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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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GPCRdb ID #Vendors UniProt IUPHAR Species p-value
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1588 2189 17 5HT2A 5-HT2A receptor Human 10.7 pEC50 = 10.7 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2189 17 5HT2A 5-HT2A receptor Human 10.7 pEC50 = 10.7 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2189 17 5HT2A 5-HT2A receptor Human 10.7 pEC50 = 10.7 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2189 17 5HT2A 5-HT2A receptor Human 10.7 pEC50 = 10.7 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2189 17 5HT2A 5-HT2A receptor Human 10.7 pEC50 = 10.7 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
5 134 60 5HT2A 5-HT2A receptor Human 9.6 pEC50 = 9.6 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor 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 5HT2A 5-HT2A receptor Human 9.6 pEC50 = 9.6 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor 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 5HT2A 5-HT2A receptor Human 9.6 pEC50 = 9.6 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor 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 5HT2A 5-HT2A receptor Human 9.6 pEC50 = 9.6 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor 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 5HT2A 5-HT2A receptor Human 9.6 pEC50 = 9.6 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor 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 5HT2A 5-HT2A receptor Human 9.6 pEC50 = 9.6 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor 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 5HT2A 5-HT2A receptor Human 9.6 pEC50 = 9.6 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor 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 5HT2A 5-HT2A receptor Human 9.6 pEC50 = 9.6 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor 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
107 136 110 5HT2A 5-HT2A receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1016/j.bmcl.2014.07.062
1833 136 110 5HT2A 5-HT2A receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1016/j.bmcl.2014.07.062
CHEMBL8165 136 110 5HT2A 5-HT2A receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1016/j.bmcl.2014.07.062
5 134 60 5HT2A 5-HT2A receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5202 134 60 5HT2A 5-HT2A receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
CHEMBL39 134 60 5HT2A 5-HT2A receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
DB08839 134 60 5HT2A 5-HT2A receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5 134 60 5HT2A 5-HT2A receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5202 134 60 5HT2A 5-HT2A receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
CHEMBL39 134 60 5HT2A 5-HT2A receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
DB08839 134 60 5HT2A 5-HT2A receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5 134 60 5HT2A 5-HT2A receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5202 134 60 5HT2A 5-HT2A receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
CHEMBL39 134 60 5HT2A 5-HT2A receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
DB08839 134 60 5HT2A 5-HT2A receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5 134 60 5HT2A 5-HT2A receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5202 134 60 5HT2A 5-HT2A receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
CHEMBL39 134 60 5HT2A 5-HT2A receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
DB08839 134 60 5HT2A 5-HT2A receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
11247569 193008 0 5HT2A 5-HT2A receptor Human 9.2 pEC50 = 9.2 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 434 4 2 4 5.2 COc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL591223 193008 0 5HT2A 5-HT2A receptor Human 9.2 pEC50 = 9.2 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 434 4 2 4 5.2 COc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
1524 2048 78 5HT2A 5-HT2A receptor Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A 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-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2013.02.020
197 2048 78 5HT2A 5-HT2A receptor Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A 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-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2013.02.020
3822 2048 78 5HT2A 5-HT2A receptor Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A 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-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2013.02.020
88 2048 78 5HT2A 5-HT2A receptor Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A 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-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2013.02.020
CHEMBL51 2048 78 5HT2A 5-HT2A receptor Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A 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-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2013.02.020
DB12465 2048 78 5HT2A 5-HT2A receptor Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A 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-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2013.02.020
5 134 60 5HT2A 5-HT2A receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
5202 134 60 5HT2A 5-HT2A receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
CHEMBL39 134 60 5HT2A 5-HT2A receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
DB08839 134 60 5HT2A 5-HT2A receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
439280 119259 96 5HT2A 5-HT2A receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
5202 134 60 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
CHEMBL39 134 60 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
DB08839 134 60 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
31101 690 31 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 690 31 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 690 31 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 690 31 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 690 31 5HT2A 5-HT2A receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
5 134 60 5HT2A 5-HT2A receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
11695000 88402 0 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
24773649 94145 0 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
CHEMBL253591 94145 0 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
11446529 77686 2 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 165 2 1 1 1.8 NC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL2094028 77686 2 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 165 2 1 1 1.8 NC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL2109749 77686 2 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 165 2 1 1 1.8 NC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
122180957 121000 0 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human 5-HT2A receptor expressed in human tsA201 cells after 30 mins by inositol phosphate turnover assayPartial agonist activity at human 5-HT2A receptor expressed in human tsA201 cells after 30 mins by inositol phosphate turnover assay
ChEMBL 393 7 1 5 3.5 COc1cc(CCNCc2cccc3c2OCO3)c(OC)cc1Br 10.1016/j.bmc.2014.12.011
CHEMBL3589578 121000 0 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human 5-HT2A receptor expressed in human tsA201 cells after 30 mins by inositol phosphate turnover assayPartial agonist activity at human 5-HT2A receptor expressed in human tsA201 cells after 30 mins by inositol phosphate turnover assay
ChEMBL 393 7 1 5 3.5 COc1cc(CCNCc2cccc3c2OCO3)c(OC)cc1Br 10.1016/j.bmc.2014.12.011
134143977 149950 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 ADMET
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A 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 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 ADMET
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A 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
10105208 61949 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
CHEMBL178124 61949 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
17954204 63382 15 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1021/jm0709034
24773816 94174 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
CHEMBL253805 94174 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
23395431 94231 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
24773650 153891 1 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)CCNCC2C 10.1021/jm0709034
CHEMBL399750 153891 1 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)CCNCC2C 10.1021/jm0709034
10105208 61949 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178124 61949 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1016/j.bmcl.2004.12.080
