Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
5 139 66 None -20 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5202 139 66 None -20 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
CHEMBL39 139 66 None -20 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
DB08839 139 66 None -20 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5 139 66 None -20 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5202 139 66 None -20 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
CHEMBL39 139 66 None -20 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
DB08839 139 66 None -20 28 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
168289382 191187 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 2 4 4 2.8 COc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5198213 191187 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 2 4 4 2.8 COc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
168289382 191187 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 2 4 4 2.8 COc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5198213 191187 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 2 4 4 2.8 COc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
107 141 116 None 6309 3 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 141 116 None 6309 3 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 141 116 None 6309 3 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
5 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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
5 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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
5 139 66 None 2 28 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 139 66 None 2 28 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 139 66 None 2 28 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 139 66 None 2 28 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
5 139 66 None 2 28 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 139 66 None 2 28 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 139 66 None 2 28 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 139 66 None 2 28 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 197729 0 None - 1 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 197729 0 None - 1 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 2141 89 None -1 11 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 2141 89 None -1 11 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 2141 89 None -1 11 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 2141 89 None -1 11 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 2141 89 None -1 11 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 2141 89 None -1 11 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
5 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 119501 104 None -9 7 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 119501 104 None -9 7 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 119501 104 None -9 7 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
5 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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
168291775 191299 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5200026 191299 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
168291775 191299 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5200026 191299 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
5 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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
5 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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
4376990 192397 4 None -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 192397 4 None -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 192397 4 None -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
4376990 192397 4 None -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 192397 4 None -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 192397 4 None -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
145 140 48 None 6 12 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.2c00129
1832 140 48 None 6 12 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.2c00129
CHEMBL7257 140 48 None 6 12 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.2c00129
DB14010 140 48 None 6 12 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.2c00129
145 140 48 None 6 12 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.1c00577
1832 140 48 None 6 12 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.1c00577
CHEMBL7257 140 48 None 6 12 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.1c00577
DB14010 140 48 None 6 12 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.1c00577
5 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 119501 104 None -9 7 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 119501 104 None -9 7 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 119501 104 None -9 7 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
152743520 189376 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 326 8 1 5 2.9 COc1cc(CCNCc2ccccc2OC)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5170895 189376 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 326 8 1 5 2.9 COc1cc(CCNCc2ccccc2OC)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
11695000 88628 0 None -17 3 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 88628 0 None -17 3 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 88628 0 None -17 3 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 94373 0 None -2 3 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 94373 0 None -2 3 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
122180957 121245 0 None 20 2 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 121245 0 None 20 2 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
10105208 62155 0 None -15 3 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 62155 0 None -15 3 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 63592 20 None -7 3 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 63592 20 None -7 3 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 94402 0 None -12 3 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 94402 0 None -12 3 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 94459 0 None -10 3 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 94459 0 None -10 3 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 154147 2 None -1 3 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 154147 2 None -1 3 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 62155 0 None -15 3 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 62155 0 None -15 3 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 63420 0 None -12 3 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 63420 0 None -12 3 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 165585 0 None -9 3 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 165585 0 None -9 3 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 67027 0 None - 1 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 67027 0 None - 1 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
96783829 192190 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assay
ChEMBL 218 2 2 1 2.6 Fc1cccc2[nH]cc(C[C@H]3CCCN3)c12 10.1021/acsmedchemlett.2c00128
CHEMBL5174204 192190 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assay
ChEMBL 218 2 2 1 2.6 Fc1cccc2[nH]cc(C[C@H]3CCCN3)c12 10.1021/acsmedchemlett.2c00128
CHEMBL5221436 192190 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assay
ChEMBL 218 2 2 1 2.6 Fc1cccc2[nH]cc(C[C@H]3CCCN3)c12 10.1021/acsmedchemlett.2c00128
24773897 94404 3 None -251 2 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 94404 3 None -251 2 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 163528 0 None -1621 3 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 163528 0 None -1621 3 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 164195 0 None -309 3 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 164195 0 None -309 3 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 120148 0 None -15 3 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 120148 0 None -15 3 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 120148 0 None -15 3 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 120140 0 None -93 3 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 120140 0 None -93 3 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 120140 0 None -93 3 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 90667 0 None -85 2 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 90667 0 None -85 2 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
157114558 192252 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5187568 192252 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5221884 192252 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1O 10.1021/acsmedchemlett.1c00694
