Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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DOI

134265828 181521 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 181521 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 72 Human Functional pEC50 = 10.1 10.1 -3 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 72 Human Functional pEC50 = 10.1 10.1 -3 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 72 Human Functional pEC50 = 10.1 10.1 -3 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 72 Human Functional pEC50 = 10.1 10.1 -3 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 72 Human Functional pEC50 = 10.1 10.1 -3 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 72 Human Functional pEC50 = 10.1 10.1 -3 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 72 Human Functional pEC50 = 10.1 10.1 -3 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 72 Human Functional pEC50 = 10.1 10.1 -3 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 199985 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 199985 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 202161 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 202161 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 164411 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 164411 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 164411 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 164411 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 164406 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 164406 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
134265620 164406 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 164406 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 72 Human Functional pEC50 = 9.9 9.9 -3 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 72 Human Functional pEC50 = 9.9 9.9 -3 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 72 Human Functional pEC50 = 9.9 9.9 -3 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 72 Human Functional pEC50 = 9.9 9.9 -3 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 72 Human Functional pEC50 = 9.9 9.9 -3 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 72 Human Functional pEC50 = 9.9 9.9 -3 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 72 Human Functional pEC50 = 9.9 9.9 -3 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 72 Human Functional pEC50 = 9.9 9.9 -3 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 72 Human Functional pEC50 = 9.8 9.8 -3 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 72 Human Functional pEC50 = 9.8 9.8 -3 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 72 Human Functional pEC50 = 9.8 9.8 -3 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 72 Human Functional pEC50 = 9.8 9.8 -3 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 72 Human Functional pEC50 = 9.8 9.8 -3 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 72 Human Functional pEC50 = 9.8 9.8 -3 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 72 Human Functional pEC50 = 9.8 9.8 -3 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 72 Human Functional pEC50 = 9.8 9.8 -3 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 72 Human Functional pEC50 = 9.8 9.8 -3 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 72 Human Functional pEC50 = 9.8 9.8 -3 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 72 Human Functional pEC50 = 9.8 9.8 -3 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 72 Human Functional pEC50 = 9.8 9.8 -3 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 120019 None 107 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 120019 None 107 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 120019 None 107 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 164013 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 164013 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 181688 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 181688 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 149633 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 149633 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 59569 None 3 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 59569 None 3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 72 Human Functional pEC50 = 9.7 9.7 -3 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 120019 None 107 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 120019 None 107 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 120019 None 107 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 59655 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 59655 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 153510 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 153510 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 72 Human Functional pEC50 = 9.5 9.5 -3 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 72 Human Functional pEC50 = 9.5 9.5 -3 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 72 Human Functional pEC50 = 9.5 9.5 -3 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 72 Human Functional pEC50 = 9.5 9.5 -3 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 72 Human Functional pEC50 = 9.5 9.5 -3 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 72 Human Functional pEC50 = 9.5 9.5 -3 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 72 Human Functional pEC50 = 9.5 9.5 -3 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 72 Human Functional pEC50 = 9.5 9.5 -3 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 192863 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 192863 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 192863 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 72 Human Functional pEC50 = 9.5 9.5 -3 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 72 Human Functional pEC50 = 9.5 9.5 -3 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 72 Human Functional pEC50 = 9.5 9.5 -3 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 72 Human Functional pEC50 = 9.5 9.5 -3 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 22 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 22 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 22 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 22 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 181785 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 181785 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 85306 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 85306 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 72 Human Functional pEC50 = 9.4 9.4 -3 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 72 Human Functional pEC50 = 9.4 9.4 -3 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 72 Human Functional pEC50 = 9.4 9.4 -3 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 72 Human Functional pEC50 = 9.4 9.4 -3 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 72 Human Functional pEC50 = 9.4 9.4 -3 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 72 Human Functional pEC50 = 9.4 9.4 -3 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 72 Human Functional pEC50 = 9.4 9.4 -3 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 72 Human Functional pEC50 = 9.4 9.4 -3 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 193009 None 5 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 193009 None 5 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 193009 None 5 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 193009 None 5 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 193009 None 5 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 193009 None 5 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 183715 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 183715 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 183715 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 183715 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 183715 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 183715 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 181849 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 181849 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 16162 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 16162 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 12499 None 1 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 12499 None 1 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 12499 None 1 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 191793 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 191793 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 151154 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 151154 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 152029 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 152029 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 191793 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 191793 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 72 Human Functional pEC50 = 9.1 9.1 -3 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 72 Human Functional pEC50 = 9.1 9.1 -3 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 72 Human Functional pEC50 = 9.1 9.1 -3 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 72 Human Functional pEC50 = 9.1 9.1 -3 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 72 Human Functional pEC50 = 9.1 9.1 -3 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 72 Human Functional pEC50 = 9.1 9.1 -3 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 72 Human Functional pEC50 = 9.1 9.1 -3 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 72 Human Functional pEC50 = 9.1 9.1 -3 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 138357 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 138357 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 138357 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 200055 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 200055 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 89071 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 89071 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 89071 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 8062 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 8062 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 25 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 25 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 25 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 150753 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 150753 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 192179 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 192179 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 192179 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 192179 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 138357 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 138357 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 138357 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 89110 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 89110 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 89110 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 163679 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 163679 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 164799 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 164799 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 183715 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 183715 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 183715 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 183715 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 183715 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 183715 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 163807 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 163807 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 164799 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 164799 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 12648 None 8 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 12648 None 8 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 12648 None 8 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 163807 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 163807 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 84838 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 84838 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 199860 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 199860 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 146152 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 146152 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 183662 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 183662 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 183662 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 183662 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 183662 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 183662 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 72 Human Functional pEC50 = 8.8 8.8 -3 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 72 Human Functional pEC50 = 8.8 8.8 -3 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 72 Human Functional pEC50 = 8.8 8.8 -3 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 72 Human Functional pEC50 = 8.8 8.8 -3 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 72 Human Functional pEC50 = 8.8 8.8 -3 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 72 Human Functional pEC50 = 8.8 8.8 -3 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 72 Human Functional pEC50 = 8.8 8.8 -3 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 72 Human Functional pEC50 = 8.8 8.8 -3 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 29 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 29 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 29 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 199312 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 199312 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 51 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 51 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 51 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 51 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 51 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 187631 None 33 Human Functional pEC50 = 8.7 8.7 54 3
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 187631 None 33 Human Functional pEC50 = 8.7 8.7 54 3
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 191906 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 191906 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 187631 None 33 Human Functional pEC50 = 8.7 8.7 54 3
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 187631 None 33 Human Functional pEC50 = 8.7 8.7 54 3
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 191906 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 191906 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 180018 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 180018 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 147450 None 1 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 147450 None 1 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 79108 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 79108 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 199984 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 199984 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 91082 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 91082 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 183727 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 183727 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 183727 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 12653 None 3 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 12653 None 3 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 12653 None 3 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 94913 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 94913 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 169204 None 6 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 169204 None 6 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 192971 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 192971 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 192971 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 197823 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 197823 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 111665 None 18 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 111665 None 18 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 149172 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 149172 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 192971 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 192971 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 192971 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 183727 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 183727 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 183727 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 61454 None 28 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 61454 None 28 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 183635 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 183635 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 183635 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 183694 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 183694 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 183694 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 164091 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 164091 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 183792 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 183792 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 183792 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 61461 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 61461 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 87307 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 87307 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 150719 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 150719 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 107514 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 107514 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
3288856 192813 None 2 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 192813 None 2 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 192813 None 2 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 149658 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 149658 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 107192 None 2 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 107192 None 2 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
10560133 107337 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 107337 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 192813 None 2 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 192813 None 2 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 192813 None 2 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 183747 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 183747 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 183747 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 197336 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 197336 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 183747 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 183747 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 183747 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 161147 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 161147 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 161147 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 87307 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 87307 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 197760 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 197760 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 120639 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 120639 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 120639 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 161147 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 161147 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 161147 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 197253 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 197253 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
11983273 77996 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 77996 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
