Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL157138 5ht2a_human Human Yes 10.7 EC50 = 0.0 nM Bind
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC
CHEMBL39 5ht2a_human Human Yes 9.6 EC50 = 0.3 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht2a_human Human Yes 9.6 EC50 = 0.3 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL8165 5ht2a_human Human Yes 9.3 EC50 = 0.5 nM Funct
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
190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2
CHEMBL39 5ht2a_human Human Yes 9.3 EC50 = 0.5 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht2a_human Human Yes 9.3 EC50 = 0.5 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht2a_mouse Mouse Yes 9.3 EC50 = 0.5 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht2a_mouse Mouse Yes 9.3 EC50 = 0.5 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL591223 5ht2a_human Human No 9.2 EC50 = 0.7 nM Funct
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
434 4 2 4 5.2 COc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Br)cnn1C
CHEMBL51 5ht2a_human Human Yes 9.0 EC50 = 1.0 nM Funct
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
395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2
CHEMBL39 5ht2a_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL350221 5ht2a_human Human Yes 8.9 EC50 = 1.3 nM Funct
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
220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O
CHEMBL39 5ht2a_human Human Yes 8.8 EC50 = 1.5 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht2a_human Human Yes 8.8 EC50 = 1.5 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht2a_human Human Yes 8.8 EC50 = 1.6 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL493 5ht2a_human Human Yes 8.8 EC50 = 1.8 nM Bind
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C
CHEMBL39 5ht2a_human Human Yes 8.7 EC50 = 1.9 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL350221 5ht2a_human Human Yes 8.7 EC50 = 1.9 nM Funct
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
220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O
CHEMBL2337490 5ht2a_human Human No 8.0 EC50 = 10 nM Funct
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
256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21
CHEMBL2365083 5ht2a_human Human No 8.0 EC50 = 10 nM Funct
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
256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21
CHEMBL253591 5ht2a_human Human No 8.0 EC50 = 10 nM Funct
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
229 0 1 1 3.2 C[C@H]1CNCCc2cc(Cl)c(Cl)cc21
CHEMBL2094028 5ht2a_human Human Yes 8.0 EC50 = 10 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
165 2 1 1 1.8 NC[C@H]1C[C@]1(F)c1ccccc1
CHEMBL2109749 5ht2a_human Human Yes 8.0 EC50 = 10 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
165 2 1 1 1.8 NC[C@H]1C[C@]1(F)c1ccccc1
CHEMBL3589578 5ht2a_human Human No 8.0 EC50 = 10.5 nM Funct
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
393 7 1 5 3.5 COc1cc(CCNCc2cccc3c2OCO3)c(OC)cc1Br
CHEMBL3956394 5ht2a_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
296 2 1 2 3.1 Fc1ccc2c(c1Cc1ccccc1)CCC1CNCCN21
CHEMBL178124 5ht2a_human Human No 7.0 EC50 = 100 nM Funct
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
229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21
CHEMBL180668 5ht2a_human Human Yes 7.0 EC50 = 100 nM Funct
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
181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2
CHEMBL253805 5ht2a_human Human No 7.0 EC50 = 100 nM Funct
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
229 0 1 1 3.2 C[C@@H]1CNCCc2cc(Cl)c(Cl)cc21
CHEMBL254215 5ht2a_human Human No 7.0 EC50 = 100 nM Funct
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
229 0 1 1 3.0 C[C@@H]1CNCCc2ccc(C(F)(F)F)cc21
CHEMBL399750 5ht2a_human Human Yes 7.0 EC50 = 100 nM Funct
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
225 1 1 2 2.6 COc1cc2c(cc1Cl)CCNCC2C
CHEMBL178124 5ht2a_human Human No 7.0 EC50 = 100 nM Funct
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
229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21
CHEMBL180166 5ht2a_human Human No 7.0 EC50 = 100 nM Funct
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
255 1 1 2 2.1 COc1cc2c(cc1Br)CCNCC2
CHEMBL426235 5ht2a_human Human No 7.0 EC50 = 100 nM Funct
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
283 2 1 2 3.1 CCC1CNCCc2cc(OC)c(Br)cc21
CHEMBL188709 5ht2a_rat Rat No 7.0 EC50 = 100 nM Funct
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
289 4 2 4 1.8 COc1cc([C@@H](O)[C@@H](C)N)c(OC)cc1Br
CHEMBL4206126 5ht2a_human Human No 6.0 EC50 = 1000 nM Funct
Agonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
285 2 1 3 2.3 FC(F)(F)CCc1ccnc2c1CC[C@@H]1CNCCN21
CHEMBL4757718 5ht2a_human Human No 6.0 EC50 = 1000 nM Funct
Agonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
284 2 1 2 2.9 FC(F)(F)CCc1cccc2c1CC[C@@H]1CNCCN21
CHEMBL253807 5ht2a_human Human Yes 6.0 EC50 = 1000 nM Funct
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
213 0 1 1 2.7 C[C@@H]1CNCCc2ccc(Cl)c(F)c21
CHEMBL4209572 5ht2a_human Human No 4.0 EC50 = 100000 nM Funct
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
189 0 1 3 0.8 c1cnc2c(c1)CC[C@@H]1CNCCN21
CHEMBL4217846 5ht2a_human Human No 4.0 EC50 = 100000 nM Funct
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
189 0 1 3 0.8 c1cc2c(cn1)N1CCNC[C@H]1CC2
CHEMBL3416049 5ht2a_human Human No 6.0 EC50 = 1005 nM Funct
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
235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN
CHEMBL3546975 5ht2a_human Human No 6.0 EC50 = 1005 nM Funct
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
235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN
CHEMBL3416061 5ht2a_human Human No 6.0 EC50 = 1025 nM Funct
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
223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@H]1C[C@@H]1CN
CHEMBL3546956 5ht2a_human Human No 6.0 EC50 = 1025 nM Funct
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
223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@H]1C[C@@H]1CN
CHEMBL2397907 5ht2a_human Human No 6.0 EC50 = 1030 nM Funct
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
232 1 1 3 0.7 COc1cccc2c1C[C@@H]1CNCCN1C2=O
CHEMBL3589595 5ht2a_human Human No 7.0 EC50 = 104.7 nM Bind
Partial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assayPartial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assay
397 8 1 4 3.9 COc1cc(CCNCc2cccc(OC)c2F)c(OC)cc1Br
CHEMBL2397910 5ht2a_human Human No 6.0 EC50 = 1046 nM Funct
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
230 0 1 2 1.3 Cc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O
CHEMBL2397915 5ht2a_human Human No 7.0 EC50 = 106 nM Funct
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
270 0 1 2 1.7 O=C1c2cc(C(F)(F)F)ccc2C[C@@H]2CNCCN12
CHEMBL80246 5ht2a_human Human No 6.0 EC50 = 1063 nM Funct
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
262 2 1 2 2.6 C[C@H](N)CN1CCc2cc(F)c(C(F)(F)F)cc21
CHEMBL2397892 5ht2a_human Human No 7.0 EC50 = 107 nM Funct
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
270 0 1 2 1.7 O=C1c2c(cccc2C(F)(F)F)C[C@@H]2CNCCN12
CHEMBL3769633 5ht2a_human Human No 6.0 EC50 = 1071.5 nM Funct
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
255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN
CHEMBL3771389 5ht2a_human Human No 6.0 EC50 = 1071.5 nM Funct
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
255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN
CHEMBL209155 5ht2a_human Human No 6.0 EC50 = 1080 nM Funct
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
255 1 1 1 3.4 FC(F)(F)c1cccc([C@H]2CC[C@H]3CNC[C@@H]23)c1
CHEMBL3769633 5ht2a_human Human No 6.0 EC50 = 1081 nM Funct
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
255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN
CHEMBL3771389 5ht2a_human Human No 6.0 EC50 = 1081 nM Funct
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
255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN
CHEMBL2397891 5ht2a_human Human No 7.0 EC50 = 109 nM Funct
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
242 1 1 2 1.5 O=C1c2c(cccc2C2CC2)C[C@@H]2CNCCN12
CHEMBL4739937 5ht2a_human Human No 7.0 EC50 = 109 nM Funct
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
217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN
CHEMBL4802378 5ht2a_human Human No 7.0 EC50 = 109 nM Funct
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
217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN
CHEMBL4739937 5ht2a_human Human No 7.0 EC50 = 109.7 nM Funct
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
217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN
CHEMBL4802378 5ht2a_human Human No 7.0 EC50 = 109.7 nM Funct
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
217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN
CHEMBL4756903 5ht2a_human Human No 7.0 EC50 = 109.7 nM Funct
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
231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4803034 5ht2a_human Human No 7.0 EC50 = 109.7 nM Funct
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
231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4090984 5ht2a_human Human No 6.0 EC50 = 1090 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
235 5 1 2 2.7 COc1ccc(F)cc1C1CC1CNC1CC1
CHEMBL4117952 5ht2a_human Human No 6.0 EC50 = 1090 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
235 5 1 2 2.7 COc1ccc(F)cc1C1CC1CNC1CC1
CHEMBL569342 5ht2a_human Human No 6.0 EC50 = 1090 nM Funct
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
368 5 1 6 1.8 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1C(F)(F)F
CHEMBL4090984 5ht2a_human Human No 6.0 EC50 = 1096.5 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
235 5 1 2 2.7 COc1ccc(F)cc1C1CC1CNC1CC1
CHEMBL4117952 5ht2a_human Human No 6.0 EC50 = 1096.5 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
235 5 1 2 2.7 COc1ccc(F)cc1C1CC1CNC1CC1
CHEMBL39 5ht2a_human Human Yes 8.0 EC50 = 11 nM Bind
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht2a_human Human Yes 8.0 EC50 = 11 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL301466 5ht2a_human Human Yes 7.9 EC50 = 11.8 nM Funct
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
271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12
CHEMBL360968 5ht2a_human Human No 7.0 EC50 = 110 nM Funct
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
283 2 1 2 3.1 CCOc1cc2c(cc1Br)C(C)CNCC2
CHEMBL170319 5ht2a_human Human No 6.0 EC50 = 1100 nM Funct
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
246 3 1 2 3.1 CNCCc1cn2c3c(cc(F)cc13)CCC2C
CHEMBL119323 5ht2a_rat Rat No 6.0 EC50 = 1100 nM Bind
Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptorTested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor
297 2 1 3 2.8 COc1cc(Br)c2c3c1[C@H](CN)CC[C@@H]3CO2
CHEMBL220207 5ht2a_human Human No 7.0 EC50 = 111 nM Funct
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
234 1 1 3 1.5 CSc1cccc2c1C(=O)N1CCNCC21
CHEMBL4756903 5ht2a_human Human No 7.0 EC50 = 111 nM Funct
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
231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4803034 5ht2a_human Human No 7.0 EC50 = 111 nM Funct
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
231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4790652 5ht2a_human Human No 7.0 EC50 = 112.2 nM Funct
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
233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2
CHEMBL4803766 5ht2a_human Human No 7.0 EC50 = 112.2 nM Funct
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
233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2
CHEMBL379637 5ht2a_rat Rat Yes 6.0 EC50 = 1120 nM Funct
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
271 3 1 3 2.1 COc1cc(Br)c(OC)c2c1[C@H](CN)C2
CHEMBL209106 5ht2a_human Human Yes 6.0 EC50 = 1120 nM Funct
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
206 1 1 2 1.6 Fc1cccc(N2CC[C@H]3CNC[C@H]32)c1
CHEMBL4632473 5ht2a_human Human No 6.0 EC50 = 1120 nM Funct
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
256 0 1 2 3.0 CC1CN2CCNCc3cc(Cl)c(Cl)c1c32
CHEMBL4790652 5ht2a_human Human No 7.0 EC50 = 113 nM Funct
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
233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2
CHEMBL4803766 5ht2a_human Human No 7.0 EC50 = 113 nM Funct
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
233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2
CHEMBL26687 5ht2a_rat Rat Yes 5.0 EC50 = 11300 nM Funct
Activity at rat 5HT2A receptor assessed as 5-HT-stimulated IP3 accumulationActivity at rat 5HT2A receptor assessed as 5-HT-stimulated IP3 accumulation
211 5 1 4 1.2 COc1cc(CCN)cc(OC)c1OC
CHEMBL570023 5ht2a_human Human No 6.9 EC50 = 114 nM Funct
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
348 5 1 6 1.8 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2Cl)n1
CHEMBL133868 5ht2a_rat Rat No 6.9 EC50 = 116 nM Funct
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
230 2 2 2 2.4 CC(N)Cc1c[nH]c2ccc3c(c12)CCCO3
CHEMBL210802 5ht2a_human Human Yes 6.9 EC50 = 116 nM Funct
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
258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CC[C@H]3CNC[C@H]32)n1
CHEMBL4761526 5ht2a_human Human No 6.9 EC50 = 117 nM Funct
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
219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2
CHEMBL4803123 5ht2a_human Human No 6.9 EC50 = 117 nM Funct
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
219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2
CHEMBL4761526 5ht2a_human Human No 6.9 EC50 = 117.5 nM Funct
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
219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2
CHEMBL4803123 5ht2a_human Human No 6.9 EC50 = 117.5 nM Funct
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
219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2
CHEMBL221113 5ht2a_human Human No 5.9 EC50 = 1170 nM Funct
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
284 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21
CHEMBL301265 5ht2a_human Human Yes 5.9 EC50 = 1174.9 nM Bind
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N
CHEMBL379637 5ht2a_rat Rat Yes 5.9 EC50 = 1180 nM Funct
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
271 3 1 3 2.1 COc1cc(Br)c(OC)c2c1[C@H](CN)C2
CHEMBL3770225 5ht2a_human Human No 6.9 EC50 = 119 nM Funct
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
229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN
CHEMBL3771396 5ht2a_human Human No 6.9 EC50 = 119 nM Funct
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
229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN
CHEMBL1177924 5ht2a_rat Rat No 7.9 EC50 = 12 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
283 2 1 3 4.1 C[C@H](N)Cc1c2ccoc2c(C(F)(F)F)c2ccoc12
CHEMBL6907 5ht2a_rat Rat No 7.9 EC50 = 12 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
283 2 1 3 4.1 C[C@H](N)Cc1c2ccoc2c(C(F)(F)F)c2ccoc12
CHEMBL234464 5ht2a_rat Rat No 7.9 EC50 = 12 nM Funct
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
263 4 1 4 1.6 COCc1c2c(c(C[C@@H](C)N)c3c1OCC3)OCC2
CHEMBL301466 5ht2a_human Human Yes 7.9 EC50 = 12 nM Funct
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
271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12
CHEMBL589769 5ht2a_human Human No 6.9 EC50 = 120 nM Funct
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
454 4 2 4 5.4 Cn1ncc(Br)c1-c1cccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)c1