24826963 90670 0 None -74 2 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 90670 0 None -74 2 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 90675 0 None -6 2 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 90675 0 None -6 2 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
157114558 192252 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5187568 192252 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5221884 192252 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1O 10.1021/acsmedchemlett.1c00694
18735309 203712 0 None -21 3 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 203712 0 None -21 3 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 90652 0 None -6 2 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 90652 0 None -6 2 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 137812 0 None -7 2 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 137812 0 None -7 2 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 137812 0 None -7 2 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
168276822 189520 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 324 6 1 5 2.8 COc1cc(CCNC2COc3ccccc32)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5173321 189520 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 324 6 1 5 2.8 COc1cc(CCNC2COc3ccccc32)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
44412405 77413 0 None -5 3 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 77413 0 None -5 3 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 137812 0 None -7 2 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 137812 0 None -7 2 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 137812 0 None -7 2 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 90651 0 None -1 2 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 90651 0 None -1 2 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
162644827 183031 0 None -16 3 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 183031 0 None -16 3 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 183031 0 None -16 3 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
162644827 183031 0 None -16 3 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 183031 0 None -16 3 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 183031 0 None -16 3 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
162657367 183090 0 None -42 3 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
CHEMBL4756903 183090 0 None -42 3 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 183090 0 None -42 3 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
45485781 195705 0 None -23 2 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 195705 0 None -23 2 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
5 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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
122180976 121264 1 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 379 8 1 4 3.8 COc1cccc(CNCCc2cc(OC)c(Br)cc2OC)c1 10.1021/acs.jmedchem.2c00702
CHEMBL3589597 121264 1 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 379 8 1 4 3.8 COc1cccc(CNCCc2cc(OC)c(Br)cc2OC)c1 10.1021/acs.jmedchem.2c00702
122180977 121265 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 365 7 2 4 3.5 COc1cc(CCNCc2cccc(O)c2)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
CHEMBL3589598 121265 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 365 7 2 4 3.5 COc1cc(CCNCc2cccc(O)c2)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
CHEMBL5080051 212880 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL None None None Oc1cccc2[nH]cc(CCN3CCC3)c12 10.1021/acsmedchemlett.2c00129
3906894 101496 17 None -1 2 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 101496 17 None -1 2 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 122540 0 None -3 3 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 122540 0 None -3 3 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 58915 0 None -6 2 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 58915 0 None -6 2 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
11437171 83063 0 None -2 3 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 83063 0 None -2 3 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
162657367 183090 0 None -42 3 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
CHEMBL4756903 183090 0 None -42 3 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 183090 0 None -42 3 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
168272608 192181 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177484 192181 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221391 192181 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
162670523 183158 0 None -41 3 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
CHEMBL4790652 183158 0 None -41 3 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 183158 0 None -41 3 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 139007 10 None - 1 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 139007 10 None - 1 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 77400 5 None -10 3 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 77400 5 None -10 3 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
168272608 192181 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177484 192181 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221391 192181 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
162670523 183158 0 None -41 3 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
CHEMBL4790652 183158 0 None -41 3 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 183158 0 None -41 3 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 96572 23 None 4 2 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 96572 23 None 4 2 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 195820 0 None -4 2 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 195820 0 None -4 2 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
168282376 192274 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5189339 192274 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222002 192274 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
168282376 192274 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5189339 192274 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222002 192274 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
9856041 23895 2 None 1202 2 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 23895 2 None 1202 2 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 77882 2 None -5 3 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 77882 2 None -5 3 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
162659049 183101 0 None -13 3 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 183101 0 None -13 3 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 183101 0 None -13 3 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
162659049 183101 0 None -13 3 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 183101 0 None -13 3 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 183101 0 None -13 3 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 83818 2 None -74 3 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 83818 2 None -74 3 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
16086382 139007 10 None - 1 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 139007 10 None - 1 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 137819 0 None -47 3 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 137819 0 None -47 3 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 137819 0 None -47 3 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
16747713 87588 0 None 6 2 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 87588 0 None 6 2 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 101496 17 None -1 2 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 101496 17 None -1 2 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
5 139 66 None -20 28 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
5202 139 66 None -20 28 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
CHEMBL39 139 66 None -20 28 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
DB08839 139 66 None -20 28 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
CHEMBL4790446 212290 2 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL4803723 212290 2 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL4790446 212290 2 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL4803723 212290 2 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
1621 2386 16 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
17 2386 16 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
5761 2386 16 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
CHEMBL263881 2386 16 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
DB04829 2386 16 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
46233391 197511 0 None - 1 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 197511 0 None - 1 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
168280534 192256 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1C(F)(F)F 10.1021/acsmedchemlett.1c00694
CHEMBL5183493 192256 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1C(F)(F)F 10.1021/acsmedchemlett.1c00694
