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Ligand source activities (1 row/activity)

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Ligand Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors UniProt IUPHAR Species p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
134265828 180646 0 5HT2C 5-HT2C receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 231 2 1 3 1.8 CCCc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4765074 180646 0 5HT2C 5-HT2C receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 231 2 1 3 1.8 CCCc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
5 134 60 5HT2C 5-HT2C receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
5202 134 60 5HT2C 5-HT2C receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
DB08839 134 60 5HT2C 5-HT2C receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
5 134 60 5HT2C 5-HT2C receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
5202 134 60 5HT2C 5-HT2C receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
DB08839 134 60 5HT2C 5-HT2C receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
46228438 193571 0 5HT2C 5-HT2C receptor Human 10.0 pEC50 = 10 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1OC1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL595195 193571 0 5HT2C 5-HT2C receptor Human 10.0 pEC50 = 10 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1OC1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
11949712 195745 0 5HT2C 5-HT2C receptor Human 10.0 pEC50 = 10 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL609306 195745 0 5HT2C 5-HT2C receptor Human 10.0 pEC50 = 10 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
134265616 163587 0 5HT2C 5-HT2C receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1016/j.bmcl.2021.127872
CHEMBL4213447 163587 0 5HT2C 5-HT2C receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1016/j.bmcl.2021.127872
134265616 163587 0 5HT2C 5-HT2C receptor Human 10.0 pEC50 = 10.0 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4213447 163587 0 5HT2C 5-HT2C receptor Human 10.0 pEC50 = 10.0 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
9901086 184954 21 5HT2C 5-HT2C receptor Human 10.0 pEC50 = 10.0 Binding
Agonist activity at 5HT2C receptor (unknown origin) relative to controlAgonist activity at 5HT2C receptor (unknown origin) relative to control
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm5019274
CHEMBL494947 184954 21 5HT2C 5-HT2C receptor Human 10.0 pEC50 = 10.0 Binding
Agonist activity at 5HT2C receptor (unknown origin) relative to controlAgonist activity at 5HT2C receptor (unknown origin) relative to control
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm5019274
134265620 163582 0 5HT2C 5-HT2C receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
CHEMBL4213379 163582 0 5HT2C 5-HT2C receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
134265620 163582 0 5HT2C 5-HT2C receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1016/j.bmcl.2021.127872
CHEMBL4213379 163582 0 5HT2C 5-HT2C receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1016/j.bmcl.2021.127872
5 134 60 5HT2C 5-HT2C receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5202 134 60 5HT2C 5-HT2C receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5 134 60 5HT2C 5-HT2C receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5202 134 60 5HT2C 5-HT2C receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5 134 60 5HT2C 5-HT2C receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5202 134 60 5HT2C 5-HT2C receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5 134 60 5HT2C 5-HT2C receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5202 134 60 5HT2C 5-HT2C receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5 134 60 5HT2C 5-HT2C receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
5202 134 60 5HT2C 5-HT2C receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
439280 119259 96 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
6971044 119259 96 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
CHEMBL350221 119259 96 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
5 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
5202 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.7b00584
134265627 163188 0 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 297 2 1 3 2.5 Fc1cccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)c1 10.1021/acsmedchemlett.8b00328
CHEMBL4208452 163188 0 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 297 2 1 3 2.5 Fc1cccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)c1 10.1021/acsmedchemlett.8b00328
5 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
5202 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
5 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
5202 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111626
CHEMBL4776557 180813 0 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 230 2 1 2 2.4 CCCc1cccc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
134147456 148832 0 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 230 2 1 2 2.4 CCCc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3947276 148832 0 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 230 2 1 2 2.4 CCCc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
16743289 59034 3 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell line
ChEMBL 200 2 1 2 2.1 NCCc1cn2c3c(cccc13)CCC2 10.1016/s0960-894x(00)00141-4
CHEMBL171774 59034 3 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell line
ChEMBL 200 2 1 2 2.1 NCCc1cn2c3c(cccc13)CCC2 10.1016/s0960-894x(00)00141-4
5 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
5202 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
439280 119259 96 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
6971044 119259 96 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
CHEMBL350221 119259 96 5HT2C 5-HT2C receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
10332474 59120 0 5HT2C 5-HT2C receptor Human 9.6 pEC50 = 9.6 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell line
ChEMBL 252 2 1 3 2.9 NCCc1cn2c3c(cc(Cl)cc13)SCC2 10.1016/s0960-894x(00)00141-4
CHEMBL172159 59120 0 5HT2C 5-HT2C receptor Human 9.6 pEC50 = 9.6 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell line
ChEMBL 252 2 1 3 2.9 NCCc1cn2c3c(cc(Cl)cc13)SCC2 10.1016/s0960-894x(00)00141-4
134152924 152708 0 5HT2C 5-HT2C receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 248 2 1 3 2.5 CCSc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3979806 152708 0 5HT2C 5-HT2C receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 248 2 1 3 2.5 CCSc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
5 134 60 5HT2C 5-HT2C receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
5202 134 60 5HT2C 5-HT2C receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
4106 2350 9 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2013.02.020
5358812 2350 9 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2013.02.020
89 2350 9 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2013.02.020
CHEMBL93240 2350 9 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2013.02.020
134265727 180910 0 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 245 2 1 3 2.0 CC(C)Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4777852 180910 0 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 245 2 1 3 2.0 CC(C)Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
76333762 84644 0 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at Homo sapiens (human) 5-HT2C receptor assessed as calcium mobilization by cell based assayAgonist activity at Homo sapiens (human) 5-HT2C receptor assessed as calcium mobilization by cell based assay
ChEMBL 248 0 1 2 3.6 Cc1c2n(c3c(C)c(Cl)ccc13)C(C)NCC2 10.1007/s00044-011-9615-3
CHEMBL2260569 84644 0 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at Homo sapiens (human) 5-HT2C receptor assessed as calcium mobilization by cell based assayAgonist activity at Homo sapiens (human) 5-HT2C receptor assessed as calcium mobilization by cell based assay
ChEMBL 248 0 1 2 3.6 Cc1c2n(c3c(C)c(Cl)ccc13)C(C)NCC2 10.1007/s00044-011-9615-3
5 134 60 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
5202 134 60 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
5 134 60 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assayAgonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b01835
5202 134 60 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assayAgonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b01835
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assayAgonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b01835
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assayAgonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b01835
146025687 182838 0 5HT2C 5-HT2C receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4779260 182838 0 5HT2C 5-HT2C receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803306 182838 0 5HT2C 5-HT2C receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
146025687 182838 0 5HT2C 5-HT2C receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4779260 182838 0 5HT2C 5-HT2C receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803306 182838 0 5HT2C 5-HT2C receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