CHEMBL191051 5ht2a_rat Rat Yes 6.9 EC50 = 120 nM Funct
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
289 5 1 4 2.1 COc1cc(C(CN)OC)c(OC)cc1Br
CHEMBL116940 5ht2a_rat Rat No 6.9 EC50 = 120 nM Bind
Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptorTested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor
295 2 1 3 3.2 COc1cc(Br)c2occ3c2c1[C@H](CN)CC3
CHEMBL3770225 5ht2a_human Human No 6.9 EC50 = 120.2 nM Funct
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
229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN
CHEMBL3771396 5ht2a_human Human No 6.9 EC50 = 120.2 nM Funct
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
229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN
CHEMBL269521 5ht2a_human Human Yes 5.9 EC50 = 1200 nM Funct
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
198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1
CHEMBL2393231 5ht2a_human Human No 5.9 EC50 = 1200 nM Funct
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
276 2 2 6 -0.0 CNc1nc(N2CCN(C)CC2)nc2c1CCNCC2
CHEMBL3040287 5ht2a_human Human No 5.9 EC50 = 1200 nM Funct
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
276 2 2 6 -0.0 CNc1nc(N2CCN(C)CC2)nc2c1CCNCC2
CHEMBL269521 5ht2a_human Human Yes 5.9 EC50 = 1202.3 nM Funct
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
198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1
CHEMBL3416033 5ht2a_human Human No 5.9 EC50 = 1215 nM Funct
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
225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN
CHEMBL3546889 5ht2a_human Human No 5.9 EC50 = 1215 nM Funct
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
225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN
CHEMBL4470610 5ht2a_human Human No 6.9 EC50 = 122 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br
CHEMBL4596162 5ht2a_human Human No 6.9 EC50 = 122 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br
CHEMBL4634942 5ht2a_human Human No 5.9 EC50 = 1220 nM Funct
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
222 0 1 2 2.4 CC1CN2CCNCc3ccc(Cl)c1c32
CHEMBL1643857 5ht2a_human Human No 5.9 EC50 = 1227 nM Funct
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
336 3 1 7 1.1 c1cc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)ccn1
CHEMBL223468 5ht2a_human Human No 6.9 EC50 = 123 nM Funct
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
246 2 1 3 1.4 CCc1ccc2c(c1OC)C(=O)N1CCNC[C@@H]21
CHEMBL2397887 5ht2a_human Human No 6.9 EC50 = 123 nM Funct
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
216 0 1 2 1.0 C[C@@H]1CNC[C@H]2Cc3ccccc3C(=O)N12
CHEMBL4470610 5ht2a_human Human No 6.9 EC50 = 123.0 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br
CHEMBL4596162 5ht2a_human Human No 6.9 EC50 = 123.0 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
243 2 1 1 2.6 NC[C@H]1C[C@]1(F)c1ccccc1Br
CHEMBL2337493 5ht2a_human Human No 6.9 EC50 = 124 nM Funct
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
222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21
CHEMBL2365469 5ht2a_human Human No 6.9 EC50 = 124 nM Funct
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
222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21
CHEMBL4634785 5ht2a_human Human No 5.9 EC50 = 1240 nM Funct
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
230 0 1 2 1.8 C1=CC2CNCCN3C[C@@H]4CCC[C@@H]4C(=C1)C23
CHEMBL80482 5ht2a_human Human No 6.9 EC50 = 125 nM Funct
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
232 2 1 3 1.7 C[C@H](N)CN1CCc2ccc3c(c21)CCCO3
CHEMBL3919795 5ht2a_human Human No 6.9 EC50 = 125.9 nM Funct
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
278 2 1 2 3.0 c1ccc(Cc2cccc3c2CCC2CNCCN32)cc1
CHEMBL39 5ht2a_human Human Yes 6.9 EC50 = 125.9 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL179337 5ht2a_human Human Yes 6.9 EC50 = 125.9 nM Funct
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
229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21
CHEMBL181076 5ht2a_human Human Yes 6.9 EC50 = 125.9 nM Funct
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
229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21
CHEMBL254009 5ht2a_human Human No 6.9 EC50 = 125.9 nM Funct
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
229 0 1 1 3.0 C[C@H]1CNCCc2ccc(C(F)(F)F)cc21
CHEMBL3330646 5ht2a_human Human Yes 5.9 EC50 = 1250 nM Funct
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
188 3 2 1 2.4 CC[C@@H](N)Cc1c[nH]c2ccccc12
CHEMBL4750216 5ht2a_human Human No 5.9 EC50 = 1258.9 nM Funct
Agonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
223 0 1 3 1.5 Clc1ccnc2c1CC[C@@H]1CNCCN21
CHEMBL375302 5ht2a_human Human No 6.9 EC50 = 126 nM Funct
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
284 1 1 2 2.6 CC[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12
CHEMBL2337494 5ht2a_human Human No 6.9 EC50 = 127 nM Funct
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
202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21
CHEMBL2365470 5ht2a_human Human No 6.9 EC50 = 127 nM Funct
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
202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21
CHEMBL2337500 5ht2a_human Human No 6.9 EC50 = 128 nM Funct
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
256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21
CHEMBL2365705 5ht2a_human Human No 6.9 EC50 = 128 nM Funct
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
256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21
CHEMBL4094164 5ht2a_human Human No 5.9 EC50 = 1288.3 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
316 7 1 4 3.1 COc1ccc(F)cc1C1CC1CNCc1cccnc1OC
CHEMBL2331794 5ht2a_human Human No 5.9 EC50 = 1288.3 nM Funct
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
244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1
CHEMBL4094164 5ht2a_human Human No 5.9 EC50 = 1290 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
316 7 1 4 3.1 COc1ccc(F)cc1C1CC1CNCc1cccnc1OC
CHEMBL101008 5ht2a_rat Rat Yes 7.9 EC50 = 13 nM Funct
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
297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2
CHEMBL101008 5ht2a_rat Rat Yes 7.9 EC50 = 13 nM Funct
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
297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2
CHEMBL520449 5ht2a_rat Rat No 7.9 EC50 = 13 nM Funct
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
309 2 1 3 3.4 CC(N)Cc1c2c(c(Br)c3ccoc13)OCCC2
CHEMBL350221 5ht2a_human Human Yes 6.9 EC50 = 130 nM Funct
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
220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O
CHEMBL1091106 5ht2a_human Human No 6.9 EC50 = 130 nM Funct
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
366 5 2 3 3.7 CC1(C)CCC(Oc2cc(F)c(CNC(=O)[C@@H]3CCCN3)cc2F)CC1
CHEMBL590483 5ht2a_human Human No 6.9 EC50 = 130 nM Funct
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
251 0 2 3 1.2 O=C1NC2CCNCCN2c2cccc(Cl)c21
CHEMBL365958 5ht2a_rat Rat No 6.9 EC50 = 130 nM Funct
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
303 5 1 4 2.5 COc1cc([C@@H](OC)[C@@H](C)N)c(OC)cc1Br
CHEMBL2331794 5ht2a_human Human No 5.9 EC50 = 1300 nM Funct
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
244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1
CHEMBL3416056 5ht2a_human Human No 5.9 EC50 = 1305 nM Funct
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
261 5 1 2 3.0 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC(F)F
CHEMBL3546908 5ht2a_human Human No 5.9 EC50 = 1305 nM Funct
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
261 5 1 2 3.0 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC(F)F
CHEMBL220274 5ht2a_human Human No 6.9 EC50 = 131 nM Funct
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
256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)C2CNCCN12
CHEMBL76781 5ht2a_human Human Yes 6.9 EC50 = 131 nM Bind
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N
CHEMBL76781 5ht2a_human Human Yes 6.9 EC50 = 131 nM Funct
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
226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N
CHEMBL4094054 5ht2a_human Human No 5.9 EC50 = 1310 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O
CHEMBL4117988 5ht2a_human Human No 5.9 EC50 = 1310 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O
CHEMBL4217787 5ht2a_human Human No 5.9 EC50 = 1310 nM Funct
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
259 1 1 3 2.4 CC(C)(C)Cc1ccnc2c1CC[C@@H]1CNCCN21
CHEMBL595553 5ht2a_human Human No 5.9 EC50 = 1311 nM Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
329 3 1 4 3.2 Clc1ccccc1O[C@@H]1CCc2ccc(N3CCNCC3)nc21
CHEMBL4094054 5ht2a_human Human No 5.9 EC50 = 1318.3 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O
CHEMBL4117988 5ht2a_human Human No 5.9 EC50 = 1318.3 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
328 7 2 3 2.8 COc1ccc(F)cc1C1CC1CNCc1ccccc1C(N)=O
CHEMBL364718 5ht2a_rat Rat No 5.9 EC50 = 1330 nM Funct
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
303 5 1 4 2.5 COc1cc([C@H](OC)[C@@H](C)N)c(OC)cc1Br
CHEMBL131736 5ht2a_rat Rat No 6.9 EC50 = 134 nM Funct
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
244 2 1 3 2.4 CC(N)Cc1cn(C)c2ccc3c(c12)CCCO3
CHEMBL4635105 5ht2a_human Human No 5.9 EC50 = 1340 nM Funct
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
236 0 1 2 2.5 CC1(C)CN2CCNCc3ccc(Cl)c1c32
CHEMBL181076 5ht2a_human Human Yes 6.9 EC50 = 135 nM Funct
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
229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21
CHEMBL2397914 5ht2a_human Human No 5.9 EC50 = 1379 nM Funct
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
258 0 1 3 1.0 O=C1c2ccc3c(c2C[C@@H]2CNCCN12)OCCC3
CHEMBL1643674 5ht2a_human Human No 6.9 EC50 = 138 nM Funct
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
231 2 2 5 0.8 CCNc1c2c(nc3ccnn13)CCNCC2
CHEMBL4117953 5ht2a_human Human No 6.9 EC50 = 138.0 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
315 7 1 3 3.7 COC1=C(C=C(C=C1)F)[C@H]2C[C@@H]2CNCC3=CC=CC=C3OC
CHEMBL494947 5ht2a_human Human Yes 6.9 EC50 = 138.0 nM Funct
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
304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1
CHEMBL4644872 5ht2a_human Human No 5.9 EC50 = 1380 nM Funct
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
236 0 1 2 2.7 Cc1cc2c3c(c1Cl)C(C)CN3CCNC2
CHEMBL4117953 5ht2a_human Human No 6.9 EC50 = 139 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
315 7 1 3 3.7 COC1=C(C=C(C=C1)F)[C@H]2C[C@@H]2CNCC3=CC=CC=C3OC
CHEMBL1186169 5ht2a_human Human Yes 5.9 EC50 = 1396 nM Funct
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
147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1
CHEMBL452719 5ht2a_human Human Yes 5.9 EC50 = 1396 nM Funct
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
147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1
CHEMBL1187354 5ht2a_human Human Yes 5.9 EC50 = 1399 nM Funct
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
147 2 1 1 1.7 NCC1CC1c1ccccc1
CHEMBL500093 5ht2a_human Human Yes 5.9 EC50 = 1399 nM Funct
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
147 2 1 1 1.7 NCC1CC1c1ccccc1
CHEMBL494947 5ht2a_human Human Yes 6.9 EC50 = 140 nM Funct
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
304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1
CHEMBL589 5ht2a_human Human Yes 6.9 EC50 = 141.3 nM Bind
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O
CHEMBL191420 5ht2a_rat Rat No 5.9 EC50 = 1410 nM Funct
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
303 5 1 4 2.5 COc1cc([C@H](OC)[C@H](C)N)c(OC)cc1Br
CHEMBL595645 5ht2a_human Human No 5.8 EC50 = 1428 nM Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
359 4 1 4 3.4 C[C@@H]1CNCCN1c1ccc2c(n1)[C@@H](OCc1cc(F)ccc1F)CC2
CHEMBL4070259 5ht2a_human Human No 6.8 EC50 = 144.5 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
321 7 1 4 3.8 COc1cscc1CNCC1CC1c1cc(F)ccc1OC
CHEMBL4116195 5ht2a_human Human No 6.8 EC50 = 144.5 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
321 7 1 4 3.8 COc1cscc1CNCC1CC1c1cc(F)ccc1OC
CHEMBL4070259 5ht2a_human Human No 6.8 EC50 = 145 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
321 7 1 4 3.8 COc1cscc1CNCC1CC1c1cc(F)ccc1OC
CHEMBL4116195 5ht2a_human Human No 6.8 EC50 = 145 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
321 7 1 4 3.8 COc1cscc1CNCC1CC1c1cc(F)ccc1OC
CHEMBL171774 5ht2a_human Human Yes 6.8 EC50 = 145 nM Funct
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
200 2 1 2 2.1 NCCc1cn2c3c(cccc13)CCC2
CHEMBL482704 5ht2a_rat Rat No 6.8 EC50 = 146 nM Funct
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
297 2 1 3 2.2 NCCc1c2c(c(Br)c3c1OCCC3)OCC2
CHEMBL4103313 5ht2a_human Human No 6.8 EC50 = 147.9 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC
CHEMBL4116143 5ht2a_human Human No 6.8 EC50 = 147.9 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC
CHEMBL39 5ht2a_human Human Yes 6.8 EC50 = 147.9 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL3416055 5ht2a_human Human No 5.8 EC50 = 1476 nM Funct
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
243 5 1 2 2.8 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCF
CHEMBL3546907 5ht2a_human Human No 5.8 EC50 = 1476 nM Funct
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
243 5 1 2 2.8 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCF
CHEMBL4103313 5ht2a_human Human No 6.8 EC50 = 148 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC
CHEMBL4116143 5ht2a_human Human No 6.8 EC50 = 148 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1sccc1OC
CHEMBL2397912 5ht2a_human Human No 6.8 EC50 = 148 nM Funct
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
246 1 1 3 1.0 COc1ccc(C)c2c1C[C@@H]1CNCCN1C2=O
CHEMBL1187088 5ht2a_human Human No 5.8 EC50 = 1485 nM Funct
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
215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1
CHEMBL490064 5ht2a_human Human No 5.8 EC50 = 1485 nM Funct
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
215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1
CHEMBL39 5ht2a_human Human Yes 6.8 EC50 = 150 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL272942 5ht2a_human Human Yes 6.8 EC50 = 150 nM Funct
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
214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O
CHEMBL181672 5ht2a_human Human Yes 6.8 EC50 = 150 nM Funct
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
195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21
CHEMBL594469 5ht2a_human Human No 5.8 EC50 = 1500 nM Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
345 4 1 4 3.0 Fc1ccc(F)c(CO[C@H]2CCc3ccc(N4CCNCC4)nc32)c1
CHEMBL4100216 5ht2a_human Human No 6.8 EC50 = 151 nM Funct
Agonist activity at recombinant human 5-HT2A receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2A receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
301 3 0 5 3.6 CCn1nc(-c2cccc3cccnc23)cc1-c1cccnn1
CHEMBL3769454 5ht2a_human Human No 6.8 EC50 = 151.4 nM Funct
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
245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN
CHEMBL3771393 5ht2a_human Human No 6.8 EC50 = 151.4 nM Funct
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
245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN
CHEMBL1093698 5ht2a_human Human No 6.8 EC50 = 153 nM Funct
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
352 5 2 3 3.3 C[C@H]1CC[C@@H](Oc2c(F)cc(CNC(=O)[C@@H]3CCCN3)cc2F)CC1
CHEMBL2393240 5ht2a_human Human No 6.8 EC50 = 153 nM Funct
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