22368315 63211 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 255 1 1 2 2.1 COc1cc2c(cc1Br)CCNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL180166 63211 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 255 1 1 2 2.1 COc1cc2c(cc1Br)CCNCC2 10.1016/j.bmcl.2004.12.080
9994008 165323 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
9973675 66813 0 5HT2A 5-HT2A receptor Rat 7.0 pEC50 = 7 Functional
Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cellsSerotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
ChEMBL 289 4 2 4 1.8 COc1cc([C@@H](O)[C@@H](C)N)c(OC)cc1Br 10.1021/jm040082s
CHEMBL188709 66813 0 5HT2A 5-HT2A receptor Rat 7.0 pEC50 = 7 Functional
Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cellsSerotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
ChEMBL 289 4 2 4 1.8 COc1cc([C@@H](O)[C@@H](C)N)c(OC)cc1Br 10.1021/jm040082s
134265732 162982 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6 ADMET
Agonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2AR (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 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6 ADMET
Agonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2AR (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
CHEMBL4757718 180033 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6 ADMET
Agonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 284 2 1 2 2.9 FC(F)(F)CCc1cccc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
24773897 94176 1 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 213 0 1 1 2.7 C[C@@H]1CNCCc2ccc(Cl)c(F)c21 10.1021/jm0709034
CHEMBL253807 94176 1 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 213 0 1 1 2.7 C[C@@H]1CNCCc2ccc(Cl)c(F)c21 10.1021/jm0709034
134265705 163266 0 5HT2A 5-HT2A receptor Human 4.0 pEC50 = 4 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 189 0 1 3 0.8 c1cnc2c(c1)CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4209572 163266 0 5HT2A 5-HT2A receptor Human 4.0 pEC50 = 4 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 189 0 1 3 0.8 c1cnc2c(c1)CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
134265590 163934 0 5HT2A 5-HT2A receptor Human 4.0 pEC50 = 4 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 189 0 1 3 0.8 c1cc2c(cn1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4217846 163934 0 5HT2A 5-HT2A receptor Human 4.0 pEC50 = 4 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 189 0 1 3 0.8 c1cc2c(cn1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
118733794 119905 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416049 119905 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546975 119905 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
118733818 119897 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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
24826871 90440 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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
122180974 121017 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assayPartial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assay
ChEMBL 397 8 1 4 3.9 COc1cc(CCNCc2cccc(OC)c2F)c(OC)cc1Br 10.1016/j.bmc.2014.12.011
CHEMBL3589595 121017 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assayPartial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assay
ChEMBL 397 8 1 4 3.9 COc1cc(CCNCc2cccc(OC)c2F)c(OC)cc1Br 10.1016/j.bmc.2014.12.011
24826963 90443 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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
11176570 90448 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 270 0 1 2 1.7 O=C1c2cc(C(F)(F)F)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397915 90448 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 270 0 1 2 1.7 O=C1c2cc(C(F)(F)F)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
18735309 198992 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
24826787 90425 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 270 0 1 2 1.7 O=C1c2c(cccc2C(F)(F)F)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397892 90425 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 270 0 1 2 1.7 O=C1c2c(cccc2C(F)(F)F)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
122442268 137561 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
44412405 77190 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 255 1 1 1 3.4 FC(F)(F)c1cccc([C@H]2CC[C@H]3CNC[C@@H]23)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209155 77190 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 255 1 1 1 3.4 FC(F)(F)c1cccc([C@H]2CC[C@H]3CNC[C@@H]23)c1 10.1016/j.bmcl.2006.03.007
122442268 137561 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
58911579 90424 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 242 1 1 2 1.5 O=C1c2c(cccc2C2CC2)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397891 90424 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 242 1 1 2 1.5 O=C1c2c(cccc2C2CC2)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL4739937 182746 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802378 182746 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4739937 182746 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802378 182746 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
CHEMBL4756903 182805 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803034 182805 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
137644936 160396 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 5 1 2 2.7 COc1ccc(F)cc1C1CC1CNC1CC1 10.1021/acs.jmedchem.7b00584
CHEMBL4090984 160396 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 5 1 2 2.7 COc1ccc(F)cc1C1CC1CNC1CC1 10.1021/acs.jmedchem.7b00584
CHEMBL4117952 160396 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 5 1 2 2.7 COc1ccc(F)cc1C1CC1CNC1CC1 10.1021/acs.jmedchem.7b00584
45485781 190982 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 368 5 1 6 1.8 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1C(F)(F)F 10.1016/j.bmcl.2009.07.136
CHEMBL569342 190982 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 368 5 1 6 1.8 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1C(F)(F)F 10.1016/j.bmcl.2009.07.136
137644936 160396 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 5 1 2 2.7 COc1ccc(F)cc1C1CC1CNC1CC1 10.1021/acs.jmedchem.7b00584
CHEMBL4090984 160396 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 5 1 2 2.7 COc1ccc(F)cc1C1CC1CNC1CC1 10.1021/acs.jmedchem.7b00584
CHEMBL4117952 160396 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 235 5 1 2 2.7 COc1ccc(F)cc1C1CC1CNC1CC1 10.1021/acs.jmedchem.7b00584
5 134 60 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8.0 Binding
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8.0 Binding
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8.0 Binding
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8.0 Binding
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 5HT2A 5-HT2A receptor Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
3906894 101270 13 5HT2A 5-HT2A receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1021/jm301656h
CHEMBL301466 101270 13 5HT2A 5-HT2A receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1021/jm301656h
10401602 122293 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCOc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL360968 122293 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCOc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
44383397 58708 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Functional antagonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell lineFunctional antagonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell line
ChEMBL 246 3 1 2 3.1 CNCCc1cn2c3c(cc(F)cc13)CCC2C 10.1016/s0960-894x(00)00141-4
CHEMBL170319 58708 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Functional antagonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell lineFunctional antagonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell line
ChEMBL 246 3 1 2 3.1 CNCCc1cn2c3c(cc(F)cc13)CCC2C 10.1016/s0960-894x(00)00141-4
11066440 13176 0 5HT2A 5-HT2A receptor Rat 6.0 pEC50 = 6.0 Binding
Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptorTested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor
ChEMBL 297 2 1 3 2.8 COc1cc(Br)c2c3c1[C@H](CN)CC[C@@H]3CO2 10.1021/jm030064v
CHEMBL119323 13176 0 5HT2A 5-HT2A receptor Rat 6.0 pEC50 = 6.0 Binding
Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptorTested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor
ChEMBL 297 2 1 3 2.8 COc1cc(Br)c2c3c1[C@H](CN)CC[C@@H]3CO2 10.1021/jm030064v
11437171 82841 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 234 1 1 3 1.5 CSc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL220207 82841 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 234 1 1 3 1.5 CSc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL4756903 182805 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803034 182805 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4790652 182873 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803766 182873 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