134265735 180974 0 5HT2C 5-HT2C receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2cncc3c2CC[C@@H]2CNCCN32)cc1 10.1016/j.bmcl.2021.127872
CHEMBL4778570 180974 0 5HT2C 5-HT2C receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2cncc3c2CC[C@@H]2CNCCN32)cc1 10.1016/j.bmcl.2021.127872
46933845 15803 0 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor assessed as 5HT-induced calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor assessed as 5HT-induced calcium mobilization by FLIPR assay
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224034 15803 0 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor assessed as 5HT-induced calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor assessed as 5HT-induced calcium mobilization by FLIPR assay
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
44572751 12211 1 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL1186509 12211 1 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL467736 12211 1 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
134155852 150352 0 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 284 2 1 3 3.1 c1csc(Cc2cccc3c2CCC2CNCCN32)c1 10.1016/j.bmcl.2016.11.016
CHEMBL3959570 150352 0 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 284 2 1 3 3.1 c1csc(Cc2cccc3c2CCC2CNCCN32)c1 10.1016/j.bmcl.2016.11.016
18520432 151227 0 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 206 0 1 2 1.6 Fc1ccc2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3967107 151227 0 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 206 0 1 2 1.6 Fc1ccc2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL4646618 177166 0 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at 5HT2C receptor (unknown origin)Agonist activity at 5HT2C receptor (unknown origin)
ChEMBL 202 0 1 2 2.0 Cc1ccc2c3c1C(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
5 134 60 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5202 134 60 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5 134 60 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5202 134 60 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
DB08839 134 60 5HT2C 5-HT2C receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
122442263 137565 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769454 137565 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771393 137565 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
11949706 193641 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 359 4 1 4 3.4 C[C@@H]1CNCCN1c1ccc2c(n1)[C@@H](OCc1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.10.112
CHEMBL595645 193641 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 359 4 1 4 3.4 C[C@@H]1CNCCN1c1ccc2c(n1)[C@@H](OCc1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.10.112
11695000 88402 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337490 88402 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365083 88402 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
46884102 7798 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 366 5 2 3 3.7 CC1(C)CCC(Oc2cc(F)c(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
CHEMBL1091106 7798 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at 5HT2C receptorAgonist activity at 5HT2C receptor
ChEMBL 366 5 2 3 3.7 CC1(C)CCC(Oc2cc(F)c(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
230 3869 9 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Binding
Agonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced phosphoinositide hydrolysis by cell based assayAgonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced phosphoinositide hydrolysis by cell based assay
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1007/s00044-011-9615-3
3045225 3869 9 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Binding
Agonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced phosphoinositide hydrolysis by cell based assayAgonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced phosphoinositide hydrolysis by cell based assay
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1007/s00044-011-9615-3
CHEMBL407909 3869 9 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Binding
Agonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced phosphoinositide hydrolysis by cell based assayAgonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced phosphoinositide hydrolysis by cell based assay
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1007/s00044-011-9615-3
230 3869 9 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.10.100
3045225 3869 9 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.10.100
CHEMBL407909 3869 9 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.10.100
134143977 149950 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 296 2 1 2 3.1 Fc1ccc2c(c1Cc1ccccc1)CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3956394 149950 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 296 2 1 2 3.1 Fc1ccc2c(c1Cc1ccccc1)CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
122442263 137565 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769454 137565 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771393 137565 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
11514226 88441 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337494 88441 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365470 88441 0 5HT2C 5-HT2C receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
134265663 162854 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 243 1 1 3 2.1 c1cc(C2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4204710 162854 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 243 1 1 3 2.1 c1cc(C2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
134265665 163975 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 231 2 1 3 1.8 CCCc1cncc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4218374 163975 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 231 2 1 3 1.8 CCCc1cncc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
146025687 182838 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4779260 182838 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803306 182838 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
146025687 182838 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4779260 182838 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803306 182838 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
134265732 162982 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 285 2 1 3 2.3 FC(F)(F)CCc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4206126 162982 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 285 2 1 3 2.3 FC(F)(F)CCc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
134265665 163975 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 231 2 1 3 1.8 CCCc1cncc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4218374 163975 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 231 2 1 3 1.8 CCCc1cncc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
16047544 12357 6 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL1187185 12357 6 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL492916 12357 6 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
134265732 162982 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 285 2 1 3 2.3 FC(F)(F)CCc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4206126 162982 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 285 2 1 3 2.3 FC(F)(F)CCc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
16115517 84177 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.4 CCc1ccc2c(c1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL223468 84177 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.4 CCc1ccc2c(c1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
11952353 193447 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 345 4 1 4 3.0 Fc1ccc(F)c(CO[C@H]2CCc3ccc(N4CCNCC4)nc32)c1 10.1016/j.bmcl.2009.10.112
CHEMBL594469 193447 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 345 4 1 4 3.0 Fc1ccc(F)c(CO[C@H]2CCc3ccc(N4CCNCC4)nc32)c1 10.1016/j.bmcl.2009.10.112
CHEMBL4639090 176619 0 5HT2C 5-HT2C receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at 5HT2C receptor (unknown origin)Agonist activity at 5HT2C receptor (unknown origin)
ChEMBL 266 0 1 2 2.5 CC1CN2CCNCc3ccc(Br)c1c32 10.1016/j.bmcl.2019.126929
134139964 145351 0 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 278 2 1 2 3.0 c1ccc(Cc2cccc3c2CCC2CNCCN32)cc1 10.1016/j.bmcl.2016.11.016
CHEMBL3919795 145351 0 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 278 2 1 2 3.0 c1ccc(Cc2cccc3c2CCC2CNCCN32)cc1 10.1016/j.bmcl.2016.11.016
CHEMBL4751981 182785 0 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802812 182785 0 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4751981 182785 0 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802812 182785 0 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
5 134 60 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2012.01.122
5202 134 60 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2012.01.122
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2012.01.122
DB08839 134 60 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2012.01.122
5 134 60 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Binding
