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
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H don H acc LogP Smiles
CHEMBL591223 5ht2a_human Human No 9.2 EC50 = 0.7 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
436 4 2 3 3.7 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)Cl)OC
CHEMBL591223 5ht2a_human Human No 9.2 EC50 = 0.7 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
436 4 2 3 3.7 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)Cl)OC
CHEMBL350221 5ht2a_human Human Yes 8.9 EC50 = 1.3 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 4 -1.2 C1=CC2=C(C=C1O)C(=CN2)CC(C(=O)O)N
CHEMBL350221 5ht2a_human Human Yes 8.9 EC50 = 1.3 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 4 -1.2 C1=CC2=C(C=C1O)C(=CN2)CC(C(=O)O)N
CHEMBL350221 5ht2a_human Human Yes 8.7 EC50 = 1.9 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 4 -1.2 C1=CC2=C(C=C1O)C(=CN2)CC(C(=O)O)N
CHEMBL253591 5ht2a_human Human No 8.0 EC50 = 10 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
230 0 1 1 3.4 CC1CNCCC2=CC(=C(C=C12)Cl)Cl
CHEMBL253591 5ht2a_human Human No 8.0 EC50 = 10 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
230 0 1 1 3.4 CC1CNCCC2=CC(=C(C=C12)Cl)Cl
CHEMBL3589578 5ht2a_human Human No 8.0 EC50 = 10.5 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
394 7 1 5 3.7 COC1=CC(=C(C=C1CCNCC2=C3C(=CC=C2)OCO3)OC)Br
CHEMBL3589578 5ht2a_human Human No 8.0 EC50 = 10.5 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
394 7 1 5 3.7 COC1=CC(=C(C=C1CCNCC2=C3C(=CC=C2)OCO3)OC)Br
CHEMBL399750 5ht2a_human Human No 7.0 EC50 = 100 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 1 1 2 2.7 CC1CNCCC2=CC(=C(C=C12)OC)Cl
CHEMBL253805 5ht2a_human Human No 7.0 EC50 = 100 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
230 0 1 1 3.4 CC1CNCCC2=CC(=C(C=C12)Cl)Cl
CHEMBL178124 5ht2a_human Human No 7.0 EC50 = 100 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 4 3.0 CC1CNCCC2=C1C=C(C=C2)C(F)(F)F
CHEMBL180668 5ht2a_human Human Yes 7.0 EC50 = 100 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
182 0 1 1 2.4 C1CNCCC2=C1C=CC(=C2)Cl
CHEMBL254215 5ht2a_human Human No 7.0 EC50 = 100 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 4 3.0 CC1CNCCC2=C1C=C(C=C2)C(F)(F)F
CHEMBL188709 5ht2a_rat Rat No 7.0 EC50 = 100 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
290 4 2 4 1.2 CC(C(C1=CC(=C(C=C1OC)Br)OC)O)N
CHEMBL399750 5ht2a_human Human No 7.0 EC50 = 100 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 1 1 2 2.7 CC1CNCCC2=CC(=C(C=C12)OC)Cl
CHEMBL253805 5ht2a_human Human No 7.0 EC50 = 100 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
230 0 1 1 3.4 CC1CNCCC2=CC(=C(C=C12)Cl)Cl
CHEMBL178124 5ht2a_human Human No 7.0 EC50 = 100 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 4 3.0 CC1CNCCC2=C1C=C(C=C2)C(F)(F)F
CHEMBL180668 5ht2a_human Human Yes 7.0 EC50 = 100 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
182 0 1 1 2.4 C1CNCCC2=C1C=CC(=C2)Cl
CHEMBL254215 5ht2a_human Human No 7.0 EC50 = 100 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 4 3.0 CC1CNCCC2=C1C=C(C=C2)C(F)(F)F
CHEMBL180166 5ht2a_human Human No 7.0 EC50 = 100 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
256 1 1 2 2.4 COC1=C(C=C2CCNCCC2=C1)Br
CHEMBL178124 5ht2a_human Human No 7.0 EC50 = 100 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 4 3.0 CC1CNCCC2=C1C=C(C=C2)C(F)(F)F
CHEMBL426235 5ht2a_human Human No 7.0 EC50 = 100 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
284 2 1 2 3.1 CCC1CNCCC2=CC(=C(C=C12)Br)OC
CHEMBL188709 5ht2a_rat Rat No 7.0 EC50 = 100 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
290 4 2 4 1.2 CC(C(C1=CC(=C(C=C1OC)Br)OC)O)N
CHEMBL253807 5ht2a_human Human Yes 6.0 EC50 = 1000 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
214 0 1 2 2.8 CC1CNCCC2=C1C(=C(C=C2)Cl)F
CHEMBL253807 5ht2a_human Human Yes 6.0 EC50 = 1000 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
214 0 1 2 2.8 CC1CNCCC2=C1C(=C(C=C2)Cl)F
CHEMBL2397907 5ht2a_human Human No 6.0 EC50 = 1030 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 0.8 COC1=CC=CC2=C1CC3CNCCN3C2=O
CHEMBL3589595 5ht2a_human Human No 7.0 EC50 = 104.7 Funct
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
398 8 1 5 4.0 COC1=CC=CC(=C1F)CNCCC2=CC(=C(C=C2OC)Br)OC
CHEMBL3589595 5ht2a_human Human No 7.0 EC50 = 104.7 Funct
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
398 8 1 5 4.0 COC1=CC=CC(=C1F)CNCCC2=CC(=C(C=C2OC)Br)OC
CHEMBL2397910 5ht2a_human Human No 6.0 EC50 = 1046 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 1.6 CC1=CC(=C2C(=C1)CC3CNCCN3C2=O)C
CHEMBL2397915 5ht2a_human Human No 7.0 EC50 = 106 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 5 1.7 C1CN2C(CC3=C(C2=O)C=C(C=C3)C(F)(F)F)CN1
CHEMBL80246 5ht2a_human Human No 6.0 EC50 = 1063 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 6 2.6 CC(CN1CCC2=CC(=C(C=C21)C(F)(F)F)F)N
CHEMBL2397892 5ht2a_human Human No 7.0 EC50 = 107 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 5 1.7 C1CN2C(CC3=C(C2=O)C(=CC=C3)C(F)(F)F)CN1
CHEMBL209155 5ht2a_human Human No 6.0 EC50 = 1080 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 4 3.4 C1CC(C2C1CNC2)C3=CC(=CC=C3)C(F)(F)F
CHEMBL209155 5ht2a_human Human No 6.0 EC50 = 1080 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 4 3.4 C1CC(C2C1CNC2)C3=CC(=CC=C3)C(F)(F)F
CHEMBL2397891 5ht2a_human Human No 7.0 EC50 = 109 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 1.7 C1CC1C2=CC=CC3=C2C(=O)N4CCNCC4C3
CHEMBL569342 5ht2a_human Human No 6.0 EC50 = 1090 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 7 1.4 C1CN(CCN1)C2=NN(C(=O)C=C2)CCOC3=CC=CC=C3C(F)(F)F
CHEMBL569342 5ht2a_human Human No 6.0 EC50 = 1090 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 7 1.4 C1CN(CCN1)C2=NN(C(=O)C=C2)CCOC3=CC=CC=C3C(F)(F)F
CHEMBL360968 5ht2a_human Human No 7.0 EC50 = 110 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
284 2 1 2 3.1 CCOC1=C(C=C2C(CNCCC2=C1)C)Br
CHEMBL170319 5ht2a_human Human No 6.0 EC50 = 1100 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 2.7 CC1CCC2=C3N1C=C(C3=CC(=C2)F)CCNC
CHEMBL119323 5ht2a_rat Rat No 6.0 EC50 = 1100 Funct
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
298 2 1 3 2.0 COC1=CC(=C2C3=C1C(CCC3CO2)CN)Br
CHEMBL220207 5ht2a_human Human No 7.0 EC50 = 111 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 0.8 CSC1=CC=CC2=C1C(=O)N3C2CNCC3
CHEMBL220207 5ht2a_human Human No 7.0 EC50 = 111 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 0.8 CSC1=CC=CC2=C1C(=O)N3C2CNCC3
CHEMBL379637 5ht2a_rat Rat No 6.0 EC50 = 1120 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
272 3 1 3 0.4 COC1=CC(=C(C2=C1C(C2)CN)OC)Br
CHEMBL209106 5ht2a_human Human Yes 6.0 EC50 = 1120 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 3 1.9 C1CN(C2C1CNC2)C3=CC(=CC=C3)F
CHEMBL379637 5ht2a_rat Rat No 6.0 EC50 = 1120 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
272 3 1 3 0.4 COC1=CC(=C(C2=C1C(C2)CN)OC)Br
CHEMBL209106 5ht2a_human Human Yes 6.0 EC50 = 1120 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 3 1.9 C1CN(C2C1CNC2)C3=CC(=CC=C3)F
CHEMBL570023 5ht2a_human Human No 6.9 EC50 = 114 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
349 5 1 4 1.5 CC1CNCCN1C2=NN(C(=O)C=C2)CCOC3=CC=CC=C3Cl
CHEMBL570023 5ht2a_human Human No 6.9 EC50 = 114 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
349 5 1 4 1.5 CC1CNCCN1C2=NN(C(=O)C=C2)CCOC3=CC=CC=C3Cl
CHEMBL210802 5ht2a_human Human Yes 6.9 EC50 = 116 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 7 1.4 C1CN(C2C1CNC2)C3=NC=CC(=N3)C(F)(F)F
CHEMBL133868 5ht2a_rat Rat Yes 6.9 EC50 = 116 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 2.2 CC(CC1=CNC2=C1C3=C(C=C2)OCCC3)N
CHEMBL210802 5ht2a_human Human Yes 6.9 EC50 = 116 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 7 1.4 C1CN(C2C1CNC2)C3=NC=CC(=N3)C(F)(F)F
CHEMBL221113 5ht2a_human Human No 5.9 EC50 = 1170 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 5 2.0 CCC1=CC(=C2C(=C1)C3CNCCN3C2=O)C(F)(F)F
CHEMBL221113 5ht2a_human Human No 5.9 EC50 = 1170 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 5 2.0 CCC1=CC(=C2C(=C1)C3CNCCN3C2=O)C(F)(F)F
CHEMBL379637 5ht2a_rat Rat No 5.9 EC50 = 1180 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
272 3 1 3 0.4 COC1=CC(=C(C2=C1C(C2)CN)OC)Br
CHEMBL379637 5ht2a_rat Rat No 5.9 EC50 = 1180 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
272 3 1 3 0.4 COC1=CC(=C(C2=C1C(C2)CN)OC)Br
CHEMBL234464 5ht2a_rat Rat No 7.9 EC50 = 12 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 1.3 CC(CC1=C2CCOC2=C(C3=C1OCC3)COC)N
CHEMBL234464 5ht2a_rat Rat No 7.9 EC50 = 12 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 1.3 CC(CC1=C2CCOC2=C(C3=C1OCC3)COC)N
CHEMBL301466 5ht2a_human Human Yes 7.9 EC50 = 12 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
272 0 2 3 1.7 C1CN2C(CN1)C(=O)NC3=CC(=C(C=C32)Cl)Cl
CHEMBL589769 5ht2a_human Human No 6.9 EC50 = 120 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
455 4 2 6 4.3 CN1C(=C(C=N1)Br)C2=CC(=CC=C2)NC(=O)NC3=CC=C(C=C3)OC(F)(F)F
CHEMBL191051 5ht2a_rat Rat Yes 6.9 EC50 = 120 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
290 5 1 4 1.3 COC1=CC(=C(C=C1C(CN)OC)OC)Br
CHEMBL589769 5ht2a_human Human No 6.9 EC50 = 120 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
455 4 2 6 4.3 CN1C(=C(C=N1)Br)C2=CC(=CC=C2)NC(=O)NC3=CC=C(C=C3)OC(F)(F)F
CHEMBL191051 5ht2a_rat Rat Yes 6.9 EC50 = 120 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
290 5 1 4 1.3 COC1=CC(=C(C=C1C(CN)OC)OC)Br
CHEMBL116940 5ht2a_rat Rat No 6.9 EC50 = 120 Funct
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
296 2 1 3 2.5 COC1=CC(=C2C3=C1C(CCC3=CO2)CN)Br
CHEMBL1643857 5ht2a_human Human No 5.9 EC50 = 1227 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 6 1.1 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC=NC=C5
CHEMBL1643857 5ht2a_human Human No 5.9 EC50 = 1227 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 6 1.1 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC=NC=C5
CHEMBL223468 5ht2a_human Human No 6.9 EC50 = 123 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 1.1 CCC1=C(C2=C(C=C1)C3CNCCN3C2=O)OC
CHEMBL223468 5ht2a_human Human No 6.9 EC50 = 123 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 1.1 CCC1=C(C2=C(C=C1)C3CNCCN3C2=O)OC
CHEMBL2397887 5ht2a_human Human No 6.9 EC50 = 123 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 1.3 CC1CNCC2N1C(=O)C3=CC=CC=C3C2
CHEMBL80482 5ht2a_human Human No 6.9 EC50 = 125 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 1.9 CC(CN1CCC2=C1C3=C(C=C2)OCCC3)N
CHEMBL179337 5ht2a_human Human Yes 6.9 EC50 = 125.9 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
230 0 1 1 3.4 CC1CNCCC2=C(C=C(C=C12)Cl)Cl
CHEMBL181076 5ht2a_human Human Yes 6.9 EC50 = 125.9 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
230 0 1 1 3.4 CC1CNCCC2=C1C(=C(C=C2)Cl)Cl
CHEMBL254009 5ht2a_human Human No 6.9 EC50 = 125.9 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 4 3.0 CC1CNCCC2=C1C=C(C=C2)C(F)(F)F
CHEMBL179337 5ht2a_human Human Yes 6.9 EC50 = 125.9 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
230 0 1 1 3.4 CC1CNCCC2=C(C=C(C=C12)Cl)Cl
CHEMBL181076 5ht2a_human Human Yes 6.9 EC50 = 125.9 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
230 0 1 1 3.4 CC1CNCCC2=C1C(=C(C=C2)Cl)Cl
CHEMBL254009 5ht2a_human Human No 6.9 EC50 = 125.9 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 4 3.0 CC1CNCCC2=C1C=C(C=C2)C(F)(F)F
CHEMBL3330646 5ht2a_human Human No 5.9 EC50 = 1250 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 2.5 CCC(CC1=CNC2=CC=CC=C21)N
CHEMBL3330646 5ht2a_human Human No 5.9 EC50 = 1250 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 2.5 CCC(CC1=CNC2=CC=CC=C21)N
CHEMBL375302 5ht2a_human Human No 6.9 EC50 = 126 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 5 2.2 CCC1C2C3=C(C(=CC=C3)C(F)(F)F)C(=O)N2CCN1
CHEMBL375302 5ht2a_human Human No 6.9 EC50 = 126 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 5 2.2 CCC1C2C3=C(C(=CC=C3)C(F)(F)F)C(=O)N2CCN1
CHEMBL101008 5ht2a_rat Rat Yes 7.9 EC50 = 13 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
298 2 1 3 2.4 CC(CC1=C2CCOC2=C(C3=C1OCC3)Br)N
CHEMBL101008 5ht2a_rat Rat Yes 7.9 EC50 = 13 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
298 2 1 3 2.4 CC(CC1=C2CCOC2=C(C3=C1OCC3)Br)N
CHEMBL520449 5ht2a_rat Rat No 7.9 EC50 = 13 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
310 2 1 3 3.1 CC(CC1=C2CCCOC2=C(C3=C1OC=C3)Br)N
CHEMBL101008 5ht2a_rat Rat Yes 7.9 EC50 = 13 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
298 2 1 3 2.4 CC(CC1=C2CCOC2=C(C3=C1OCC3)Br)N
CHEMBL101008 5ht2a_rat Rat Yes 7.9 EC50 = 13 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
298 2 1 3 2.4 CC(CC1=C2CCOC2=C(C3=C1OCC3)Br)N
CHEMBL520449 5ht2a_rat Rat No 7.9 EC50 = 13 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
310 2 1 3 3.1 CC(CC1=C2CCCOC2=C(C3=C1OC=C3)Br)N
CHEMBL350221 5ht2a_human Human Yes 6.9 EC50 = 130 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 4 -1.2 C1=CC2=C(C=C1O)C(=CN2)CC(C(=O)O)N
CHEMBL1091106 5ht2a_human Human No 6.9 EC50 = 130 Funct
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
366 5 2 5 3.8 CC1(CCC(CC1)OC2=C(C=C(C(=C2)F)CNC(=O)C3CCCN3)F)C
CHEMBL590483 5ht2a_human Human No 6.9 EC50 = 130 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
252 0 2 3 1.6 C1CNCCN2C1NC(=O)C3=C2C=CC=C3Cl
CHEMBL365958 5ht2a_rat Rat No 6.9 EC50 = 130 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
304 5 1 4 1.7 CC(C(C1=CC(=C(C=C1OC)Br)OC)OC)N
CHEMBL350221 5ht2a_human Human Yes 6.9 EC50 = 130 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 4 -1.2 C1=CC2=C(C=C1O)C(=CN2)CC(C(=O)O)N
CHEMBL1091106 5ht2a_human Human No 6.9 EC50 = 130 Funct
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
366 5 2 5 3.8 CC1(CCC(CC1)OC2=C(C=C(C(=C2)F)CNC(=O)C3CCCN3)F)C
CHEMBL590483 5ht2a_human Human No 6.9 EC50 = 130 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
252 0 2 3 1.6 C1CNCCN2C1NC(=O)C3=C2C=CC=C3Cl
CHEMBL365958 5ht2a_rat Rat No 6.9 EC50 = 130 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
304 5 1 4 1.7 CC(C(C1=CC(=C(C=C1OC)Br)OC)OC)N
CHEMBL2331794 5ht2a_human Human No 5.9 EC50 = 1300 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 2.1 C1CNCCC2=C1C(=NO2)OCC3=CC=CC=C3
CHEMBL220274 5ht2a_human Human No 6.9 EC50 = 131 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 5 1.2 C1CN2C(CN1)C3=C(C2=O)C(=CC=C3)C(F)(F)F
CHEMBL76781 5ht2a_human Human Yes 6.9 EC50 = 131 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
227 2 1 2 2.2 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N
CHEMBL220274 5ht2a_human Human No 6.9 EC50 = 131 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 5 1.2 C1CN2C(CN1)C3=C(C2=O)C(=CC=C3)C(F)(F)F
CHEMBL76781 5ht2a_human Human Yes 6.9 EC50 = 131 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
227 2 1 2 2.2 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N
CHEMBL76781 5ht2a_human Human Yes 6.9 EC50 = 131 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
227 2 1 2 2.2 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N
CHEMBL595553 5ht2a_human Human No 5.9 EC50 = 1311 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
330 3 1 4 3.2 C1CC2=C(C1OC3=CC=CC=C3Cl)N=C(C=C2)N4CCNCC4
CHEMBL595553 5ht2a_human Human No 5.9 EC50 = 1311 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
330 3 1 4 3.2 C1CC2=C(C1OC3=CC=CC=C3Cl)N=C(C=C2)N4CCNCC4
CHEMBL364718 5ht2a_rat Rat No 5.9 EC50 = 1330 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
304 5 1 4 1.7 CC(C(C1=CC(=C(C=C1OC)Br)OC)OC)N
CHEMBL364718 5ht2a_rat Rat No 5.9 EC50 = 1330 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
304 5 1 4 1.7 CC(C(C1=CC(=C(C=C1OC)Br)OC)OC)N
