 201703 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 203 0 2 3 0.2 O=C1NC2CNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
162650828 183756 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 285 6 1 3 3.8 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4750271 183756 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 285 6 1 3 3.8 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4802701 183756 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 285 6 1 3 3.8 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
44573002 12690 None 0 Human Functional pEC50 = 6.9 6.9 19 2
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]1c1ccc(Br)cc1 10.1021/jm801354e
CHEMBL1187408 12690 None 0 Human Functional pEC50 = 6.9 6.9 19 2
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]1c1ccc(Br)cc1 10.1021/jm801354e
CHEMBL501854 12690 None 0 Human Functional pEC50 = 6.9 6.9 19 2
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]1c1ccc(Br)cc1 10.1021/jm801354e
162650828 183756 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 285 6 1 3 3.8 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4750271 183756 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 285 6 1 3 3.8 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4802701 183756 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 285 6 1 3 3.8 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
11209786 137327 None 0 Human Functional pEC50 = 7.9 7.9 36 3
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 296 1 1 2 2.7 O=C1c2c(cc(C3CC3)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL375170 137327 None 0 Human Functional pEC50 = 7.9 7.9 36 3
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 296 1 1 2 2.7 O=C1c2c(cc(C3CC3)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
24826867 91129 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 230 1 1 2 1.2 CCc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397890 91129 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 230 1 1 2 1.2 CCc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
24826963 91149 None 0 Human Functional pEC50 = 7.9 7.9 74 2
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 230 0 1 2 1.3 Cc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397910 91149 None 0 Human Functional pEC50 = 7.9 7.9 74 2
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 230 0 1 2 1.3 Cc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
25084025 12705 None 0 Human Functional pEC50 = 7.9 7.9 10 3
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]1c1cccc(Br)c1 10.1021/jm801354e
CHEMBL1187522 12705 None 0 Human Functional pEC50 = 7.9 7.9 10 3
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]1c1cccc(Br)c1 10.1021/jm801354e
CHEMBL506727 12705 None 0 Human Functional pEC50 = 7.9 7.9 10 3
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]1c1cccc(Br)c1 10.1021/jm801354e
44573162 172696 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 406 4 1 4 2.9 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CC[C@@H](Oc2ccccc2Cl)C1 10.1016/j.bmcl.2009.02.071
CHEMBL448971 172696 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 406 4 1 4 2.9 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CC[C@@H](Oc2ccccc2Cl)C1 10.1016/j.bmcl.2009.02.071
137652713 158624 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 340 5 0 4 4.0 COCCN(C)C(=O)c1sc(-c2cccc3ccccc23)nc1C 10.1021/acs.jmedchem.7b00385
CHEMBL4091448 158624 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 340 5 0 4 4.0 COCCN(C)C(=O)c1sc(-c2cccc3ccccc23)nc1C 10.1021/acs.jmedchem.7b00385
122442260 138441 None 0 Human Functional pEC50 = 7.9 7.9 2 3
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 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769543 138441 None 0 Human Functional pEC50 = 7.9 7.9 2 3
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 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771390 138441 None 0 Human Functional pEC50 = 7.9 7.9 2 3
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 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
162645074 183730 None 0 Human Functional pEC50 = 7.8 7.8 20 3
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
CHEMBL4740346 183730 None 0 Human Functional pEC50 = 7.8 7.8 20 3
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
CHEMBL4802388 183730 None 0 Human Functional pEC50 = 7.8 7.8 20 3
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
136044083 111730 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 255 2 2 4 1.5 Oc1nc(Cc2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL3286558 111730 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 255 2 2 4 1.5 Oc1nc(Cc2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
5132936 192942 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 272 1 2 2 3.6 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5181253 192942 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 272 1 2 2 3.6 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5221648 192942 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 272 1 2 2 3.6 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL4913232 216564 None 7 Human Functional pEC50 = 6.8 6.8 6 2
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL None None None C1=CC2(CCNCC2)Oc2ccccc21 10.1021/acsmedchemlett.3c00454
168274581 192923 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 280 1 4 3 2.8 Oc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5176473 192923 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 280 1 4 3 2.8 Oc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221497 192923 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 280 1 4 3 2.8 Oc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
5132936 192942 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 272 1 2 2 3.6 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5181253 192942 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 272 1 2 2 3.6 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5221648 192942 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 272 1 2 2 3.6 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
168274581 192923 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 280 1 4 3 2.8 Oc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5176473 192923 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 280 1 4 3 2.8 Oc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221497 192923 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 280 1 4 3 2.8 Oc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
57469772 195096 None 1 Human Functional pEC50 = 6.8 6.8 3 2
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5396618 195096 None 1 Human Functional pEC50 = 6.8 6.8 3 2
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
1355 2011 None 45 Human Functional pEC50 = 7.8 7.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
142 2011 None 45 Human Functional pEC50 = 7.8 7.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
CHEMBL478 2011 None 45 Human Functional pEC50 = 7.8 7.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
DB12110 2011 None 45 Human Functional pEC50 = 7.8 7.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
162645074 183730 None 0 Human Functional pEC50 = 7.8 7.8 20 3
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
CHEMBL4740346 183730 None 0 Human Functional pEC50 = 7.8 7.8 20 3
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
CHEMBL4802388 183730 None 0 Human Functional pEC50 = 7.8 7.8 20 3
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
1355 2011 None 45 Human Functional pEC50 = 7.8 7.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
142 2011 None 45 Human Functional pEC50 = 7.8 7.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
CHEMBL478 2011 None 45 Human Functional pEC50 = 7.8 7.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
DB12110 2011 None 45 Human Functional pEC50 = 7.8 7.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
1355 2011 None 45 Human Functional pEC50 = 7.8 7.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/acs.jmedchem.7b00385
142 2011 None 45 Human Functional pEC50 = 7.8 7.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/acs.jmedchem.7b00385
CHEMBL478 2011 None 45 Human Functional pEC50 = 7.8 7.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/acs.jmedchem.7b00385
DB12110 2011 None 45 Human Functional pEC50 = 7.8 7.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/acs.jmedchem.7b00385
137647926 157862 None 0 Human Functional pEC50 = 7.8 7.8 58 2
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 300 3 0 4 4.2 CCn1nc(-c2cccc3ccccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
CHEMBL4082753 157862 None 0 Human Functional pEC50 = 7.8 7.8 58 2
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 300 3 0 4 4.2 CCn1nc(-c2cccc3ccccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
44409290 74677 None 0 Human Functional pEC50 = 7.8 7.8 1 2
Efficacy against human recombinant 5HT2C receptor induced intracellular calcium mobilization in CHO cells by FLIPREfficacy against human recombinant 5HT2C receptor induced intracellular calcium mobilization in CHO cells by FLIPR
ChEMBL 273 4 1 4 1.7 C[C@@H]1CNC[C@H]2Cc3ccc(COCC4CC4)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL203013 74677 None 0 Human Functional pEC50 = 7.8 7.8 1 2
Efficacy against human recombinant 5HT2C receptor induced intracellular calcium mobilization in CHO cells by FLIPREfficacy against human recombinant 5HT2C receptor induced intracellular calcium mobilization in CHO cells by FLIPR
ChEMBL 273 4 1 4 1.7 C[C@@H]1CNC[C@H]2Cc3ccc(COCC4CC4)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL4752798 216552 None 0 Human Functional pEC50 = 7.8 7.8 3 2
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 Oc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL4802821 216552 None 0 Human Functional pEC50 = 7.8 7.8 3 2
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 Oc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL4752798 216552 None 0 Human Functional pEC50 = 7.8 7.8 3 2
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 Oc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL4802821 216552 None 0 Human Functional pEC50 = 7.8 7.8 3 2
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 Oc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
122442254 138432 None 0 Human Functional pEC50 = 7.8 7.8 26 3
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 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770963 138432 None 0 Human Functional pEC50 = 7.8 7.8 26 3
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 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771381 138432 None 0 Human Functional pEC50 = 7.8 7.8 26 3
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 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
57888169 193016 None 0 Human Functional pEC50 = 7.8 7.8 4 2
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 3 2 1 4.6 Clc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5194866 193016 None 0 Human Functional pEC50 = 7.8 7.8 4 2
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 3 2 1 4.6 Clc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222124 193016 None 0 Human Functional pEC50 = 7.8 7.8 4 2
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 3 2 1 4.6 Clc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
23652278 62651 None 11 Human Functional pEC50 = 7.8 7.8 16 3
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 C[C@@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL178365 62651 None 11 Human Functional pEC50 = 7.8 7.8 16 3
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 C[C@@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
57888169 193016 None 0 Human Functional pEC50 = 7.8 7.8 4 2
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 3 2 1 4.6 Clc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5194866 193016 None 0 Human Functional pEC50 = 7.8 7.8 4 2
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 3 2 1 4.6 Clc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222124 193016 None 0 Human Functional pEC50 = 7.8 7.8 4 2
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 3 2 1 4.6 Clc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
12901777 138085 None 27 Human Functional pEC50 = 5.8 5.8 - 1
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 188 0 1 2 0.8 O=C1c2ccccc2C2CNCCN12 10.1021/jm0612968
CHEMBL376455 138085 None 27 Human Functional pEC50 = 5.8 5.8 - 1
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 188 0 1 2 0.8 O=C1c2ccccc2C2CNCCN12 10.1021/jm0612968
72197481 102457 None 0 Human Functional pEC50 = 5.8 5.8 -4 2
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 3 2 6 1.8 CN1CCN(c2nc3c(c(Nc4ccc(F)cc4)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
CHEMBL2393240 102457 None 0 Human Functional pEC50 = 5.8 5.8 -4 2
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 3 2 6 1.8 CN1CCN(c2nc3c(c(Nc4ccc(F)cc4)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
CHEMBL3039632 102457 None 0 Human Functional pEC50 = 5.8 5.8 -4 2
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 3 2 6 1.8 CN1CCN(c2nc3c(c(Nc4ccc(F)cc4)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
122442266 138430 None 0 Human Functional pEC50 = 6.8 6.8 51 2
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=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769499 138430 None 0 Human Functional pEC50 = 6.8 6.8 51 2
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=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771379 138430 None 0 Human Functional pEC50 = 6.8 6.8 51 2
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=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
168280043 192968 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5188736 192968 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221859 192968 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
4312735 192983 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5183950 192983 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221924 192983 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
122442266 138430 None 0 Human Functional pEC50 = 6.8 6.8 51 2
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=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769499 138430 None 0 Human Functional pEC50 = 6.8 6.8 51 2
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=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771379 138430 None 0 Human Functional pEC50 = 6.8 6.8 51 2
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=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
168280043 192968 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5188736 192968 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221859 192968 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
4312735 192983 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5183950 192983 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221924 192983 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
137641376 158352 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 356 2 0 4 3.9 Cc1sc(-c2cccc(Cl)c2Cl)nc1C(=O)N1CCOCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4088662 158352 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 356 2 0 4 3.9 Cc1sc(-c2cccc(Cl)c2Cl)nc1C(=O)N1CCOCC1 10.1021/acs.jmedchem.7b00385
137645858 157991 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 324 2 0 4 3.4 O=C(c1cnc(-c2cccc3ccccc23)s1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4084236 157991 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 324 2 0 4 3.4 O=C(c1cnc(-c2cccc3ccccc23)s1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
25071230 111733 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 1 4 1.8 CN(C)c1nc(Cc2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL3286563 111733 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 1 4 1.8 CN(C)c1nc(Cc2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
118733820 120730 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416062 120730 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546957 120730 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
44572258 12691 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 257 3 1 1 4.1 NC[C@H]1C[C@@H]1c1cccc(-c2ccc(Cl)cc2)c1 10.1021/jm801354e
CHEMBL1187449 12691 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 257 3 1 1 4.1 NC[C@H]1C[C@@H]1c1cccc(-c2ccc(Cl)cc2)c1 10.1021/jm801354e
CHEMBL502979 12691 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 257 3 1 1 4.1 NC[C@H]1C[C@@H]1c1cccc(-c2ccc(Cl)cc2)c1 10.1021/jm801354e
11128034 74004 None 10 Human Functional pEC50 = 6.8 6.8 - 1
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 227 1 1 1 3.1 FC(F)(F)c1cccc(C2=CCNCC2)c1 10.1016/j.bmcl.2012.01.122
CHEMBL2011565 74004 None 10 Human Functional pEC50 = 6.8 6.8 - 1
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 227 1 1 1 3.1 FC(F)(F)c1cccc(C2=CCNCC2)c1 10.1016/j.bmcl.2012.01.122
CHEMBL2021626 74004 None 10 Human Functional pEC50 = 6.8 6.8 - 1
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 227 1 1 1 3.1 FC(F)(F)c1cccc(C2=CCNCC2)c1 10.1016/j.bmcl.2012.01.122
10943967 195516 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayAgonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 219 0 1 2 2.4 Fc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5405200 195516 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayAgonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 219 0 1 2 2.4 Fc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
10943967 195516 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayAgonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 219 0 1 2 2.4 Fc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5405200 195516 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayAgonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 219 0 1 2 2.4 Fc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
3572096 193007 None 0 Human Functional pEC50 = 6.8 6.8 2 3
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 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5186011 193007 None 0 Human Functional pEC50 = 6.8 6.8 2 3
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 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222066 193007 None 0 Human Functional pEC50 = 6.8 6.8 2 3
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 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
168288743 193056 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5192627 193056 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222395 193056 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
134138627 148130 None 0 Human Functional pEC50 = 6.8 6.8 -19 2
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 266 1 1 3 2.5 COc1ccc2c(c1Cl)N1CCCNC[C@H]1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3934644 148130 None 0 Human Functional pEC50 = 6.8 6.8 -19 2
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 266 1 1 3 2.5 COc1ccc2c(c1Cl)N1CCCNC[C@H]1CC2 10.1016/j.bmcl.2016.11.016
12834 210385 None 21 Rat Functional pEC50 = 6.8 6.8 -18 2
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 2 1 2.2 CC(N)Cc1c[nH]c2ccc(F)cc12 10.1021/jm970030l
CHEMBL96816 210385 None 21 Rat Functional pEC50 = 6.8 6.8 -18 2
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 2 1 2.2 CC(N)Cc1c[nH]c2ccc(F)cc12 10.1021/jm970030l
57469772 195096 None 1 Human Functional pEC50 = 6.8 6.8 3 2
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5396618 195096 None 1 Human Functional pEC50 = 6.8 6.8 3 2
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
172466878 196691 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 215 0 1 2 2.5 Cc1cccc2c1C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
CHEMBL5430054 196691 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 215 0 1 2 2.5 Cc1cccc2c1C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
CHEMBL4913232 216564 None 7 Human Functional pEC50 = 6.8 6.8 6 2
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL None None None C1=CC2(CCNCC2)Oc2ccccc21 10.1021/acsmedchemlett.3c00454
44420683 84167 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 284 0 1 2 2.6 CC1(C)CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
CHEMBL220789 84167 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 284 0 1 2 2.6 CC1(C)CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
4240627 193043 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5198376 193043 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222297 193043 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
9964324 210392 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
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)Cn1ccc2cc(F)ccc21 10.1021/jm970030l
CHEMBL96883 210392 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
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)Cn1ccc2cc(F)ccc21 10.1021/jm970030l
3572096 193007 None 0 Human Functional pEC50 = 6.8 6.8 2 3
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 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5186011 193007 None 0 Human Functional pEC50 = 6.8 6.8 2 3
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 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222066 193007 None 0 Human Functional pEC50 = 6.8 6.8 2 3
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 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
168288743 193056 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5192627 193056 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222395 193056 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
11302765 84282 None 4 Human Functional pEC50 = 7.8 7.8 74 3
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 284 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL221113 84282 None 4 Human Functional pEC50 = 7.8 7.8 74 3
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 284 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
24826787 91131 None 0 Human Functional pEC50 = 7.8 7.8 6 2
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 270 0 1 2 1.7 O=C1c2c(cccc2C(F)(F)F)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397892 91131 None 0 Human Functional pEC50 = 7.8 7.8 6 2
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 270 0 1 2 1.7 O=C1c2c(cccc2C(F)(F)F)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
71681897 91153 None 0 Human Functional pEC50 = 7.8 7.8 87 2
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 258 0 1 3 1.0 O=C1c2ccc3c(c2C[C@@H]2CNCCN12)OCCC3 10.1016/j.bmcl.2013.04.061
CHEMBL2397914 91153 None 0 Human Functional pEC50 = 7.8 7.8 87 2
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 258 0 1 3 1.0 O=C1c2ccc3c(c2C[C@@H]2CNCCN12)OCCC3 10.1016/j.bmcl.2013.04.061
44572806 12658 None 0 Human Functional pEC50 = 7.8 7.8 4 3
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 177 3 1 2 1.8 COc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL1187195 12658 None 0 Human Functional pEC50 = 7.8 7.8 4 3
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 177 3 1 2 1.8 COc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL493129 12658 None 0 Human Functional pEC50 = 7.8 7.8 4 3
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 177 3 1 2 1.8 COc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
46230097 201822 None 0 Human Functional pEC50 = 7.8 7.8 6 3
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 217 0 2 3 0.6 O=C1NC2CCNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
CHEMBL590816 201822 None 0 Human Functional pEC50 = 7.8 7.8 6 3
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 217 0 2 3 0.6 O=C1NC2CCNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
25070577 111729 None 5 Human Functional pEC50 = 7.8 7.8 6 5
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 304 3 2 4 2.3 CNc1nc(C(F)(F)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL3286557 111729 None 5 Human Functional pEC50 = 7.8 7.8 6 5
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 304 3 2 4 2.3 CNc1nc(C(F)(F)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
137654798 159020 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 4 3.2 Cc1nn(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4095663 159020 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 4 3.2 Cc1nn(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
122442250 138431 None 0 Human Functional pEC50 = 7.8 7.8 8 3
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 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770689 138431 None 0 Human Functional pEC50 = 7.8 7.8 8 3
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 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771380 138431 None 0 Human Functional pEC50 = 7.8 7.8 8 3
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 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442254 138432 None 0 Human Functional pEC50 = 7.8 7.8 26 3
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 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770963 138432 None 0 Human Functional pEC50 = 7.8 7.8 26 3
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 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771381 138432 None 0 Human Functional pEC50 = 7.8 7.8 26 3
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 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
23652278 62651 None 11 Human Functional pEC50 = 7.8 7.8 16 3
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 C[C@@H]1CNCCc2ccc(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178365 62651 None 11 Human Functional pEC50 = 7.8 7.8 16 3
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 C[C@@H]1CNCCc2ccc(Cl)cc21 10.1016/j.bmcl.2004.12.080
1497577 158964 None 14 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human 5-HT2C receptor expressed in human HeLa-K1 cells assessed as potentiation of 5-HT-induced inositol monophosphate release after 20 mins by HTRF assayPositive allosteric modulation of human 5-HT2C receptor expressed in human HeLa-K1 cells assessed as potentiation of 5-HT-induced inositol monophosphate release after 20 mins by HTRF assay
ChEMBL 313 5 1 3 4.7 c1ccc(Cn2cc(CNc3cccnc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00994
CHEMBL4095079 158964 None 14 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human 5-HT2C receptor expressed in human HeLa-K1 cells assessed as potentiation of 5-HT-induced inositol monophosphate release after 20 mins by HTRF assayPositive allosteric modulation of human 5-HT2C receptor expressed in human HeLa-K1 cells assessed as potentiation of 5-HT-induced inositol monophosphate release after 20 mins by HTRF assay
ChEMBL 313 5 1 3 4.7 c1ccc(Cn2cc(CNc3cccnc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00994
11658860 2344 None 24 Dog Functional pEC50 = 7.8 7.8 -1 11
Agonist activity at dog 5HT2C receptorAgonist activity at dog 5HT2C receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
2941 2344 None 24 Dog Functional pEC50 = 7.8 7.8 -1 11
Agonist activity at dog 5HT2C receptorAgonist activity at dog 5HT2C receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
4374 2344 None 24 Dog Functional pEC50 = 7.8 7.8 -1 11
Agonist activity at dog 5HT2C receptorAgonist activity at dog 5HT2C receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
CHEMBL360328 2344 None 24 Dog Functional pEC50 = 7.8 7.8 -1 11
Agonist activity at dog 5HT2C receptorAgonist activity at dog 5HT2C receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
DB04871 2344 None 24 Dog Functional pEC50 = 7.8 7.8 -1 11
Agonist activity at dog 5HT2C receptorAgonist activity at dog 5HT2C receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
122442250 138431 None 0 Human Functional pEC50 = 7.8 7.8 8 3
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 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770689 138431 None 0 Human Functional pEC50 = 7.8 7.8 8 3
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 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771380 138431 None 0 Human Functional pEC50 = 7.8 7.8 8 3
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 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442263 138444 None 0 Human Functional pEC50 = 7.8 7.8 15 3
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 138444 None 0 Human Functional pEC50 = 7.8 7.8 15 3
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 138444 None 0 Human Functional pEC50 = 7.8 7.8 15 3
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
107992 2553 None 33 Human Functional pEC50 = 6.8 6.8 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
165 2553 None 33 Human Functional pEC50 = 6.8 6.8 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
CHEMBL269521 2553 None 33 Human Functional pEC50 = 6.8 6.8 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
DB12111 2553 None 33 Human Functional pEC50 = 6.8 6.8 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
45484910 201033 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 348 4 1 6 1.7 Cc1ccc(Cl)cc1OCc1nc(N2CCNCC2)cc(=O)n1C 10.1016/j.bmcl.2009.07.133
CHEMBL578365 201033 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 348 4 1 6 1.7 Cc1ccc(Cl)cc1OCc1nc(N2CCNCC2)cc(=O)n1C 10.1016/j.bmcl.2009.07.133
10379910 63321 None 0 Human Functional pEC50 = 6.8 6.8 6 2
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 297 2 1 2 3.3 COc1cc2c(cc1Br)C(C(C)C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL179329 63321 None 0 Human Functional pEC50 = 6.8 6.8 6 2
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 297 2 1 2 3.3 COc1cc2c(cc1Br)C(C(C)C)CNCC2 10.1016/j.bmcl.2004.12.080
137637069 156099 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 301 3 0 5 3.6 CCn1nc(-c2cccc3cnccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
CHEMBL4062011 156099 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 301 3 0 5 3.6 CCn1nc(-c2cccc3cnccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
4240627 193043 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5198376 193043 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222297 193043 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
44572761 12684 None 0 Human Functional pEC50 = 6.8 6.8 3 3
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 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1ccccc1O 10.1021/jm801354e
CHEMBL1187377 12684 None 0 Human Functional pEC50 = 6.8 6.8 3 3
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 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1ccccc1O 10.1021/jm801354e
CHEMBL501117 12684 None 0 Human Functional pEC50 = 6.8 6.8 3 3
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 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1ccccc1O 10.1021/jm801354e
107992 2553 None 33 Human Functional pEC50 = 6.8 6.8 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
165 2553 None 33 Human Functional pEC50 = 6.8 6.8 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
CHEMBL269521 2553 None 33 Human Functional pEC50 = 6.8 6.8 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
DB12111 2553 None 33 Human Functional pEC50 = 6.8 6.8 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
137629850 161290 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4073406 161290 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4117722 161290 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
2761023 98820 None 45 Human Functional pEC50 = 6.8 6.8 -43 3
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 198 1 2 1 2.5 C1=C(c2c[nH]c3ccccc23)CCNC1 10.1016/j.bmcl.2012.01.122
CHEMBL2011570 98820 None 45 Human Functional pEC50 = 6.8 6.8 -43 3
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 198 1 2 1 2.5 C1=C(c2c[nH]c3ccccc23)CCNC1 10.1016/j.bmcl.2012.01.122
CHEMBL27811 98820 None 45 Human Functional pEC50 = 6.8 6.8 -43 3
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 198 1 2 1 2.5 C1=C(c2c[nH]c3ccccc23)CCNC1 10.1016/j.bmcl.2012.01.122
45484848 201234 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 342 6 1 6 1.8 Cc1cc(=O)n(CCCOc2ccccc2)c(N2CCNC[C@H]2C)n1 10.1016/j.bmcl.2009.07.133
CHEMBL583192 201234 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 342 6 1 6 1.8 Cc1cc(=O)n(CCCOc2ccccc2)c(N2CCNC[C@H]2C)n1 10.1016/j.bmcl.2009.07.133
2794808 202494 None 46 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 203 1 1 4 1.2 c1cc2occc2c(N2CCNCC2)n1 10.1016/j.bmcl.2009.10.112
CHEMBL595555 202494 None 46 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 203 1 1 4 1.2 c1cc2occc2c(N2CCNCC2)n1 10.1016/j.bmcl.2009.10.112
45485751 200111 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 334 5 1 6 1.4 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1Cl 10.1016/j.bmcl.2009.07.136
CHEMBL570937 200111 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 334 5 1 6 1.4 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1Cl 10.1016/j.bmcl.2009.07.136
137629850 161290 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4073406 161290 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4117722 161290 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
122442268 138440 None 0 Human Functional pEC50 = 6.8 6.8 7 2
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 138440 None 0 Human Functional pEC50 = 6.8 6.8 7 2
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 138440 None 0 Human Functional pEC50 = 6.8 6.8 7 2
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
122461993 138446 None 0 Human Functional pEC50 = 6.8 6.8 3 2
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 138446 None 0 Human Functional pEC50 = 6.8 6.8 3 2
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 138446 None 0 Human Functional pEC50 = 6.8 6.8 3 2
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
122442268 138440 None 0 Human Functional pEC50 = 6.8 6.8 7 2
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 138440 None 0 Human Functional pEC50 = 6.8 6.8 7 2
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 138440 None 0 Human Functional pEC50 = 6.8 6.8 7 2
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
122461993 138446 None 0 Human Functional pEC50 = 6.8 6.8 3 2
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 138446 None 0 Human Functional pEC50 = 6.8 6.8 3 2
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 138446 None 0 Human Functional pEC50 = 6.8 6.8 3 2
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
172466878 196691 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 215 0 1 2 2.5 Cc1cccc2c1C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
CHEMBL5430054 196691 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 215 0 1 2 2.5 Cc1cccc2c1C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
137645024 158161 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 300 3 0 4 4.2 CCn1nc(-c2cccc3ccccc23)cc1-c1ncccn1 10.1021/acs.jmedchem.7b00385
CHEMBL4086216 158161 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 300 3 0 4 4.2 CCn1nc(-c2cccc3ccccc23)cc1-c1ncccn1 10.1021/acs.jmedchem.7b00385
16115644 137047 None 0 Human Functional pEC50 = 7.8 7.8 1 3
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 CCc1cc2c(cc1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374436 137047 None 0 Human Functional pEC50 = 7.8 7.8 1 3
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 CCc1cc2c(cc1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
11666237 89146 None 0 Human Functional pEC50 = 7.8 7.8 30 3
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 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337496 89146 None 0 Human Functional pEC50 = 7.8 7.8 30 3
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 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365472 89146 None 0 Human Functional pEC50 = 7.8 7.8 30 3
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 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
137631812 156659 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 366 2 1 4 4.3 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCCC(O)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4068476 156659 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 366 2 1 4 4.3 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCCC(O)CC1 10.1021/acs.jmedchem.7b00385
1355 2011 None 45 Human Functional pEC50 = 6.8 6.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.063
142 2011 None 45 Human Functional pEC50 = 6.8 6.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.063
CHEMBL478 2011 None 45 Human Functional pEC50 = 6.8 6.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.063
DB12110 2011 None 45 Human Functional pEC50 = 6.8 6.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.063
44573165 187309 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 390 6 1 5 2.2 COc1cc(S(=O)(=O)N(C)Cc2ccccc2)c(OC)c2c1CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492362 187309 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 390 6 1 5 2.2 COc1cc(S(=O)(=O)N(C)Cc2ccccc2)c(OC)c2c1CCNCC2 10.1016/j.bmcl.2009.02.071
1355 2011 None 45 Human Functional pEC50 = 6.8 6.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
142 2011 None 45 Human Functional pEC50 = 6.8 6.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
CHEMBL478 2011 None 45 Human Functional pEC50 = 6.8 6.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
DB12110 2011 None 45 Human Functional pEC50 = 6.8 6.8 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
14515725 87344 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
CHEMBL2331807 87344 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
58911604 91140 None 1 Human Functional pEC50 = 6.8 6.8 - 1
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=C1c2ccc(Cl)cc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397901 91140 None 1 Human Functional pEC50 = 6.8 6.8 - 1
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=C1c2ccc(Cl)cc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
168274213 192919 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)cc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5178487 192919 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)cc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5221472 192919 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)cc1O 10.1021/acsmedchemlett.1c00694
168291006 193084 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 380 1 2 2 5.2 Cc1cc(C2NCCc3c2[nH]c2ccc(Cl)cc32)sc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5199780 193084 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 380 1 2 2 5.2 Cc1cc(C2NCCc3c2[nH]c2ccc(Cl)cc32)sc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5222544 193084 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 380 1 2 2 5.2 Cc1cc(C2NCCc3c2[nH]c2ccc(Cl)cc32)sc1Br 10.1021/acsmedchemlett.1c00694
168274213 192919 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)cc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5178487 192919 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)cc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5221472 192919 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)cc1O 10.1021/acsmedchemlett.1c00694
168291006 193084 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 380 1 2 2 5.2 Cc1cc(C2NCCc3c2[nH]c2ccc(Cl)cc32)sc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5199780 193084 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 380 1 2 2 5.2 Cc1cc(C2NCCc3c2[nH]c2ccc(Cl)cc32)sc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5222544 193084 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 380 1 2 2 5.2 Cc1cc(C2NCCc3c2[nH]c2ccc(Cl)cc32)sc1Br 10.1021/acsmedchemlett.1c00694
16115148 84873 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 206 0 1 2 0.9 O=C1c2c(F)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL223469 84873 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 206 0 1 2 0.9 O=C1c2c(F)cccc2C2CNCCN12 10.1021/jm0612968
14515725 87344 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
CHEMBL2331807 87344 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
58911681 91019 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 216 0 1 2 1.0 C[C@@H]1CN2C(=O)c3ccccc3C[C@@H]2CN1 10.1016/j.bmcl.2013.04.061
CHEMBL2396668 91019 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 216 0 1 2 1.0 C[C@@H]1CN2C(=O)c3ccccc3C[C@@H]2CN1 10.1016/j.bmcl.2013.04.061
168282202 192993 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185430 192993 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221991 192993 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