Binding to human 5HT2C receptor expressed in CHO cellsBinding to human 5HT2C receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
5202 134 60 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Binding
Binding to human 5HT2C receptor expressed in CHO cellsBinding to human 5HT2C receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Binding
Binding to human 5HT2C receptor expressed in CHO cellsBinding to human 5HT2C receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
DB08839 134 60 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Binding
Binding to human 5HT2C receptor expressed in CHO cellsBinding to human 5HT2C receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
5 134 60 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
5202 134 60 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
CHEMBL39 134 60 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
DB08839 134 60 5HT2C 5-HT2C receptor Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
152 349 14 5HT2C 5-HT2C receptor Rat 8.7 pEC50 = 8.7 Functional
Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cellsActivity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
2107 349 14 5HT2C 5-HT2C receptor Rat 8.7 pEC50 = 8.7 Functional
Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cellsActivity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
CHEMBL275854 349 14 5HT2C 5-HT2C receptor Rat 8.7 pEC50 = 8.7 Functional
Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cellsActivity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
46230099 192901 0 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 251 0 2 3 1.2 O=C1NC2CCNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
CHEMBL590483 192901 0 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 251 0 2 3 1.2 O=C1NC2CCNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
11658860 2206 41 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
2941 2206 41 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
4374 2206 41 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
CHEMBL360328 2206 41 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
DB04871 2206 41 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
9901086 184954 21 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
CHEMBL494947 184954 21 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
9901086 184954 21 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
CHEMBL494947 184954 21 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
134265831 179152 0 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 203 0 1 3 1.1 Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4747291 179152 0 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 203 0 1 3 1.1 Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
112713234 146647 1 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 202 0 1 2 1.7 Cc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3930174 146647 1 5HT2C 5-HT2C receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 202 0 1 2 1.7 Cc1cccc2c1CCC1CNCCN21 10.1016/j.bmcl.2016.11.016
16115271 78461 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 298 1 1 2 2.8 CC(C)[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL2113264 78461 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 298 1 1 2 2.8 CC(C)[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
46228437 193570 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL595194 193570 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
166 3157 5 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assayAgonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/acs.jmedchem.6b01194
3045227 3157 5 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assayAgonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/acs.jmedchem.6b01194
CHEMBL76781 3157 5 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assayAgonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/acs.jmedchem.6b01194
24826868 90410 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 236 0 1 2 1.3 O=C1c2cc(Cl)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397877 90410 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 236 0 1 2 1.3 O=C1c2cc(Cl)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL4782824 182850 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803449 182850 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
44572800 12362 2 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1 10.1021/jm801354e
CHEMBL1187194 12362 2 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1 10.1021/jm801354e
CHEMBL493128 12362 2 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1 10.1021/jm801354e
23395431 94231 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 C[C@@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
CHEMBL254215 94231 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 C[C@@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
10331841 168365 5 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1021/jm0709034
CHEMBL440752 168365 5 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1021/jm0709034
45485742 191413 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 318 5 1 5 2.2 Clc1ccccc1CCOc1cncc(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.136
CHEMBL572228 191413 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 318 5 1 5 2.2 Clc1ccccc1CCOc1cncc(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.136
90644511 110935 7 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 282 3 2 4 2.4 CNc1nc(Cc2ccccc2)nc2c1CCNC[C@@H]2C 10.1021/jm5003292
CHEMBL3286556 110935 7 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 282 3 2 4 2.4 CNc1nc(Cc2ccccc2)nc2c1CCNC[C@@H]2C 10.1021/jm5003292
134146228 148371 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 300 1 1 3 3.1 COc1cc2c(c(Cl)c1Cl)N1CCCNC[C@H]1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3943620 148371 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 300 1 1 3 3.1 COc1cc2c(c(Cl)c1Cl)N1CCCNC[C@H]1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL4782824 182850 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803449 182850 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
166 3157 5 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assayAgonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/acs.jmedchem.6b01194
3045227 3157 5 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assayAgonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/acs.jmedchem.6b01194
CHEMBL76781 3157 5 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assayAgonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/acs.jmedchem.6b01194
25070582 60904 17 5HT2C 5-HT2C receptor Dog 8.0 pEC50 = 8.0 Functional
Agonist activity at dog 5HT2C receptorAgonist activity at dog 5HT2C receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 60904 17 5HT2C 5-HT2C receptor Dog 8.0 pEC50 = 8.0 Functional
Agonist activity at dog 5HT2C receptorAgonist activity at dog 5HT2C receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
146025684 182758 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4743977 182758 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802486 182758 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
146025688 182817 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4761064 182817 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803134 182817 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
137630842 160289 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assayAgonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assay
ChEMBL 347 9 1 3 4.1 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.7b00584
CHEMBL4091672 160289 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assayAgonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assay
ChEMBL 347 9 1 3 4.1 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.7b00584
CHEMBL4117120 160289 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assayAgonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assay
ChEMBL 347 9 1 3 4.1 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.7b00584
134265705 163266 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 189 0 1 3 0.8 c1cnc2c(c1)CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4209572 163266 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 189 0 1 3 0.8 c1cnc2c(c1)CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4799299 182915 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4804137 182915 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
25070581 60911 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770380 60911 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
71562661 86639 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
CHEMBL2331794 86639 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
134144277 149916 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 280 2 1 3 3.2 c1ccc(Oc2cccc3c2CCC2CNCCN32)cc1 10.1016/j.bmcl.2016.11.016
CHEMBL3956136 149916 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 280 2 1 3 3.2 c1ccc(Oc2cccc3c2CCC2CNCCN32)cc1 10.1016/j.bmcl.2016.11.016
19036360 106790 0 5HT2C 5-HT2C receptor Rat 7.0 pEC50 = 7 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 270 3 1 3 3.2 COc1ccc2c(c1)-c1c(ccn1CC(C)N)C2(C)C 10.1021/jm970030l