356 3 2 6 1.8 CN1CCN(c2nc3c(c(Nc4ccc(F)cc4)n2)CCNCC3)CC1
CHEMBL3039632 5ht2a_human Human No 6.8 EC50 = 153 nM Funct
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
356 3 2 6 1.8 CN1CCN(c2nc3c(c(Nc4ccc(F)cc4)n2)CCNCC3)CC1
CHEMBL4537637 5ht2a_human Human No 6.8 EC50 = 154.9 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1
CHEMBL4595810 5ht2a_human Human No 6.8 EC50 = 154.9 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1
CHEMBL4537637 5ht2a_human Human No 6.8 EC50 = 156 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1
CHEMBL4595810 5ht2a_human Human No 6.8 EC50 = 156 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
179 3 1 1 2.1 CNC[C@H]1C[C@]1(F)c1ccccc1
CHEMBL4776557 5ht2a_human Human No 6.8 EC50 = 158.5 nM Funct
Agonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
230 2 1 2 2.4 CCCc1cccc2c1CC[C@@H]1CNCCN21
CHEMBL360328 5ht2a_human Human Yes 6.8 EC50 = 158.5 nM Funct
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
195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2
CHEMBL181672 5ht2a_human Human Yes 6.8 EC50 = 158.5 nM Funct
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
195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21
CHEMBL178252 5ht2a_human Human Yes 5.8 EC50 = 1584.9 nM Funct
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
179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21
CHEMBL367796 5ht2a_human Human Yes 5.8 EC50 = 1584.9 nM Funct
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
161 0 1 1 1.9 CC1CNCCc2ccccc21
CHEMBL398926 5ht2a_human Human Yes 5.8 EC50 = 1584.9 nM Funct
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
209 0 1 1 2.8 CC1(C)CNCCc2ccc(Cl)cc21
CHEMBL39 5ht2a_human Human Yes 7.8 EC50 = 16 nM Bind
Agonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assayAgonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL178366 5ht2a_human Human No 7.8 EC50 = 16 nM Funct
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
229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21
CHEMBL234682 5ht2a_rat Rat No 7.8 EC50 = 16.9 nM Funct
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
311 4 1 6 3.4 Cc1noc(Cc2c3ccoc3c(C[C@@H](C)N)c3ccoc23)n1
CHEMBL576631 5ht2a_canlf Dog No 5.8 EC50 = 1600 nM Funct
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
293 2 1 5 1.7 Cc1nnc2c3c(nc(Cc4ccccc4)n12)CCNCC3
CHEMBL3963971 5ht2a_human Human No 5.8 EC50 = 1600 nM Funct
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assay
161 3 1 1 2.4 C[C@H](N)C/C=C\c1ccccc1
CHEMBL178252 5ht2a_human Human Yes 5.8 EC50 = 1600 nM Funct
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
179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21
CHEMBL367796 5ht2a_human Human Yes 5.8 EC50 = 1600 nM Funct
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
161 0 1 1 1.9 CC1CNCCc2ccccc21
CHEMBL1186115 5ht2a_human Human No 5.8 EC50 = 1606 nM Funct
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
161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN
CHEMBL450599 5ht2a_human Human No 5.8 EC50 = 1606 nM Funct
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
161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN
CHEMBL4209138 5ht2a_rat Rat No 6.8 EC50 = 161 nM Funct
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
378 5 1 4 2.7 O=C(NCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccccn1
CHEMBL4570151 5ht2a_human Human No 6.8 EC50 = 162 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
179 2 1 1 2.1 Cc1cccc([C@@]2(F)C[C@@H]2CN)c1
CHEMBL4597482 5ht2a_human Human No 6.8 EC50 = 162 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
179 2 1 1 2.1 Cc1cccc([C@@]2(F)C[C@@H]2CN)c1
CHEMBL4570151 5ht2a_human Human No 6.8 EC50 = 162.2 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
179 2 1 1 2.1 Cc1cccc([C@@]2(F)C[C@@H]2CN)c1
CHEMBL4597482 5ht2a_human Human No 6.8 EC50 = 162.2 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
179 2 1 1 2.1 Cc1cccc([C@@]2(F)C[C@@H]2CN)c1
CHEMBL222566 5ht2a_human Human No 5.8 EC50 = 1620 nM Funct
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
282 1 1 2 2.4 C=Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21
CHEMBL451543 5ht2a_human Human No 6.8 EC50 = 164 nM Funct
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
222 3 1 3 2.1 CSc1ccc2c(c1)N(C[C@H](C)N)CC2
CHEMBL360328 5ht2a_human Human Yes 6.8 EC50 = 166.0 nM Funct
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
195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2
CHEMBL3771152 5ht2a_human Human No 6.8 EC50 = 166.0 nM Funct
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
271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN
CHEMBL3771392 5ht2a_human Human No 6.8 EC50 = 166.0 nM Funct
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
271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN
CHEMBL3416065 5ht2a_human Human No 5.8 EC50 = 1666 nM Funct
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
239 5 1 2 2.8 C=C(F)COc1ccc(F)cc1[C@H]1C[C@@H]1CN
CHEMBL3546960 5ht2a_human Human No 5.8 EC50 = 1666 nM Funct
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
239 5 1 2 2.8 C=C(F)COc1ccc(F)cc1[C@H]1C[C@@H]1CN
CHEMBL374562 5ht2a_human Human No 6.8 EC50 = 167 nM Funct
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
270 0 1 2 2.1 Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21
CHEMBL478 5ht2a_human Human Yes 6.8 EC50 = 167 nM Funct
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
196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1
CHEMBL3771152 5ht2a_human Human No 6.8 EC50 = 167 nM Funct
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
271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN
CHEMBL3771392 5ht2a_human Human No 6.8 EC50 = 167 nM Funct
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
271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN
CHEMBL2337499 5ht2a_human Human No 5.8 EC50 = 1674 nM Funct
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
250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O
CHEMBL2365399 5ht2a_human Human No 5.8 EC50 = 1674 nM Funct
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
250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O
CHEMBL1185954 5ht2a_human Human No 6.8 EC50 = 168 nM Funct
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
181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccccc1Cl
CHEMBL443128 5ht2a_human Human No 6.8 EC50 = 168 nM Funct
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
181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccccc1Cl
CHEMBL209714 5ht2a_human Human No 6.8 EC50 = 168 nM Funct
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
256 1 1 2 2.5 FC(F)(F)c1cccc(N2CC[C@H]3CNC[C@H]32)c1
CHEMBL1187522 5ht2a_human Human No 5.8 EC50 = 1680 nM Funct
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
225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1cccc(Br)c1
CHEMBL506727 5ht2a_human Human No 5.8 EC50 = 1680 nM Funct
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
225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1cccc(Br)c1
CHEMBL3769454 5ht2a_human Human No 7.8 EC50 = 17.8 nM Funct
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
245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN
CHEMBL3771393 5ht2a_human Human No 7.8 EC50 = 17.8 nM Funct
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
245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN
CHEMBL134519 5ht2a_rat Rat Yes 7.8 EC50 = 17.8 nM Funct
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
321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC
CHEMBL179337 5ht2a_human Human Yes 6.8 EC50 = 170 nM Funct
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
229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21
CHEMBL394664 5ht2a_rat Rat No 6.8 EC50 = 175 nM Funct
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
249 3 2 4 0.9 C[C@@H](N)Cc1c2c(c(CO)c3c1OCC3)OCC2
CHEMBL222514 5ht2a_human Human No 6.8 EC50 = 176 nM Funct
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
256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@@H]2CNCCN12
CHEMBL223896 5ht2a_human Human No 5.8 EC50 = 1780 nM Funct
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
222 0 1 2 1.4 O=C1c2c(Cl)cccc2C2CNCCN12
CHEMBL379637 5ht2a_rat Rat Yes 7.8 EC50 = 18 nM Funct
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
271 3 1 3 2.1 COc1cc(Br)c(OC)c2c1[C@H](CN)C2
CHEMBL39 5ht2a_human Human Yes 7.7 EC50 = 18.6 nM Bind
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL3330643 5ht2a_human Human Yes 7.7 EC50 = 18.8 nM Funct
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
194 2 2 1 2.3 NCCc1c[nH]c2c(Cl)cccc12
CHEMBL30713 5ht2a_human Human Yes 7.7 EC50 = 18.9 nM Funct
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
174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12
CHEMBL565547 5ht2a_canlf Dog No 5.8 EC50 = 1800 nM Funct
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
293 2 1 5 1.7 Cc1nc2c3c(nc(Cc4ccccc4)n2n1)CCNCC3
CHEMBL80731 5ht2a_human Human No 6.7 EC50 = 181 nM Funct
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
254 4 1 3 2.6 CCSc1cc2c(cc1F)CCN2C[C@H](C)N
CHEMBL27173 5ht2a_rat Rat No 6.7 EC50 = 181 nM Funct
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
216 2 2 2 2.0 NCCc1c[nH]c2ccc3c(c12)CCCO3
CHEMBL142862 5ht2a_rat Rat No 4.7 EC50 = 18100 nM Bind
Evaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptorEvaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptor
236 4 1 2 2.4 COc1ccc2[nH]cc(CCN(C)C)c2c1F
CHEMBL3416057 5ht2a_human Human No 5.7 EC50 = 1811 nM Funct
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
261 5 1 2 3.0 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC(F)F
CHEMBL3546909 5ht2a_human Human No 5.7 EC50 = 1811 nM Funct
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
261 5 1 2 3.0 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC(F)F
CHEMBL4472830 5ht2a_human Human No 5.7 EC50 = 1819.7 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1
CHEMBL4598081 5ht2a_human Human No 5.7 EC50 = 1819.7 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1
CHEMBL4472830 5ht2a_human Human No 5.7 EC50 = 1829 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1
CHEMBL4598081 5ht2a_human Human No 5.7 EC50 = 1829 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
165 2 1 1 1.8 NC[C@@H]1C[C@@]1(F)c1ccccc1
CHEMBL275854 5ht2a_rat Rat Yes 6.7 EC50 = 184 nM Funct
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
190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N
CHEMBL3930376 5ht2a_human Human No 5.7 EC50 = 1860 nM Funct
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assay
161 3 1 1 2.4 CC(N)C/C=C\c1ccccc1
CHEMBL4101789 5ht2a_human Human No 5.7 EC50 = 1862.1 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F
CHEMBL4116752 5ht2a_human Human No 5.7 EC50 = 1862.1 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F
CHEMBL4073406 5ht2a_human Human No 5.7 EC50 = 1862.1 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F
CHEMBL4117722 5ht2a_human Human No 5.7 EC50 = 1862.1 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F
CHEMBL2337497 5ht2a_human Human No 5.7 EC50 = 1872 nM Funct
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
250 1 2 2 1.7 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O
CHEMBL2364998 5ht2a_human Human No 5.7 EC50 = 1872 nM Funct
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
250 1 2 2 1.7 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O
CHEMBL4101789 5ht2a_human Human No 5.7 EC50 = 1880 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F
CHEMBL4116752 5ht2a_human Human No 5.7 EC50 = 1880 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
303 6 1 2 3.9 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1F
CHEMBL4073406 5ht2a_human Human No 5.7 EC50 = 1880 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F
CHEMBL4117722 5ht2a_human Human No 5.7 EC50 = 1880 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
303 6 1 2 3.9 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1F
CHEMBL1187194 5ht2a_human Human Yes 5.7 EC50 = 1886 nM Funct
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
181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1
CHEMBL493128 5ht2a_human Human Yes 5.7 EC50 = 1886 nM Funct
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
181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1
CHEMBL1182731 5ht2a_rat Rat No 7.7 EC50 = 19 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
293 2 1 3 3.8 C[C@H](N)Cc1c2ccoc2c(Br)c2ccoc12
CHEMBL263083 5ht2a_rat Rat No 7.7 EC50 = 19 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
293 2 1 3 3.8 C[C@H](N)Cc1c2ccoc2c(Br)c2ccoc12
CHEMBL598808 5ht2a_human Human No 7.7 EC50 = 19 nM Funct
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
404 3 2 3 5.1 Cn1ncc(Br)c1-c1cccc(NC(=O)Nc2ccc(Cl)cc2)c1
CHEMBL4648350 5ht2a_mouse Mouse No 7.7 EC50 = 19 nM Funct
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
190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12
CHEMBL519145 5ht2a_rat Rat No 7.7 EC50 = 19 nM Funct
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
311 2 1 3 2.6 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCCC2
CHEMBL30713 5ht2a_human Human Yes 7.7 EC50 = 19.1 nM Funct
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
174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12
CHEMBL4648350 5ht2a_mouse Mouse No 7.7 EC50 = 19.1 nM Funct
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
190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12
CHEMBL134519 5ht2a_rat Rat Yes 7.7 EC50 = 19.8 nM Funct
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC
CHEMBL178366 5ht2a_human Human No 7.7 EC50 = 20.0 nM Funct
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
229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21
CHEMBL360328 5ht2a_human Human Yes 6.7 EC50 = 190 nM Funct
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
195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2
CHEMBL360328 5ht2a_human Human Yes 5.7 EC50 = 1920 nM Funct
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2
CHEMBL1186590 5ht2a_human Human No 5.7 EC50 = 1929 nM Funct
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
161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1
CHEMBL471202 5ht2a_human Human No 5.7 EC50 = 1929 nM Funct
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
161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1
CHEMBL2397894 5ht2a_human Human No 6.7 EC50 = 193 nM Funct
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
232 1 1 3 0.7 COc1cccc2c1C(=O)N1CCNC[C@H]1C2
CHEMBL4757142 5ht2a_human Human No 5.7 EC50 = 1949.8 nM Funct
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
251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2
CHEMBL4802987 5ht2a_human Human No 5.7 EC50 = 1949.8 nM Funct
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
251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2
CHEMBL4757142 5ht2a_human Human No 5.7 EC50 = 1960 nM Funct
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
251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2
CHEMBL4802987 5ht2a_human Human No 5.7 EC50 = 1960 nM Funct
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
251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2
CHEMBL3935339 5ht2a_human Human No 6.7 EC50 = 199.5 nM Funct
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
322 2 1 4 2.7 c1cc(Cc2ccc3c(c2)OCO3)c2c(c1)N1CCNCC1CC2
CHEMBL253811 5ht2a_human Human Yes 6.7 EC50 = 199.5 nM Funct
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
203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N