45484742 200974 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 243 3 2 3 1.7 c1ccc(COc2n[nH]c3c2CCNCC3)cc1 10.1016/j.bmcl.2009.07.063
CHEMBL577903 200974 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 243 3 2 3 1.7 c1ccc(COc2n[nH]c3c2CCNCC3)cc1 10.1016/j.bmcl.2009.07.063
185717 4449 None 16 Human Functional pEC50 = 5.8 5.8 - 1
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 193 1 1 1 2.7 Clc1ccc(C2=CCNCC2)cc1 10.1016/j.bmcl.2012.01.122
CHEMBL101664 4449 None 16 Human Functional pEC50 = 5.8 5.8 - 1
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 193 1 1 1 2.7 Clc1ccc(C2=CCNCC2)cc1 10.1016/j.bmcl.2012.01.122
CHEMBL2011566 4449 None 16 Human Functional pEC50 = 5.8 5.8 - 1
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 193 1 1 1 2.7 Clc1ccc(C2=CCNCC2)cc1 10.1016/j.bmcl.2012.01.122
118733784 120726 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 271 6 1 3 3.1 CSCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416044 120726 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 271 6 1 3 3.1 CSCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546953 120726 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 271 6 1 3 3.1 CSCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
168282202 192993 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185430 192993 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221991 192993 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
16115267 84827 None 0 Human Functional pEC50 = 7.8 7.8 2 3
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 270 0 1 2 2.2 C[C@@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL223272 84827 None 0 Human Functional pEC50 = 7.8 7.8 2 3
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 270 0 1 2 2.2 C[C@@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
11176570 91154 None 1 Human Functional pEC50 = 7.8 7.8 6 2
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 270 0 1 2 1.7 O=C1c2cc(C(F)(F)F)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397915 91154 None 1 Human Functional pEC50 = 7.8 7.8 6 2
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 270 0 1 2 1.7 O=C1c2cc(C(F)(F)F)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
44572170 12469 None 0 Human Functional pEC50 = 7.8 7.8 2 3
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]1c1ccc(Cl)cc1Cl 10.1021/jm801354e
CHEMBL1186164 12469 None 0 Human Functional pEC50 = 7.8 7.8 2 3
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]1c1ccc(Cl)cc1Cl 10.1021/jm801354e
CHEMBL452458 12469 None 0 Human Functional pEC50 = 7.8 7.8 2 3
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]1c1ccc(Cl)cc1Cl 10.1021/jm801354e
70683433 74484 None 0 Human Functional pEC50 = 7.8 7.8 18 3
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 191 4 1 2 2.1 CCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2022185 74484 None 0 Human Functional pEC50 = 7.8 7.8 18 3
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 191 4 1 2 2.1 CCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2027895 74484 None 0 Human Functional pEC50 = 7.8 7.8 18 3
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 191 4 1 2 2.1 CCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
53325936 56818 None 0 Human Functional pEC50 = 7.8 7.8 12 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 335 3 1 6 1.7 c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643675 56818 None 0 Human Functional pEC50 = 7.8 7.8 12 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 335 3 1 6 1.7 c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
137633983 156562 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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(c1nc(-c2cccc(Cl)c2Cl)cs1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4067417 156562 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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(c1nc(-c2cccc(Cl)c2Cl)cs1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
122442307 138442 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3770950 138442 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771391 138442 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
166 3359 None 19 Human Functional pEC50 = 7.8 7.8 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
3045227 3359 None 19 Human Functional pEC50 = 7.8 7.8 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
CHEMBL76781 3359 None 19 Human Functional pEC50 = 7.8 7.8 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
122442307 138442 None 0 Human Functional pEC50 = 7.7 7.7 1 2
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 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3770950 138442 None 0 Human Functional pEC50 = 7.7 7.7 1 2
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 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771391 138442 None 0 Human Functional pEC50 = 7.7 7.7 1 2
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 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
54583743 61483 None 0 Human Functional pEC50 = 6.8 6.8 -5 2
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 273 2 1 3 2.4 Clc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
CHEMBL1770382 61483 None 0 Human Functional pEC50 = 6.8 6.8 -5 2
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 273 2 1 3 2.4 Clc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
44383397 59260 None 0 Human Functional pEC50 = 6.8 6.8 6 2
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 246 3 1 2 3.1 CNCCc1cn2c3c(cc(F)cc13)CCC2C 10.1016/s0960-894x(00)00141-4
CHEMBL170319 59260 None 0 Human Functional pEC50 = 6.8 6.8 6 2
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 246 3 1 2 3.1 CNCCc1cn2c3c(cc(F)cc13)CCC2C 10.1016/s0960-894x(00)00141-4
44412150 77762 None 0 Human Functional pEC50 = 6.8 6.8 1 3
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 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CCC3CNCC32)n1 10.1016/j.bmcl.2006.03.007
CHEMBL208936 77762 None 0 Human Functional pEC50 = 6.8 6.8 1 3
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 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CCC3CNCC32)n1 10.1016/j.bmcl.2006.03.007
146464686 192106 None 0 Human Functional pEC50 = 4.8 4.8 -8 2
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 266 1 3 4 1.9 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5201492 192106 None 0 Human Functional pEC50 = 4.8 4.8 -8 2
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 266 1 3 4 1.9 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
137633009 156503 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 4 3.1 Cn1cc(-c2cccc3ccccc23)nc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4066653 156503 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 4 3.1 Cn1cc(-c2cccc3ccccc23)nc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
46884099 8206 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 348 4 2 2 4.0 O=C(NCc1ccc(-c2cc(Cl)cc(Cl)c2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1092167 8206 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 348 4 2 2 4.0 O=C(NCc1ccc(-c2cc(Cl)cc(Cl)c2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
118733782 120725 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 255 6 1 3 2.4 COCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416043 120725 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 255 6 1 3 2.4 COCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546952 120725 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 255 6 1 3 2.4 COCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
11150514 84911 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@H]2CNCCN12 10.1021/jm0612968
CHEMBL223584 84911 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@H]2CNCCN12 10.1021/jm0612968
3939391 193059 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 316 1 2 1 4.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5197949 193059 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 316 1 2 1 4.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222415 193059 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 316 1 2 1 4.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
44573223 187306 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 296 2 1 4 0.4 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCOCC1 10.1016/j.bmcl.2009.02.071
CHEMBL492357 187306 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 296 2 1 4 0.4 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCOCC1 10.1016/j.bmcl.2009.02.071
3939391 193059 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 316 1 2 1 4.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5197949 193059 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 316 1 2 1 4.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222415 193059 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 316 1 2 1 4.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
137631000 161232 None 0 Human Functional pEC50 = 5.7 5.7 1 2
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 319 6 1 2 4.4 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1Cl 10.1021/acs.jmedchem.7b00584
CHEMBL4083787 161232 None 0 Human Functional pEC50 = 5.7 5.7 1 2
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 319 6 1 2 4.4 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1Cl 10.1021/acs.jmedchem.7b00584
CHEMBL4117262 161232 None 0 Human Functional pEC50 = 5.7 5.7 1 2
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 319 6 1 2 4.4 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1Cl 10.1021/acs.jmedchem.7b00584
137631000 161232 None 0 Human Functional pEC50 = 5.7 5.7 1 2
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 319 6 1 2 4.4 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1Cl 10.1021/acs.jmedchem.7b00584
CHEMBL4083787 161232 None 0 Human Functional pEC50 = 5.7 5.7 1 2
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 319 6 1 2 4.4 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1Cl 10.1021/acs.jmedchem.7b00584
CHEMBL4117262 161232 None 0 Human Functional pEC50 = 5.7 5.7 1 2
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 319 6 1 2 4.4 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1Cl 10.1021/acs.jmedchem.7b00584
10966027 204448 None 36 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 219 1 1 4 1.7 c1cc2sccc2c(N2CCNCC2)n1 10.1016/j.bmcl.2009.10.112
CHEMBL608135 204448 None 36 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 219 1 1 4 1.7 c1cc2sccc2c(N2CCNCC2)n1 10.1016/j.bmcl.2009.10.112
137643658 158294 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 363 3 1 4 3.4 Cc1nc(-c2cccc3ccccc23)n(C)c1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4087951 158294 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 363 3 1 4 3.4 Cc1nc(-c2cccc3ccccc23)n(C)c1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
53317924 56867 None 0 Human Functional pEC50 = 6.7 6.7 6 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 406 4 1 7 1.7 CC(=O)N(C)c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643858 56867 None 0 Human Functional pEC50 = 6.7 6.7 6 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 406 4 1 7 1.7 CC(=O)N(C)c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
162643473 183721 None 0 Human Functional pEC50 = 7.7 7.7 14 3
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 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4777303 183721 None 0 Human Functional pEC50 = 7.7 7.7 14 3
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 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802306 183721 None 0 Human Functional pEC50 = 7.7 7.7 14 3
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 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
44302714 102814 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 291 0 2 3 2.6 FC(F)(F)c1cc2c(cc1Cl)N1CCNC[C@@H]1CN2 10.1016/s0960-894x(00)00400-5
CHEMBL305123 102814 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 291 0 2 3 2.6 FC(F)(F)c1cc2c(cc1Cl)N1CCNC[C@@H]1CN2 10.1016/s0960-894x(00)00400-5
10017993 203530 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 305 0 2 3 2.1 O=C1Nc2cc(C(F)(F)F)c(Cl)cc2N2CCNC[C@H]12 10.1016/s0960-894x(00)00400-5
CHEMBL60280 203530 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 305 0 2 3 2.1 O=C1Nc2cc(C(F)(F)F)c(Cl)cc2N2CCNC[C@H]12 10.1016/s0960-894x(00)00400-5
162643473 183721 None 0 Human Functional pEC50 = 7.7 7.7 14 3
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 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4777303 183721 None 0 Human Functional pEC50 = 7.7 7.7 14 3
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 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802306 183721 None 0 Human Functional pEC50 = 7.7 7.7 14 3
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 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
11160564 63324 None 2 Human Functional pEC50 = 7.7 7.7 7 3
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 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1021/jm0709034
CHEMBL179337 63324 None 2 Human Functional pEC50 = 7.7 7.7 7 3
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 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1021/jm0709034
24773728 94913 None 0 Human Functional pEC50 = 7.7 7.7 15 3
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 209 1 1 1 3.0 CC[C@@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL253810 94913 None 0 Human Functional pEC50 = 7.7 7.7 15 3
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 209 1 1 1 3.0 CC[C@@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
11264345 130467 None 3 Human Functional pEC50 = 7.7 7.7 38 3
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 213 0 1 1 2.7 CC1CNCCc2ccc(Cl)c(F)c21 10.1021/jm0709034
CHEMBL368016 130467 None 3 Human Functional pEC50 = 7.7 7.7 38 3
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 213 0 1 1 2.7 CC1CNCCc2ccc(Cl)c(F)c21 10.1021/jm0709034
134132665 144645 None 0 Human Functional pEC50 = 7.7 7.7 39 2
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 258 2 1 3 2.3 c1cc(OC2CCC2)c2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3907399 144645 None 0 Human Functional pEC50 = 7.7 7.7 39 2
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 258 2 1 3 2.3 c1cc(OC2CCC2)c2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
134148291 150169 None 0 Human Functional pEC50 = 7.7 7.7 31 2
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 CCCc1ccc2c(c1)CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3950846 150169 None 0 Human Functional pEC50 = 7.7 7.7 31 2
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 CCCc1ccc2c(c1)CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
134155992 151481 None 0 Human Functional pEC50 = 7.7 7.7 398 2
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 310 2 1 2 3.5 Fc1ccc2c(c1Cc1ccccc1)CC[C@@H]1CNCCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3961589 151481 None 0 Human Functional pEC50 = 7.7 7.7 398 2
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 310 2 1 2 3.5 Fc1ccc2c(c1Cc1ccccc1)CC[C@@H]1CNCCCN21 10.1016/j.bmcl.2016.11.016
134151626 153493 None 0 Human Functional pEC50 = 7.7 7.7 63 2
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 2 1 3 1.6 COCc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3978882 153493 None 0 Human Functional pEC50 = 7.7 7.7 63 2
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 2 1 3 1.6 COCc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
25070582 61474 None 27 Human Functional pEC50 = 6.7 6.7 -2 9
Agonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 61474 None 27 Human Functional pEC50 = 6.7 6.7 -2 9
Agonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
25070582 61474 None 27 Human Functional pEC50 = 6.7 6.7 -2 9
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 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1021/jm5003292
CHEMBL1770373 61474 None 27 Human Functional pEC50 = 6.7 6.7 -2 9
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 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1021/jm5003292
137655535 159087 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 303 3 0 5 3.5 CCn1nc(-c2cccc3ccccc23)cc1-c1ncnn1C 10.1021/acs.jmedchem.7b00385
CHEMBL4096385 159087 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 303 3 0 5 3.5 CCn1nc(-c2cccc3ccccc23)cc1-c1ncnn1C 10.1021/acs.jmedchem.7b00385
155512645 169786 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 169786 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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
168275195 192932 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 Cc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5181991 192932 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 Cc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221539 192932 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 Cc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
168282109 192992 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 3 3.7 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5183544 192992 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 3 3.7 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221988 192992 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 3 3.7 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
54585651 61472 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 4 1 3 2.3 c1ccc(CCCc2ncc3c(n2)CCNC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770367 61472 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 4 1 3 2.3 c1ccc(CCCc2ncc3c(n2)CCNC3)cc1 10.1016/j.bmcl.2010.11.120
168275195 192932 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 Cc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5181991 192932 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 Cc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221539 192932 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 Cc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
168282109 192992 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 3 3.7 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5183544 192992 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 3 3.7 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221988 192992 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 3 3.7 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
54581791 61484 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
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 273 2 1 3 2.4 Clc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770383 61484 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
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 273 2 1 3 2.4 Clc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
71681898 91123 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 216 0 0 2 1.0 CN1CCN2C(=O)c3ccccc3C[C@@H]2C1 10.1016/j.bmcl.2013.04.061
CHEMBL2397884 91123 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 216 0 0 2 1.0 CN1CCN2C(=O)c3ccccc3C[C@@H]2C1 10.1016/j.bmcl.2013.04.061
54583742 61476 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 Fc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
CHEMBL1770375 61476 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 Fc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
168279029 192963 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Br)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5188817 192963 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Br)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5221792 192963 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Br)ccc1O 10.1021/acsmedchemlett.1c00694
168279029 192963 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Br)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5188817 192963 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Br)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5221792 192963 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Br)ccc1O 10.1021/acsmedchemlett.1c00694
44572254 12558 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 263 3 1 2 4.2 NC[C@H]1C[C@@H]1c1ccccc1-c1cc2ccccc2o1 10.1021/jm801354e
CHEMBL1186710 12558 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 263 3 1 2 4.2 NC[C@H]1C[C@@H]1c1ccccc1-c1cc2ccccc2o1 10.1021/jm801354e
CHEMBL475021 12558 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 263 3 1 2 4.2 NC[C@H]1C[C@@H]1c1ccccc1-c1cc2ccccc2o1 10.1021/jm801354e
44573218 193166 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
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 320 3 2 3 2.3 O=S(=O)(Nc1ccccc1F)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL522349 193166 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
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 320 3 2 3 2.3 O=S(=O)(Nc1ccccc1F)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
24773900 123499 None 6 Human Functional pEC50 = 6.7 6.7 1 3
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)C(C)CNCC2 10.1021/jm0709034
CHEMBL361742 123499 None 6 Human Functional pEC50 = 6.7 6.7 1 3
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)C(C)CNCC2 10.1021/jm0709034
24773978 154505 None 0 Human Functional pEC50 = 6.7 6.7 7 2
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 209 0 1 1 2.8 CC1(C)CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL398926 154505 None 0 Human Functional pEC50 = 6.7 6.7 7 2
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 209 0 1 1 2.8 CC1(C)CNCCc2ccc(Cl)cc21 10.1021/jm0709034
168275014 192929 None 0 Human Functional pEC50 = 6.7 6.7 3 2
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 218 1 2 1 2.9 CCC1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177386 192929 None 0 Human Functional pEC50 = 6.7 6.7 3 2
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 218 1 2 1 2.9 CCC1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221524 192929 None 0 Human Functional pEC50 = 6.7 6.7 3 2
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 218 1 2 1 2.9 CCC1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
134141640 147364 None 0 Human Functional pEC50 = 6.7 6.7 3 2
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 250 0 1 2 2.8 Clc1ccc2c(c1)CCC1CCNCCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3928762 147364 None 0 Human Functional pEC50 = 6.7 6.7 3 2
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 250 0 1 2 2.8 Clc1ccc2c(c1)CCC1CCNCCCN21 10.1016/j.bmcl.2016.11.016
166 3359 None 19 Rat Functional pEC50 = 6.7 6.7 -79 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm970030l
3045227 3359 None 19 Rat Functional pEC50 = 6.7 6.7 -79 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm970030l
CHEMBL76781 3359 None 19 Rat Functional pEC50 = 6.7 6.7 -79 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm970030l
18516642 111873 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
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 254 2 1 2 3.5 Cc1ccc2c(c1)-c1c(ccn1CC(C)N)C2(C)C 10.1021/jm970030l
CHEMBL328761 111873 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
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 254 2 1 2 3.5 Cc1ccc2c(c1)-c1c(ccn1CC(C)N)C2(C)C 10.1021/jm970030l
10330734 157028 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
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
CHEMBL40726 157028 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
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
19036480 209925 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
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 258 2 1 2 3.3 CC(N)Cn1ccc2c1-c1cc(F)ccc1C2(C)C 10.1021/jm970030l
CHEMBL94272 209925 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
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 258 2 1 2 3.3 CC(N)Cn1ccc2c1-c1cc(F)ccc1C2(C)C 10.1021/jm970030l
12763911 74002 None 44 Human Functional pEC50 = 5.7 5.7 - 1
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 175 1 1 1 2.5 Cc1cccc(C2CCNCC2)c1 10.1016/j.bmcl.2012.01.122
CHEMBL2011548 74002 None 44 Human Functional pEC50 = 5.7 5.7 - 1
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 175 1 1 1 2.5 Cc1cccc(C2CCNCC2)c1 10.1016/j.bmcl.2012.01.122
CHEMBL2021617 74002 None 44 Human Functional pEC50 = 5.7 5.7 - 1
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 175 1 1 1 2.5 Cc1cccc(C2CCNCC2)c1 10.1016/j.bmcl.2012.01.122
10538127 98132 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
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 242 3 1 3 2.4 COc1ccc2c(c1)Cc1ccn(CC(C)N)c1-2 10.1021/jm970030l
CHEMBL273304 98132 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
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 242 3 1 3 2.4 COc1ccc2c(c1)Cc1ccn(CC(C)N)c1-2 10.1021/jm970030l
10753358 98624 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
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 252 2 1 2 2.8 CC(N)Cn1ccc2cc(Br)ccc21 10.1021/jm970030l
CHEMBL276673 98624 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
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 252 2 1 2 2.8 CC(N)Cn1ccc2cc(Br)ccc21 10.1021/jm970030l
9855823 112042 None 1 Rat Functional pEC50 = 5.7 5.7 - 1
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 208 2 1 2 2.6 CC(N)Cn1ccc2cc(Cl)ccc21 10.1021/jm970030l
CHEMBL328844 112042 None 1 Rat Functional pEC50 = 5.7 5.7 - 1
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 208 2 1 2 2.6 CC(N)Cn1ccc2cc(Cl)ccc21 10.1021/jm970030l
82045793 195951 None 1 Human Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1ccc2c(c1)C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
CHEMBL5414076 195951 None 1 Human Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1ccc2c(c1)C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
82045782 196339 None 1 Human Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 215 0 1 2 2.5 Cc1cccc2c1OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5421733 196339 None 1 Human Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 215 0 1 2 2.5 Cc1cccc2c1OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
172456495 196441 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 207 0 1 2 2.1 Clc1ccc2c(c1)OC1(C=C2)CNC1 10.1021/acsmedchemlett.3c00454
CHEMBL5424008 196441 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 207 0 1 2 2.1 Clc1ccc2c(c1)OC1(C=C2)CNC1 10.1021/acsmedchemlett.3c00454
11695000 89105 None 0 Human Functional pEC50 = 8.7 8.7 7 3
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 89105 None 0 Human Functional pEC50 = 8.7 8.7 7 3
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 89105 None 0 Human Functional pEC50 = 8.7 8.7 7 3
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
46230098 201785 None 0 Human Functional pEC50 = 8.7 8.7 30 4
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 231 0 2 3 0.9 Cc1cccc2c1C(=O)NC1CCNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590580 201785 None 0 Human Functional pEC50 = 8.7 8.7 30 4
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 231 0 2 3 0.9 Cc1cccc2c1C(=O)NC1CCNCCN21 10.1016/j.bmcl.2009.12.014
137661673 159443 None 0 Human Functional pEC50 = 8.7 8.7 1 3
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 301 3 0 5 3.6 CCn1nc(-c2cccc3cccnc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
CHEMBL4100216 159443 None 0 Human Functional pEC50 = 8.7 8.7 1 3
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 301 3 0 5 3.6 CCn1nc(-c2cccc3cccnc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
10064386 63337 None 2 Human Functional pEC50 = 8.7 8.7 30 3
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 317 1 1 2 2.5 COc1cc2c(cc1I)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL179378 63337 None 2 Human Functional pEC50 = 8.7 8.7 30 3
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 317 1 1 2 2.5 COc1cc2c(cc1I)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
11658860 2344 None 24 Human Functional pEC50 = 8.7 8.7 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.7b00584
2941 2344 None 24 Human Functional pEC50 = 8.7 8.7 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.7b00584
4374 2344 None 24 Human Functional pEC50 = 8.7 8.7 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.7b00584
CHEMBL360328 2344 None 24 Human Functional pEC50 = 8.7 8.7 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.7b00584
DB04871 2344 None 24 Human Functional pEC50 = 8.7 8.7 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.7b00584
57799324 89126 None 0 Human Functional pEC50 = 8.7 8.7 9 2
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 236 0 2 2 1.4 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337501 89126 None 0 Human Functional pEC50 = 8.7 8.7 9 2
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 236 0 2 2 1.4 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365359 89126 None 0 Human Functional pEC50 = 8.7 8.7 9 2
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 236 0 2 2 1.4 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
166 3359 None 19 Human Functional pEC50 = 8.7 8.7 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/acs.jmedchem.6b01194
3045227 3359 None 19 Human Functional pEC50 = 8.7 8.7 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/acs.jmedchem.6b01194
CHEMBL76781 3359 None 19 Human Functional pEC50 = 8.7 8.7 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/acs.jmedchem.6b01194
166 3359 None 19 Human Functional pEC50 = 8.7 8.7 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/acs.jmedchem.6b01194
3045227 3359 None 19 Human Functional pEC50 = 8.7 8.7 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/acs.jmedchem.6b01194
CHEMBL76781 3359 None 19 Human Functional pEC50 = 8.7 8.7 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/acs.jmedchem.6b01194
46830177 8063 None 22 Human Functional pEC50 = 8.6 8.6 190 2
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 378 6 2 4 3.6 COc1cc(OC2CCC(C)(C)CC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1091105 8063 None 22 Human Functional pEC50 = 8.6 8.6 190 2
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 378 6 2 4 3.6 COc1cc(OC2CCC(C)(C)CC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
10219723 179215 None 16 Human Functional pEC50 = 8.6 8.6 17 3
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells by [3H]-inositol phosphate accumulation assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells by [3H]-inositol phosphate accumulation assay
ChEMBL 185 2 1 1 2.7 CC(N)Cc1ccc2ccccc2c1 10.1039/C6MD00245E
CHEMBL471839 179215 None 16 Human Functional pEC50 = 8.6 8.6 17 3
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells by [3H]-inositol phosphate accumulation assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells by [3H]-inositol phosphate accumulation assay
ChEMBL 185 2 1 1 2.7 CC(N)Cc1ccc2ccccc2c1 10.1039/C6MD00245E
137630842 161208 None 0 Human Functional pEC50 = 8.6 8.6 4 3
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 347 9 1 3 4.1 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.7b00584
CHEMBL4091672 161208 None 0 Human Functional pEC50 = 8.6 8.6 4 3
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 347 9 1 3 4.1 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.7b00584
CHEMBL4117120 161208 None 0 Human Functional pEC50 = 8.6 8.6 4 3
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 347 9 1 3 4.1 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.7b00584
137630842 161208 None 0 Human Functional pEC50 = 8.6 8.6 4 3
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 347 9 1 3 4.1 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.7b00584
CHEMBL4091672 161208 None 0 Human Functional pEC50 = 8.6 8.6 4 3
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 347 9 1 3 4.1 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.7b00584
CHEMBL4117120 161208 None 0 Human Functional pEC50 = 8.6 8.6 4 3
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 347 9 1 3 4.1 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.7b00584
11171464 149568 None 0 Human Functional pEC50 = 8.6 8.6 25 2
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 188 0 1 2 1.4 c1ccc2c(c1)CC[C@@H]1CNCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3946277 149568 None 0 Human Functional pEC50 = 8.6 8.6 25 2
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 188 0 1 2 1.4 c1ccc2c(c1)CC[C@@H]1CNCCN21 10.1016/j.bmcl.2016.11.016
162657367 183788 None 0 Human Functional pEC50 = 8.6 8.6 32 3
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 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4756903 183788 None 0 Human Functional pEC50 = 8.6 8.6 32 3
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 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803034 183788 None 0 Human Functional pEC50 = 8.6 8.6 32 3
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 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
57799306 89143 None 0 Human Functional pEC50 = 8.6 8.6 12 3
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 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337493 89143 None 0 Human Functional pEC50 = 8.6 8.6 12 3
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 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365469 89143 None 0 Human Functional pEC50 = 8.6 8.6 12 3
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 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
162657367 183788 None 0 Human Functional pEC50 = 8.6 8.6 32 3
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 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4756903 183788 None 0 Human Functional pEC50 = 8.6 8.6 32 3
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 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803034 183788 None 0 Human Functional pEC50 = 8.6 8.6 32 3
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 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
72197669 102542 None 0 Human Functional pEC50 = 8.6 8.6 -2 2
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 348 4 2 4 3.6 Fc1ccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL2393247 102542 None 0 Human Functional pEC50 = 8.6 8.6 -2 2
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 348 4 2 4 3.6 Fc1ccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL3040281 102542 None 0 Human Functional pEC50 = 8.6 8.6 -2 2
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 348 4 2 4 3.6 Fc1ccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
11658860 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
2941 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
4374 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
CHEMBL360328 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
DB04871 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
11658860 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.7b00584
2941 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.7b00584
4374 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.7b00584
CHEMBL360328 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.7b00584
DB04871 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.7b00584
11658860 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
2941 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
4374 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
CHEMBL360328 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
DB04871 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
162650400 183755 None 0 Human Functional pEC50 = 8.6 8.6 22 3
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
CHEMBL4748110 183755 None 0 Human Functional pEC50 = 8.6 8.6 22 3
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
CHEMBL4802669 183755 None 0 Human Functional pEC50 = 8.6 8.6 22 3
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
162670523 183856 None 0 Human Functional pEC50 = 8.6 8.6 20 3
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 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4790652 183856 None 0 Human Functional pEC50 = 8.6 8.6 20 3
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 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803766 183856 None 0 Human Functional pEC50 = 8.6 8.6 20 3
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 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
162650400 183755 None 0 Human Functional pEC50 = 8.6 8.6 22 3
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
CHEMBL4748110 183755 None 0 Human Functional pEC50 = 8.6 8.6 22 3
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
CHEMBL4802669 183755 None 0 Human Functional pEC50 = 8.6 8.6 22 3
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
162670523 183856 None 0 Human Functional pEC50 = 8.6 8.6 20 3
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 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4790652 183856 None 0 Human Functional pEC50 = 8.6 8.6 20 3
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 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803766 183856 None 0 Human Functional pEC50 = 8.6 8.6 20 3
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 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
11658860 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
2941 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
4374 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
CHEMBL360328 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
DB04871 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
11658860 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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 2344 None 24 Human Functional pEC50 = 8.6 8.6 1 11
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
155532108 176671 None 0 Human Functional pEC50 = 8.6 8.6 -1 3
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 183 2 1 1 2.0 NC[C@H]1C[C@]1(F)c1cccc(F)c1 10.1016/j.ejmech.2019.111626
CHEMBL4466591 176671 None 0 Human Functional pEC50 = 8.6 8.6 -1 3
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 183 2 1 1 2.0 NC[C@H]1C[C@]1(F)c1cccc(F)c1 10.1016/j.ejmech.2019.111626
CHEMBL4597360 176671 None 0 Human Functional pEC50 = 8.6 8.6 -1 3
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 183 2 1 1 2.0 NC[C@H]1C[C@]1(F)c1cccc(F)c1 10.1016/j.ejmech.2019.111626
5 139 None 45 Rat Functional pEC50 = 8.6 8.6 -40 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
5202 139 None 45 Rat Functional pEC50 = 8.6 8.6 -40 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
CHEMBL39 139 None 45 Rat Functional pEC50 = 8.6 8.6 -40 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
DB08839 139 None 45 Rat Functional pEC50 = 8.6 8.6 -40 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
11737939 84261 None 0 Human Functional pEC50 = 7.7 7.7 2 2
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 256 0 1 2 2.1 O=C1c2c(ccc(Cl)c2Cl)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL220900 84261 None 0 Human Functional pEC50 = 7.7 7.7 2 2
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 256 0 1 2 2.1 O=C1c2c(ccc(Cl)c2Cl)[C@@H]2CNCCN12 10.1021/jm0612968
11499800 89141 None 0 Human Functional pEC50 = 7.7 7.7 10 3
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 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337503 89141 None 0 Human Functional pEC50 = 7.7 7.7 10 3
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 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365465 89141 None 0 Human Functional pEC50 = 7.7 7.7 10 3
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 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
162652983 183769 None 0 Human Functional pEC50 = 7.7 7.7 12 3
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 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4752412 183769 None 0 Human Functional pEC50 = 7.7 7.7 12 3
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 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802814 183769 None 0 Human Functional pEC50 = 7.7 7.7 12 3
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 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
4407909 192975 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192975 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192975 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
137660072 159501 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 365 3 1 3 4.7 Cc1cc(-c2cccc3ccccc23)sc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4100812 159501 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 365 3 1 3 4.7 Cc1cc(-c2cccc3ccccc23)sc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