CHEMBL5221899 192256 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1C(F)(F)F 10.1021/acsmedchemlett.1c00694
15185771 67530 5 None - 1 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 67530 5 None - 1 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
168280534 192256 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1C(F)(F)F 10.1021/acsmedchemlett.1c00694
CHEMBL5183493 192256 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1C(F)(F)F 10.1021/acsmedchemlett.1c00694
CHEMBL5221899 192256 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1C(F)(F)F 10.1021/acsmedchemlett.1c00694
122442251 137819 0 None -47 3 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 137819 0 None -47 3 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 137819 0 None -47 3 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 2506 47 None -6 2 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 2506 47 None -6 2 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 2506 47 None -6 2 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 2506 47 None -6 2 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 102002 0 None - 1 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 102002 0 None - 1 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 102002 0 None - 1 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 2506 47 None -6 2 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 2506 47 None -6 2 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 2506 47 None -6 2 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 2506 47 None -6 2 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 120119 0 None -93 3 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 120119 0 None -93 3 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 120119 0 None -93 3 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
53324327 56541 0 None -2 3 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 56541 0 None -2 3 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 84400 0 None -87 3 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 84400 0 None -87 3 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 90647 0 None -40 3 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 90647 0 None -40 3 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
168268736 192177 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177718 192177 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221369 192177 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
168268736 192177 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177718 192177 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221369 192177 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
57799306 88666 0 None -47 3 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 88666 0 None -47 3 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 88666 0 None -47 3 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
9881119 203752 0 None -4 3 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 203752 0 None -4 3 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
5 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 62959 4 None -7 3 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 62959 4 None -7 3 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 63963 3 None -42 3 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 63963 3 None -42 3 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 94428 0 None -15 3 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 94428 0 None -15 3 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
3991761 192284 2 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 2 2 2 3.6 COc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5183437 192284 2 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 2 2 2 3.6 COc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222058 192284 2 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 2 2 2 3.6 COc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
728636 113792 4 None - 1 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 113792 4 None - 1 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
16115388 136828 0 None 2 3 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 136828 0 None 2 3 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
3991761 192284 2 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 2 2 2 3.6 COc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5183437 192284 2 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 2 2 2 3.6 COc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222058 192284 2 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 2 2 2 3.6 COc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
11514226 88667 0 None -114 3 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 88667 0 None -114 3 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 88667 0 None -114 3 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 88684 0 None -38 3 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 88684 0 None -38 3 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 88684 0 None -38 3 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
71562661 86865 0 None -3 2 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 86865 0 None -3 2 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
10017554 4260 25 None - 1 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 4260 25 None - 1 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 4260 25 None - 1 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 4260 25 None - 1 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 191586 0 None - 1 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 191586 0 None - 1 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
1621 2386 16 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
17 2386 16 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
5761 2386 16 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
CHEMBL263881 2386 16 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
DB04829 2386 16 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
439280 119501 104 None -9 7 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 119501 104 None -9 7 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 119501 104 None -9 7 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 7964 0 None -128 2 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 7964 0 None -128 2 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
5 139 66 None -20 28 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
5202 139 66 None -20 28 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
CHEMBL39 139 66 None -20 28 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
DB08839 139 66 None -20 28 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
46230099 197622 0 None -70 3 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 197622 0 None -70 3 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 126864 0 None - 1 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 126864 0 None - 1 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 86865 0 None -3 2 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 86865 0 None -3 2 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 120131 0 None -1 3 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 120131 0 None -1 3 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 120131 0 None -1 3 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 83071 0 None -5 3 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 83071 0 None -5 3 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 3295 12 None -36 4 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 3295 12 None -36 4 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 3295 12 None -36 4 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
134265622 164190 0 None -223 3 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 164190 0 None -223 3 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 198343 0 None -60 3 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 198343 0 None -60 3 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
168277051 192225 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5178562 192225 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221669 192225 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
168277051 192225 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5178562 192225 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221669 192225 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
168295524 192418 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 2 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5205848 192418 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 2 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222868 192418 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 2 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
168276542 189708 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 391 6 1 4 4.1 COc1cc(CCNC2CCOc3ccccc32)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
CHEMBL5176147 189708 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 391 6 1 4 4.1 COc1cc(CCNC2CCOc3ccccc32)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