CHEMBL178231 5ht2a_human Human Yes 6.7 EC50 = 199.5 nM Funct
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
229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21
CHEMBL181172 5ht2a_human Human Yes 6.7 EC50 = 199.5 nM Funct
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
195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21
CHEMBL253806 5ht2a_human Human No 6.7 EC50 = 199.5 nM Funct
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
225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@@H](C)CNCC2
CHEMBL3912721 5ht2a_human Human No 5.7 EC50 = 1995.3 nM Funct
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
256 2 1 2 2.8 c1cc(CC2CCC2)c2c(c1)N1CCNCC1CC2
CHEMBL275854 5ht2a_human Human Yes 8.7 EC50 = 2 nM Funct
Agonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N
CHEMBL39 5ht2a_human Human Yes 8.6 EC50 = 2.3 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht2a_human Human Yes 8.6 EC50 = 2.3 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht2a_human Human Yes 8.6 EC50 = 2.4 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht2a_human Human Yes 8.6 EC50 = 2.4 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht2a_human Human Yes 8.6 EC50 = 2.6 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht2a_human Human Yes 8.6 EC50 = 2.6 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL275628 5ht2a_human Human Yes 8.6 EC50 = 2.6 nM Funct
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
178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2
CHEMBL4466591 5ht2a_human Human No 8.6 EC50 = 2.7 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
183 2 1 1 2.0 NC[C@H]1C[C@]1(F)c1cccc(F)c1
CHEMBL4597360 5ht2a_human Human No 8.6 EC50 = 2.7 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
183 2 1 1 2.0 NC[C@H]1C[C@]1(F)c1cccc(F)c1
CHEMBL1177916 5ht2a_rat Rat Yes 8.6 EC50 = 2.7 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
293 2 1 3 3.8 C[C@H](CC1=C2C=COC2=C(C3=C1OC=C3)Br)N
CHEMBL2391541 5ht2a_human Human Yes 8.6 EC50 = 2.8 nM Funct
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
270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12
CHEMBL69700 5ht2a_rat Rat Yes 7.7 EC50 = 20 nM Funct
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
273 4 1 3 2.4 COc1cc(C[C@@H](C)N)c(OC)cc1Br
CHEMBL3769543 5ht2a_human Human No 7.7 EC50 = 20.9 nM Funct
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
245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN
CHEMBL3771390 5ht2a_human Human No 7.7 EC50 = 20.9 nM Funct
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
245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN
CHEMBL316527 5ht2a_rat Rat Yes 5.7 EC50 = 2000 nM Funct
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2A receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2A receptor
235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2
CHEMBL3769454 5ht2a_human Human No 6.7 EC50 = 203 nM Funct
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
245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN
CHEMBL3771393 5ht2a_human Human No 6.7 EC50 = 203 nM Funct
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
245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN
CHEMBL201132 5ht2a_rat Rat Yes 6.7 EC50 = 204 nM Funct
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
317 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(I)c21
CHEMBL4210997 5ht2a_rat Rat No 5.7 EC50 = 2040 nM Funct
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
450 8 1 4 3.9 O=C(NCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1ccccn1
CHEMBL4300305 5ht2a_rat Rat No 5.7 EC50 = 2040 nM Funct
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
450 8 1 4 3.9 O=C(NCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1ccccn1
CHEMBL1643858 5ht2a_human Human No 5.7 EC50 = 2046 nM Funct
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
406 4 1 7 1.7 CC(=O)N(C)c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1
CHEMBL2397904 5ht2a_human Human No 6.7 EC50 = 206 nM Funct
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
216 0 1 2 1.0 Cc1cccc2c1C[C@@H]1CNCCN1C2=O
CHEMBL6557 5ht2a_human Human Yes 6.7 EC50 = 208.9 nM Funct
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
200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2
CHEMBL2337488 5ht2a_human Human No 5.7 EC50 = 2089 nM Funct
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
298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21
CHEMBL2364960 5ht2a_human Human No 5.7 EC50 = 2089 nM Funct
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
298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21
CHEMBL3330641 5ht2a_human Human Yes 6.7 EC50 = 209 nM Funct
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
174 2 1 2 1.7 Cn1cc(CCN)c2ccccc21
CHEMBL445106 5ht2a_rat Rat No 5.7 EC50 = 2090 nM Bind
Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptorTested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor
283 1 1 3 2.2 COc1cc(Br)c2c3c1C[C@H](N)C[C@@H]3CO2
CHEMBL2337501 5ht2a_human Human No 7.7 EC50 = 21 nM Funct
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
236 0 2 2 1.4 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21
CHEMBL2365359 5ht2a_human Human No 7.7 EC50 = 21 nM Funct
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
236 0 2 2 1.4 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21
CHEMBL3769543 5ht2a_human Human No 7.7 EC50 = 21 nM Funct
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
245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN
CHEMBL3771390 5ht2a_human Human No 7.7 EC50 = 21 nM Funct
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
245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN
CHEMBL6557 5ht2a_human Human Yes 6.7 EC50 = 210 nM Funct
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
200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2
CHEMBL3769987 5ht2a_human Human No 6.7 EC50 = 212 nM Funct
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
229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN
CHEMBL3771387 5ht2a_human Human No 6.7 EC50 = 212 nM Funct
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
229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN
CHEMBL4803813 5ht2a_human Human No 6.7 EC50 = 213 nM Funct
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
243 5 1 3 3.1 C=CCOC1=C(C2=C(C=C1)OC=C2)[C@H]3C[C@@H]3CN
CHEMBL25800 5ht2a_rat Rat Yes 6.7 EC50 = 213 nM Funct
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
230 2 1 3 2.0 Cn1cc(CCN)c2c3c(ccc21)OCCC3
CHEMBL4803813 5ht2a_human Human No 6.7 EC50 = 213.8 nM Funct
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
243 5 1 3 3.1 C=CCOC1=C(C2=C(C=C1)OC=C2)[C@H]3C[C@@H]3CN
CHEMBL3769987 5ht2a_human Human No 6.7 EC50 = 213.8 nM Funct
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
229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN
CHEMBL3771387 5ht2a_human Human No 6.7 EC50 = 213.8 nM Funct
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
229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN
CHEMBL1186135 5ht2a_human Human No 5.7 EC50 = 2166 nM Funct
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
177 3 1 2 1.8 COc1ccccc1[C@H]1C[C@@H]1CN
CHEMBL451368 5ht2a_human Human No 5.7 EC50 = 2166 nM Funct
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
177 3 1 2 1.8 COc1ccccc1[C@H]1C[C@@H]1CN
CHEMBL4803134 5ht2a_human Human No 5.7 EC50 = 2187.8 nM Funct
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
277 6 1 3 3.4 CCC1=CC2=C(O1)C=CC(=C2[C@H]3C[C@@H]3CN)OCCF
CHEMBL2397890 5ht2a_human Human No 7.7 EC50 = 22 nM Funct
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
230 1 1 2 1.2 CCc1cccc2c1C(=O)N1CCNC[C@H]1C2
CHEMBL4803306 5ht2a_human Human No 7.7 EC50 = 22 nM Funct
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
249 5 1 3 2.8 C1[C@@H]([C@H]1C2=C(C=CC3=C2C=CO3)OCCF)CN
CHEMBL6607 5ht2a_rat Rat Yes 7.7 EC50 = 22 nM Funct
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
273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC
CHEMBL179244 5ht2a_human Human No 7.7 EC50 = 22 nM Funct
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
345 3 1 2 4.3 CC1CNCCc2cc(OCc3ccccc3)c(Br)cc21
CHEMBL4803306 5ht2a_human Human No 7.7 EC50 = 22.4 nM Funct
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
249 5 1 3 2.8 C1[C@@H]([C@H]1C2=C(C=CC3=C2C=CO3)OCCF)CN
CHEMBL4516935 5ht2a_human Human No 7.6 EC50 = 22.9 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1
CHEMBL4596490 5ht2a_human Human No 7.6 EC50 = 22.9 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1
CHEMBL373531 5ht2a_human Human No 6.7 EC50 = 220 nM Funct
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
252 1 1 3 1.4 COc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O
CHEMBL178231 5ht2a_human Human Yes 6.7 EC50 = 220 nM Funct
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
229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21
CHEMBL208936 5ht2a_human Human No 6.7 EC50 = 220 nM Funct
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
258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CCC3CNCC32)n1
CHEMBL593547 5ht2a_human Human Yes 5.7 EC50 = 2202 nM Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
217 1 1 3 1.4 c1cc2c(nc1N1CCNCC1)CCCC2
CHEMBL4803134 5ht2a_human Human No 5.7 EC50 = 2210 nM Funct
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
277 6 1 3 3.4 CCC1=CC2=C(O1)C=CC(=C2[C@H]3C[C@@H]3CN)OCCF
CHEMBL202616 5ht2a_human Human No 6.7 EC50 = 222 nM Bind
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
365 5 1 3 5.5 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2ccccc2c1
CHEMBL4073529 5ht2a_human Human No 5.7 EC50 = 2220 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
341 6 1 3 4.9 COc1ccc(F)cc1C1CC1CNCc1cccc2ccsc12
CHEMBL4116914 5ht2a_human Human No 5.7 EC50 = 2220 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
341 6 1 3 4.9 COc1ccc(F)cc1C1CC1CNCc1cccc2ccsc12
CHEMBL4073529 5ht2a_human Human No 5.7 EC50 = 2238.7 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
341 6 1 3 4.9 COc1ccc(F)cc1C1CC1CNCc1cccc2ccsc12
CHEMBL4116914 5ht2a_human Human No 5.7 EC50 = 2238.7 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
341 6 1 3 4.9 COc1ccc(F)cc1C1CC1CNCc1cccc2ccsc12
CHEMBL6557 5ht2a_human Human Yes 7.6 EC50 = 23 nM Funct
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
200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2
CHEMBL4516935 5ht2a_human Human No 7.6 EC50 = 23 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1
CHEMBL4596490 5ht2a_human Human No 7.6 EC50 = 23 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
199 2 1 1 2.5 NC[C@H]1C[C@]1(F)c1cccc(Cl)c1
CHEMBL30713 5ht2a_human Human Yes 7.6 EC50 = 23.1 nM Funct
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
174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12
CHEMBL6557 5ht2a_human Human Yes 7.6 EC50 = 23.4 nM Funct
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
200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2
CHEMBL4117120 5ht2a_human Human No 7.6 EC50 = 24.0 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
347 9 1 3 4.1 COC1=CC=CC=C1CNC[C@H]2C[C@@H]2C3=C(C=CC(=C3)F)OCCF
CHEMBL65547 5ht2a_rat Rat Yes 5.6 EC50 = 2300 nM Bind
Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptorTested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor
204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C
CHEMBL1643671 5ht2a_human Human No 5.6 EC50 = 2310 nM Funct
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
257 1 1 5 1.0 c1cc2nc3c(c(N4CCCC4)n2n1)CCNCC3
CHEMBL143202 5ht2a_rat Rat Yes 5.6 EC50 = 2310 nM Bind
Evaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptorEvaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptor
232 5 2 2 2.8 CCN(CC)CCc1c[nH]c2cccc(O)c12
CHEMBL4802794 5ht2a_human Human No 5.6 EC50 = 2320 nM Funct
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
251 5 1 3 2.0 C1COC2=C1C(=C(C=C2)OCCF)[C@H]3C[C@@H]3CN
CHEMBL3770599 5ht2a_human Human No 5.6 EC50 = 2332 nM Funct
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
245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F
CHEMBL3771378 5ht2a_human Human No 5.6 EC50 = 2332 nM Funct
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
245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F
CHEMBL3770689 5ht2a_human Human No 6.6 EC50 = 234.4 nM Funct
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
229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN
CHEMBL3771380 5ht2a_human Human No 6.6 EC50 = 234.4 nM Funct
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
229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN
CHEMBL4802794 5ht2a_human Human No 5.6 EC50 = 2344.2 nM Funct
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
251 5 1 3 2.0 C1COC2=C1C(=C(C=C2)OCCF)[C@H]3C[C@@H]3CN
CHEMBL3770599 5ht2a_human Human No 5.6 EC50 = 2344.2 nM Funct
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
245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F
CHEMBL3771378 5ht2a_human Human No 5.6 EC50 = 2344.2 nM Funct
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
245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F
CHEMBL1643670 5ht2a_human Human No 5.6 EC50 = 2348 nM Funct
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
243 1 1 5 0.6 c1cc2nc3c(c(N4CCC4)n2n1)CCNCC3
CHEMBL1186686 5ht2a_human Human No 6.6 EC50 = 235 nM Funct
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
179 2 1 1 2.2 Cc1cc([C@H]2C[C@@H]2CN)ccc1F
CHEMBL474633 5ht2a_human Human No 6.6 EC50 = 235 nM Funct
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
179 2 1 1 2.2 Cc1cc([C@H]2C[C@@H]2CN)ccc1F
CHEMBL3770689 5ht2a_human Human No 6.6 EC50 = 235 nM Funct
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
229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN
CHEMBL3771380 5ht2a_human Human No 6.6 EC50 = 235 nM Funct
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
229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN
CHEMBL437314 5ht2a_rat Rat Yes 6.6 EC50 = 236 nM Funct
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21
CHEMBL595195 5ht2a_human Human No 6.6 EC50 = 236 nM Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
329 3 1 4 3.2 Clc1ccccc1OC1CCc2ccc(N3CCNCC3)nc21
CHEMBL4204710 5ht2a_human Human No 6.6 EC50 = 236 nM Funct
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
243 1 1 3 2.1 c1cc(C2CCC2)c2c(n1)N1CCNC[C@H]1CC2
CHEMBL1182828 5ht2a_rat Rat No 5.6 EC50 = 2360 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
219 2 1 3 1.4 C[C@H](N)Cc1c2c(cc3c1OCC3)OCC2
CHEMBL268587 5ht2a_rat Rat No 5.6 EC50 = 2360 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
219 2 1 3 1.4 C[C@H](N)Cc1c2c(cc3c1OCC3)OCC2
CHEMBL4066538 5ht2a_human Human No 6.6 EC50 = 238 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
329 7 1 3 4.3 COc1ccccc1C(C)NCC1CC1c1cc(F)ccc1OC
CHEMBL4116576 5ht2a_human Human No 6.6 EC50 = 238 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
329 7 1 3 4.3 COc1ccccc1C(C)NCC1CC1c1cc(F)ccc1OC
CHEMBL4066538 5ht2a_human Human No 6.6 EC50 = 239.9 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
329 7 1 3 4.3 COc1ccccc1C(C)NCC1CC1c1cc(F)ccc1OC
CHEMBL4116576 5ht2a_human Human No 6.6 EC50 = 239.9 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
329 7 1 3 4.3 COc1ccccc1C(C)NCC1CC1c1cc(F)ccc1OC
CHEMBL342986 5ht2a_rat Rat Yes 5.6 EC50 = 2390 nM Bind
Evaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptorEvaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptor
246 6 1 2 3.1 CCN(CC)CCc1c[nH]c2ccc(OC)cc12
CHEMBL1186737 5ht2a_human Human No 5.6 EC50 = 2392 nM Funct
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