CHEMBL318639 106790 0 5HT2C 5-HT2C receptor Rat 7.0 pEC50 = 7 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 270 3 1 3 3.2 COc1ccc2c(c1)-c1c(ccn1CC(C)N)C2(C)C 10.1021/jm970030l
132820208 148857 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 232 1 1 3 1.8 COc1cccc2c1CC[C@@H]1CNCCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3947432 148857 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 232 1 1 3 1.8 COc1cccc2c1CC[C@@H]1CNCCCN21 10.1016/j.bmcl.2016.11.016
10609802 106470 2 5HT2C 5-HT2C receptor Rat 6.0 pEC50 = 6 Functional
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptor
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2 10.1021/jm970219x
CHEMBL316527 106470 2 5HT2C 5-HT2C receptor Rat 6.0 pEC50 = 6 Functional
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptor
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2 10.1021/jm970219x
10560133 106615 0 5HT2C 5-HT2C receptor Rat 5.0 pEC50 = 5 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 204 3 1 3 2.0 COc1ccc2c(ccn2CC(C)N)c1 10.1021/jm970030l
CHEMBL317564 106615 0 5HT2C 5-HT2C receptor Rat 5.0 pEC50 = 5 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 204 3 1 3 2.0 COc1ccc2c(ccn2CC(C)N)c1 10.1021/jm970030l
CHEMBL4789175 182870 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@@H]3C[C@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803726 182870 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@@H]3C[C@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
45485787 190927 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 378 5 1 6 1.5 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1Br 10.1016/j.bmcl.2009.07.136
CHEMBL568897 190927 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 378 5 1 6 1.5 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1Br 10.1016/j.bmcl.2009.07.136
CHEMBL4789175 182870 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@@H]3C[C@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803726 182870 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@@H]3C[C@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
137631035 160322 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4101194 160322 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4117313 160322 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
71562661 86639 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
CHEMBL2331794 86639 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
45484785 191350 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assay
ChEMBL 328 6 1 6 1.4 Cc1cc(=O)n(CCCOc2ccccc2)c(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.133
CHEMBL571733 191350 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assay
ChEMBL 328 6 1 6 1.4 Cc1cc(=O)n(CCCOc2ccccc2)c(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.133
118733766 119871 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416035 119871 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546870 119871 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
137631035 160322 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4101194 160322 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4117313 160322 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
45484866 190844 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assay
ChEMBL 366 5 1 6 2.0 CCn1c(COc2cc(F)ccc2Cl)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
CHEMBL568437 190844 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assay
ChEMBL 366 5 1 6 2.0 CCn1c(COc2cc(F)ccc2Cl)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
11983273 77405 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Induction of 5HT2C receptor mediated increase in intracellular calcium concentration in HEK293 cellsInduction of 5HT2C receptor mediated increase in intracellular calcium concentration in HEK293 cells
ChEMBL 256 1 1 2 2.5 FC(F)(F)c1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209714 77405 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Induction of 5HT2C receptor mediated increase in intracellular calcium concentration in HEK293 cellsInduction of 5HT2C receptor mediated increase in intracellular calcium concentration in HEK293 cells
ChEMBL 256 1 1 2 2.5 FC(F)(F)c1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
137655846 157866 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 349 3 1 3 4.3 Cc1cc(-c2cccc3ccccc23)oc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4093102 157866 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 349 3 1 3 4.3 Cc1cc(-c2cccc3ccccc23)oc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
122461343 137570 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769704 137570 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771398 137570 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122461343 137570 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769704 137570 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771398 137570 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
137635172 155014 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 337 2 1 4 3.3 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCNCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4059943 155014 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 337 2 1 4 3.3 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCNCC1 10.1021/acs.jmedchem.7b00385
155553235 175698 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@@H]1C[C@@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4544700 175698 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@@H]1C[C@@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4597226 175698 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@@H]1C[C@@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
11231392 84231 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.6 CC(C)Oc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL223628 84231 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.6 CC(C)Oc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
45484687 192054 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 339 3 1 5 1.9 O=c1cc2c(nn1Cc1ccccc1OC(F)(F)F)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL577410 192054 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 339 3 1 5 1.9 O=c1cc2c(nn1Cc1ccccc1OC(F)(F)F)CCNCC2 10.1016/j.bmcl.2009.07.063
1534 102327 48 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 102327 48 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 102327 48 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
1534 102327 48 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 102327 48 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 102327 48 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
122461993 137567 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769581 137567 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771395 137567 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
155553235 175698 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@@H]1C[C@@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4544700 175698 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@@H]1C[C@@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4597226 175698 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@@H]1C[C@@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
58911532 90432 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 244 2 1 2 1.6 CCCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397899 90432 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 244 2 1 2 1.6 CCCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
122461993 137567 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769581 137567 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771395 137567 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
118733776 119883 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
CHEMBL3416040 119883 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
CHEMBL3546903 119883 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
16115652 82842 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 286 1 1 3 1.8 COc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL220211 82842 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 286 1 1 3 1.8 COc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
11630623 88430 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337499 88430 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365399 88430 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
118733818 119897 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416061 119897 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546956 119897 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
146025684 182758 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4743977 182758 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802486 182758 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
146025688 182817 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4761064 182817 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803134 182817 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
44572168 12196 1 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/jm801354e
CHEMBL1186458 12196 1 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/jm801354e
CHEMBL464475 12196 1 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/jm801354e