137655846 158690 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 158690 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 138362 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 138362 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 138362 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 214063 None 2 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 214063 None 2 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 138362 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 138362 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 138362 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 155823 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 155823 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 214063 None 2 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 214063 None 2 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 192965 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 192965 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 192965 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 192837 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 192837 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 192837 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 176549 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 176549 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 176549 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 84894 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 84894 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 198464 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 198464 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 103040 None 53 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 103040 None 53 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 103040 None 53 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 103040 None 53 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 103040 None 53 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 103040 None 53 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 138359 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 138359 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 138359 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 192837 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 192837 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 192837 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 192965 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 192965 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 192965 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 176549 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 176549 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 176549 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 91104 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 91104 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 138359 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 138359 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 138359 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 120651 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 120651 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 120651 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 83491 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 83491 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 89099 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 89099 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 89099 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 120665 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 120665 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 120665 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 183635 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 183635 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 183635 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 183694 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 183694 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 183694 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 12484 None 1 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 12484 None 1 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 12484 None 1 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 197552 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 197552 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 51 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 51 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 51 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 51 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 51 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 64332 None 63 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 64332 None 63 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 64637 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 64637 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 166149 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 166149 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 78427 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 78427 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 61455 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 61455 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 199311 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 199311 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 169683 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 169683 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 198331 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 198331 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 111672 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 111672 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 183657 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 183657 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 183657 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 192988 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 192988 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 192988 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 120654 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 120654 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 120654 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 183657 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 183657 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 183657 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 192988 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 192988 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 192988 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 197828 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 197828 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
162659576 183697 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 183697 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 183697 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 138348 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 138348 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 138348 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 138353 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 138353 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 138353 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
162659576 183697 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 183697 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 183697 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 193173 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 193173 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 138348 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 138348 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 138348 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 138353 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 138353 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 138353 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 192207 None 2 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 192207 None 2 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 192207 None 2 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 192207 None 2 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 12558 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 12558 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 12558 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 156303 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 156303 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 12542 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 12542 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 12542 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 141686 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 141686 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 89085 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 89085 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 89085 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 91099 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 91099 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 91112 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 91112 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 183681 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 183681 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 183681 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 187422 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 187422 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 158010 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 158010 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 158458 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 158458 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 176462 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 176462 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 176462 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 101979 None 24 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 101979 None 24 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 72062 None 32 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 72062 None 32 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 63938 None 23 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 63938 None 23 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 169204 None 6 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 169204 None 6 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 183681 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 183681 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 183681 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 164055 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 164055 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 176462 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 176462 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 176462 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 63938 None 23 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 63938 None 23 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 64332 None 63 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 64332 None 63 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 214071 None 2 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 214071 None 2 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 88 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 88 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 88 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 88 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 88030 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 88030 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 214071 None 2 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 214071 None 2 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 161026 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 161026 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 161026 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 199738 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 199738 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 161215 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 161215 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 161215 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 203409 None 11 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 203409 None 11 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 74459 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 74459 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 74459 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 98020 None 77 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 98020 None 77 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 160990 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 160990 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 160990 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 161215 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 161215 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 161215 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 200056 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 200056 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 160978 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 160978 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 160978 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 102490 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 102490 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 102490 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 87305 None 5 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 87305 None 5 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 160978 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 160978 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 160978 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 87305 None 5 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 87305 None 5 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 160990 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 160990 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 160990 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
70681346 74463 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 74463 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 74463 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 120645 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 120645 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 120645 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 193046 None 2 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 193046 None 2 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 193046 None 2 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 203409 None 11 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 203409 None 11 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 193046 None 2 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 193046 None 2 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 193046 None 2 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 61457 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 61457 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 198371 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 198371 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 142644 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 142644 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 142656 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 142656 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 143595 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 143595 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 79675 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 79675 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
46228441 199865 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 199865 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 120642 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 120642 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 120642 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 64425 None 2 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 64425 None 2 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 192923 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 192923 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 192923 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 152794 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 152794 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 207193 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 207193 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 207788 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 207788 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 192923 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 192923 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 192923 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 73985 None 55 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 73985 None 55 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 73985 None 55 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 156059 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 156059 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 53212 None 97 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 53212 None 97 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 53212 None 97 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 12683 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 12683 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 12683 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 192792 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 192792 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 192792 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 157828 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 157828 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 120644 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 120644 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 120644 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 161026 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 161026 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 161026 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 12674 None 18 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 12674 None 18 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 12674 None 18 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 12702 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 12702 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 12702 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 156831 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 156831 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 157853 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 157853 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 138351 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 138351 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 138351 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 190416 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 190416 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 138351 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 138351 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 138351 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 190416 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 190416 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 138354 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 138354 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 138354 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 192792 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 192792 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 192792 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 171287 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 171287 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 142656 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 142656 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 205433 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 205433 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 193005 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 193005 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 193005 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 193005 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 193005 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 193005 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 120649 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 120649 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 120649 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 199250 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 199250 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 138361 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 138361 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 138361 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 12520 None 1 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 12520 None 1 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 12520 None 1 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 138361 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 138361 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 138361 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 91088 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 91088 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 138001 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 138001 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 12458 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 12458 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 12458 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 102469 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 102469 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 202195 None 2 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 202195 None 2 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 199247 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 199247 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 183650 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 183650 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 183650 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 12686 None 1 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 12686 None 1 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 12686 None 1 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 183650 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 183650 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 183650 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 137240 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 137240 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 91095 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 91095 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 91115 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 91115 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 12701 None 1 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 12701 None 1 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 12701 None 1 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 172593 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 172593 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 158532 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 158532 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 138354 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 138354 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 138354 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 183624 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 183624 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 183624 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 111667 None 1 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 111667 None 1 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 192833 None 1 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 192833 None 1 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 192833 None 1 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 192814 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 192814 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 192814 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 192833 None 1 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 192833 None 1 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 192833 None 1 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 192814 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 192814 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 192814 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