16086382 138755 5 5HT2A 5-HT2A receptor Rat 6.0 pEC50 = 6.0 Functional
Activity at rat 5HT2A receptor expressed in NIH3T3 cells assessed as stimulation of 2-arachidonylglycerol productionActivity at rat 5HT2A receptor expressed in NIH3T3 cells assessed as stimulation of 2-arachidonylglycerol production
ChEMBL 271 3 1 3 2.1 COc1cc(Br)c(OC)c2c1[C@H](CN)C2 10.1021/jm060656o
CHEMBL379637 138755 5 5HT2A 5-HT2A receptor Rat 6.0 pEC50 = 6.0 Functional
Activity at rat 5HT2A receptor expressed in NIH3T3 cells assessed as stimulation of 2-arachidonylglycerol productionActivity at rat 5HT2A receptor expressed in NIH3T3 cells assessed as stimulation of 2-arachidonylglycerol production
ChEMBL 271 3 1 3 2.1 COc1cc(Br)c(OC)c2c1[C@H](CN)C2 10.1021/jm060656o
44412404 77177 3 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 206 1 1 2 1.6 Fc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209106 77177 3 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 206 1 1 2 1.6 Fc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
CHEMBL4632473 176185 0 5HT2A 5-HT2A receptor Human 6.0 pEC50 = 6.0 ADMET
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
ChEMBL 256 0 1 2 3.0 CC1CN2CCNCc3cc(Cl)c(Cl)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4790652 182873 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803766 182873 0 5HT2A 5-HT2A receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
4076 96345 22 5HT2A 5-HT2A receptor Rat 5.0 pEC50 = 5.0 Functional
Activity at rat 5HT2A receptor assessed as 5-HT-stimulated IP3 accumulationActivity at rat 5HT2A receptor assessed as 5-HT-stimulated IP3 accumulation
ChEMBL 211 5 1 4 1.2 COc1cc(CCN)cc(OC)c1OC 10.1021/jm060272y
CHEMBL26687 96345 22 5HT2A 5-HT2A receptor Rat 5.0 pEC50 = 5.0 Functional
Activity at rat 5HT2A receptor assessed as 5-HT-stimulated IP3 accumulationActivity at rat 5HT2A receptor assessed as 5-HT-stimulated IP3 accumulation
ChEMBL 211 5 1 4 1.2 COc1cc(CCN)cc(OC)c1OC 10.1021/jm060272y
45485779 191097 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 348 5 1 6 1.8 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2Cl)n1 10.1016/j.bmcl.2009.07.136
CHEMBL570023 191097 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 348 5 1 6 1.8 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2Cl)n1 10.1016/j.bmcl.2009.07.136
9856041 23721 0 5HT2A 5-HT2A receptor Rat 6.9 pEC50 = 6.9 Functional
In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cellsIn vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells
ChEMBL 230 2 2 2 2.4 CC(N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL133868 23721 0 5HT2A 5-HT2A receptor Rat 6.9 pEC50 = 6.9 Functional
In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cellsIn vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells
ChEMBL 230 2 2 2 2.4 CC(N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
24849050 77658 2 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CC[C@H]3CNC[C@H]32)n1 10.1016/j.bmcl.2006.03.007
CHEMBL210802 77658 2 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CC[C@H]3CNC[C@H]32)n1 10.1016/j.bmcl.2006.03.007
CHEMBL4761526 182816 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803123 182816 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4761526 182816 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803123 182816 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
11302765 83595 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 284 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL221113 83595 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 284 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
119570 2967 79 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N nan
2233 2967 79 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N nan
953 2967 79 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N nan
CHEMBL301265 2967 79 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N nan
DB00413 2967 79 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N nan
16086382 138755 5 5HT2A 5-HT2A receptor Rat 5.9 pEC50 = 5.9 Functional
Activity at rat 5HT2A receptor expressed in NIH3T3 cells assessed as stimulation of arachidonic acid releaseActivity at rat 5HT2A receptor expressed in NIH3T3 cells assessed as stimulation of arachidonic acid release
ChEMBL 271 3 1 3 2.1 COc1cc(Br)c(OC)c2c1[C@H](CN)C2 10.1021/jm060656o
CHEMBL379637 138755 5 5HT2A 5-HT2A receptor Rat 5.9 pEC50 = 5.9 Functional
Activity at rat 5HT2A receptor expressed in NIH3T3 cells assessed as stimulation of arachidonic acid releaseActivity at rat 5HT2A receptor expressed in NIH3T3 cells assessed as stimulation of arachidonic acid release
ChEMBL 271 3 1 3 2.1 COc1cc(Br)c(OC)c2c1[C@H](CN)C2 10.1021/jm060656o
122442251 137568 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770225 137568 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771396 137568 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
10543655 10790 0 5HT2A 5-HT2A receptor Rat 7.9 pEC50 = 7.9 Binding
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
ChEMBL 283 2 1 3 4.1 C[C@H](N)Cc1c2ccoc2c(C(F)(F)F)c2ccoc12 10.1021/jm000491y
CHEMBL1177924 10790 0 5HT2A 5-HT2A receptor Rat 7.9 pEC50 = 7.9 Binding
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
ChEMBL 283 2 1 3 4.1 C[C@H](N)Cc1c2ccoc2c(C(F)(F)F)c2ccoc12 10.1021/jm000491y
CHEMBL6907 10790 0 5HT2A 5-HT2A receptor Rat 7.9 pEC50 = 7.9 Binding
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
ChEMBL 283 2 1 3 4.1 C[C@H](N)Cc1c2ccoc2c(C(F)(F)F)c2ccoc12 10.1021/jm000491y
16747713 87362 0 5HT2A 5-HT2A receptor Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2A receptor in rat A7r5 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 5HT2A 5-HT2A receptor Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2A receptor in rat A7r5 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
3906894 101270 13 5HT2A 5-HT2A receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1021/jm301656h
CHEMBL301466 101270 13 5HT2A 5-HT2A receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1021/jm301656h
46233391 192790 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 454 4 2 4 5.4 Cn1ncc(Br)c1-c1cccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)c1 10.1021/jm9007328
CHEMBL589769 192790 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 454 4 2 4 5.4 Cn1ncc(Br)c1-c1cccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)c1 10.1021/jm9007328
15185771 67313 4 5HT2A 5-HT2A receptor Rat 6.9 pEC50 = 6.9 Functional
Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cellsSerotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
ChEMBL 289 5 1 4 2.1 COc1cc(C(CN)OC)c(OC)cc1Br 10.1021/jm040082s
CHEMBL191051 67313 4 5HT2A 5-HT2A receptor Rat 6.9 pEC50 = 6.9 Functional
Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cellsSerotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
ChEMBL 289 5 1 4 2.1 COc1cc(C(CN)OC)c(OC)cc1Br 10.1021/jm040082s
10017429 10258 0 5HT2A 5-HT2A receptor Rat 6.9 pEC50 = 6.9 Binding
Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptorTested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor
ChEMBL 295 2 1 3 3.2 COc1cc(Br)c2occ3c2c1[C@H](CN)CC3 10.1021/jm030064v
CHEMBL116940 10258 0 5HT2A 5-HT2A receptor Rat 6.9 pEC50 = 6.9 Binding
Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptorTested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor
ChEMBL 295 2 1 3 3.2 COc1cc(Br)c2occ3c2c1[C@H](CN)CC3 10.1021/jm030064v
122442251 137568 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770225 137568 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771396 137568 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
107992 2397 40 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
165 2397 40 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
CHEMBL269521 2397 40 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
DB12111 2397 40 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
72197306 101776 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A 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-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 276 2 2 6 -0.0 CNc1nc(N2CCN(C)CC2)nc2c1CCNCC2 10.1016/j.ejmech.2013.02.020
CHEMBL2393231 101776 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A 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-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 276 2 2 6 -0.0 CNc1nc(N2CCN(C)CC2)nc2c1CCNCC2 10.1016/j.ejmech.2013.02.020
CHEMBL3040287 101776 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A 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-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 276 2 2 6 -0.0 CNc1nc(N2CCN(C)CC2)nc2c1CCNCC2 10.1016/j.ejmech.2013.02.020
107992 2397 40 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
165 2397 40 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
CHEMBL269521 2397 40 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