CHEMBL131736 5ht2a_rat Rat No 6.9 EC50 = 134 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 2 2.1 CC(CC1=CN(C2=C1C3=C(C=C2)OCCC3)C)N
CHEMBL181076 5ht2a_human Human Yes 6.9 EC50 = 135 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
230 0 1 1 3.4 CC1CNCCC2=C1C(=C(C=C2)Cl)Cl
CHEMBL2397914 5ht2a_human Human No 5.9 EC50 = 1379 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 1.2 C1CC2=C(C3=C(C=C2)C(=O)N4CCNCC4C3)OC1
CHEMBL1643674 5ht2a_human Human No 6.9 EC50 = 138 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 4 0.9 CCNC1=C2CCNCCC2=NC3=CC=NN31
CHEMBL1643674 5ht2a_human Human No 6.9 EC50 = 138 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 4 0.9 CCNC1=C2CCNCCC2=NC3=CC=NN31
CHEMBL494947 5ht2a_human Human Yes 6.9 EC50 = 140 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
305 4 1 5 2.0 C1CN(CCN1)C2=CN=CC(=N2)OCC3=CC(=CC=C3)Cl
CHEMBL589 5ht2a_human Human Yes 6.9 EC50 = 141.3 Funct
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 2.7 CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL191420 5ht2a_rat Rat No 5.9 EC50 = 1410 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
304 5 1 4 1.7 CC(C(C1=CC(=C(C=C1OC)Br)OC)OC)N
CHEMBL191420 5ht2a_rat Rat No 5.9 EC50 = 1410 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
304 5 1 4 1.7 CC(C(C1=CC(=C(C=C1OC)Br)OC)OC)N
CHEMBL595645 5ht2a_human Human No 5.8 EC50 = 1428 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
359 4 1 6 2.9 CC1CNCCN1C2=NC3=C(CCC3OCC4=C(C=CC(=C4)F)F)C=C2
CHEMBL595645 5ht2a_human Human No 5.9 EC50 = 1428 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
359 4 1 6 2.9 CC1CNCCN1C2=NC3=C(CCC3OCC4=C(C=CC(=C4)F)F)C=C2
CHEMBL171774 5ht2a_human Human Yes 6.8 EC50 = 145 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 1 1.6 C1CC2=CC=CC3=C2N(C1)C=C3CCN
CHEMBL482704 5ht2a_rat Rat No 6.8 EC50 = 146 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
298 2 1 3 2.3 C1CC2=C(C(=C3CCOC3=C2Br)CCN)OC1
CHEMBL482704 5ht2a_rat Rat No 6.8 EC50 = 146 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
298 2 1 3 2.3 C1CC2=C(C(=C3CCOC3=C2Br)CCN)OC1
CHEMBL2397912 5ht2a_human Human No 6.8 EC50 = 148 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 1.2 CC1=C2C(=C(C=C1)OC)CC3CNCCN3C2=O
CHEMBL181672 5ht2a_human Human Yes 6.8 EC50 = 150 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
196 0 1 1 2.7 CC1CNCCC2=C1C=CC(=C2)Cl
CHEMBL594469 5ht2a_human Human No 5.8 EC50 = 1500 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
345 4 1 6 2.5 C1CC2=C(C1OCC3=C(C=CC(=C3)F)F)N=C(C=C2)N4CCNCC4
CHEMBL594469 5ht2a_human Human No 5.8 EC50 = 1500 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
345 4 1 6 2.5 C1CC2=C(C1OCC3=C(C=CC(=C3)F)F)N=C(C=C2)N4CCNCC4
CHEMBL1093698 5ht2a_human Human No 6.8 EC50 = 153 Funct
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
352 5 2 5 3.4 CC1CCC(CC1)OC2=C(C=C(C=C2F)CNC(=O)C3CCCN3)F
CHEMBL1093698 5ht2a_human Human No 6.8 EC50 = 153 Funct
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
352 5 2 5 3.4 CC1CCC(CC1)OC2=C(C=C(C=C2F)CNC(=O)C3CCCN3)F
CHEMBL360328 5ht2a_human Human Yes 6.8 EC50 = 158.5 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL181672 5ht2a_human Human Yes 6.8 EC50 = 158.5 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
196 0 1 1 2.7 CC1CNCCC2=C1C=CC(=C2)Cl
CHEMBL360328 5ht2a_human Human Yes 6.8 EC50 = 158.5 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL181672 5ht2a_human Human Yes 6.8 EC50 = 158.5 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
196 0 1 1 2.7 CC1CNCCC2=C1C=CC(=C2)Cl
CHEMBL178252 5ht2a_human Human Yes 5.8 EC50 = 1584.9 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 2 2.2 CC1CNCCC2=C1C=C(C=C2)F
CHEMBL367796 5ht2a_human Human Yes 5.8 EC50 = 1584.9 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 2.1 CC1CNCCC2=CC=CC=C12
CHEMBL398926 5ht2a_human Human Yes 5.8 EC50 = 1584.9 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
210 0 1 1 3.3 CC1(CNCCC2=C1C=C(C=C2)Cl)C
CHEMBL178252 5ht2a_human Human Yes 5.8 EC50 = 1584.9 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 2 2.2 CC1CNCCC2=C1C=C(C=C2)F
CHEMBL367796 5ht2a_human Human Yes 5.8 EC50 = 1584.9 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 2.1 CC1CNCCC2=CC=CC=C12
CHEMBL398926 5ht2a_human Human Yes 5.8 EC50 = 1584.9 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
210 0 1 1 3.3 CC1(CNCCC2=C1C=C(C=C2)Cl)C
CHEMBL178366 5ht2a_human Human No 7.8 EC50 = 16 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
230 0 1 1 3.4 CC1CNCCC2=CC(=C(C=C12)Cl)Cl
CHEMBL234682 5ht2a_rat Rat No 7.8 EC50 = 16.9 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 3.1 CC1=NOC(=N1)CC2=C3C=COC3=C(C4=C2OC=C4)CC(C)N
CHEMBL234682 5ht2a_rat Rat No 7.8 EC50 = 16.9 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 3.1 CC1=NOC(=N1)CC2=C3C=COC3=C(C4=C2OC=C4)CC(C)N
CHEMBL576631 5ht2a_canlf Dog No 5.8 EC50 = 1600 Funct
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
293 2 1 4 2.8 CC1=NN=C2N1C(=NC3=C2CCNCC3)CC4=CC=CC=C4
CHEMBL576631 5ht2a_canlf Dog No 5.8 EC50 = 1600 Funct
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
293 2 1 4 2.8 CC1=NN=C2N1C(=NC3=C2CCNCC3)CC4=CC=CC=C4
CHEMBL178252 5ht2a_human Human Yes 5.8 EC50 = 1600 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 2 2.2 CC1CNCCC2=C1C=C(C=C2)F
CHEMBL367796 5ht2a_human Human Yes 5.8 EC50 = 1600 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 2.1 CC1CNCCC2=CC=CC=C12
CHEMBL222566 5ht2a_human Human No 5.8 EC50 = 1620 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 5 2.0 C=CC1=CC2=C(C(=C1)C(F)(F)F)C(=O)N3C2CNCC3
CHEMBL222566 5ht2a_human Human No 5.8 EC50 = 1620 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 5 2.0 C=CC1=CC2=C(C(=C1)C(F)(F)F)C(=O)N3C2CNCC3
CHEMBL451543 5ht2a_human Human No 6.8 EC50 = 164 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 CC(CN1CCC2=C1C=C(C=C2)SC)N
CHEMBL360328 5ht2a_human Human Yes 6.8 EC50 = 166.0 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL360328 5ht2a_human Human Yes 6.8 EC50 = 166.0 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL374562 5ht2a_human Human No 6.8 EC50 = 167 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 5 1.6 CC1=CC(=C2C(=C1)C3CNCCN3C2=O)C(F)(F)F
CHEMBL374562 5ht2a_human Human No 6.8 EC50 = 167 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 5 1.6 CC1=CC(=C2C(=C1)C3CNCCN3C2=O)C(F)(F)F
CHEMBL209714 5ht2a_human Human No 6.8 EC50 = 168 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 5 2.7 C1CN(C2C1CNC2)C3=CC=CC(=C3)C(F)(F)F
CHEMBL209714 5ht2a_human Human No 6.8 EC50 = 168 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 5 2.7 C1CN(C2C1CNC2)C3=CC=CC(=C3)C(F)(F)F
CHEMBL134519 5ht2a_rat Rat Yes 7.8 EC50 = 17.8 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 2.5 CC(CC1=CC(=C(C=C1OC)I)OC)N
CHEMBL134519 5ht2a_rat Rat Yes 7.8 EC50 = 17.8 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 2.5 CC(CC1=CC(=C(C=C1OC)I)OC)N
CHEMBL179337 5ht2a_human Human Yes 6.8 EC50 = 170 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
230 0 1 1 3.4 CC1CNCCC2=C(C=C(C=C12)Cl)Cl
CHEMBL394664 5ht2a_rat Rat No 6.8 EC50 = 175 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 0.8 CC(CC1=C2CCOC2=C(C3=C1OCC3)CO)N
CHEMBL394664 5ht2a_rat Rat No 6.8 EC50 = 175 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 0.8 CC(CC1=C2CCOC2=C(C3=C1OCC3)CO)N
CHEMBL222514 5ht2a_human Human No 6.8 EC50 = 176 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 5 1.2 C1CN2C(CN1)C3=C(C2=O)C(=CC=C3)C(F)(F)F
CHEMBL222514 5ht2a_human Human No 6.8 EC50 = 176 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 5 1.2 C1CN2C(CN1)C3=C(C2=O)C(=CC=C3)C(F)(F)F
CHEMBL223896 5ht2a_human Human No 5.8 EC50 = 1780 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
223 0 1 2 1.0 C1CN2C(CN1)C3=C(C2=O)C(=CC=C3)Cl
CHEMBL223896 5ht2a_human Human No 5.8 EC50 = 1780 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
223 0 1 2 1.0 C1CN2C(CN1)C3=C(C2=O)C(=CC=C3)Cl
CHEMBL379637 5ht2a_rat Rat No 7.8 EC50 = 18 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
272 3 1 3 0.4 COC1=CC(=C(C2=C1C(C2)CN)OC)Br
CHEMBL379637 5ht2a_rat Rat No 7.8 EC50 = 18 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
272 3 1 3 0.4 COC1=CC(=C(C2=C1C(C2)CN)OC)Br
CHEMBL3330643 5ht2a_human Human Yes 7.7 EC50 = 18.8 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
195 2 2 1 2.0 C1=CC2=C(C(=C1)Cl)NC=C2CCN
CHEMBL3330643 5ht2a_human Human Yes 7.7 EC50 = 18.8 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
195 2 2 1 2.0 C1=CC2=C(C(=C1)Cl)NC=C2CCN
CHEMBL30713 5ht2a_human Human Yes 7.7 EC50 = 18.9 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 2.0 CC(CC1=CNC2=CC=CC=C21)N
CHEMBL565547 5ht2a_canlf Dog No 5.8 EC50 = 1800 Funct
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
293 2 1 4 2.4 CC1=NN2C(=NC3=C(C2=N1)CCNCC3)CC4=CC=CC=C4
CHEMBL565547 5ht2a_canlf Dog No 5.8 EC50 = 1800 Funct
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
293 2 1 4 2.4 CC1=NN2C(=NC3=C(C2=N1)CCNCC3)CC4=CC=CC=C4
CHEMBL80731 5ht2a_human Human No 6.7 EC50 = 181 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 4 2.5 CCSC1=C(C=C2CCN(C2=C1)CC(C)N)F
CHEMBL27173 5ht2a_rat Rat No 6.7 EC50 = 181 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 1.7 C1CC2=C(C=CC3=C2C(=CN3)CCN)OC1
CHEMBL142862 5ht2a_rat Rat No 4.7 EC50 = 18100 Funct
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 3 2.4 CN(C)CCC1=CNC2=C1C(=C(C=C2)OC)F
CHEMBL598808 5ht2a_human Human No 7.7 EC50 = 19 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
406 3 2 2 3.8 CN1C(=C(C=N1)Br)C2=CC(=CC=C2)NC(=O)NC3=CC=C(C=C3)Cl
CHEMBL519145 5ht2a_rat Rat No 7.7 EC50 = 19 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
312 2 1 3 2.7 CC(CC1=C2CCCOC2=C(C3=C1OCC3)Br)N
CHEMBL598808 5ht2a_human Human No 7.7 EC50 = 19 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
406 3 2 2 3.8 CN1C(=C(C=N1)Br)C2=CC(=CC=C2)NC(=O)NC3=CC=C(C=C3)Cl
CHEMBL519145 5ht2a_rat Rat No 7.7 EC50 = 19 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
312 2 1 3 2.7 CC(CC1=C2CCCOC2=C(C3=C1OCC3)Br)N
CHEMBL134519 5ht2a_rat Rat Yes 7.7 EC50 = 19.8 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 2.5 CC(CC1=CC(=C(C=C1OC)I)OC)N
CHEMBL134519 5ht2a_rat Rat Yes 7.7 EC50 = 19.8 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 2.5 CC(CC1=CC(=C(C=C1OC)I)OC)N
CHEMBL178366 5ht2a_human Human No 7.7 EC50 = 20.0 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
230 0 1 1 3.4 CC1CNCCC2=CC(=C(C=C12)Cl)Cl
CHEMBL178366 5ht2a_human Human No 7.7 EC50 = 20.0 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
230 0 1 1 3.4 CC1CNCCC2=CC(=C(C=C12)Cl)Cl
CHEMBL360328 5ht2a_human Human Yes 6.7 EC50 = 190 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL2397894 5ht2a_human Human No 6.7 EC50 = 193 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 0.8 COC1=CC=CC2=C1C(=O)N3CCNCC3C2
CHEMBL178231 5ht2a_human Human Yes 6.7 EC50 = 199.5 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
230 0 1 1 3.4 CC1CNCCC2=C1C(=C(C=C2)Cl)Cl
CHEMBL181172 5ht2a_human Human Yes 6.7 EC50 = 199.5 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL253811 5ht2a_human Human Yes 6.7 EC50 = 199.5 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 4 2.5 CC(CC1=CC(=CC=C1)C(F)(F)F)N
CHEMBL253806 5ht2a_human Human No 6.7 EC50 = 199.5 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 1 1 2 2.7 CC1CNCCC2=CC(=C(C=C12)Cl)OC
CHEMBL178231 5ht2a_human Human Yes 6.7 EC50 = 199.5 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
230 0 1 1 3.4 CC1CNCCC2=C1C(=C(C=C2)Cl)Cl
CHEMBL181172 5ht2a_human Human Yes 6.7 EC50 = 199.5 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL253811 5ht2a_human Human Yes 6.7 EC50 = 199.5 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 4 2.5 CC(CC1=CC(=CC=C1)C(F)(F)F)N
CHEMBL253806 5ht2a_human Human No 6.7 EC50 = 199.5 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 1 1 2 2.7 CC1CNCCC2=CC(=C(C=C12)Cl)OC
CHEMBL275628 5ht2a_human Human Yes 8.6 EC50 = 2.6 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 2 0.7 C1=CC2=C(C=C1F)C(=CN2)CCN
CHEMBL275628 5ht2a_human Human Yes 8.6 EC50 = 2.6 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 2 0.7 C1=CC2=C(C=C1F)C(=CN2)CCN
CHEMBL69700 5ht2a_rat Rat Yes 7.7 EC50 = 20 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
274 4 1 3 2.6 CC(CC1=CC(=C(C=C1OC)Br)OC)N
CHEMBL69700 5ht2a_rat Rat Yes 7.7 EC50 = 20 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
274 4 1 3 2.6 CC(CC1=CC(=C(C=C1OC)Br)OC)N
CHEMBL316527 5ht2a_rat Rat Yes 5.7 EC50 = 2000 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 1.2 COC1=C2C(=C(C3=C1OCC3)CCN)CCO2
CHEMBL201132 5ht2a_rat Rat Yes 6.7 EC50 = 204 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 0.8 CC(CN1C2=C(C(=O)C=CC2=CN1)I)N
CHEMBL201132 5ht2a_rat Rat Yes 6.7 EC50 = 204 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 0.8 CC(CN1C2=C(C(=O)C=CC2=CN1)I)N
CHEMBL1643858 5ht2a_human Human No 5.7 EC50 = 2046 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 6 1.5 CC(=O)N(C)C1=CC=C(C=C1)OC2CN(C2)C3=C4CCNCCC4=NC5=CC=NN53
CHEMBL1643858 5ht2a_human Human No 5.7 EC50 = 2046 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 6 1.5 CC(=O)N(C)C1=CC=C(C=C1)OC2CN(C2)C3=C4CCNCCC4=NC5=CC=NN53
CHEMBL2397904 5ht2a_human Human No 6.7 EC50 = 206 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 1.2 CC1=CC=CC2=C1CC3CNCCN3C2=O
CHEMBL3330641 5ht2a_human Human Yes 6.7 EC50 = 209 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 1 1.3 CN1C=C(C2=CC=CC=C21)CCN
CHEMBL3330641 5ht2a_human Human Yes 6.7 EC50 = 209 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 1 1.3 CN1C=C(C2=CC=CC=C21)CCN
CHEMBL445106 5ht2a_rat Rat No 5.7 EC50 = 2090 Funct
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
284 1 1 3 1.9 COC1=CC(=C2C3=C1CC(CC3CO2)N)Br
CHEMBL6557 5ht2a_human Human Yes 6.7 EC50 = 210 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 1 1.9 CN1C2=C(CCNCC2)C3=CC=CC=C31
CHEMBL25800 5ht2a_rat Rat Yes 6.7 EC50 = 213 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 2 1.7 CN1C=C(C2=C1C=CC3=C2CCCO3)CCN
CHEMBL2397890 5ht2a_human Human No 7.7 EC50 = 22 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 1.6 CCC1=CC=CC2=C1C(=O)N3CCNCC3C2
CHEMBL179244 5ht2a_human Human No 7.7 EC50 = 22 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
346 3 1 2 4.3 CC1CNCCC2=CC(=C(C=C12)Br)OCC3=CC=CC=C3
CHEMBL373531 5ht2a_human Human No 6.7 EC50 = 220 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
253 1 1 3 0.9 COC1=C2C3CNCCN3C(=O)C2=C(C=C1)Cl
CHEMBL208936 5ht2a_human Human No 6.7 EC50 = 220 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 7 1.4 C1CN(C2C1CNC2)C3=NC=CC(=N3)C(F)(F)F
CHEMBL373531 5ht2a_human Human No 6.7 EC50 = 220 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
253 1 1 3 0.9 COC1=C2C3CNCCN3C(=O)C2=C(C=C1)Cl
CHEMBL178231 5ht2a_human Human Yes 6.7 EC50 = 220 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
230 0 1 1 3.4 CC1CNCCC2=C1C(=C(C=C2)Cl)Cl
CHEMBL208936 5ht2a_human Human No 6.7 EC50 = 220 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 7 1.4 C1CN(C2C1CNC2)C3=NC=CC(=N3)C(F)(F)F
CHEMBL593547 5ht2a_human Human Yes 5.7 EC50 = 2202 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
217 1 1 3 1.9 C1CCC2=C(C1)C=CC(=N2)N3CCNCC3
CHEMBL593547 5ht2a_human Human Yes 5.7 EC50 = 2202 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
217 1 1 3 1.9 C1CCC2=C(C1)C=CC(=N2)N3CCNCC3
CHEMBL202616 5ht2a_human Human No 6.7 EC50 = 222 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
365 5 1 2 4.9 CC(CN1C=CC2=C1C3=C(C=C2)N=CC=C3)NCC4=CC5=CC=CC=C5C=C4
CHEMBL202616 5ht2a_human Human No 6.7 EC50 = 222 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
365 5 1 2 4.9 CC(CN1C=CC2=C1C3=C(C=C2)N=CC=C3)NCC4=CC5=CC=CC=C5C=C4