11160564 63324 None 2 Human Functional pEC50 = 7.7 7.7 7 3
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 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL179337 63324 None 2 Human Functional pEC50 = 7.7 7.7 7 3
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 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1016/j.bmcl.2004.12.080
72197484 102549 None 0 Human Functional pEC50 = 7.7 7.7 -1 9
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 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL2393243 102549 None 0 Human Functional pEC50 = 7.7 7.7 -1 9
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 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL3040324 102549 None 0 Human Functional pEC50 = 7.7 7.7 -1 9
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 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
168276733 192940 None 0 Human Functional pEC50 = 7.7 7.7 4 2
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 272 1 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5180401 192940 None 0 Human Functional pEC50 = 7.7 7.7 4 2
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 272 1 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5221642 192940 None 0 Human Functional pEC50 = 7.7 7.7 4 2
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 272 1 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
162652983 183769 None 0 Human Functional pEC50 = 7.7 7.7 12 3
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 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4752412 183769 None 0 Human Functional pEC50 = 7.7 7.7 12 3
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 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802814 183769 None 0 Human Functional pEC50 = 7.7 7.7 12 3
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 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
168276733 192940 None 0 Human Functional pEC50 = 7.7 7.7 4 2
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 272 1 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5180401 192940 None 0 Human Functional pEC50 = 7.7 7.7 4 2
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 272 1 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5221642 192940 None 0 Human Functional pEC50 = 7.7 7.7 4 2
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 272 1 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
4407909 192975 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192975 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192975 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
168275014 192929 None 0 Human Functional pEC50 = 6.7 6.7 3 2
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 218 1 2 1 2.9 CCC1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177386 192929 None 0 Human Functional pEC50 = 6.7 6.7 3 2
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 218 1 2 1 2.9 CCC1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221524 192929 None 0 Human Functional pEC50 = 6.7 6.7 3 2
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 218 1 2 1 2.9 CCC1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
10751567 4541 None 1 Rat Functional pEC50 = 5.7 5.7 - 1
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptor
ChEMBL 223 4 1 4 1.1 COc1cc(CCN)c2c(c1OC)OCC2 10.1021/jm970219x
CHEMBL102347 4541 None 1 Rat Functional pEC50 = 5.7 5.7 - 1
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptor
ChEMBL 223 4 1 4 1.1 COc1cc(CCN)c2c(c1OC)OCC2 10.1021/jm970219x
38240 108055 None 15 Rat Functional pEC50 = 5.7 5.7 - 1
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptor
ChEMBL 225 6 1 4 1.6 CCOc1c(OC)cc(CCN)cc1OC 10.1021/jm970219x
CHEMBL319415 108055 None 15 Rat Functional pEC50 = 5.7 5.7 - 1
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptor
ChEMBL 225 6 1 4 1.6 CCOc1c(OC)cc(CCN)cc1OC 10.1021/jm970219x
24773648 64446 None 1 Human Functional pEC50 = 5.7 5.7 - 1
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 191 1 1 2 1.9 COc1ccc2c(c1)CCNCC2C 10.1016/j.bmcl.2004.12.080
CHEMBL181324 64446 None 1 Human Functional pEC50 = 5.7 5.7 - 1
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 191 1 1 2 1.9 COc1ccc2c(c1)CCNCC2C 10.1016/j.bmcl.2004.12.080
4401618 193132 None 2 Human Functional pEC50 = 5.7 5.7 -9 2
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 280 1 2 1 3.9 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5207633 193132 None 2 Human Functional pEC50 = 5.7 5.7 -9 2
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 280 1 2 1 3.9 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222820 193132 None 2 Human Functional pEC50 = 5.7 5.7 -9 2
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 280 1 2 1 3.9 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
82045782 196339 None 1 Human Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 215 0 1 2 2.5 Cc1cccc2c1OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5421733 196339 None 1 Human Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 215 0 1 2 2.5 Cc1cccc2c1OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
4401618 193132 None 2 Human Functional pEC50 = 5.7 5.7 -9 2
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 280 1 2 1 3.9 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5207633 193132 None 2 Human Functional pEC50 = 5.7 5.7 -9 2
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 280 1 2 1 3.9 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222820 193132 None 2 Human Functional pEC50 = 5.7 5.7 -9 2
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 280 1 2 1 3.9 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
118733814 120722 None 0 Human Functional pEC50 = 6.7 6.7 23 2
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
CHEMBL3416059 120722 None 0 Human Functional pEC50 = 6.7 6.7 23 2
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
CHEMBL3546910 120722 None 0 Human Functional pEC50 = 6.7 6.7 23 2
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
164513426 195281 None 0 Human Functional pEC50 = 5.7 5.7 -48 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 2 2 2.2 C[C@@H]1C=C(c2c[nH]c3ncccc23)CNC1 10.1021/acsmedchemlett.3c00566
CHEMBL5399968 195281 None 0 Human Functional pEC50 = 5.7 5.7 -48 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 2 2 2.2 C[C@@H]1C=C(c2c[nH]c3ncccc23)CNC1 10.1021/acsmedchemlett.3c00566
168285159 193023 None 0 Human Functional pEC50 = 6.7 6.7 -1 3
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 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5196522 193023 None 0 Human Functional pEC50 = 6.7 6.7 -1 3
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 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222172 193023 None 0 Human Functional pEC50 = 6.7 6.7 -1 3
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 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
4363390 192979 None 0 Human Functional pEC50 = 5.7 5.7 -21 2
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 344 1 2 1 4.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5184885 192979 None 0 Human Functional pEC50 = 5.7 5.7 -21 2
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 344 1 2 1 4.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5221904 192979 None 0 Human Functional pEC50 = 5.7 5.7 -21 2
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 344 1 2 1 4.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
168285159 193023 None 0 Human Functional pEC50 = 6.7 6.7 -1 3
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 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5196522 193023 None 0 Human Functional pEC50 = 6.7 6.7 -1 3
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 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222172 193023 None 0 Human Functional pEC50 = 6.7 6.7 -1 3
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 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
4363390 192979 None 0 Human Functional pEC50 = 5.7 5.7 -21 2
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 344 1 2 1 4.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5184885 192979 None 0 Human Functional pEC50 = 5.7 5.7 -21 2
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 344 1 2 1 4.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5221904 192979 None 0 Human Functional pEC50 = 5.7 5.7 -21 2
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 344 1 2 1 4.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
172467762 196799 None 0 Human Functional pEC50 = 7.7 7.7 13 3
Agonist activity at 5HT2C receptor (unknown origin)Agonist activity at 5HT2C receptor (unknown origin)
ChEMBL 235 5 1 2 2.7 NC[C@@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1016/j.bmcl.2024.129654
CHEMBL5432445 196799 None 0 Human Functional pEC50 = 7.7 7.7 13 3
Agonist activity at 5HT2C receptor (unknown origin)Agonist activity at 5HT2C receptor (unknown origin)
ChEMBL 235 5 1 2 2.7 NC[C@@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1016/j.bmcl.2024.129654
162668367 183845 None 0 Human Functional pEC50 = 7.7 7.7 21 3
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 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4786831 183845 None 0 Human Functional pEC50 = 7.7 7.7 21 3
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 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803642 183845 None 0 Human Functional pEC50 = 7.7 7.7 21 3
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 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
46937339 74235 None 0 Human Functional pEC50 = 7.7 7.7 13 3
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 235 5 1 2 2.7 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1021/ml200206z
CHEMBL2023357 74235 None 0 Human Functional pEC50 = 7.7 7.7 13 3
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 235 5 1 2 2.7 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1021/ml200206z
46937339 74235 None 0 Human Functional pEC50 = 7.7 7.7 13 3
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium mobilizationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium mobilization
ChEMBL 235 5 1 2 2.7 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1021/jm5019274
CHEMBL2023357 74235 None 0 Human Functional pEC50 = 7.7 7.7 13 3
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium mobilizationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium mobilization
ChEMBL 235 5 1 2 2.7 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1021/jm5019274
45484972 200810 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 346 5 1 5 2.1 CCn1c(CCc2ccccc2Cl)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
CHEMBL576453 200810 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 346 5 1 5 2.1 CCn1c(CCc2ccccc2Cl)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
45484934 200894 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 346 4 1 5 2.0 C[C@@H]1CNCCN1c1cc(=O)n(C)c(CCc2ccccc2Cl)n1 10.1016/j.bmcl.2009.07.133
CHEMBL577250 200894 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 346 4 1 5 2.0 C[C@@H]1CNCCN1c1cc(=O)n(C)c(CCc2ccccc2Cl)n1 10.1016/j.bmcl.2009.07.133
122442263 138444 None 0 Human Functional pEC50 = 7.7 7.7 15 3
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 138444 None 0 Human Functional pEC50 = 7.7 7.7 15 3
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 138444 None 0 Human Functional pEC50 = 7.7 7.7 15 3
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
44315697 207963 None 0 Human Functional pEC50 = 7.7 7.7 1 3
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 254 4 1 3 2.6 CCSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
CHEMBL80731 207963 None 0 Human Functional pEC50 = 7.7 7.7 1 3
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 254 4 1 3 2.6 CCSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
162668367 183845 None 0 Human Functional pEC50 = 7.7 7.7 21 3
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 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4786831 183845 None 0 Human Functional pEC50 = 7.7 7.7 21 3
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 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803642 183845 None 0 Human Functional pEC50 = 7.7 7.7 21 3
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 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
11658860 2344 None 24 Human Functional pEC50 = 6.7 6.7 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
2941 2344 None 24 Human Functional pEC50 = 6.7 6.7 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
4374 2344 None 24 Human Functional pEC50 = 6.7 6.7 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
CHEMBL360328 2344 None 24 Human Functional pEC50 = 6.7 6.7 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
DB04871 2344 None 24 Human Functional pEC50 = 6.7 6.7 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
54587669 61480 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 Cc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
CHEMBL1770379 61480 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 Cc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
53323196 56865 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cncc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
CHEMBL1643856 56865 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cncc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
118733802 120717 None 0 Human Functional pEC50 = 6.7 6.7 1 3
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 3.4 C=C(C)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416053 120717 None 0 Human Functional pEC50 = 6.7 6.7 1 3
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 3.4 C=C(C)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546905 120717 None 0 Human Functional pEC50 = 6.7 6.7 1 3
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 3.4 C=C(C)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
82045793 195951 None 1 Human Functional pEC50 = 6.7 6.7 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1ccc2c(c1)C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
CHEMBL5414076 195951 None 1 Human Functional pEC50 = 6.7 6.7 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1ccc2c(c1)C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
11673842 89122 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 264 2 2 2 2.1 CCCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337498 89122 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 264 2 2 2 2.1 CCCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365254 89122 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 264 2 2 2 2.1 CCCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
122180957 121837 None 0 Human Functional pEC50 = 6.7 6.7 -20 2
Partial agonist activity at human 5-HT2C receptor expressed in human tsA201 cells after 30 mins by inositol phosphate turnover assayPartial agonist activity at human 5-HT2C receptor expressed in human tsA201 cells after 30 mins by inositol phosphate turnover assay
ChEMBL 393 7 1 5 3.5 COc1cc(CCNCc2cccc3c2OCO3)c(OC)cc1Br 10.1016/j.bmc.2014.12.011
CHEMBL3589578 121837 None 0 Human Functional pEC50 = 6.7 6.7 -20 2
Partial agonist activity at human 5-HT2C receptor expressed in human tsA201 cells after 30 mins by inositol phosphate turnover assayPartial agonist activity at human 5-HT2C receptor expressed in human tsA201 cells after 30 mins by inositol phosphate turnover assay
ChEMBL 393 7 1 5 3.5 COc1cc(CCNCc2cccc3c2OCO3)c(OC)cc1Br 10.1016/j.bmc.2014.12.011
70696051 74488 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 271 4 1 2 3.6 COc1ccc(-c2ccc(F)cc2)cc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2022181 74488 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 271 4 1 2 3.6 COc1ccc(-c2ccc(F)cc2)cc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2027920 74488 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 271 4 1 2 3.6 COc1ccc(-c2ccc(F)cc2)cc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
46228422 202492 None 0 Human Functional pEC50 = 7.7 7.7 33 3
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
CHEMBL595553 202492 None 0 Human Functional pEC50 = 7.7 7.7 33 3
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
9844378 8096 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced calcium mobilization by cell based assayAgonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced calcium mobilization by cell based assay
ChEMBL 409 5 1 6 3.5 Cc1noc(C)c1COc1cc(F)c(COC(=O)N2[C@@H](C)CNC[C@H]2C)c(F)c1 10.1007/s00044-011-9615-3
CHEMBL1091452 8096 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced calcium mobilization by cell based assayAgonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced calcium mobilization by cell based assay
ChEMBL 409 5 1 6 3.5 Cc1noc(C)c1COc1cc(F)c(COC(=O)N2[C@@H](C)CNC[C@H]2C)c(F)c1 10.1007/s00044-011-9615-3
146025688 183800 None 0 Human Functional pEC50 = 7.7 7.7 20 3
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 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4761064 183800 None 0 Human Functional pEC50 = 7.7 7.7 20 3
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 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803134 183800 None 0 Human Functional pEC50 = 7.7 7.7 20 3
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 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
118733824 120733 None 0 Human Functional pEC50 = 7.7 7.7 75 2
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 2.8 C=C(F)COc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416065 120733 None 0 Human Functional pEC50 = 7.7 7.7 75 2
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 2.8 C=C(F)COc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546960 120733 None 0 Human Functional pEC50 = 7.7 7.7 75 2
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 2.8 C=C(F)COc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
24826788 91132 None 0 Human Functional pEC50 = 7.7 7.7 17 2
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=C1c2c(Cl)cccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397893 91132 None 0 Human Functional pEC50 = 7.7 7.7 17 2
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=C1c2c(Cl)cccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
11264345 130467 None 3 Human Functional pEC50 = 7.7 7.7 38 3
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 213 0 1 1 2.7 CC1CNCCc2ccc(Cl)c(F)c21 10.1016/j.bmcl.2004.12.080
CHEMBL368016 130467 None 3 Human Functional pEC50 = 7.7 7.7 38 3
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 213 0 1 1 2.7 CC1CNCCc2ccc(Cl)c(F)c21 10.1016/j.bmcl.2004.12.080
44412389 78125 None 0 Human Functional pEC50 = 7.7 7.7 1 3
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 272 1 1 4 1.7 C[C@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1 10.1016/j.bmcl.2006.03.007
CHEMBL210215 78125 None 0 Human Functional pEC50 = 7.7 7.7 1 3
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 272 1 1 4 1.7 C[C@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1 10.1016/j.bmcl.2006.03.007
146025688 183800 None 0 Human Functional pEC50 = 7.7 7.7 20 3
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 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4761064 183800 None 0 Human Functional pEC50 = 7.7 7.7 20 3
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 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803134 183800 None 0 Human Functional pEC50 = 7.7 7.7 20 3
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 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
146025689 183823 None 0 Human Functional pEC50 = 7.7 7.7 17 2
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 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4781163 183823 None 0 Human Functional pEC50 = 7.7 7.7 17 2
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 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803350 183823 None 0 Human Functional pEC50 = 7.7 7.7 17 2
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 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
168271458 190717 None 0 Human Functional pEC50 = 7.7 7.7 3 2
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 266 1 2 1 3.5 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5180800 190717 None 0 Human Functional pEC50 = 7.7 7.7 3 2
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 266 1 2 1 3.5 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
168271458 190717 None 0 Human Functional pEC50 = 7.7 7.7 3 2
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 266 1 2 1 3.5 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5180800 190717 None 0 Human Functional pEC50 = 7.7 7.7 3 2
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 266 1 2 1 3.5 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
137630214 161153 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 209 4 1 2 2.2 CNC[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4082227 161153 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 209 4 1 2 2.2 CNC[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116620 161153 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 209 4 1 2 2.2 CNC[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
155539425 172954 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 2.1 Cc1c(Cc2ccccc2)nnc2c1CCNCC2 10.1016/j.bmcl.2016.06.060
CHEMBL4514905 172954 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 2.1 Cc1c(Cc2ccccc2)nnc2c1CCNCC2 10.1016/j.bmcl.2016.06.060
122442310 138445 None 0 Human Functional pEC50 = 6.7 6.7 4 2
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 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770011 138445 None 0 Human Functional pEC50 = 6.7 6.7 4 2
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 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771394 138445 None 0 Human Functional pEC50 = 6.7 6.7 4 2
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 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
122442310 138445 None 0 Human Functional pEC50 = 6.7 6.7 4 2
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 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770011 138445 None 0 Human Functional pEC50 = 6.7 6.7 4 2
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 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771394 138445 None 0 Human Functional pEC50 = 6.7 6.7 4 2
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 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
137629242 161096 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 COc1cscc1CNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4070259 161096 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 COc1cscc1CNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116195 161096 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 COc1cscc1CNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
45484878 199276 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 314 4 1 6 1.1 Cc1ccccc1OCc1nc(N2CCNCC2)cc(=O)n1C 10.1016/j.bmcl.2009.07.133
CHEMBL565735 199276 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 314 4 1 6 1.1 Cc1ccccc1OCc1nc(N2CCNCC2)cc(=O)n1C 10.1016/j.bmcl.2009.07.133
155551165 176744 None 0 Human Functional pEC50 = 6.6 6.6 -7 3
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 333 7 1 3 3.8 COc1ccccc1CNCC1CC1(F)c1cc(F)ccc1OC 10.1016/j.ejmech.2019.111626
CHEMBL4541617 176744 None 0 Human Functional pEC50 = 6.6 6.6 -7 3
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 333 7 1 3 3.8 COc1ccccc1CNCC1CC1(F)c1cc(F)ccc1OC 10.1016/j.ejmech.2019.111626
CHEMBL4597957 176744 None 0 Human Functional pEC50 = 6.6 6.6 -7 3
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 333 7 1 3 3.8 COc1ccccc1CNCC1CC1(F)c1cc(F)ccc1OC 10.1016/j.ejmech.2019.111626
137629242 161096 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 COc1cscc1CNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4070259 161096 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 COc1cscc1CNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116195 161096 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 COc1cscc1CNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
137629898 161113 None 0 Human Functional pEC50 = 6.6 6.6 16 2
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 COc1cccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)c1 10.1021/acs.jmedchem.7b00584
CHEMBL4067525 161113 None 0 Human Functional pEC50 = 6.6 6.6 16 2
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 COc1cccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)c1 10.1021/acs.jmedchem.7b00584
CHEMBL4116318 161113 None 0 Human Functional pEC50 = 6.6 6.6 16 2
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 COc1cccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)c1 10.1021/acs.jmedchem.7b00584
71562661 87341 None 0 Human Functional pEC50 = 6.6 6.6 3 2
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 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
CHEMBL2331794 87341 None 0 Human Functional pEC50 = 6.6 6.6 3 2
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 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
155551165 176744 None 0 Human Functional pEC50 = 6.6 6.6 -7 3
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 333 7 1 3 3.8 COc1ccccc1CNCC1CC1(F)c1cc(F)ccc1OC 10.1016/j.ejmech.2019.111626
CHEMBL4541617 176744 None 0 Human Functional pEC50 = 6.6 6.6 -7 3
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 333 7 1 3 3.8 COc1ccccc1CNCC1CC1(F)c1cc(F)ccc1OC 10.1016/j.ejmech.2019.111626
CHEMBL4597957 176744 None 0 Human Functional pEC50 = 6.6 6.6 -7 3
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 333 7 1 3 3.8 COc1ccccc1CNCC1CC1(F)c1cc(F)ccc1OC 10.1016/j.ejmech.2019.111626
146025689 183823 None 0 Human Functional pEC50 = 7.6 7.6 17 2
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 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4781163 183823 None 0 Human Functional pEC50 = 7.6 7.6 17 2
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 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803350 183823 None 0 Human Functional pEC50 = 7.6 7.6 17 2
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 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
137630214 161153 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 209 4 1 2 2.2 CNC[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4082227 161153 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 209 4 1 2 2.2 CNC[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116620 161153 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 209 4 1 2 2.2 CNC[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
44572755 12463 None 0 Human Functional pEC50 = 7.6 7.6 2 3
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 161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL1186115 12463 None 0 Human Functional pEC50 = 7.6 7.6 2 3
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 161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL450599 12463 None 0 Human Functional pEC50 = 7.6 7.6 2 3
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 161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
53325937 56821 None 0 Human Functional pEC50 = 7.6 7.6 -7 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643678 56821 None 0 Human Functional pEC50 = 7.6 7.6 -7 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
24849050 78331 None 1 Human Functional pEC50 = 7.6 7.6 2 3
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 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CC[C@H]3CNC[C@H]32)n1 10.1016/j.bmcl.2006.03.007
CHEMBL210802 78331 None 1 Human Functional pEC50 = 7.6 7.6 2 3
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 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CC[C@H]3CNC[C@H]32)n1 10.1016/j.bmcl.2006.03.007
137640063 161316 None 3 Human Functional pEC50 = 7.6 7.6 4 2
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
CHEMBL4072722 161316 None 3 Human Functional pEC50 = 7.6 7.6 4 2
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
CHEMBL4117953 161316 None 3 Human Functional pEC50 = 7.6 7.6 4 2
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
172466550 196777 None 0 Human Functional pEC50 = 7.6 7.6 12 3
Agonist activity at 5-HT2C (unknown origin)Agonist activity at 5-HT2C (unknown origin)
ChEMBL 271 0 2 2 3.5 Oc1cc2c3c(c1Cl)-c1ccccc1CC3NCC2 10.1016/j.ejmech.2023.115414
CHEMBL5432040 196777 None 0 Human Functional pEC50 = 7.6 7.6 12 3
Agonist activity at 5-HT2C (unknown origin)Agonist activity at 5-HT2C (unknown origin)
ChEMBL 271 0 2 2 3.5 Oc1cc2c3c(c1Cl)-c1ccccc1CC3NCC2 10.1016/j.ejmech.2023.115414
137640063 161316 None 3 Human Functional pEC50 = 7.6 7.6 4 2
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
CHEMBL4072722 161316 None 3 Human Functional pEC50 = 7.6 7.6 4 2
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
CHEMBL4117953 161316 None 3 Human Functional pEC50 = 7.6 7.6 4 2
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
122442300 138436 None 0 Human Functional pEC50 = 7.6 7.6 4 3
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 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769421 138436 None 0 Human Functional pEC50 = 7.6 7.6 4 3
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 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771385 138436 None 0 Human Functional pEC50 = 7.6 7.6 4 3
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 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
122442251 138447 None 0 Human Functional pEC50 = 7.6 7.6 15 3
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 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770225 138447 None 0 Human Functional pEC50 = 7.6 7.6 15 3
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 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771396 138447 None 0 Human Functional pEC50 = 7.6 7.6 15 3
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 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
71562661 87341 None 0 Human Functional pEC50 = 6.6 6.6 3 2
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 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
CHEMBL2331794 87341 None 0 Human Functional pEC50 = 6.6 6.6 3 2
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 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
24773894 63000 None 2 Human Functional pEC50 = 6.6 6.6 9 2
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 229 0 1 1 3.2 C[C@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
CHEMBL178566 63000 None 2 Human Functional pEC50 = 6.6 6.6 9 2
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 229 0 1 1 3.2 C[C@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
72197480 102456 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 368 4 2 7 1.7 COc1cccc(Nc2nc(N3CCN(C)CC3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393239 102456 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 368 4 2 7 1.7 COc1cccc(Nc2nc(N3CCN(C)CC3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3039631 102456 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 368 4 2 7 1.7 COc1cccc(Nc2nc(N3CCN(C)CC3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
137629898 161113 None 0 Human Functional pEC50 = 6.6 6.6 16 2
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 COc1cccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)c1 10.1021/acs.jmedchem.7b00584
CHEMBL4067525 161113 None 0 Human Functional pEC50 = 6.6 6.6 16 2
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 COc1cccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)c1 10.1021/acs.jmedchem.7b00584
CHEMBL4116318 161113 None 0 Human Functional pEC50 = 6.6 6.6 16 2
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 COc1cccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)c1 10.1021/acs.jmedchem.7b00584
44572367 12547 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1ccccc1C#CCCCCO 10.1021/jm801354e
CHEMBL1186673 12547 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1ccccc1C#CCCCCO 10.1021/jm801354e
CHEMBL474230 12547 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1ccccc1C#CCCCCO 10.1021/jm801354e
122442310 138445 None 0 Human Functional pEC50 = 6.6 6.6 4 2
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 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770011 138445 None 0 Human Functional pEC50 = 6.6 6.6 4 2
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 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771394 138445 None 0 Human Functional pEC50 = 6.6 6.6 4 2
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 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
122442310 138445 None 0 Human Functional pEC50 = 6.6 6.6 4 2
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 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770011 138445 None 0 Human Functional pEC50 = 6.6 6.6 4 2
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 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771394 138445 None 0 Human Functional pEC50 = 6.6 6.6 4 2
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 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
85542158 195546 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
11414184 83531 None 0 Human Functional pEC50 = 7.6 7.6 5 3
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 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)C2CNCCN12 10.1021/jm0612968
CHEMBL220274 83531 None 0 Human Functional pEC50 = 7.6 7.6 5 3
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 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)C2CNCCN12 10.1021/jm0612968
70687695 74504 None 0 Human Functional pEC50 = 7.6 7.6 12 2
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 205 5 1 2 2.5 CCCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2022186 74504 None 0 Human Functional pEC50 = 7.6 7.6 12 2
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 205 5 1 2 2.5 CCCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2027987 74504 None 0 Human Functional pEC50 = 7.6 7.6 12 2
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 205 5 1 2 2.5 CCCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
5 139 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
5202 139 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
CHEMBL39 139 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
DB08839 139 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
137639485 156996 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 336 2 0 3 4.9 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCCCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4072217 156996 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 336 2 0 3 4.9 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCCCC1 10.1021/acs.jmedchem.7b00385
122442300 138436 None 0 Human Functional pEC50 = 7.6 7.6 4 3
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 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769421 138436 None 0 Human Functional pEC50 = 7.6 7.6 4 3
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 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771385 138436 None 0 Human Functional pEC50 = 7.6 7.6 4 3
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 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
122442251 138447 None 0 Human Functional pEC50 = 7.6 7.6 15 3
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 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770225 138447 None 0 Human Functional pEC50 = 7.6 7.6 15 3
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 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771396 138447 None 0 Human Functional pEC50 = 7.6 7.6 15 3
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 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL4757837 216555 None 0 Human Functional pEC50 = 7.6 7.6 -1 2
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)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL4802974 216555 None 0 Human Functional pEC50 = 7.6 7.6 -1 2
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)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL4757837 216555 None 0 Human Functional pEC50 = 7.6 7.6 -1 2
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)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL4802974 216555 None 0 Human Functional pEC50 = 7.6 7.6 -1 2
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)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
85542158 195546 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
13139 2491 None 15 Rat Functional pEC50 = 4.6 4.6 -9 2
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptor
ChEMBL 211 5 1 4 1.2 COC1=CC(=CC(=C1OC)OC)CCN 10.1021/jm970219x
4076 2491 None 15 Rat Functional pEC50 = 4.6 4.6 -9 2
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptor
ChEMBL 211 5 1 4 1.2 COC1=CC(=CC(=C1OC)OC)CCN 10.1021/jm970219x
CHEMBL26687 2491 None 15 Rat Functional pEC50 = 4.6 4.6 -9 2
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptor
ChEMBL 211 5 1 4 1.2 COC1=CC(=CC(=C1OC)OC)CCN 10.1021/jm970219x
11416698 91141 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 COc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397902 91141 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 COc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
118733786 120727 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 271 6 1 3 3.1 CSCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416045 120727 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 271 6 1 3 3.1 CSCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546954 120727 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 271 6 1 3 3.1 CSCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
137629237 161095 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
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 310 6 1 3 3.6 COc1ccc(F)cc1C1CC1CNCc1ccccc1C#N 10.1021/acs.jmedchem.7b00584
CHEMBL4064809 161095 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
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 310 6 1 3 3.6 COc1ccc(F)cc1C1CC1CNCc1ccccc1C#N 10.1021/acs.jmedchem.7b00584
CHEMBL4116194 161095 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
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 310 6 1 3 3.6 COc1ccc(F)cc1C1CC1CNCc1ccccc1C#N 10.1021/acs.jmedchem.7b00584
137629237 161095 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
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 310 6 1 3 3.6 COc1ccc(F)cc1C1CC1CNCc1ccccc1C#N 10.1021/acs.jmedchem.7b00584
CHEMBL4064809 161095 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
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 310 6 1 3 3.6 COc1ccc(F)cc1C1CC1CNCc1ccccc1C#N 10.1021/acs.jmedchem.7b00584
CHEMBL4116194 161095 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
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 310 6 1 3 3.6 COc1ccc(F)cc1C1CC1CNCc1ccccc1C#N 10.1021/acs.jmedchem.7b00584
82553 205253 None 44 Human Functional pEC50 = 5.6 5.6 - 1
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 159 1 1 1 2.1 C1=C(c2ccccc2)CCNC1 10.1016/j.bmcl.2012.01.122
CHEMBL1901802 205253 None 44 Human Functional pEC50 = 5.6 5.6 - 1
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 159 1 1 1 2.1 C1=C(c2ccccc2)CCNC1 10.1016/j.bmcl.2012.01.122
CHEMBL6224 205253 None 44 Human Functional pEC50 = 5.6 5.6 - 1
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 159 1 1 1 2.1 C1=C(c2ccccc2)CCNC1 10.1016/j.bmcl.2012.01.122
16115521 84699 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 COc1cc2c(cc1Cl)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL222466 84699 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 COc1cc2c(cc1Cl)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
118733772 120712 None 0 Human Functional pEC50 = 5.6 5.6 2 2
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 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416038 120712 None 0 Human Functional pEC50 = 5.6 5.6 2 2
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 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546893 120712 None 0 Human Functional pEC50 = 5.6 5.6 2 2
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 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
172456495 196441 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 207 0 1 2 2.1 Clc1ccc2c(c1)OC1(C=C2)CNC1 10.1021/acsmedchemlett.3c00454
CHEMBL5424008 196441 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 207 0 1 2 2.1 Clc1ccc2c(c1)OC1(C=C2)CNC1 10.1021/acsmedchemlett.3c00454