DB12111 2397 40 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
118733762 119876 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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
155534560 175570 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br 10.1016/j.ejmech.2019.111626
CHEMBL4470610 175570 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br 10.1016/j.ejmech.2019.111626
CHEMBL4596162 175570 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br 10.1016/j.ejmech.2019.111626
CHEMBL4634942 176334 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
ChEMBL 222 0 1 2 2.4 CC1CN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
53324327 56336 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)ccn1 10.1016/j.bmcl.2010.11.089
CHEMBL1643857 56336 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)ccn1 10.1016/j.bmcl.2010.11.089
16115517 84177 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
11206703 90420 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 C[C@@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
CHEMBL2397887 90420 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 C[C@@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
155534560 175570 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br 10.1016/j.ejmech.2019.111626
CHEMBL4470610 175570 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br 10.1016/j.ejmech.2019.111626
CHEMBL4596162 175570 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br 10.1016/j.ejmech.2019.111626
57799306 88440 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337493 88440 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365469 88440 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL4634785 176324 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
ChEMBL 230 0 1 2 1.8 C1=CC2CNCCN3C[C@@H]4CCC[C@@H]4C(=C1)C23 10.1016/j.bmcl.2019.126929
9881119 199032 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 232 2 1 3 1.7 C[C@H](N)CN1CCc2ccc3c(c21)CCCO3 10.1016/j.bmcl.2003.05.001
CHEMBL80482 199032 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 232 2 1 3 1.7 C[C@H](N)CN1CCc2ccc3c(c21)CCCO3 10.1016/j.bmcl.2003.05.001
134139964 145351 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A 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 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A 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
5 134 60 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
5202 134 60 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
CHEMBL39 134 60 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
DB08839 134 60 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
11160564 62750 2 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1021/jm0709034
CHEMBL179337 62750 2 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1021/jm0709034
11608308 63753 1 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
CHEMBL181076 63753 1 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
24773809 94200 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 C[C@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
CHEMBL254009 94200 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
728636 113565 3 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 188 3 2 1 2.4 CC[C@@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2014.07.062
CHEMBL3330646 113565 3 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 188 3 2 1 2.4 CC[C@@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2014.07.062
134265669 179379 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Agonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 223 0 1 3 1.5 Clc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
CHEMBL4750216 179379 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Agonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
ChEMBL 223 0 1 3 1.5 Clc1ccnc2c1CC[C@@H]1CNCCN21 10.1016/j.bmcl.2021.127872
16115388 136577 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 284 1 1 2 2.6 CC[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
CHEMBL375302 136577 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 284 1 1 2 2.6 CC[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
11514226 88441 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
11609026 88458 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337500 88458 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365705 88458 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
137655657 157958 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 316 7 1 4 3.1 COc1ccc(F)cc1C1CC1CNCc1cccnc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4094164 157958 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 316 7 1 4 3.1 COc1ccc(F)cc1C1CC1CNCc1cccnc1OC 10.1021/acs.jmedchem.7b00584
71562661 86639 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
CHEMBL2331794 86639 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
137655657 157958 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 316 7 1 4 3.1 COc1ccc(F)cc1C1CC1CNCc1cccnc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4094164 157958 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 316 7 1 4 3.1 COc1ccc(F)cc1C1CC1CNCc1cccnc1OC 10.1021/acs.jmedchem.7b00584
10017554 4093 19 5HT2A 5-HT2A receptor Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
CHEMBL101008 4093 19 5HT2A 5-HT2A receptor Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
10017554 4093 19 5HT2A 5-HT2A receptor Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulationAgonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulation
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1016/j.bmc.2008.04.030
CHEMBL101008 4093 19 5HT2A 5-HT2A receptor Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulationAgonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulation
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1016/j.bmc.2008.04.030
44586224 187455 0 5HT2A 5-HT2A receptor Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulationAgonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulation
ChEMBL 309 2 1 3 3.4 CC(N)Cc1c2c(c(Br)c3ccoc13)OCCC2 10.1016/j.bmc.2008.04.030
CHEMBL520449 187455 0 5HT2A 5-HT2A receptor Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulationAgonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulation
ChEMBL 309 2 1 3 3.4 CC(N)Cc1c2c(c(Br)c3ccoc13)OCCC2 10.1016/j.bmc.2008.04.030
439280 119259 96 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1016/j.bmcl.2015.07.030
6971044 119259 96 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1016/j.bmcl.2015.07.030
CHEMBL350221 119259 96 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1016/j.bmcl.2015.07.030
46884102 7798 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A 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 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A 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
46230099 192901 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A 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 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A 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
10363198 126615 0 5HT2A 5-HT2A receptor Rat 6.9 pEC50 = 6.9 Functional
Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cellsSerotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
ChEMBL 303 5 1 4 2.5 COc1cc([C@@H](OC)[C@@H](C)N)c(OC)cc1Br 10.1021/jm040082s
CHEMBL365958 126615 0 5HT2A 5-HT2A receptor Rat 6.9 pEC50 = 6.9 Functional
Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cellsSerotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
ChEMBL 303 5 1 4 2.5 COc1cc([C@@H](OC)[C@@H](C)N)c(OC)cc1Br 10.1021/jm040082s
71562661 86639 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
CHEMBL2331794 86639 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
118733808 119888 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
CHEMBL3416056 119888 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
CHEMBL3546908 119888 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
11414184 82849 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)C2CNCCN12 10.1021/jm0612968
CHEMBL220274 82849 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)C2CNCCN12 10.1021/jm0612968
166 3157 5 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Binding
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
3045227 3157 5 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Binding
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
CHEMBL76781 3157 5 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Binding
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
166 3157 5 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
3045227 3157 5 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
CHEMBL76781 3157 5 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
137655188 160400 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O 10.1021/acs.jmedchem.7b00584
CHEMBL4094054 160400 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O 10.1021/acs.jmedchem.7b00584