1355 2011 None 88 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 88 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 88 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 88 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 183624 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 183624 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 183624 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 88 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 88 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 88 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 88 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 88 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 88 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 88 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 88 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 157770 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 157770 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 74651 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 74651 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 214065 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 214065 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 214065 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 214065 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 138345 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 138345 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 138345 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 192907 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 192907 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 192907 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 62631 None 17 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 62631 None 17 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 192907 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 192907 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 192907 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 137998 None 32 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 137998 None 32 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 102402 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 102402 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 102402 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 138343 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 138343 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 138343 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 192859 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 192859 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 192859 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 192874 None 1 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 192874 None 1 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 192874 None 1 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 138343 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 138343 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 138343 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 192859 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 192859 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 192859 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 192874 None 1 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 192874 None 1 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 192874 None 1 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 158260 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 158260 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 157899 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 157899 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 111670 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 111670 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 120666 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 120666 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 120666 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 12687 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 12687 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 12687 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 73978 None 15 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 73978 None 15 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 73978 None 15 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
3572096 192898 None 1 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 192898 None 1 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 192898 None 1 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 192947 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 192947 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 192947 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 148042 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 148042 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 207926 None 26 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 207926 None 26 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
44420683 84133 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 84133 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 192934 None 1 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 192934 None 1 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 192934 None 1 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 207933 None 2 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 207933 None 2 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 192898 None 1 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 192898 None 1 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 192898 None 1 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 192947 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 192947 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 192947 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 84248 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 84248 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 91097 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 91097 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 91119 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 91119 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 12654 None 1 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 12654 None 1 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 12654 None 1 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 199366 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 199366 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 111666 None 4 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 111666 None 4 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 158928 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 158928 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 138344 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 138344 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 138344 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 138345 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 138345 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 138345 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 62631 None 17 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 62631 None 17 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 158872 None 15 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 158872 None 15 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 51 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 51 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 51 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 51 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 51 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 138344 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 138344 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 138344 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 138357 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 138357 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 138357 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 49 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 49 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 49 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 49 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 198577 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 198577 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 63301 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 63301 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 156008 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 156008 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 192934 None 1 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 192934 None 1 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 192934 None 1 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 12680 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 12680 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 12680 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 49 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 49 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 49 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 49 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 161196 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 161196 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 161196 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 98766 None 71 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 98766 None 71 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 98766 None 71 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 198778 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 198778 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 200038 None 76 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 200038 None 76 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 197655 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 197655 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 161196 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 161196 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 161196 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 138353 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 138353 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 138353 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 138359 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 138359 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 138359 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 138353 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 138353 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 138353 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 138359 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 138359 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 138359 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
137645024 158069 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 158069 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 136960 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 136960 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 89112 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 89112 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 89112 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 156568 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 156568 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 88 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 88 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 88 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 88 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 187203 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 187203 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 88 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 88 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 88 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 88 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 87310 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 87310 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 91106 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 91106 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 192810 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 192810 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 192810 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 192975 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 192975 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 192975 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 192810 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 192810 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 192810 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 192975 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 192975 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 192975 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 84839 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 84839 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 87310 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 87310 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 90985 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 90985 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 192884 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 192884 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 192884 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 198518 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 198518 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 4448 None 24 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 4448 None 24 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 4448 None 24 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 120662 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 120662 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 120662 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 192884 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 192884 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 192884 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 84793 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 84793 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 91120 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 91120 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 12465 None 1 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 12465 None 1 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 12465 None 1 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 74458 None 1 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 74458 None 1 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 74458 None 1 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 56802 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 56802 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 156471 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 156471 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 138355 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 138355 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 138355 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 18 Human Functional pEC50 = 7.8 7.8 -2 4
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 18 Human Functional pEC50 = 7.8 7.8 -2 4
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 18 Human Functional pEC50 = 7.8 7.8 -2 4
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 138355 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 138355 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 138355 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 61463 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 61463 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 59242 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 59242 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 77733 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 77733 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 191997 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 191997 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 156412 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 156412 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 8204 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 8204 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 120661 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 120661 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 120661 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 84877 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 84877 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 192950 None 1 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 192950 None 1 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 192950 None 1 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 187200 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 187200 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 192950 None 1 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 192950 None 1 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 192950 None 1 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 161138 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 161138 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 161138 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 161138 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 161138 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 161138 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 201991 None 50 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 201991 None 50 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 158202 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 158202 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 56851 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 56851 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 183615 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 183615 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 183615 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 102759 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 102759 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 201073 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 201073 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 183615 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 183615 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 183615 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 63304 None 4 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 63304 None 4 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 94860 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 94860 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 130399 None 5 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 130399 None 5 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 144557 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 144557 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 150081 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 150081 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 151392 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 151392 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 153404 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 153404 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 61454 None 28 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 61454 None 28 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 61454 None 28 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 61454 None 28 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 158995 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 158995 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 169683 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 169683 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 192823 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 192823 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 192823 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 192883 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 192883 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 192883 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 61452 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 61452 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 192823 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 192823 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 192823 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 192883 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 192883 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 192883 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 61464 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 61464 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 91089 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 91089 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 61456 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 61456 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 192854 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 192854 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 192854 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 192854 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 192854 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 192854 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 12554 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 12554 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 12554 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 193057 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 193057 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 123432 None 8 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 123432 None 8 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 154416 None 1 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 154416 None 1 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 192820 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 192820 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 192820 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 147276 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 147276 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 18 Rat Functional pEC50 = 6.7 6.7 -79 4
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 18 Rat Functional pEC50 = 6.7 6.7 -79 4
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 18 Rat Functional pEC50 = 6.7 6.7 -79 4
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 111810 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 111810 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 156936 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 156936 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 207466 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 207466 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 73976 None 80 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 73976 None 80 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 73976 None 80 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 98079 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 98079 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 98571 None 2 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 98571 None 2 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 111979 None 3 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 111979 None 3 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