CHEMBL6557 5ht2a_human Human Yes 7.6 EC50 = 23 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 1 1.9 CN1C2=C(CCNCC2)C3=CC=CC=C31
CHEMBL30713 5ht2a_human Human Yes 7.6 EC50 = 23.1 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 CC(CC1=CNC2=CC=CC=C21)N
CHEMBL30713 5ht2a_human Human Yes 7.6 EC50 = 23.1 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 CC(CC1=CNC2=CC=CC=C21)N
CHEMBL1643671 5ht2a_human Human No 5.6 EC50 = 2310 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 4 1.2 C1CCN(C1)C2=C3CCNCCC3=NC4=CC=NN42
CHEMBL1643671 5ht2a_human Human No 5.6 EC50 = 2310 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 4 1.2 C1CCN(C1)C2=C3CCNCCC3=NC4=CC=NN42
CHEMBL143202 5ht2a_rat Rat Yes 5.6 EC50 = 2310 Funct
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 2.7 CCN(CC)CCC1=CNC2=C1C(=CC=C2)O
CHEMBL1643670 5ht2a_human Human No 5.6 EC50 = 2348 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 4 0.8 C1CN(C1)C2=C3CCNCCC3=NC4=CC=NN42
CHEMBL1643670 5ht2a_human Human No 5.6 EC50 = 2348 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 4 0.8 C1CN(C1)C2=C3CCNCCC3=NC4=CC=NN42
CHEMBL437314 5ht2a_rat Rat No 6.6 EC50 = 236 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 0.1 CC(CN1C2=CC(=O)C=CC2=CN1)N
CHEMBL595195 5ht2a_human Human No 6.6 EC50 = 236 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
330 3 1 4 3.2 C1CC2=C(C1OC3=CC=CC=C3Cl)N=C(C=C2)N4CCNCC4
CHEMBL437314 5ht2a_rat Rat No 6.6 EC50 = 236 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 0.1 CC(CN1C2=CC(=O)C=CC2=CN1)N
CHEMBL595195 5ht2a_human Human No 6.6 EC50 = 236 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
330 3 1 4 3.2 C1CC2=C(C1OC3=CC=CC=C3Cl)N=C(C=C2)N4CCNCC4
CHEMBL342986 5ht2a_rat Rat Yes 5.6 EC50 = 2390 Funct
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 2.2 CCN(CC)CCC1=CNC2=C1C=C(C=C2)OC
CHEMBL2331794 5ht2a_human Human No 6.6 EC50 = 240 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 2.1 C1CNCCC2=C1C(=NO2)OCC3=CC=CC=C3
CHEMBL2331807 5ht2a_human Human No 5.6 EC50 = 2400 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 3 1.3 C1CNCCC2=C1C(=O)N(O2)CC3=CC=CC=C3
CHEMBL178566 5ht2a_human Human Yes 5.6 EC50 = 2400 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
230 0 1 1 3.4 CC1CNCCC2=C1C(=C(C=C2)Cl)Cl
CHEMBL482675 5ht2a_rat Rat Yes 6.6 EC50 = 241 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
312 2 1 3 2.7 C1CC2=C(C3=C(CCCO3)C(=C2OC1)Br)CCN
CHEMBL482675 5ht2a_rat Rat Yes 6.6 EC50 = 241 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
312 2 1 3 2.7 C1CC2=C(C3=C(CCCO3)C(=C2OC1)Br)CCN
CHEMBL337825 5ht2a_human Human Yes 5.6 EC50 = 2443 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 1.5 COC1=CC2=C(C=C1)C(=CN2)CCN
CHEMBL337825 5ht2a_human Human Yes 5.6 EC50 = 2443 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 1.5 COC1=CC2=C(C=C1)C(=CN2)CCN
CHEMBL3330648 5ht2a_human Human No 6.6 EC50 = 246 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 2 2.9 CCC(CC1=CNC2=C1C=C(C=C2)F)N
CHEMBL3330648 5ht2a_human Human No 6.6 EC50 = 246 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 2 2.9 CCC(CC1=CNC2=C1C=C(C=C2)F)N
CHEMBL590816 5ht2a_human Human No 6.6 EC50 = 248 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 1.0 C1CNCCN2C1NC(=O)C3=CC=CC=C32
CHEMBL590816 5ht2a_human Human No 6.6 EC50 = 248 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 1.0 C1CNCCN2C1NC(=O)C3=CC=CC=C32
CHEMBL3330647 5ht2a_human Human Yes 6.6 EC50 = 249 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
223 3 2 1 2.2 CCC(CC1=CNC2=C1C=C(C=C2)Cl)N
CHEMBL3330647 5ht2a_human Human Yes 6.6 EC50 = 249 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
223 3 2 1 2.2 CCC(CC1=CNC2=C1C=C(C=C2)Cl)N
CHEMBL210484 5ht2a_human Human No 7.6 EC50 = 25 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 7 1.8 CC1CC2CNCC2N1C3=NC=CC(=N3)C(F)(F)F
CHEMBL210484 5ht2a_human Human No 7.6 EC50 = 25 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 7 1.8 CC1CC2CNCC2N1C3=NC=CC(=N3)C(F)(F)F
CHEMBL178365 5ht2a_human Human Yes 6.6 EC50 = 251.2 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL253809 5ht2a_human Human No 6.6 EC50 = 251.2 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
210 1 1 1 3.1 CCC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL361742 5ht2a_human Human Yes 6.6 EC50 = 251.2 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 2.1 CC1CNCCC2=C1C=C(C=C2)OC
CHEMBL178365 5ht2a_human Human Yes 6.6 EC50 = 251.2 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL253809 5ht2a_human Human No 6.6 EC50 = 251.2 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
210 1 1 1 3.1 CCC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL361742 5ht2a_human Human Yes 6.6 EC50 = 251.2 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 2.1 CC1CNCCC2=C1C=C(C=C2)OC
CHEMBL178566 5ht2a_human Human Yes 5.6 EC50 = 2511.9 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
230 0 1 1 3.4 CC1CNCCC2=C1C(=C(C=C2)Cl)Cl
CHEMBL178566 5ht2a_human Human Yes 5.6 EC50 = 2511.9 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
230 0 1 1 3.4 CC1CNCCC2=C1C(=C(C=C2)Cl)Cl
CHEMBL570937 5ht2a_human Human No 6.6 EC50 = 254 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
335 5 1 4 1.1 C1CN(CCN1)C2=NN(C(=O)C=C2)CCOC3=CC=CC=C3Cl
CHEMBL570937 5ht2a_human Human No 6.6 EC50 = 254 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
335 5 1 4 1.1 C1CN(CCN1)C2=NN(C(=O)C=C2)CCOC3=CC=CC=C3Cl
CHEMBL482702 5ht2a_rat Rat Yes 6.6 EC50 = 258 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
326 2 1 3 3.1 CC(CC1=C2CCCOC2=C(C3=C1OCCC3)Br)N
CHEMBL360328 5ht2a_human Human Yes 6.6 EC50 = 258 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL482702 5ht2a_rat Rat Yes 6.6 EC50 = 258 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
326 2 1 3 3.1 CC(CC1=C2CCCOC2=C(C3=C1OCCC3)Br)N
CHEMBL394508 5ht2a_rat Rat No 7.6 EC50 = 26 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 6 1 5 1.8 CC(CC1=C2C(=C(C3=C1CCO3)CCC(=O)OC)CCO2)N
CHEMBL394508 5ht2a_rat Rat No 7.6 EC50 = 26 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 6 1 5 1.8 CC(CC1=C2C(=C(C3=C1CCO3)CCC(=O)OC)CCO2)N
CHEMBL181172 5ht2a_human Human Yes 6.6 EC50 = 260 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL143031 5ht2a_rat Rat No 5.6 EC50 = 2600 Funct
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 3 2.1 CN(C)CCC1=CNC2=CC(=CC(=C21)O)F
CHEMBL1643854 5ht2a_human Human No 5.6 EC50 = 2634 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 6 2.2 COC1=CC=C(C=C1)OC2CN(C2)C3=C4CCNCCC4=NC5=CC=NN53
CHEMBL1643854 5ht2a_human Human No 5.6 EC50 = 2634 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 6 2.2 COC1=CC=C(C=C1)OC2CN(C2)C3=C4CCNCCC4=NC5=CC=NN53
CHEMBL178365 5ht2a_human Human Yes 6.6 EC50 = 265 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL1643679 5ht2a_human Human No 5.6 EC50 = 2676 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 6 2.2 COC1=CC=CC=C1OC2CN(C2)C3=C4CCNCCC4=NC5=CC=NN53
CHEMBL1643679 5ht2a_human Human No 5.6 EC50 = 2676 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 6 2.2 COC1=CC=CC=C1OC2CN(C2)C3=C4CCNCCC4=NC5=CC=NN53
CHEMBL355474 5ht2a_human Human No 6.6 EC50 = 269 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 2.1 CC1CCC2=C3N1C=C(C3=CC(=C2)F)CCN
CHEMBL292821 5ht2a_rat Rat Yes 7.6 EC50 = 27 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
260 4 1 3 2.1 COC1=CC(=C(C=C1CCN)OC)Br
CHEMBL292821 5ht2a_rat Rat Yes 7.6 EC50 = 27 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
260 4 1 3 2.1 COC1=CC(=C(C=C1CCN)OC)Br
CHEMBL2391541 5ht2a_human Human Yes 7.6 EC50 = 27.5 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 2.8 COC1=CC2=C(C=C1)NC=C2CCN(CC=C)CC=C
CHEMBL134519 5ht2a_rat Rat Yes 7.6 EC50 = 27.7 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 2.5 CC(CC1=CC(=C(C=C1OC)I)OC)N
CHEMBL382635 5ht2a_human Human Yes 7.6 EC50 = 28.1 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 2 1.6 C1=CC2=C(C(=C1)F)C(=CN2)CCN
CHEMBL382635 5ht2a_human Human Yes 7.6 EC50 = 28.1 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 2 1.6 C1=CC2=C(C(=C1)F)C(=CN2)CCN
CHEMBL31115 5ht2a_rat Rat Yes 6.6 EC50 = 285 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 1.0 CC(CC1=CNC2=C1C=C(C=C2)OC)N
CHEMBL220211 5ht2a_human Human No 6.5 EC50 = 289 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 6 1.2 COC1=CC(=C2C(=C1)C3CNCCN3C2=O)C(F)(F)F
CHEMBL220211 5ht2a_human Human No 6.5 EC50 = 289 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 6 1.2 COC1=CC(=C2C(=C1)C3CNCCN3C2=O)C(F)(F)F
CHEMBL135076 5ht2a_rat Rat No 6.5 EC50 = 292 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 2.2 CC(CC1=CNC2=C1C3=C(C=C2)OCCC3)N
CHEMBL1643678 5ht2a_human Human No 8.5 EC50 = 3 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 2.3 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC=C(C=C5)F
CHEMBL1643678 5ht2a_human Human No 8.5 EC50 = 3 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 2.3 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC=C(C=C5)F
CHEMBL394325 5ht2a_rat Rat No 8.4 EC50 = 3.6 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 2.1 CC(CC1=C2C=COC2=C(C3=C1OC=C3)COC)N
CHEMBL394325 5ht2a_rat Rat No 8.4 EC50 = 3.6 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 2.1 CC(CC1=C2C=COC2=C(C3=C1OC=C3)COC)N
CHEMBL182184 5ht2a_human Human No 7.5 EC50 = 30 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
270 1 1 2 2.8 CC1CNCCC2=CC(=C(C=C12)Br)OC
CHEMBL102347 5ht2a_rat Rat Yes 5.5 EC50 = 3000 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 1.2 COC1=C(C2=C(CCO2)C(=C1)CCN)OC
CHEMBL360328 5ht2a_human Human Yes 6.5 EC50 = 302 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL360328 5ht2a_human Human Yes 6.5 EC50 = 302 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL572228 5ht2a_human Human No 6.5 EC50 = 308 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
319 5 1 5 2.5 C1CN(CCN1)C2=CN=CC(=N2)OCCC3=CC=CC=C3Cl
CHEMBL572228 5ht2a_human Human No 6.5 EC50 = 308 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
319 5 1 5 2.5 C1CN(CCN1)C2=CN=CC(=N2)OCCC3=CC=CC=C3Cl
CHEMBL400600 5ht2a_human Human No 7.5 EC50 = 31.6 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 1 1 2 2.7 CC1CNCCC2=CC(=C(C=C12)Cl)OC
CHEMBL400600 5ht2a_human Human No 7.5 EC50 = 31.6 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 1 1 2 2.7 CC1CNCCC2=CC(=C(C=C12)Cl)OC
CHEMBL253810 5ht2a_human Human No 6.5 EC50 = 316.2 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
210 1 1 1 3.1 CCC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL253810 5ht2a_human Human No 6.5 EC50 = 316.2 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
210 1 1 1 3.1 CCC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL492301 5ht2a_human Human No 7.5 EC50 = 32 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
421 4 1 5 3.8 C1CN(CCC1OC2=CC=CC=C2Cl)S(=O)(=O)C3=CC4=C(CCNCC4)C=C3
CHEMBL1643677 5ht2a_human Human No 7.5 EC50 = 32 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 2.3 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC(=CC=C5)F
CHEMBL201930 5ht2a_human Human Yes 7.5 EC50 = 32 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
225 2 1 2 1.7 CC(CN1C=CC2=C1C3=C(C=C2)N=CC=C3)N
CHEMBL198124 5ht2a_human Human Yes 7.5 EC50 = 32 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 2 3.1 CCCCN1C=C(C2=C1C=CC=C2O)CCN(C)C
CHEMBL492301 5ht2a_human Human No 7.5 EC50 = 32 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
421 4 1 5 3.8 C1CN(CCC1OC2=CC=CC=C2Cl)S(=O)(=O)C3=CC4=C(CCNCC4)C=C3
CHEMBL1643677 5ht2a_human Human No 7.5 EC50 = 32 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 2.3 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC(=CC=C5)F
CHEMBL201930 5ht2a_human Human Yes 7.5 EC50 = 32 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
225 2 1 2 1.7 CC(CN1C=CC2=C1C3=C(C=C2)N=CC=C3)N
CHEMBL198124 5ht2a_human Human Yes 7.5 EC50 = 32 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 2 3.1 CCCCN1C=C(C2=C1C=CC=C2O)CCN(C)C
CHEMBL391196 5ht2a_rat Rat No 7.5 EC50 = 32.7 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
314 2 2 4 1.3 CC(C(C1=C2CCOC2=C(C3=C1OCC3)Br)O)N
CHEMBL391196 5ht2a_rat Rat No 7.5 EC50 = 32.7 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
314 2 2 4 1.3 CC(C(C1=C2CCOC2=C(C3=C1OCC3)Br)O)N
CHEMBL379780 5ht2a_rat Rat Yes 5.5 EC50 = 3200 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 1.3 COC1=C(C(=C2CCC(C2=C1)CN)OC)OC
CHEMBL379780 5ht2a_rat Rat Yes 5.5 EC50 = 3200 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 1.3 COC1=C(C(=C2CCC(C2=C1)CN)OC)OC
CHEMBL223466 5ht2a_human Human No 5.5 EC50 = 3280 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
251 1 1 2 1.8 CCC1=C2C3CNCCN3C(=O)C2=C(C=C1)Cl
CHEMBL223466 5ht2a_human Human No 5.5 EC50 = 3280 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
251 1 1 2 1.8 CCC1=C2C3CNCCN3C(=O)C2=C(C=C1)Cl
CHEMBL393077 5ht2a_rat Rat No 7.5 EC50 = 33 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 1.6 CC(CC1=C2C=COC2=C(C3=C1OC=C3)CO)N
CHEMBL393077 5ht2a_rat Rat No 7.5 EC50 = 33 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 1.6 CC(CC1=C2C=COC2=C(C3=C1OC=C3)CO)N
CHEMBL3589596 5ht2a_human Human No 7.5 EC50 = 33.9 Funct
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
396 8 2 5 4.0 COC1=CC=CC(=C1O)CNCCC2=CC(=C(C=C2OC)Br)OC
CHEMBL3589596 5ht2a_human Human No 7.5 EC50 = 33.9 Funct
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
396 8 2 5 4.0 COC1=CC=CC(=C1O)CNCCC2=CC(=C(C=C2OC)Br)OC
CHEMBL444612 5ht2a_rat Rat Yes 4.5 EC50 = 33900 Funct
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 2 3.6 CCN(CC)CCC1=CNC2=C1C=CC(=C2)F
CHEMBL331864 5ht2a_rat Rat No 6.5 EC50 = 340 Funct
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
298 2 1 3 2.0 COC1=CC(=C2C3=C1C(CCC3CO2)CN)Br
CHEMBL1770373 5ht2a_canlf Dog Yes 5.5 EC50 = 3400 Funct
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 2.1 C1CNCCC2=NC(=NC=C21)CC3=CC=CC=C3
CHEMBL1770373 5ht2a_canlf Dog Yes 5.5 EC50 = 3400 Funct
Agonist activity at 5HT2A receptor in dog femoral arteryAgonist activity at 5HT2A receptor in dog femoral artery
239 2 1 3 2.1 C1CNCCC2=NC(=NC=C21)CC3=CC=CC=C3
CHEMBL1770373 5ht2a_canlf Dog Yes 5.5 EC50 = 3400 Funct
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 2.1 C1CNCCC2=NC(=NC=C21)CC3=CC=CC=C3
CHEMBL1770373 5ht2a_canlf Dog Yes 5.5 EC50 = 3400 Funct
Agonist activity at 5HT2A receptor in dog femoral arteryAgonist activity at 5HT2A receptor in dog femoral artery
239 2 1 3 2.1 C1CNCCC2=NC(=NC=C21)CC3=CC=CC=C3
CHEMBL194378 5ht2a_human Human Yes 5.5 EC50 = 3475 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 5 -1.6 CN(C)CCC1=CNC2=C1C(=CC=C2)OP(=O)(O)O
CHEMBL194378 5ht2a_human Human Yes 5.5 EC50 = 3475 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 5 -1.6 CN(C)CCC1=CNC2=C1C(=CC=C2)OP(=O)(O)O
CHEMBL172159 5ht2a_human Human No 6.5 EC50 = 348 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
253 2 1 2 2.2 C1CSC2=C3N1C=C(C3=CC(=C2)Cl)CCN
CHEMBL202458 5ht2a_human Human No 6.5 EC50 = 359 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
359 5 1 4 3.5 CC(CN1C=CC2=C1C3=C(C=C2)N=CC=C3)NCC4=CC5=C(C=C4)OCO5
CHEMBL202458 5ht2a_human Human No 6.5 EC50 = 359 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
359 5 1 4 3.5 CC(CN1C=CC2=C1C3=C(C=C2)N=CC=C3)NCC4=CC5=C(C=C4)OCO5
CHEMBL212197 5ht2a_rat Rat Yes 7.4 EC50 = 36 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
272 3 1 3 0.4 COC1=CC(=C(C2=C1C(C2)CN)OC)Br
CHEMBL201454 5ht2a_human Human No 7.4 EC50 = 36 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
260 2 1 2 2.3 CC(CN1C=CC2=CC(=C3C(=C21)C=CC=N3)Cl)N
CHEMBL212197 5ht2a_rat Rat Yes 7.4 EC50 = 36 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
272 3 1 3 0.4 COC1=CC(=C(C2=C1C(C2)CN)OC)Br