CHEMBL4117988 160400 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O 10.1021/acs.jmedchem.7b00584
134265622 163929 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 259 1 1 3 2.4 CC(C)(C)Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4217787 163929 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 259 1 1 3 2.4 CC(C)(C)Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
46228422 193622 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL595553 193622 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
137655188 160400 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O 10.1021/acs.jmedchem.7b00584
CHEMBL4094054 160400 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O 10.1021/acs.jmedchem.7b00584
CHEMBL4117988 160400 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O 10.1021/acs.jmedchem.7b00584
9977915 124891 0 5HT2A 5-HT2A receptor Rat 5.9 pEC50 = 5.9 Functional
Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cellsSerotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
ChEMBL 303 5 1 4 2.5 COc1cc([C@H](OC)[C@@H](C)N)c(OC)cc1Br 10.1021/jm040082s
CHEMBL364718 124891 0 5HT2A 5-HT2A receptor Rat 5.9 pEC50 = 5.9 Functional
Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cellsSerotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
ChEMBL 303 5 1 4 2.5 COc1cc([C@H](OC)[C@@H](C)N)c(OC)cc1Br 10.1021/jm040082s
10131066 21215 0 5HT2A 5-HT2A receptor Rat 6.9 pEC50 = 6.9 Functional
In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cellsIn vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells
ChEMBL 244 2 1 3 2.4 CC(N)Cc1cn(C)c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL131736 21215 0 5HT2A 5-HT2A receptor Rat 6.9 pEC50 = 6.9 Functional
In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cellsIn vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells
ChEMBL 244 2 1 3 2.4 CC(N)Cc1cn(C)c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL4635105 176343 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
ChEMBL 236 0 1 2 2.5 CC1(C)CN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
11608308 63753 1 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
CHEMBL181076 63753 1 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
71681897 90447 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 258 0 1 3 1.0 O=C1c2ccc3c(c2C[C@@H]2CNCCN12)OCCC3 10.1016/j.bmcl.2013.04.061
CHEMBL2397914 90447 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 258 0 1 3 1.0 O=C1c2ccc3c(c2C[C@@H]2CNCCN12)OCCC3 10.1016/j.bmcl.2013.04.061
53324165 56287 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 231 2 2 5 0.8 CCNc1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
CHEMBL1643674 56287 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 231 2 2 5 0.8 CCNc1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
137640063 160397 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4072722 160397 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4117953 160397 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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
9901086 184954 21 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A 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 5HT2A 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 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
CHEMBL494947 184954 21 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A 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 5HT2A 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 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
CHEMBL4644872 177048 0 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 ADMET
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
ChEMBL 236 0 1 2 2.7 Cc1cc2c3c(c1Cl)C(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
137640063 160397 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4072722 160397 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 315 7 1 3 3.7 COc1ccccc1CNC[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4117953 160397 0 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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
44572657 12179 3 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
CHEMBL1186169 12179 3 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
CHEMBL452719 12179 3 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
12370465 12383 12 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
9901086 184954 21 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A 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 5HT2A 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 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
CHEMBL494947 184954 21 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A 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 5HT2A 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 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
2402 3168 48 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O nan
5095 3168 48 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O nan
7295 3168 48 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O nan
CHEMBL589 3168 48 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O nan
DB00268 3168 48 5HT2A 5-HT2A receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O nan
10042913 67464 0 5HT2A 5-HT2A receptor Rat 5.9 pEC50 = 5.9 Functional
Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cellsSerotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
ChEMBL 303 5 1 4 2.5 COc1cc([C@H](OC)[C@H](C)N)c(OC)cc1Br 10.1021/jm040082s
CHEMBL191420 67464 0 5HT2A 5-HT2A receptor Rat 5.9 pEC50 = 5.9 Functional
Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cellsSerotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
ChEMBL 303 5 1 4 2.5 COc1cc([C@H](OC)[C@H](C)N)c(OC)cc1Br 10.1021/jm040082s
11949706 193641 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A 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 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A 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
137629242 160177 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1cscc1CNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4070259 160177 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1cscc1CNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116195 160177 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1cscc1CNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
137629242 160177 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1cscc1CNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4070259 160177 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1cscc1CNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
CHEMBL4116195 160177 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 321 7 1 4 3.8 COc1cscc1CNCC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.7b00584
16743289 59034 3 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell line
ChEMBL 200 2 1 2 2.1 NCCc1cn2c3c(cccc13)CCC2 10.1016/s0960-894x(00)00141-4
CHEMBL171774 59034 3 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell line
ChEMBL 200 2 1 2 2.1 NCCc1cn2c3c(cccc13)CCC2 10.1016/s0960-894x(00)00141-4
44586223 183247 0 5HT2A 5-HT2A receptor Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulationAgonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulation
ChEMBL 297 2 1 3 2.2 NCCc1c2c(c(Br)c3c1OCCC3)OCC2 10.1016/j.bmc.2008.04.030
CHEMBL482704 183247 0 5HT2A 5-HT2A receptor Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulationAgonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulation
ChEMBL 297 2 1 3 2.2 NCCc1c2c(c(Br)c3c1OCCC3)OCC2 10.1016/j.bmc.2008.04.030
137628797 160165 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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
5 134 60 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5202 134 60 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
CHEMBL39 134 60 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
DB08839 134 60 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
118733806 119887 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3416055 119887 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3546907 119887 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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
137628797 160165 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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
24826957 90445 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 246 1 1 3 1.0 COc1ccc(C)c2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397912 90445 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 246 1 1 3 1.0 COc1ccc(C)c2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
44572804 12332 1 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1 10.1021/jm801354e
CHEMBL1187088 12332 1 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1 10.1021/jm801354e