44626357 191142 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 382 5 1 6 2.1 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2C(F)(F)F)n1 10.1016/j.bmcl.2009.07.136
CHEMBL570274 191142 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 382 5 1 6 2.1 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2C(F)(F)F)n1 10.1016/j.bmcl.2009.07.136
137630842 160289 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assayAgonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assay
ChEMBL 347 9 1 3 4.1 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.7b00584
CHEMBL4091672 160289 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assayAgonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assay
ChEMBL 347 9 1 3 4.1 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.7b00584
CHEMBL4117120 160289 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assayAgonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assay
ChEMBL 347 9 1 3 4.1 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.7b00584
11658860 2206 41 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
2941 2206 41 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
4374 2206 41 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL360328 2206 41 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
DB04871 2206 41 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
10465263 63776 50 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL181172 63776 50 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1016/j.bmcl.2004.12.080
10036629 64081 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL181787 64081 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
9994008 165323 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCC1CNCCc2cc(OC)c(Br)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL426235 165323 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCC1CNCCc2cc(OC)c(Br)cc21 10.1016/j.bmcl.2004.12.080
44414290 77781 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Inhibition of 5HT2C assessed as intracellular calcium concentrationInhibition of 5HT2C assessed as intracellular calcium concentration
ChEMBL 193 0 1 1 2.2 Clc1ccc2c(c1)C[C@@H]1CNC[C@H]21 10.1016/j.bmcl.2006.04.070
CHEMBL211153 77781 0 5HT2C 5-HT2C receptor Human 8.0 pEC50 = 8.0 Functional
Inhibition of 5HT2C assessed as intracellular calcium concentrationInhibition of 5HT2C assessed as intracellular calcium concentration
ChEMBL 193 0 1 1 2.2 Clc1ccc2c(c1)C[C@@H]1CNC[C@H]21 10.1016/j.bmcl.2006.04.070
54584720 60905 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 3 1 3 2.0 c1ccc(CCc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770374 60905 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 3 1 3 2.0 c1ccc(CCc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
46230094 192900 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 237 0 2 3 0.8 O=C1NC2CNCCN2c2ccc(Cl)cc21 10.1016/j.bmcl.2009.12.014
CHEMBL590482 192900 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 237 0 2 3 0.8 O=C1NC2CNCCN2c2ccc(Cl)cc21 10.1016/j.bmcl.2009.12.014
155512645 168843 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5-HT2C receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.3 CC(c1ccccc1)c1cc2c(nn1)CCNCC2 10.1016/j.bmcl.2016.06.060
CHEMBL4437696 168843 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5-HT2C receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.3 CC(c1ccccc1)c1cc2c(nn1)CCNCC2 10.1016/j.bmcl.2016.06.060
45484865 191921 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assay
ChEMBL 339 5 1 7 1.1 CCn1c(COc2cccc(C#N)c2)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
CHEMBL576253 191921 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as calcium mobilisation by FLIPR assay
ChEMBL 339 5 1 7 1.1 CCn1c(COc2cccc(C#N)c2)nc(N2CCNCC2)cc1=O 10.1016/j.bmcl.2009.07.133
59312249 110942 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 282 3 2 4 2.4 CNc1nc(C(C)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL3286565 110942 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 282 3 2 4 2.4 CNc1nc(C(C)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL4752604 182780 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4802785 182780 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
118733804 119886 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3416054 119886 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3546906 119886 0 5HT2C 5-HT2C receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL4752604 182780 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4802785 182780 0 5HT2C 5-HT2C receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
45485764 191418 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 325 5 1 7 0.6 N#Cc1ccccc1OCCn1nc(N2CCNCC2)ccc1=O 10.1016/j.bmcl.2009.07.136
CHEMBL572253 191418 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 325 5 1 7 0.6 N#Cc1ccccc1OCCn1nc(N2CCNCC2)ccc1=O 10.1016/j.bmcl.2009.07.136
CHEMBL4762960 182820 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803163 182820 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
122442272 137556 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137556 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137556 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442268 137561 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769633 137561 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771389 137561 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL4762960 182820 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803163 182820 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
44573226 187838 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 404 4 1 4 2.7 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCC(Oc2ccccc2F)CC1 10.1016/j.bmcl.2009.02.071
CHEMBL523169 187838 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 404 4 1 4 2.7 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCC(Oc2ccccc2F)CC1 10.1016/j.bmcl.2009.02.071
122442272 137556 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137556 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137556 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442268 137561 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769633 137561 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771389 137561 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
44572308 12269 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 252 5 2 2 3.4 NC[C@H]1C[C@@H]1c1cccc(NCc2ccccc2)c1 10.1021/jm801354e
CHEMBL1186720 12269 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 252 5 2 2 3.4 NC[C@H]1C[C@@H]1c1cccc(NCc2ccccc2)c1 10.1021/jm801354e
CHEMBL475384 12269 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 252 5 2 2 3.4 NC[C@H]1C[C@@H]1c1cccc(NCc2ccccc2)c1 10.1021/jm801354e
137632218 155494 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 342 2 0 4 3.6 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4065444 155494 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 342 2 0 4 3.6 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
44572306 12253 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 3.0 NC[C@H]1C[C@@H]1c1ccc(-c2ccco2)cc1 10.1021/jm801354e
CHEMBL1186669 12253 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 3.0 NC[C@H]1C[C@@H]1c1ccc(-c2ccco2)cc1 10.1021/jm801354e
CHEMBL474206 12253 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 3.0 NC[C@H]1C[C@@H]1c1ccc(-c2ccco2)cc1 10.1021/jm801354e
11300712 140885 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 252 1 1 3 1.4 COc1c(Cl)ccc2c1C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL385577 140885 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 252 1 1 3 1.4 COc1c(Cl)ccc2c1C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
11579853 88416 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337504 88416 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365200 88416 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2C receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL4638807 176597 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at 5HT2C receptor (unknown origin)Agonist activity at 5HT2C receptor (unknown origin)
ChEMBL 222 0 1 2 2.2 Clc1ccc2c3c1CCCN3CCNC2 10.1016/j.bmcl.2019.126929
58911582 90427 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397894 90427 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
24826871 90440 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397907 90440 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL4757214 182804 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803017 182804 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
44573160 184745 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 392 4 1 4 2.5 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CC(Oc2cccc(Cl)c2)C1 10.1016/j.bmcl.2009.02.071
CHEMBL493757 184745 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 392 4 1 4 2.5 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CC(Oc2cccc(Cl)c2)C1 10.1016/j.bmcl.2009.02.071
137645674 157190 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 348 3 2 2 4.0 Cc1[nH]c(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
CHEMBL4085497 157190 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 348 3 2 2 4.0 Cc1[nH]c(-c2cccc3ccccc23)cc1C(=O)N1CCC(CO)CC1 10.1021/acs.jmedchem.7b00385