168295524 192418 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 2 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5205848 192418 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 2 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222868 192418 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 2 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
9977915 125140 0 None - 1 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 125140 0 None - 1 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 21388 0 None 1513 2 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 21388 0 None 1513 2 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
168280316 192251 0 None -41 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5187275 192251 0 None -41 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221883 192251 0 None -41 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
168280316 192251 0 None -41 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5187275 192251 0 None -41 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221883 192251 0 None -41 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
11608308 63963 3 None -42 3 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 63963 3 None -42 3 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 90674 0 None -87 2 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 90674 0 None -87 2 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 56492 0 None -2 3 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 56492 0 None -2 3 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
9901086 187038 28 None -95 3 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 187038 28 None -95 3 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
168290116 192352 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 292 3 3 2 3.7 Oc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5193251 192352 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 292 3 3 2 3.7 Oc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222481 192352 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 292 3 3 2 3.7 Oc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
168290116 192352 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 292 3 3 2 3.7 Oc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5193251 192352 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 292 3 3 2 3.7 Oc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222481 192352 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 292 3 3 2 3.7 Oc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
44572657 12346 5 None -263 3 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 12346 5 None -263 3 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 12346 5 None -263 3 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 12550 16 None -109 3 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 12550 16 None -109 3 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 12550 16 None -109 3 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 187038 28 None -95 3 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 187038 28 None -95 3 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
10042913 67680 0 None - 1 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 67680 0 None - 1 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
168288579 192331 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 3 2 3.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5197871 192331 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 3 2 3.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5222382 192331 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 3 2 3.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
168288579 192331 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 3 2 3.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5197871 192331 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 3 2 3.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5222382 192331 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 3 2 3.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
11949706 198362 0 None -1445 2 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 198362 0 None -1445 2 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
16743289 59242 3 None -724 2 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 59242 3 None -724 2 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 183531 0 None - 1 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 183531 0 None - 1 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
168283046 192280 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185474 192280 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222039 192280 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
5 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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
168283046 192280 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185474 192280 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222039 192280 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
118733806 120130 0 None -46 3 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 120130 0 None -46 3 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 120130 0 None -46 3 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
24826957 90672 0 None -24 2 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 90672 0 None -24 2 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 12499 1 None -48 3 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 12499 1 None -48 3 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 12499 1 None -48 3 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
CHEMBL4757837 212287 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL4802974 212287 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL4757837 212287 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL4802974 212287 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
5 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 139 66 None -20 28 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 97557 74 None -1 4 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 97557 74 None -1 4 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 64248 12 None -5 3 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 64248 12 None -5 3 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 198168 0 None -1071 3 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 198168 0 None -1071 3 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
168268703 192164 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5170024 192164 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221265 192164 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
168268703 192164 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5170024 192164 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221265 192164 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
122442263 137816 0 None -15 3 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 137816 0 None -15 3 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 137816 0 None -15 3 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
46884137 8342 0 None -3 2 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
CHEMBL1093698 8342 0 None -3 2 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 101916 0 None 4 2 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 101916 0 None 4 2 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 101916 0 None 4 2 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
168280955 192263 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5184449 192263 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221926 192263 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
168280955 192263 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5184449 192263 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221926 192263 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
168288855 192336 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Cl)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5194467 192336 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Cl)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5222402 192336 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Cl)ccc1O 10.1021/acsmedchemlett.1c00694
11658860 2302 47 None -26 4 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 2302 47 None -26 4 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 2302 47 None -26 4 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 2302 47 None -26 4 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 2302 47 None -26 4 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 64248 12 None -5 3 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 64248 12 None -5 3 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
168280043 192247 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5188736 192247 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221859 192247 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