11695000 89071 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 89071 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 89071 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 199329 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 199329 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 159349 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 159349 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 63317 None 4 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 63317 None 4 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 51 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 51 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 51 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 51 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 51 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 89092 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 89092 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 89092 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 18 Human Functional pEC50 = 8.7 8.7 -2 4
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 18 Human Functional pEC50 = 8.7 8.7 -2 4
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 18 Human Functional pEC50 = 8.7 8.7 -2 4
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 18 Human Functional pEC50 = 8.7 8.7 -2 4
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 18 Human Functional pEC50 = 8.7 8.7 -2 4
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 18 Human Functional pEC50 = 8.7 8.7 -2 4
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 8061 None 30 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 8061 None 30 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 179109 None 22 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 179109 None 22 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 161114 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 161114 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 161114 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 161114 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 161114 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 161114 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 149480 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 149480 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 183682 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 183682 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 183682 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 89109 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 89109 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 89109 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 183682 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 183682 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 183682 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 102487 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 102487 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 102487 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 183649 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 183649 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 183649 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 183750 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 183750 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 183750 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 183649 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 183649 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 183649 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 183750 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 183750 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 183750 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 176566 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 176566 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 176566 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 72 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 72 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 72 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 72 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 84227 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 84227 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 89107 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 89107 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 89107 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 183663 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 183663 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 183663 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 192866 None 1 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 192866 None 1 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 192866 None 1 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 159407 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 159407 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 63304 None 4 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 63304 None 4 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 102494 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 102494 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 102494 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 192831 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 192831 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 192831 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 183663 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 183663 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 183663 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 192831 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 192831 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 192831 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 192866 None 1 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 192866 None 1 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 192866 None 1 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 192820 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 192820 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 192820 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 4539 None 3 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 4539 None 3 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 107999 None 22 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 107999 None 22 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 64425 None 2 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 64425 None 2 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 193023 None 5 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 193023 None 5 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 193023 None 5 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
4401618 193023 None 5 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 193023 None 5 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 193023 None 5 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 120658 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 120658 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 120658 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
168285159 192914 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 192914 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 192914 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 192870 None 2 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 192870 None 2 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 192870 None 2 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 192914 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 192914 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 192914 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 192870 None 2 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 192870 None 2 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 192870 None 2 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
162668367 183739 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 183739 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 183739 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 74209 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 74209 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 74209 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 74209 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 198354 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 198354 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 198438 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 198438 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 138357 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 138357 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 138357 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 205505 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 205505 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 183739 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 183739 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 183739 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 51 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 51 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 51 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 51 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 51 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 61460 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 61460 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 56849 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 56849 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 120653 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 120653 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 120653 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
11673842 89088 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 89088 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 89088 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 121772 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 121772 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 74462 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 74462 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 74462 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 200036 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 200036 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 8094 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 8094 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 183694 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 183694 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 183694 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 120669 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 120669 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 120669 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 91098 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 91098 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 130399 None 5 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 130399 None 5 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 78096 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 78096 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 183694 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 183694 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 183694 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 183717 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 183717 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 183717 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 190608 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 190608 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 190608 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 190608 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 161059 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 161059 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 161059 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 172851 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 172851 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 138358 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 138358 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 138358 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 138358 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 138358 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 138358 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 161002 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 161002 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 161002 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 196820 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 196820 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 176639 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 176639 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 176639 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 161002 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 161002 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 161002 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 161019 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 161019 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 161019 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 87307 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 87307 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 176639 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 176639 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 176639 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 183717 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 183717 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 183717 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 161059 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 161059 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 161059 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 12459 None 1 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 12459 None 1 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 12459 None 1 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 56805 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 56805 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 78300 None 2 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 78300 None 2 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 161222 None 2 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 161222 None 2 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 161222 None 2 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
137640063 161222 None 2 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 161222 None 2 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 161222 None 2 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 138349 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 138349 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 138349 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 138360 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 138360 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 138360 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 87307 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 87307 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 62980 None 3 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 62980 None 3 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 102401 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 102401 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 102401 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 161019 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 161019 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 161019 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 12543 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 12543 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 12543 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 138358 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 138358 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 138358 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 138358 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 138358 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 138358 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
11414184 83498 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 83498 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 74478 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 74478 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 74478 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 72 Human Functional pEC50 = 7.6 7.6 -3 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 72 Human Functional pEC50 = 7.6 7.6 -3 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 72 Human Functional pEC50 = 7.6 7.6 -3 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 72 Human Functional pEC50 = 7.6 7.6 -3 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 156904 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 156904 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 138349 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 138349 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 138349 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 138360 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 138360 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 138360 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 214068 None 1 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 214068 None 1 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 214068 None 1 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 214068 None 1 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
13139 2491 None 29 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 29 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 29 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 91107 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 91107 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 120663 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 120663 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 120663 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 161001 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 161001 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 161001 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 161001 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 161001 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 161001 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 202795 None 71 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 202795 None 71 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 202795 None 71 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 84665 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 84665 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 120648 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 120648 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 120648 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
46228433 199740 None 8 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 199740 None 8 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 183717 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 183717 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 183717 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 91113 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 91113 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 183666 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 183666 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 183666 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 72 Human Functional pEC50 = 7.6 7.6 -3 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 72 Human Functional pEC50 = 7.6 7.6 -3 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 72 Human Functional pEC50 = 7.6 7.6 -3 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 72 Human Functional pEC50 = 7.6 7.6 -3 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 197507 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 197507 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 197827 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 197827 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 56804 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 56804 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 159399 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 159399 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 138342 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 138342 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 138342 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 102503 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 102503 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 102503 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 183717 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 183717 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 183717 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 183666 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 183666 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 183666 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 72 Human Functional pEC50 = 7.6 7.6 -3 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 72 Human Functional pEC50 = 7.6 7.6 -3 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 72 Human Functional pEC50 = 7.6 7.6 -3 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 72 Human Functional pEC50 = 7.6 7.6 -3 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 32 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 32 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 32 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 64594 None 15 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 64594 None 15 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 138342 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 138342 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 138342 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 147912 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 147912 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 151331 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 151331 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 183789 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 183789 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 183789 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 120660 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 120660 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 120660 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 153017 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 153017 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 79573 None 2 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 79573 None 2 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 107357 None 3 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 107357 None 3 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 108543 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 108543 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 207079 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 207079 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 207388 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 207388 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