CHEMBL201454 5ht2a_human Human No 7.4 EC50 = 36 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
260 2 1 2 2.3 CC(CN1C=CC2=CC(=C3C(=C21)C=CC=N3)Cl)N
CHEMBL80366 5ht2a_human Human No 6.4 EC50 = 367 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
229 2 1 3 2.3 CC(CN1CCC2=CC(=C(C=C21)Cl)F)N
CHEMBL2397897 5ht2a_human Human No 7.4 EC50 = 37 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 1.6 CCC1=CC2=C(CC3CNCCN3C2=O)C=C1
CHEMBL376676 5ht2a_human Human No 6.4 EC50 = 370 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 5 1.7 CC1CNCC2N1C(=O)C3=C2C=CC=C3C(F)(F)F
CHEMBL376676 5ht2a_human Human No 6.4 EC50 = 370 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 5 1.7 CC1CNCC2N1C(=O)C3=C2C=CC=C3C(F)(F)F
CHEMBL374436 5ht2a_human Human No 6.4 EC50 = 374 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 1.1 CCC1=C(C=C2C(=C1)C3CNCCN3C2=O)OC
CHEMBL374436 5ht2a_human Human No 6.4 EC50 = 374 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 1.1 CCC1=C(C=C2C(=C1)C3CNCCN3C2=O)OC
CHEMBL80862 5ht2a_human Human No 6.4 EC50 = 378 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 2.4 CCSC1=CC2=C(CCN2CC(C)N)C=C1
CHEMBL3330640 5ht2a_human Human Yes 7.4 EC50 = 38.3 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 2.4 CCNCCC1=CNC2=CC=CC=C21
CHEMBL3330640 5ht2a_human Human Yes 7.4 EC50 = 38.3 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 2.4 CCNCCC1=CNC2=CC=CC=C21
CHEMBL2397893 5ht2a_human Human No 6.4 EC50 = 381 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
237 0 1 2 1.5 C1CN2C(CC3=C(C2=O)C(=CC=C3)Cl)CN1
CHEMBL1288716 5ht2a_human Human Yes 8.4 EC50 = 4.1 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
195 2 2 1 1.2 C1=CC2=C(C=C1Cl)C(=CN2)CCN
CHEMBL1288716 5ht2a_human Human Yes 8.4 EC50 = 4.1 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
195 2 2 1 1.2 C1=CC2=C(C=C1Cl)C(=CN2)CCN
CHEMBL381160 5ht2a_human Human Yes 8.3 EC50 = 4.6 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 2 1.9 C1=CC2=C(C=C1F)NC=C2CCN
CHEMBL381160 5ht2a_human Human Yes 8.3 EC50 = 4.6 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 2 1.9 C1=CC2=C(C=C1F)NC=C2CCN
CHEMBL3589582 5ht2a_human Human No 8.3 EC50 = 4.6 Funct
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
392 7 1 4 3.9 COC1=CC(=C(C=C1CCNCC2=CC=CC3=C2OCC3)OC)Br
CHEMBL3589582 5ht2a_human Human No 8.3 EC50 = 4.6 Funct
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
392 7 1 4 3.9 COC1=CC(=C(C=C1CCNCC2=CC=CC3=C2OCC3)OC)Br
CHEMBL1643853 5ht2a_human Human No 7.4 EC50 = 40 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 6 2.2 COC1=CC=CC(=C1)OC2CN(C2)C3=C4CCNCCC4=NC5=CC=NN53
CHEMBL210215 5ht2a_human Human No 7.4 EC50 = 40 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 7 1.8 CC1CC2CNCC2N1C3=NC=CC(=N3)C(F)(F)F
CHEMBL1643853 5ht2a_human Human No 7.4 EC50 = 40 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 6 2.2 COC1=CC=CC(=C1)OC2CN(C2)C3=C4CCNCCC4=NC5=CC=NN53
CHEMBL210215 5ht2a_human Human No 7.4 EC50 = 40 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 7 1.8 CC1CC2CNCC2N1C3=NC=CC(=N3)C(F)(F)F
CHEMBL76781 5ht2a_human Human Yes 6.4 EC50 = 400 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
227 2 1 2 2.2 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N
CHEMBL76781 5ht2a_human Human Yes 6.4 EC50 = 400 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
227 2 1 2 2.2 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N
CHEMBL319415 5ht2a_rat Rat Yes 5.4 EC50 = 4000 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 1.2 CCOC1=C(C=C(C=C1OC)CCN)OC
CHEMBL570274 5ht2a_human Human No 7.4 EC50 = 41 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 7 1.8 CC1CNCCN1C2=NN(C(=O)C=C2)CCOC3=CC=CC=C3C(F)(F)F
CHEMBL570274 5ht2a_human Human No 7.4 EC50 = 41 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 7 1.8 CC1CNCCN1C2=NN(C(=O)C=C2)CCOC3=CC=CC=C3C(F)(F)F
CHEMBL209254 5ht2a_human Human No 6.4 EC50 = 416 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
223 1 1 2 2.5 C1CN(C2C1CNC2)C3=CC(=CC=C3)Cl
CHEMBL209254 5ht2a_human Human No 6.4 EC50 = 416 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
223 1 1 2 2.5 C1CN(C2C1CNC2)C3=CC(=CC=C3)Cl
CHEMBL179915 5ht2a_human Human No 7.4 EC50 = 42 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 5 3.0 CC1CNCCC2=CC(=C(C=C12)C(F)(F)F)OC
CHEMBL371300 5ht2a_rat Rat Yes 7.4 EC50 = 42.7 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 0.1 CC(CN1C2=CC(=O)C=CC2=CN1)N
CHEMBL371300 5ht2a_rat Rat Yes 7.4 EC50 = 42.7 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 0.1 CC(CN1C2=CC(=O)C=CC2=CN1)N
CHEMBL76301 5ht2a_human Human No 6.4 EC50 = 432 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 3 2.3 CC(CN1CCC2=CC(=C(C=C21)I)F)N
CHEMBL204839 5ht2a_human Human Yes 7.4 EC50 = 44.7 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 1.7 CC1=CC=CC2=C1NC=C2CCN
CHEMBL204839 5ht2a_human Human Yes 7.4 EC50 = 44.7 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 1.7 CC1=CC=CC2=C1NC=C2CCN
CHEMBL1091105 5ht2a_human Human Yes 6.4 EC50 = 440 Funct
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
378 6 2 5 3.7 CC1(CCC(CC1)OC2=C(C=C(C(=C2)OC)CNC(=O)C3CCCN3)F)C
CHEMBL1091105 5ht2a_human Human Yes 6.4 EC50 = 440 Funct
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
378 6 2 5 3.7 CC1(CCC(CC1)OC2=C(C=C(C(=C2)OC)CNC(=O)C3CCCN3)F)C
CHEMBL201062 5ht2a_human Human No 6.4 EC50 = 446 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
225 2 1 2 1.7 CC(CN1C=CC2=C1C3=C(C=CC=N3)C=C2)N
CHEMBL201062 5ht2a_human Human No 6.4 EC50 = 446 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
225 2 1 2 1.7 CC(CN1C=CC2=C1C3=C(C=CC=N3)C=C2)N
CHEMBL223628 5ht2a_human Human No 6.4 EC50 = 449 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 1.1 CC(C)OC1=CC=CC2=C1C(=O)N3C2CNCC3
CHEMBL223628 5ht2a_human Human No 6.4 EC50 = 449 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 1.1 CC(C)OC1=CC=CC2=C1C(=O)N3C2CNCC3
CHEMBL215781 5ht2a_rat Rat No 6.3 EC50 = 460 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
272 3 1 3 0.4 COC1=CC(=C(C2=C1C(C2)CN)OC)Br
CHEMBL215781 5ht2a_rat Rat No 6.3 EC50 = 460 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
272 3 1 3 0.4 COC1=CC(=C(C2=C1C(C2)CN)OC)Br
CHEMBL2397878 5ht2a_human Human No 7.3 EC50 = 47 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 0.8 COC1=CC2=C(CC3CNCCN3C2=O)C=C1
CHEMBL31115 5ht2a_rat Rat Yes 7.3 EC50 = 47.5 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 1.0 CC(CC1=CNC2=C1C=C(C=C2)OC)N
CHEMBL31115 5ht2a_rat Rat Yes 7.3 EC50 = 47.5 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 1.0 CC(CC1=CNC2=C1C=C(C=C2)OC)N
CHEMBL201897 5ht2a_human Human No 6.3 EC50 = 473 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
225 2 1 2 1.6 CC(CN1C=CC2=C1C3=C(C=C2)C=CN=C3)N
CHEMBL201897 5ht2a_human Human No 6.3 EC50 = 473 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
225 2 1 2 1.6 CC(CN1C=CC2=C1C3=C(C=C2)C=CN=C3)N
CHEMBL234837 5ht2a_rat Rat No 7.3 EC50 = 49.2 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 2.3 CC1=NOC(=N1)CC2=C3CCOC3=C(C4=C2OCC4)CC(C)N
CHEMBL234837 5ht2a_rat Rat No 7.3 EC50 = 49.2 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 2.3 CC1=NOC(=N1)CC2=C3CCOC3=C(C4=C2OCC4)CC(C)N
CHEMBL142368 5ht2a_rat Rat No 5.3 EC50 = 4920 Funct
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 3 2.1 CN(C)CCC1=CNC2=C(C=CC(=C12)O)F
CHEMBL3330644 5ht2a_human Human Yes 6.3 EC50 = 496 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 1.3 COC1=CC=CC2=C1NC=C2CCN
CHEMBL3330644 5ht2a_human Human Yes 6.3 EC50 = 496 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 1.3 COC1=CC=CC2=C1NC=C2CCN
CHEMBL232997 5ht2a_rat Rat No 5.3 EC50 = 4970 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 5 -1.1 CC(CC1=C2C(=C(C3=C1CCO3)CC(=O)O)CCO2)N
CHEMBL232997 5ht2a_rat Rat No 5.3 EC50 = 4970 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 5 -1.1 CC(CC1=C2C(=C(C3=C1CCO3)CC(=O)O)CCO2)N
CHEMBL1288717 5ht2a_human Human Yes 8.3 EC50 = 5.1 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
239 2 2 1 1.3 C1=CC2=C(C=C1Br)C(=CN2)CCN
CHEMBL1288717 5ht2a_human Human Yes 8.3 EC50 = 5.1 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
239 2 2 1 1.3 C1=CC2=C(C=C1Br)C(=CN2)CCN
CHEMBL76781 5ht2a_human Human Yes 7.3 EC50 = 50.1 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
227 2 1 2 2.2 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N
CHEMBL76781 5ht2a_human Human Yes 7.3 EC50 = 50.1 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
227 2 1 2 2.2 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N
CHEMBL348588 5ht2a_human Human Yes 7.3 EC50 = 50.7 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 2.1 CNCCC1=CNC2=CC=CC=C21
CHEMBL348588 5ht2a_human Human Yes 7.3 EC50 = 50.7 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 2.1 CNCCC1=CNC2=CC=CC=C21
CHEMBL1093699 5ht2a_human Human No 6.3 EC50 = 500 Funct
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
364 7 2 5 3.6 COC1=CC(=C(C=C1CNC(=O)C2CCCN2)F)OCC3CCCCC3
CHEMBL1093699 5ht2a_human Human No 6.3 EC50 = 500 Funct
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
364 7 2 5 3.6 COC1=CC(=C(C=C1CNC(=O)C2CCCN2)F)OCC3CCCCC3
CHEMBL440752 5ht2a_human Human Yes 6.3 EC50 = 501.2 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
240 0 1 1 2.8 CC1CNCCC2=C1C=C(C=C2)Br
CHEMBL440752 5ht2a_human Human Yes 6.3 EC50 = 501.2 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
240 0 1 1 2.8 CC1CNCCC2=C1C=C(C=C2)Br
CHEMBL363772 5ht2a_rat Rat No 5.3 EC50 = 5040 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
304 5 1 4 1.7 CC(C(C1=CC(=C(C=C1OC)Br)OC)OC)N
CHEMBL363772 5ht2a_rat Rat No 5.3 EC50 = 5040 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
304 5 1 4 1.7 CC(C(C1=CC(=C(C=C1OC)Br)OC)OC)N
CHEMBL440752 5ht2a_human Human Yes 6.3 EC50 = 510 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
240 0 1 1 2.8 CC1CNCCC2=C1C=C(C=C2)Br
CHEMBL375170 5ht2a_human Human No 6.3 EC50 = 513 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 5 2.1 C1CC1C2=CC3=C(C(=C2)C(F)(F)F)C(=O)N4C3CNCC4
CHEMBL375170 5ht2a_human Human No 6.3 EC50 = 513 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 5 2.1 C1CC1C2=CC3=C(C(=C2)C(F)(F)F)C(=O)N4C3CNCC4
CHEMBL1643855 5ht2a_human Human No 5.3 EC50 = 5165 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 6 1.5 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC=CC=N5
CHEMBL1643855 5ht2a_human Human No 5.3 EC50 = 5165 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 6 1.5 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC=CC=N5
CHEMBL2397896 5ht2a_human Human No 7.3 EC50 = 53 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 1.2 CC1=CC2=C(CC3CNCCN3C2=O)C=C1
CHEMBL142936 5ht2a_rat Rat Yes 5.3 EC50 = 5370 Funct
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 3.3 CCN(CC)CCC1=CNC2=CC=CC=C21
CHEMBL3589594 5ht2a_human Human No 5.3 EC50 = 5370.3 Funct
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
410 9 1 5 4.1 COC1=C(C(=CC=C1)OC)CNCCC2=CC(=C(C=C2OC)Br)OC
CHEMBL3589594 5ht2a_human Human No 5.3 EC50 = 5370.3 Funct
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
410 9 1 5 4.1 COC1=C(C(=CC=C1)OC)CNCCC2=CC(=C(C=C2OC)Br)OC
CHEMBL199775 5ht2a_rat Rat Yes 7.3 EC50 = 54 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 3 1.0 CC(CN1C2=C(C=CC(=C2)OC)C=N1)N
CHEMBL199775 5ht2a_rat Rat Yes 7.3 EC50 = 54 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 3 1.0 CC(CN1C2=C(C=CC(=C2)OC)C=N1)N
CHEMBL2331807 5ht2a_human Human No 6.3 EC50 = 549.5 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 3 1.3 C1CNCCC2=C1C(=O)N(O2)CC3=CC=CC=C3
CHEMBL2113264 5ht2a_human Human No 7.3 EC50 = 56 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 5 2.6 CC(C)C1CNCC2N1C(=O)C3=C2C=CC=C3C(F)(F)F
CHEMBL2113264 5ht2a_human Human No 7.3 EC50 = 56 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 5 2.6 CC(C)C1CNCC2N1C(=O)C3=C2C=CC=C3C(F)(F)F
CHEMBL593545 5ht2a_human Human No 6.2 EC50 = 578 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
344 3 1 4 3.6 C1CC(C2=C(C1)C=CC(=N2)N3CCNCC3)OC4=CC=CC=C4Cl
CHEMBL593545 5ht2a_human Human No 6.2 EC50 = 578 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
344 3 1 4 3.6 C1CC(C2=C(C1)C=CC(=N2)N3CCNCC3)OC4=CC=CC=C4Cl
CHEMBL197653 5ht2a_rat Rat Yes 7.2 EC50 = 58.1 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 5 0.5 CC(CN1C2=C(C(=O)C=CC2=CN1)F)N
CHEMBL197653 5ht2a_rat Rat Yes 7.2 EC50 = 58.1 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 5 0.5 CC(CN1C2=C(C(=O)C=CC2=CN1)F)N
CHEMBL1643672 5ht2a_human Human No 6.2 EC50 = 585 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 4 1.5 C1CCN(CC1)C2=C3CCNCCC3=NC4=CC=NN42
CHEMBL1643672 5ht2a_human Human No 6.2 EC50 = 585 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 4 1.5 C1CCN(CC1)C2=C3CCNCCC3=NC4=CC=NN42
CHEMBL373245 5ht2a_rat Rat Yes 7.2 EC50 = 59.7 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
226 2 2 4 1.0 CC(CN1C2=C(C(=O)C=CC2=CN1)Cl)N
CHEMBL373245 5ht2a_rat Rat Yes 7.2 EC50 = 59.7 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
226 2 2 4 1.0 CC(CN1C2=C(C(=O)C=CC2=CN1)Cl)N
CHEMBL331241 5ht2a_human Human Yes 8.2 EC50 = 6 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 1.9 CC1=CC2=C(C=C1)NC=C2CCN
CHEMBL331241 5ht2a_human Human Yes 8.2 EC50 = 6 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 1.9 CC1=CC2=C(C=C1)NC=C2CCN
CHEMBL232995 5ht2a_rat Rat No 8.2 EC50 = 6.2 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 8 1 6 2.8 CC(CC1=C2CCOC2=C(C3=C1OCC3)COCC(=O)OC4=CC=CC=C4)N
CHEMBL232995 5ht2a_rat Rat No 8.2 EC50 = 6.2 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 8 1 6 2.8 CC(CC1=C2CCOC2=C(C3=C1OCC3)COCC(=O)OC4=CC=CC=C4)N
CHEMBL1906905 5ht2a_human Human Yes 8.2 EC50 = 6.3 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
209 2 2 1 1.6 CC(CC1=CNC2=C1C=C(C=C2)Cl)N
CHEMBL1906905 5ht2a_human Human Yes 8.2 EC50 = 6.3 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
209 2 2 1 1.6 CC(CC1=CNC2=C1C=C(C=C2)Cl)N
CHEMBL76307 5ht2a_human Human No 6.2 EC50 = 602 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
211 2 1 2 2.2 CC(CN1CCC2=C1C=C(C=C2)Cl)N
CHEMBL179378 5ht2a_human Human Yes 7.2 EC50 = 61 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 2.7 CC1CNCCC2=CC(=C(C=C12)I)OC
CHEMBL211309 5ht2a_rat Rat Yes 5.2 EC50 = 6100 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 1.3 COC1=C(C(=C2CCC(C2=C1)CN)OC)OC
CHEMBL211309 5ht2a_rat Rat Yes 5.2 EC50 = 6100 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 1.3 COC1=C(C(=C2CCC(C2=C1)CN)OC)OC
CHEMBL360328 5ht2a_human Human Yes 6.2 EC50 = 616 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL360328 5ht2a_human Human Yes 6.2 EC50 = 616 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
196 0 1 1 2.7 CC1CNCCC2=C1C=C(C=C2)Cl
CHEMBL77880 5ht2a_human Human Yes 7.2 EC50 = 62 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
218 2 1 3 1.6 CC(CN1CCC2=C1C3=C(C=C2)OCC3)N
CHEMBL1643856 5ht2a_human Human No 7.2 EC50 = 63 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 6 1.1 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CN=CC=C5
CHEMBL1643856 5ht2a_human Human No 7.2 EC50 = 63 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 6 1.1 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CN=CC=C5
CHEMBL178313 5ht2a_human Human No 7.2 EC50 = 63 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
256 0 2 2 2.5 CC1CNCCC2=CC(=C(C=C12)Br)O
CHEMBL181787 5ht2a_human Human No 7.2 EC50 = 63.1 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 1 1 2 2.7 CC1CNCCC2=CC(=C(C=C12)Cl)OC
CHEMBL360492 5ht2a_human Human No 7.2 EC50 = 63.1 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
214 0 1 2 2.8 CC1CNCCC2=CC(=C(C=C12)Cl)F
CHEMBL181787 5ht2a_human Human No 7.2 EC50 = 63.1 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 1 1 2 2.7 CC1CNCCC2=CC(=C(C=C12)Cl)OC