CHEMBL490064 12332 1 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1 10.1021/jm801354e
5 134 60 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5202 134 60 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
CHEMBL39 134 60 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
DB08839 134 60 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A 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 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
7153 97330 60 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A 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 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A 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
22292784 64038 8 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1016/j.bmcl.2004.12.080
CHEMBL181672 64038 8 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1016/j.bmcl.2004.12.080
11952353 193447 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A 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 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A 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
137661673 158524 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5-HT2A receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2A receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 301 3 0 5 3.6 CCn1nc(-c2cccc3cccnc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
CHEMBL4100216 158524 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5-HT2A receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2A receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL 301 3 0 5 3.6 CCn1nc(-c2cccc3cccnc23)cc1-c1cccnn1 10.1021/acs.jmedchem.7b00385
122442263 137565 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
CHEMBL1093698 8175 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
ChEMBL 352 5 2 3 3.3 C[C@H]1CC[C@@H](Oc2c(F)cc(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
72197481 101690 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A 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-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 3 2 6 1.8 CN1CCN(c2nc3c(c(Nc4ccc(F)cc4)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
CHEMBL2393240 101690 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A 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-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 3 2 6 1.8 CN1CCN(c2nc3c(c(Nc4ccc(F)cc4)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
CHEMBL3039632 101690 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A 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-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 3 2 6 1.8 CN1CCN(c2nc3c(c(Nc4ccc(F)cc4)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
155548667 175522 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4537637 175522 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4595810 175522 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
155548667 175522 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4537637 175522 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4595810 175522 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4776557 180813 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2AR (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
11658860 2206 41 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
2941 2206 41 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
4374 2206 41 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
CHEMBL360328 2206 41 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
DB04871 2206 41 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
22292784 64038 8 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1021/jm0709034
CHEMBL181672 64038 8 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1021/jm0709034
10329912 62001 3 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21 10.1021/jm0709034
CHEMBL178252 62001 3 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21 10.1021/jm0709034
24773979 129386 13 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1021/jm0709034
CHEMBL367796 129386 13 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1021/jm0709034
24773978 153614 1 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 209 0 1 1 2.8 CC1(C)CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL398926 153614 1 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 209 0 1 1 2.8 CC1(C)CNCCc2ccc(Cl)cc21 10.1021/jm0709034
5 134 60 5HT2A 5-HT2A receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assayAgonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm400408r
5202 134 60 5HT2A 5-HT2A receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assayAgonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm400408r
CHEMBL39 134 60 5HT2A 5-HT2A receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assayAgonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm400408r
DB08839 134 60 5HT2A 5-HT2A receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assayAgonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm400408r
9991444 62081 0 5HT2A 5-HT2A receptor Human 7.8 pEC50 = 7.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178366 62081 0 5HT2A 5-HT2A receptor Human 7.8 pEC50 = 7.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
44431701 87476 0 5HT2A 5-HT2A receptor Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 311 4 1 6 3.4 Cc1noc(Cc2c3ccoc3c(C[C@@H](C)N)c3ccoc23)n1 10.1016/j.bmcl.2007.03.073
CHEMBL234682 87476 0 5HT2A 5-HT2A receptor Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 311 4 1 6 3.4 Cc1noc(Cc2c3ccoc3c(C[C@@H](C)N)c3ccoc23)n1 10.1016/j.bmcl.2007.03.073
45484663 191958 0 5HT2A 5-HT2A receptor Dog 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
ChEMBL 293 2 1 5 1.7 Cc1nnc2c3c(nc(Cc4ccccc4)n12)CCNCC3 10.1016/j.bmcl.2009.07.063
CHEMBL576631 191958 0 5HT2A 5-HT2A receptor Dog 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
ChEMBL 293 2 1 5 1.7 Cc1nnc2c3c(nc(Cc4ccccc4)n12)CCNCC3 10.1016/j.bmcl.2009.07.063
132118109 150860 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assay
ChEMBL 161 3 1 1 2.4 C[C@H](N)C/C=C\c1ccccc1 10.1039/C6MD00245E
CHEMBL3963971 150860 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 ADMET
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assay
ChEMBL 161 3 1 1 2.4 C[C@H](N)C/C=C\c1ccccc1 10.1039/C6MD00245E
10329912 62001 3 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178252 62001 3 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21 10.1016/j.bmcl.2004.12.080
24773979 129386 13 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1016/j.bmcl.2004.12.080
CHEMBL367796 129386 13 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1016/j.bmcl.2004.12.080
44572755 12171 1 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL1186115 12171 1 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL450599 12171 1 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
18700190 163233 0 5HT2A 5-HT2A receptor Rat 6.8 pEC50 = 6.8 Functional
Antagonist activity at 5-HT2A receptor in Sprague-Dawley rat ielum assessed as reduction in 5-HT-evoked contractionAntagonist activity at 5-HT2A receptor in Sprague-Dawley rat ielum assessed as reduction in 5-HT-evoked contraction
ChEMBL 378 5 1 4 2.7 O=C(NCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccccn1 10.1016/j.bmc.2017.09.018
CHEMBL4209138 163233 0 5HT2A 5-HT2A receptor Rat 6.8 pEC50 = 6.8 Functional
Antagonist activity at 5-HT2A receptor in Sprague-Dawley rat ielum assessed as reduction in 5-HT-evoked contractionAntagonist activity at 5-HT2A receptor in Sprague-Dawley rat ielum assessed as reduction in 5-HT-evoked contraction
ChEMBL 378 5 1 4 2.7 O=C(NCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccccn1 10.1016/j.bmc.2017.09.018
155564300 175727 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 179 2 1 1 2.1 Cc1cccc([C@@]2(F)C[C@@H]2CN)c1 10.1016/j.ejmech.2019.111626
CHEMBL4570151 175727 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 179 2 1 1 2.1 Cc1cccc([C@@]2(F)C[C@@H]2CN)c1 10.1016/j.ejmech.2019.111626
CHEMBL4597482 175727 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 179 2 1 1 2.1 Cc1cccc([C@@]2(F)C[C@@H]2CN)c1 10.1016/j.ejmech.2019.111626
155564300 175727 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 179 2 1 1 2.1 Cc1cccc([C@@]2(F)C[C@@H]2CN)c1 10.1016/j.ejmech.2019.111626
CHEMBL4570151 175727 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 179 2 1 1 2.1 Cc1cccc([C@@]2(F)C[C@@H]2CN)c1 10.1016/j.ejmech.2019.111626
CHEMBL4597482 175727 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 179 2 1 1 2.1 Cc1cccc([C@@]2(F)C[C@@H]2CN)c1 10.1016/j.ejmech.2019.111626
11427139 84026 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 282 1 1 2 2.4 C=Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL222566 84026 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 282 1 1 2 2.4 C=Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
44315993 172033 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 222 3 1 3 2.1 CSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