70681342 74468 None 1 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 74468 None 1 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 74468 None 1 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 176448 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 176448 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 176448 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 161054 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 161054 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 161054 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 214067 None 2 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 214067 None 2 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 161054 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 161054 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 161054 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 83433 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 83433 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 89064 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 89064 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 89064 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 183635 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 183635 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 183635 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
162658153 183685 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 183685 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 183685 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 183789 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 183789 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 183789 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 12462 None 1 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 12462 None 1 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 12462 None 1 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 198490 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 198490 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 198779 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 198779 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 197303 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 197303 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 88 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 88 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 88 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 88 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 172877 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 172877 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 183635 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 183635 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 183635 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
162658153 183685 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 183685 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 183685 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 199903 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 199903 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 161108 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 161108 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 161108 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 200128 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 200128 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 183704 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 183704 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 183704 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 95754 None 16 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 95754 None 16 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 196833 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 196833 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 198635 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 198635 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
162660358 183704 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 183704 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 183704 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 161108 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 161108 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 161108 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
3568128 192933 None 1 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 192933 None 1 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 192933 None 1 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 192933 None 1 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 192933 None 1 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 192933 None 1 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 154431 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 154431 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 89108 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 89108 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 89108 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 158757 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 158757 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 187191 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 187191 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 197213 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 197213 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 138356 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 138356 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 138356 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 138356 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 138356 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 138356 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 156048 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 156048 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 83443 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 83443 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 91109 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 91109 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 161125 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 161125 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 161125 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 49 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 49 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 49 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 49 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 193216 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 193216 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 123069 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 123069 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 205473 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 205473 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 161125 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 161125 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 161125 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 49 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 49 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 49 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 49 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 193027 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 193027 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 193027 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 84769 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 84769 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 183621 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 183621 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 183621 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 193013 None 2 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 193013 None 2 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 193013 None 2 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 193027 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 193027 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 193027 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 183621 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 183621 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 183621 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 193013 None 2 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 193013 None 2 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 193013 None 2 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 120647 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 120647 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 120647 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 176373 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 176373 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 176373 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 12705 None 2 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 12705 None 2 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 12705 None 2 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 192757 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 192757 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 192757 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 202018 None 1 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 202018 None 1 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 12552 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 12552 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 12552 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 158642 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 158642 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 176373 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 176373 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 176373 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 198403 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 198403 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 192959 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 192959 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 192959 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 192861 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 192861 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 192861 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 192861 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 192861 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 192861 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 192959 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 192959 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 192959 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 87306 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 87306 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 191997 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 191997 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 137608 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 137608 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 120659 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 120659 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 120659 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 91083 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 91083 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 91092 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 91092 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 12460 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 12460 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 12460 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 176566 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 176566 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 176566 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 62605 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 62605 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 64181 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 64181 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 64309 None 4 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 64309 None 4 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 104880 None 75 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 104880 None 75 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 180904 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 180904 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 64309 None 4 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 64309 None 4 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 138346 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 138346 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 138346 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 138360 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 138360 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 138360 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 145240 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 145240 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 150696 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 150696 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 153833 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 153833 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 138360 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 138360 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 138360 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 89126 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 89126 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 89126 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 89127 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 89127 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 89127 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 12650 None 2 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 12650 None 2 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 12650 None 2 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 12706 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 12706 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 12706 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 199902 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 199902 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 51 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 51 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 51 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 51 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 51 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 120670 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 120670 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 120670 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 138346 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 138346 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 138346 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 51 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 51 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 51 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 51 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 51 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 12547 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 12547 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 12547 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 51 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 51 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 51 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 51 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 51 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 133606 None 33 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 133606 None 33 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 138351 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 138351 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 138351 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 138351 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 138351 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 138351 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 18 Human Functional pEC50 = 8.4 8.4 -2 4
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 18 Human Functional pEC50 = 8.4 8.4 -2 4
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 18 Human Functional pEC50 = 8.4 8.4 -2 4
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 62632 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 62632 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 94827 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 94827 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 94858 None 3 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 94858 None 3 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 143067 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 143067 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 89056 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 89056 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 89056 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 12623 None 1 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 12623 None 1 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 12623 None 1 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 198576 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 198576 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 198491 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 198491 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 157842 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 157842 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 193347 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 193347 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 138346 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 138346 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 138346 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 26 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 26 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 26 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 7 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 7 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 7 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 7 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 7 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 7 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 192757 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 192757 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 192757 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
54585653 61465 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 61465 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 87306 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 87306 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 12551 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 12551 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 12551 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 12432 None 1 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 12432 None 1 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 12432 None 1 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 183677 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 183677 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 183677 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 161000 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 161000 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 161000 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
137629241 161000 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 161000 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 161000 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 74485 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 74485 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 74485 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 192995 None 2 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 192995 None 2 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 192995 None 2 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
137629785 161186 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 161186 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 161186 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 138350 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 138350 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 138350 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
137629785 161186 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 161186 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 161186 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 192995 None 2 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 192995 None 2 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 192995 None 2 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 138350 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 138350 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 138350 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 176421 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 176421 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 176421 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
44622848 193347 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 193347 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 198958 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 198958 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 187190 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 187190 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 187231 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 187231 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 193313 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 193313 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 205452 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 205452 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 183695 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 183695 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 183695 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
122442270 138346 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 138346 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 138346 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 148566 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 148566 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 61458 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 61458 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 171478 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 171478 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 175228 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 175228 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 158605 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 158605 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