137642857 157635 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 373 4 0 4 4.9 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)Cc1cccnc1 10.1021/acs.jmedchem.7b00385
CHEMBL4090637 157635 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 373 4 0 4 4.9 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)Cc1cccnc1 10.1021/acs.jmedchem.7b00385
155540515 175611 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4516935 175611 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4596490 175611 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
3906894 101270 13 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonistic activity for 5-HT2c (5-HT2C) by measuring [3H]inositol monophosphate fromation in CHO cells in which the human 5-HT2C receptor subtype was stably expressedAgonistic activity for 5-HT2c (5-HT2C) by measuring [3H]inositol monophosphate fromation in CHO cells in which the human 5-HT2C receptor subtype was stably expressed
ChEMBL 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1016/s0960-894x(00)00400-5
CHEMBL301466 101270 13 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonistic activity for 5-HT2c (5-HT2C) by measuring [3H]inositol monophosphate fromation in CHO cells in which the human 5-HT2C receptor subtype was stably expressedAgonistic activity for 5-HT2c (5-HT2C) by measuring [3H]inositol monophosphate fromation in CHO cells in which the human 5-HT2C receptor subtype was stably expressed
ChEMBL 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1016/s0960-894x(00)00400-5
44404883 71484 22 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2C receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2C receptor determined by phosphoinositide hydrolysis assay
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL197664 71484 22 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2C receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2C receptor determined by phosphoinositide hydrolysis assay
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
17954204 63382 15 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL180668 63382 15 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2004.12.080
10331841 168365 5 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL440752 168365 5 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL4757214 182804 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803017 182804 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
134265618 163230 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNCC1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4209052 163230 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNCC1CC2 10.1021/acsmedchemlett.8b00328
155540515 175611 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4516935 175611 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
CHEMBL4596490 175611 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111626
17954204 63382 15 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1021/jm0709034
CHEMBL180668 63382 15 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1021/jm0709034
10465263 63776 50 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL181172 63776 50 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
1355 1880 76 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2016.11.016
142 1880 76 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2016.11.016
CHEMBL478 1880 76 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2016.11.016
DB12110 1880 76 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2016.11.016
16747713 87362 0 5HT2C 5-HT2C receptor Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2C receptor expressed in rat SR3T3 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2C receptor expressed in rat SR3T3 cells assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 263 4 1 4 1.6 COCc1c2c(c(C[C@@H](C)N)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
CHEMBL234464 87362 0 5HT2C 5-HT2C receptor Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2C receptor expressed in rat SR3T3 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2C receptor expressed in rat SR3T3 cells assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 263 4 1 4 1.6 COCc1c2c(c(C[C@@H](C)N)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
137629964 160201 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 6 1 2 2.7 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CNC 10.1021/acs.jmedchem.7b00584
CHEMBL4098721 160201 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 6 1 2 2.7 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CNC 10.1021/acs.jmedchem.7b00584
CHEMBL4116380 160201 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 6 1 2 2.7 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CNC 10.1021/acs.jmedchem.7b00584
46228430 193325 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL593545 193325 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
137646604 160390 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 291 6 1 3 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1cccs1 10.1021/acs.jmedchem.7b00584
CHEMBL4085380 160390 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 291 6 1 3 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1cccs1 10.1021/acs.jmedchem.7b00584
CHEMBL4117915 160390 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 291 6 1 3 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1cccs1 10.1021/acs.jmedchem.7b00584
27559 196989 7 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
CHEMBL6557 196989 7 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
70693926 73874 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 217 5 1 2 2.5 NC[C@H]1C[C@@H]1c1ccccc1OCC1CC1 10.1021/ml200206z
CHEMBL2022189 73874 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 217 5 1 2 2.5 NC[C@H]1C[C@@H]1c1ccccc1OCC1CC1 10.1021/ml200206z
CHEMBL2027896 73874 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 217 5 1 2 2.5 NC[C@H]1C[C@@H]1c1ccccc1OCC1CC1 10.1021/ml200206z
7153 97330 60 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O 10.1016/j.bmc.2007.10.100
CHEMBL272942 97330 60 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O 10.1016/j.bmc.2007.10.100
137628797 160165 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4103313 160165 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116143 160165 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC 10.1021/acs.jmedchem.7b00584
137646604 160390 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 291 6 1 3 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1cccs1 10.1021/acs.jmedchem.7b00584
CHEMBL4085380 160390 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 291 6 1 3 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1cccs1 10.1021/acs.jmedchem.7b00584
CHEMBL4117915 160390 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 291 6 1 3 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1cccs1 10.1021/acs.jmedchem.7b00584
46228423 193642 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 360 4 1 6 3.3 Clc1cccc(COc2nc(N3CCNCC3)nc3sccc23)c1 10.1016/j.bmcl.2009.10.112
CHEMBL595646 193642 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 360 4 1 6 3.3 Clc1cccc(COc2nc(N3CCNCC3)nc3sccc23)c1 10.1016/j.bmcl.2009.10.112
137628895 160153 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)cc1 10.1021/acs.jmedchem.7b00584
CHEMBL4078425 160153 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)cc1 10.1021/acs.jmedchem.7b00584
CHEMBL4115999 160153 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)cc1 10.1021/acs.jmedchem.7b00584
72197308 101778 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAgonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 290 2 1 6 -0.0 CN1CCN(c2nc3c(c(N(C)C)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
CHEMBL2393233 101778 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAgonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 290 2 1 6 -0.0 CN1CCN(c2nc3c(c(N(C)C)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
CHEMBL3040291 101778 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAgonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 290 2 1 6 -0.0 CN1CCN(c2nc3c(c(N(C)C)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
CHEMBL4640047 176679 0 5HT2C 5-HT2C receptor Human 4.9 pEC50 = 4.9 Binding
Agonist activity at 5HT2C receptor (unknown origin)Agonist activity at 5HT2C receptor (unknown origin)
ChEMBL 222 0 1 2 2.4 CC1CN2CCNCc3cc(Cl)cc1c32 10.1016/j.bmcl.2019.126929
14515726 86637 5 5HT2C 5-HT2C receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 168 1 1 4 0.4 COc1noc2c1CCNCC2 10.1021/jm301656h
CHEMBL2331792 86637 5 5HT2C 5-HT2C receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 168 1 1 4 0.4 COc1noc2c1CCNCC2 10.1021/jm301656h
137628895 160153 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)cc1 10.1021/acs.jmedchem.7b00584
CHEMBL4078425 160153 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)cc1 10.1021/acs.jmedchem.7b00584
CHEMBL4115999 160153 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)cc1 10.1021/acs.jmedchem.7b00584
14515726 86637 5 5HT2C 5-HT2C receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 168 1 1 4 0.4 COc1noc2c1CCNCC2 10.1021/jm301656h
CHEMBL2331792 86637 5 5HT2C 5-HT2C receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 168 1 1 4 0.4 COc1noc2c1CCNCC2 10.1021/jm301656h