CHEMBL451543 172033 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 222 3 1 3 2.1 CSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
11658860 2206 41 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
122442273 137564 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771152 137564 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771392 137564 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
118733824 119901 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.8 C=C(F)COc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416065 119901 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.8 C=C(F)COc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546960 119901 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.8 C=C(F)COc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
16115654 136187 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.1 Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374562 136187 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.1 Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
1355 1880 76 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
142 1880 76 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
CHEMBL478 1880 76 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
DB12110 1880 76 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
122442273 137564 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771152 137564 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771392 137564 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
11630623 88430 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
44572749 12149 1 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccccc1Cl 10.1021/jm801354e
CHEMBL1185954 12149 1 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccccc1Cl 10.1021/jm801354e
CHEMBL443128 12149 1 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccccc1Cl 10.1021/jm801354e
11983273 77405 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO 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 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO 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
25084025 12410 1 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
122442263 137565 0 5HT2A 5-HT2A receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
157 1938 5 5HT2A 5-HT2A receptor Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1016/j.bmcl.2007.03.073
9840090 1938 5 5HT2A 5-HT2A receptor Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1016/j.bmcl.2007.03.073
CHEMBL134519 1938 5 5HT2A 5-HT2A receptor Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1016/j.bmcl.2007.03.073
11160564 62750 2 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL179337 62750 2 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1016/j.bmcl.2004.12.080
44431687 148738 0 5HT2A 5-HT2A receptor Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 249 3 2 4 0.9 C[C@@H](N)Cc1c2c(c(CO)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
CHEMBL394664 148738 0 5HT2A 5-HT2A receptor Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 249 3 2 4 0.9 C[C@@H](N)Cc1c2c(c(CO)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
11221167 84020 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL222514 84020 0 5HT2A 5-HT2A receptor Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
11737032 84353 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 222 0 1 2 1.4 O=C1c2c(Cl)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL223896 84353 0 5HT2A 5-HT2A receptor Human 5.8 pEC50 = 5.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 222 0 1 2 1.4 O=C1c2c(Cl)cccc2C2CNCCN12 10.1021/jm0612968
16086382 138755 5 5HT2A 5-HT2A receptor Rat 7.8 pEC50 = 7.8 Functional
Activity at rat 5HT2A receptor expressed in NIH3T3 cells assessed as stimulation of phospholipase C-mediated IP productionActivity at rat 5HT2A receptor expressed in NIH3T3 cells assessed as stimulation of phospholipase C-mediated IP production
ChEMBL 271 3 1 3 2.1 COc1cc(Br)c(OC)c2c1[C@H](CN)C2 10.1021/jm060656o
CHEMBL379637 138755 5 5HT2A 5-HT2A receptor Rat 7.8 pEC50 = 7.8 Functional
Activity at rat 5HT2A receptor expressed in NIH3T3 cells assessed as stimulation of phospholipase C-mediated IP productionActivity at rat 5HT2A receptor expressed in NIH3T3 cells assessed as stimulation of phospholipase C-mediated IP production
ChEMBL 271 3 1 3 2.1 COc1cc(Br)c(OC)c2c1[C@H](CN)C2 10.1021/jm060656o
5 134 60 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 nan
5202 134 60 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 nan
CHEMBL39 134 60 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 nan
DB08839 134 60 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 nan
145709 113563 15 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 194 2 2 1 2.3 NCCc1c[nH]c2c(Cl)cccc12 10.1016/j.bmcl.2014.07.062
CHEMBL3330643 113563 15 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 194 2 2 1 2.3 NCCc1c[nH]c2c(Cl)cccc12 10.1016/j.bmcl.2014.07.062
1534 102327 48 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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
44622849 190384 0 5HT2A 5-HT2A receptor Dog 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
ChEMBL 293 2 1 5 1.7 Cc1nc2c3c(nc(Cc4ccccc4)n2n1)CCNCC3 10.1016/j.bmcl.2009.07.063
CHEMBL565547 190384 0 5HT2A 5-HT2A receptor Dog 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
ChEMBL 293 2 1 5 1.7 Cc1nc2c3c(nc(Cc4ccccc4)n2n1)CCNCC3 10.1016/j.bmcl.2009.07.063
44315697 199064 0 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 254 4 1 3 2.6 CCSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
CHEMBL80731 199064 0 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 254 4 1 3 2.6 CCSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
10353268 97081 1 5HT2A 5-HT2A receptor Rat 6.7 pEC50 = 6.7 Functional
In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cellsIn vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells
ChEMBL 216 2 2 2 2.0 NCCc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL27173 97081 1 5HT2A 5-HT2A receptor Rat 6.7 pEC50 = 6.7 Functional
In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cellsIn vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells
ChEMBL 216 2 2 2 2.0 NCCc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
10082834 34065 1 5HT2A 5-HT2A receptor Rat 4.7 pEC50 = 4.7 Binding
Evaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptorEvaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptor
ChEMBL 236 4 1 2 2.4 COc1ccc2[nH]cc(CCN(C)C)c2c1F 10.1021/jm000339w
CHEMBL142862 34065 1 5HT2A 5-HT2A receptor Rat 4.7 pEC50 = 4.7 Binding
Evaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptorEvaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptor
ChEMBL 236 4 1 2 2.4 COc1ccc2[nH]cc(CCN(C)C)c2c1F 10.1021/jm000339w
118733810 119889 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
CHEMBL3416057 119889 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
CHEMBL3546909 119889 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
155535970 175804 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4472830 175804 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4598081 175804 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
155535970 175804 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4472830 175804 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
CHEMBL4598081 175804 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1 10.1016/j.ejmech.2019.111626
152 349 14 5HT2A 5-HT2A receptor Rat 6.7 pEC50 = 6.7 Functional
In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cellsIn vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm030205t
2107 349 14 5HT2A 5-HT2A receptor Rat 6.7 pEC50 = 6.7 Functional
In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cellsIn vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm030205t
CHEMBL275854 349 14 5HT2A 5-HT2A receptor Rat 6.7 pEC50 = 6.7 Functional
In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cellsIn vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm030205t
132118110 146677 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assay
ChEMBL 161 3 1 1 2.4 CC(N)C/C=C\c1ccccc1 10.1039/C6MD00245E
CHEMBL3930376 146677 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assay
ChEMBL 161 3 1 1 2.4 CC(N)C/C=C\c1ccccc1 10.1039/C6MD00245E
137630488 160251 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4101789 160251 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4116752 160251 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
137629850 160371 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4073406 160371 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4117722 160371 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