155534560 176421 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 176421 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 176421 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 157960 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 157960 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 164758 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 164758 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 62980 None 3 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 62980 None 3 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 130169 None 21 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 130169 None 21 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 79574 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 79574 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
1400243 94756 None 101 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 94756 None 101 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 198182 None 1 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 198182 None 1 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
45484896 198592 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 198592 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 77768 None 6 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 77768 None 6 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 120655 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 120655 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 120655 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 91100 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 91100 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 159532 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 159532 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 192863 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 192863 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 192863 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 164758 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 164758 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
58911666 91091 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 91091 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 183695 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 183695 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 183695 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 198881 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 198881 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 111671 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 111671 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 164454 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 164454 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 91090 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 91090 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 61459 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 61459 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 74461 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 74461 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 74461 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 12527 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 12527 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 12527 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 91111 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 91111 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 159015 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 159015 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 197734 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 197734 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
168295067 193022 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 193022 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 193022 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 193022 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 193022 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 193022 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 199289 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 199289 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 130169 None 21 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 130169 None 21 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 187258 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 187258 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 74474 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 74474 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 74474 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 137596 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 137596 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 12562 None 1 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 12562 None 1 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 12562 None 1 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 64594 None 15 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 64594 None 15 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 73981 None 65 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 73981 None 65 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 73981 None 65 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 176545 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 176545 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 176545 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 193011 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 193011 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 193011 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 193011 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 193011 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 193011 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 91086 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 91086 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 138343 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 138343 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 138343 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
122442266 138343 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 138343 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 138343 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 197780 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 197780 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 197304 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 197304 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 56800 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 56800 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 136354 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 136354 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 120672 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 120672 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 120672 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 187192 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 187192 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 159624 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 159624 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 85016 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 85016 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 56848 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 56848 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
168272608 192793 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 192793 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 192793 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 8017 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 8017 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
137635711 156065 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 156065 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
168268703 192776 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 192776 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 192776 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 61453 None 33 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 61453 None 33 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 192793 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 192793 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 192793 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 74473 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 74473 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 74473 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 156318 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 156318 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 156751 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 156751 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 138352 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 138352 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 138352 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
122442281 138352 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 138352 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 138352 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 145126 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 145126 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 192776 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 192776 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 192776 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 111669 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 111669 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 94859 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 94859 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 146792 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 146792 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
10329912 62551 None 8 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 62551 None 8 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 106197 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 106197 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 161790 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 161790 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 192858 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 192858 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 192858 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
137644936 161221 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 161221 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 161221 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 85302 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 85302 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 91102 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 91102 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 62632 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 62632 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 63485 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 63485 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 120667 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 120667 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 120667 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 89070 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 89070 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 89070 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 192794 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 192794 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 192794 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 192794 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 192794 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 192794 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 72609 None 9 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 72609 None 9 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 87249 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 87249 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 61454 None 28 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 61454 None 28 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 61454 None 28 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 61454 None 28 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 205123 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 205123 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 18 Human Functional pEC50 = 8.3 8.3 -2 4
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 18 Human Functional pEC50 = 8.3 8.3 -2 4
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 18 Human Functional pEC50 = 8.3 8.3 -2 4
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 78328 None 3 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 78328 None 3 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 78328 None 3 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 18 Human Functional pEC50 = 8.3 8.3 -2 4
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 18 Human Functional pEC50 = 8.3 8.3 -2 4
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 18 Human Functional pEC50 = 8.3 8.3 -2 4
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 78328 None 3 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 78328 None 3 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 78328 None 3 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 51 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 12444 None 2 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 12444 None 2 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 12444 None 2 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 136132 None 2 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 136132 None 2 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 8443 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 8443 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 205522 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 205522 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 183659 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 183659 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 183659 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 183745 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 183745 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 183745 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 199861 None 47 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 199861 None 47 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 192858 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 192858 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 192858 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 192790 None 1 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 192790 None 1 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 192790 None 1 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 197824 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 197824 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 161225 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 161225 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 161225 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 192790 None 1 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 192790 None 1 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 192790 None 1 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 176655 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 176655 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 176655 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 161225 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 161225 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 161225 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 89060 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 89060 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 89060 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 183659 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 183659 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 183659 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 183745 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 183745 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 183745 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 187230 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 187230 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 156920 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 156920 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 120456 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 120456 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 192983 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 192983 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 192983 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 138350 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 138350 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 138350 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 62551 None 8 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 62551 None 8 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 176655 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 176655 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 176655 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 87310 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 87310 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 192913 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 192913 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 192913 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 199290 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 199290 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 83490 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 83490 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 12521 None 1 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 12521 None 1 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 12521 None 1 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 192983 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 192983 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 192983 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 138350 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 138350 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 138350 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 87310 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 87310 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 192913 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 192913 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 192913 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 123432 None 8 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 123432 None 8 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 77781 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 77781 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 84687 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 84687 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 89111 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 89111 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 89111 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 201545 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 201545 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 156214 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 156214 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 72 Human Functional pEC50 = 7.4 7.4 -3 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 72 Human Functional pEC50 = 7.4 7.4 -3 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 72 Human Functional pEC50 = 7.4 7.4 -3 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 72 Human Functional pEC50 = 7.4 7.4 -3 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 192791 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 192791 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 192791 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 158782 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 158782 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 138355 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 138355 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 138355 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 158782 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 158782 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 138355 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 138355 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 138355 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 8442 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 8442 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 72 Human Functional pEC50 = 7.4 7.4 -3 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 72 Human Functional pEC50 = 7.4 7.4 -3 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 72 Human Functional pEC50 = 7.4 7.4 -3 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 72 Human Functional pEC50 = 7.4 7.4 -3 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 192791 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 192791 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 192791 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 204934 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 204934 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 176422 None 5 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 176422 None 5 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 176422 None 5 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 183740 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 183740 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 183740 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 192789 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 192789 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 192789 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 183740 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 183740 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 183740 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 192789 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 192789 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 192789 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 192852 None 1 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 192852 None 1 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 192852 None 1 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 176422 None 5 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 176422 None 5 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 176422 None 5 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 192852 None 1 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 192852 None 1 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 192852 None 1 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 199248 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 199248 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 202708 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 202708 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 157391 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 157391 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 159565 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 159565 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 56799 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 56799 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 84837 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 84837 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 198513 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 198513 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 187198 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 187198 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 192985 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 192985 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 192985 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 155986 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 155986 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 192844 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 192844 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 192844 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 192844 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 192844 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 192844 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 192985 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 192985 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 192985 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 197552 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 197552 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 187297 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 187297 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 197391 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 197391 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 157778 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 157778 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 158940 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 158940 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