137628797 160165 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4103313 160165 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116143 160165 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC 10.1021/acs.jmedchem.7b00584
70681346 73878 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 231 5 1 2 2.9 NC[C@H]1C[C@@H]1c1ccccc1OCC1CCC1 10.1021/ml200206z
CHEMBL2022190 73878 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 231 5 1 2 2.9 NC[C@H]1C[C@@H]1c1ccccc1OCC1CCC1 10.1021/ml200206z
CHEMBL2027922 73878 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 231 5 1 2 2.9 NC[C@H]1C[C@@H]1c1ccccc1OCC1CCC1 10.1021/ml200206z
118733764 119877 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416034 119877 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546890 119877 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
27559 196989 7 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
CHEMBL6557 196989 7 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
25070907 60907 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
CHEMBL1770376 60907 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
45484682 191961 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 323 2 1 4 2.0 O=c1cc2c(nn1Cc1ccc(C(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL576651 191961 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 323 2 1 4 2.0 O=c1cc2c(nn1Cc1ccc(C(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
134136722 141842 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 270 2 1 2 3.1 c1cc(CC2CCC2)c2c(c1)N1CCCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3891704 141842 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 270 2 1 2 3.1 c1cc(CC2CCC2)c2c(c1)N1CCCNCC1CC2 10.1016/j.bmcl.2016.11.016
134136932 141854 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 216 0 1 2 2.2 c1ccc2c(c1)CCC1CCNCCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3891802 141854 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 216 0 1 2 2.2 c1ccc2c(c1)CCC1CCNCCCN21 10.1016/j.bmcl.2016.11.016
134133531 142793 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 264 1 1 2 3.1 c1ccc(-c2cccc3c2CCC2CNCCN32)cc1 10.1016/j.bmcl.2016.11.016
CHEMBL3899449 142793 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 264 1 1 2 3.1 c1ccc(-c2cccc3c2CCC2CNCCN32)cc1 10.1016/j.bmcl.2016.11.016
10774796 79029 0 5HT2C 5-HT2C receptor Rat 6.9 pEC50 = 6.9 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 210 2 1 2 2.3 C[C@@H](N)Cn1ccc2cc(F)c(F)cc21 10.1021/jm970030l
CHEMBL2115252 79029 0 5HT2C 5-HT2C receptor Rat 6.9 pEC50 = 6.9 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 210 2 1 2 2.3 C[C@@H](N)Cn1ccc2cc(F)c(F)cc21 10.1021/jm970030l
46228441 193452 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 246 3 1 6 0.6 CCCn1cnc2c(N3CCNCC3)ncnc21 10.1016/j.bmcl.2009.10.112
CHEMBL594489 193452 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 246 3 1 6 0.6 CCCn1cnc2c(N3CCNCC3)ncnc21 10.1016/j.bmcl.2009.10.112
118733812 119874 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
CHEMBL3416058 119874 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
CHEMBL3546873 119874 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
24773648 63869 2 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 191 1 1 2 1.9 COc1ccc2c(c1)CCNCC2C 10.1021/jm0709034
CHEMBL181324 63869 2 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 191 1 1 2 1.9 COc1ccc2c(c1)CCNCC2C 10.1021/jm0709034
134153263 151993 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 216 0 1 2 2.1 CC1(C)CC2CNCCN2c2ccccc21 10.1016/j.bmcl.2016.11.016
CHEMBL3973690 151993 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 216 0 1 2 2.1 CC1(C)CC2CNCCN2c2ccccc21 10.1016/j.bmcl.2016.11.016
10631592 200733 0 5HT2C 5-HT2C receptor Rat 5.9 pEC50 = 5.9 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 192 2 1 2 2.1 CC(N)Cn1ccc2c(F)cccc21 10.1021/jm970030l
CHEMBL92565 200733 0 5HT2C 5-HT2C receptor Rat 5.9 pEC50 = 5.9 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 192 2 1 2 2.1 CC(N)Cn1ccc2c(F)cccc21 10.1021/jm970030l
10774565 201323 0 5HT2C 5-HT2C receptor Rat 4.9 pEC50 = 4.9 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 204 3 1 3 2.0 COc1cccc2c1ccn2CC(C)N 10.1021/jm970030l
CHEMBL96095 201323 0 5HT2C 5-HT2C receptor Rat 4.9 pEC50 = 4.9 Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the ratEfficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
ChEMBL 204 3 1 3 2.0 COc1cccc2c1ccn2CC(C)N 10.1021/jm970030l
11736340 73402 37 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 229 1 1 1 3.2 FC(F)(F)c1cccc(C2CCNCC2)c1 10.1016/j.bmcl.2012.01.122
CHEMBL2011553 73402 37 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 229 1 1 1 3.2 FC(F)(F)c1cccc(C2CCNCC2)c1 10.1016/j.bmcl.2012.01.122
CHEMBL2021656 73402 37 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 229 1 1 1 3.2 FC(F)(F)c1cccc(C2CCNCC2)c1 10.1016/j.bmcl.2012.01.122
CHEMBL4645583 177090 0 5HT2C 5-HT2C receptor Human 4.9 pEC50 = 4.9 Binding
Agonist activity at 5HT2C receptor (unknown origin)Agonist activity at 5HT2C receptor (unknown origin)
ChEMBL 174 0 1 2 1.2 c1cc2c3c(c1)CNCCN3CC2 10.1016/j.bmcl.2019.126929
137636435 155250 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 326 2 0 4 3.1 O=C(c1csc(-c2cccc(Cl)c2F)n1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
CHEMBL4062613 155250 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 326 2 0 4 3.1 O=C(c1csc(-c2cccc(Cl)c2F)n1)N1CCOCC1 10.1021/acs.jmedchem.7b00385
702235 52719 86 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 200 1 2 1 2.6 c1ccc2c(C3CCNCC3)c[nH]c2c1 10.1016/j.bmcl.2012.01.122
CHEMBL15988 52719 86 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 200 1 2 1 2.6 c1ccc2c(C3CCNCC3)c[nH]c2c1 10.1016/j.bmcl.2012.01.122
CHEMBL2011564 52719 86 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assayAgonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
ChEMBL 200 1 2 1 2.6 c1ccc2c(C3CCNCC3)c[nH]c2c1 10.1016/j.bmcl.2012.01.122
44572164 12392 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1F 10.1021/jm801354e
CHEMBL1187390 12392 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1F 10.1021/jm801354e
CHEMBL501526 12392 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1F 10.1021/jm801354e
137647246 157010 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 354 2 0 4 3.7 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CC2CC1CO2 10.1021/acs.jmedchem.7b00385
CHEMBL4083432 157010 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 354 2 0 4 3.7 O=C(c1csc(-c2cccc(Cl)c2Cl)n1)N1CC2CC1CO2 10.1021/acs.jmedchem.7b00385
118733762 119876 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416033 119876 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546889 119876 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
137629964 160201 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 6 1 2 2.7 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CNC 10.1021/acs.jmedchem.7b00584
CHEMBL4098721 160201 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 6 1 2 2.7 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CNC 10.1021/acs.jmedchem.7b00584
CHEMBL4116380 160201 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 6 1 2 2.7 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CNC 10.1021/acs.jmedchem.7b00584
12370465 12383 12 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
CHEMBL1187354 12383 12 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
CHEMBL500093 12383 12 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
44572207 12411 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F 10.1021/jm801354e
CHEMBL1187556 12411 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F 10.1021/jm801354e
CHEMBL508680 12411 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F 10.1021/jm801354e
137638508 156017 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 376 4 0 5 4.3 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)Cc1ccn(C)n1 10.1021/acs.jmedchem.7b00385
CHEMBL4071321 156017 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 376 4 0 5 4.3 Cc1nc(-c2cccc3ccccc23)sc1C(=O)N(C)Cc1ccn(C)n1 10.1021/acs.jmedchem.7b00385
137647007 157035 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 301 3 0 5 3.6 CCn1nc(-c2cccc3ccncc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
CHEMBL4083752 157035 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 301 3 0 5 3.6 CCn1nc(-c2cccc3ccncc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
122442286 137559 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 137559 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 137559 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442286 137559 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 137559 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 137559 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442260 137562 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769543 137562 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771390 137562 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
155527636 170448 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5-HT2C receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2cc3c(nn2)CCNCC3)cc1 10.1016/j.bmcl.2016.06.060