CHEMBL360492 5ht2a_human Human No 7.2 EC50 = 63.1 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
214 0 1 2 2.8 CC1CNCCC2=CC(=C(C=C12)Cl)F
CHEMBL594717 5ht2a_human Human No 6.2 EC50 = 630 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
355 4 1 5 3.2 CC1CNCCN1C2=NC3=C(CCC3OCC4=C(C=CC(=C4)F)C)C=C2
CHEMBL594717 5ht2a_human Human No 6.2 EC50 = 630 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
355 4 1 5 3.2 CC1CNCCN1C2=NC3=C(CCC3OCC4=C(C=CC(=C4)F)C)C=C2
CHEMBL197664 5ht2a_human Human Yes 6.2 EC50 = 633 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
218 3 1 2 1.9 CN1C=C(C2=C1C=CC=C2O)CCN(C)C
CHEMBL197664 5ht2a_human Human Yes 6.2 EC50 = 633 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
218 3 1 2 1.9 CN1C=C(C2=C1C=CC=C2O)CCN(C)C
CHEMBL202538 5ht2a_human Human No 6.2 EC50 = 638 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
350 5 1 2 4.3 CC(CN1C=CC2=C1C3=C(C=C2)N=CC=C3)NCC4=CC=CC=C4Cl
CHEMBL202538 5ht2a_human Human No 6.2 EC50 = 638 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
350 5 1 2 4.3 CC(CN1C=CC2=C1C3=C(C=C2)N=CC=C3)NCC4=CC=CC=C4Cl
CHEMBL2397889 5ht2a_human Human No 7.2 EC50 = 64 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 1.2 CC1=CC=CC2=C1C(=O)N3CCNCC3C2
CHEMBL89738 5ht2a_human Human No 4.2 EC50 = 64000 Funct
Effective concentration against human 5-hydroxytryptamine 2A receptor in CHO cells using 8-OH-DPA radioligandEffective concentration against human 5-hydroxytryptamine 2A receptor in CHO cells using 8-OH-DPA radioligand
254 0 1 1 3.4 C1CCCC2=C(CC1)C3=C4N2CCNCC4=CC=C3
CHEMBL1643676 5ht2a_human Human No 6.2 EC50 = 648 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 2.3 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC=CC=C5F
CHEMBL1643676 5ht2a_human Human No 6.2 EC50 = 648 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 2.3 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC=CC=C5F
CHEMBL572252 5ht2a_human Human No 7.2 EC50 = 65 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
349 5 1 4 1.5 CC(COC1=CC=CC=C1Cl)N2C(=O)C=CC(=N2)N3CCNCC3
CHEMBL572252 5ht2a_human Human No 7.2 EC50 = 65 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
349 5 1 4 1.5 CC(COC1=CC=CC=C1Cl)N2C(=O)C=CC(=N2)N3CCNCC3
CHEMBL412876 5ht2a_rat Rat Yes 6.2 EC50 = 660 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 3 1 2 2.7 CN(C)CCC1=CNC2=C1C3=C(C=C2)OCCC3
CHEMBL1770373 5ht2a_human Human Yes 7.2 EC50 = 68 Funct
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
239 2 1 3 2.1 C1CNCCC2=NC(=NC=C21)CC3=CC=CC=C3
CHEMBL1770373 5ht2a_human Human Yes 7.2 EC50 = 68 Funct
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
239 2 1 3 2.1 C1CNCCC2=NC(=NC=C21)CC3=CC=CC=C3
CHEMBL6620 5ht2a_rat Rat Yes 7.2 EC50 = 68.4 Funct
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
263 4 1 6 2.8 CC(CC1=CC(=C(C=C1OC)C(F)(F)F)OC)N
CHEMBL595194 5ht2a_human Human No 7.2 EC50 = 70 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
344 3 1 4 3.6 C1CC(C2=C(C1)C=CC(=N2)N3CCNCC3)OC4=CC=CC=C4Cl
CHEMBL590580 5ht2a_human Human No 7.2 EC50 = 70 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
231 0 2 3 1.3 CC1=C2C(=CC=C1)N3CCNCCC3NC2=O
CHEMBL595194 5ht2a_human Human No 7.2 EC50 = 70 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
344 3 1 4 3.6 C1CC(C2=C(C1)C=CC(=N2)N3CCNCC3)OC4=CC=CC=C4Cl
CHEMBL590580 5ht2a_human Human No 7.2 EC50 = 70 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
231 0 2 3 1.3 CC1=C2C(=CC=C1)N3CCNCCC3NC2=O
CHEMBL2397881 5ht2a_human Human No 6.2 EC50 = 707 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
202 0 1 2 0.8 C1CN2C(CC3=CC=CC=C3C2=O)CN1
CHEMBL397321 5ht2a_rat Rat No 7.2 EC50 = 71 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
307 7 1 5 1.2 CC(CC1=C2CCOC2=C(C3=C1OCC3)COCCOC)N
CHEMBL397321 5ht2a_rat Rat No 7.2 EC50 = 71 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
307 7 1 5 1.2 CC(CC1=C2CCOC2=C(C3=C1OCC3)COCCOC)N
CHEMBL309760 5ht2a_human Human Yes 6.1 EC50 = 719 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
255 2 1 2 2.3 CC(CN1CCC2=C1C=C(C=C2)Br)N
CHEMBL360492 5ht2a_human Human No 7.1 EC50 = 72 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
214 0 1 2 2.8 CC1CNCCC2=CC(=C(C=C12)Cl)F
CHEMBL199385 5ht2a_rat Rat Yes 7.1 EC50 = 74.4 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
177 2 2 4 -0.3 C1=CC2=CNN(C2=CC1=O)CCN
CHEMBL199385 5ht2a_rat Rat Yes 7.1 EC50 = 74.4 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
177 2 2 4 -0.3 C1=CC2=CNN(C2=CC1=O)CCN
CHEMBL6737 5ht2a_rat Rat No 6.1 EC50 = 740 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
195 4 1 3 1.7 CC(CC1=C(C=CC(=C1)OC)OC)N
CHEMBL6737 5ht2a_rat Rat No 6.1 EC50 = 740 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
195 4 1 3 1.7 CC(CC1=C(C=CC(=C1)OC)OC)N
CHEMBL3330642 5ht2a_human Human Yes 7.1 EC50 = 75.3 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 1.9 CC1=CC2=C(C=C1)C(=CN2)CCN
CHEMBL3330642 5ht2a_human Human Yes 7.1 EC50 = 75.3 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 1.9 CC1=CC2=C(C=C1)C(=CN2)CCN
CHEMBL494947 5ht2a_human Human Yes 7.1 EC50 = 76 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
305 4 1 5 2.0 C1CN(CCN1)C2=CN=CC(=N2)OCC3=CC(=CC=C3)Cl
CHEMBL76474 5ht2a_human Human Yes 7.1 EC50 = 76 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
240 3 1 4 2.2 CC(CN1CCC2=CC(=C(C=C21)SC)F)N
CHEMBL1643859 5ht2a_human Human No 6.1 EC50 = 762 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
390 3 2 6 1.0 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC6=C(C=C5)NC(=O)C6
CHEMBL1643859 5ht2a_human Human No 6.1 EC50 = 762 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
390 3 2 6 1.0 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC6=C(C=C5)NC(=O)C6
CHEMBL202324 5ht2a_human Human No 6.1 EC50 = 777 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
265 5 1 2 2.8 CC(CN1C=CC2=C1C3=C(C=C2)N=CC=C3)NCC=C
CHEMBL202324 5ht2a_human Human No 6.1 EC50 = 777 Funct
Binding to human 5HT2A receptor expressed in CHO cellsBinding to human 5HT2A receptor expressed in CHO cells
265 5 1 2 2.8 CC(CN1C=CC2=C1C3=C(C=C2)N=CC=C3)NCC=C
CHEMBL1643675 5ht2a_human Human No 5.1 EC50 = 7774 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
335 3 1 5 2.2 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC=CC=C5
CHEMBL1643675 5ht2a_human Human No 5.1 EC50 = 7774 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
335 3 1 5 2.2 C1CNCCC2=NC3=CC=NN3C(=C21)N4CC(C4)OC5=CC=CC=C5
CHEMBL219837 5ht2a_human Human No 7.1 EC50 = 78 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 5 1.7 CC1C2C3=C(C(=CC=C3)C(F)(F)F)C(=O)N2CCN1
CHEMBL520133 5ht2a_rat Rat No 7.1 EC50 = 78 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
312 2 1 3 2.7 CC(CC1=C2CCOC2=C(C3=C1OCCC3)Br)N
CHEMBL219837 5ht2a_human Human No 7.1 EC50 = 78 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 5 1.7 CC1C2C3=C(C(=CC=C3)C(F)(F)F)C(=O)N2CCN1
CHEMBL520133 5ht2a_rat Rat No 7.1 EC50 = 78 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
312 2 1 3 2.7 CC(CC1=C2CCOC2=C(C3=C1OCCC3)Br)N
CHEMBL337590 5ht2a_rat Rat No 5.1 EC50 = 7900 Funct
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 3 2.4 CN(C)CCC1=CNC2=CC(=C(C=C21)OC)F
CHEMBL368016 5ht2a_human Human Yes 6.1 EC50 = 794.3 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
214 0 1 2 2.8 CC1CNCCC2=C1C(=C(C=C2)Cl)F
CHEMBL368016 5ht2a_human Human Yes 6.1 EC50 = 794.3 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
214 0 1 2 2.8 CC1CNCCC2=C1C(=C(C=C2)Cl)F
CHEMBL2331793 5ht2a_human Human No 5.1 EC50 = 7943.3 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
182 2 1 4 0.9 CCOC1=NOC2=C1CCNCC2
CHEMBL96816 5ht2a_human Human Yes 8.1 EC50 = 8.5 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
192 2 2 2 1.1 CC(CC1=CNC2=C1C=C(C=C2)F)N
CHEMBL96816 5ht2a_human Human Yes 8.1 EC50 = 8.5 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
192 2 2 2 1.1 CC(CC1=CNC2=C1C=C(C=C2)F)N
CHEMBL180867 5ht2a_human Human No 7.1 EC50 = 80 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
270 1 1 2 2.8 CC1CNCCC2=CC(=C(C=C12)Br)OC
CHEMBL181787 5ht2a_human Human No 7.1 EC50 = 80 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
226 1 1 2 2.7 CC1CNCCC2=CC(=C(C=C12)Cl)OC
CHEMBL180815 5ht2a_human Human No 7.1 EC50 = 80 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
270 1 1 2 2.8 CC1CNCCC2=CC(=C(C=C12)Br)OC
CHEMBL133455 5ht2a_rat Rat Yes 7.1 EC50 = 80.1 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 2.2 CC(CC1=CNC2=C1C3=C(C=C2)OCCC3)N
CHEMBL200104 5ht2a_rat Rat Yes 7.1 EC50 = 81.3 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 2 2 4 0.5 CC1=C2C(=CNN2CC(C)N)C=CC1=O
CHEMBL200104 5ht2a_rat Rat Yes 7.1 EC50 = 81.3 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 2 2 4 0.5 CC1=C2C(=CNN2CC(C)N)C=CC1=O
CHEMBL397166 5ht2a_rat Rat No 5.1 EC50 = 8192 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
301 3 1 6 2.0 CC1=NOC(=N1)C2=C3CCOC3=C(C4=C2OCC4)CC(C)N
CHEMBL397166 5ht2a_rat Rat No 5.1 EC50 = 8192 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
301 3 1 6 2.0 CC1=NOC(=N1)C2=C3CCOC3=C(C4=C2OCC4)CC(C)N
CHEMBL191286 5ht2a_rat Rat No 6.1 EC50 = 840 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
290 4 2 4 1.2 CC(C(C1=CC(=C(C=C1OC)Br)OC)O)N
CHEMBL368016 5ht2a_human Human Yes 6.1 EC50 = 840 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
214 0 1 2 2.8 CC1CNCCC2=C1C(=C(C=C2)Cl)F
CHEMBL191286 5ht2a_rat Rat No 6.1 EC50 = 840 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
290 4 2 4 1.2 CC(C(C1=CC(=C(C=C1OC)Br)OC)O)N
CHEMBL219734 5ht2a_human Human No 7.1 EC50 = 87 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
272 1 1 6 1.5 C1CN2C(CN1)C3=C(C2=O)C(=CC=C3)OC(F)(F)F
CHEMBL609306 5ht2a_human Human No 7.1 EC50 = 87 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
330 3 1 4 3.2 C1CC2=C(C1OC3=CC=CC=C3Cl)N=C(C=C2)N4CCNCC4
CHEMBL219734 5ht2a_human Human No 7.1 EC50 = 87 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
272 1 1 6 1.5 C1CN2C(CN1)C3=C(C2=O)C(=CC=C3)OC(F)(F)F
CHEMBL609306 5ht2a_human Human No 7.1 EC50 = 87 Funct
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
330 3 1 4 3.2 C1CC2=C(C1OC3=CC=CC=C3Cl)N=C(C=C2)N4CCNCC4
CHEMBL234683 5ht2a_rat Rat No 7.1 EC50 = 87.8 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
314 2 2 4 1.3 CC(C(C1=C2CCOC2=C(C3=C1OCC3)Br)O)N
CHEMBL234683 5ht2a_rat Rat No 7.1 EC50 = 87.8 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
314 2 2 4 1.3 CC(C(C1=C2CCOC2=C(C3=C1OCC3)Br)O)N
CHEMBL385577 5ht2a_human Human No 6.1 EC50 = 872 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
253 1 1 3 0.9 COC1=C(C=CC2=C1C(=O)N3C2CNCC3)Cl
CHEMBL385577 5ht2a_human Human No 6.1 EC50 = 872 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
253 1 1 3 0.9 COC1=C(C=CC2=C1C(=O)N3C2CNCC3)Cl
CHEMBL232996 5ht2a_rat Rat No 6.1 EC50 = 880 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 1 5 1.5 CC(CC1=C2C(=C(C3=C1CCO3)C(=O)OC)CCO2)N
CHEMBL232996 5ht2a_rat Rat No 6.1 EC50 = 880 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 1 5 1.5 CC(CC1=C2C(=C(C3=C1CCO3)C(=O)OC)CCO2)N
CHEMBL2023357 5ht2a_human Human No 6.1 EC50 = 894 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
235 5 1 3 2.2 C1CC1COC2=C(C=C(C=C2)F)C3CC3CN
CHEMBL2023357 5ht2a_human Human No 6.1 EC50 = 894 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
235 5 1 3 2.2 C1CC1COC2=C(C=C(C=C2)F)C3CC3CN
CHEMBL343529 5ht2a_human Human Yes 8.0 EC50 = 9.0 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 1.3 COC1=CC=CC2=C1C(=CN2)CCN
CHEMBL343529 5ht2a_human Human Yes 8.1 EC50 = 9.0 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 1.3 COC1=CC=CC2=C1C(=CN2)CCN
CHEMBL482703 5ht2a_rat Rat No 8.0 EC50 = 9.4 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
298 2 1 3 2.3 C1CC2=C(C3=C(CCO3)C(=C2OC1)Br)CCN
CHEMBL482703 5ht2a_rat Rat No 8.0 EC50 = 9.4 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
298 2 1 3 2.3 C1CC2=C(C3=C(CCO3)C(=C2OC1)Br)CCN
CHEMBL180668 5ht2a_human Human Yes 7.1 EC50 = 90 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
182 0 1 1 2.4 C1CNCCC2=C1C=CC(=C2)Cl
CHEMBL223272 5ht2a_human Human No 7.0 EC50 = 91 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 5 1.7 CC1CNCC2N1C(=O)C3=C2C=CC=C3C(F)(F)F
CHEMBL223272 5ht2a_human Human No 7.0 EC50 = 91 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 5 1.7 CC1CNCC2N1C(=O)C3=C2C=CC=C3C(F)(F)F
CHEMBL2397913 5ht2a_human Human No 6.0 EC50 = 921 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 1.2 CC1=C(C2=C(C=C1)C(=O)N3CCNCC3C2)OC
CHEMBL407909 5ht2a_human Human Yes 7.0 EC50 = 93 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
243 3 1 3 2.2 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N
CHEMBL407909 5ht2a_human Human Yes 7.0 EC50 = 93 Funct
Agonist activity at Homo sapiens (human) 5-HT2A receptor assessed as 5-HT-induced phosphoinositide hydrolysis by cell based assayAgonist activity at Homo sapiens (human) 5-HT2A receptor assessed as 5-HT-induced phosphoinositide hydrolysis by cell based assay
243 3 1 3 2.2 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N
CHEMBL407909 5ht2a_human Human Yes 7.0 EC50 = 93 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
243 3 1 3 2.2 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N
CHEMBL361742 5ht2a_human Human Yes 6.0 EC50 = 940 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
191 1 1 2 2.1 CC1CNCCC2=C1C=C(C=C2)OC
CHEMBL197646 5ht2a_human Human No 6.0 EC50 = 949 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
206 3 1 2 2.6 CN(C)CCC1=CNC2=C1C(=CC=C2)F
CHEMBL197646 5ht2a_human Human No 6.0 EC50 = 949 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
206 3 1 2 2.6 CN(C)CCC1=CNC2=C1C(=CC=C2)F
CHEMBL590531 5ht2a_human Human No 6.0 EC50 = 952 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
231 0 2 3 1.3 CC1=CC2=C(C=C1)C(=O)NC3N2CCNCC3
CHEMBL590531 5ht2a_human Human No 6.0 EC50 = 952 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
231 0 2 3 1.3 CC1=CC2=C(C=C1)C(=O)NC3N2CCNCC3
CHEMBL2397877 5ht2a_human Human No 7.0 EC50 = 97 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
237 0 1 2 1.5 C1CN2C(CC3=C(C2=O)C=C(C=C3)Cl)CN1
CHEMBL415029 5ht2a_human Human No 7.0 EC50 = 97 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
298 2 1 2 3.6 CC1CNCCC2=CC(=C(C=C12)Br)OC(C)C
CHEMBL375642 5ht2a_human Human No 6.0 EC50 = 994 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 0 5 1.7 CN1CCN2C(C1)C3=C(C2=O)C(=CC=C3)C(F)(F)F
CHEMBL375642 5ht2a_human Human No 6.0 EC50 = 994 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 0 5 1.7 CN1CCN2C(C1)C3=C(C2=O)C(=CC=C3)C(F)(F)F
CHEMBL1927096 5ht2a_rat Rat No 10.7 IC50 = 0.0 Funct
Displacement of [3H]ketanserin from Sprague-Dawley rat brain cortex serotonin 5-HT2A receptor after 15 mins by liquid scintillation countingDisplacement of [3H]ketanserin from Sprague-Dawley rat brain cortex serotonin 5-HT2A receptor after 15 mins by liquid scintillation counting
350 7 1 7 1.2 C1CN(CCN1CCCN=C(C2=CC=CC=N2)NC#N)C3=NC=CC=N3
CHEMBL3652592 5ht2a_human Human No 10.6 IC50 = 0.0 Funct
BindingDB_Patents: Radioligand Binding Assays. Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 µM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 µM. Assays were conducted in a total volume of 200 µl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 µM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.BindingDB_Patents: Radioligand Binding Assays. Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 µM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 µM. Assays were conducted in a total volume of 200 µl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 µM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.