175 2 1 1 2.4 Cc1ccc([C@H]2C[C@@H]2CN)cc1C
CHEMBL475643 5ht2a_human Human No 5.6 EC50 = 2392 nM Funct
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
175 2 1 1 2.4 Cc1ccc([C@H]2C[C@@H]2CN)cc1C
CHEMBL2331807 5ht2a_human Human No 5.6 EC50 = 2398.8 nM Funct
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
244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2
CHEMBL4117120 5ht2a_human Human No 7.6 EC50 = 24 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
347 9 1 3 4.1 COC1=CC=CC=C1CNC[C@H]2C[C@@H]2C3=C(C=CC(=C3)F)OCCF
CHEMBL65547 5ht2a_human Human Yes 7.6 EC50 = 24 nM Funct
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assay
204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C
CHEMBL2331794 5ht2a_human Human No 6.6 EC50 = 240 nM Funct
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
244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1
CHEMBL2331807 5ht2a_human Human No 5.6 EC50 = 2400 nM Funct
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
244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2
CHEMBL178566 5ht2a_human Human Yes 5.6 EC50 = 2400 nM Funct
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
229 0 1 1 3.2 C[C@H]1CNCCc2ccc(Cl)c(Cl)c21
CHEMBL482675 5ht2a_rat Rat Yes 6.6 EC50 = 241 nM Funct
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
311 2 1 3 2.6 C1CC2=C(C3=C(CCCO3)C(=C2OC1)Br)CCN
CHEMBL337825 5ht2a_human Human Yes 5.6 EC50 = 2443 nM Funct
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
190 3 2 2 1.7 COc1ccc2c(CCN)c[nH]c2c1
CHEMBL360328 5ht2a_human Human Yes 6.6 EC50 = 245.5 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2
CHEMBL360328 5ht2a_human Human Yes 6.6 EC50 = 245.5 nM Funct
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
195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2
CHEMBL2331794 5ht2a_human Human No 6.6 EC50 = 245.5 nM Funct
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
244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1
CHEMBL3330648 5ht2a_human Human No 6.6 EC50 = 246 nM Funct
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
206 3 2 1 2.6 CCC(N)Cc1c[nH]c2ccc(F)cc12
CHEMBL1187585 5ht2a_human Human No 6.6 EC50 = 247 nM Funct
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
163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1cccc(O)c1
CHEMBL510383 5ht2a_human Human No 6.6 EC50 = 247 nM Funct
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
163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1cccc(O)c1
CHEMBL360328 5ht2a_human Human Yes 6.6 EC50 = 248 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2
CHEMBL360328 5ht2a_human Human Yes 6.6 EC50 = 248 nM Funct
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
195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2
CHEMBL590816 5ht2a_human Human No 6.6 EC50 = 248 nM Funct
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
217 0 2 3 0.6 O=C1NC2CCNCCN2c2ccccc21
CHEMBL3330647 5ht2a_human Human Yes 6.6 EC50 = 249 nM Funct
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
222 3 2 1 3.1 CCC(N)Cc1c[nH]c2ccc(Cl)cc12
CHEMBL210484 5ht2a_human Human No 7.6 EC50 = 25 nM Funct
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
272 1 1 4 1.7 C[C@@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1
CHEMBL4646572 5ht2a_human Human No 6.6 EC50 = 250 nM Funct
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
334 1 1 2 3.4 FC(F)(F)CC1CN2CCNCc3ccc(Br)c1c32
CHEMBL478 5ht2a_human Human Yes 6.6 EC50 = 251.2 nM Funct
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1
CHEMBL178365 5ht2a_human Human Yes 6.6 EC50 = 251.2 nM Funct
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
195 0 1 1 2.6 C[C@@H]1CNCCc2ccc(Cl)cc21
CHEMBL253809 5ht2a_human Human Yes 6.6 EC50 = 251.2 nM Funct
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
209 1 1 1 3.0 CC[C@H]1CNCCc2ccc(Cl)cc21
CHEMBL361742 5ht2a_human Human Yes 6.6 EC50 = 251.2 nM Funct
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
191 1 1 2 1.9 COc1ccc2c(c1)C(C)CNCC2
CHEMBL4209052 5ht2a_human Human No 5.6 EC50 = 2510 nM Funct
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
257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNCC1CC2
CHEMBL4079976 5ht2a_human Human No 5.6 EC50 = 2511.9 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
329 7 0 3 4.1 COc1ccccc1CN(C)CC1CC1c1cc(F)ccc1OC
CHEMBL4117263 5ht2a_human Human No 5.6 EC50 = 2511.9 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
329 7 0 3 4.1 COc1ccccc1CN(C)CC1CC1c1cc(F)ccc1OC
CHEMBL178566 5ht2a_human Human Yes 5.6 EC50 = 2511.9 nM Funct
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
229 0 1 1 3.2 C[C@H]1CNCCc2ccc(Cl)c(Cl)c21
CHEMBL570937 5ht2a_human Human No 6.6 EC50 = 254 nM Funct
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
334 5 1 6 1.4 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1Cl
CHEMBL4079976 5ht2a_human Human No 5.6 EC50 = 2540 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
329 7 0 3 4.1 COc1ccccc1CN(C)CC1CC1c1cc(F)ccc1OC
CHEMBL4117263 5ht2a_human Human No 5.6 EC50 = 2540 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
329 7 0 3 4.1 COc1ccccc1CN(C)CC1CC1c1cc(F)ccc1OC
CHEMBL4753812 5ht2a_human Human No 6.6 EC50 = 257.0 nM Funct
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
257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4802839 5ht2a_human Human No 6.6 EC50 = 257.0 nM Funct
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
257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL482702 5ht2a_rat Rat Yes 6.6 EC50 = 258 nM Funct
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
325 2 1 3 3.0 CC(CC1=C2CCCOC2=C(C3=C1OCCC3)Br)N
CHEMBL360328 5ht2a_human Human Yes 6.6 EC50 = 258 nM Funct
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
195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2
CHEMBL4740346 5ht2a_human Human No 5.6 EC50 = 2598 nM Funct
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
259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN
CHEMBL4802388 5ht2a_human Human No 5.6 EC50 = 2598 nM Funct
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
259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN
CHEMBL394508 5ht2a_rat Rat No 7.6 EC50 = 26 nM Funct
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
305 5 1 5 1.6 COC(=O)CCc1c2c(c(C[C@@H](C)N)c3c1OCC3)OCC2
CHEMBL76781 5ht2a_human Human Yes 7.6 EC50 = 26.9 nM Funct
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
226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N
CHEMBL4753812 5ht2a_human Human No 6.6 EC50 = 260 nM Funct
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
257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4802839 5ht2a_human Human No 6.6 EC50 = 260 nM Funct
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
257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL181172 5ht2a_human Human Yes 6.6 EC50 = 260 nM Funct
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
195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21
CHEMBL143031 5ht2a_rat Rat No 5.6 EC50 = 2600 nM Bind
Evaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptorEvaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptor
222 3 2 2 2.1 CN(C)CCc1c[nH]c2cc(F)cc(O)c12
CHEMBL26687 5ht2a_rat Rat Yes 5.6 EC50 = 2600 nM Bind
Tested for its ability to activate phospholipase c by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptorTested for its ability to activate phospholipase c by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor
211 5 1 4 1.2 COc1cc(CCN)cc(OC)c1OC
CHEMBL4740346 5ht2a_human Human No 5.6 EC50 = 2630.3 nM Funct
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
259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN
CHEMBL4802388 5ht2a_human Human No 5.6 EC50 = 2630.3 nM Funct
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
259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN
CHEMBL1643854 5ht2a_human Human No 5.6 EC50 = 2634 nM Funct
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
365 4 1 7 1.7 COc1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1
CHEMBL178365 5ht2a_human Human Yes 6.6 EC50 = 265 nM Funct
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
195 0 1 1 2.6 C[C@@H]1CNCCc2ccc(Cl)cc21
CHEMBL1643679 5ht2a_human Human No 5.6 EC50 = 2676 nM Funct
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
365 4 1 7 1.7 COc1ccccc1OC1CN(c2c3c(nc4ccnn24)CCNCC3)C1
CHEMBL355474 5ht2a_human Human No 6.6 EC50 = 269 nM Funct
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
232 2 1 2 2.8 CC1CCc2cc(F)cc3c(CCN)cn1c23
CHEMBL4116620 5ht2a_human Human No 6.6 EC50 = 269.2 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
209 4 1 2 2.2 CNC[C@H]1C[C@@H]1C2=C(C=CC(=C2)F)OC
CHEMBL292821 5ht2a_rat Rat Yes 7.6 EC50 = 27 nM Funct
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
259 4 1 3 2.0 COc1cc(CCN)c(OC)cc1Br
CHEMBL76781 5ht2a_human Human Yes 7.6 EC50 = 27 nM Funct
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
226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N
CHEMBL4116028 5ht2a_human Human No 7.6 EC50 = 27.5 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
341 9 1 3 4.3 COC1=CC=CC=C1CNC[C@H]2C[C@@H]2C3=C(C=CC(=C3)F)OCC=C
CHEMBL2391541 5ht2a_human Human Yes 7.6 EC50 = 27.5 nM Funct
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
270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12
CHEMBL134519 5ht2a_rat Rat Yes 7.6 EC50 = 27.7 nM Funct
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
321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC
CHEMBL2393244 5ht2a_human Human No 7.6 EC50 = 27.9 nM Funct
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
348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1
CHEMBL3040288 5ht2a_human Human No 7.6 EC50 = 27.9 nM Funct
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
348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1
CHEMBL4116620 5ht2a_human Human No 6.6 EC50 = 271 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
209 4 1 2 2.2 CNC[C@H]1C[C@@H]1C2=C(C=CC(=C2)F)OC
CHEMBL1177908 5ht2a_rat Rat No 7.6 EC50 = 28 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
287 2 1 3 2.5 C[C@@H](N)Cc1c2c(c(C(F)(F)F)c3c1OCC3)OCC2
CHEMBL6452 5ht2a_rat Rat No 7.6 EC50 = 28 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
287 2 1 3 2.5 C[C@@H](N)Cc1c2c(c(C(F)(F)F)c3c1OCC3)OCC2
CHEMBL4116028 5ht2a_human Human No 7.6 EC50 = 28 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
341 9 1 3 4.3 COC1=CC=CC=C1CNC[C@H]2C[C@@H]2C3=C(C=CC(=C3)F)OCC=C
CHEMBL382635 5ht2a_human Human Yes 7.6 EC50 = 28.1 nM Funct
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
178 2 2 1 1.8 NCCc1c[nH]c2cccc(F)c12
CHEMBL4098721 5ht2a_human Human No 6.6 EC50 = 281.8 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
235 6 1 2 2.7 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CNC
CHEMBL4116380 5ht2a_human Human No 6.6 EC50 = 281.8 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
235 6 1 2 2.7 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CNC
CHEMBL4098721 5ht2a_human Human No 6.6 EC50 = 284 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
235 6 1 2 2.7 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CNC
CHEMBL4116380 5ht2a_human Human No 6.6 EC50 = 284 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
235 6 1 2 2.7 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CNC
CHEMBL31115 5ht2a_rat Rat Yes 6.5 EC50 = 285 nM Funct
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
204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1
CHEMBL4213971 5ht2a_human Human No 5.5 EC50 = 2880 nM Funct
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
267 0 1 3 1.6 Brc1ccnc2c1CC[C@@H]1CNCCN21
CHEMBL220211 5ht2a_human Human No 6.5 EC50 = 289 nM Funct
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
286 1 1 3 1.8 COc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21
CHEMBL478 5ht2a_human Human Yes 6.5 EC50 = 290 nM Funct
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
196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1
CHEMBL478 5ht2a_human Human Yes 6.5 EC50 = 290 nM Funct
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
196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1
CHEMBL478 5ht2a_human Human Yes 6.5 EC50 = 290 nM Funct
Agonist activity at recombinant human 5-HT2A receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assayAgonist activity at recombinant human 5-HT2A receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1
CHEMBL2393234 5ht2a_human Human No 5.5 EC50 = 2900 nM Funct
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
318 4 1 6 0.8 CCN(CC)c1nc(N2CCN(C)CC2)nc2c1CCNCC2
CHEMBL3040350 5ht2a_human Human No 5.5 EC50 = 2900 nM Funct
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
318 4 1 6 0.8 CCN(CC)c1nc(N2CCN(C)CC2)nc2c1CCNCC2
CHEMBL135076 5ht2a_rat Rat No 6.5 EC50 = 292 nM Funct
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
230 2 2 2 2.4 C[C@@H](N)Cc1c[nH]c2ccc3c(c12)CCCO3
CHEMBL4777303 5ht2a_human Human No 6.5 EC50 = 295 nM Funct
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
219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2
CHEMBL4802306 5ht2a_human Human No 6.5 EC50 = 295 nM Funct
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
219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2
CHEMBL4777303 5ht2a_human Human No 6.5 EC50 = 295.1 nM Funct
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
219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2
CHEMBL4802306 5ht2a_human Human No 6.5 EC50 = 295.1 nM Funct
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
219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2
CHEMBL4759181 5ht2a_human Human No 6.5 EC50 = 295.1 nM Funct
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
245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4803103 5ht2a_human Human No 6.5 EC50 = 295.1 nM Funct
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
245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4083787 5ht2a_human Human No 5.5 EC50 = 2951.2 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
319 6 1 2 4.4 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1Cl
CHEMBL4117262 5ht2a_human Human No 5.5 EC50 = 2951.2 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
319 6 1 2 4.4 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1Cl
CHEMBL4759181 5ht2a_human Human No 6.5 EC50 = 298 nM Funct
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
245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4803103 5ht2a_human Human No 6.5 EC50 = 298 nM Funct
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
245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4083787 5ht2a_human Human No 5.5 EC50 = 2990 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
319 6 1 2 4.4 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1Cl
CHEMBL4117262 5ht2a_human Human No 5.5 EC50 = 2990 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
319 6 1 2 4.4 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCc1ccccc1Cl
CHEMBL3416066 5ht2a_human Human No 5.5 EC50 = 2994 nM Funct
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
227 5 1 2 2.2 NC[C@@H]1C[C@H]1c1cc(F)ccc1OCCF
CHEMBL3546874 5ht2a_human Human No 5.5 EC50 = 2994 nM Funct
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
227 5 1 2 2.2 NC[C@@H]1C[C@H]1c1cc(F)ccc1OCCF
CHEMBL1643678 5ht2a_human Human No 8.5 EC50 = 3 nM Funct
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
353 3 1 6 1.8 Fc1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1
CHEMBL4466591 5ht2a_human Human No 8.5 EC50 = 3 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
183 2 1 1 2.0 NC[C@H]1C[C@]1(F)c1cccc(F)c1