46228433 202196 None 6 Human Functional pEC50 = 7.6 7.6 87 2
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 217 1 1 3 1.4 c1cc2c(nc1N1CCNCC1)CCCC2 10.1016/j.bmcl.2009.10.112
CHEMBL593547 202196 None 6 Human Functional pEC50 = 7.6 7.6 87 2
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 217 1 1 3 1.4 c1cc2c(nc1N1CCNCC1)CCCC2 10.1016/j.bmcl.2009.10.112
146025689 183823 None 0 Human Functional pEC50 = 7.6 7.6 17 2
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 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4781163 183823 None 0 Human Functional pEC50 = 7.6 7.6 17 2
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 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803350 183823 None 0 Human Functional pEC50 = 7.6 7.6 17 2
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 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
11630147 91147 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 246 2 1 3 1.1 CCOc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397908 91147 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 246 2 1 3 1.1 CCOc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
162653458 183772 None 0 Human Functional pEC50 = 7.6 7.6 6 3
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 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4753812 183772 None 0 Human Functional pEC50 = 7.6 7.6 6 3
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 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802839 183772 None 0 Human Functional pEC50 = 7.6 7.6 6 3
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 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
5 139 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2009.07.063
5202 139 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2009.07.063
CHEMBL39 139 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2009.07.063
DB08839 139 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2009.07.063
45485779 199963 None 0 Human Functional pEC50 = 7.6 7.6 4 2
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 348 5 1 6 1.8 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2Cl)n1 10.1016/j.bmcl.2009.07.136
CHEMBL570023 199963 None 0 Human Functional pEC50 = 7.6 7.6 4 2
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 348 5 1 6 1.8 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2Cl)n1 10.1016/j.bmcl.2009.07.136
45485725 200283 None 0 Human Functional pEC50 = 7.6 7.6 2 3
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 348 5 1 6 1.9 C[C@@H](COc1ccccc1Cl)n1nc(N2CCNCC2)ccc1=O 10.1016/j.bmcl.2009.07.136
CHEMBL572252 200283 None 0 Human Functional pEC50 = 7.6 7.6 2 3
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 348 5 1 6 1.9 C[C@@H](COc1ccccc1Cl)n1nc(N2CCNCC2)ccc1=O 10.1016/j.bmcl.2009.07.136
53321948 56820 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
CHEMBL1643677 56820 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
137661221 159493 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 286 2 0 4 3.7 Cn1nc(-c2cccc3ccccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
CHEMBL4100745 159493 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 286 2 0 4 3.7 Cn1nc(-c2cccc3ccccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
122442293 138429 None 0 Human Functional pEC50 = 7.6 7.6 19 3
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 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3770599 138429 None 0 Human Functional pEC50 = 7.6 7.6 19 3
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 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3771378 138429 None 0 Human Functional pEC50 = 7.6 7.6 19 3
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 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
72197486 102558 None 0 Human Functional pEC50 = 7.6 7.6 -1 8
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 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393245 102558 None 0 Human Functional pEC50 = 7.6 7.6 -1 8
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 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040361 102558 None 0 Human Functional pEC50 = 7.6 7.6 -1 8
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 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
146025689 183823 None 0 Human Functional pEC50 = 7.6 7.6 17 2
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 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4781163 183823 None 0 Human Functional pEC50 = 7.6 7.6 17 2
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 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803350 183823 None 0 Human Functional pEC50 = 7.6 7.6 17 2
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 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
162653458 183772 None 0 Human Functional pEC50 = 7.6 7.6 6 3
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 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4753812 183772 None 0 Human Functional pEC50 = 7.6 7.6 6 3
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 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802839 183772 None 0 Human Functional pEC50 = 7.6 7.6 6 3
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 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
5 139 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
5202 139 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
CHEMBL39 139 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
DB08839 139 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
216 2860 None 26 Human Functional pEC50 = 7.6 7.6 -1 3
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 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/jm0709034
9815618 2860 None 26 Human Functional pEC50 = 7.6 7.6 -1 3
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 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/jm0709034
CHEMBL253811 2860 None 26 Human Functional pEC50 = 7.6 7.6 -1 3
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 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/jm0709034
22292784 64615 None 16 Human Functional pEC50 = 7.6 7.6 5 3
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 CC1CNCCc2cc(Cl)ccc21 10.1021/jm0709034
CHEMBL181672 64615 None 16 Human Functional pEC50 = 7.6 7.6 5 3
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 CC1CNCCc2cc(Cl)ccc21 10.1021/jm0709034
122442293 138429 None 0 Human Functional pEC50 = 7.6 7.6 19 3
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 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3770599 138429 None 0 Human Functional pEC50 = 7.6 7.6 19 3
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 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3771378 138429 None 0 Human Functional pEC50 = 7.6 7.6 19 3
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 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
132820207 148000 None 0 Human Functional pEC50 = 7.6 7.6 25 2
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 220 0 1 2 1.9 Fc1ccc2c(c1)CC[C@@H]1CNCCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3933563 148000 None 0 Human Functional pEC50 = 7.6 7.6 25 2
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 220 0 1 2 1.9 Fc1ccc2c(c1)CC[C@@H]1CNCCCN21 10.1016/j.bmcl.2016.11.016
134155579 151420 None 0 Human Functional pEC50 = 7.6 7.6 3 2
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 250 0 1 2 2.8 Clc1cccc2c1N1CCCNCCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3961026 151420 None 0 Human Functional pEC50 = 7.6 7.6 3 2
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 250 0 1 2 2.8 Clc1cccc2c1N1CCCNCCC1CC2 10.1016/j.bmcl.2016.11.016
162676555 183895 None 0 Human Functional pEC50 = 7.6 7.6 22 2
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 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4800666 183895 None 0 Human Functional pEC50 = 7.6 7.6 22 2
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 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4804119 183895 None 0 Human Functional pEC50 = 7.6 7.6 22 2
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 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
118733778 120724 None 0 Human Functional pEC50 = 6.6 6.6 19 2
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
CHEMBL3416041 120724 None 0 Human Functional pEC50 = 6.6 6.6 19 2
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
CHEMBL3546951 120724 None 0 Human Functional pEC50 = 6.6 6.6 19 2
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
68803474 153106 None 0 Human Functional pEC50 = 6.6 6.6 3 2
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 218 1 1 3 1.4 COc1ccc2c(c1)CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3975593 153106 None 0 Human Functional pEC50 = 6.6 6.6 3 2
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 218 1 1 3 1.4 COc1ccc2c(c1)CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
3045239 79604 None 1 Rat Functional pEC50 = 6.6 6.6 - 1
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 242 3 1 3 2.4 COc1ccc2c(c1)-c1c(ccn1C[C@H](C)N)C2 10.1021/jm970030l
CHEMBL2114265 79604 None 1 Rat Functional pEC50 = 6.6 6.6 - 1
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 242 3 1 3 2.4 COc1ccc2c(c1)-c1c(ccn1C[C@H](C)N)C2 10.1021/jm970030l
10487869 107413 None 1 Rat Functional pEC50 = 5.6 5.6 - 1
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 188 2 1 2 2.3 Cc1cccc2c1ccn2CC(C)N 10.1021/jm970030l
CHEMBL317677 107413 None 1 Rat Functional pEC50 = 5.6 5.6 - 1
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 188 2 1 2 2.3 Cc1cccc2c1ccn2CC(C)N 10.1021/jm970030l
19036385 108599 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
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 290 2 1 2 3.2 CC(N)Cn1ccc2c1-c1cc(Br)ccc1C2 10.1021/jm970030l
CHEMBL320145 108599 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
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 290 2 1 2 3.2 CC(N)Cn1ccc2c1-c1cc(Br)ccc1C2 10.1021/jm970030l
19036374 209537 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
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 246 2 1 2 3.1 CC(N)Cn1ccc2c1-c1cc(Cl)ccc1C2 10.1021/jm970030l
CHEMBL91855 209537 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
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 246 2 1 2 3.1 CC(N)Cn1ccc2c1-c1cc(Cl)ccc1C2 10.1021/jm970030l
10845306 209847 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
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 188 2 1 2 2.3 Cc1ccc2c(ccn2CC(C)N)c1 10.1021/jm970030l
CHEMBL93850 209847 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
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 188 2 1 2 2.3 Cc1ccc2c(ccn2CC(C)N)c1 10.1021/jm970030l
172448310 195732 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.1 CC1CNCCC12C=Cc1ccc(Cl)cc1O2 10.1021/acsmedchemlett.3c00454
CHEMBL5409777 195732 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.1 CC1CNCCC12C=Cc1ccc(Cl)cc1O2 10.1021/acsmedchemlett.3c00454
70681342 74494 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 219 5 1 2 2.8 CC(C)COc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2022187 74494 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 219 5 1 2 2.8 CC(C)COc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2027941 74494 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 219 5 1 2 2.8 CC(C)COc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
154703875 176553 None 1 Human Functional pEC50 = 5.6 5.6 -6 2
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 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4586582 176553 None 1 Human Functional pEC50 = 5.6 5.6 -6 2
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 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596341 176553 None 1 Human Functional pEC50 = 5.6 5.6 -6 2
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 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
137630172 161148 None 0 Human Functional pEC50 = 5.6 5.6 -10 2
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 329 7 1 3 4.3 COc1ccccc1C(C)NCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4066538 161148 None 0 Human Functional pEC50 = 5.6 5.6 -10 2
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 329 7 1 3 4.3 COc1ccccc1C(C)NCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116576 161148 None 0 Human Functional pEC50 = 5.6 5.6 -10 2
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 329 7 1 3 4.3 COc1ccccc1C(C)NCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4802921 216554 None 0 Human Functional pEC50 = 6.6 6.6 1 2
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 Cc1cccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL4802921 216554 None 0 Human Functional pEC50 = 6.6 6.6 1 2
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 Cc1cccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
137630172 161148 None 0 Human Functional pEC50 = 5.6 5.6 -10 2
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 329 7 1 3 4.3 COc1ccccc1C(C)NCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4066538 161148 None 0 Human Functional pEC50 = 5.6 5.6 -10 2
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 329 7 1 3 4.3 COc1ccccc1C(C)NCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116576 161148 None 0 Human Functional pEC50 = 5.6 5.6 -10 2
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 329 7 1 3 4.3 COc1ccccc1C(C)NCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
11448649 83465 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 272 1 1 3 1.7 O=C1c2c(OC(F)(F)F)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL219734 83465 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 272 1 1 3 1.7 O=C1c2c(OC(F)(F)F)cccc2C2CNCCN12 10.1021/jm0612968
11716185 89098 None 0 Human Functional pEC50 = 7.6 7.6 70 2
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 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337497 89098 None 0 Human Functional pEC50 = 7.6 7.6 70 2
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 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2364998 89098 None 0 Human Functional pEC50 = 7.6 7.6 70 2
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 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
146025684 183741 None 0 Human Functional pEC50 = 7.6 7.6 6 3
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 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4743977 183741 None 0 Human Functional pEC50 = 7.6 7.6 6 3
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 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802486 183741 None 0 Human Functional pEC50 = 7.6 7.6 6 3
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 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
168941654 195567 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 199 1 2 2 1.9 C1=C(c2n[nH]c3ccccc23)CNCC1 10.1021/acsmedchemlett.3c00566
CHEMBL5406172 195567 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 199 1 2 2 1.9 C1=C(c2n[nH]c3ccccc23)CNCC1 10.1021/acsmedchemlett.3c00566
162658153 183791 None 0 Human Functional pEC50 = 7.6 7.6 10 3
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 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4758641 183791 None 0 Human Functional pEC50 = 7.6 7.6 10 3
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 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803076 183791 None 0 Human Functional pEC50 = 7.6 7.6 10 3
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 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
162676555 183895 None 0 Human Functional pEC50 = 7.6 7.6 22 2
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 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4800666 183895 None 0 Human Functional pEC50 = 7.6 7.6 22 2
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 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4804119 183895 None 0 Human Functional pEC50 = 7.6 7.6 22 2
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 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
44572759 12466 None 0 Human Functional pEC50 = 7.6 7.6 7 3
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 177 3 1 2 1.8 COc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL1186135 12466 None 0 Human Functional pEC50 = 7.6 7.6 7 3
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 177 3 1 2 1.8 COc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL451368 12466 None 0 Human Functional pEC50 = 7.6 7.6 7 3
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 177 3 1 2 1.8 COc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
45484945 200946 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 326 4 1 5 1.7 Cc1ccccc1CCc1nc(N2CCNC[C@H]2C)cc(=O)n1C 10.1016/j.bmcl.2009.07.133
CHEMBL577690 200946 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 326 4 1 5 1.7 Cc1ccccc1CCc1nc(N2CCNC[C@H]2C)cc(=O)n1C 10.1016/j.bmcl.2009.07.133
45484903 201235 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 346 4 1 5 2.0 C[C@@H]1CNCCN1c1cc(=O)n(C)c(CCc2cccc(Cl)c2)n1 10.1016/j.bmcl.2009.07.133
CHEMBL583193 201235 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 346 4 1 5 2.0 C[C@@H]1CNCCN1c1cc(=O)n(C)c(CCc2cccc(Cl)c2)n1 10.1016/j.bmcl.2009.07.133
45484700 199759 None 0 Human Functional pEC50 = 7.6 7.6 3 2
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 295 3 1 4 1.9 O=c1cc2c(nn1Cc1ccc(C3CC3)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL568692 199759 None 0 Human Functional pEC50 = 7.6 7.6 3 2
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 295 3 1 4 1.9 O=c1cc2c(nn1Cc1ccc(C3CC3)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
1355 2011 None 45 Human Functional pEC50 = 7.6 7.6 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
142 2011 None 45 Human Functional pEC50 = 7.6 7.6 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
CHEMBL478 2011 None 45 Human Functional pEC50 = 7.6 7.6 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
DB12110 2011 None 45 Human Functional pEC50 = 7.6 7.6 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
44315993 172980 None 0 Human Functional pEC50 = 7.6 7.6 -2 3
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 222 3 1 3 2.1 CSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
CHEMBL451543 172980 None 0 Human Functional pEC50 = 7.6 7.6 -2 3
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 222 3 1 3 2.1 CSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
146025684 183741 None 0 Human Functional pEC50 = 7.6 7.6 6 3
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 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4743977 183741 None 0 Human Functional pEC50 = 7.6 7.6 6 3
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 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802486 183741 None 0 Human Functional pEC50 = 7.6 7.6 6 3
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 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
168941654 195567 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 199 1 2 2 1.9 C1=C(c2n[nH]c3ccccc23)CNCC1 10.1021/acsmedchemlett.3c00566
CHEMBL5406172 195567 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 199 1 2 2 1.9 C1=C(c2n[nH]c3ccccc23)CNCC1 10.1021/acsmedchemlett.3c00566
162658153 183791 None 0 Human Functional pEC50 = 7.6 7.6 10 3
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 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4758641 183791 None 0 Human Functional pEC50 = 7.6 7.6 10 3
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 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803076 183791 None 0 Human Functional pEC50 = 7.6 7.6 10 3
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 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
46228442 202359 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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)nc3ccsc23)c1 10.1016/j.bmcl.2009.10.112
CHEMBL594718 202359 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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)nc3ccsc23)c1 10.1016/j.bmcl.2009.10.112
137630777 161202 None 0 Human Functional pEC50 = 5.6 5.6 2 2
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 COc1cccc(CNC[C@@H]2C[C@H]2c2cc(F)ccc2OC)c1 10.1021/acs.jmedchem.7b00584
CHEMBL4093447 161202 None 0 Human Functional pEC50 = 5.6 5.6 2 2
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 COc1cccc(CNC[C@@H]2C[C@H]2c2cc(F)ccc2OC)c1 10.1021/acs.jmedchem.7b00584
CHEMBL4117067 161202 None 0 Human Functional pEC50 = 5.6 5.6 2 2
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 COc1cccc(CNC[C@@H]2C[C@H]2c2cc(F)ccc2OC)c1 10.1021/acs.jmedchem.7b00584
12986497 202584 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 305 0 2 3 2.1 O=C1Nc2cc(C(F)(F)F)c(Cl)cc2N2CCNC[C@@H]12 10.1016/s0960-894x(00)00400-5
CHEMBL59619 202584 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 305 0 2 3 2.1 O=C1Nc2cc(C(F)(F)F)c(Cl)cc2N2CCNC[C@@H]12 10.1016/s0960-894x(00)00400-5
162660358 183810 None 0 Human Functional pEC50 = 6.6 6.6 2 2
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 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4762722 183810 None 0 Human Functional pEC50 = 6.6 6.6 2 2
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 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803207 183810 None 0 Human Functional pEC50 = 6.6 6.6 2 2
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 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
6604933 95807 None 13 Human Functional pEC50 = 6.6 6.6 - 1
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 226 0 1 2 2.6 c1cc2c3c(c1)c1c(n3CCNC2)CCCC1 10.1021/jm801354e
CHEMBL258465 95807 None 13 Human Functional pEC50 = 6.6 6.6 - 1
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 226 0 1 2 2.6 c1cc2c3c(c1)c1c(n3CCNC2)CCCC1 10.1021/jm801354e
45484833 199289 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 362 6 1 6 2.1 Cc1cc(=O)n(CCCOc2cccc(Cl)c2)c(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.133
CHEMBL565764 199289 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 362 6 1 6 2.1 Cc1cc(=O)n(CCCOc2cccc(Cl)c2)c(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.133
45484902 201091 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 312 4 1 5 1.4 C[C@@H]1CNCCN1c1cc(=O)n(C)c(CCc2ccccc2)n1 10.1016/j.bmcl.2009.07.133
CHEMBL579042 201091 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 312 4 1 5 1.4 C[C@@H]1CNCCN1c1cc(=O)n(C)c(CCc2ccccc2)n1 10.1016/j.bmcl.2009.07.133
168941715 196900 None 0 Human Functional pEC50 = 6.6 6.6 -23 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5434434 196900 None 0 Human Functional pEC50 = 6.6 6.6 -23 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
162660358 183810 None 0 Human Functional pEC50 = 6.6 6.6 2 2
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 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4762722 183810 None 0 Human Functional pEC50 = 6.6 6.6 2 2
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 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803207 183810 None 0 Human Functional pEC50 = 6.6 6.6 2 2
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 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
137630777 161202 None 0 Human Functional pEC50 = 5.6 5.6 2 2
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 COc1cccc(CNC[C@@H]2C[C@H]2c2cc(F)ccc2OC)c1 10.1021/acs.jmedchem.7b00584
CHEMBL4093447 161202 None 0 Human Functional pEC50 = 5.6 5.6 2 2
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 COc1cccc(CNC[C@@H]2C[C@H]2c2cc(F)ccc2OC)c1 10.1021/acs.jmedchem.7b00584
CHEMBL4117067 161202 None 0 Human Functional pEC50 = 5.6 5.6 2 2
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 COc1cccc(CNC[C@@H]2C[C@H]2c2cc(F)ccc2OC)c1 10.1021/acs.jmedchem.7b00584
168941715 196900 None 0 Human Functional pEC50 = 6.6 6.6 -23 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5434434 196900 None 0 Human Functional pEC50 = 6.6 6.6 -23 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
172448310 195732 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.1 CC1CNCCC12C=Cc1ccc(Cl)cc1O2 10.1021/acsmedchemlett.3c00454
CHEMBL5409777 195732 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.1 CC1CNCCC12C=Cc1ccc(Cl)cc1O2 10.1021/acsmedchemlett.3c00454
3568128 193042 None 0 Human Functional pEC50 = 5.6 5.6 -6 3
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(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5195443 193042 None 0 Human Functional pEC50 = 5.6 5.6 -6 3
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(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222291 193042 None 0 Human Functional pEC50 = 5.6 5.6 -6 3
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(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
3568128 193042 None 0 Human Functional pEC50 = 5.6 5.6 -6 3
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(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5195443 193042 None 0 Human Functional pEC50 = 5.6 5.6 -6 3
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(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222291 193042 None 0 Human Functional pEC50 = 5.6 5.6 -6 3
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(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
73417116 154521 None 0 Human Functional pEC50 = 5.6 5.6 -4 5
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 266 2 2 2 3.0 N[C@@H]1C[C@H]1c1ccccc1.N[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
CHEMBL3989843 154521 None 0 Human Functional pEC50 = 5.6 5.6 -4 5
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 266 2 2 2 3.0 N[C@@H]1C[C@H]1c1ccccc1.N[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
57799326 89142 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 242 1 2 2 1.7 Cc1cc(C2CC2)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337104 89142 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 242 1 2 2 1.7 Cc1cc(C2CC2)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365468 89142 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 242 1 2 2 1.7 Cc1cc(C2CC2)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
137655882 158849 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 302 3 0 4 4.1 CCn1nc(-c2cccc3ccccc23)cc1-c1nccn1C 10.1021/acs.jmedchem.7b00385
CHEMBL4093978 158849 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 302 3 0 4 4.1 CCn1nc(-c2cccc3ccccc23)cc1-c1nccn1C 10.1021/acs.jmedchem.7b00385
44573227 187297 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 420 4 1 4 3.3 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCC(Oc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2009.02.071
CHEMBL492302 187297 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 420 4 1 4 3.3 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCC(Oc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2009.02.071
45484869 199669 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 298 4 1 5 1.0 Cn1c(CCc2ccccc2)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
CHEMBL568236 199669 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 298 4 1 5 1.0 Cn1c(CCc2ccccc2)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
122442273 138443 None 0 Human Functional pEC50 = 6.6 6.6 1 3
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=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771152 138443 None 0 Human Functional pEC50 = 6.6 6.6 1 3
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=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771392 138443 None 0 Human Functional pEC50 = 6.6 6.6 1 3
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=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442273 138443 None 0 Human Functional pEC50 = 6.6 6.6 1 3
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=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771152 138443 None 0 Human Functional pEC50 = 6.6 6.6 1 3
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=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771392 138443 None 0 Human Functional pEC50 = 6.6 6.6 1 3
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=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
137636430 156139 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 338 2 0 4 3.7 Cc1sc(-c2cccc3ccccc23)nc1C(=O)N1CCOCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4062529 156139 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 338 2 0 4 3.7 Cc1sc(-c2cccc3ccccc23)nc1C(=O)N1CCOCC1 10.1021/acs.jmedchem.7b00385
16115381 83476 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
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 270 0 1 2 2.2 C[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
CHEMBL219837 83476 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
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 270 0 1 2 2.2 C[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
58911534 91143 None 0 Human Functional pEC50 = 7.6 7.6 7 2
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 216 0 1 2 1.0 Cc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397904 91143 None 0 Human Functional pEC50 = 7.6 7.6 7 2
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 216 0 1 2 1.0 Cc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
137630892 161219 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 347 9 1 3 4.1 COc1ccc(F)cc1C1CC1CNCc1ccccc1OCCF 10.1021/acs.jmedchem.7b00584
CHEMBL4086286 161219 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 347 9 1 3 4.1 COc1ccc(F)cc1C1CC1CNCc1ccccc1OCCF 10.1021/acs.jmedchem.7b00584
CHEMBL4117192 161219 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 347 9 1 3 4.1 COc1ccc(F)cc1C1CC1CNCc1ccccc1OCCF 10.1021/acs.jmedchem.7b00584
107992 2553 None 33 Human Functional pEC50 = 7.6 7.6 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
165 2553 None 33 Human Functional pEC50 = 7.6 7.6 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
CHEMBL269521 2553 None 33 Human Functional pEC50 = 7.6 7.6 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
DB12111 2553 None 33 Human Functional pEC50 = 7.6 7.6 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
44573161 193325 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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(Oc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2009.02.071
CHEMBL523521 193325 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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(Oc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2009.02.071
10401602 123135 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 CCOc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL360968 123135 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 CCOc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
9881119 207931 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 232 2 1 3 1.7 C[C@H](N)CN1CCc2ccc3c(c21)CCCO3 10.1016/j.bmcl.2003.05.001
CHEMBL80482 207931 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 232 2 1 3 1.7 C[C@H](N)CN1CCc2ccc3c(c21)CCCO3 10.1016/j.bmcl.2003.05.001
137630892 161219 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 347 9 1 3 4.1 COc1ccc(F)cc1C1CC1CNCc1ccccc1OCCF 10.1021/acs.jmedchem.7b00584
CHEMBL4086286 161219 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 347 9 1 3 4.1 COc1ccc(F)cc1C1CC1CNCc1ccccc1OCCF 10.1021/acs.jmedchem.7b00584
CHEMBL4117192 161219 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 347 9 1 3 4.1 COc1ccc(F)cc1C1CC1CNCc1ccccc1OCCF 10.1021/acs.jmedchem.7b00584
107992 2553 None 33 Human Functional pEC50 = 7.6 7.6 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
165 2553 None 33 Human Functional pEC50 = 7.6 7.6 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
CHEMBL269521 2553 None 33 Human Functional pEC50 = 7.6 7.6 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
DB12111 2553 None 33 Human Functional pEC50 = 7.6 7.6 6 2
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 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
168295069 193136 None 0 Human Functional pEC50 = 5.6 5.6 -3 2
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 317 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccncc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5208635 193136 None 0 Human Functional pEC50 = 5.6 5.6 -3 2
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 317 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccncc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5222843 193136 None 0 Human Functional pEC50 = 5.6 5.6 -3 2
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 317 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccncc1Cl 10.1021/acsmedchemlett.1c00694
11288140 84803 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 213 0 1 3 0.7 N#Cc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL223090 84803 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 213 0 1 3 0.7 N#Cc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
162644225 183727 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 2.5 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4777891 183727 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 2.5 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802348 183727 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 2.5 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
4646586 193122 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 2 2 4.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5209080 193122 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 2 2 4.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222774 193122 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 2 2 4.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
168295069 193136 None 0 Human Functional pEC50 = 5.6 5.6 -3 2
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 317 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccncc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5208635 193136 None 0 Human Functional pEC50 = 5.6 5.6 -3 2
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 317 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccncc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5222843 193136 None 0 Human Functional pEC50 = 5.6 5.6 -3 2
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 317 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccncc1Cl 10.1021/acsmedchemlett.1c00694
162644225 183727 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 2.5 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4777891 183727 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 2.5 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802348 183727 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 2.5 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
4646586 193122 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 2 2 4.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5209080 193122 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 2 2 4.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222774 193122 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 2 2 4.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
118733770 120711 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 253 6 1 2 3.6 CCCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416037 120711 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 253 6 1 2 3.6 CCCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546892 120711 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 253 6 1 2 3.6 CCCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
155548667 176478 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
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 179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4537637 176478 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
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 179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4595810 176478 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
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 179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
44572747 12709 None 0 Human Functional pEC50 = 7.5 7.5 2 2
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 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccccc1F 10.1021/jm801354e
CHEMBL1187580 12709 None 0 Human Functional pEC50 = 7.5 7.5 2 2
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 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccccc1F 10.1021/jm801354e
CHEMBL510308 12709 None 0 Human Functional pEC50 = 7.5 7.5 2 2
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 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccccc1F 10.1021/jm801354e
168268706 192866 None 0 Human Functional pEC50 = 7.5 7.5 1 2
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 282 1 3 2 3.2 Oc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5170614 192866 None 0 Human Functional pEC50 = 7.5 7.5 1 2
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 282 1 3 2 3.2 Oc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221142 192866 None 0 Human Functional pEC50 = 7.5 7.5 1 2
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 282 1 3 2 3.2 Oc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
12986493 204475 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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)cc2N2CCNC[C@@H]12 10.1016/s0960-894x(00)00400-5
CHEMBL60830 204475 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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)cc2N2CCNC[C@@H]12 10.1016/s0960-894x(00)00400-5
44572698 12556 None 0 Human Functional pEC50 = 5.5 5.5 -5 2
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 197 2 1 1 2.9 NC[C@H]1C[C@@H]1c1ccc2ccccc2c1 10.1021/jm801354e
CHEMBL1186700 12556 None 0 Human Functional pEC50 = 5.5 5.5 -5 2
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 197 2 1 1 2.9 NC[C@H]1C[C@@H]1c1ccc2ccccc2c1 10.1021/jm801354e
CHEMBL474885 12556 None 0 Human Functional pEC50 = 5.5 5.5 -5 2
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 197 2 1 1 2.9 NC[C@H]1C[C@@H]1c1ccc2ccccc2c1 10.1021/jm801354e
137656030 158734 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 301 3 0 5 3.6 CCn1nc(-c2nccc3ccccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
CHEMBL4092473 158734 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 301 3 0 5 3.6 CCn1nc(-c2nccc3ccccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
155548667 176478 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
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 179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4537637 176478 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
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 179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4595810 176478 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
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 179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
45484726 200859 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 257 2 1 4 0.9 Cn1c2c(c(=O)n1Cc1ccccc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL576912 200859 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 257 2 1 4 0.9 Cn1c2c(c(=O)n1Cc1ccccc1)CCNCC2 10.1016/j.bmcl.2009.07.063
168289654 193068 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 270 1 3 3 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5193914 193068 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 270 1 3 3 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5222453 193068 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 270 1 3 3 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
168280142 192970 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 290 1 2 2 3.4 Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5183068 192970 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 290 1 2 2 3.4 Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5221869 192970 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 290 1 2 2 3.4 Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
168280142 192970 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 290 1 2 2 3.4 Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5183068 192970 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 290 1 2 2 3.4 Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5221869 192970 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 290 1 2 2 3.4 Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