382 7 2 6 1.7 CN1C(=CC=N1)C2=C(C=CC(=C2)NC(=O)C(=O)C3=CC=C(C=C3)F)OCCN
CHEMBL3652592 5ht2a_human Human No 10.6 IC50 = 0.0 Funct
Radioligand Binding Assays : Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 μM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 μM. Assays were conducted in a total volume of 200 μl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 μM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.Radioligand Binding Assays : Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 μM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 μM. Assays were conducted in a total volume of 200 μl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 μM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.
382 7 2 6 1.7 CN1C(=CC=N1)C2=C(C=CC(=C2)NC(=O)C(=O)C3=CC=C(C=C3)F)OCCN
CHEMBL3665544 5ht2a_human Human No 10.1 IC50 = 0.1 Funct
BindingDB_Patents: Radioligand Binding Assay. Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125I]DOI as radioligand. To define nonspecific binding, 10 µM DOI was used for all assays. For competitive binding studies, 0.5 nM [125I]DOI was used and compounds were assayed over a range of 0.01 nM to 10 µM. Assays were conducted in a total volume of 200 µl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 µM pargyline). Assay incubations were performed for 60 mM at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvester.BindingDB_Patents: Radioligand Binding Assay. Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125I]DOI as radioligand. To define nonspecific binding, 10 µM DOI was used for all assays. For competitive binding studies, 0.5 nM [125I]DOI was used and compounds were assayed over a range of 0.01 nM to 10 µM. Assays were conducted in a total volume of 200 µl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 µM pargyline). Assay incubations were performed for 60 mM at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvester.
497 10 2 8 3.6 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)C3=CC(=CC=C3)C(F)(F)F)OCCNCCOC
CHEMBL3665544 5ht2a_human Human No 10.1 IC50 = 0.1 Funct
Radioligand Binding Assay: Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125I]DOI as radioligand. To define nonspecific binding, 10 μM DOI was used for all assays. For competitive binding studies, 0.5 nM [125I]DOI was used and compounds were assayed over a range of 0.01 nM to 10 μM. Assays were conducted in a total volume of 200 μl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 μM pargyline). Assay incubations were performed for 60 mM at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvester.Radioligand Binding Assay: Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125I]DOI as radioligand. To define nonspecific binding, 10 μM DOI was used for all assays. For competitive binding studies, 0.5 nM [125I]DOI was used and compounds were assayed over a range of 0.01 nM to 10 μM. Assays were conducted in a total volume of 200 μl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 μM pargyline). Assay incubations were performed for 60 mM at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvester.
497 10 2 8 3.6 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)C3=CC(=CC=C3)C(F)(F)F)OCCNCCOC
CHEMBL394325 5ht2a_rat Rat No 10.0 IC50 = 0.1 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
259 4 1 4 2.1 CC(CC1=C2C=COC2=C(C3=C1OC=C3)COC)N
CHEMBL394325 5ht2a_rat Rat No 10.0 IC50 = 0.1 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
259 4 1 4 2.1 CC(CC1=C2C=COC2=C(C3=C1OC=C3)COC)N
CHEMBL134519 5ht2a_rat Rat Yes 9.7 IC50 = 0.2 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
321 4 1 3 2.5 CC(CC1=CC(=C(C=C1OC)I)OC)N
CHEMBL134519 5ht2a_rat Rat Yes 9.7 IC50 = 0.2 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
321 4 1 3 2.5 CC(CC1=CC(=C(C=C1OC)I)OC)N
CHEMBL603078 5ht2a_human Human No 9.6 IC50 = 0.3 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
419 4 2 4 3.2 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)F)OC
CHEMBL603078 5ht2a_human Human No 9.6 IC50 = 0.3 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
419 4 2 4 3.2 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)F)OC
CHEMBL3652595 5ht2a_human Human No 9.6 IC50 = 0.3 Funct
Radioligand Binding Assays : Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 μM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 μM. Assays were conducted in a total volume of 200 μl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 μM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.Radioligand Binding Assays : Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 μM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 μM. Assays were conducted in a total volume of 200 μl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 μM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.
445 6 2 7 3.3 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)C3CCC(CC3)C(F)(F)F)OCCN
CHEMBL3652595 5ht2a_human Human No 9.6 IC50 = 0.3 Funct
BindingDB_Patents: Radioligand Binding Assays. Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 µM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 µM. Assays were conducted in a total volume of 200 µl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 µM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.BindingDB_Patents: Radioligand Binding Assays. Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 µM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 µM. Assays were conducted in a total volume of 200 µl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 µM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.
445 6 2 7 3.3 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)C3CCC(CC3)C(F)(F)F)OCCN
CHEMBL234464 5ht2a_rat Rat No 9.6 IC50 = 0.3 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
263 4 1 4 1.3 CC(CC1=C2CCOC2=C(C3=C1OCC3)COC)N
CHEMBL234464 5ht2a_rat Rat No 9.6 IC50 = 0.3 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
263 4 1 4 1.3 CC(CC1=C2CCOC2=C(C3=C1OCC3)COC)N
CHEMBL232995 5ht2a_rat Rat No 9.5 IC50 = 0.3 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
383 8 1 6 2.8 CC(CC1=C2CCOC2=C(C3=C1OCC3)COCC(=O)OC4=CC=CC=C4)N
CHEMBL232995 5ht2a_rat Rat No 9.5 IC50 = 0.3 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
383 8 1 6 2.8 CC(CC1=C2CCOC2=C(C3=C1OCC3)COCC(=O)OC4=CC=CC=C4)N
CHEMBL101008 5ht2a_rat Rat Yes 9.5 IC50 = 0.3 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
298 2 1 3 2.4 CC(CC1=C2CCOC2=C(C3=C1OCC3)Br)N
CHEMBL101008 5ht2a_rat Rat Yes 9.5 IC50 = 0.3 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
298 2 1 3 2.4 CC(CC1=C2CCOC2=C(C3=C1OCC3)Br)N
CHEMBL393077 5ht2a_rat Rat No 9.5 IC50 = 0.3 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
245 3 2 4 1.6 CC(CC1=C2C=COC2=C(C3=C1OC=C3)CO)N
CHEMBL393077 5ht2a_rat Rat No 9.5 IC50 = 0.3 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
245 3 2 4 1.6 CC(CC1=C2C=COC2=C(C3=C1OC=C3)CO)N
CHEMBL79834 5ht2a_human Human Yes 9.5 IC50 = 0.3 Funct
Compound was evaluated for its inverse agonist activity against 5-hydroxytryptamine 2A receptorCompound was evaluated for its inverse agonist activity against 5-hydroxytryptamine 2A receptor
383 6 1 5 3.4 C1CN(CCC12C(=O)NCN2C3=CC=CC=C3)CCCOC4=CC=C(C=C4)F
CHEMBL85 5ht2a_human Human Yes 9.5 IC50 = 0.3 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
411 4 0 6 2.7 CC1=C(C(=O)N2CCCCC2=N1)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F
CHEMBL234682 5ht2a_rat Rat No 9.4 IC50 = 0.4 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
311 4 1 6 3.1 CC1=NOC(=N1)CC2=C3C=COC3=C(C4=C2OC=C4)CC(C)N
CHEMBL234682 5ht2a_rat Rat No 9.4 IC50 = 0.4 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
311 4 1 6 3.1 CC1=NOC(=N1)CC2=C3C=COC3=C(C4=C2OC=C4)CC(C)N
CHEMBL12713 5ht2a_rat Rat Yes 9.4 IC50 = 0.4 Funct
Binding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranesBinding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranes
441 5 1 3 4.1 C1CN(CCC1C2=CN(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F)CCN5CCNC5=O
CHEMBL602874 5ht2a_human Human No 9.4 IC50 = 0.4 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
436 4 2 3 3.7 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC(=CC=C3)Cl)OC
CHEMBL599226 5ht2a_human Human No 9.4 IC50 = 0.4 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
469 4 2 6 4.0 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=CC(=C3)C(F)(F)F)OC
CHEMBL603609 5ht2a_human Human No 9.4 IC50 = 0.4 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
431 5 2 4 3.1 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)OC)OC
CHEMBL602874 5ht2a_human Human No 9.4 IC50 = 0.4 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
436 4 2 3 3.7 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC(=CC=C3)Cl)OC
CHEMBL599226 5ht2a_human Human No 9.4 IC50 = 0.4 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
469 4 2 6 4.0 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=CC(=C3)C(F)(F)F)OC
CHEMBL603609 5ht2a_human Human No 9.4 IC50 = 0.4 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
431 5 2 4 3.1 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)OC)OC
CHEMBL35057 5ht2a_rat Rat Yes 9.4 IC50 = 0.4 Funct
Binding affinity against rat 5-hydroxytryptamine 2 receptor in rat cerebral cortex tissue using [3H]spiperone as radioligandBinding affinity against rat 5-hydroxytryptamine 2 receptor in rat cerebral cortex tissue using [3H]spiperone as radioligand
441 6 0 6 4.3 C1CCC2(C1)CC(=O)N(C(=O)C2)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54
CHEMBL134519 5ht2a_rat Rat Yes 9.4 IC50 = 0.4 Funct
In vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortexIn vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex
321 4 1 3 2.5 CC(CC1=CC(=C(C=C1OC)I)OC)N
CHEMBL134519 5ht2a_rat Rat Yes 9.3 IC50 = 0.5 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
321 4 1 3 2.5 CC(CC1=CC(=C(C=C1OC)I)OC)N
CHEMBL134519 5ht2a_rat Rat Yes 9.3 IC50 = 0.5 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
321 4 1 3 2.5 CC(CC1=CC(=C(C=C1OC)I)OC)N
CHEMBL303313 5ht2a_rat Rat Yes 9.3 IC50 = 0.5 Funct
Ability to displace [3H]ketanserin (0.5 nM) from cerebral cortex of rat 5-hydroxytryptamine 2A receptorAbility to displace [3H]ketanserin (0.5 nM) from cerebral cortex of rat 5-hydroxytryptamine 2A receptor
345 1 0 3 4.3 CN1CCN(CC1)C2CC3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL64875 5ht2a_rat Rat No 9.3 IC50 = 0.5 Funct
Ability to displace [3H]ketanserin (0.5 nM) from cerebral cortex of rat 5-hydroxytryptamine 2A receptorAbility to displace [3H]ketanserin (0.5 nM) from cerebral cortex of rat 5-hydroxytryptamine 2A receptor
345 1 0 3 4.3 CN1CCN(CC1)C2CC3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL602284 5ht2a_human Human No 9.3 IC50 = 0.5 Funct
Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in avCHO-K1 cellsDisplacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in avCHO-K1 cells
524 9 0 6 6.8 C1CCC(CC1)CN(CCCN2CCN(CC2)C3=CC=C(C=C3)F)S(=O)(=O)C4=CC5=CC=CC=C5C=C4
CHEMBL602284 5ht2a_human Human No 9.3 IC50 = 0.5 Funct
Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in avCHO-K1 cellsDisplacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in avCHO-K1 cells
524 9 0 6 6.8 C1CCC(CC1)CN(CCCN2CCN(CC2)C3=CC=C(C=C3)F)S(=O)(=O)C4=CC5=CC=CC=C5C=C4
CHEMBL131736 5ht2a_rat Rat No 9.3 IC50 = 0.5 Funct
In vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortexIn vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex
244 2 1 2 2.1 CC(CC1=CN(C2=C1C3=C(C=C2)OCCC3)C)N
CHEMBL133455 5ht2a_rat Rat Yes 9.3 IC50 = 0.5 Funct
In vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortexIn vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex
230 2 2 2 2.2 CC(CC1=CNC2=C1C3=C(C=C2)OCCC3)N
CHEMBL610208 5ht2a_human Human No 9.3 IC50 = 0.5 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
391 4 2 3 3.7 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)Cl)OC
CHEMBL603061 5ht2a_human Human No 9.3 IC50 = 0.5 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
393 4 2 5 3.3 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)NC3=CC(=C(C=C3)F)F)OC
CHEMBL599225 5ht2a_human Human No 9.3 IC50 = 0.5 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
480 4 2 3 3.8 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)Br)OC
CHEMBL610208 5ht2a_human Human No 9.3 IC50 = 0.5 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
391 4 2 3 3.7 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)Cl)OC
CHEMBL603061 5ht2a_human Human No 9.3 IC50 = 0.5 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
393 4 2 5 3.3 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)NC3=CC(=C(C=C3)F)F)OC
CHEMBL599225 5ht2a_human Human No 9.3 IC50 = 0.5 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
480 4 2 3 3.8 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)Br)OC
CHEMBL3665547 5ht2a_human Human No 9.3 IC50 = 0.5 Funct
Radioligand Binding Assay: Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125I]DOI as radioligand. To define nonspecific binding, 10 μM DOI was used for all assays. For competitive binding studies, 0.5 nM [125I]DOI was used and compounds were assayed over a range of 0.01 nM to 10 μM. Assays were conducted in a total volume of 200 μl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 μM pargyline). Assay incubations were performed for 60 mM at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvester.Radioligand Binding Assay: Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125I]DOI as radioligand. To define nonspecific binding, 10 μM DOI was used for all assays. For competitive binding studies, 0.5 nM [125I]DOI was used and compounds were assayed over a range of 0.01 nM to 10 μM. Assays were conducted in a total volume of 200 μl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 μM pargyline). Assay incubations were performed for 60 mM at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvester.
402 7 2 5 2.6 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)C3=CC(=CC=C3)OC)OCCO
CHEMBL3699819 5ht2a_rat Rat No 9.3 IC50 = 0.5 Funct
Receptor Binding Assay: Materials for the Receptor Binding AssayIsotope ligand [3H]-Ketanserin (67.0 Ci/mmol) was purchased from PerkinElmer Company; Methysergide was purchased from RBI Company; GF/C glass fiber filter paper was purchased from Whatman Company; Tris was imported and divided into aliquots; PPO, POPOP were purchased from Shanghai No. 1 Reagent Factory; lipid-soluble scintillation solution. Beckman LS-6500 Multi-function Liquid Scintillation Counter was used.Procedures(1) The prepared membrane was first applied with appropriate amount of buffer (0.05 M Tris-HCl buffer: 6.05 g of Tris was dissolved in 1000 ml of double-distilled water, and concentrated HCl was used to adjust to pH 7.5), and homogenizer was used for evenly dispersing. 15 tubes were mixed into a 100 ml container, and appropriate amount of homogenized liquid was added to give 50 ml of membrane suspension, which was reserved for future use.(2) 100 uL of membrane preparation and 100 uL of buffer.Receptor Binding Assay: Materials for the Receptor Binding AssayIsotope ligand [3H]-Ketanserin (67.0 Ci/mmol) was purchased from PerkinElmer Company; Methysergide was purchased from RBI Company; GF/C glass fiber filter paper was purchased from Whatman Company; Tris was imported and divided into aliquots; PPO, POPOP were purchased from Shanghai No. 1 Reagent Factory; lipid-soluble scintillation solution. Beckman LS-6500 Multi-function Liquid Scintillation Counter was used.Procedures(1) The prepared membrane was first applied with appropriate amount of buffer (0.05 M Tris-HCl buffer: 6.05 g of Tris was dissolved in 1000 ml of double-distilled water, and concentrated HCl was used to adjust to pH 7.5), and homogenizer was used for evenly dispersing. 15 tubes were mixed into a 100 ml container, and appropriate amount of homogenized liquid was added to give 50 ml of membrane suspension, which was reserved for future use.(2) 100 uL of membrane preparation and 100 uL of buffer.
469 8 1 9 3.9 C1CN(CCC1C2=NOC3=C2C=CC(=C3)F)CCCSC4=NN=C(O4)C5=CC=C(C=C5)CO
CHEMBL3665547 5ht2a_human Human No 9.3 IC50 = 0.5 Funct
BindingDB_Patents: Radioligand Binding Assay. Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125I]DOI as radioligand. To define nonspecific binding, 10 µM DOI was used for all assays. For competitive binding studies, 0.5 nM [125I]DOI was used and compounds were assayed over a range of 0.01 nM to 10 µM. Assays were conducted in a total volume of 200 µl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 µM pargyline). Assay incubations were performed for 60 mM at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvester.BindingDB_Patents: Radioligand Binding Assay. Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125I]DOI as radioligand. To define nonspecific binding, 10 µM DOI was used for all assays. For competitive binding studies, 0.5 nM [125I]DOI was used and compounds were assayed over a range of 0.01 nM to 10 µM. Assays were conducted in a total volume of 200 µl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 µM pargyline). Assay incubations were performed for 60 mM at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvester.