11312820 136334 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 136334 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 193039 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 193039 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 193039 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 91110 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 91110 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 197696 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 197696 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 138361 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 138361 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 138361 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 137366 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 137366 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 61455 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 61455 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 193039 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 193039 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 193039 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 196821 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 196821 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
11483068 84812 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 84812 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 12649 None 1 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 12649 None 1 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 12649 None 1 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 138361 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 138361 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 138361 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 100596 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 100596 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 197817 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 197817 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 197170 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 197170 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 197170 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 197170 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 136402 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 136402 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 91094 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 91094 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 56803 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 56803 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 157630 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 157630 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 64109 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 64109 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 64883 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 64883 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 180245 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 180245 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 182403 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 182403 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 12437 None 1 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 12437 None 1 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 12437 None 1 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 12467 None 6 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 12467 None 6 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 12467 None 6 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 183759 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 183759 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 183759 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 183759 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 183759 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 183759 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 12655 None 2 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 12655 None 2 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 12655 None 2 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 56797 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 56797 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 72055 None 2 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 72055 None 2 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 120789 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 120789 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 164753 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 164753 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 193080 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 193080 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 192880 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 192880 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 192880 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 154697 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 154697 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 192880 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 192880 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 192880 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 199986 None 2 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 199986 None 2 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 158361 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 158361 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 161076 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 161076 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 161076 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 207823 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 207823 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
137630488 161076 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 161076 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 161076 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 77798 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 77798 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 70300 None 19 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 70300 None 19 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 70300 None 19 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 70300 None 19 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 70300 None 19 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 192622 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 192622 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 138342 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 138342 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 138342 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 111668 None 1 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 111668 None 1 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 197369 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 197369 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 138342 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 138342 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 138342 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 141978 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 141978 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 120643 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 120643 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 120643 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 166006 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 166006 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 18 Human Functional pEC50 = 7.3 7.3 -2 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 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 18 Human Functional pEC50 = 7.3 7.3 -2 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 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 18 Human Functional pEC50 = 7.3 7.3 -2 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 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmc.2007.10.100
137629973 161027 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 161027 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 161027 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 161035 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 161035 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 161035 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 176531 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 176531 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 176531 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 176531 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 176531 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 176531 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 161027 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 161027 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 161027 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 200112 None 45 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 200112 None 45 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 161035 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 161035 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 161035 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 156237 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 156237 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
11233293 84162 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 84162 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 84797 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 84797 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 168917 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 168917 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 160991 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 160991 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 160991 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 91085 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 91085 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 91103 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 91103 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 74459 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 74459 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 74459 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 160991 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 160991 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 160991 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 91093 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 91093 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 183703 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 183703 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 183703 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 196789 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 196789 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 63283 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 63283 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 183703 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 183703 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 183703 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 187259 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 187259 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 78185 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 78185 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 56850 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 56850 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
137658409 159682 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 159682 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
137632069 156388 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 156388 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
11361103 91105 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 91105 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 89097 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 89097 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 89097 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 159257 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 159257 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 72225 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 72225 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 176548 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 176548 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 176548 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 136974 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 136974 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 91117 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 91117 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 12546 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 12546 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 12546 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 157154 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 157154 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 157700 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 157700 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 62528 None 4 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 62528 None 4 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 166071 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 166071 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 183690 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 183690 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 183690 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 183690 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 183690 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 183690 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 181809 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 181809 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 62499 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 62499 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 122772 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 122772 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 154857 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 154857 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 147226 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 147226 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 148123 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 148123 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 183623 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 183623 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 183623 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 199319 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 199319 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 72712 None 3 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 72712 None 3 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 204961 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 204961 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 183623 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 183623 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 183623 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 120671 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 120671 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 120671 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 91084 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 91084 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 191025 None 1 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 191025 None 1 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 191025 None 1 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 191025 None 1 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 176548 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 176548 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 176548 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 199329 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 199329 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 192770 None 1 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 192770 None 1 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 192770 None 1 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 138356 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 138356 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 138356 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 192770 None 1 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 192770 None 1 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 192770 None 1 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 138356 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 138356 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 138356 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 91108 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 91108 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 161208 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 161208 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 161208 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 200146 None 2 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 200146 None 2 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 161208 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 161208 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 161208 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 89061 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 89061 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 89061 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 197669 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 197669 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 214064 None 31 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 214064 None 31 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 137040 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 137040 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 120673 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 120673 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 120673 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 56801 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 intracellular calcium release by FLIPR assay
ChEMBL 231 2 2 5 0.8 CCNc1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
CHEMBL1643674 56801 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 intracellular calcium release by FLIPR assay
ChEMBL 231 2 2 5 0.8 CCNc1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
137654926 158701 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 350 3 1 4 3.6 Cc1nc(-c2cccc3ccccc23)oc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4093250 158701 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 350 3 1 4 3.6 Cc1nc(-c2cccc3ccccc23)oc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4749189 214064 None 31 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 214064 None 31 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
134137441 142493 None 0 Human Functional pEC50 = 7.2 7.2 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 230 2 1 2 2.4 CCCc1ccc2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3890492 142493 None 0 Human Functional pEC50 = 7.2 7.2 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 230 2 1 2 2.4 CCCc1ccc2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
134139670 146165 None 0 Human Functional pEC50 = 7.2 7.2 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)CC[C@@H]1CCNCCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3919861 146165 None 0 Human Functional pEC50 = 7.2 7.2 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)CC[C@@H]1CCNCCCN21 10.1016/j.bmcl.2016.11.016
15640062 148374 None 0 Human Functional pEC50 = 7.2 7.2 -1 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 Cc1cccc2c1N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3937394 148374 None 0 Human Functional pEC50 = 7.2 7.2 -1 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 Cc1cccc2c1N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
132820209 150241 None 0 Human Functional pEC50 = 6.2 6.2 1 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 COc1ccc2c(c1)CC[C@@H]1CNCCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3952329 150241 None 0 Human Functional pEC50 = 6.2 6.2 1 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 COc1ccc2c(c1)CC[C@@H]1CNCCCN21 10.1016/j.bmcl.2016.11.016
10679289 207210 None 2 Rat Functional pEC50 = 6.2 6.2 - 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)Cn1ccc2ccc(F)cc21 10.1021/jm970030l
CHEMBL92656 207210 None 2 Rat Functional pEC50 = 6.2 6.2 - 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)Cn1ccc2ccc(F)cc21 10.1021/jm970030l
19036356 207278 None 0 Rat Functional pEC50 = 6.2 6.2 - 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 230 2 1 2 2.5 CC(N)Cn1ccc2c1-c1cc(F)ccc1C2 10.1021/jm970030l
CHEMBL93154 207278 None 0 Rat Functional pEC50 = 6.2 6.2 - 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 230 2 1 2 2.5 CC(N)Cn1ccc2c1-c1cc(F)ccc1C2 10.1021/jm970030l
10705346 207932 None 0 Rat Functional pEC50 = 5.2 5.2 - 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 COc1cccc2c1-c1c(ccn1CC(C)N)C2 10.1021/jm970030l