168289654 193068 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 270 1 3 3 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5193914 193068 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 270 1 3 3 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5222453 193068 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 270 1 3 3 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
20026449 87340 None 1 Human Functional pEC50 = 5.5 5.5 2 2
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 182 2 1 4 0.8 CCOc1noc2c1CCNCC2 10.1021/jm301656h
CHEMBL2331793 87340 None 1 Human Functional pEC50 = 5.5 5.5 2 2
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 182 2 1 4 0.8 CCOc1noc2c1CCNCC2 10.1021/jm301656h
146464686 192106 None 0 Human Functional pEC50 = 5.5 5.5 -8 2
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 266 1 3 4 1.9 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5201492 192106 None 0 Human Functional pEC50 = 5.5 5.5 -8 2
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 266 1 3 4 1.9 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
44420682 137695 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 270 0 0 2 2.1 CN1CCN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2C1 10.1021/jm0612968
CHEMBL375642 137695 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 270 0 0 2 2.1 CN1CCN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2C1 10.1021/jm0612968
118733816 120723 None 0 Human Functional pEC50 = 6.5 6.5 2 2
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
CHEMBL3416060 120723 None 0 Human Functional pEC50 = 6.5 6.5 2 2
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
CHEMBL3546911 120723 None 0 Human Functional pEC50 = 6.5 6.5 2 2
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
11313985 91117 None 0 Human Functional pEC50 = 8.5 8.5 15 3
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 COc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397878 91117 None 0 Human Functional pEC50 = 8.5 8.5 15 3
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 COc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
11206703 91126 None 0 Human Functional pEC50 = 8.5 8.5 12 3
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 216 0 1 2 1.0 C[C@@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
CHEMBL2397887 91126 None 0 Human Functional pEC50 = 8.5 8.5 12 3
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 216 0 1 2 1.0 C[C@@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
44572166 12464 None 0 Human Functional pEC50 = 8.5 8.5 7 3
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 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
CHEMBL1186133 12464 None 0 Human Functional pEC50 = 8.5 8.5 7 3
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 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
CHEMBL451232 12464 None 0 Human Functional pEC50 = 8.5 8.5 7 3
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 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
155532108 176671 None 0 Human Functional pEC50 = 8.5 8.5 -1 3
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 183 2 1 1 2.0 NC[C@H]1C[C@]1(F)c1cccc(F)c1 10.1016/j.ejmech.2019.111626
CHEMBL4466591 176671 None 0 Human Functional pEC50 = 8.5 8.5 -1 3
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 183 2 1 1 2.0 NC[C@H]1C[C@]1(F)c1cccc(F)c1 10.1016/j.ejmech.2019.111626
CHEMBL4597360 176671 None 0 Human Functional pEC50 = 8.5 8.5 -1 3
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 183 2 1 1 2.0 NC[C@H]1C[C@]1(F)c1cccc(F)c1 10.1016/j.ejmech.2019.111626
11777150 62625 None 0 Human Functional pEC50 = 8.5 8.5 20 3
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 255 0 2 2 2.4 CC1CNCCc2cc(O)c(Br)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178313 62625 None 0 Human Functional pEC50 = 8.5 8.5 20 3
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 255 0 2 2 2.4 CC1CNCCc2cc(O)c(Br)cc21 10.1016/j.bmcl.2004.12.080
44389645 64202 None 0 Human Functional pEC50 = 8.5 8.5 26 3
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 269 1 1 2 2.7 COc1cc2c(cc1Br)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL180867 64202 None 0 Human Functional pEC50 = 8.5 8.5 26 3
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 269 1 1 2 2.7 COc1cc2c(cc1Br)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
11608308 64330 None 3 Human Functional pEC50 = 8.5 8.5 42 3
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 229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
CHEMBL181076 64330 None 3 Human Functional pEC50 = 8.5 8.5 42 3
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 229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
36906 104936 None 31 Rat Functional pEC50 = 8.5 8.5 -1 3
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 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm050663x
CHEMBL31115 104936 None 31 Rat Functional pEC50 = 8.5 8.5 -1 3
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 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm050663x
162656505 181010 None 0 Human Functional pEC50 = 8.5 8.5 316 3
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 284 2 1 2 2.9 FC(F)(F)CCc1cccc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4757718 181010 None 0 Human Functional pEC50 = 8.5 8.5 316 3
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 284 2 1 2 2.9 FC(F)(F)CCc1cccc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
11608308 64330 None 3 Human Functional pEC50 = 8.5 8.5 42 3
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 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
CHEMBL181076 64330 None 3 Human Functional pEC50 = 8.5 8.5 42 3
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 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
122442270 138433 None 1 Human Functional pEC50 = 8.5 8.5 6 3
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 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770753 138433 None 1 Human Functional pEC50 = 8.5 8.5 6 3
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 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771382 138433 None 1 Human Functional pEC50 = 8.5 8.5 6 3
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 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442251 138447 None 0 Human Functional pEC50 = 8.5 8.5 15 3
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 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770225 138447 None 0 Human Functional pEC50 = 8.5 8.5 15 3
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 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771396 138447 None 0 Human Functional pEC50 = 8.5 8.5 15 3
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 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
134142903 145328 None 0 Human Functional pEC50 = 8.5 8.5 630 3
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 256 2 1 2 2.8 c1cc(CC2CCC2)c2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3912721 145328 None 0 Human Functional pEC50 = 8.5 8.5 630 3
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 256 2 1 2 2.8 c1cc(CC2CCC2)c2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
83753960 150784 None 0 Human Functional pEC50 = 8.5 8.5 39 2
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)CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3955996 150784 None 0 Human Functional pEC50 = 8.5 8.5 39 2
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)CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
134156657 153922 None 0 Human Functional pEC50 = 8.5 8.5 12 2
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 242 1 1 2 2.7 c1cc(C2CCC2)c2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3982618 153922 None 0 Human Functional pEC50 = 8.5 8.5 12 2
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 242 1 1 2 2.7 c1cc(C2CCC2)c2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
122442251 138447 None 0 Human Functional pEC50 = 8.5 8.5 15 3
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 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770225 138447 None 0 Human Functional pEC50 = 8.5 8.5 15 3
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 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771396 138447 None 0 Human Functional pEC50 = 8.5 8.5 15 3
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 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
11652452 89160 None 0 Human Functional pEC50 = 8.5 8.5 9 3
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 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337492 89160 None 0 Human Functional pEC50 = 8.5 8.5 9 3
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 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365703 89160 None 0 Human Functional pEC50 = 8.5 8.5 9 3
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 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
11609026 89161 None 0 Human Functional pEC50 = 8.5 8.5 38 3
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 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337500 89161 None 0 Human Functional pEC50 = 8.5 8.5 38 3
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 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365705 89161 None 0 Human Functional pEC50 = 8.5 8.5 38 3
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 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
44572798 12654 None 1 Human Functional pEC50 = 8.5 8.5 1 3
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 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1cccc(F)c1 10.1021/jm801354e
CHEMBL1187187 12654 None 1 Human Functional pEC50 = 8.5 8.5 1 3
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 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1cccc(F)c1 10.1021/jm801354e
CHEMBL492926 12654 None 1 Human Functional pEC50 = 8.5 8.5 1 3
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 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1cccc(F)c1 10.1021/jm801354e
44572808 12710 None 0 Human Functional pEC50 = 8.5 8.5 1 3
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 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1cccc(O)c1 10.1021/jm801354e
CHEMBL1187585 12710 None 0 Human Functional pEC50 = 8.5 8.5 1 3
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 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1cccc(O)c1 10.1021/jm801354e
CHEMBL510383 12710 None 0 Human Functional pEC50 = 8.5 8.5 1 3
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 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1cccc(O)c1 10.1021/jm801354e
11949710 202358 None 0 Human Functional pEC50 = 8.5 8.5 50 3
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL594717 202358 None 0 Human Functional pEC50 = 8.5 8.5 50 3
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
11658860 2344 None 24 Human Functional pEC50 = 8.5 8.5 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
2941 2344 None 24 Human Functional pEC50 = 8.5 8.5 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
4374 2344 None 24 Human Functional pEC50 = 8.5 8.5 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
CHEMBL360328 2344 None 24 Human Functional pEC50 = 8.5 8.5 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
DB04871 2344 None 24 Human Functional pEC50 = 8.5 8.5 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
92042921 120734 None 0 Human Functional pEC50 = 8.5 8.5 104 2
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 227 5 1 2 2.2 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/jm5019274
CHEMBL3416067 120734 None 0 Human Functional pEC50 = 8.5 8.5 104 2
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 227 5 1 2 2.2 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/jm5019274
CHEMBL3546961 120734 None 0 Human Functional pEC50 = 8.5 8.5 104 2
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 227 5 1 2 2.2 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/jm5019274
122442270 138433 None 1 Human Functional pEC50 = 8.5 8.5 6 3
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 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770753 138433 None 1 Human Functional pEC50 = 8.5 8.5 6 3
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 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771382 138433 None 1 Human Functional pEC50 = 8.5 8.5 6 3
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 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
11658860 2344 None 24 Human Functional pEC50 = 8.5 8.5 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
2941 2344 None 24 Human Functional pEC50 = 8.5 8.5 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
4374 2344 None 24 Human Functional pEC50 = 8.5 8.5 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
CHEMBL360328 2344 None 24 Human Functional pEC50 = 8.5 8.5 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
DB04871 2344 None 24 Human Functional pEC50 = 8.5 8.5 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
44572174 12551 None 0 Human Functional pEC50 = 8.5 8.5 2 3
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 195 2 1 1 2.7 Cc1cccc(Cl)c1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL1186687 12551 None 0 Human Functional pEC50 = 8.5 8.5 2 3
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 195 2 1 1 2.7 Cc1cccc(Cl)c1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL474634 12551 None 0 Human Functional pEC50 = 8.5 8.5 2 3
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 195 2 1 1 2.7 Cc1cccc(Cl)c1[C@H]1C[C@@H]1CN 10.1021/jm801354e
11658860 2344 None 24 Human Functional pEC50 = 8.4 8.4 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
2941 2344 None 24 Human Functional pEC50 = 8.4 8.4 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
4374 2344 None 24 Human Functional pEC50 = 8.4 8.4 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
CHEMBL360328 2344 None 24 Human Functional pEC50 = 8.4 8.4 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
DB04871 2344 None 24 Human Functional pEC50 = 8.4 8.4 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
135453290 133675 None 29 Rat Functional pEC50 = 8.4 8.4 -1 7
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 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL371300 133675 None 29 Rat Functional pEC50 = 8.4 8.4 -1 7
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 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
122442286 138438 None 0 Human Functional pEC50 = 8.4 8.4 13 3
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 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 138438 None 0 Human Functional pEC50 = 8.4 8.4 13 3
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 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 138438 None 0 Human Functional pEC50 = 8.4 8.4 13 3
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 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442286 138438 None 0 Human Functional pEC50 = 8.4 8.4 13 3
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 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 138438 None 0 Human Functional pEC50 = 8.4 8.4 13 3
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 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 138438 None 0 Human Functional pEC50 = 8.4 8.4 13 3
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 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
166 3359 None 19 Human Functional pEC50 = 8.4 8.4 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm0709034
3045227 3359 None 19 Human Functional pEC50 = 8.4 8.4 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm0709034
CHEMBL76781 3359 None 19 Human Functional pEC50 = 8.4 8.4 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm0709034
9991444 62652 None 1 Human Functional pEC50 = 8.4 8.4 4 3
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 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
CHEMBL178366 62652 None 1 Human Functional pEC50 = 8.4 8.4 4 3
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 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
24773649 94880 None 0 Human Functional pEC50 = 8.4 8.4 2 3
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 3.2 C[C@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
CHEMBL253591 94880 None 0 Human Functional pEC50 = 8.4 8.4 2 3
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 3.2 C[C@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
24773897 94911 None 2 Human Functional pEC50 = 8.4 8.4 251 2
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 213 0 1 1 2.7 C[C@@H]1CNCCc2ccc(Cl)c(F)c21 10.1021/jm0709034
CHEMBL253807 94911 None 2 Human Functional pEC50 = 8.4 8.4 251 2
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 213 0 1 1 2.7 C[C@@H]1CNCCc2ccc(Cl)c(F)c21 10.1021/jm0709034
134137343 143154 None 0 Human Functional pEC50 = 8.4 8.4 15 2
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 266 1 1 3 2.5 COc1cc2c(cc1Cl)CC[C@@H]1CNCCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3895184 143154 None 0 Human Functional pEC50 = 8.4 8.4 15 2
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 266 1 1 3 2.5 COc1cc2c(cc1Cl)CC[C@@H]1CNCCCN21 10.1016/j.bmcl.2016.11.016
11587397 89090 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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
CHEMBL2337489 89090 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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
CHEMBL2364893 89090 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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
44572804 12627 None 0 Human Functional pEC50 = 7.5 7.5 2 3
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 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1 10.1021/jm801354e
CHEMBL1187088 12627 None 0 Human Functional pEC50 = 7.5 7.5 2 3
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 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1 10.1021/jm801354e
CHEMBL490064 12627 None 0 Human Functional pEC50 = 7.5 7.5 2 3
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 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1 10.1021/jm801354e
45484858 201032 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 368 4 1 6 1.8 Cn1c(COc2ccccc2C(F)(F)F)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
CHEMBL578364 201032 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 368 4 1 6 1.8 Cn1c(COc2ccccc2C(F)(F)F)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
45484662 200947 None 0 Human Functional pEC50 = 7.5 7.5 2 2
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 289 2 1 4 1.6 O=c1cc2c(nn1Cc1cccc(Cl)c1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL577691 200947 None 0 Human Functional pEC50 = 7.5 7.5 2 2
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 289 2 1 4 1.6 O=c1cc2c(nn1Cc1cccc(Cl)c1)CCNCC2 10.1016/j.bmcl.2009.07.063
137647004 157934 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 326 4 1 4 3.3 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)CCO 10.1021/acs.jmedchem.7b00385
CHEMBL4083671 157934 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 326 4 1 4 3.3 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)CCO 10.1021/acs.jmedchem.7b00385
44622848 193456 None 0 Human Functional pEC50 = 7.5 7.5 11 2
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 255 2 1 4 1.0 O=c1cc2c(nn1Cc1ccccc1)CCNCC2 10.1016/j.bmcl.2016.06.060
CHEMBL524778 193456 None 0 Human Functional pEC50 = 7.5 7.5 11 2
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 255 2 1 4 1.0 O=c1cc2c(nn1Cc1ccccc1)CCNCC2 10.1016/j.bmcl.2016.06.060
122442270 138433 None 1 Human Functional pEC50 = 7.5 7.5 6 3
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 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770753 138433 None 1 Human Functional pEC50 = 7.5 7.5 6 3
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 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771382 138433 None 1 Human Functional pEC50 = 7.5 7.5 6 3
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 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
11291 3220 None 14 Human Functional pEC50 = 7.5 7.5 -1 4
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 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1016/j.bmcl.2005.06.104
4980 3220 None 14 Human Functional pEC50 = 7.5 7.5 -1 4
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 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1016/j.bmcl.2005.06.104
CHEMBL65547 3220 None 14 Human Functional pEC50 = 7.5 7.5 -1 4
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 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1016/j.bmcl.2005.06.104
157 2069 None 2 Rat Functional pEC50 = 7.5 7.5 -2 3
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 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
9840090 2069 None 2 Rat Functional pEC50 = 7.5 7.5 -2 3
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 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
CHEMBL134519 2069 None 2 Rat Functional pEC50 = 7.5 7.5 -2 3
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 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
157 2069 None 2 Rat Functional pEC50 = 7.5 7.5 -2 3
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 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1016/j.bmcl.2007.03.073
9840090 2069 None 2 Rat Functional pEC50 = 7.5 7.5 -2 3
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 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1016/j.bmcl.2007.03.073
CHEMBL134519 2069 None 2 Rat Functional pEC50 = 7.5 7.5 -2 3
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 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1016/j.bmcl.2007.03.073
168268706 192866 None 0 Human Functional pEC50 = 7.5 7.5 1 2
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 282 1 3 2 3.2 Oc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5170614 192866 None 0 Human Functional pEC50 = 7.5 7.5 1 2
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 282 1 3 2 3.2 Oc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221142 192866 None 0 Human Functional pEC50 = 7.5 7.5 1 2
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 282 1 3 2 3.2 Oc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
145 140 None 16 Human Functional pEC50 = 7.5 7.5 -33 12
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
1832 140 None 16 Human Functional pEC50 = 7.5 7.5 -33 12
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
CHEMBL7257 140 None 16 Human Functional pEC50 = 7.5 7.5 -33 12
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
DB14010 140 None 16 Human Functional pEC50 = 7.5 7.5 -33 12
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
54585653 61485 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 307 2 1 3 2.8 FC(F)(F)c1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
CHEMBL1770385 61485 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 307 2 1 3 2.8 FC(F)(F)c1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
20026449 87340 None 1 Human Functional pEC50 = 5.5 5.5 2 2
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 182 2 1 4 0.8 CCOc1noc2c1CCNCC2 10.1021/jm301656h
CHEMBL2331793 87340 None 1 Human Functional pEC50 = 5.5 5.5 2 2
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 182 2 1 4 0.8 CCOc1noc2c1CCNCC2 10.1021/jm301656h
44572252 12555 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 241 3 1 1 3.6 NC[C@H]1C[C@@H]1c1ccccc1-c1ccc(F)cc1 10.1021/jm801354e
CHEMBL1186699 12555 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 241 3 1 1 3.6 NC[C@H]1C[C@@H]1c1ccccc1-c1ccc(F)cc1 10.1021/jm801354e
CHEMBL474860 12555 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 241 3 1 1 3.6 NC[C@H]1C[C@@H]1c1ccccc1-c1ccc(F)cc1 10.1021/jm801354e
12370466 12436 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 147 2 1 1 1.7 NC[C@H]1C[C@H]1c1ccccc1 10.1021/jm801354e
CHEMBL1185943 12436 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 147 2 1 1 1.7 NC[C@H]1C[C@H]1c1ccccc1 10.1021/jm801354e
CHEMBL442657 12436 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 147 2 1 1 1.7 NC[C@H]1C[C@H]1c1ccccc1 10.1021/jm801354e
162656326 183783 None 0 Human Functional pEC50 = 6.5 6.5 6 2
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 251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4757142 183783 None 0 Human Functional pEC50 = 6.5 6.5 6 2
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 251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802987 183783 None 0 Human Functional pEC50 = 6.5 6.5 6 2
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 251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
137629241 161094 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
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 301 6 2 3 3.4 COc1ccc(F)cc1C1CC1CNCc1ccccc1O 10.1021/acs.jmedchem.7b00584
CHEMBL4102683 161094 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
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 301 6 2 3 3.4 COc1ccc(F)cc1C1CC1CNCc1ccccc1O 10.1021/acs.jmedchem.7b00584
CHEMBL4116193 161094 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
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 301 6 2 3 3.4 COc1ccc(F)cc1C1CC1CNCc1ccccc1O 10.1021/acs.jmedchem.7b00584
172453443 196056 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at 5-HT2C (unknown origin)Agonist activity at 5-HT2C (unknown origin)
ChEMBL 271 0 2 2 3.5 Oc1cc2c3c(c1Cl)-c1ccccc1C[C@H]3NCC2 10.1016/j.ejmech.2023.115414
CHEMBL5415990 196056 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at 5-HT2C (unknown origin)Agonist activity at 5-HT2C (unknown origin)
ChEMBL 271 0 2 2 3.5 Oc1cc2c3c(c1Cl)-c1ccccc1C[C@H]3NCC2 10.1016/j.ejmech.2023.115414
137629241 161094 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
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 301 6 2 3 3.4 COc1ccc(F)cc1C1CC1CNCc1ccccc1O 10.1021/acs.jmedchem.7b00584
CHEMBL4102683 161094 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
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 301 6 2 3 3.4 COc1ccc(F)cc1C1CC1CNCc1ccccc1O 10.1021/acs.jmedchem.7b00584
CHEMBL4116193 161094 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
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 301 6 2 3 3.4 COc1ccc(F)cc1C1CC1CNCc1ccccc1O 10.1021/acs.jmedchem.7b00584
70693928 74511 None 0 Human Functional pEC50 = 6.5 6.5 3 2
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 253 5 1 2 3.3 NC[C@H]1C[C@@H]1c1ccccc1OCc1ccccc1 10.1021/ml200206z
CHEMBL2022192 74511 None 0 Human Functional pEC50 = 6.5 6.5 3 2
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 253 5 1 2 3.3 NC[C@H]1C[C@@H]1c1ccccc1OCc1ccccc1 10.1021/ml200206z
CHEMBL2028036 74511 None 0 Human Functional pEC50 = 6.5 6.5 3 2
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 253 5 1 2 3.3 NC[C@H]1C[C@@H]1c1ccccc1OCc1ccccc1 10.1021/ml200206z
3568612 193104 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5203138 193104 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222646 193104 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
11096110 195637 None 4 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 219 0 1 2 2.4 Fc1ccc2c(c1)C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
CHEMBL5407824 195637 None 4 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 219 0 1 2 2.4 Fc1ccc2c(c1)C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
137629785 161280 None 0 Human Functional pEC50 = 6.5 6.5 2 2
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
CHEMBL4095562 161280 None 0 Human Functional pEC50 = 6.5 6.5 2 2
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
CHEMBL4117659 161280 None 0 Human Functional pEC50 = 6.5 6.5 2 2
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
122442324 138437 None 0 Human Functional pEC50 = 6.5 6.5 12 2
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=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770174 138437 None 0 Human Functional pEC50 = 6.5 6.5 12 2
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=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771386 138437 None 0 Human Functional pEC50 = 6.5 6.5 12 2
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=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
160875 178950 None 25 Human Functional pEC50 = 6.5 6.5 12 3
Partial agonist activity at 5-HT2CR (unknown origin) expressed in HEK293T cells assessed as increase in calcium flux measured for 3 mins by FLIPR assayPartial agonist activity at 5-HT2CR (unknown origin) expressed in HEK293T cells assessed as increase in calcium flux measured for 3 mins by FLIPR assay
ChEMBL 267 1 2 3 2.8 COc1c(O)cc2c3c1-c1ccccc1C[C@H]3NCC2 10.1021/acsmedchemlett.3c00454
CHEMBL469423 178950 None 25 Human Functional pEC50 = 6.5 6.5 12 3
Partial agonist activity at 5-HT2CR (unknown origin) expressed in HEK293T cells assessed as increase in calcium flux measured for 3 mins by FLIPR assayPartial agonist activity at 5-HT2CR (unknown origin) expressed in HEK293T cells assessed as increase in calcium flux measured for 3 mins by FLIPR assay
ChEMBL 267 1 2 3 2.8 COc1c(O)cc2c3c1-c1ccccc1C[C@H]3NCC2 10.1021/acsmedchemlett.3c00454
624491 126257 None 9 Human Functional pEC50 = 6.5 6.5 123 2
Partial agonist activity at human 5-HT2C stably transfected in HEK293T cells measured after 18 to 24 hrs by FLIPR assayPartial agonist activity at human 5-HT2C stably transfected in HEK293T cells measured after 18 to 24 hrs by FLIPR assay
ChEMBL 281 2 1 3 3.1 COc1cc2c3c(c1OC)-c1ccccc1CC3NCC2 10.1016/j.ejmech.2023.115414
CHEMBL36496 126257 None 9 Human Functional pEC50 = 6.5 6.5 123 2
Partial agonist activity at human 5-HT2C stably transfected in HEK293T cells measured after 18 to 24 hrs by FLIPR assayPartial agonist activity at human 5-HT2C stably transfected in HEK293T cells measured after 18 to 24 hrs by FLIPR assay
ChEMBL 281 2 1 3 3.1 COc1cc2c3c(c1OC)-c1ccccc1CC3NCC2 10.1016/j.ejmech.2023.115414
137629785 161280 None 0 Human Functional pEC50 = 6.5 6.5 2 2
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
CHEMBL4095562 161280 None 0 Human Functional pEC50 = 6.5 6.5 2 2
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
CHEMBL4117659 161280 None 0 Human Functional pEC50 = 6.5 6.5 2 2
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
3568612 193104 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5203138 193104 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222646 193104 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
122442324 138437 None 0 Human Functional pEC50 = 6.5 6.5 12 2
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=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770174 138437 None 0 Human Functional pEC50 = 6.5 6.5 12 2
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=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771386 138437 None 0 Human Functional pEC50 = 6.5 6.5 12 2
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=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
155534560 176526 None 0 Human Functional pEC50 = 6.5 6.5 -2 2
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 243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br 10.1016/j.ejmech.2019.111626
CHEMBL4470610 176526 None 0 Human Functional pEC50 = 6.5 6.5 -2 2
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 243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br 10.1016/j.ejmech.2019.111626
CHEMBL4596162 176526 None 0 Human Functional pEC50 = 6.5 6.5 -2 2
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 243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br 10.1016/j.ejmech.2019.111626
149663072 196095 None 0 Human Functional pEC50 = 7.5 7.5 2 2
Agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayAgonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
CHEMBL5416800 196095 None 0 Human Functional pEC50 = 7.5 7.5 2 2
Agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayAgonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
44622848 193456 None 0 Human Functional pEC50 = 7.5 7.5 11 2
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 255 2 1 4 1.0 O=c1cc2c(nn1Cc1ccccc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL524778 193456 None 0 Human Functional pEC50 = 7.5 7.5 11 2
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 255 2 1 4 1.0 O=c1cc2c(nn1Cc1ccccc1)CCNCC2 10.1016/j.bmcl.2009.07.063
45484673 201414 None 0 Human Functional pEC50 = 7.5 7.5 8 2
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 289 2 1 4 1.6 O=c1cc2c(nn1Cc1ccc(Cl)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL585012 201414 None 0 Human Functional pEC50 = 7.5 7.5 8 2
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 289 2 1 4 1.6 O=c1cc2c(nn1Cc1ccc(Cl)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
44225654 187296 None 0 Human Functional pEC50 = 7.5 7.5 1 2
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 420 4 1 4 3.3 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCC(Oc2ccccc2Cl)CC1 10.1016/j.bmcl.2009.02.071
CHEMBL492301 187296 None 0 Human Functional pEC50 = 7.5 7.5 1 2
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 420 4 1 4 3.3 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCC(Oc2ccccc2Cl)CC1 10.1016/j.bmcl.2009.02.071
44573224 187337 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 406 4 1 4 2.9 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CC[C@H](Oc2ccccc2Cl)C1 10.1016/j.bmcl.2009.02.071
CHEMBL492557 187337 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 406 4 1 4 2.9 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CC[C@H](Oc2ccccc2Cl)C1 10.1016/j.bmcl.2009.02.071
44573159 193422 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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(Oc2ccccc2Cl)C1 10.1016/j.bmcl.2009.02.071
CHEMBL524171 193422 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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(Oc2ccccc2Cl)C1 10.1016/j.bmcl.2009.02.071
44316017 207910 None 0 Human Functional pEC50 = 7.5 7.5 -4 3
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 228 2 1 2 2.2 C[C@H](N)CN1CCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL80366 207910 None 0 Human Functional pEC50 = 7.5 7.5 -4 3
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 228 2 1 2 2.2 C[C@H](N)CN1CCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2003.05.001
162659286 183801 None 0 Human Functional pEC50 = 7.5 7.5 12 3
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
CHEMBL4762225 183801 None 0 Human Functional pEC50 = 7.5 7.5 12 3
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
CHEMBL4803142 183801 None 0 Human Functional pEC50 = 7.5 7.5 12 3
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
149663072 196095 None 0 Human Functional pEC50 = 7.5 7.5 2 2
Agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayAgonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
CHEMBL5416800 196095 None 0 Human Functional pEC50 = 7.5 7.5 2 2
Agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayAgonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
122442270 138433 None 1 Human Functional pEC50 = 7.5 7.5 6 3
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 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770753 138433 None 1 Human Functional pEC50 = 7.5 7.5 6 3
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 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771382 138433 None 1 Human Functional pEC50 = 7.5 7.5 6 3
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 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
132820211 148654 None 0 Human Functional pEC50 = 7.5 7.5 3 2
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 COc1cccc2c1N1CCCNC[C@H]1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3938893 148654 None 0 Human Functional pEC50 = 7.5 7.5 3 2
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 COc1cccc2c1N1CCCNC[C@H]1CC2 10.1016/j.bmcl.2016.11.016
54584721 61478 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 Fc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770377 61478 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 Fc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
155529999 171581 None 0 Human Functional pEC50 = 6.5 6.5 2 2
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 273 2 1 3 2.4 Clc1ccccc1Cc1cc2c(nn1)CCNCC2 10.1016/j.bmcl.2016.06.060
CHEMBL4463588 171581 None 0 Human Functional pEC50 = 6.5 6.5 2 2
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 273 2 1 3 2.4 Clc1ccccc1Cc1cc2c(nn1)CCNCC2 10.1016/j.bmcl.2016.06.060
155562772 175332 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 273 2 1 3 2.4 Clc1ccc(Cc2cc3c(nn2)CCNCC3)cc1 10.1016/j.bmcl.2016.06.060
CHEMBL4571641 175332 None 0 Human Functional pEC50 = 6.5 6.5 1 2
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 273 2 1 3 2.4 Clc1ccc(Cc2cc3c(nn2)CCNCC3)cc1 10.1016/j.bmcl.2016.06.060
137653689 158697 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 340 2 0 3 4.7 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CCCCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4092132 158697 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 340 2 0 3 4.7 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CCCCC1 10.1021/acs.jmedchem.7b00385
172454425 195597 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.3 Clc1ccc2c(c1)OC1(C=C2)CCCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5406797 195597 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.3 Clc1ccc2c(c1)OC1(C=C2)CCCNCC1 10.1021/acsmedchemlett.3c00454
155534560 176526 None 0 Human Functional pEC50 = 6.5 6.5 -2 2
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 243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br 10.1016/j.ejmech.2019.111626
CHEMBL4470610 176526 None 0 Human Functional pEC50 = 6.5 6.5 -2 2
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 243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br 10.1016/j.ejmech.2019.111626
CHEMBL4596162 176526 None 0 Human Functional pEC50 = 6.5 6.5 -2 2
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 243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br 10.1016/j.ejmech.2019.111626
137645667 158052 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 301 3 0 5 3.6 CCn1nc(-c2ccnc3ccccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
CHEMBL4084723 158052 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 301 3 0 5 3.6 CCn1nc(-c2ccnc3ccccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
134265590 164853 None 0 Human Functional pEC50 = 6.5 6.5 2 3
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 c1cc2c(cn1)N1CCNC[C@H]1CC2 10.1016/j.bmcl.2021.127872
CHEMBL4217846 164853 None 0 Human Functional pEC50 = 6.5 6.5 2 3
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 c1cc2c(cn1)N1CCNC[C@H]1CC2 10.1016/j.bmcl.2021.127872
24773894 63000 None 2 Human Functional pEC50 = 6.5 6.5 9 2
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 3.2 C[C@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
CHEMBL178566 63000 None 2 Human Functional pEC50 = 6.5 6.5 9 2
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 3.2 C[C@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
24773979 130237 None 20 Human Functional pEC50 = 6.5 6.5 4 3
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 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1021/jm0709034
CHEMBL367796 130237 None 20 Human Functional pEC50 = 6.5 6.5 4 3
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 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1021/jm0709034
10704473 79605 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
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 226 2 1 2 2.8 C[C@H](N)Cn1ccc2c(Cl)c(F)ccc21 10.1021/jm970030l
CHEMBL2114266 79605 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
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 226 2 1 2 2.8 C[C@H](N)Cn1ccc2c(Cl)c(F)ccc21 10.1021/jm970030l
82045957 195718 None 1 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 221 0 1 2 2.5 Clc1ccc2c(c1)OC1(C=C2)CCNC1 10.1021/acsmedchemlett.3c00454
CHEMBL5409492 195718 None 1 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 221 0 1 2 2.5 Clc1ccc2c(c1)OC1(C=C2)CCNC1 10.1021/acsmedchemlett.3c00454
1400243 94809 None 55 Human Functional pEC50 = 5.5 5.5 - 1
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 147 0 1 1 1.4 c1ccc2c(c1)CCNCC2 10.1021/jm0709034
CHEMBL253155 94809 None 55 Human Functional pEC50 = 5.5 5.5 - 1
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 147 0 1 1 1.4 c1ccc2c(c1)CCNCC2 10.1021/jm0709034