402 7 2 5 2.6 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)C3=CC(=CC=C3)OC)OCCO
CHEMBL3699819 5ht2a_rat Rat No 9.3 IC50 = 0.5 Funct
BindingDB_Patents: Receptor Binding Assay. Materials for the Receptor Binding AssayIsotope ligand [3H]-Ketanserin (67.0 Ci/mmol) was purchased from PerkinElmer Company; Methysergide was purchased from RBI Company; GF/C glass fiber filter paper was purchased from Whatman Company; Tris was imported and divided into aliquots; PPO, POPOP were purchased from Shanghai No. 1 Reagent Factory; lipid-soluble scintillation solution. Beckman LS-6500 Multi-function Liquid Scintillation Counter was used.Procedures(1) The prepared membrane was first applied with appropriate amount of buffer (0.05 M Tris-HCl buffer: 6.05 g of Tris was dissolved in 1000 ml of double-distilled water, and concentrated HCl was used to adjust to pH 7.5), and homogenizer was used for evenly dispersing. 15 tubes were mixed into a 100 ml container, and appropriate amount of homogenized liquid was added to give 50 ml of membrane suspension, which was reserved for future use.(2) 100 uL of membrane preparation and 100 uL of buffer.BindingDB_Patents: Receptor Binding Assay. Materials for the Receptor Binding AssayIsotope ligand [3H]-Ketanserin (67.0 Ci/mmol) was purchased from PerkinElmer Company; Methysergide was purchased from RBI Company; GF/C glass fiber filter paper was purchased from Whatman Company; Tris was imported and divided into aliquots; PPO, POPOP were purchased from Shanghai No. 1 Reagent Factory; lipid-soluble scintillation solution. Beckman LS-6500 Multi-function Liquid Scintillation Counter was used.Procedures(1) The prepared membrane was first applied with appropriate amount of buffer (0.05 M Tris-HCl buffer: 6.05 g of Tris was dissolved in 1000 ml of double-distilled water, and concentrated HCl was used to adjust to pH 7.5), and homogenizer was used for evenly dispersing. 15 tubes were mixed into a 100 ml container, and appropriate amount of homogenized liquid was added to give 50 ml of membrane suspension, which was reserved for future use.(2) 100 uL of membrane preparation and 100 uL of buffer.
469 8 1 9 3.9 C1CN(CCC1C2=NOC3=C2C=CC(=C3)F)CCCSC4=NN=C(O4)C5=CC=C(C=C5)CO
CHEMBL373245 5ht2a_rat Rat Yes 9.3 IC50 = 0.5 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
226 2 2 4 1.0 CC(CN1C2=C(C(=O)C=CC2=CN1)Cl)N
CHEMBL373245 5ht2a_rat Rat Yes 9.3 IC50 = 0.5 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
226 2 2 4 1.0 CC(CN1C2=C(C(=O)C=CC2=CN1)Cl)N
CHEMBL371300 5ht2a_rat Rat Yes 9.2 IC50 = 0.6 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
191 2 2 4 0.1 CC(CN1C2=CC(=O)C=CC2=CN1)N
CHEMBL371300 5ht2a_rat Rat Yes 9.2 IC50 = 0.6 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
191 2 2 4 0.1 CC(CN1C2=CC(=O)C=CC2=CN1)N
CHEMBL347997 5ht2a_rat Rat No 9.2 IC50 = 0.6 Funct
Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptorInhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor
466 7 1 9 2.1 C1CN(CCC1C2=NOC3=C2C=CC(=C3)F)CCCOC4=CC5=C(C=C4)C(=O)C(=CO5)C(=O)O
CHEMBL194837 5ht2a_human Human No 9.2 IC50 = 0.6 Funct
Inhibitory concentration against 5-hydroxytryptamine 2A receptorInhibitory concentration against 5-hydroxytryptamine 2A receptor
448 8 1 5 5.0 CC1=CC(=NC2=C1C=C(C=C2)NC(=O)COC3=C(C=C(C=C3)Cl)Cl)OCCN(C)C
CHEMBL194837 5ht2a_human Human No 9.2 IC50 = 0.6 Funct
Inhibitory concentration against 5-hydroxytryptamine 2A receptorInhibitory concentration against 5-hydroxytryptamine 2A receptor
448 8 1 5 5.0 CC1=CC(=NC2=C1C=C(C=C2)NC(=O)COC3=C(C=C(C=C3)Cl)Cl)OCCN(C)C
CHEMBL598172 5ht2a_human Human Yes 9.2 IC50 = 0.6 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
437 4 2 5 3.3 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=C(C=C(C=C3)F)F)OC
CHEMBL598172 5ht2a_human Human Yes 9.2 IC50 = 0.6 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
437 4 2 5 3.3 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=C(C=C(C=C3)F)F)OC
CHEMBL391196 5ht2a_rat Rat No 9.2 IC50 = 0.7 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
314 2 2 4 1.3 CC(C(C1=C2CCOC2=C(C3=C1OCC3)Br)O)N
CHEMBL600012 5ht2a_human Human No 9.2 IC50 = 0.7 Funct
Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in avCHO-K1 cellsDisplacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in avCHO-K1 cells
506 9 0 5 6.7 C1CCC(CC1)CN(CCCN2CCN(CC2)C3=CC=CC=C3)S(=O)(=O)C4=CC5=CC=CC=C5C=C4
CHEMBL391196 5ht2a_rat Rat No 9.2 IC50 = 0.7 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
314 2 2 4 1.3 CC(C(C1=C2CCOC2=C(C3=C1OCC3)Br)O)N
CHEMBL600012 5ht2a_human Human No 9.2 IC50 = 0.7 Funct
Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in avCHO-K1 cellsDisplacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in avCHO-K1 cells
506 9 0 5 6.7 C1CCC(CC1)CN(CCCN2CCN(CC2)C3=CC=CC=C3)S(=O)(=O)C4=CC5=CC=CC=C5C=C4
CHEMBL133868 5ht2a_rat Rat Yes 9.2 IC50 = 0.7 Funct
In vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortexIn vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex
230 2 2 2 2.2 CC(CC1=CNC2=C1C3=C(C=C2)OCCC3)N
CHEMBL197653 5ht2a_rat Rat Yes 9.1 IC50 = 0.7 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
209 2 2 5 0.5 CC(CN1C2=C(C(=O)C=CC2=CN1)F)N
CHEMBL197653 5ht2a_rat Rat Yes 9.1 IC50 = 0.7 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
209 2 2 5 0.5 CC(CN1C2=C(C(=O)C=CC2=CN1)F)N
CHEMBL200104 5ht2a_rat Rat Yes 9.1 IC50 = 0.7 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
205 2 2 4 0.5 CC1=C2C(=CNN2CC(C)N)C=CC1=O
CHEMBL200104 5ht2a_rat Rat Yes 9.1 IC50 = 0.7 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
205 2 2 4 0.5 CC1=C2C(=CNN2CC(C)N)C=CC1=O
CHEMBL199385 5ht2a_rat Rat Yes 9.1 IC50 = 0.8 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
177 2 2 4 -0.3 C1=CC2=CNN(C2=CC1=O)CCN
CHEMBL199385 5ht2a_rat Rat Yes 9.1 IC50 = 0.8 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
177 2 2 4 -0.3 C1=CC2=CNN(C2=CC1=O)CCN
CHEMBL602873 5ht2a_human Human No 9.1 IC50 = 0.8 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
504 4 2 6 4.6 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)OC
CHEMBL602064 5ht2a_human Human No 9.1 IC50 = 0.8 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
419 4 2 4 3.2 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC(=CC=C3)F)OC
CHEMBL602873 5ht2a_human Human No 9.1 IC50 = 0.8 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
504 4 2 6 4.6 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)OC
CHEMBL591223 5ht2a_human Human No 9.1 IC50 = 0.8 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
436 4 2 3 3.7 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)Cl)OC
CHEMBL602064 5ht2a_human Human No 9.1 IC50 = 0.8 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
419 4 2 4 3.2 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC(=CC=C3)F)OC
CHEMBL221250 5ht2a_human Human No 9.1 IC50 = 0.8 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
301 4 2 3 3.2 CCC1(CCCC1)NC2=NCCNC(=C2)C3=CC=C(C=C3)F
CHEMBL221250 5ht2a_human Human No 9.1 IC50 = 0.8 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
301 4 2 3 3.2 CCC1(CCCC1)NC2=NCCNC(=C2)C3=CC=C(C=C3)F
CHEMBL394508 5ht2a_rat Rat No 9.1 IC50 = 0.9 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
305 6 1 5 1.8 CC(CC1=C2C(=C(C3=C1CCO3)CCC(=O)OC)CCO2)N
CHEMBL394508 5ht2a_rat Rat No 9.1 IC50 = 0.9 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
305 6 1 5 1.8 CC(CC1=C2C(=C(C3=C1CCO3)CCC(=O)OC)CCO2)N
CHEMBL397321 5ht2a_rat Rat No 9.1 IC50 = 0.9 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
307 7 1 5 1.2 CC(CC1=C2CCOC2=C(C3=C1OCC3)COCCOC)N
CHEMBL421244 5ht2a_rat Rat No 9.1 IC50 = 0.9 Funct
Binding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranesBinding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranes
431 8 1 4 3.5 CN(CCN1CCNC1=O)CCOC2=CN(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F
CHEMBL397321 5ht2a_rat Rat No 9.1 IC50 = 0.9 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
307 7 1 5 1.2 CC(CC1=C2CCOC2=C(C3=C1OCC3)COCCOC)N
CHEMBL122269 5ht2a_rat Rat No 9.0 IC50 = 1.0 Funct
Binding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranesBinding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranes
415 7 1 3 3.8 CN(CCC1=CN(C2=C1C=CC(=C2)Cl)C3=CC=C(C=C3)F)CCN4CCNC4=O
CHEMBL606622 5ht2a_human Human No 9.0 IC50 = 1 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
447 5 2 4 3.9 CC(C)N1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)F)OC
CHEMBL598173 5ht2a_human Human No 9.0 IC50 = 1 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
393 4 2 5 3.3 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)NC3=C(C=C(C=C3)F)F)OC
CHEMBL605001 5ht2a_human Human No 9.0 IC50 = 1 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
357 4 2 3 3.1 CN1C(=CC=N1)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)Cl)OC
CHEMBL232594 5ht2a_rat Rat No 9.0 IC50 = 1 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
329 5 1 6 2.6 CC1=NOC(=N1)CCC2=C3CCOC3=C(C4=C2OCC4)CC(C)N
CHEMBL394664 5ht2a_rat Rat No 9.0 IC50 = 1 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
249 3 2 4 0.8 CC(CC1=C2CCOC2=C(C3=C1OCC3)CO)N
CHEMBL3652594 5ht2a_human Human No 9.0 IC50 = 1 Funct
Radioligand Binding Assays : Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 μM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 μM. Assays were conducted in a total volume of 200 μl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 μM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.Radioligand Binding Assays : Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 μM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 μM. Assays were conducted in a total volume of 200 μl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 μM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.
457 6 2 8 3.4 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)C3=CC(=C(C=C3)F)C(F)(F)F)OCCN
CHEMBL606622 5ht2a_human Human No 9.0 IC50 = 1 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
447 5 2 4 3.9 CC(C)N1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)F)OC
CHEMBL598173 5ht2a_human Human No 9.0 IC50 = 1 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
393 4 2 5 3.3 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)NC3=C(C=C(C=C3)F)F)OC
CHEMBL605001 5ht2a_human Human No 9.0 IC50 = 1 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
357 4 2 3 3.1 CN1C(=CC=N1)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)Cl)OC
CHEMBL341229 5ht2a_rat Rat No 9.0 IC50 = 1 Funct
Binding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranesBinding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranes
429 8 1 3 4.1 CN(CCCN1CCNC1=O)CCC2=CN(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F
CHEMBL3652594 5ht2a_human Human No 9.0 IC50 = 1 Funct
BindingDB_Patents: Radioligand Binding Assays. Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 µM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 µM. Assays were conducted in a total volume of 200 µl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 µM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.BindingDB_Patents: Radioligand Binding Assays. Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 µM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 µM. Assays were conducted in a total volume of 200 µl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 µM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.
457 6 2 8 3.4 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)C3=CC(=C(C=C3)F)C(F)(F)F)OCCN
CHEMBL232594 5ht2a_rat Rat No 9.0 IC50 = 1 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
329 5 1 6 2.6 CC1=NOC(=N1)CCC2=C3CCOC3=C(C4=C2OCC4)CC(C)N
CHEMBL394664 5ht2a_rat Rat No 9.0 IC50 = 1 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
249 3 2 4 0.8 CC(CC1=C2CCOC2=C(C3=C1OCC3)CO)N
CHEMBL373966 5ht2a_human Human No 9.0 IC50 = 1.1 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
319 4 2 4 3.3 CCC1(CCCC1)NC2=NCCNC(=C2)C3=C(C=C(C=C3)F)F
CHEMBL115486 5ht2a_rat Rat No 9.0 IC50 = 1.1 Funct
Binding affinity against rat 5-hydroxytryptamine 2 receptor in rat cerebral cortex tissue using [3H]spiperone as radioligandBinding affinity against rat 5-hydroxytryptamine 2 receptor in rat cerebral cortex tissue using [3H]spiperone as radioligand
457 6 1 7 3.4 C1CCC2(C1)CC(=O)N(C(=O)C2O)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54
CHEMBL136630 5ht2a_rat Rat No 9.0 IC50 = 1.1 Funct
Binding affinity for 5-hydroxytryptamine 2A receptor, activity is expressed as IC50 values.Binding affinity for 5-hydroxytryptamine 2A receptor, activity is expressed as IC50 values.
373 2 0 3 4.8 CC1(CN(CCN1C)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F)C
CHEMBL373966 5ht2a_human Human No 9.0 IC50 = 1.1 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
319 4 2 4 3.3 CCC1(CCCC1)NC2=NCCNC(=C2)C3=C(C=C(C=C3)F)F
CHEMBL84931 5ht2a_human Human No 8.9 IC50 = 1.1 Funct
Binding affinity at human cloned 5-hydroxytryptamine 2A receptor expressed in L929 cells by [125I]R91150 displacement.Binding affinity at human cloned 5-hydroxytryptamine 2A receptor expressed in L929 cells by [125I]R91150 displacement.
312 2 0 4 4.0 CN(C)CC1CC2C3=CC=CC=C3CC4=C(N2O1)C=C(C=C4)F
CHEMBL447864 5ht2a_human Human Yes 8.9 IC50 = 1.2 Funct
Displacement of [3H]ketanserin from 5HT2A receptorDisplacement of [3H]ketanserin from 5HT2A receptor
262 4 1 2 3.8 CC1=CC=C(C=C1)OC2=C(C=CC(=C2)Cl)CNC
CHEMBL447864 5ht2a_human Human Yes 8.9 IC50 = 1.2 Funct
Displacement of [3H]ketanserin from 5HT2A receptorDisplacement of [3H]ketanserin from 5HT2A receptor
262 4 1 2 3.8 CC1=CC=C(C=C1)OC2=C(C=CC(=C2)Cl)CNC
CHEMBL3652596 5ht2a_human Human No 8.9 IC50 = 1.2 Funct
Radioligand Binding Assays : Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 μM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 μM. Assays were conducted in a total volume of 200 μl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 μM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.Radioligand Binding Assays : Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 μM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 μM. Assays were conducted in a total volume of 200 μl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 μM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.
484 7 2 6 3.0 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)C(=O)C3=CC(=CS3)Br)OCCN
CHEMBL3652596 5ht2a_human Human No 8.9 IC50 = 1.2 Funct
BindingDB_Patents: Radioligand Binding Assays. Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 µM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 µM. Assays were conducted in a total volume of 200 µl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 µM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.BindingDB_Patents: Radioligand Binding Assays. Radioligand binding assays for human 5-HT2A receptor was conducted using the 5-HT2 agonist [125]DOI as radioligand. To define nonspecific binding, 10 µM DOI was used for all assays. For competitive binding studies, 0.5 nM [125]DOI was used and compounds were assayed over a range of 0.01 nM to 10 µM. Assays were conducted in a total volume of 200 µl in 96-well Perkin Elmer GF/C filter plates in assay buffer (50 mM Tris-HCl, pH 7.4, 0.5 mM EDTA, 5 mM MgCl2, and 10 µM pargyline). Assay incubations were performed for 60 min at room temperature and were terminated by rapid filtration under vacuum pressure of the reaction mixture over Whatman GF/C glass fiber filters presoaked in 0.5% PEI using a Brandell cell harvestor.
484 7 2 6 3.0 CN1C(=C(C=N1)Cl)C2=C(C=CC(=C2)NC(=O)C(=O)C3=CC(=CS3)Br)OCCN
CHEMBL604586 5ht2a_human Human No 8.9 IC50 = 1.3 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
464 5 2 3 4.4 CC(C)N1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)Cl)OC
CHEMBL598171 5ht2a_human Human No 8.9 IC50 = 1.3 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
437 4 2 5 3.3 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC(=CC(=C3)F)F)OC
CHEMBL606178 5ht2a_human Human No 8.9 IC50 = 1.3 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
470 4 2 3 4.4 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=C(C=C(C=C3)Cl)Cl)OC
CHEMBL604586 5ht2a_human Human No 8.9 IC50 = 1.3 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
464 5 2 3 4.4 CC(C)N1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)Cl)OC
CHEMBL598171 5ht2a_human Human No 8.9 IC50 = 1.3 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
437 4 2 5 3.3 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC(=CC(=C3)F)F)OC
CHEMBL606178 5ht2a_human Human No 8.9 IC50 = 1.3 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
470 4 2 3 4.4 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=C(C=C(C=C3)Cl)Cl)OC
CHEMBL436513 5ht2a_human Human No 8.9 IC50 = 1.4 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
319 4 2 4 3.2 CC(C)(C1CCC1)NC2=NCCNC(=C2)C3=C(C=C(C=C3)F)F
CHEMBL436513 5ht2a_human Human No 8.9 IC50 = 1.4 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
319 4 2 4 3.2 CC(C)(C1CCC1)NC2=NCCNC(=C2)C3=C(C=C(C=C3)F)F
CHEMBL150412 5ht2a_rat Rat No 8.9 IC50 = 1.4 Funct
Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptorInhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor
467 8 0 8 3.7 COCC1=COC2=C(C1=O)C=CC(=C2)OCCCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F
CHEMBL85 5ht2a_rat Rat Yes 8.9 IC50 = 1.4 Funct
Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptorInhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor
411 4 0 6 2.7 CC1=C(C(=O)N2CCCCC2=N1)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F
CHEMBL219265 5ht2a_human Human No 8.8 IC50 = 1.5 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
289 5 2 3 3.2 CCC(C)(CC)NC1=NCCNC(=C1)C2=CC=C(C=C2)F
CHEMBL140032 5ht2a_rat Rat No 8.8 IC50 = 1.5 Funct
Binding affinity for 5-hydroxytryptamine 2A receptor, activity is expressed as IC50 values.Binding affinity for 5-hydroxytryptamine 2A receptor, activity is expressed as IC50 values.