CHEMBL96876 207932 None 0 Rat Functional pEC50 = 5.2 5.2 - 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 COc1cccc2c1-c1c(ccn1CC(C)N)C2 10.1021/jm970030l
44573155 189159 None 0 Human Functional pEC50 = 6.2 6.2 -6 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 4 2 3 1.1 O=S(=O)(NCC1CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL511044 189159 None 0 Human Functional pEC50 = 6.2 6.2 -6 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 4 2 3 1.1 O=S(=O)(NCC1CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
10898996 187260 None 2 Human Functional pEC50 = 6.2 6.2 - 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 161 3 1 1 2.0 CNC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
CHEMBL492700 187260 None 2 Human Functional pEC50 = 6.2 6.2 - 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 161 3 1 1 2.0 CNC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
58911579 91096 None 0 Human Functional pEC50 = 7.2 7.2 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 242 1 1 2 1.5 O=C1c2c(cccc2C2CC2)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397891 91096 None 0 Human Functional pEC50 = 7.2 7.2 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 242 1 1 2 1.5 O=C1c2c(cccc2C2CC2)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
45484946 196765 None 0 Human Functional pEC50 = 7.2 7.2 - 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 380 4 1 5 2.4 C[C@@H]1CNCCN1c1cc(=O)n(C)c(CCc2ccccc2C(F)(F)F)n1 10.1016/j.bmcl.2009.07.133
CHEMBL565351 196765 None 0 Human Functional pEC50 = 7.2 7.2 - 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 380 4 1 5 2.4 C[C@@H]1CNCCN1c1cc(=O)n(C)c(CCc2ccccc2C(F)(F)F)n1 10.1016/j.bmcl.2009.07.133
18735305 204933 None 0 Human Functional pEC50 = 7.2 7.2 -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 320 2 1 2 2.1 C[C@H](N)CN1CCc2cc(F)c(I)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL76301 204933 None 0 Human Functional pEC50 = 7.2 7.2 -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 320 2 1 2 2.1 C[C@H](N)CN1CCc2cc(F)c(I)cc21 10.1016/j.bmcl.2003.05.001
118733760 120638 None 1 Human Functional pEC50 = 6.2 6.2 3 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 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416032 120638 None 1 Human Functional pEC50 = 6.2 6.2 3 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 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546869 120638 None 1 Human Functional pEC50 = 6.2 6.2 3 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 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
53317923 56846 None 0 Human Functional pEC50 = 7.2 7.2 -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 365 4 1 7 1.7 COc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
CHEMBL1643853 56846 None 0 Human Functional pEC50 = 7.2 7.2 -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 365 4 1 7 1.7 COc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
156013985 177175 None 0 Human Functional pEC50 = 7.2 7.2 18 2
Agonist activity at recombinant human 5HT2C receptor expressed in CHO cells assessed as accumulation of inositol phosphate measured after 30 mins in presence of [3H]inositol by scintillation counter methodAgonist activity at recombinant human 5HT2C receptor expressed in CHO cells assessed as accumulation of inositol phosphate measured after 30 mins in presence of [3H]inositol by scintillation counter method
ChEMBL 230 0 1 2 1.8 C1=CC2CNCCN3C[C@@H]4CCC[C@@H]4C(=C1)C23 10.1016/j.bmcl.2019.126929
CHEMBL4634785 177175 None 0 Human Functional pEC50 = 7.2 7.2 18 2
Agonist activity at recombinant human 5HT2C receptor expressed in CHO cells assessed as accumulation of inositol phosphate measured after 30 mins in presence of [3H]inositol by scintillation counter methodAgonist activity at recombinant human 5HT2C receptor expressed in CHO cells assessed as accumulation of inositol phosphate measured after 30 mins in presence of [3H]inositol by scintillation counter method
ChEMBL 230 0 1 2 1.8 C1=CC2CNCCN3C[C@@H]4CCC[C@@H]4C(=C1)C23 10.1016/j.bmcl.2019.126929
168282376 192886 None 0 Human Functional pEC50 = 7.2 7.2 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 360 1 3 2 4.0 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5189339 192886 None 0 Human Functional pEC50 = 7.2 7.2 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 360 1 3 2 4.0 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222002 192886 None 0 Human Functional pEC50 = 7.2 7.2 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 360 1 3 2 4.0 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
168282376 192886 None 0 Human Functional pEC50 = 7.2 7.2 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 360 1 3 2 4.0 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5189339 192886 None 0 Human Functional pEC50 = 7.2 7.2 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 360 1 3 2 4.0 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222002 192886 None 0 Human Functional pEC50 = 7.2 7.2 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 360 1 3 2 4.0 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
46228435 200147 None 0 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 218 1 1 5 0.9 Cc1cc2c(N3CCNCC3)ncnc2o1 10.1016/j.bmcl.2009.10.112
CHEMBL596328 200147 None 0 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 218 1 1 5 0.9 Cc1cc2c(N3CCNCC3)ncnc2o1 10.1016/j.bmcl.2009.10.112
45484681 197095 None 0 Human Functional pEC50 = 5.2 5.2 - 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 280 2 1 5 0.9 N#Cc1ccc(Cn2nc3c(cc2=O)CCNCC3)cc1 10.1016/j.bmcl.2009.07.063
CHEMBL567587 197095 None 0 Human Functional pEC50 = 5.2 5.2 - 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 280 2 1 5 0.9 N#Cc1ccc(Cn2nc3c(cc2=O)CCNCC3)cc1 10.1016/j.bmcl.2009.07.063
118733780 120640 None 0 Human Functional pEC50 = 6.2 6.2 7 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 6 1 3 2.4 COCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416042 120640 None 0 Human Functional pEC50 = 6.2 6.2 7 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 6 1 3 2.4 COCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546871 120640 None 0 Human Functional pEC50 = 6.2 6.2 7 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 6 1 3 2.4 COCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
137630996 161139 None 0 Human Functional pEC50 = 6.2 6.2 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 329 7 0 3 4.1 COc1ccccc1CN(C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4079976 161139 None 0 Human Functional pEC50 = 6.2 6.2 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 329 7 0 3 4.1 COc1ccccc1CN(C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4117263 161139 None 0 Human Functional pEC50 = 6.2 6.2 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 329 7 0 3 4.1 COc1ccccc1CN(C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
137630996 161139 None 0 Human Functional pEC50 = 6.2 6.2 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 329 7 0 3 4.1 COc1ccccc1CN(C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4079976 161139 None 0 Human Functional pEC50 = 6.2 6.2 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 329 7 0 3 4.1 COc1ccccc1CN(C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4117263 161139 None 0 Human Functional pEC50 = 6.2 6.2 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 329 7 0 3 4.1 COc1ccccc1CN(C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
137646111 157918 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 356 2 1 4 3.7 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CCC(O)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4084377 157918 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 356 2 1 4 3.7 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CCC(O)CC1 10.1021/acs.jmedchem.7b00385
137660422 159172 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 374 2 1 4 4.2 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCc2[nH]cnc2C1 10.1021/acs.jmedchem.7b00385
CHEMBL4098357 159172 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 374 2 1 4 4.2 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCc2[nH]cnc2C1 10.1021/acs.jmedchem.7b00385
10017556 161878 None 0 Human Functional pEC50 = 7.2 7.2 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 297 2 1 2 3.5 CC(C)Oc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL415029 161878 None 0 Human Functional pEC50 = 7.2 7.2 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 297 2 1 2 3.5 CC(C)Oc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
168286640 192928 None 0 Human Functional pEC50 = 7.2 7.2 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 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5194223 192928 None 0 Human Functional pEC50 = 7.2 7.2 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 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222252 192928 None 0 Human Functional pEC50 = 7.2 7.2 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 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL4802359 214062 None 1 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 None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
118733768 120646 None 0 Human Functional pEC50 = 6.2 6.2 - 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
CHEMBL3416036 120646 None 0 Human Functional pEC50 = 6.2 6.2 - 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
CHEMBL3546891 120646 None 0 Human Functional pEC50 = 6.2 6.2 - 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
CHEMBL4795286 214072 None 0 Human Functional pEC50 = 6.2 6.2 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 Oc1cccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL4803900 214072 None 0 Human Functional pEC50 = 6.2 6.2 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 Oc1cccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
44431699 88289 None 0 Rat Functional pEC50 = 6.2 6.2 -5 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 315 4 1 6 1.7 Cc1noc(Cc2c3c(c(C[C@@H](C)N)c4c2OCC4)OCC3)n1 10.1016/j.bmcl.2007.03.073
CHEMBL234837 88289 None 0 Rat Functional pEC50 = 6.2 6.2 -5 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 315 4 1 6 1.7 Cc1noc(Cc2c3c(c(C[C@@H](C)N)c4c2OCC4)OCC3)n1 10.1016/j.bmcl.2007.03.073
168286640 192928 None 0 Human Functional pEC50 = 7.2 7.2 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 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5194223 192928 None 0 Human Functional pEC50 = 7.2 7.2 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 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222252 192928 None 0 Human Functional pEC50 = 7.2 7.2 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 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL4802359 214062 None 1 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 None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL4795286 214072 None 0 Human Functional pEC50 = 6.2 6.2 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 Oc1cccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL4803900 214072 None 0 Human Functional pEC50 = 6.2 6.2 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 Oc1cccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
44572256 12553 None 0 Human Functional pEC50 = 6.2 6.2 - 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 241 3 1 1 3.6 NC[C@H]1C[C@@H]1c1cccc(-c2ccc(F)cc2)c1 10.1021/jm801354e
CHEMBL1186705 12553 None 0 Human Functional pEC50 = 6.2 6.2 - 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 241 3 1 1 3.6 NC[C@H]1C[C@@H]1c1cccc(-c2ccc(F)cc2)c1 10.1021/jm801354e
CHEMBL474950 12553 None 0 Human Functional pEC50 = 6.2 6.2 - 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 241 3 1 1 3.6 NC[C@H]1C[C@@H]1c1cccc(-c2ccc(F)cc2)c1 10.1021/jm801354e
44573217 187339 None 0 Human Functional pEC50 = 6.2 6.2 -10 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 302 3 2 3 2.2 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL493152 187339 None 0 Human Functional pEC50 = 6.2 6.2 -10 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 302 3 2 3 2.2 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
11221167 84680 None 0 Human Functional pEC50 = 8.2 8.2 25 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)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL222514 84680 None 0 Human Functional pEC50 = 8.2 8.2 25 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)[C@@H]2CNCCN12 10.1021/jm0612968
44572178 12561 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 175 2 1 1 2.4 Cc1cccc([C@H]2C[C@@H]2CN)c1C 10.1021/jm801354e
CHEMBL1186736 12561 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 175 2 1 1 2.4 Cc1cccc([C@H]2C[C@@H]2CN)c1C 10.1021/jm801354e
CHEMBL475642 12561 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 175 2 1 1 2.4 Cc1cccc([C@H]2C[C@@H]2CN)c1C 10.1021/jm801354e
44573229 172676 None 0 Human Functional pEC50 = 8.2 8.2 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 305 2 1 3 2.3 O=S(=O)(c1ccc2c(c1)CCNCC2)c1ccccc1F 10.1016/j.bmcl.2009.02.071
CHEMBL449999 172676 None 0 Human Functional pEC50 = 8.2 8.2 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 305 2 1 3 2.3 O=S(=O)(c1ccc2c(c1)CCNCC2)c1ccccc1F 10.1016/j.bmcl.2009.02.071
137641125 157010 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 316 3 1 6 3.2 CCn1nc(-c2cccc3ccncc23)cc1-c1ccc(N)nn1 10.1021/acs.jmedchem.7b00385
CHEMBL4073363 157010 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 316 3 1 6 3.2 CCn1nc(-c2cccc3ccncc23)cc1-c1ccc(N)nn1 10.1021/acs.jmedchem.7b00385
10105208 62499 None 0 Human Functional pEC50 = 8.2 8.2 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 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178124 62499 None 0 Human Functional pEC50 = 8.2 8.2 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 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1016/j.bmcl.2004.12.080
9990808 122772 None 0 Human Functional pEC50 = 8.2 8.2 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 213 0 1 1 2.7 CC1CNCCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL360492 122772 None 0 Human Functional pEC50 = 8.2 8.2 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 213 0 1 1 2.7 CC1CNCCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
122442309 138347 None 0 Human Functional pEC50 = 8.1 8.1 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 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769828 138347 None 0 Human Functional pEC50 = 8.1 8.1 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 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771383 138347 None 0 Human Functional pEC50 = 8.1 8.1 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 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
135414348 72809 None 2 Rat Functional pEC50 = 8.1 8.1 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 2 2 4 1.4 Cc1c(O)ccc2cnn(C[C@H](C)N)c12 10.1021/jm050663x
CHEMBL200104 72809 None 2 Rat Functional pEC50 = 8.1 8.1 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 2 2 4 1.4 Cc1c(O)ccc2cnn(C[C@H](C)N)c12 10.1021/jm050663x
3906894 101979 None 24 Human Functional pEC50 = 8.1 8.1 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 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1021/jm301656h
CHEMBL301466 101979 None 24 Human Functional pEC50 = 8.1 8.1 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 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1021/jm301656h
122442309 138347 None 0 Human Functional pEC50 = 8.1 8.1 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 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769828 138347 None 0 Human Functional pEC50 = 8.1 8.1 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 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771383 138347 None 0 Human Functional pEC50 = 8.1 8.1 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 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
3906894 101979 None 24 Human Functional pEC50 = 8.1 8.1 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 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1021/jm301656h
CHEMBL301466 101979 None 24 Human Functional pEC50 = 8.1 8.1 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 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1021/jm301656h
134265675 164367 None 0 Human Functional pEC50 = 8.1 8.1 13 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 Fc1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
CHEMBL4212834 164367 None 0 Human Functional pEC50 = 8.1 8.1 13 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 Fc1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
168273228 192799 None 0 Human Functional pEC50 = 8.1 8.1 -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 354 4 3 5 3.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(O)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5178632 192799 None 0 Human Functional pEC50 = 8.1 8.1 -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 354 4 3 5 3.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(O)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221423 192799 None 0 Human Functional pEC50 = 8.1 8.1 -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 354 4 3 5 3.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(O)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
11658860 2344 None 51 Human Functional pEC50 = 8.1 8.1 1 11
Agonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in presence of [3H]inositol by scintillation counter methodAgonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in presence of [3H]inositol by scintillation counter method
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
2941 2344 None 51 Human Functional pEC50 = 8.1 8.1 1 11
Agonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in presence of [3H]inositol by scintillation counter methodAgonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in presence of [3H]inositol by scintillation counter method
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
4374 2344 None 51 Human Functional pEC50 = 8.1 8.1 1 11
Agonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in presence of [3H]inositol by scintillation counter methodAgonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in presence of [3H]inositol by scintillation counter method
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
CHEMBL360328 2344 None 51 Human Functional pEC50 = 8.1 8.1 1 11
Agonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in presence of [3H]inositol by scintillation counter methodAgonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in presence of [3H]inositol by scintillation counter method
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
DB04871 2344 None 51 Human Functional pEC50 = 8.1 8.1 1 11
Agonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in presence of [3H]inositol by scintillation counter methodAgonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in presence of [3H]inositol by scintillation counter method
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
122442250 138344 None 0 Human Functional pEC50 = 8.1 8.1 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 138344 None 0 Human Functional pEC50 = 8.1 8.1 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 138344 None 0 Human Functional pEC50 = 8.1 8.1 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
12986494 198682 None 2 Human Functional pEC50 = 8.1 8.1 - 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)N1CCNCC1CN2 10.1016/s0960-894x(00)00400-5
CHEMBL58009 198682 None 2 Human Functional pEC50 = 8.1 8.1 - 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)N1CCNCC1CN2 10.1016/s0960-894x(00)00400-5
27559 203409 None 11 Human Functional pEC50 = 8.1 8.1 -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 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
CHEMBL6557 203409 None 11 Human Functional pEC50 = 8.1 8.1 -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 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
27559 203409 None 11 Human Functional pEC50 = 8.1 8.1 -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 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
CHEMBL6557 203409 None 11 Human Functional pEC50 = 8.1 8.1 -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 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
122442250 138344 None 0 Human Functional pEC50 = 8.1 8.1 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 138344 None 0 Human Functional pEC50 = 8.1 8.1 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 138344 None 0 Human Functional pEC50 = 8.1 8.1 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
1355 2011 None 88 Human Functional pEC50 = 8.1 8.1 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0709034
142 2011 None 88 Human Functional pEC50 = 8.1 8.1 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0709034
CHEMBL478 2011 None 88 Human Functional pEC50 = 8.1 8.1 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0709034
DB12110 2011 None 88 Human Functional pEC50 = 8.1 8.1 4 6
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 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0709034
11658860 2344 None 51 Human Functional pEC50 = 8.1 8.1 1 11
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 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
2941 2344 None 51 Human Functional pEC50 = 8.1 8.1 1 11
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 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
4374 2344 None 51 Human Functional pEC50 = 8.1 8.1 1 11
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 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
CHEMBL360328 2344 None 51 Human Functional pEC50 = 8.1 8.1 1 11
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 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
DB04871 2344 None 51 Human Functional pEC50 = 8.1 8.1 1 11
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 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
11447552 62528 None 4 Human Functional pEC50 = 8.1 8.1 30 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 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
CHEMBL178231 62528 None 4 Human Functional pEC50 = 8.1 8.1 30 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 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
10036629 64637 None 0 Human Functional pEC50 = 8.1 8.1 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 225 1 1 2 2.6 COc1cc2c(cc1Cl)C(C)CNCC2 10.1021/jm0709034
CHEMBL181787 64637 None 0 Human Functional pEC50 = 8.1 8.1 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 225 1 1 2 2.6 COc1cc2c(cc1Cl)C(C)CNCC2 10.1021/jm0709034
24773816 94856 None 0 Human Functional pEC50 = 8.1 8.1 12 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
CHEMBL253805 94856 None 0 Human Functional pEC50 = 8.1 8.1 12 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
24773895 94857 None 0 Human Functional pEC50 = 8.1 8.1 25 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
CHEMBL253806 94857 None 0 Human Functional pEC50 = 8.1 8.1 25 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
24773809 94882 None 0 Human Functional pEC50 = 8.1 8.1 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 C[C@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
CHEMBL254009 94882 None 0 Human Functional pEC50 = 8.1 8.1 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 C[C@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
168273228 192799 None 0