5745501 200638 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
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 226 2 1 2 2.8 C[C@@H](N)Cn1ccc2cc(F)c(Cl)cc21 10.1021/jm970030l
CHEMBL574985 200638 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
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 226 2 1 2 2.8 C[C@@H](N)Cn1ccc2cc(F)c(Cl)cc21 10.1021/jm970030l
172454425 195597 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.3 Clc1ccc2c(c1)OC1(C=C2)CCCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5406797 195597 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.3 Clc1ccc2c(c1)OC1(C=C2)CCCNCC1 10.1021/acsmedchemlett.3c00454
11096110 195637 None 4 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 219 0 1 2 2.4 Fc1ccc2c(c1)C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
CHEMBL5407824 195637 None 4 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 219 0 1 2 2.4 Fc1ccc2c(c1)C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
45484896 201048 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 325 4 1 7 0.6 Cn1c(COc2cccc(C#N)c2)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
CHEMBL578564 201048 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 325 4 1 7 0.6 Cn1c(COc2cccc(C#N)c2)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
44412404 77797 None 4 Human Functional pEC50 = 6.5 6.5 -2 3
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 206 1 1 2 1.6 Fc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209106 77797 None 4 Human Functional pEC50 = 6.5 6.5 -2 3
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 206 1 1 2 1.6 Fc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
118733806 120719 None 0 Human Functional pEC50 = 7.5 7.5 19 3
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
CHEMBL3416055 120719 None 0 Human Functional pEC50 = 7.5 7.5 19 3
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
CHEMBL3546907 120719 None 0 Human Functional pEC50 = 7.5 7.5 19 3
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
58911644 91134 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 227 0 1 3 0.5 N#Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397895 91134 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 227 0 1 3 0.5 N#Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
137662193 159626 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 356 2 0 4 4.0 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CCCOCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4102342 159626 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 356 2 0 4 4.0 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CCCOCC1 10.1021/acs.jmedchem.7b00385
168280316 192972 None 0 Human Functional pEC50 = 5.5 5.5 41 2
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 192972 None 0 Human Functional pEC50 = 5.5 5.5 41 2
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 192972 None 0 Human Functional pEC50 = 5.5 5.5 41 2
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
134265590 164853 None 0 Human Functional pEC50 = 6.5 6.5 2 3
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 189 0 1 3 0.8 c1cc2c(cn1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4217846 164853 None 0 Human Functional pEC50 = 6.5 6.5 2 3
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 189 0 1 3 0.8 c1cc2c(cn1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
82045957 195718 None 1 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 221 0 1 2 2.5 Clc1ccc2c(c1)OC1(C=C2)CCNC1 10.1021/acsmedchemlett.3c00454
CHEMBL5409492 195718 None 1 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 221 0 1 2 2.5 Clc1ccc2c(c1)OC1(C=C2)CCNC1 10.1021/acsmedchemlett.3c00454
58911666 91125 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 216 0 1 2 1.0 C[C@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
CHEMBL2397886 91125 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 216 0 1 2 1.0 C[C@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
162659286 183801 None 0 Human Functional pEC50 = 7.5 7.5 12 3
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
CHEMBL4762225 183801 None 0 Human Functional pEC50 = 7.5 7.5 12 3
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
CHEMBL4803142 183801 None 0 Human Functional pEC50 = 7.5 7.5 12 3
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
45484661 201337 None 0 Human Functional pEC50 = 7.5 7.5 2 2
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 289 2 1 4 1.6 O=c1cc2c(nn1Cc1ccccc1Cl)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL584210 201337 None 0 Human Functional pEC50 = 7.5 7.5 2 2
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 289 2 1 4 1.6 O=c1cc2c(nn1Cc1ccccc1Cl)CCNCC2 10.1016/j.bmcl.2009.07.063
25070911 111734 None 0 Human Functional pEC50 = 7.5 7.5 7 2
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 324 3 1 5 1.6 c1ccc(Cc2nc3c(c(N4CCOCC4)n2)CCNCC3)cc1 10.1021/jm5003292
CHEMBL3286564 111734 None 0 Human Functional pEC50 = 7.5 7.5 7 2
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 324 3 1 5 1.6 c1ccc(Cc2nc3c(c(N4CCOCC4)n2)CCNCC3)cc1 10.1021/jm5003292
145966293 164549 None 0 Human Functional pEC50 = 7.5 7.5 14 3
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 267 0 1 3 1.6 Brc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4213971 164549 None 0 Human Functional pEC50 = 7.5 7.5 14 3
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 267 0 1 3 1.6 Brc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
11148641 91124 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 216 0 1 2 1.0 C[C@H]1CN2C(=O)c3ccccc3C[C@@H]2CN1 10.1016/j.bmcl.2013.04.061
CHEMBL2397885 91124 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 216 0 1 2 1.0 C[C@H]1CN2C(=O)c3ccccc3C[C@@H]2CN1 10.1016/j.bmcl.2013.04.061
54587668 61479 None 0 Human Functional pEC50 = 6.5 6.5 3 2
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 Cc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
CHEMBL1770378 61479 None 0 Human Functional pEC50 = 6.5 6.5 3 2
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 Cc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
70696049 74487 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 271 4 1 2 3.6 COc1ccc(-c2ccccc2F)cc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2022179 74487 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 271 4 1 2 3.6 COc1ccc(-c2ccccc2F)cc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2027919 74487 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 271 4 1 2 3.6 COc1ccc(-c2ccccc2F)cc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
44572371 12531 None 0 Human Functional pEC50 = 6.5 6.5 5 2
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 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1cccc(C#CCCCCO)c1 10.1021/jm801354e
CHEMBL1186608 12531 None 0 Human Functional pEC50 = 6.5 6.5 5 2
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 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1cccc(C#CCCCCO)c1 10.1021/jm801354e
CHEMBL472678 12531 None 0 Human Functional pEC50 = 6.5 6.5 5 2
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 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1cccc(C#CCCCCO)c1 10.1021/jm801354e
11222829 91145 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 270 0 1 2 1.7 O=C1c2cccc(C(F)(F)F)c2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397906 91145 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 270 0 1 2 1.7 O=C1c2cccc(C(F)(F)F)c2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
137654351 159107 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 350 3 1 5 2.6 Cc1nn(-c2cccc3ccccc23)nc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4096587 159107 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 350 3 1 5 2.6 Cc1nn(-c2cccc3ccccc23)nc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
45484734 200190 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 179 0 1 4 -0.5 Cn1nc2c(cc1=O)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL571512 200190 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 179 0 1 4 -0.5 Cn1nc2c(cc1=O)CCNCC2 10.1016/j.bmcl.2009.07.063
172446803 195136 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.4 NC1CCC2(C=Cc3ccc(Cl)cc3O2)CC1 10.1021/acsmedchemlett.3c00454
CHEMBL5397301 195136 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.4 NC1CCC2(C=Cc3ccc(Cl)cc3O2)CC1 10.1021/acsmedchemlett.3c00454
168295067 193131 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 346 2 2 2 4.7 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(F)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5206340 193131 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 346 2 2 2 4.7 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(F)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222815 193131 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 346 2 2 2 4.7 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(F)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
168295067 193131 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 346 2 2 2 4.7 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(F)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5206340 193131 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 346 2 2 2 4.7 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(F)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222815 193131 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 346 2 2 2 4.7 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(F)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
11701315 201745 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 217 0 2 3 0.5 Cc1ccc2c(c1)N1CCNCC1NC2=O 10.1016/j.bmcl.2009.12.014
CHEMBL590331 201745 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 217 0 2 3 0.5 Cc1ccc2c(c1)N1CCNCC1NC2=O 10.1016/j.bmcl.2009.12.014
24773979 130237 None 20 Human Functional pEC50 = 6.5 6.5 4 3
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 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1016/j.bmcl.2004.12.080
CHEMBL367796 130237 None 20 Human Functional pEC50 = 6.5 6.5 4 3
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 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1016/j.bmcl.2004.12.080
44572694 187364 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 189 4 1 1 2.8 CC(C)NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
CHEMBL492696 187364 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 189 4 1 1 2.8 CC(C)NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
70689811 74500 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 267 4 1 2 3.7 COc1ccc(-c2ccccc2C)cc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2023356 74500 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 267 4 1 2 3.7 COc1ccc(-c2ccccc2C)cc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2027981 74500 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 267 4 1 2 3.7 COc1ccc(-c2ccccc2C)cc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
16115515 137683 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 290 0 1 2 2.5 O=C1c2c(C(F)(F)F)ccc(Cl)c2[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL375575 137683 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 290 0 1 2 2.5 O=C1c2c(C(F)(F)F)ccc(Cl)c2[C@@H]2CNCCN12 10.1021/jm0612968
44572180 12566 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 175 2 1 1 2.4 Cc1ccc([C@H]2C[C@@H]2CN)cc1C 10.1021/jm801354e
CHEMBL1186737 12566 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 175 2 1 1 2.4 Cc1ccc([C@H]2C[C@@H]2CN)cc1C 10.1021/jm801354e
CHEMBL475643 12566 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 175 2 1 1 2.4 Cc1ccc([C@H]2C[C@@H]2CN)cc1C 10.1021/jm801354e
22292784 64615 None 16 Human Functional pEC50 = 7.5 7.5 5 3
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 CC1CNCCc2cc(Cl)ccc21 10.1016/j.bmcl.2004.12.080
CHEMBL181672 64615 None 16 Human Functional pEC50 = 7.5 7.5 5 3
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 CC1CNCCc2cc(Cl)ccc21 10.1016/j.bmcl.2004.12.080
18545468 74007 None 41 Human Functional pEC50 = 5.5 5.5 - 1
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 237 1 1 1 2.8 Brc1ccc(C2=CCNCC2)cc1 10.1016/j.bmcl.2012.01.122
CHEMBL2011569 74007 None 41 Human Functional pEC50 = 5.5 5.5 - 1
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 237 1 1 1 2.8 Brc1ccc(C2=CCNCC2)cc1 10.1016/j.bmcl.2012.01.122
CHEMBL2021636 74007 None 41 Human Functional pEC50 = 5.5 5.5 - 1
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 237 1 1 1 2.8 Brc1ccc(C2=CCNCC2)cc1 10.1016/j.bmcl.2012.01.122
154706030 176650 None 1 Human Functional pEC50 = 5.5 5.5 -35 2
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 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4580817 176650 None 1 Human Functional pEC50 = 5.5 5.5 -35 2
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 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597188 176650 None 1 Human Functional pEC50 = 5.5 5.5 -35 2
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 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
168294162 193120 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5208129 193120 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222770 193120 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
168294162 193120 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5208129 193120 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222770 193120 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
24826786 91120 None 0 Human Functional pEC50 = 7.4 7.4 19 2
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 202 0 1 2 0.7 O=C1c2ccccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397881 91120 None 0 Human Functional pEC50 = 7.4 7.4 19 2
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 202 0 1 2 0.7 O=C1c2ccccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
122442266 138430 None 0 Human Functional pEC50 = 7.4 7.4 51 2
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=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769499 138430 None 0 Human Functional pEC50 = 7.4 7.4 51 2
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=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771379 138430 None 0 Human Functional pEC50 = 7.4 7.4 51 2
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=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
145 140 None 16 Human Functional pEC50 = 7.4 7.4 -33 12
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
1832 140 None 16 Human Functional pEC50 = 7.4 7.4 -33 12
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
CHEMBL7257 140 None 16 Human Functional pEC50 = 7.4 7.4 -33 12
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
DB14010 140 None 16 Human Functional pEC50 = 7.4 7.4 -33 12
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
122442266 138430 None 0 Human Functional pEC50 = 7.4 7.4 51 2
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=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769499 138430 None 0 Human Functional pEC50 = 7.4 7.4 51 2
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=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771379 138430 None 0 Human Functional pEC50 = 7.4 7.4 51 2
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=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
45485727 200236 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 348 5 1 6 1.8 C[C@@H](Cn1nc(N2CCNCC2)ccc1=O)Oc1ccccc1Cl 10.1016/j.bmcl.2009.07.136
CHEMBL571826 200236 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 348 5 1 6 1.8 C[C@@H](Cn1nc(N2CCNCC2)ccc1=O)Oc1ccccc1Cl 10.1016/j.bmcl.2009.07.136
45484927 199760 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 352 4 1 6 1.6 Cn1c(COc2cc(F)ccc2Cl)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
CHEMBL568741 199760 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 352 4 1 6 1.6 Cn1c(COc2cc(F)ccc2Cl)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
53320653 56816 None 0 Human Functional pEC50 = 6.4 6.4 2 2
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 245 2 1 5 0.9 CCN(C)c1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
CHEMBL1643673 56816 None 0 Human Functional pEC50 = 6.4 6.4 2 2
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 245 2 1 5 0.9 CCN(C)c1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
11187156 136441 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 312 3 1 2 3.1 CCCCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL373483 136441 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 312 3 1 2 3.1 CCCCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
118733792 120736 None 0 Human Functional pEC50 = 6.4 6.4 12 2
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 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416048 120736 None 0 Human Functional pEC50 = 6.4 6.4 12 2
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 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546974 120736 None 0 Human Functional pEC50 = 6.4 6.4 12 2
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 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
44573228 187298 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 480 6 1 6 3.3 COc1cc(S(=O)(=O)N2CCC(Oc3ccccc3Cl)CC2)c(OC)c2c1CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492303 187298 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 480 6 1 6 3.3 COc1cc(S(=O)(=O)N2CCC(Oc3ccccc3Cl)CC2)c(OC)c2c1CCNCC2 10.1016/j.bmcl.2009.02.071
137658246 159718 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 1 3 3.8 Cc1cn(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4103426 159718 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 1 3 3.8 Cc1cn(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
11737032 85050 None 0 Human Functional pEC50 = 7.4 7.4 13 3
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 222 0 1 2 1.4 O=C1c2c(Cl)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL223896 85050 None 0 Human Functional pEC50 = 7.4 7.4 13 3
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 222 0 1 2 1.4 O=C1c2c(Cl)cccc2C2CNCCN12 10.1021/jm0612968
53321865 56864 None 0 Human Functional pEC50 = 7.4 7.4 19 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)nc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643855 56864 None 0 Human Functional pEC50 = 7.4 7.4 19 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)nc1 10.1016/j.bmcl.2010.11.089
82045806 196920 None 1 Human Functional pEC50 = 5.4 5.4 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 231 1 1 3 2.2 COc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5434839 196920 None 1 Human Functional pEC50 = 5.4 5.4 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 231 1 1 3 2.2 COc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
168272608 192902 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177484 192902 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221391 192902 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
46884100 8019 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 314 5 2 3 3.0 O=C(NCc1ccc(Oc2cccc(F)c2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1090757 8019 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 314 5 2 3 3.0 O=C(NCc1ccc(Oc2cccc(F)c2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
172444062 195485 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 1 3 2.0 Cn1nc(C2=CCCNC2)c2ccccc21 10.1021/acsmedchemlett.3c00566
CHEMBL5404610 195485 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 1 3 2.0 Cn1nc(C2=CCCNC2)c2ccccc21 10.1021/acsmedchemlett.3c00566
137635711 156156 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 387 5 0 4 5.0 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)CCc1cccnc1 10.1021/acs.jmedchem.7b00385
CHEMBL4062681 156156 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 387 5 0 4 5.0 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)CCc1cccnc1 10.1021/acs.jmedchem.7b00385
172444062 195485 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 1 3 2.0 Cn1nc(C2=CCCNC2)c2ccccc21 10.1021/acsmedchemlett.3c00566
CHEMBL5404610 195485 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 1 3 2.0 Cn1nc(C2=CCCNC2)c2ccccc21 10.1021/acsmedchemlett.3c00566
168268703 192885 None 0 Human Functional pEC50 = 7.4 7.4 3 2
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 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5170024 192885 None 0 Human Functional pEC50 = 7.4 7.4 3 2
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 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221265 192885 None 0 Human Functional pEC50 = 7.4 7.4 3 2
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 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
54585652 61473 None 21 Human Functional pEC50 = 6.4 6.4 - 1
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 211 1 1 3 1.8 c1ccc(-c2ncc3c(n2)CNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770368 61473 None 21 Human Functional pEC50 = 6.4 6.4 - 1
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 211 1 1 3 1.8 c1ccc(-c2ncc3c(n2)CNCC3)cc1 10.1016/j.bmcl.2010.11.120
168272608 192902 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177484 192902 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221391 192902 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
70689809 74499 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 253 4 1 2 3.4 COc1ccc(-c2ccccc2)cc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2023355 74499 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 253 4 1 2 3.4 COc1ccc(-c2ccccc2)cc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2027980 74499 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 253 4 1 2 3.4 COc1ccc(-c2ccccc2)cc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
137632042 156409 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 350 3 1 4 3.6 Cc1oc(-c2cccc3ccccc23)nc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4065606 156409 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 350 3 1 4 3.6 Cc1oc(-c2cccc3ccccc23)nc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
137639705 156843 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 302 3 0 4 4.1 CCn1nc(-c2cccc3ccccc23)cc1-c1cncn1C 10.1021/acs.jmedchem.7b00385
CHEMBL4070587 156843 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 302 3 0 4 4.1 CCn1nc(-c2cccc3ccccc23)cc1-c1cncn1C 10.1021/acs.jmedchem.7b00385
122442281 138439 None 0 Human Functional pEC50 = 6.4 6.4 5 2
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(Cl)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3770058 138439 None 0 Human Functional pEC50 = 6.4 6.4 5 2
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(Cl)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3771388 138439 None 0 Human Functional pEC50 = 6.4 6.4 5 2
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(Cl)c1F 10.1021/acs.jmedchem.5b01153
85542158 195546 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
122442281 138439 None 0 Human Functional pEC50 = 6.4 6.4 5 2
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(Cl)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3770058 138439 None 0 Human Functional pEC50 = 6.4 6.4 5 2
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(Cl)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3771388 138439 None 0 Human Functional pEC50 = 6.4 6.4 5 2
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(Cl)c1F 10.1021/acs.jmedchem.5b01153
44431705 145214 None 0 Rat Functional pEC50 = 7.4 7.4 -6 2
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 313 2 2 4 1.7 C[C@@H](N)[C@H](O)c1c2c(c(Br)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
CHEMBL391196 145214 None 0 Rat Functional pEC50 = 7.4 7.4 -6 2
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 313 2 2 4 1.7 C[C@@H](N)[C@H](O)c1c2c(c(Br)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
168268703 192885 None 0 Human Functional pEC50 = 7.4 7.4 3 2
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 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5170024 192885 None 0 Human Functional pEC50 = 7.4 7.4 3 2
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 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221265 192885 None 0 Human Functional pEC50 = 7.4 7.4 3 2
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 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
25070909 111732 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 268 3 2 4 1.8 CNc1nc(Cc2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL3286561 111732 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 268 3 2 4 1.8 CNc1nc(Cc2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
24773814 94912 None 1 Human Functional pEC50 = 7.4 7.4 6 3
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 209 1 1 1 3.0 CC[C@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL253809 94912 None 1 Human Functional pEC50 = 7.4 7.4 6 3
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 209 1 1 1 3.0 CC[C@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
132820212 146880 None 0 Human Functional pEC50 = 7.4 7.4 3 2
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 266 1 1 3 2.5 COc1cc2c(cc1Cl)N1CCCNC[C@H]1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3924644 146880 None 0 Human Functional pEC50 = 7.4 7.4 3 2
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 266 1 1 3 2.5 COc1cc2c(cc1Cl)N1CCCNC[C@H]1CC2 10.1016/j.bmcl.2016.11.016
85542158 195546 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
10329912 62571 None 7 Human Functional pEC50 = 6.4 6.4 3 2
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 179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21 10.1021/jm0709034
CHEMBL178252 62571 None 7 Human Functional pEC50 = 6.4 6.4 3 2
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 179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21 10.1021/jm0709034
18986247 106253 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
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 226 2 1 2 2.8 CC(N)Cn1ccc2cc(Cl)c(F)cc21 10.1021/jm970030l
CHEMBL313856 106253 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
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 226 2 1 2 2.8 CC(N)Cn1ccc2cc(Cl)c(F)cc21 10.1021/jm970030l
10586264 161884 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
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 242 3 1 3 2.4 COc1ccc2c(c1)-c1c(ccn1CC(C)N)C2 10.1021/jm970030l
CHEMBL414163 161884 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
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 242 3 1 3 2.4 COc1ccc2c(c1)-c1c(ccn1CC(C)N)C2 10.1021/jm970030l
168280026 192967 None 0 Human Functional pEC50 = 5.4 5.4 -10 2
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 285 1 2 2 3.1 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccnc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5188655 192967 None 0 Human Functional pEC50 = 5.4 5.4 -10 2
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 285 1 2 2 3.1 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccnc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5221857 192967 None 0 Human Functional pEC50 = 5.4 5.4 -10 2
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 285 1 2 2 3.1 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccnc1F 10.1021/acsmedchemlett.1c00694
172446803 195136 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.4 NC1CCC2(C=Cc3ccc(Cl)cc3O2)CC1 10.1021/acsmedchemlett.3c00454
CHEMBL5397301 195136 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.4 NC1CCC2(C=Cc3ccc(Cl)cc3O2)CC1 10.1021/acsmedchemlett.3c00454
82045806 196920 None 1 Human Functional pEC50 = 5.4 5.4 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 231 1 1 3 2.2 COc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5434839 196920 None 1 Human Functional pEC50 = 5.4 5.4 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 231 1 1 3 2.2 COc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
137644936 161315 None 0 Human Functional pEC50 = 6.4 6.4 1 3
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 5 1 2 2.7 COc1ccc(F)cc1C1CC1CNC1CC1 10.1021/acs.jmedchem.7b00584
CHEMBL4090984 161315 None 0 Human Functional pEC50 = 6.4 6.4 1 3
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 5 1 2 2.7 COc1ccc(F)cc1C1CC1CNC1CC1 10.1021/acs.jmedchem.7b00584
CHEMBL4117952 161315 None 0 Human Functional pEC50 = 6.4 6.4 1 3
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 5 1 2 2.7 COc1ccc(F)cc1C1CC1CNC1CC1 10.1021/acs.jmedchem.7b00584
9838040 85336 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced calcium mobilization by cell based assayAgonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced calcium mobilization by cell based assay
ChEMBL 258 4 1 3 2.9 CCOc1ccc2c(c1)c(C[C@H](C)N)c1n2CCC1 10.1007/s00044-011-9615-3
CHEMBL2260565 85336 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced calcium mobilization by cell based assayAgonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced calcium mobilization by cell based assay
ChEMBL 258 4 1 3 2.9 CCOc1ccc2c(c1)c(C[C@H](C)N)c1n2CCC1 10.1007/s00044-011-9615-3
24826869 91136 None 0 Human Functional pEC50 = 8.4 8.4 7 3
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 230 1 1 2 1.2 CCc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397897 91136 None 0 Human Functional pEC50 = 8.4 8.4 7 3
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 230 1 1 2 1.2 CCc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
9991444 62652 None 1 Human Functional pEC50 = 8.4 8.4 4 3
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 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178366 62652 None 1 Human Functional pEC50 = 8.4 8.4 4 3
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 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
10015414 63505 None 0 Human Functional pEC50 = 8.4 8.4 10 3
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 259 1 1 2 3.0 COc1cc2c(cc1C(F)(F)F)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL179915 63505 None 0 Human Functional pEC50 = 8.4 8.4 10 3
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 259 1 1 2 3.0 COc1cc2c(cc1C(F)(F)F)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
92042919 120731 None 0 Human Functional pEC50 = 8.4 8.4 89 2
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 221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416063 120731 None 0 Human Functional pEC50 = 8.4 8.4 89 2
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 221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546958 120731 None 0 Human Functional pEC50 = 8.4 8.4 89 2
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 221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
11493484 89104 None 0 Human Functional pEC50 = 8.4 8.4 23 3
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 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337106 89104 None 0 Human Functional pEC50 = 8.4 8.4 23 3
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 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365079 89104 None 0 Human Functional pEC50 = 8.4 8.4 23 3
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 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
168272754 192903 None 0 Human Functional pEC50 = 8.4 8.4 6 2
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 282 1 3 2 3.2 Oc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5179588 192903 None 0 Human Functional pEC50 = 8.4 8.4 6 2
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 282 1 3 2 3.2 Oc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221399 192903 None 0 Human Functional pEC50 = 8.4 8.4 6 2
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 282 1 3 2 3.2 Oc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
168272754 192903 None 0 Human Functional pEC50 = 8.4 8.4 6 2
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 282 1 3 2 3.2 Oc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5179588 192903 None 0 Human Functional pEC50 = 8.4 8.4 6 2
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 282 1 3 2 3.2 Oc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221399 192903 None 0 Human Functional pEC50 = 8.4 8.4 6 2
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 282 1 3 2 3.2 Oc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
135520431 72634 None 4 Rat Functional pEC50 = 8.4 8.4 1 2
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 177 2 2 4 0.7 NCCn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL199385 72634 None 4 Rat Functional pEC50 = 8.4 8.4 1 2
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 177 2 2 4 0.7 NCCn1ncc2ccc(O)cc21 10.1021/jm050663x
44431689 87283 None 0 Rat Functional pEC50 = 8.4 8.4 13 2
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 383 7 1 6 2.6 C[C@@H](N)Cc1c2c(c(COCC(=O)Oc3ccccc3)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
CHEMBL232995 87283 None 0 Rat Functional pEC50 = 8.4 8.4 13 2
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 383 7 1 6 2.6 C[C@@H](N)Cc1c2c(c(COCC(=O)Oc3ccccc3)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
25070582 61474 None 27 Human Functional pEC50 = 8.4 8.4 -2 9
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 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 61474 None 27 Human Functional pEC50 = 8.4 8.4 -2 9
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 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
25070582 61474 None 27 Human Functional pEC50 = 8.4 8.4 -2 9
Agonist activity at human 5HT2C receptor highly expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor highly expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 61474 None 27 Human Functional pEC50 = 8.4 8.4 -2 9
Agonist activity at human 5HT2C receptor highly expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor highly expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
9859257 207581 None 0 Human Functional pEC50 = 8.4 8.4 -1 3
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 218 2 1 3 1.3 C[C@H](N)CN1CCc2ccc3c(c21)CCO3 10.1016/j.bmcl.2003.05.001
CHEMBL77880 207581 None 0 Human Functional pEC50 = 8.4 8.4 -1 3
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 218 2 1 3 1.3 C[C@H](N)CN1CCc2ccc3c(c21)CCO3 10.1016/j.bmcl.2003.05.001
166 3359 None 19 Human Functional pEC50 = 8.3 8.3 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm301656h
3045227 3359 None 19 Human Functional pEC50 = 8.3 8.3 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm301656h
CHEMBL76781 3359 None 19 Human Functional pEC50 = 8.3 8.3 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm301656h
11446529 78359 None 2 Human Functional pEC50 = 8.3 8.3 2 3
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 165 2 1 1 1.8 NC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL2094028 78359 None 2 Human Functional pEC50 = 8.3 8.3 2 3
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 165 2 1 1 1.8 NC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL2109749 78359 None 2 Human Functional pEC50 = 8.3 8.3 2 3
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 165 2 1 1 1.8 NC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
166 3359 None 19 Human Functional pEC50 = 8.3 8.3 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm301656h
3045227 3359 None 19 Human Functional pEC50 = 8.3 8.3 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm301656h
CHEMBL76781 3359 None 19 Human Functional pEC50 = 8.3 8.3 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm301656h
11446529 78359 None 2 Human Functional pEC50 = 8.3 8.3 2 3
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 165 2 1 1 1.8 NC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL2094028 78359 None 2 Human Functional pEC50 = 8.3 8.3 2 3
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 165 2 1 1 1.8 NC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL2109749 78359 None 2 Human Functional pEC50 = 8.3 8.3 2 3
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 165 2 1 1 1.8 NC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
11658860 2344 None 24 Human Functional pEC50 = 8.3 8.3 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.ejmech.2019.111626
2941 2344 None 24 Human Functional pEC50 = 8.3 8.3 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.ejmech.2019.111626
4374 2344 None 24 Human Functional pEC50 = 8.3 8.3 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.ejmech.2019.111626
CHEMBL360328 2344 None 24 Human Functional pEC50 = 8.3 8.3 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.ejmech.2019.111626
DB04871 2344 None 24 Human Functional pEC50 = 8.3 8.3 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.ejmech.2019.111626
11658860 2344 None 24 Human Functional pEC50 = 8.3 8.3 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.ejmech.2019.111626
2941 2344 None 24 Human Functional pEC50 = 8.3 8.3 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.ejmech.2019.111626
4374 2344 None 24 Human Functional pEC50 = 8.3 8.3 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.ejmech.2019.111626
CHEMBL360328 2344 None 24 Human Functional pEC50 = 8.3 8.3 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.ejmech.2019.111626
DB04871 2344 None 24 Human Functional pEC50 = 8.3 8.3 1 11
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 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.ejmech.2019.111626
44572802 12448 None 1 Human Functional pEC50 = 8.3 8.3 13 3
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 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL1186019 12448 None 1 Human Functional pEC50 = 8.3 8.3 13 3
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 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL445747 12448 None 1 Human Functional pEC50 = 8.3 8.3 13 3
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 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
135509961 136216 None 1 Rat Functional pEC50 = 8.3 8.3 1 2
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 225 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(Cl)c21 10.1021/jm050663x
CHEMBL373245 136216 None 1 Rat Functional pEC50 = 8.3 8.3 1 2
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 225 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(Cl)c21 10.1021/jm050663x
46884138 8445 None 0 Human Functional pEC50 = 8.3 8.3 100 3
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 364 7 2 4 3.2 COc1cc(OCC2CCCCC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1093699 8445 None 0 Human Functional pEC50 = 8.3 8.3 100 3
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 364 7 2 4 3.2 COc1cc(OCC2CCCCC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
44316027 207980 None 0 Human Functional pEC50 = 7.4 7.4 1 3
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 236 4 1 3 2.5 CCSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
CHEMBL80862 207980 None 0 Human Functional pEC50 = 7.4 7.4 1 3
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 236 4 1 3 2.5 CCSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
146025685 183765 None 0 Human Functional pEC50 = 7.4 7.4 19 2
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 251 5 1 3 2.0 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4752976 183765 None 0 Human Functional pEC50 = 7.4 7.4 19 2
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 251 5 1 3 2.0 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802794 183765 None 0 Human Functional pEC50 = 7.4 7.4 19 2
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 251 5 1 3 2.0 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
162669436 183851 None 0 Human Functional pEC50 = 7.4 7.4 19 3
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 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4789310 183851 None 0 Human Functional pEC50 = 7.4 7.4 19 3
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 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803705 183851 None 0 Human Functional pEC50 = 7.4 7.4 19 3
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 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
2760428 202317 None 33 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 220 1 1 5 1.1 c1nc(N2CCNCC2)c2sccc2n1 10.1016/j.bmcl.2009.10.112
CHEMBL594477 202317 None 33 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 220 1 1 5 1.1 c1nc(N2CCNCC2)c2sccc2n1 10.1016/j.bmcl.2009.10.112
168280026 192967 None 0 Human Functional pEC50 = 5.4 5.4 -10 2
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 285 1 2 2 3.1 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccnc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5188655 192967 None 0 Human Functional pEC50 = 5.4 5.4 -10 2