CHEMBL4460600 170448 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5-HT2C receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2cc3c(nn2)CCNCC3)cc1 10.1016/j.bmcl.2016.06.060
134136932 141854 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 216 0 1 2 2.2 c1ccc2c(c1)CCC1CCNCCCN21 10.1016/j.bmcl.2016.11.016
CHEMBL3891802 141854 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 216 0 1 2 2.2 c1ccc2c(c1)CCC1CCNCCCN21 10.1016/j.bmcl.2016.11.016
18735309 198992 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 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 198992 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 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
CHEMBL4646559 177161 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Binding
Agonist activity at 5HT2C receptor (unknown origin)Agonist activity at 5HT2C receptor (unknown origin)
ChEMBL 272 0 1 4 1.0 O=S1(=O)CCN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
118733798 119881 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416051 119881 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546894 119881 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
46230047 192839 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 217 0 2 3 0.5 Cc1ccc2c(c1)C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590089 192839 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 217 0 2 3 0.5 Cc1ccc2c(c1)C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
122442275 137569 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770862 137569 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771397 137569 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
44573004 12232 1 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1 10.1021/jm801354e
CHEMBL1186590 12232 1 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1 10.1021/jm801354e
CHEMBL471202 12232 1 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1 10.1021/jm801354e
122442275 137569 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770862 137569 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771397 137569 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
11195293 90416 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 C[C@@]12CNCCN1C(=O)c1ccccc1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397883 90416 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 C[C@@]12CNCCN1C(=O)c1ccccc1C2 10.1016/j.bmcl.2013.04.061
11290492 137209 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 218 1 1 3 0.8 COc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL376456 137209 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 218 1 1 3 0.8 COc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
44572369 12170 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 171 2 1 1 1.7 C#Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL1186108 12170 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 171 2 1 1 1.7 C#Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL450178 12170 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 171 2 1 1 1.7 C#Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
9839494 101757 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonistic activity for 5-HT2c (5-HT2C) by measuring [3H]inositol monophosphate fromation in CHO cells in which the human 5-HT2C receptor subtype was stably expressedAgonistic activity for 5-HT2c (5-HT2C) by measuring [3H]inositol monophosphate fromation in CHO cells in which the human 5-HT2C receptor subtype was stably expressed
ChEMBL 305 0 2 3 2.1 O=C1Nc2cc(C(F)(F)F)c(Cl)cc2N2CCNCC12 10.1016/s0960-894x(00)00400-5
CHEMBL304013 101757 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonistic activity for 5-HT2c (5-HT2C) by measuring [3H]inositol monophosphate fromation in CHO cells in which the human 5-HT2C receptor subtype was stably expressedAgonistic activity for 5-HT2c (5-HT2C) by measuring [3H]inositol monophosphate fromation in CHO cells in which the human 5-HT2C receptor subtype was stably expressed
ChEMBL 305 0 2 3 2.1 O=C1Nc2cc(C(F)(F)F)c(Cl)cc2N2CCNCC12 10.1016/s0960-894x(00)00400-5
46228424 195779 2 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 281 1 1 5 0.9 Brc1cn2ccnc2c(N2CCNCC2)n1 10.1016/j.bmcl.2009.10.112
CHEMBL609595 195779 2 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2C receptor by FLIPR assayAgonist activity against human 5HT2C receptor by FLIPR assay
ChEMBL 281 1 1 5 0.9 Brc1cn2ccnc2c(N2CCNCC2)n1 10.1016/j.bmcl.2009.10.112
46230046 192836 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 203 0 2 3 0.2 O=C1NC2CNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
CHEMBL590077 192836 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 203 0 2 3 0.2 O=C1NC2CNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
CHEMBL4750271 182773 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 285 6 1 3 3.8 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4802701 182773 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 285 6 1 3 3.8 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
44573002 12395 1 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Br)cc1 10.1021/jm801354e
CHEMBL1187408 12395 1 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Br)cc1 10.1021/jm801354e
CHEMBL501854 12395 1 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Br)cc1 10.1021/jm801354e
CHEMBL4750271 182773 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 285 6 1 3 3.8 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4802701 182773 0 5HT2C 5-HT2C receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 285 6 1 3 3.8 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCC3CC3)ccc2o1 10.1021/acs.jmedchem.6b01194
11209786 136452 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 296 1 1 2 2.7 O=C1c2c(cc(C3CC3)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL375170 136452 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 296 1 1 2 2.7 O=C1c2c(cc(C3CC3)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
24826867 90423 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 230 1 1 2 1.2 CCc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397890 90423 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 230 1 1 2 1.2 CCc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
24826963 90443 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 230 0 1 2 1.3 Cc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397910 90443 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2C receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 230 0 1 2 1.3 Cc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
25084025 12410 1 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1cccc(Br)c1 10.1021/jm801354e
CHEMBL1187522 12410 1 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1cccc(Br)c1 10.1021/jm801354e
CHEMBL506727 12410 1 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1cccc(Br)c1 10.1021/jm801354e
44573162 171749 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 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 171749 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 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 157709 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 340 5 0 4 4.0 COCCN(C)C(=O)c1sc(-c2cccc3ccccc23)nc1C 10.1021/acs.jmedchem.7b00385
CHEMBL4091448 157709 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 340 5 0 4 4.0 COCCN(C)C(=O)c1sc(-c2cccc3ccccc23)nc1C 10.1021/acs.jmedchem.7b00385
122442260 137562 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769543 137562 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771390 137562 0 5HT2C 5-HT2C receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL4740346 182747 0 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802388 182747 0 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4644315 177011 0 5HT2C 5-HT2C receptor Human 5.9 pEC50 = 5.9 Binding
Agonist activity at 5HT2C receptor (unknown origin)Agonist activity at 5HT2C receptor (unknown origin)
ChEMBL 202 0 1 2 1.9 c1cc2c3c(c1)CNCCN3CCCC2 10.1016/j.bmcl.2019.126929
136044083 110937 1 5HT2C 5-HT2C receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 255 2 2 4 1.5 Oc1nc(Cc2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL3286558 110937 1 5HT2C 5-HT2C receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 255 2 2 4 1.5 Oc1nc(Cc2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
1355 1880 76 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
142 1880 76 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
CHEMBL478 1880 76 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
DB12110 1880 76 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
CHEMBL4740346 182747 0 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802388 182747 0 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
1355 1880 76 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
142 1880 76 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
CHEMBL478 1880 76 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
DB12110 1880 76 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
1355 1880 76 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/acs.jmedchem.7b00385
142 1880 76 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/acs.jmedchem.7b00385
CHEMBL478 1880 76 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/acs.jmedchem.7b00385
DB12110 1880 76 5HT2C 5-HT2C receptor Human 7.8 pEC50 = 7.8 Functional