3568612 192383 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5203138 192383 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222646 192383 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
10329912 62207 6 None -3 2 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 62207 6 None -3 2 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 129634 17 None -4 3 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 129634 17 None -4 3 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 153870 1 None -7 2 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 153870 1 None -7 2 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
168288855 192336 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Cl)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5194467 192336 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Cl)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5222402 192336 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Cl)ccc1O 10.1021/acsmedchemlett.1c00694
168280043 192247 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5188736 192247 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221859 192247 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
9991444 62288 0 None -4 3 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 62288 0 None -4 3 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 87702 0 None 8 3 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 87702 0 None 8 3 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
3568612 192383 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5203138 192383 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222646 192383 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
45484663 196681 0 None - 1 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 196681 0 None - 1 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
10329912 62207 6 None -3 2 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 62207 6 None -3 2 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 129634 17 None -4 3 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 129634 17 None -4 3 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 12338 1 None -70 3 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 12338 1 None -70 3 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 12338 1 None -70 3 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 163495 0 None - 1 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 163495 0 None - 1 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
11427139 84249 0 None -38 3 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 84249 0 None -38 3 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 172298 0 None -16 3 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 172298 0 None -16 3 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
168288743 192335 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5192627 192335 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222395 192335 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
11658860 2302 47 None -26 4 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 2302 47 None -26 4 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 2302 47 None -26 4 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 2302 47 None -26 4 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 2302 47 None -26 4 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 137815 0 None -1 3 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 137815 0 None -1 3 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 137815 0 None -1 3 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 120144 0 None -75 2 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 120144 0 None -75 2 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 120144 0 None -75 2 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 136437 0 None -27 3 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 136437 0 None -27 3 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
168288743 192335 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5192627 192335 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222395 192335 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
1355 1972 82 None -4 6 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 1972 82 None -4 6 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 1972 82 None -4 6 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 1972 82 None -4 6 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 137815 0 None -1 3 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 137815 0 None -1 3 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 137815 0 None -1 3 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 88656 0 None -151 3 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 88656 0 None -151 3 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 88656 0 None -151 3 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 12316 1 None -32 3 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 12316 1 None -32 3 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 12316 1 None -32 3 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
168290300 191379 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 314 7 1 4 3.0 COc1cc(CCNCc2ccccc2F)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5201317 191379 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 314 7 1 4 3.0 COc1cc(CCNCc2ccccc2F)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
11983273 77627 0 None -2 3 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 77627 0 None -2 3 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 12577 1 None -117 3 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 12577 1 None -117 3 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 12577 1 None -117 3 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
168280082 190589 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 340 7 1 6 2.6 COc1cc(CCNCc2cccc3c2OCO3)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5189232 190589 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 340 7 1 6 2.6 COc1cc(CCNCc2cccc3c2OCO3)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
122442263 137816 0 None -15 3 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 137816 0 None -15 3 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 137816 0 None -15 3 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 2030 5 None 4 4 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 2030 5 None 4 4 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 2030 5 None 4 4 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 62959 4 None -7 3 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 62959 4 None -7 3 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
168276542 189708 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 391 6 1 4 4.1 COc1cc(CCNC2CCOc3ccccc32)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
CHEMBL5176147 189708 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 391 6 1 4 4.1 COc1cc(CCNC2CCOc3ccccc32)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
44431687 148995 0 None - 1 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 148995 0 None - 1 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 84243 0 None -25 3 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 84243 0 None -25 3 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
168268771 192179 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5174331 192179 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221385 192179 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
168268771 192179 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5174331 192179 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221385 192179 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
11737032 84578 0 None -47 3 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 84578 0 None -47 3 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 139007 10 None - 1 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 139007 10 None - 1 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
145709 113790 19 None - 1 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 113790 19 None - 1 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 102553 51 None 3 3 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 102553 51 None 3 3 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 102553 51 None 3 3 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 195106 0 None - 1 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 195106 0 None - 1 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 203784 0 None -8 3 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 203784 0 None -8 3 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 97308 1 None 2 5 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 97308 1 None 2 5 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
118733810 120132 0 None -19 3 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 120132 0 None -19 3 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 120132 0 None -19 3 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
3568128 192321 1 None -4 3 Human 5.7 pEC50 = 5.7