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 285 1 2 2 3.1 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccnc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5221857 192967 None 0 Human Functional pEC50 = 5.4 5.4 -10 2
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 285 1 2 2 3.1 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccnc1F 10.1021/acsmedchemlett.1c00694
4543677 192899 None 0 Human Functional pEC50 = 6.4 6.4 1 3
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 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5179287 192899 None 0 Human Functional pEC50 = 6.4 6.4 1 3
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 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221372 192899 None 0 Human Functional pEC50 = 6.4 6.4 1 3
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 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
45485786 200280 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 362 6 1 6 2.2 CC[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2Cl)n1 10.1016/j.bmcl.2009.07.136
CHEMBL572231 200280 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 362 6 1 6 2.2 CC[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2Cl)n1 10.1016/j.bmcl.2009.07.136
137655188 161319 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O 10.1021/acs.jmedchem.7b00584
CHEMBL4094054 161319 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O 10.1021/acs.jmedchem.7b00584
CHEMBL4117988 161319 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O 10.1021/acs.jmedchem.7b00584
4543677 192899 None 0 Human Functional pEC50 = 6.4 6.4 1 3
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 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5179287 192899 None 0 Human Functional pEC50 = 6.4 6.4 1 3
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 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221372 192899 None 0 Human Functional pEC50 = 6.4 6.4 1 3
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 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
155535970 176760 None 0 Human Functional pEC50 = 5.4 5.4 -4 3
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 165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4472830 176760 None 0 Human Functional pEC50 = 5.4 5.4 -4 3
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 165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4598081 176760 None 0 Human Functional pEC50 = 5.4 5.4 -4 3
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 165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
137655188 161319 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O 10.1021/acs.jmedchem.7b00584
CHEMBL4094054 161319 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O 10.1021/acs.jmedchem.7b00584
CHEMBL4117988 161319 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O 10.1021/acs.jmedchem.7b00584
11595191 89094 None 0 Human Functional pEC50 = 7.4 7.4 6 3
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 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337488 89094 None 0 Human Functional pEC50 = 7.4 7.4 6 3
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 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2364960 89094 None 0 Human Functional pEC50 = 7.4 7.4 6 3
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 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
146025685 183765 None 0 Human Functional pEC50 = 7.4 7.4 19 2
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 251 5 1 3 2.0 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4752976 183765 None 0 Human Functional pEC50 = 7.4 7.4 19 2
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 251 5 1 3 2.0 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802794 183765 None 0 Human Functional pEC50 = 7.4 7.4 19 2
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 251 5 1 3 2.0 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
162669436 183851 None 0 Human Functional pEC50 = 7.4 7.4 19 3
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 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4789310 183851 None 0 Human Functional pEC50 = 7.4 7.4 19 3
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 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803705 183851 None 0 Human Functional pEC50 = 7.4 7.4 19 3
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 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
42601404 187336 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 372 4 1 4 2.2 CN(CC1COc2ccccc21)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492556 187336 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 372 4 1 4 2.2 CN(CC1COc2ccccc21)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
137639630 157012 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 1 3 3.7 Cn1cc(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4072337 157012 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 1 3 3.7 Cn1cc(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
44383324 120520 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 246 2 1 2 3.1 Cc1c(CCN)c2cc(F)cc3c2n1C(C)CC3 10.1016/s0960-894x(00)00141-4
CHEMBL353998 120520 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 246 2 1 2 3.1 Cc1c(CCN)c2cc(F)cc3c2n1C(C)CC3 10.1016/s0960-894x(00)00141-4
168291564 193092 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
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 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5201470 193092 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
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 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222574 193092 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
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 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
122442324 138437 None 0 Human Functional pEC50 = 7.4 7.4 12 2
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=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770174 138437 None 0 Human Functional pEC50 = 7.4 7.4 12 2
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=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771386 138437 None 0 Human Functional pEC50 = 7.4 7.4 12 2
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=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
10329912 62571 None 7 Human Functional pEC50 = 6.4 6.4 3 2
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 179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178252 62571 None 7 Human Functional pEC50 = 6.4 6.4 3 2
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 179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21 10.1016/j.bmcl.2004.12.080
155535970 176760 None 0 Human Functional pEC50 = 5.4 5.4 -4 3
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 165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4472830 176760 None 0 Human Functional pEC50 = 5.4 5.4 -4 3
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 165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4598081 176760 None 0 Human Functional pEC50 = 5.4 5.4 -4 3
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 165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
14515725 87344 None 0 Human Functional pEC50 = 6.4 6.4 1 2
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 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
CHEMBL2331807 87344 None 0 Human Functional pEC50 = 6.4 6.4 1 2
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 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
168284944 193022 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 3 2.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5192557 193022 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 3 2.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222162 193022 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 3 2.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
46230048 201746 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 217 0 2 3 0.5 Cc1cccc2c1N1CCNCC1NC2=O 10.1016/j.bmcl.2009.12.014
CHEMBL590332 201746 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 217 0 2 3 0.5 Cc1cccc2c1N1CCNCC1NC2=O 10.1016/j.bmcl.2009.12.014
11437171 83523 None 0 Human Functional pEC50 = 7.4 7.4 2 3
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 234 1 1 3 1.5 CSc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL220207 83523 None 0 Human Functional pEC50 = 7.4 7.4 2 3
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 234 1 1 3 1.5 CSc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
44573014 12525 None 0 Human Functional pEC50 = 7.4 7.4 10 3
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 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)cc1F 10.1021/jm801354e
CHEMBL1186595 12525 None 0 Human Functional pEC50 = 7.4 7.4 10 3
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 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)cc1F 10.1021/jm801354e
CHEMBL471802 12525 None 0 Human Functional pEC50 = 7.4 7.4 10 3
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 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)cc1F 10.1021/jm801354e
168291564 193092 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
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 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5201470 193092 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
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 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222574 193092 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
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 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
122442324 138437 None 0 Human Functional pEC50 = 7.4 7.4 12 2
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=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770174 138437 None 0 Human Functional pEC50 = 7.4 7.4 12 2
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=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771386 138437 None 0 Human Functional pEC50 = 7.4 7.4 12 2
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=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
14515725 87344 None 0 Human Functional pEC50 = 6.4 6.4 1 2
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 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
CHEMBL2331807 87344 None 0 Human Functional pEC50 = 6.4 6.4 1 2
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 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
168284944 193022 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 3 2.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5192557 193022 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 3 2.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222162 193022 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 3 2.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
24773900 123499 None 6 Human Functional pEC50 = 6.4 6.4 1 3
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 191 1 1 2 1.9 COc1ccc2c(c1)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL361742 123499 None 6 Human Functional pEC50 = 6.4 6.4 1 3
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 191 1 1 2 1.9 COc1ccc2c(c1)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
44412405 77810 None 0 Human Functional pEC50 = 6.4 6.4 -2 3
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 255 1 1 1 3.4 FC(F)(F)c1cccc([C@H]2CC[C@H]3CNC[C@@H]23)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209155 77810 None 0 Human Functional pEC50 = 6.4 6.4 -2 3
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 255 1 1 1 3.4 FC(F)(F)c1cccc([C@H]2CC[C@H]3CNC[C@@H]23)c1 10.1016/j.bmcl.2006.03.007
11427139 84721 None 0 Human Functional pEC50 = 7.4 7.4 38 3
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 282 1 1 2 2.4 C=Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL222566 84721 None 0 Human Functional pEC50 = 7.4 7.4 38 3
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 282 1 1 2 2.4 C=Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
11492300 89145 None 1 Human Functional pEC50 = 7.4 7.4 - 1
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 188 0 2 2 0.5 O=C1N[C@H]2CNC[C@@H]2c2ccccc21 10.1016/j.bmcl.2012.10.091
CHEMBL2337495 89145 None 1 Human Functional pEC50 = 7.4 7.4 - 1
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 188 0 2 2 0.5 O=C1N[C@H]2CNC[C@@H]2c2ccccc21 10.1016/j.bmcl.2012.10.091
CHEMBL2365471 89145 None 1 Human Functional pEC50 = 7.4 7.4 - 1
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 188 0 2 2 0.5 O=C1N[C@H]2CNC[C@@H]2c2ccccc21 10.1016/j.bmcl.2012.10.091
46230049 204002 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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=C1NC2CNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
CHEMBL605402 204002 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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=C1NC2CNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
137637165 156305 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 351 2 0 4 3.7 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCN(C)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4064423 156305 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 351 2 0 4 3.7 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCN(C)CC1 10.1021/acs.jmedchem.7b00385
5 139 None 45 Human Functional pEC50 = 7.4 7.4 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5202 139 None 45 Human Functional pEC50 = 7.4 7.4 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
CHEMBL39 139 None 45 Human Functional pEC50 = 7.4 7.4 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
DB08839 139 None 45 Human Functional pEC50 = 7.4 7.4 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
168268771 192900 None 0 Human Functional pEC50 = 7.4 7.4 4 2
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 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5174331 192900 None 0 Human Functional pEC50 = 7.4 7.4 4 2
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 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221385 192900 None 0 Human Functional pEC50 = 7.4 7.4 4 2
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 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
137655657 158874 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 316 7 1 4 3.1 COc1ccc(F)cc1C1CC1CNCc1cccnc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4094164 158874 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 316 7 1 4 3.1 COc1ccc(F)cc1C1CC1CNCc1cccnc1OC 10.1021/acs.jmedchem.7b00584
122442307 138442 None 0 Human Functional pEC50 = 6.4 6.4 1 2
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 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3770950 138442 None 0 Human Functional pEC50 = 6.4 6.4 1 2
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 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771391 138442 None 0 Human Functional pEC50 = 6.4 6.4 1 2
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 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
137655657 158874 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 316 7 1 4 3.1 COc1ccc(F)cc1C1CC1CNCc1cccnc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4094164 158874 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 316 7 1 4 3.1 COc1ccc(F)cc1C1CC1CNCc1cccnc1OC 10.1021/acs.jmedchem.7b00584
122442307 138442 None 0 Human Functional pEC50 = 6.4 6.4 1 2
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 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3770950 138442 None 0 Human Functional pEC50 = 6.4 6.4 1 2
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 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771391 138442 None 0 Human Functional pEC50 = 6.4 6.4 1 2
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 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
46884137 8444 None 0 Human Functional pEC50 = 7.4 7.4 3 2
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 352 5 2 3 3.3 C[C@H]1CC[C@@H](Oc2c(F)cc(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
CHEMBL1093698 8444 None 0 Human Functional pEC50 = 7.4 7.4 3 2
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 352 5 2 3 3.3 C[C@H]1CC[C@@H](Oc2c(F)cc(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
5 139 None 45 Human Functional pEC50 = 7.4 7.4 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5202 139 None 45 Human Functional pEC50 = 7.4 7.4 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
CHEMBL39 139 None 45 Human Functional pEC50 = 7.4 7.4 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
DB08839 139 None 45 Human Functional pEC50 = 7.4 7.4 -2 26
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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
168268771 192900 None 0 Human Functional pEC50 = 7.4 7.4 4 2
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 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5174331 192900 None 0 Human Functional pEC50 = 7.4 7.4 4 2
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 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221385 192900 None 0 Human Functional pEC50 = 7.4 7.4 4 2
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 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
168 3982 None 15 Human Functional pEC50 = 7.4 7.4 -3 5
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 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
6604042 3982 None 15 Human Functional pEC50 = 7.4 7.4 -3 5
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 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
CHEMBL309760 3982 None 15 Human Functional pEC50 = 7.4 7.4 -3 5
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 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
18735313 207392 None 1 Human Functional pEC50 = 7.4 7.4 -6 3
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 210 2 1 2 2.1 C[C@H](N)CN1CCc2ccc(Cl)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL76307 207392 None 1 Human Functional pEC50 = 7.4 7.4 -6 3
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 210 2 1 2 2.1 C[C@H](N)CN1CCc2ccc(Cl)cc21 10.1016/j.bmcl.2003.05.001
21072529 176527 None 4 Human Functional pEC50 = 5.4 5.4 -1 3
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 183 2 1 1 2.0 NCC1C(c2ccccc2)C1(F)F 10.1016/j.ejmech.2019.111626
CHEMBL4457840 176527 None 4 Human Functional pEC50 = 5.4 5.4 -1 3
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 183 2 1 1 2.0 NCC1C(c2ccccc2)C1(F)F 10.1016/j.ejmech.2019.111626
CHEMBL4596163 176527 None 4 Human Functional pEC50 = 5.4 5.4 -1 3
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 183 2 1 1 2.0 NCC1C(c2ccccc2)C1(F)F 10.1016/j.ejmech.2019.111626
162668416 183846 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 285 6 1 3 3.8 CCc1cc2c([C@@H]3C[C@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4787862 183846 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 285 6 1 3 3.8 CCc1cc2c([C@@H]3C[C@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803644 183846 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 285 6 1 3 3.8 CCc1cc2c([C@@H]3C[C@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
168268736 192898 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177718 192898 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221369 192898 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
162668416 183846 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 285 6 1 3 3.8 CCc1cc2c([C@@H]3C[C@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4787862 183846 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 285 6 1 3 3.8 CCc1cc2c([C@@H]3C[C@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803644 183846 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 285 6 1 3 3.8 CCc1cc2c([C@@H]3C[C@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
168268736 192898 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177718 192898 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221369 192898 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
4995534 192961 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 366 1 2 2 4.9 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5188386 192961 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 366 1 2 2 4.9 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221773 192961 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 366 1 2 2 4.9 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)s1 10.1021/acsmedchemlett.1c00694
21072529 176527 None 4 Human Functional pEC50 = 5.4 5.4 -1 3
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 183 2 1 1 2.0 NCC1C(c2ccccc2)C1(F)F 10.1016/j.ejmech.2019.111626
CHEMBL4457840 176527 None 4 Human Functional pEC50 = 5.4 5.4 -1 3
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 183 2 1 1 2.0 NCC1C(c2ccccc2)C1(F)F 10.1016/j.ejmech.2019.111626
CHEMBL4596163 176527 None 4 Human Functional pEC50 = 5.4 5.4 -1 3
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 183 2 1 1 2.0 NCC1C(c2ccccc2)C1(F)F 10.1016/j.ejmech.2019.111626
4995534 192961 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 366 1 2 2 4.9 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5188386 192961 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 366 1 2 2 4.9 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221773 192961 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 366 1 2 2 4.9 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)s1 10.1021/acsmedchemlett.1c00694
11615459 201704 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 217 0 2 3 0.5 Cc1cccc2c1C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590078 201704 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 217 0 2 3 0.5 Cc1cccc2c1C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
12986496 205165 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 257 0 2 3 2.2 Clc1cc2c(cc1Cl)N1CCNC[C@H]1CN2 10.1016/s0960-894x(00)00400-5
CHEMBL61695 205165 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 257 0 2 3 2.2 Clc1cc2c(cc1Cl)N1CCNC[C@H]1CN2 10.1016/s0960-894x(00)00400-5
137651715 157483 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 304 3 0 6 2.9 CCn1nc(-c2cccc3ccccc23)cc1-c1nnnn1C 10.1021/acs.jmedchem.7b00385
CHEMBL4078339 157483 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 304 3 0 6 2.9 CCn1nc(-c2cccc3ccccc23)cc1-c1nnnn1C 10.1021/acs.jmedchem.7b00385
137658074 159659 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 301 3 0 5 3.6 CCn1nc(-c2cccc3ncccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
CHEMBL4102653 159659 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 301 3 0 5 3.6 CCn1nc(-c2cccc3ncccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
53324629 56815 None 0 Human Functional pEC50 = 5.3 5.3 -7 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 271 1 1 5 1.4 c1cc2nc3c(c(N4CCCCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
CHEMBL1643672 56815 None 0 Human Functional pEC50 = 5.3 5.3 -7 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 271 1 1 5 1.4 c1cc2nc3c(c(N4CCCCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
16115511 84871 None 0 Human Functional pEC50 = 7.3 7.3 6 3
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 250 1 1 2 2.0 CCc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL223466 84871 None 0 Human Functional pEC50 = 7.3 7.3 6 3
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 250 1 1 2 2.0 CCc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
45484909 200969 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 332 4 1 6 1.2 Cc1ccc(F)cc1OCc1nc(N2CCNCC2)cc(=O)n1C 10.1016/j.bmcl.2009.07.133
CHEMBL577832 200969 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 332 4 1 6 1.2 Cc1ccc(F)cc1OCc1nc(N2CCNCC2)cc(=O)n1C 10.1016/j.bmcl.2009.07.133
44573154 187304 None 0 Human Functional pEC50 = 7.3 7.3 17 2
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 350 4 2 3 2.5 O=S(=O)(NCc1ccccc1Cl)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492349 187304 None 0 Human Functional pEC50 = 7.3 7.3 17 2
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 350 4 2 3 2.5 O=S(=O)(NCc1ccccc1Cl)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
168291896 193094 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
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 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201903 193094 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
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 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222595 193094 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
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 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
137635932 156077 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 308 2 0 4 2.9 O=C(c1csc(-c2ccccc2Cl)n1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4061625 156077 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 308 2 0 4 2.9 O=C(c1csc(-c2ccccc2Cl)n1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
168277801 192953 None 0 Human Functional pEC50 = 6.3 6.3 1 2
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 294 3 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5176879 192953 None 0 Human Functional pEC50 = 6.3 6.3 1 2
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 294 3 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221724 192953 None 0 Human Functional pEC50 = 6.3 6.3 1 2
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 294 3 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
168277801 192953 None 0 Human Functional pEC50 = 6.3 6.3 1 2
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 294 3 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5176879 192953 None 0 Human Functional pEC50 = 6.3 6.3 1 2
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 294 3 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221724 192953 None 0 Human Functional pEC50 = 6.3 6.3 1 2
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 294 3 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
168291896 193094 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
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 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201903 193094 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
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 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222595 193094 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
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 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
44626357 200008 None 0 Human Functional pEC50 = 7.3 7.3 1 2
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 382 5 1 6 2.1 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2C(F)(F)F)n1 10.1016/j.bmcl.2009.07.133
CHEMBL570274 200008 None 0 Human Functional pEC50 = 7.3 7.3 1 2
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 382 5 1 6 2.1 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2C(F)(F)F)n1 10.1016/j.bmcl.2009.07.133
44573156 187403 None 0 Human Functional pEC50 = 7.3 7.3 2 2
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 254 2 1 3 0.6 CN(C)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492949 187403 None 0 Human Functional pEC50 = 7.3 7.3 2 2
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 254 2 1 3 0.6 CN(C)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
45485781 199847 None 0 Human Functional pEC50 = 7.3 7.3 23 2
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 368 5 1 6 1.8 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1C(F)(F)F 10.1016/j.bmcl.2009.07.136
CHEMBL569342 199847 None 0 Human Functional pEC50 = 7.3 7.3 23 2
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 368 5 1 6 1.8 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1C(F)(F)F 10.1016/j.bmcl.2009.07.136
137646716 157870 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 365 3 1 3 4.7 Cc1sc(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4082829 157870 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 365 3 1 3 4.7 Cc1sc(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
137655705 159032 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 352 2 1 4 3.9 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCC(O)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4095818 159032 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 352 2 1 4 3.9 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCC(O)CC1 10.1021/acs.jmedchem.7b00385
172448310 195732 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.1 CC1CNCCC12C=Cc1ccc(Cl)cc1O2 10.1021/acsmedchemlett.3c00454
CHEMBL5409777 195732 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.1 CC1CNCCC12C=Cc1ccc(Cl)cc1O2 10.1021/acsmedchemlett.3c00454
11312820 136421 None 1 Human Functional pEC50 = 6.3 6.3 - 1
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 270 0 1 2 2.2 C[C@H]1CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
CHEMBL373402 136421 None 1 Human Functional pEC50 = 6.3 6.3 - 1
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 270 0 1 2 2.2 C[C@H]1CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
168295538 193148 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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 2 3 2 3.3 Oc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5207179 193148 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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 2 3 2 3.3 Oc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222923 193148 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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 2 3 2 3.3 Oc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
58911668 91144 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 230 1 1 2 1.2 CCc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397905 91144 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 230 1 1 2 1.2 CCc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
45484686 200152 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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(nn1Cc1ccc(OC(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL571288 200152 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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(nn1Cc1ccc(OC(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
122442275 138448 None 0 Human Functional pEC50 = 7.3 7.3 9 3
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770862 138448 None 0 Human Functional pEC50 = 7.3 7.3 9 3
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771397 138448 None 0 Human Functional pEC50 = 7.3 7.3 9 3
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
16115388 137453 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 284 1 1 2 2.6 CC[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
CHEMBL375302 137453 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 284 1 1 2 2.6 CC[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
54584720 61475 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression 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 61475 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression 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
168295538 193148 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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 2 3 2 3.3 Oc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5207179 193148 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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 2 3 2 3.3 Oc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222923 193148 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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 2 3 2 3.3 Oc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
45484879 199277 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 368 4 1 6 1.8 Cn1c(COc2cccc(C(F)(F)F)c2)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
CHEMBL565736 199277 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 368 4 1 6 1.8 Cn1c(COc2cccc(C(F)(F)F)c2)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
82045795 195992 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 279 0 1 2 3.0 Brc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5414815 195992 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 279 0 1 2 3.0 Brc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
11483068 84846 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 250 1 1 2 2.0 CCc1cc(Cl)c2c(c1)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL223440 84846 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 250 1 1 2 2.0 CCc1cc(Cl)c2c(c1)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
44572757 12653 None 0 Human Functional pEC50 = 7.3 7.3 7 2
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 2.8 NC[C@H]1C[C@@H]1c1ccccc1C(F)(F)F 10.1021/jm801354e
CHEMBL1187186 12653 None 0 Human Functional pEC50 = 7.3 7.3 7 2
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 2.8 NC[C@H]1C[C@@H]1c1ccccc1C(F)(F)F 10.1021/jm801354e
CHEMBL492917 12653 None 0 Human Functional pEC50 = 7.3 7.3 7 2
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 2.8 NC[C@H]1C[C@@H]1c1ccccc1C(F)(F)F 10.1021/jm801354e
122442275 138448 None 0 Human Functional pEC50 = 7.3 7.3 9 3
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770862 138448 None 0 Human Functional pEC50 = 7.3 7.3 9 3
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771397 138448 None 0 Human Functional pEC50 = 7.3 7.3 9 3
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 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
12986495 100650 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 257 0 2 3 2.2 Clc1cc2c(cc1Cl)N1CCNC[C@@H]1CN2 10.1016/s0960-894x(00)00400-5
CHEMBL291794 100650 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 257 0 2 3 2.2 Clc1cc2c(cc1Cl)N1CCNC[C@@H]1CN2 10.1016/s0960-894x(00)00400-5
45484888 200273 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 334 4 1 6 1.4 Cn1c(COc2cccc(Cl)c2)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
CHEMBL572183 200273 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 334 4 1 6 1.4 Cn1c(COc2cccc(Cl)c2)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
45484727 199626 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 227 2 1 3 1.6 c1ccc(Cn2cc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2009.07.063
CHEMBL568005 199626 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 227 2 1 3 1.6 c1ccc(Cn2cc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2009.07.063
45484727 199626 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 227 2 1 3 1.6 c1ccc(Cn2cc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2016.06.060
CHEMBL568005 199626 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 227 2 1 3 1.6 c1ccc(Cn2cc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2016.06.060
16115513 136489 None 0 Human Functional pEC50 = 8.3 8.3 43 2
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 COc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL373531 136489 None 0 Human Functional pEC50 = 8.3 8.3 43 2
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 COc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
24826790 91128 None 0 Human Functional pEC50 = 8.3 8.3 12 2
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 216 0 1 2 1.0 Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397889 91128 None 0 Human Functional pEC50 = 8.3 8.3 12 2
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 216 0 1 2 1.0 Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
53324630 56819 None 0 Human Functional pEC50 = 8.3 8.3 18 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1ccccc1OC1CN(c2c3c(nc4ccnn24)CCNCC3)C1 10.1016/j.bmcl.2010.11.089
CHEMBL1643676 56819 None 0 Human Functional pEC50 = 8.3 8.3 18 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1ccccc1OC1CN(c2c3c(nc4ccnn24)CCNCC3)C1 10.1016/j.bmcl.2010.11.089
137647635 157722 None 0 Human Functional pEC50 = 8.3 8.3 9 3
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 316 3 1 6 3.2 CCn1nc(-c2cccc3cccnc23)cc1-c1ccc(N)nn1 10.1021/acs.jmedchem.7b00385
CHEMBL4081247 157722 None 0 Human Functional pEC50 = 8.3 8.3 9 3
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 316 3 1 6 3.2 CCn1nc(-c2cccc3cccnc23)cc1-c1ccc(N)nn1 10.1021/acs.jmedchem.7b00385
9881885 64130 None 0 Human Functional pEC50 = 8.3 8.3 15 3
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 269 1 1 2 2.7 COc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL180815 64130 None 0 Human Functional pEC50 = 8.3 8.3 15 3
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 269 1 1 2 2.7 COc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
44389646 64904 None 0 Human Functional pEC50 = 8.3 8.3 6 3
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 269 1 1 2 2.7 COc1cc2c(cc1Br)[C@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL182184 64904 None 0 Human Functional pEC50 = 8.3 8.3 6 3
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 269 1 1 2 2.7 COc1cc2c(cc1Br)[C@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
134265669 180351 None 0 Human Functional pEC50 = 8.3 8.3 10 3
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 223 0 1 3 1.5 Clc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4750216 180351 None 0 Human Functional pEC50 = 8.3 8.3 10 3
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 223 0 1 3 1.5 Clc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
134265737 182509 None 0 Human Functional pEC50 = 8.3 8.3 158 2
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 233 2 1 4 1.0 COCc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4785566 182509 None 0 Human Functional pEC50 = 8.3 8.3 158 2
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 233 2 1 4 1.0 COCc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
44572749 12441 None 0 Human Functional pEC50 = 8.3 8.3 6 3
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]1c1ccccc1Cl 10.1021/jm801354e
CHEMBL1185954 12441 None 0 Human Functional pEC50 = 8.3 8.3 6 3
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]1c1ccccc1Cl 10.1021/jm801354e
CHEMBL443128 12441 None 0 Human Functional pEC50 = 8.3 8.3 6 3
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]1c1ccccc1Cl 10.1021/jm801354e
44572657 12471 None 5 Human Functional pEC50 = 8.3 8.3 7 3
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 147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
CHEMBL1186169 12471 None 5 Human Functional pEC50 = 8.3 8.3 7 3
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 147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
CHEMBL452719 12471 None 5 Human Functional pEC50 = 8.3 8.3 7 3
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 147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
146025686 183865 None 0 Human Functional pEC50 = 8.3 8.3 21 3
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 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4790992 183865 None 0 Human Functional pEC50 = 8.3 8.3 21 3
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 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803813 183865 None 0 Human Functional pEC50 = 8.3 8.3 21 3
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 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
146025686 183865 None 0 Human Functional pEC50 = 8.3 8.3 21 3
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 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4790992 183865 None 0 Human Functional pEC50 = 8.3 8.3 21 3
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 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803813 183865 None 0 Human Functional pEC50 = 8.3 8.3 21 3
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 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
44572810 12659 None 0 Human Functional pEC50 = 8.3 8.3 3 3
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 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
CHEMBL1187196 12659 None 0 Human Functional pEC50 = 8.3 8.3 3 3
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 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
CHEMBL493130 12659 None 0 Human Functional pEC50 = 8.3 8.3 3 3
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 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