CHEMBL4597360 5ht2a_human Human No 8.5 EC50 = 3 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
183 2 1 1 2.0 NC[C@H]1C[C@]1(F)c1cccc(F)c1
CHEMBL394325 5ht2a_rat Rat No 8.4 EC50 = 3.6 nM Funct
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
259 4 1 4 3.2 COCc1c2ccoc2c(C[C@@H](C)N)c2ccoc12
CHEMBL1177930 5ht2a_rat Rat No 8.4 EC50 = 3.8 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
283 2 1 3 4.1 C[C@@H](N)Cc1c2ccoc2c(C(F)(F)F)c2ccoc12
CHEMBL7132 5ht2a_rat Rat No 8.4 EC50 = 3.8 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
283 2 1 3 4.1 C[C@@H](N)Cc1c2ccoc2c(C(F)(F)F)c2ccoc12
CHEMBL1182827 5ht2a_rat Rat No 7.5 EC50 = 30 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
287 2 1 3 2.5 C[C@H](N)Cc1c2c(c(C(F)(F)F)c3c1OCC3)OCC2
CHEMBL268542 5ht2a_rat Rat No 7.5 EC50 = 30 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
287 2 1 3 2.5 C[C@H](N)Cc1c2c(c(C(F)(F)F)c3c1OCC3)OCC2
CHEMBL182184 5ht2a_human Human No 7.5 EC50 = 30 nM Funct
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
269 1 1 2 2.7 COc1cc2c(cc1Br)[C@H](C)CNCC2
CHEMBL4541617 5ht2a_human Human No 7.5 EC50 = 30.9 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
333 7 1 3 3.8 COc1ccccc1CNCC1CC1(F)c1cc(F)ccc1OC
CHEMBL4597957 5ht2a_human Human No 7.5 EC50 = 30.9 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
333 7 1 3 3.8 COc1ccccc1CNCC1CC1(F)c1cc(F)ccc1OC
CHEMBL102347 5ht2a_rat Rat Yes 5.5 EC50 = 3000 nM Funct
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast expressing 5-hydroxytryptamine 2A receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast expressing 5-hydroxytryptamine 2A receptor
223 4 1 4 1.1 COc1cc(CCN)c2c(c1OC)OCC2
CHEMBL360328 5ht2a_human Human Yes 6.5 EC50 = 302 nM Funct
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
195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2
CHEMBL39 5ht2a_human Human Yes 6.5 EC50 = 302 nM Bind
Partial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assayPartial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL2022185 5ht2a_human Human No 5.5 EC50 = 3020 nM Funct
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
191 4 1 2 2.1 CCOc1ccccc1[C@H]1C[C@@H]1CN
CHEMBL2027895 5ht2a_human Human No 5.5 EC50 = 3020 nM Funct
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
191 4 1 2 2.1 CCOc1ccccc1[C@H]1C[C@@H]1CN
CHEMBL2337503 5ht2a_human Human No 6.5 EC50 = 303 nM Funct
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
216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O
CHEMBL2365465 5ht2a_human Human No 6.5 EC50 = 303 nM Funct
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
216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O
CHEMBL4075150 5ht2a_human Human No 6.5 EC50 = 307 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
329 8 1 3 3.8 COc1ccccc1CCNCC1CC1c1cc(F)ccc1OC
CHEMBL4117857 5ht2a_human Human No 6.5 EC50 = 307 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
329 8 1 3 3.8 COc1ccccc1CCNCC1CC1c1cc(F)ccc1OC
CHEMBL572228 5ht2a_human Human No 6.5 EC50 = 308 nM Funct
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
318 5 1 5 2.2 Clc1ccccc1CCOc1cncc(N2CCNCC2)n1
CHEMBL4075150 5ht2a_human Human No 6.5 EC50 = 309.0 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
329 8 1 3 3.8 COc1ccccc1CCNCC1CC1c1cc(F)ccc1OC
CHEMBL4117857 5ht2a_human Human No 6.5 EC50 = 309.0 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
329 8 1 3 3.8 COc1ccccc1CCNCC1CC1c1cc(F)ccc1OC
CHEMBL4541617 5ht2a_human Human No 7.5 EC50 = 31 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
333 7 1 3 3.8 COc1ccccc1CNCC1CC1(F)c1cc(F)ccc1OC
CHEMBL4597957 5ht2a_human Human No 7.5 EC50 = 31 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
333 7 1 3 3.8 COc1ccccc1CNCC1CC1(F)c1cc(F)ccc1OC
CHEMBL400600 5ht2a_human Human No 7.5 EC50 = 31.6 nM Funct
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
225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@H](C)CNCC2
CHEMBL253810 5ht2a_human Human No 6.5 EC50 = 316.2 nM Funct
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
209 1 1 1 3.0 CC[C@@H]1CNCCc2ccc(Cl)cc21
CHEMBL4575163 5ht2a_human Human No 6.5 EC50 = 316.2 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
285 6 1 2 3.7 COc1ccccc1CNC[C@H]1C[C@]1(F)c1ccccc1
CHEMBL4594655 5ht2a_human Human No 6.5 EC50 = 316.2 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
285 6 1 2 3.7 COc1ccccc1CNC[C@H]1C[C@]1(F)c1ccccc1
CHEMBL492301 5ht2a_human Human No 7.5 EC50 = 32 nM Funct
Agonist activity at human 5HT2A receptor expressed in mouse Swiss 3T3 cells by FLIPR assayAgonist activity at human 5HT2A receptor expressed in mouse Swiss 3T3 cells by FLIPR assay
420 4 1 4 3.3 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCC(Oc2ccccc2Cl)CC1
CHEMBL1643677 5ht2a_human Human No 7.5 EC50 = 32 nM Funct
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
353 3 1 6 1.8 Fc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1
CHEMBL201930 5ht2a_human Human No 7.5 EC50 = 32 nM Bind
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ncccc3c21
CHEMBL198124 5ht2a_human Human No 7.5 EC50 = 32 nM Funct
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assay
260 6 1 3 3.3 CCCCn1cc(CCN(C)C)c2c(O)cccc21
CHEMBL360328 5ht2a_human Human Yes 7.5 EC50 = 32.4 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2
CHEMBL391196 5ht2a_rat Rat No 7.5 EC50 = 32.7 nM Funct
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
313 2 2 4 1.7 C[C@@H](N)[C@H](O)c1c2c(c(Br)c3c1OCC3)OCC2
CHEMBL4575163 5ht2a_human Human No 6.5 EC50 = 320 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
285 6 1 2 3.7 COc1ccccc1CNC[C@H]1C[C@]1(F)c1ccccc1
CHEMBL4594655 5ht2a_human Human No 6.5 EC50 = 320 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
285 6 1 2 3.7 COc1ccccc1CNC[C@H]1C[C@]1(F)c1ccccc1
CHEMBL379780 5ht2a_rat Rat Yes 5.5 EC50 = 3200 nM Funct
Activity at rat 5HT2A receptor assessed as 5-HT-stimulated IP3 accumulationActivity at rat 5HT2A receptor assessed as 5-HT-stimulated IP3 accumulation
237 4 1 4 1.7 COc1cc2c(c(OC)c1OC)CC[C@H]2CN
CHEMBL190461 5ht2a_rat Rat Yes 4.5 EC50 = 32000 nM Bind
Displacement of [3H] ketanserin from rat 5-HT2aR expressed in mouse NIH/3T3 cells incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H] ketanserin from rat 5-HT2aR expressed in mouse NIH/3T3 cells incubated for 30 mins by liquid scintillation counting method
314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C
CHEMBL223466 5ht2a_human Human No 5.5 EC50 = 3280 nM Funct
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
250 1 1 2 2.0 CCc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O
CHEMBL393077 5ht2a_rat Rat No 7.5 EC50 = 33 nM Funct
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
245 3 2 4 2.6 C[C@@H](N)Cc1c2ccoc2c(CO)c2ccoc12
CHEMBL360328 5ht2a_human Human Yes 7.5 EC50 = 33 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2
CHEMBL3589596 5ht2a_human Human No 7.5 EC50 = 33.9 nM Bind
Partial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assayPartial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assay
395 8 2 5 3.5 COc1cc(CCNCc2cccc(OC)c2O)c(OC)cc1Br
CHEMBL1187556 5ht2a_human Human No 6.5 EC50 = 330 nM Funct
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
213 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F
CHEMBL508680 5ht2a_human Human No 6.5 EC50 = 330 nM Funct
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
213 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F
CHEMBL444612 5ht2a_rat Rat Yes 4.5 EC50 = 33900 nM Bind
Evaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptorEvaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptor
234 5 1 1 3.2 CCN(CC)CCc1c[nH]c2cc(F)ccc12
CHEMBL331864 5ht2a_rat Rat No 6.5 EC50 = 340 nM Bind
Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptorTested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor
297 2 1 3 2.8 COc1cc(Br)c2c3c1[C@H](CN)CC[C@H]3CO2
CHEMBL1770373 5ht2a_canlf Dog Yes 5.5 EC50 = 3400 nM Bind
Agonist activity at 5-HT2A receptor in beagle dog femoral arteries tissue after 1 hrAgonist activity at 5-HT2A receptor in beagle dog femoral arteries tissue after 1 hr
239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1
CHEMBL1770373 5ht2a_canlf Dog Yes 5.5 EC50 = 3400 nM Funct
Agonist activity at 5HT2A receptor in dog femoral arteryAgonist activity at 5HT2A receptor in dog femoral artery
239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1
CHEMBL194378 5ht2a_human Human Yes 5.5 EC50 = 3475 nM Funct
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assay
284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12
CHEMBL172159 5ht2a_human Human No 6.5 EC50 = 348 nM Funct
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
252 2 1 3 2.9 NCCc1cn2c3c(cc(Cl)cc13)SCC2
CHEMBL1186458 5ht2a_human Human No 6.5 EC50 = 349 nM Funct
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
215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1cccc(Cl)c1Cl
CHEMBL464475 5ht2a_human Human No 6.5 EC50 = 349 nM Funct
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
215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1cccc(Cl)c1Cl
CHEMBL1182730 5ht2a_rat Rat Yes 7.5 EC50 = 35 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
297 2 1 3 2.2 C[C@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2
CHEMBL263078 5ht2a_rat Rat Yes 7.5 EC50 = 35 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
297 2 1 3 2.2 C[C@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2
CHEMBL39 5ht2a_rat Rat Yes 6.5 EC50 = 351 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL4515411 5ht2a_human Human No 6.5 EC50 = 352 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
213 3 1 2 2.0 COc1ccc(F)cc1C1(F)CC1CN
CHEMBL4597225 5ht2a_human Human No 6.5 EC50 = 352 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
213 3 1 2 2.0 COc1ccc(F)cc1C1(F)CC1CN
CHEMBL4104218 5ht2a_human Human No 5.5 EC50 = 3530 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
319 6 1 2 4.4 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1Cl
CHEMBL4116381 5ht2a_human Human No 5.5 EC50 = 3530 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
319 6 1 2 4.4 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1Cl
CHEMBL4759878 5ht2a_human Human No 6.5 EC50 = 354.8 nM Funct
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
261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4803107 5ht2a_human Human No 6.5 EC50 = 354.8 nM Funct
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
261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4515411 5ht2a_human Human No 6.5 EC50 = 354.8 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
213 3 1 2 2.0 COc1ccc(F)cc1C1(F)CC1CN
CHEMBL4597225 5ht2a_human Human No 6.5 EC50 = 354.8 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
213 3 1 2 2.0 COc1ccc(F)cc1C1(F)CC1CN
CHEMBL4104218 5ht2a_human Human No 5.5 EC50 = 3548.1 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
319 6 1 2 4.4 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1Cl
CHEMBL4116381 5ht2a_human Human No 5.5 EC50 = 3548.1 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
319 6 1 2 4.4 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCc1ccccc1Cl
CHEMBL4759878 5ht2a_human Human No 6.5 EC50 = 358 nM Funct
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
261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4803107 5ht2a_human Human No 6.5 EC50 = 358 nM Funct
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
261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL3416067 5ht2a_human Human No 6.5 EC50 = 359 nM Funct
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
227 5 1 2 2.2 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF
CHEMBL3546961 5ht2a_human Human No 6.5 EC50 = 359 nM Funct
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
227 5 1 2 2.2 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF
CHEMBL202458 5ht2a_human Human No 6.5 EC50 = 359 nM Bind
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
359 5 1 5 4.1 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2c(c1)OCO2
CHEMBL212197 5ht2a_rat Rat Yes 7.4 EC50 = 36 nM Funct
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
271 3 1 3 2.1 COc1cc(Br)c(OC)c2c1C(CN)C2
CHEMBL201454 5ht2a_human Human No 7.4 EC50 = 36 nM Bind
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
259 2 1 3 3.2 C[C@H](N)Cn1ccc2cc(Cl)c3ncccc3c21
CHEMBL1186736 5ht2a_human Human No 6.4 EC50 = 360 nM Funct
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
175 2 1 1 2.4 Cc1cccc([C@H]2C[C@@H]2CN)c1C
CHEMBL475642 5ht2a_human Human No 6.4 EC50 = 360 nM Funct
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
175 2 1 1 2.4 Cc1cccc([C@H]2C[C@@H]2CN)c1C
CHEMBL3769828 5ht2a_human Human No 6.4 EC50 = 361 nM Funct
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
245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF
CHEMBL3771383 5ht2a_human Human No 6.4 EC50 = 361 nM Funct
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
245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF
CHEMBL3769828 5ht2a_human Human No 6.4 EC50 = 363.1 nM Funct
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
245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF
CHEMBL3771383 5ht2a_human Human No 6.4 EC50 = 363.1 nM Funct
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
245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF
CHEMBL80366 5ht2a_human Human No 6.4 EC50 = 367 nM Funct
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
228 2 1 2 2.2 C[C@H](N)CN1CCc2cc(F)c(Cl)cc21
CHEMBL4457840 5ht2a_human Human Yes 5.4 EC50 = 3679 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
183 2 1 1 2.0 NCC1C(c2ccccc2)C1(F)F
CHEMBL4596163 5ht2a_human Human Yes 5.4 EC50 = 3679 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
183 2 1 1 2.0 NCC1C(c2ccccc2)C1(F)F
CHEMBL2397897 5ht2a_human Human No 7.4 EC50 = 37 nM Funct
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
230 1 1 2 1.2 CCc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2
CHEMBL4751981 5ht2a_human Human No 7.4 EC50 = 37 nM Funct
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
217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4802812 5ht2a_human Human No 7.4 EC50 = 37 nM Funct
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
217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4751981 5ht2a_human Human No 7.4 EC50 = 37.2 nM Funct
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
217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4802812 5ht2a_human Human No 7.4 EC50 = 37.2 nM Funct
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
217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4208452 5ht2a_human Human No 7.4 EC50 = 37.2 nM Funct
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
297 2 1 3 2.5 Fc1cccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)c1
CHEMBL376676 5ht2a_human Human No 6.4 EC50 = 370 nM Funct
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
270 0 1 2 2.2 C[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12
CHEMBL4067525 5ht2a_human Human No 5.4 EC50 = 3700 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
315 7 1 3 3.7 COc1cccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)c1
CHEMBL4116318 5ht2a_human Human No 5.4 EC50 = 3700 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
315 7 1 3 3.7 COc1cccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)c1
CHEMBL4067525 5ht2a_human Human No 5.4 EC50 = 3715.4 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
315 7 1 3 3.7 COc1cccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)c1
CHEMBL4116318 5ht2a_human Human No 5.4 EC50 = 3715.4 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