11716185 88395 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 250 1 2 2 1.7 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337497 88395 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 250 1 2 2 1.7 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2364998 88395 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 250 1 2 2 1.7 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
137630488 160251 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4101789 160251 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4116752 160251 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
137629850 160371 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4073406 160371 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
CHEMBL4117722 160371 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL 303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F 10.1021/acs.jmedchem.7b00584
44572800 12362 2 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
10496688 11646 1 5HT2A 5-HT2A receptor Rat 7.7 pEC50 = 7.7 Binding
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
ChEMBL 293 2 1 3 3.8 C[C@H](N)Cc1c2ccoc2c(Br)c2ccoc12 10.1021/jm000491y
CHEMBL1182731 11646 1 5HT2A 5-HT2A receptor Rat 7.7 pEC50 = 7.7 Binding
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
ChEMBL 293 2 1 3 3.8 C[C@H](N)Cc1c2ccoc2c(Br)c2ccoc12 10.1021/jm000491y
CHEMBL263083 11646 1 5HT2A 5-HT2A receptor Rat 7.7 pEC50 = 7.7 Binding
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
ChEMBL 293 2 1 3 3.8 C[C@H](N)Cc1c2ccoc2c(Br)c2ccoc12 10.1021/jm000491y
9822580 194105 0 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 404 3 2 3 5.1 Cn1ncc(Br)c1-c1cccc(NC(=O)Nc2ccc(Cl)cc2)c1 10.1021/jm9007328
CHEMBL598808 194105 0 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 404 3 2 3 5.1 Cn1ncc(Br)c1-c1cccc(NC(=O)Nc2ccc(Cl)cc2)c1 10.1021/jm9007328
CHEMBL4648350 177275 0 5HT2A 5-HT2A receptor Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acs.jnatprod.9b01061
25022622 187268 0 5HT2A 5-HT2A receptor Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulationAgonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulation
ChEMBL 311 2 1 3 2.6 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCCC2 10.1016/j.bmc.2008.04.030
CHEMBL519145 187268 0 5HT2A 5-HT2A receptor Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulationAgonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulation
ChEMBL 311 2 1 3 2.6 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCCC2 10.1016/j.bmc.2008.04.030
1534 102327 48 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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
CHEMBL4648350 177275 0 5HT2A 5-HT2A receptor Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acs.jnatprod.9b01061
157 1938 5 5HT2A 5-HT2A receptor Rat 7.7 pEC50 = 7.7 Functional
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
9840090 1938 5 5HT2A 5-HT2A receptor Rat 7.7 pEC50 = 7.7 Functional
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
CHEMBL134519 1938 5 5HT2A 5-HT2A receptor Rat 7.7 pEC50 = 7.7 Functional
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
9991444 62081 0 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
CHEMBL178366 62081 0 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
11658860 2206 41 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
11658860 2206 41 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
2941 2206 41 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
4374 2206 41 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
CHEMBL360328 2206 41 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
DB04871 2206 41 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
44573004 12232 1 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
58911582 90427 0 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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
CHEMBL4757142 182800 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802987 182800 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4757142 182800 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802987 182800 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
134149355 147322 0 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 ADMET
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 322 2 1 4 2.7 c1cc(Cc2ccc3c(c2)OCO3)c2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3935339 147322 0 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 ADMET
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 322 2 1 4 2.7 c1cc(Cc2ccc3c(c2)OCO3)c2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
216 2691 20 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/jm0709034
9815618 2691 20 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/jm0709034
CHEMBL253811 2691 20 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/jm0709034
11447552 61978 2 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
CHEMBL178231 61978 2 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
10465263 63776 50 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
24773895 94175 0 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@@H](C)CNCC2 10.1021/jm0709034
CHEMBL253806 94175 0 5HT2A 5-HT2A receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@@H](C)CNCC2 10.1021/jm0709034
134142903 144437 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 256 2 1 2 2.8 c1cc(CC2CCC2)c2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
CHEMBL3912721 144437 0 5HT2A 5-HT2A receptor Human 5.7 pEC50 = 5.7 ADMET
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
ChEMBL 256 2 1 2 2.8 c1cc(CC2CCC2)c2c(c1)N1CCNCC1CC2 10.1016/j.bmcl.2016.11.016
152 349 14 5HT2A 5-HT2A receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1016/j.bmcl.2018.04.059
2107 349 14 5HT2A 5-HT2A receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1016/j.bmcl.2018.04.059
CHEMBL275854 349 14 5HT2A 5-HT2A receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1016/j.bmcl.2018.04.059
5 134 60 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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
5 134 60 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of 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
5 134 60 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A 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 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A 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
146 130 72 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 10.1016/j.bmcl.2014.07.062
164682 130 72 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 10.1016/j.bmcl.2014.07.062
CHEMBL275628 130 72 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 10.1016/j.bmcl.2014.07.062
155532108 175715 0 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@]1(F)c1cccc(F)c1 10.1016/j.ejmech.2019.111626
CHEMBL4466591 175715 0 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@]1(F)c1cccc(F)c1 10.1016/j.ejmech.2019.111626
CHEMBL4597360 175715 0 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 ADMET
Agonist activity at recombinant human 5HT2A receptor 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 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@]1(F)c1cccc(F)c1 10.1016/j.ejmech.2019.111626
10544447 10786 3 5HT2A 5-HT2A receptor Rat 8.6 pEC50 = 8.6 Binding
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
ChEMBL 293 2 1 3 3.8 C[C@@H](N)Cc1c2ccoc2c(Br)c2ccoc12 10.1021/jm000491y
CHEMBL1177916 10786 3 5HT2A 5-HT2A receptor Rat 8.6 pEC50 = 8.6 Binding
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
ChEMBL 293 2 1 3 3.8 C[C@@H](N)Cc1c2ccoc2c(Br)c2ccoc12 10.1021/jm000491y
CHEMBL6706 10786 3 5HT2A 5-HT2A receptor Rat 8.6 pEC50 = 8.6 Binding
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
ChEMBL 293 2 1 3 3.8 C[C@@H](N)Cc1c2ccoc2c(Br)c2ccoc12 10.1021/jm000491y
50878551 90073 57 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90073 57 5HT2A 5-HT2A receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
12626561 197588 2 5HT2A 5-HT2A receptor Rat 7.7 pEC50 = 7.7 Functional
Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cellsSerotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
ChEMBL 273 4 1 3 2.4 COc1cc(C[C@@H](C)N)c(OC)cc1Br 10.1021/jm040082s
CHEMBL69700 197588 2 5HT2A 5-HT2A receptor Rat 7.7 pEC50 = 7.7 Functional
Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cellsSerotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
ChEMBL 273 4 1 3 2.4 COc1cc(C[C@@H](C)N)c(OC)cc1Br 10.1021/jm040082s
122442260 137562 0 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 5HT2A 5-HT2A receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
10609802 106470 2 5HT2A 5-HT2A receptor Rat 5.7 pEC50 = 5.7 Functional
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2A receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2A receptor
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2 10.1021/jm970219x
CHEMBL316527 106470 2 5HT2A 5-HT2A receptor Rat 5.7 pEC50 = 5.7 Functional
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2A receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2A receptor
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)