53325935 56813 None 0 Human Functional pEC50 = 8.3 8.3 17 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 243 1 1 5 0.6 c1cc2nc3c(c(N4CCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
CHEMBL1643670 56813 None 0 Human Functional pEC50 = 8.3 8.3 17 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 243 1 1 5 0.6 c1cc2nc3c(c(N4CCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
135399866 72079 None 1 Rat Functional pEC50 = 8.3 8.3 1 2
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 209 2 2 4 1.2 C[C@H](N)Cn1ncc2ccc(O)c(F)c21 10.1021/jm050663x
CHEMBL197653 72079 None 1 Rat Functional pEC50 = 8.3 8.3 1 2
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 209 2 2 4 1.2 C[C@H](N)Cn1ncc2ccc(O)c(F)c21 10.1021/jm050663x
9794638 120853 None 0 Human Functional pEC50 = 8.2 8.2 46 2
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 232 2 1 2 2.8 CC1CCc2cc(F)cc3c(CCN)cn1c23 10.1016/s0960-894x(00)00141-4
CHEMBL355474 120853 None 0 Human Functional pEC50 = 8.2 8.2 46 2
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 232 2 1 2 2.8 CC1CCc2cc(F)cc3c(CCN)cn1c23 10.1016/s0960-894x(00)00141-4
134265622 164848 None 0 Human Functional pEC50 = 8.2 8.2 81 3
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 259 1 1 3 2.4 CC(C)(C)Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4217787 164848 None 0 Human Functional pEC50 = 8.2 8.2 81 3
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 259 1 1 3 2.4 CC(C)(C)Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
44573221 193189 None 0 Human Functional pEC50 = 7.3 7.3 7 2
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 280 2 1 3 1.2 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCCC1 10.1016/j.bmcl.2009.02.071
CHEMBL522514 193189 None 0 Human Functional pEC50 = 7.3 7.3 7 2
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 280 2 1 3 1.2 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCCC1 10.1016/j.bmcl.2009.02.071
168281505 192989 None 0 Human Functional pEC50 = 7.3 7.3 4 2
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 285 1 2 3 3.1 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5188678 192989 None 0 Human Functional pEC50 = 7.3 7.3 4 2
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 285 1 2 3 3.1 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221963 192989 None 0 Human Functional pEC50 = 7.3 7.3 4 2
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 285 1 2 3 3.1 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
24773650 154787 None 2 Human Functional pEC50 = 7.3 7.3 1 3
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 225 1 1 2 2.6 COc1cc2c(cc1Cl)CCNCC2C 10.1021/jm0709034
CHEMBL399750 154787 None 2 Human Functional pEC50 = 7.3 7.3 1 3
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 225 1 1 2 2.6 COc1cc2c(cc1Cl)CCNCC2C 10.1021/jm0709034
168281505 192989 None 0 Human Functional pEC50 = 7.3 7.3 4 2
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 285 1 2 3 3.1 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5188678 192989 None 0 Human Functional pEC50 = 7.3 7.3 4 2
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 285 1 2 3 3.1 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221963 192989 None 0 Human Functional pEC50 = 7.3 7.3 4 2
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 285 1 2 3 3.1 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
498210 202442 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 248 2 1 5 0.8 COc1nc(N2CCNCC2)nc2c1CCCC2 10.1016/j.bmcl.2009.10.112
CHEMBL595196 202442 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 248 2 1 5 0.8 COc1nc(N2CCNCC2)nc2c1CCCC2 10.1016/j.bmcl.2009.10.112
137642149 158453 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 302 2 0 4 2.9 Cc1cccc(-c2nc(C(=O)N3CCOCC3)cs2)c1C 10.1021/acs.jmedchem.7b00385
CHEMBL4089670 158453 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 302 2 0 4 2.9 Cc1cccc(-c2nc(C(=O)N3CCOCC3)cs2)c1C 10.1021/acs.jmedchem.7b00385
137630488 161170 None 0 Human Functional pEC50 = 6.3 6.3 3 2
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 303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4101789 161170 None 0 Human Functional pEC50 = 6.3 6.3 3 2
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 303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4116752 161170 None 0 Human Functional pEC50 = 6.3 6.3 3 2
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 303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
19036377 210282 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
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 226 2 1 2 2.7 Cc1ccc2c(c1)-c1c(ccn1CC(C)N)C2 10.1021/jm970030l
CHEMBL96312 210282 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
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 226 2 1 2 2.7 Cc1ccc2c(c1)-c1c(ccn1CC(C)N)C2 10.1021/jm970030l
172448310 195732 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.1 CC1CNCCC12C=Cc1ccc(Cl)cc1O2 10.1021/acsmedchemlett.3c00454
CHEMBL5409777 195732 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 249 0 1 2 3.1 CC1CNCCC12C=Cc1ccc(Cl)cc1O2 10.1021/acsmedchemlett.3c00454
82045795 195992 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 279 0 1 2 3.0 Brc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5414815 195992 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 279 0 1 2 3.0 Brc1ccc2c(c1)OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
137630488 161170 None 0 Human Functional pEC50 = 6.3 6.3 3 2
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 303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4101789 161170 None 0 Human Functional pEC50 = 6.3 6.3 3 2
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 303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4116752 161170 None 0 Human Functional pEC50 = 6.3 6.3 3 2
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 303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
44412403 77827 None 0 Human Functional pEC50 = 6.3 6.3 -8 3
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 222 1 1 2 2.1 Clc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209254 77827 None 0 Human Functional pEC50 = 6.3 6.3 -8 3
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 222 1 1 2 2.1 Clc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
10624 70324 None 12 Human Functional pEC50 = 6.3 6.3 -6 3
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 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
10624.0 70324 None 12 Human Functional pEC50 = 6.3 6.3 -6 3
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 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
138543650 70324 None 12 Human Functional pEC50 = 6.3 6.3 -6 3
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 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL194378 70324 None 12 Human Functional pEC50 = 6.3 6.3 -6 3
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 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
DB11664 70324 None 12 Human Functional pEC50 = 6.3 6.3 -6 3
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 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
44573225 192731 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 386 4 1 4 2.6 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCC(Oc2ccccc2)CC1 10.1016/j.bmcl.2009.02.071
CHEMBL521644 192731 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 386 4 1 4 2.6 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCC(Oc2ccccc2)CC1 10.1016/j.bmcl.2009.02.071
122442293 138429 None 0 Human Functional pEC50 = 6.3 6.3 19 3
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 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3770599 138429 None 0 Human Functional pEC50 = 6.3 6.3 19 3
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 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3771378 138429 None 0 Human Functional pEC50 = 6.3 6.3 19 3
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 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
59312310 111731 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 269 3 1 4 1.8 COc1nc(Cc2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL3286560 111731 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 269 3 1 4 1.8 COc1nc(Cc2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
45485769 199825 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 348 5 1 6 1.7 Cc1cc(=O)n(CCOc2ccccc2Cl)nc1N1CCNCC1 10.1016/j.bmcl.2009.07.136
CHEMBL569208 199825 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 348 5 1 6 1.7 Cc1cc(=O)n(CCOc2ccccc2Cl)nc1N1CCNCC1 10.1016/j.bmcl.2009.07.136
122442293 138429 None 0 Human Functional pEC50 = 6.3 6.3 19 3
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 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3770599 138429 None 0 Human Functional pEC50 = 6.3 6.3 19 3
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 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3771378 138429 None 0 Human Functional pEC50 = 6.3 6.3 19 3
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 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
11253485 142065 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 204 0 2 3 0.5 O=C1c2c(O)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL387344 142065 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 204 0 2 3 0.5 O=C1c2c(O)cccc2C2CNCCN12 10.1021/jm0612968
118733826 120707 None 0 Human Functional pEC50 = 6.3 6.3 5 2
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 227 5 1 2 2.2 NC[C@@H]1C[C@H]1c1cc(F)ccc1OCCF 10.1021/jm5019274
CHEMBL3416066 120707 None 0 Human Functional pEC50 = 6.3 6.3 5 2
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 227 5 1 2 2.2 NC[C@@H]1C[C@H]1c1cc(F)ccc1OCCF 10.1021/jm5019274
CHEMBL3546874 120707 None 0 Human Functional pEC50 = 6.3 6.3 5 2
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 227 5 1 2 2.2 NC[C@@H]1C[C@H]1c1cc(F)ccc1OCCF 10.1021/jm5019274
44412308 166101 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CC[C@@H]3CNC[C@@H]32)n1 10.1016/j.bmcl.2006.03.007
CHEMBL425423 166101 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CC[C@@H]3CNC[C@@H]32)n1 10.1016/j.bmcl.2006.03.007
166 3359 None 19 Human Functional pEC50 = 7.3 7.3 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmc.2007.10.100
3045227 3359 None 19 Human Functional pEC50 = 7.3 7.3 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmc.2007.10.100
CHEMBL76781 3359 None 19 Human Functional pEC50 = 7.3 7.3 -2 5
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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmc.2007.10.100
137629973 161121 None 0 Human Functional pEC50 = 6.3 6.3 6 2
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 319 6 1 2 4.4 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1Cl 10.1021/acs.jmedchem.7b00584
CHEMBL4104218 161121 None 0 Human Functional pEC50 = 6.3 6.3 6 2
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 319 6 1 2 4.4 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1Cl 10.1021/acs.jmedchem.7b00584
CHEMBL4116381 161121 None 0 Human Functional pEC50 = 6.3 6.3 6 2
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 319 6 1 2 4.4 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1Cl 10.1021/acs.jmedchem.7b00584
137629588 161129 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 336 6 1 3 4.3 COc1ccc(F)cc1C1CC1CNCc1cccc2cccnc12 10.1021/acs.jmedchem.7b00584
CHEMBL4064935 161129 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 336 6 1 3 4.3 COc1ccc(F)cc1C1CC1CNCc1cccc2cccnc12 10.1021/acs.jmedchem.7b00584
CHEMBL4116446 161129 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 336 6 1 3 4.3 COc1ccc(F)cc1C1CC1CNCc1cccc2cccnc12 10.1021/acs.jmedchem.7b00584
155516860 176636 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 179 2 1 1 2.1 Cc1cccc([C@]2(F)C[C@H]2CN)c1 10.1016/j.ejmech.2019.111626
CHEMBL4443782 176636 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 179 2 1 1 2.1 Cc1cccc([C@]2(F)C[C@H]2CN)c1 10.1016/j.ejmech.2019.111626
CHEMBL4597089 176636 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 179 2 1 1 2.1 Cc1cccc([C@]2(F)C[C@H]2CN)c1 10.1016/j.ejmech.2019.111626
155516860 176636 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 179 2 1 1 2.1 Cc1cccc([C@]2(F)C[C@H]2CN)c1 10.1016/j.ejmech.2019.111626
CHEMBL4443782 176636 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 179 2 1 1 2.1 Cc1cccc([C@]2(F)C[C@H]2CN)c1 10.1016/j.ejmech.2019.111626
CHEMBL4597089 176636 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 179 2 1 1 2.1 Cc1cccc([C@]2(F)C[C@H]2CN)c1 10.1016/j.ejmech.2019.111626
137629973 161121 None 0 Human Functional pEC50 = 6.3 6.3 6 2
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 319 6 1 2 4.4 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1Cl 10.1021/acs.jmedchem.7b00584
CHEMBL4104218 161121 None 0 Human Functional pEC50 = 6.3 6.3 6 2
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 319 6 1 2 4.4 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1Cl 10.1021/acs.jmedchem.7b00584
CHEMBL4116381 161121 None 0 Human Functional pEC50 = 6.3 6.3 6 2
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 319 6 1 2 4.4 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1Cl 10.1021/acs.jmedchem.7b00584
16768198 202568 None 34 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 220 1 1 5 1.1 c1nc(N2CCNCC2)c2ccsc2n1 10.1016/j.bmcl.2009.10.112
CHEMBL596108 202568 None 34 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 220 1 1 5 1.1 c1nc(N2CCNCC2)c2ccsc2n1 10.1016/j.bmcl.2009.10.112
137629588 161129 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 336 6 1 3 4.3 COc1ccc(F)cc1C1CC1CNCc1cccc2cccnc12 10.1021/acs.jmedchem.7b00584
CHEMBL4064935 161129 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 336 6 1 3 4.3 COc1ccc(F)cc1C1CC1CNCc1cccc2cccnc12 10.1021/acs.jmedchem.7b00584
CHEMBL4116446 161129 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 336 6 1 3 4.3 COc1ccc(F)cc1C1CC1CNCc1cccc2cccnc12 10.1021/acs.jmedchem.7b00584
137637650 156328 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 301 3 0 5 3.6 CCn1nc(-c2cncc3ccccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
CHEMBL4064770 156328 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 301 3 0 5 3.6 CCn1nc(-c2cncc3ccccc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
85542158 195546 None 0 Human Functional pEC50 = 6.3 6.3 -1 3
Agonist activity at 5-HT2C receptor (unknown origin)Agonist activity at 5-HT2C receptor (unknown origin)
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 6.3 6.3 -1 3
Agonist activity at 5-HT2C receptor (unknown origin)Agonist activity at 5-HT2C receptor (unknown origin)
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 6.3 6.3 -1 3
Agonist activity at 5-HT2C receptor (unknown origin)Agonist activity at 5-HT2C receptor (unknown origin)
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
11233293 84196 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 310 1 1 2 2.9 CC1(c2cc3c(c(C(F)(F)F)c2)C(=O)N2CCNC[C@@H]32)CC1 10.1021/jm0612968
CHEMBL220833 84196 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 310 1 1 2 2.9 CC1(c2cc3c(c(C(F)(F)F)c2)C(=O)N2CCNC[C@@H]32)CC1 10.1021/jm0612968
16115392 84831 None 0 Human Functional pEC50 = 7.3 7.3 5 2
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 236 0 1 2 1.7 Cc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL223292 84831 None 0 Human Functional pEC50 = 7.3 7.3 5 2
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 236 0 1 2 1.7 Cc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
44414183 169020 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Inhibition of 5HT2C assessed as intracellular calcium concentrationInhibition of 5HT2C assessed as intracellular calcium concentration
ChEMBL 207 0 1 1 2.8 C[C@H]1c2cc(Cl)ccc2[C@H]2CNC[C@H]21 10.1016/j.bmcl.2006.04.070
CHEMBL438611 169020 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Inhibition of 5HT2C assessed as intracellular calcium concentrationInhibition of 5HT2C assessed as intracellular calcium concentration
ChEMBL 207 0 1 1 2.8 C[C@H]1c2cc(Cl)ccc2[C@H]2CNC[C@H]21 10.1016/j.bmcl.2006.04.070
137628784 161085 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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)cc1C1CC1CNCc1ccsc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4091197 161085 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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)cc1C1CC1CNCc1ccsc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116144 161085 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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)cc1C1CC1CNCc1ccsc1OC 10.1021/acs.jmedchem.7b00584
11324968 91119 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 216 0 1 2 1.0 Cc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397880 91119 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 216 0 1 2 1.0 Cc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
24826870 91137 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 230 1 1 2 1.2 CCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397898 91137 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 230 1 1 2 1.2 CCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
70693926 74485 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 74485 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 74485 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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
137628784 161085 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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)cc1C1CC1CNCc1ccsc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4091197 161085 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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)cc1C1CC1CNCc1ccsc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116144 161085 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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)cc1C1CC1CNCc1ccsc1OC 10.1021/acs.jmedchem.7b00584
11171955 91127 None 0 Human Functional pEC50 = 7.3 7.3 4 2
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 216 0 1 2 1.2 C[C@@H]1c2ccccc2C(=O)N2CCNC[C@@H]12 10.1016/j.bmcl.2013.04.061
CHEMBL2397888 91127 None 0 Human Functional pEC50 = 7.3 7.3 4 2
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 216 0 1 2 1.2 C[C@@H]1c2ccccc2C(=O)N2CCNC[C@@H]12 10.1016/j.bmcl.2013.04.061
162660343 183809 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4762474 183809 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803205 183809 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
45484827 199245 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 362 6 1 6 2.1 Cc1cc(=O)n(CCCOc2ccccc2Cl)c(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.133
CHEMBL565531 199245 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 362 6 1 6 2.1 Cc1cc(=O)n(CCCOc2ccccc2Cl)c(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.133
10472780 63303 None 0 Human Functional pEC50 = 7.3 7.3 -2 2
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 345 3 1 2 4.3 CC1CNCCc2cc(OCc3ccccc3)c(Br)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL179244 63303 None 0 Human Functional pEC50 = 7.3 7.3 -2 2
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 345 3 1 2 4.3 CC1CNCCc2cc(OCc3ccccc3)c(Br)cc21 10.1016/j.bmcl.2004.12.080
162660343 183809 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4762474 183809 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803205 183809 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
44572696 187365 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 237 5 1 1 3.6 c1ccc(CNC[C@H]2C[C@@H]2c2ccccc2)cc1 10.1021/jm801354e
CHEMBL492698 187365 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 237 5 1 1 3.6 c1ccc(CNC[C@H]2C[C@@H]2c2ccccc2)cc1 10.1021/jm801354e
44412388 78214 None 0 Human Functional pEC50 = 7.2 7.2 -2 3
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 272 1 1 4 1.7 C[C@@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1 10.1016/j.bmcl.2006.03.007
CHEMBL210484 78214 None 0 Human Functional pEC50 = 7.2 7.2 -2 3
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 272 1 1 4 1.7 C[C@@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1 10.1016/j.bmcl.2006.03.007
53324327 56866 None 0 Human Functional pEC50 = 6.2 6.2 1 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)ccn1 10.1016/j.bmcl.2010.11.089
CHEMBL1643857 56866 None 0 Human Functional pEC50 = 6.2 6.2 1 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)ccn1 10.1016/j.bmcl.2010.11.089
172469352 197023 None 0 Human Functional pEC50 = 6.2 6.2 -57 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 214 1 3 3 1.5 Nc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5437030 197023 None 0 Human Functional pEC50 = 6.2 6.2 -57 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 214 1 3 3 1.5 Nc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
172469352 197023 None 0 Human Functional pEC50 = 6.2 6.2 -57 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 214 1 3 3 1.5 Nc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5437030 197023 None 0 Human Functional pEC50 = 6.2 6.2 -57 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 214 1 3 3 1.5 Nc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
137658409 159776 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 299 3 0 3 4.8 CCn1nc(-c2cccc3ccccc23)cc1-c1ccccn1 10.1021/acs.jmedchem.7b00385
CHEMBL4104126 159776 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 299 3 0 3 4.8 CCn1nc(-c2cccc3ccccc23)cc1-c1ccccn1 10.1021/acs.jmedchem.7b00385
170453288 196449 None 2 Human Functional pEC50 = 7.2 7.2 -6 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 277 1 2 2 2.7 Brc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5424175 196449 None 2 Human Functional pEC50 = 7.2 7.2 -6 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 277 1 2 2 2.7 Brc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
137632069 156479 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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 288 2 0 4 3.6 Cn1ccnc1-c1cc(-c2cccc3ccccc23)nn1C 10.1021/acs.jmedchem.7b00385
CHEMBL4066433 156479 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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 288 2 0 4 3.6 Cn1ccnc1-c1cc(-c2cccc3ccccc23)nn1C 10.1021/acs.jmedchem.7b00385
170453288 196449 None 2 Human Functional pEC50 = 7.2 7.2 -6 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 277 1 2 2 2.7 Brc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5424175 196449 None 2 Human Functional pEC50 = 7.2 7.2 -6 3
Agonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2C receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 277 1 2 2 2.7 Brc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
11361103 91139 None 1 Human Functional pEC50 = 6.2 6.2 - 1
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 270 0 1 2 1.7 O=C1c2ccc(C(F)(F)F)cc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397900 91139 None 1 Human Functional pEC50 = 6.2 6.2 - 1
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 270 0 1 2 1.7 O=C1c2ccc(C(F)(F)F)cc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
11644842 89131 None 0 Human Functional pEC50 = 7.2 7.2 12 2
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 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337105 89131 None 0 Human Functional pEC50 = 7.2 7.2 12 2
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 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365394 89131 None 0 Human Functional pEC50 = 7.2 7.2 12 2
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 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
137659281 159350 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 296 2 0 3 4.0 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)C 10.1021/acs.jmedchem.7b00385
CHEMBL4099179 159350 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 296 2 0 3 4.0 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)C 10.1021/acs.jmedchem.7b00385
44404886 72249 None 0 Human Functional pEC50 = 6.2 6.2 -19 2
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 260 6 1 3 3.3 CCCCn1cc(CCN(C)C)c2c(O)cccc21 10.1016/j.bmcl.2005.06.104
CHEMBL198124 72249 None 0 Human Functional pEC50 = 6.2 6.2 -19 2
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 260 6 1 3 3.3 CCCCn1cc(CCN(C)C)c2c(O)cccc21 10.1016/j.bmcl.2005.06.104
155539961 176653 None 0 Human Functional pEC50 = 6.2 6.2 -5 3
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 213 3 1 2 2.0 COc1ccc(F)cc1C1(F)CC1CN 10.1016/j.ejmech.2019.111626
CHEMBL4515411 176653 None 0 Human Functional pEC50 = 6.2 6.2 -5 3
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 213 3 1 2 2.0 COc1ccc(F)cc1C1(F)CC1CN 10.1016/j.ejmech.2019.111626
CHEMBL4597225 176653 None 0 Human Functional pEC50 = 6.2 6.2 -5 3
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 213 3 1 2 2.0 COc1ccc(F)cc1C1(F)CC1CN 10.1016/j.ejmech.2019.111626
16115654 137061 None 0 Human Functional pEC50 = 8.2 8.2 27 3
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 270 0 1 2 2.1 Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374562 137061 None 0 Human Functional pEC50 = 8.2 8.2 27 3
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 270 0 1 2 2.1 Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
24826957 91151 None 0 Human Functional pEC50 = 8.2 8.2 24 2
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 246 1 1 3 1.0 COc1ccc(C)c2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397912 91151 None 0 Human Functional pEC50 = 8.2 8.2 24 2
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 246 1 1 3 1.0 COc1ccc(C)c2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
44572172 12550 None 0 Human Functional pEC50 = 8.2 8.2 -1 3
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 179 2 1 1 2.2 Cc1cc([C@H]2C[C@@H]2CN)ccc1F 10.1021/jm801354e
CHEMBL1186686 12550 None 0 Human Functional pEC50 = 8.2 8.2 -1 3
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 179 2 1 1 2.2 Cc1cc([C@H]2C[C@@H]2CN)ccc1F 10.1021/jm801354e
CHEMBL474633 12550 None 0 Human Functional pEC50 = 8.2 8.2 -1 3
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 179 2 1 1 2.2 Cc1cc([C@H]2C[C@@H]2CN)ccc1F 10.1021/jm801354e
137652480 157246 None 0 Human Functional pEC50 = 8.2 8.2 12 2
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 4 3.1 Cn1nc(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4075267 157246 None 0 Human Functional pEC50 = 8.2 8.2 12 2
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 4 3.1 Cn1nc(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
137646921 157792 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 366 3 1 4 4.1 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4081863 157792 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 366 3 1 4 4.1 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
11447552 62548 None 2 Human Functional pEC50 = 8.2 8.2 30 3
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 229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
CHEMBL178231 62548 None 2 Human Functional pEC50 = 8.2 8.2 30 3
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 229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
15984073 166166 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Inhibition of 5HT2C assessed as intracellular calcium concentrationInhibition of 5HT2C assessed as intracellular calcium concentration
ChEMBL 237 1 1 2 2.8 COc1cc2c(cc1Cl)[C@H](C)[C@@H]1CNC[C@H]21 10.1016/j.bmcl.2006.04.070
CHEMBL425777 166166 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Inhibition of 5HT2C assessed as intracellular calcium concentrationInhibition of 5HT2C assessed as intracellular calcium concentration
ChEMBL 237 1 1 2 2.8 COc1cc2c(cc1Cl)[C@H](C)[C@@H]1CNC[C@H]21 10.1016/j.bmcl.2006.04.070
162658689 183796 None 0 Human Functional pEC50 = 8.2 8.2 28 3
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 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4759181 183796 None 0 Human Functional pEC50 = 8.2 8.2 28 3
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 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803103 183796 None 0 Human Functional pEC50 = 8.2 8.2 28 3
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 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
162658689 183796 None 0 Human Functional pEC50 = 8.2 8.2 28 3
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 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4759181 183796 None 0 Human Functional pEC50 = 8.2 8.2 28 3
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 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803103 183796 None 0 Human Functional pEC50 = 8.2 8.2 28 3
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 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
134265637 181915 None 0 Human Functional pEC50 = 8.2 8.2 2 3
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 229 1 1 3 1.7 c1cc(C2CC2)c2c(n1)N1CCNC[C@H]1CC2 10.1016/j.bmcl.2021.127872
CHEMBL4778104 181915 None 0 Human Functional pEC50 = 8.2 8.2 2 3
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 229 1 1 3 1.7 c1cc(C2CC2)c2c(n1)N1CCNC[C@H]1CC2 10.1016/j.bmcl.2021.127872
10105208 62519 None 0 Human Functional pEC50 = 8.2 8.2 15 3
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 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
CHEMBL178124 62519 None 0 Human Functional pEC50 = 8.2 8.2 15 3
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 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
9990808 122838 None 0 Human Functional pEC50 = 8.2 8.2 10 3
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 213 0 1 1 2.7 CC1CNCCc2cc(F)c(Cl)cc21 10.1021/jm0709034
CHEMBL360492 122838 None 0 Human Functional pEC50 = 8.2 8.2 10 3
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 213 0 1 1 2.7 CC1CNCCc2cc(F)c(Cl)cc21 10.1021/jm0709034
24773651 154947 None 0 Human Functional pEC50 = 8.2 8.2 5 3
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 225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@H](C)CNCC2 10.1021/jm0709034
CHEMBL400600 154947 None 0 Human Functional pEC50 = 8.2 8.2 5 3
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 225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@H](C)CNCC2 10.1021/jm0709034
134141127 147314 None 0 Human Functional pEC50 = 8.2 8.2 -3 2
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 240 0 1 2 2.2 Fc1ccc2c(c1Cl)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3928388 147314 None 0 Human Functional pEC50 = 8.2 8.2 -3 2
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 240 0 1 2 2.2 Fc1ccc2c(c1Cl)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
134149355 148211 None 0 Human Functional pEC50 = 8.2 8.2 31 3
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 322 2 1 4 2.7 c1cc(Cc2ccc3c(c2)OCO3)c2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3935339 148211 None 0 Human Functional pEC50 = 8.2 8.2 31 3
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 322 2 1 4 2.7 c1cc(Cc2ccc3c(c2)OCO3)c2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
162644827 183729 None 0 Human Functional pEC50 = 8.2 8.2 16 3
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
CHEMBL4739937 183729 None 0 Human Functional pEC50 = 8.2 8.2 16 3
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
CHEMBL4802378 183729 None 0 Human Functional pEC50 = 8.2 8.2 16 3
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
46230100 201775 None 0 Human Functional pEC50 = 8.2 8.2 38 2
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 231 0 2 3 0.9 Cc1ccc2c(c1)N1CCNCCC1NC2=O 10.1016/j.bmcl.2009.12.014
CHEMBL590531 201775 None 0 Human Functional pEC50 = 8.2 8.2 38 2
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 231 0 2 3 0.9 Cc1ccc2c(c1)N1CCNCCC1NC2=O 10.1016/j.bmcl.2009.12.014
11708275 72737 None 1 Rat Functional pEC50 = 8.2 8.2 -1 2
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 205 3 1 4 1.4 COc1ccc2cnn(C[C@H](C)N)c2c1 10.1021/jm050663x
CHEMBL199775 72737 None 1 Rat Functional pEC50 = 8.2 8.2 -1 2
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 205 3 1 4 1.4 COc1ccc2cnn(C[C@H](C)N)c2c1 10.1021/jm050663x
11264955 207419 None 0 Human Functional pEC50 = 8.2 8.2 -1 3
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 240 3 1 3 2.3 CSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
CHEMBL76474 207419 None 0 Human Functional pEC50 = 8.2 8.2 -1 3
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 240 3 1 3 2.3 CSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
162644827 183729 None 0 Human Functional pEC50 = 8.2 8.2 16 3
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
CHEMBL4739937 183729 None 0 Human Functional pEC50 = 8.2 8.2 16 3
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
CHEMBL4802378 183729 None 0 Human Functional pEC50 = 8.2 8.2 16 3
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
118733790 120735 None 0 Human Functional pEC50 = 7.2 7.2 36 2
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 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416047 120735 None 0 Human Functional pEC50 = 7.2 7.2 36 2
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 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546973 120735 None 0 Human Functional pEC50 = 7.2 7.2 36 2
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 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
68690817 91118 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 227 0 1 3 0.5 N#Cc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397879 91118 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 227 0 1 3 0.5 N#Cc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
4305260 191134 None 0 Human Functional pEC50 = 6.2 6.2 1 2
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 288 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5186877 191134 None 0 Human Functional pEC50 = 6.2 6.2 1 2
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 288 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
4305260 191134 None 0 Human Functional pEC50 = 6.2 6.2 1 2
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 288 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5186877 191134 None 0 Human Functional pEC50 = 6.2 6.2 1 2
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 288 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
155539961 176653 None 0 Human Functional pEC50 = 6.2 6.2 -5 3
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 213 3 1 2 2.0 COc1ccc(F)cc1C1(F)CC1CN 10.1016/j.ejmech.2019.111626
CHEMBL4515411 176653 None 0 Human Functional pEC50 = 6.2 6.2 -5 3
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 213 3 1 2 2.0 COc1ccc(F)cc1C1(F)CC1CN 10.1016/j.ejmech.2019.111626
CHEMBL4597225 176653 None 0 Human Functional pEC50 = 6.2 6.2 -5 3
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 213 3 1 2 2.0 COc1ccc(F)cc1C1(F)CC1CN 10.1016/j.ejmech.2019.111626
46230098 201785 None 0 Rat Functional pEC50 = 7.2 7.2 -30 4
Agonist activity at 5HT2C receptor in rat fundusAgonist activity at 5HT2C receptor in rat fundus
ChEMBL 231 0 2 3 0.9 Cc1cccc2c1C(=O)NC1CCNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590580 201785 None 0 Rat Functional pEC50 = 7.2 7.2 -30 4
Agonist activity at 5HT2C receptor in rat fundusAgonist activity at 5HT2C receptor in rat fundus
ChEMBL 231 0 2 3 0.9 Cc1cccc2c1C(=O)NC1CCNCCN21 10.1016/j.bmcl.2009.12.014
3071387 192879 None 0 Human Functional pEC50 = 7.2 7.2 3 2
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 216 1 3 2 2.5 CCC1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5172342 192879 None 0 Human Functional pEC50 = 7.2 7.2 3 2
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 216 1 3 2 2.5 CCC1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221228 192879 None 0 Human Functional pEC50 = 7.2 7.2 3 2
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 216 1 3 2 2.5 CCC1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
122442273 138443 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771152 138443 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771392 138443 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
3071387 192879 None 0 Human Functional pEC50 = 7.2 7.2 3 2
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 216 1 3 2 2.5 CCC1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5172342 192879 None 0 Human Functional pEC50 = 7.2 7.2 3 2
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 216 1 3 2 2.5 CCC1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221228 192879 None 0 Human Functional pEC50 = 7.2 7.2 3 2
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 216 1 3 2 2.5 CCC1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
122442273 138443 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771152 138443 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771392 138443 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
68691189 91142 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 227 0 1 3 0.5 N#Cc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397903 91142 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 227 0 1 3 0.5 N#Cc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
137650864 161302 None 0 Human Functional pEC50 = 6.2 6.2 -6 3
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 329 8 1 3 3.8 COc1ccccc1CCNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4075150 161302 None 0 Human Functional pEC50 = 6.2 6.2 -6 3
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 329 8 1 3 3.8 COc1ccccc1CCNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4117857 161302 None 0 Human Functional pEC50 = 6.2 6.2 -6 3
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 329 8 1 3 3.8 COc1ccccc1CCNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
46228434 202602 None 1 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 254 1 1 5 1.8 Clc1nc(N2CCNCC2)nc2sccc12 10.1016/j.bmcl.2009.10.112
CHEMBL596327 202602 None 1 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 254 1 1 5 1.8 Clc1nc(N2CCNCC2)nc2sccc12 10.1016/j.bmcl.2009.10.112
137650864 161302 None 0 Human Functional pEC50 = 6.2 6.2 -6 3
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 329 8 1 3 3.8 COc1ccccc1CCNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4075150 161302 None 0 Human Functional pEC50 = 6.2 6.2 -6 3
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 329 8 1 3 3.8 COc1ccccc1CCNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4117857 161302 None 0 Human Functional pEC50 = 6.2 6.2 -6 3
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 329 8 1 3 3.8 COc1ccccc1CCNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
57799321 89095 None 1 Human Functional pEC50 = 7.2 7.2 - 1
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
CHEMBL2337491 89095 None 1 Human Functional pEC50 = 7.2 7.2 - 1
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
CHEMBL2364961 89095 None 1 Human Functional pEC50 = 7.2 7.2 - 1
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
45484654 200125 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 235 3 1 4 1.0 CC(C)CCn1nc2c(cc1=O)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL571064 200125 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 235 3 1 4 1.0 CC(C)CCn1nc2c(cc1=O)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL4749189 216551 None 26 Human Functional pEC50 = 7.2 7.2 4 2
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 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL4802743 216551 None 26 Human Functional pEC50 = 7.2 7.2 4 2
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 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
11739217 137127 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 300 2 1 3 2.2 CCOc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374660 137127 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 300 2 1 3 2.2 CCOc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
118733794 120737 None 0 Human Functional pEC50 = 7.2 7.2 15 3
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 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416049 120737 None 0 Human Functional pEC50 = 7.2 7.2 15 3
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 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546975 120737 None 0 Human Functional pEC50 = 7.2 7.2 15 3
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 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
53324165 56817 None 0 Human Functional pEC50 = 7.2 7.2 2 3
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of i