315 7 1 3 3.7 COc1cccc(CNC[C@H]2C[C@@H]2c2cc(F)ccc2OC)c1
CHEMBL4457840 5ht2a_human Human Yes 5.4 EC50 = 3715.4 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
183 2 1 1 2.0 NCC1C(c2ccccc2)C1(F)F
CHEMBL4596163 5ht2a_human Human Yes 5.4 EC50 = 3715.4 nM Funct
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
183 2 1 1 2.0 NCC1C(c2ccccc2)C1(F)F
CHEMBL374436 5ht2a_human Human No 6.4 EC50 = 374 nM Funct
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
246 2 1 3 1.4 CCc1cc2c(cc1OC)C(=O)N1CCNC[C@@H]21
CHEMBL3416063 5ht2a_human Human No 6.4 EC50 = 374 nM Funct
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
221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CN
CHEMBL3546958 5ht2a_human Human No 6.4 EC50 = 374 nM Funct
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
221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CN
CHEMBL80862 5ht2a_human Human No 6.4 EC50 = 378 nM Funct
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
236 4 1 3 2.5 CCSc1ccc2c(c1)N(C[C@H](C)N)CC2
CHEMBL3769454 5ht2a_human Human No 7.4 EC50 = 38 nM Funct
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
245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN
CHEMBL3771393 5ht2a_human Human No 7.4 EC50 = 38 nM Funct
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
245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN
CHEMBL4567689 5ht2a_human Human No 7.4 EC50 = 38.0 nM Funct
Positive allosteric modulation of 5HT2A receptor (unknown origin) expressed in HEK293 cells co-expressing NFAT-RE assessed as increase in serotonin-induced reponse after 6 to 12 hrs by Bright-Glo luciferase reporter gene assayPositive allosteric modulation of 5HT2A receptor (unknown origin) expressed in HEK293 cells co-expressing NFAT-RE assessed as increase in serotonin-induced reponse after 6 to 12 hrs by Bright-Glo luciferase reporter gene assay
320 5 0 3 3.6 O=C(c1ccc(N2CCN(Cc3ccccc3)CC2)cc1)C1CC1
CHEMBL3330640 5ht2a_human Human Yes 7.4 EC50 = 38.3 nM Funct
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
188 4 2 1 2.3 CCNCCc1c[nH]c2ccccc12
CHEMBL2397893 5ht2a_human Human No 6.4 EC50 = 381 nM Funct
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
236 0 1 2 1.3 O=C1c2c(Cl)cccc2C[C@@H]2CNCCN12
CHEMBL4762225 5ht2a_human Human No 6.4 EC50 = 389.1 nM Funct
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
249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12
CHEMBL4803142 5ht2a_human Human No 6.4 EC50 = 389.1 nM Funct
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
249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12
CHEMBL4782824 5ht2a_human Human No 6.4 EC50 = 389.1 nM Funct
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
245 5 1 3 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4803449 5ht2a_human Human No 6.4 EC50 = 389.1 nM Funct
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
245 5 1 3 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4782824 5ht2a_human Human No 6.4 EC50 = 392 nM Funct
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
245 5 1 3 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4803449 5ht2a_human Human No 6.4 EC50 = 392 nM Funct
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
245 5 1 3 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN
CHEMBL4762225 5ht2a_human Human No 6.4 EC50 = 393 nM Funct
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
249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12
CHEMBL4803142 5ht2a_human Human No 6.4 EC50 = 393 nM Funct
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
249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12
CHEMBL4086286 5ht2a_human Human No 6.4 EC50 = 398 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
347 9 1 3 4.1 COc1ccc(F)cc1C1CC1CNCc1ccccc1OCCF
CHEMBL4117192 5ht2a_human Human No 6.4 EC50 = 398 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
347 9 1 3 4.1 COc1ccc(F)cc1C1CC1CNCc1ccccc1OCCF
CHEMBL4778104 5ht2a_human Human No 6.4 EC50 = 398.1 nM Funct
Agonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
229 1 1 3 1.7 c1cc(C2CC2)c2c(n1)N1CCNC[C@H]1CC2
CHEMBL4086286 5ht2a_human Human No 6.4 EC50 = 398.1 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
347 9 1 3 4.1 COc1ccc(F)cc1C1CC1CNCc1ccccc1OCCF
CHEMBL4117192 5ht2a_human Human No 6.4 EC50 = 398.1 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
347 9 1 3 4.1 COc1ccc(F)cc1C1CC1CNCc1ccccc1OCCF
CHEMBL1288716 5ht2a_human Human Yes 8.4 EC50 = 4.1 nM Funct
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
194 2 2 1 2.3 NCCc1c[nH]c2ccc(Cl)cc12
CHEMBL65547 5ht2a_human Human Yes 8.4 EC50 = 4.3 nM Funct
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
204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C
CHEMBL65547 5ht2a_human Human Yes 8.4 EC50 = 4.3 nM Funct
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
204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C
CHEMBL381160 5ht2a_human Human Yes 8.3 EC50 = 4.6 nM Funct
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
178 2 2 1 1.8 NCCc1c[nH]c2cc(F)ccc12
CHEMBL3589582 5ht2a_human Human No 8.3 EC50 = 4.6 nM Bind
Partial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assayPartial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assay
391 7 1 4 3.7 COc1cc(CCNCc2cccc3c2OCC3)c(OC)cc1Br
CHEMBL1643853 5ht2a_human Human No 7.4 EC50 = 40 nM Funct
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
365 4 1 7 1.7 COc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1
CHEMBL210215 5ht2a_human Human No 7.4 EC50 = 40 nM Funct
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
272 1 1 4 1.7 C[C@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1
CHEMBL76781 5ht2a_human Human Yes 6.4 EC50 = 400 nM Funct
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
226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N
CHEMBL26687 5ht2a_rat Rat Yes 5.4 EC50 = 4000 nM Funct
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2A receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2A receptor
211 5 1 4 1.2 COc1cc(CCN)cc(OC)c1OC
CHEMBL319415 5ht2a_rat Rat Yes 5.4 EC50 = 4000 nM Funct
Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2A receptorEffect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2A receptor
225 6 1 4 1.6 CCOc1c(OC)cc(CCN)cc1OC
CHEMBL4639970 5ht2a_human Human No 5.4 EC50 = 4000 nM Funct
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
256 1 1 2 2.6 FC(F)(F)CC1CN2CCNCc3cccc1c32
CHEMBL3416039 5ht2a_human Human No 5.4 EC50 = 4002 nM Funct
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
239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@H]1C[C@@H]1CN
CHEMBL3546902 5ht2a_human Human No 5.4 EC50 = 4002 nM Funct
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
239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@H]1C[C@@H]1CN
CHEMBL570274 5ht2a_human Human No 7.4 EC50 = 41 nM Funct
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
382 5 1 6 2.1 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2C(F)(F)F)n1
CHEMBL209254 5ht2a_human Human No 6.4 EC50 = 416 nM Funct
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
222 1 1 2 2.1 Clc1cccc(N2CC[C@H]3CNC[C@H]32)c1
CHEMBL179915 5ht2a_human Human No 7.4 EC50 = 42 nM Funct
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
259 1 1 2 3.0 COc1cc2c(cc1C(F)(F)F)C(C)CNCC2
CHEMBL371300 5ht2a_rat Rat Yes 7.4 EC50 = 42.7 nM Funct
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21
CHEMBL269521 5ht2a_human Human Yes 6.4 EC50 = 420 nM Funct
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
198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1
CHEMBL4205290 5ht2a_rat Rat No 5.4 EC50 = 4250 nM Funct
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
340 6 1 5 1.6 COc1ccccc1N1CCN(CC1)CCNC(=O)c1ccccn1
CHEMBL3769581 5ht2a_human Human No 6.4 EC50 = 426 nM Funct
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
271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN
CHEMBL3771395 5ht2a_human Human No 6.4 EC50 = 426 nM Funct
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
271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN
CHEMBL269521 5ht2a_human Human Yes 6.4 EC50 = 426.6 nM Funct
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
198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1
CHEMBL3769581 5ht2a_human Human No 6.4 EC50 = 426.6 nM Funct
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
271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN
CHEMBL3771395 5ht2a_human Human No 6.4 EC50 = 426.6 nM Funct
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
271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN
CHEMBL4063091 5ht2a_human Human No 5.4 EC50 = 4260 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
249 6 1 2 2.9 COc1ccc(F)cc1C1CC1CNCC1CC1
CHEMBL4118002 5ht2a_human Human No 5.4 EC50 = 4260 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
249 6 1 2 2.9 COc1ccc(F)cc1C1CC1CNCC1CC1
CHEMBL4063091 5ht2a_human Human No 5.4 EC50 = 4265.8 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
249 6 1 2 2.9 COc1ccc(F)cc1C1CC1CNCC1CC1
CHEMBL4118002 5ht2a_human Human No 5.4 EC50 = 4265.8 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
249 6 1 2 2.9 COc1ccc(F)cc1C1CC1CNCC1CC1
CHEMBL76301 5ht2a_human Human No 6.4 EC50 = 432 nM Funct
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
320 2 1 2 2.1 C[C@H](N)CN1CCc2cc(F)c(I)cc21
CHEMBL4117915 5ht2a_human Human No 6.4 EC50 = 436.5 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
291 6 1 3 3.8 COC1=C(C=C(C=C1)F)[C@H]2C[C@@H]2CNCC3=CC=CS3
CHEMBL3770963 5ht2a_human Human No 6.4 EC50 = 436.5 nM Funct
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
213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN
CHEMBL3771381 5ht2a_human Human No 6.4 EC50 = 436.5 nM Funct
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
213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN
CHEMBL1187187 5ht2a_human Human Yes 6.4 EC50 = 437 nM Funct
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
165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1cccc(F)c1
CHEMBL492926 5ht2a_human Human Yes 6.4 EC50 = 437 nM Funct
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
165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1cccc(F)c1
CHEMBL3770963 5ht2a_human Human No 6.4 EC50 = 437 nM Funct
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
213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN
CHEMBL3771381 5ht2a_human Human No 6.4 EC50 = 437 nM Funct
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
213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN
CHEMBL4117915 5ht2a_human Human No 6.4 EC50 = 438 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
291 6 1 3 3.8 COC1=C(C=C(C=C1)F)[C@H]2C[C@@H]2CNCC3=CC=CS3
CHEMBL1522572 5ht2a_human Human Yes 7.4 EC50 = 44.7 nM Funct
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
174 2 2 1 2.0 Cc1cccc2c(CCN)c[nH]c12
CHEMBL204839 5ht2a_human Human Yes 7.4 EC50 = 44.7 nM Funct
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
174 2 2 1 2.0 Cc1cccc2c(CCN)c[nH]c12
CHEMBL1091105 5ht2a_human Human Yes 6.4 EC50 = 440 nM Funct
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
378 6 2 4 3.6 COc1cc(OC2CCC(C)(C)CC2)c(F)cc1CNC(=O)[C@@H]1CCCN1
CHEMBL201062 5ht2a_human Human No 6.4 EC50 = 446 nM Bind
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cccnc3c21
CHEMBL1186561 5ht2a_human Human No 5.4 EC50 = 4482 nM Funct
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
181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1
CHEMBL469729 5ht2a_human Human No 5.4 EC50 = 4482 nM Funct
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
181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1
CHEMBL223628 5ht2a_human Human No 6.4 EC50 = 449 nM Funct
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
246 2 1 3 1.6 CC(C)Oc1cccc2c1C(=O)N1CCNCC21
CHEMBL4460604 5ht2a_human Human No 7.3 EC50 = 45.7 nM Funct
Positive allosteric modulation of 5HT2A receptor (unknown origin) expressed in HEK293 cells co-expressing NFAT-RE assessed as increase in serotonin-induced reponse after 6 to 12 hrs by Bright-Glo luciferase reporter gene assayPositive allosteric modulation of 5HT2A receptor (unknown origin) expressed in HEK293 cells co-expressing NFAT-RE assessed as increase in serotonin-induced reponse after 6 to 12 hrs by Bright-Glo luciferase reporter gene assay
257 4 0 5 2.4 O=C(c1ccc(-n2cnc([N+](=O)[O-])c2)cc1)C1CC1
CHEMBL4636196 5ht2a_human Human No 5.4 EC50 = 4500 nM Funct
Partial agonist activity at 5HT2A receptor (unknown origin)Partial agonist activity at 5HT2A receptor (unknown origin)
214 0 1 2 2.0 c1cc2c3c(c1)C1(CCC1)CN3CCNC2
CHEMBL4757214 5ht2a_human Human No 6.3 EC50 = 456 nM Funct
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
257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12
CHEMBL4803017 5ht2a_human Human No 6.3 EC50 = 456 nM Funct
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
257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12
CHEMBL4064935 5ht2a_human Human No 6.3 EC50 = 457.1 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
336 6 1 3 4.3 COc1ccc(F)cc1C1CC1CNCc1cccc2cccnc12
CHEMBL4116446 5ht2a_human Human No 6.3 EC50 = 457.1 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
336 6 1 3 4.3 COc1ccc(F)cc1C1CC1CNCc1cccc2cccnc12
CHEMBL4757214 5ht2a_human Human No 6.3 EC50 = 457.1 nM Funct
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
257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12
CHEMBL4803017 5ht2a_human Human No 6.3 EC50 = 457.1 nM Funct
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
257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12
CHEMBL3770963 5ht2a_human Human No 6.3 EC50 = 457.1 nM Funct
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
213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN
CHEMBL3771381 5ht2a_human Human No 6.3 EC50 = 457.1 nM Funct
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
213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN
CHEMBL215781 5ht2a_rat Rat No 6.3 EC50 = 460 nM Funct
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
271 3 1 3 2.1 COc1cc(Br)c(OC)c2c1[C@@H](CN)C2
CHEMBL4064935 5ht2a_human Human No 6.3 EC50 = 460 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
336 6 1 3 4.3 COc1ccc(F)cc1C1CC1CNCc1cccc2cccnc12
CHEMBL4116446 5ht2a_human Human No 6.3 EC50 = 460 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
336 6 1 3 4.3 COc1ccc(F)cc1C1CC1CNCc1cccc2cccnc12
CHEMBL3770963 5ht2a_human Human No 6.3 EC50 = 461 nM Funct
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
213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN
CHEMBL3771381 5ht2a_human Human No 6.3 EC50 = 461 nM Funct
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
213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN
CHEMBL7257 5ht2a_rat Rat Yes 6.3 EC50 = 462 nM Funct
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL4091197 5ht2a_human Human No 6.3 EC50 = 463 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1ccsc1OC
CHEMBL4116144 5ht2a_human Human No 6.3 EC50 = 463 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1ccsc1OC
CHEMBL1186735 5ht2a_human Human No 6.3 EC50 = 465 nM Funct
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
239 2 1 1 2.8 Cc1ccc([C@H]2C[C@@H]2CN)c(Br)c1
CHEMBL475641 5ht2a_human Human No 6.3 EC50 = 465 nM Funct
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
239 2 1 1 2.8 Cc1ccc([C@H]2C[C@@H]2CN)c(Br)c1
CHEMBL471839 5ht2a_human Human Yes 6.3 EC50 = 466 nM Funct
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells by [3H]-inositol phosphate accumulation assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells by [3H]-inositol phosphate accumulation assay
185 2 1 1 2.7 CC(N)Cc1ccc2ccccc2c1
CHEMBL4091197 5ht2a_human Human No 6.3 EC50 = 467.7 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1ccsc1OC
CHEMBL4116144 5ht2a_human Human No 6.3 EC50 = 467.7 nM Funct
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
321 7 1 4 3.8 COc1ccc(F)cc1C1CC1CNCc1ccsc1OC
CHEMBL39 5ht2a_human Human Yes 7.3 EC50 = 47 nM Bind
Agonist activity at 5-HT2A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by Fluo-4 dye based FLIPR assayAgonist activity at 5-HT2A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by Fluo-4 dye based FLIPR assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL2397878 5ht2a_human Human No 7.3 EC50 = 47 nM Funct
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
232 1 1 3 0.7 COc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2
CHEMBL31115 5ht2a_rat Rat Yes 7.3 EC50 = 47.5 nM Funct
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1
CHEMBL201897 5ht2a_human Human No 6.3 EC50 = 473 nM Bind
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ccncc3c21
CHEMBL3769968 5ht2a_human Human No 6.3 EC50 = 489.8 nM Funct
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
239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN
CHEMBL3771384 5ht2a_human Human No 6.3 EC50 = 489.8 nM Funct
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
239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN
CHEMBL234837 5ht2a_rat Rat No 7.3 EC50 = 49.2 nM Funct
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
315 4 1 6 1.7 Cc1noc(Cc2c3c(c(C[C@@H](C)N)c4c2OCC4)OCC3)n1
CHEMBL3769968 5ht2a_human Human No 6.3 EC50 = 491 nM Funct
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
239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN
CHEMBL3771384 5ht2a_human Human No 6.3 EC50 = 491 nM Funct
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
239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN
CHEMBL142368 5ht2a_rat Rat No 5.3 EC50 = 4920 nM Bind
Evaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptorEvaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptor
222 3 2 2 2.1 CN(C)CCc1c[nH]c2c(F)ccc(O)c12
CHEMBL3974905 5ht2a_human Human No 5.3 EC50 = 4950 nM Funct
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assay
159 1 1 1 1.8 C[C@H](N)CC#Cc1ccccc1
CHEMBL3330644 5ht2a_human Human Yes 6.3 EC50 = 496 nM Funct
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
190 3 2 2 1.7 COc1cccc2c(CCN)c[nH]c12
CHEMBL232997 5ht2a_rat Rat No 5.3 EC50 = 4970 nM Funct
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
277 4 2 4 1.1 C[C@@H](N)Cc1c2c(c(CC(=O)O)c3c1OCC3)OCC2
CHEMBL1288717 5ht2a_human Human Yes 8.3 EC50 = 5.1 nM Funct
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
238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12
CHEMBL39 5ht2a_human Human Yes 8.2 EC50 = 5.8 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL4213379 5ht2a_human Human No 7.3 EC50 = 50.1 nM Funct
Agonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assayAgonist activity at 5-HT2AR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1
CHEMBL76781 5ht2a_human Human Yes 7.3 EC50 = 50.1 nM Funct
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
226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N
CHEMBL4533952 5ht2a_human Human No 7.3 EC50 = 50.1 nM Funct
Positive allosteric modulation of 5HT2A receptor (unknown origin) expressed in HEK293 cells co-expressing NFAT-RE assessed as increase in serotonin-induced reponse after 6 to 12 hrs by Bright-Glo luciferase reporter gene assayPositive allosteric modulation of 5HT2A receptor (unknown origin) expressed in HEK293 cells co-expressing NFAT-RE assessed as increase in serotonin-induced reponse after 6 to 12 hrs by Bright-Glo luciferase reporter gene assay
212 3 0 3 2.5 O=C(c1ccc(-n2ccnc2)cc1)C1CC1
CHEMBL348588 5ht2a_human Human Yes 7.3 EC50 = 50.7 nM Funct
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
174 3 2 1 1.9 CNCCc1c[nH]c2ccccc12
CHEMBL1093699 5ht2a_human Human No 6.3 EC50 = 500 nM Funct
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
364 7 2 4 3.2 COc1cc(OCC2CCCCC2)c(F)cc1CNC(=O)[C@@H]1CCCN1
CHEMBL3947276 5ht2a_human Human No 6.3 EC50 = 501.2 nM Funct
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation countingAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
230 2 1 2 2.4 CCCc1cccc2c1CCC1CNCCN21
CHEMBL440752 5ht2a_human Human Yes 6.3 EC50 = 501.2 nM Funct
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
239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21
CHEMBL363772 5ht2a_rat Rat No 5.3 EC50 = 5040 nM Funct
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
303 5 1 4 2.5 COc1cc([C@@H](OC)[C@H](C)N)c(OC)cc1Br
CHEMBL1187196 5ht2a_human Human Yes 6.3 EC50 = 508 nM Funct
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
165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1
CHEMBL493130 5ht2a_human Human Yes 6.3 EC50 = 508 nM Funct
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
165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1
CHEMBL1186164 5ht2a_human Human No 7.3 EC50 = 51 nM Funct
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
215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1Cl
CHEMBL452458 5ht2a_human Human No 7.3 EC50 = 51 nM Funct
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
215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1Cl
CHEMBL440752 5ht2a_human Human Yes 6.3 EC50 = 510 nM Funct
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
239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21
CHEMBL3770753 5ht2a_human Human No 6.3 EC50 = 511 nM Funct
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
213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN
CHEMBL3771382 5ht2a_human Human No 6.3 EC50 = 511 nM Funct
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
213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN
CHEMBL3770753 5ht2a_human Human No 6.3 EC50 = 512.9 nM Funct
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
213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN
CHEMBL3771382 5ht2a_human Human No 6.3 EC50 = 512.9 nM Funct
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
213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN
CHEMBL375170 5ht2a_human Human No 6.3 EC50 = 513 nM Funct
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
296 1 1 2 2.7 O=C1c2c(cc(C3CC3)cc2C(F)(F)F)[C@@H]2CNCCN12
CHEMBL1187377 5ht2a_human Human No 6.3 EC50 = 513 nM Funct
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
163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1ccccc1O
CHEMBL501117 5ht2a_human Human No 6.3 EC50 = 513 nM Funct
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
163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1ccccc1O
CHEMBL1643855 5ht2a_human Human No 5.3 EC50 = 5165 nM Funct
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
336 3 1 7 1.1 c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)nc1
CHEMBL2397896 5ht2a_human Human No 7.3 EC50 = 53 nM Funct
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
216 0 1 2 1.0 Cc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2
CHEMBL4213379 5ht2a_human Human No 7.3 EC50 = 53.2 nM Funct
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
279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1
CHEMBL142936 5ht2a_rat Rat Yes 5.3 EC50 = 5370 nM Bind
Evaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptorEvaluated for the effective concentration at [125I]-DOI-labeled rat 5-hydroxytryptamine 2A receptor
216 5 1 1 3.1 CCN(CC)CCc1c[nH]c2ccccc12
CHEMBL3589594 5ht2a_human Human No 5.3 EC50 = 5370.3 nM Bind
Partial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assayPartial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assay
409 9 1 5 3.8 COc1cc(CCNCc2c(OC)cccc2OC)c(OC)cc1Br
CHEMBL199775 5ht2a_rat Rat Yes 7.3 EC50 = 54 nM Funct
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
205 3 1 4 1.4 COc1ccc2cnn(C[C@H](C)N)c2c1
CHEMBL1186595 5ht2a_human Human No 6.3 EC50 = 547 nM Funct
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
183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)cc1F
CHEMBL471802 5ht2a_human Human No 6.3 EC50 = 547 nM Funct
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
183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)cc1F
CHEMBL2331807 5ht2a_human Human No 6.3 EC50 = 549.5 nM Funct
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
244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2
CHEMBL39 5ht2a_rat Rat Yes 7.3 EC50 = 55.8 nM Funct
The receptor (5-hydroxytryptamine 2A ) mediated mobilization of intracellular calcium [Ca2+] was studied in rat smooth muscle cellsThe receptor (5-hydroxytryptamine 2A ) mediated mobilization of intracellular calcium [Ca2+] was studied in rat smooth muscle cells
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL2331807 5ht2a_human Human No 6.3 EC50 = 550 nM Funct
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
244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2
CHEMBL2113264 5ht2a_human Human No 7.3 EC50 = 56 nM Funct
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
298 1 1 2 2.8 CC(C)[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12
CHEMBL3982376 5ht2a_human Human Yes 5.3 EC50 = 5620 nM Funct
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as induction of calcium mobilization incubated for 15 mins by calcium 5 dye-based fluorescence assay
161 3 1 1 2.4 CC(N)C/C=C/c1ccccc1
CHEMBL1182816 5ht2a_rat Rat No 5.3 EC50 = 5650 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
219 2 1 3 1.4 C[C@@H](N)Cc1c2c(cc3c1OCC3)OCC2
CHEMBL268072 5ht2a_rat Rat No 5.3 EC50 = 5650 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
219 2 1 3 1.4 C[C@@H](N)Cc1c2c(cc3c1OCC3)OCC2
CHEMBL6616 5ht2a_rat Rat Yes 7.2 EC50 = 57 nM Funct
Agonist activity at rat 5-HT2A receptor expressed in African clawed frog oocytes assessed as increase in current amplitudeAgonist activity at rat 5-HT2A receptor expressed in African clawed frog oocytes assessed as increase in current amplitude
321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC
CHEMBL39 5ht2a_rat Rat Yes 7.2 EC50 = 57.9 nM Funct
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL593545 5ht2a_human Human No 6.2 EC50 = 578 nM Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
343 3 1 4 3.6 Clc1ccccc1O[C@@H]1CCCc2ccc(N3CCNCC3)nc21
CHEMBL1187169 5ht2a_human Human No 6.2 EC50 = 578 nM Funct
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
183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)c(F)c1
CHEMBL492306 5ht2a_human Human No 6.2 EC50 = 578 nM Funct
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
183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)c(F)c1
CHEMBL275854 5ht2a_rat Rat Yes 7.2 EC50 = 58 nM Funct
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N
CHEMBL197653 5ht2a_rat Rat Yes 7.2 EC50 = 58.1 nM Funct
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
209 2 2 4 1.2 C[C@H](N)Cn1ncc2ccc(O)c(F)c21
CHEMBL4800666 5ht2a_human Human No 6.2 EC50 = 585 nM Funct
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
231 4 1 3 2.9 CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN
CHEMBL4804119 5ht2a_human Human No 6.2 EC50 = 585 nM Funct
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
231 4 1 3 2.9 CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN
CHEMBL1186019 5ht2a_human Human Yes 6.2 EC50 = 585 nM Funct
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
161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1
CHEMBL445747 5ht2a_human Human Yes 6.2 EC50 = 585 nM Funct
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
161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1
CHEMBL1643672 5ht2a_human Human No 6.2 EC50 = 585 nM Funct
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
271 1 1 5 1.4 c1cc2nc3c(c(N4CCCCC4)n2n1)CCNCC3
CHEMBL4800666 5ht2a_human Human No 6.2 EC50 = 588.8 nM Funct
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
231 4 1 3 2.9 CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN
CHEMBL4804119 5ht2a_human Human No 6.2 EC50 = 588.8 nM Funct
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
231 4 1 3 2.9 CCOc1ccc2occc2c1[C@@H]1C[C@H]1CN
CHEMBL373245 5ht2a_rat Rat Yes 7.2 EC50 = 59.7 nM Funct
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cellsActivity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
225 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(Cl)c21
CHEMBL1177923 5ht2a_rat Rat No 6.2 EC50 = 590 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
215 2 1 3 3.1 C[C@@H](N)Cc1c2ccoc2cc2ccoc12
CHEMBL6871 5ht2a_rat Rat No 6.2 EC50 = 590 nM Bind
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptorAbility to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
215 2 1 3 3.1 C[C@@H](N)Cc1c2ccoc2cc2ccoc12
CHEMBL331241 5ht2a_human Human Yes 8.2 EC50 = 6 nM Funct
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
174 2 2 1 2.0 Cc1ccc2[nH]cc(CCN)c2c1
CHEMBL2393243 5ht2a_human Human No 8.2 EC50 = 6.1 nM Funct
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
330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1
CHEMBL3040324 5ht2a_human Human No 8.2 EC50 = 6.1 nM Funct
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
330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1
CHEMBL232995 5ht2a_rat Rat No 8.2 EC50 = 6.2 nM Funct
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
383 7 1 6 2.6 C[C@@H](N)Cc1c2c(c(COCC(=O)Oc3ccccc3)c3c1OCC3)OCC2
CHEMBL1906905 5ht2a_human Human Yes 8.2 EC50 = 6.3 nM Funct
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
208 2 2 1 2.7 CC(N)Cc1c[nH]c2ccc(Cl)cc12
CHEMBL6616 5ht2a_human Human Yes 8.2 EC50 = 6.3 nM Bind
Partial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assayPartial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assay
321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC
CHEMBL2393245 5ht2a_human Human No 8.2 EC50 = 6.4 nM Funct
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
364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1
CHEMBL3040361 5ht2a_human Human No 8.2 EC50 = 6.4 nM Funct
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
364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1
CHEMBL6607 5ht2a_rat Rat Yes 7.2 EC50 = 60 nM Funct
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
273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC
CHEMBL76307 5ht2a_human Human Yes 6.2 EC50 = 602 nM Funct
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
210 2 1 2 2.1 C[C@H](N)CN1CCc2ccc(Cl)cc21
CHEMBL2337106 5ht2a_human Human No 6.2 EC50 = 605 nM Funct
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
284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21
CHEMBL2365079 5ht2a_human Human No 6.2 EC50 = 605 nM Funct
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
284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21
CHEMBL2337496 5ht2a_human Human No 6.2 EC50 = 605 nM Funct
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
236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O
CHEMBL2365472 5ht2a_human Human No 6.2 EC50 = 605 nM Funct
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
236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O
CHEMBL179378 5ht2a_human Human Yes 7.2 EC50 = 61 nM Funct
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
317 1 1 2 2.5 COc1cc2c(cc1I)C(C)CNCC2
CHEMBL211309 5ht2a_rat Rat Yes 5.2 EC50 = 6100 nM Funct
Activity at rat 5HT2A receptor assessed as 5-HT-stimulated IP3 accumulationActivity at rat 5HT2A receptor assessed as 5-HT-stimulated IP3 accumulation
237 4 1 4 1.7 COc1cc2c(c(OC)c1OC)CCC2CN
CHEMBL1187195 5ht2a