338 2 1 3 4.1 CC1=CC2=C(C=C1)C(CC2N3CCNC(C3)(C)C)C4=CC=C(C=C4)F
CHEMBL331545 5ht2a_rat Rat No 8.8 IC50 = 1.5 Funct
Binding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranesBinding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranes
483 6 0 3 5.0 CC(C)N1CCN(C1=O)CCN2CCC(CC2)C3=CN(C4=C3C=CC(=C4)Cl)C5=CC=C(C=C5)F
CHEMBL219265 5ht2a_human Human No 8.8 IC50 = 1.5 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
289 5 2 3 3.2 CCC(C)(CC)NC1=NCCNC(=C1)C2=CC=C(C=C2)F
CHEMBL135076 5ht2a_rat Rat No 8.8 IC50 = 1.5 Funct
In vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortexIn vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex
230 2 2 2 2.2 CC(CC1=CNC2=C1C3=C(C=C2)OCCC3)N
CHEMBL1113 5ht2a_human Human Yes 8.8 IC50 = 1.6 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
314 1 1 3 2.6 C1CN(CCN1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl
CHEMBL1113 5ht2a_human Human Yes 8.8 IC50 = 1.6 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
314 1 1 3 2.6 C1CN(CCN1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl
CHEMBL599193 5ht2a_human Human No 8.8 IC50 = 1.6 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
450 5 2 3 4.1 CCOC1=C(C=C(C=C1)NC(=O)NC2=CC=C(C=C2)Cl)C3=C(C=NN3C)Br
CHEMBL605636 5ht2a_human Human No 8.8 IC50 = 1.6 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
422 2 3 4 3.2 CN1C(=C2C=C(C=CC2=O)NC(=O)NC3=CC=C(C=C3)Cl)C(=CN1)Br
CHEMBL601097 5ht2a_human Human No 8.8 IC50 = 1.6 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
419 4 2 4 3.2 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=CC=C3F)OC
CHEMBL599194 5ht2a_human Human No 8.8 IC50 = 1.6 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
464 5 2 3 4.5 CC(C)OC1=C(C=C(C=C1)NC(=O)NC2=CC=C(C=C2)Cl)C3=C(C=NN3C)Br
CHEMBL606191 5ht2a_human Human No 8.8 IC50 = 1.6 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
469 4 2 6 4.0 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)C(F)(F)F)OC
CHEMBL599193 5ht2a_human Human No 8.8 IC50 = 1.6 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
450 5 2 3 4.1 CCOC1=C(C=C(C=C1)NC(=O)NC2=CC=C(C=C2)Cl)C3=C(C=NN3C)Br
CHEMBL605636 5ht2a_human Human No 8.8 IC50 = 1.6 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
422 2 3 4 3.2 CN1C(=C2C=C(C=CC2=O)NC(=O)NC3=CC=C(C=C3)Cl)C(=CN1)Br
CHEMBL601097 5ht2a_human Human No 8.8 IC50 = 1.6 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
419 4 2 4 3.2 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=CC=C3F)OC
CHEMBL599194 5ht2a_human Human No 8.8 IC50 = 1.6 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
464 5 2 3 4.5 CC(C)OC1=C(C=C(C=C1)NC(=O)NC2=CC=C(C=C2)Cl)C3=C(C=NN3C)Br
CHEMBL606191 5ht2a_human Human No 8.8 IC50 = 1.6 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
469 4 2 6 4.0 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)C(F)(F)F)OC
CHEMBL234837 5ht2a_rat Rat No 8.8 IC50 = 1.6 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
315 4 1 6 2.3 CC1=NOC(=N1)CC2=C3CCOC3=C(C4=C2OCC4)CC(C)N
CHEMBL219215 5ht2a_human Human No 8.8 IC50 = 1.6 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
301 3 2 3 3.2 CC1(CCCCC1)NC2=NCCNC(=C2)C3=CC=C(C=C3)F
CHEMBL234837 5ht2a_rat Rat No 8.8 IC50 = 1.6 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
315 4 1 6 2.3 CC1=NOC(=N1)CC2=C3CCOC3=C(C4=C2OCC4)CC(C)N
CHEMBL219215 5ht2a_human Human No 8.8 IC50 = 1.6 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
301 3 2 3 3.2 CC1(CCCCC1)NC2=NCCNC(=C2)C3=CC=C(C=C3)F
CHEMBL201132 5ht2a_rat Rat Yes 8.8 IC50 = 1.7 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
317 2 2 4 0.8 CC(CN1C2=C(C(=O)C=CC2=CN1)I)N
CHEMBL201132 5ht2a_rat Rat Yes 8.8 IC50 = 1.7 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
317 2 2 4 0.8 CC(CN1C2=C(C(=O)C=CC2=CN1)I)N
CHEMBL136226 5ht2a_rat Rat No 8.8 IC50 = 1.7 Funct
Binding affinity for 5-hydroxytryptamine 2A receptor, activity is expressed as IC50 values.Binding affinity for 5-hydroxytryptamine 2A receptor, activity is expressed as IC50 values.
361 2 0 3 4.4 CC1(CN(CCN1C)C2CC(C3=C2C=C(C=C3)Cl)C4=CSC=C4)C
CHEMBL27173 5ht2a_rat Rat No 8.8 IC50 = 1.8 Funct
In vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortexIn vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex
216 2 2 2 1.7 C1CC2=C(C=CC3=C2C(=CN3)CCN)OC1
CHEMBL569475 5ht2a_human Human No 8.7 IC50 = 1.9 Funct
Agonist activity at 5HT2A receptor expressed in HEK cells assessed as inhibition of serotonin-induced inositol phosphate accumulationAgonist activity at 5HT2A receptor expressed in HEK cells assessed as inhibition of serotonin-induced inositol phosphate accumulation
519 7 2 4 4.3 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)Cl)OCCN4CCCC4
CHEMBL569475 5ht2a_human Human No 8.7 IC50 = 1.9 Funct
Agonist activity at 5HT2A receptor expressed in HEK cells assessed as inhibition of serotonin-induced inositol phosphate accumulationAgonist activity at 5HT2A receptor expressed in HEK cells assessed as inhibition of serotonin-induced inositol phosphate accumulation
519 7 2 4 4.3 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC=C(C=C3)Cl)OCCN4CCCC4
CHEMBL332425 5ht2a_rat Rat No 8.7 IC50 = 1.9 Funct
Binding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranesBinding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranes
429 8 1 3 4.1 CN(CCCN1CCNC1=O)CCC2=CN(C3=C2C=CC(=C3)Cl)C4=CC=C(C=C4)F
CHEMBL310183 5ht2a_human Human No 8.7 IC50 = 1.9 Funct
Binding affinity for human cloned 5-hydroxytryptamine 2A receptor expressed in L929 cells using [125I]R91150 as radioligandBinding affinity for human cloned 5-hydroxytryptamine 2A receptor expressed in L929 cells using [125I]R91150 as radioligand
331 2 0 4 4.1 CN(C)CC1CC2C3=CC=CC=C3OC4=C(N2O1)C=C(C=C4)Cl
CHEMBL199775 5ht2a_rat Rat Yes 8.7 IC50 = 1.9 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
205 3 1 3 1.0 CC(CN1C2=C(C=CC(=C2)OC)C=N1)N
CHEMBL199775 5ht2a_rat Rat Yes 8.7 IC50 = 1.9 Funct
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortexInhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
205 3 1 3 1.0 CC(CN1C2=C(C=CC(=C2)OC)C=N1)N
CHEMBL1909072 5ht2a_human Human Yes 8.7 IC50 = 1.9 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
402 5 1 4 4.4 C1CN(CCC1C(=O)N)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL1909072 5ht2a_human Human Yes 8.7 IC50 = 1.9 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
402 5 1 4 4.4 C1CN(CCC1C(=O)N)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL599828 5ht2a_human Human No 8.7 IC50 = 2.0 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
537 4 2 9 4.9 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)OC
CHEMBL599828 5ht2a_human Human No 8.7 IC50 = 2.0 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
537 4 2 9 4.9 CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)OC
CHEMBL1080712 5ht2a_human Human No 8.0 IC50 = 10 Funct
Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cells after 60 minsDisplacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cells after 60 mins
445 8 2 3 5.1 CC1=C(C(=CC=C1)N2CCN(CC2)CCCCNC(=O)C3=C(NC(=C3)C4=CC=CC=C4)C)C
CHEMBL1080712 5ht2a_human Human No 8.0 IC50 = 10 Funct
Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cells after 60 minsDisplacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cells after 60 mins
445 8 2 3 5.1 CC1=C(C(=CC=C1)N2CCN(CC2)CCCCNC(=O)C3=C(NC(=C3)C4=CC=CC=C4)C)C
CHEMBL326775 5ht2a_rat Rat No 8.0 IC50 = 10.2 Funct
Binding affinity against rat 5-hydroxytryptamine 2 receptor in rat cerebral cortex tissue using [3H]spiperone as radioligandBinding affinity against rat 5-hydroxytryptamine 2 receptor in rat cerebral cortex tissue using [3H]spiperone as radioligand
457 6 1 7 3.3 C1CCC2(C1)CC(=O)N(C(=O)C2)CCC(CN3CCN(CC3)C4=NSC5=CC=CC=C54)O
CHEMBL1852422 5ht2a_human Human No 8.0 IC50 = 10.3 Funct
Binding Assay: For serotonin 5-HT2A binding, an aliquot of human recombinant serotonin 5-HT2A receptor (PerkinElmer Life and Analytical Sciences, USA) expressed in CHO-K1 cells (5 ug/well) and 1 nM [3H]Ketanserin (PerkinElmer) were used in the presence of mianserin (20 uM) as a nonspecific. The reaction mixture was incubated for 60 min at 27° C. using 50 mM Tris-HCl (pH 7.4) buffer containing 4 mM CaCl2 and 0.1% ascorbic acid, and harvested through filtermate A glass fiber filter (Wallac, Finland) presoaked in 0.5% polyethyleneimine (PEI) by microbeta filtermate-96 harvester (PerkinElmer) to terminate the reaction, and then washed with ice cold 50 mM Tris-HCl buffer solution (pH 7.4). The filter was then covered with MeltiLex, sealed in a sample bag, dried in an oven. The radioactivity retained in the filter was finally counted using MicroBeta Plus (Wallac). For serotonin 5-HT2C binding, frozen membranes from stable CHO-K1 cell line expressing the human recombinant 5-HT2C receptor.Binding Assay: For serotonin 5-HT2A binding, an aliquot of human recombinant serotonin 5-HT2A receptor (PerkinElmer Life and Analytical Sciences, USA) expressed in CHO-K1 cells (5 ug/well) and 1 nM [3H]Ketanserin (PerkinElmer) were used in the presence of mianserin (20 uM) as a nonspecific. The reaction mixture was incubated for 60 min at 27° C. using 50 mM Tris-HCl (pH 7.4) buffer containing 4 mM CaCl2 and 0.1% ascorbic acid, and harvested through filtermate A glass fiber filter (Wallac, Finland) presoaked in 0.5% polyethyleneimine (PEI) by microbeta filtermate-96 harvester (PerkinElmer) to terminate the reaction, and then washed with ice cold 50 mM Tris-HCl buffer solution (pH 7.4). The filter was then covered with MeltiLex, sealed in a sample bag, dried in an oven. The radioactivity retained in the filter was finally counted using MicroBeta Plus (Wallac). For serotonin 5-HT2C binding, frozen membranes from stable CHO-K1 cell line expressing the human recombinant 5-HT2C receptor.
516 8 1 5 5.3 CC1=C(N=C(N1C2=CC=CC=C2OC)C)C(=O)NCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL1852422 5ht2a_human Human No 8.0 IC50 = 10.3 Funct
BindingDB_Patents: Binding Assay. For serotonin 5-HT2A binding, an aliquot of human recombinant serotonin 5-HT2A receptor (PerkinElmer Life and Analytical Sciences, USA) expressed in CHO-K1 cells (5 ug/well) and 1 nM [3H]Ketanserin (PerkinElmer) were used in the presence of mianserin (20 uM) as a nonspecific. The reaction mixture was incubated for 60 min at 27° C. using 50 mM Tris-HCl (pH 7.4) buffer containing 4 mM CaCl2 and 0.1% ascorbic acid, and harvested through filtermate A glass fiber filter (Wallac, Finland) presoaked in 0.5% polyethyleneimine (PEI) by microbeta filtermate-96 harvester (PerkinElmer) to terminate the reaction, and then washed with ice cold 50 mM Tris-HCl buffer solution (pH 7.4). The filter was then covered with MeltiLex, sealed in a sample bag, dried in an oven. The radioactivity retained in the filter was finally counted using MicroBeta Plus (Wallac). For serotonin 5-HT2C binding, frozen membranes from stable CHO-K1 cell line expressing the human recombinant 5-HT2C receptor.BindingDB_Patents: Binding Assay. For serotonin 5-HT2A binding, an aliquot of human recombinant serotonin 5-HT2A receptor (PerkinElmer Life and Analytical Sciences, USA) expressed in CHO-K1 cells (5 ug/well) and 1 nM [3H]Ketanserin (PerkinElmer) were used in the presence of mianserin (20 uM) as a nonspecific. The reaction mixture was incubated for 60 min at 27° C. using 50 mM Tris-HCl (pH 7.4) buffer containing 4 mM CaCl2 and 0.1% ascorbic acid, and harvested through filtermate A glass fiber filter (Wallac, Finland) presoaked in 0.5% polyethyleneimine (PEI) by microbeta filtermate-96 harvester (PerkinElmer) to terminate the reaction, and then washed with ice cold 50 mM Tris-HCl buffer solution (pH 7.4). The filter was then covered with MeltiLex, sealed in a sample bag, dried in an oven. The radioactivity retained in the filter was finally counted using MicroBeta Plus (Wallac). For serotonin 5-HT2C binding, frozen membranes from stable CHO-K1 cell line expressing the human recombinant 5-HT2C receptor.
516 8 1 5 5.3 CC1=C(N=C(N1C2=CC=CC=C2OC)C)C(=O)NCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL85155 5ht2a_human Human No 8.0 IC50 = 10.5 Funct
Binding affinity at human cloned 5-hydroxytryptamine 2A receptor expressed in L929 cells by [125I]R91150 displacement.Binding affinity at human cloned 5-hydroxytryptamine 2A receptor expressed in L929 cells by [125I]R91150 displacement.
308 2 0 3 4.2 CC1=CC2=C(C=C1)C3CC(ON3C4=CC=CC=C4C2)CN(C)C
CHEMBL314107 5ht2a_human Human No 8.0 IC50 = 10.7 Funct
Binding affinity at human cloned 5-hydroxytryptamine 2A receptor expressed in L929 cells by [125I]R91150 displacement.Binding affinity at human cloned 5-hydroxytryptamine 2A receptor expressed in L929 cells by [125I]R91150 displacement.
330 2 0 5 4.1 CN(C)CC1CC2C3=C(CC4=C(N2O1)C=C(C=C4)F)C=CC(=C3)F
CHEMBL715 5ht2a_human Human Yes 7.0 IC50 = 100 Funct
Antagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAntagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
312 1 1 5 2.8 CC1=CC2=C(NC3=CC=CC=C3N=C2S1)N4CCN(CC4)C
CHEMBL1278088 5ht2a_rat Rat Yes 7.0 IC50 = 100 Funct
Inhibition of rat 5HT2 receptorInhibition of rat 5HT2 receptor
433 6 1 6 2.8 C1CCC2=C(C1)C(=O)N(C(=N2)CCCCN3CCN(CC3)C4=NC5=CC=CC=C5C=C4)N
CHEMBL715 5ht2a_human Human Yes 7.0 IC50 = 100 Funct
Antagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAntagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
312 1 1 5 2.8 CC1=CC2=C(NC3=CC=CC=C3N=C2S1)N4CCN(CC4)C
CHEMBL123584 5ht2a_rat Rat No 7.0 IC50 = 100 Funct
Binding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranesBinding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranes
388 5 0 4 4.2 CN1CCN(CC1)CCOC2=CN(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F
CHEMBL122384 5ht2a_rat Rat No 7.0 IC50 = 100 Funct
Binding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranesBinding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranes
345 6 0 2 5.4 CN(C)CCCCC1=CN(C2=C1C=C(C=C2)Cl)C3=CC=C(C=C3)F
CHEMBL1278088 5ht2a_rat Rat Yes 7.0 IC50 = 100 Funct
Inhibition of rat 5HT2 receptorInhibition of rat 5HT2 receptor
433 6 1 6 2.8 C1CCC2=C(C1)C(=O)N(C(=N2)CCCCN3CCN(CC3)C4=NC5=CC=CC=C5C=C4)N
CHEMBL447733 5ht2a_human Human No 6.0 IC50 = 1000 Funct
Displacement of [3H]ketanserin from 5HT2A receptorDisplacement of [3H]ketanserin from 5HT2A receptor
263 4 0 4 3.5 CN(C)CC1=CC=CC=C1OC2=CC(=C(C=C2)F)F
CHEMBL61819 5ht2a_bovin Bovine No 6.0 IC50 = 1000 Funct
Affinity towards 5-hydroxytryptamine 2A receptor in membranes from bovine frontal cortex using [3H]ketanserinAffinity towards 5-hydroxytryptamine 2A receptor in membranes from bovine frontal cortex using [3H]ketanserin
412 7 0 5 4.4 CN1C2=C(C=C(C=C2)CCCCN3CCN(CC3)C4=CC=CC=C4OC)SC1=O
CHEMBL83073 5ht2a_human Human No 6.0 IC50 = 1000 Funct
Binding affinity at human cloned 5-hydroxytryptamine 2A receptor expressed in L929 cells by [125I]R91150 displacement.Binding affinity at human cloned 5-hydroxytryptamine 2A receptor expressed in L929 cells by [125I]R91150 displacement.
362 2 0 6 4.7 CN(C)CC1CC2C3=C(CC4=CC=CC=C4N2O1)C(=CC=C3)C(F)(F)F
CHEMBL280608 5ht2a_bovin Bovine No 6.0 IC50 = 1000 Funct
Binding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortexBinding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortex
419 9 1 6 3.9 CCCN(CCNS(=O)(=O)C1=CC=C(C=C1)C)C2CC3=C(C=CC=C3OC)OC2
CHEMBL51888 5ht2a_bovin Bovine No 6.0 IC50 = 1000 Funct
Binding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortexBinding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortex
419 9 1 6 3.9 CCCN(CCNS(=O)(=O)C1=CC=C(C=C1)C)C2CC3=C(C=CC=C3OC)OC2
CHEMBL11592 5ht2a_human Human Yes 6.0 IC50 = 1000 Funct
Binding affinity towards 5-hydroxytryptamine 2A receptor by displacement of [3H]ketanserinBinding affinity towards 5-hydroxytryptamine 2A receptor by displacement of [3H]ketanserin
443 9 0 5 4.6 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C3CC4=C(C=CC=C4OC)OC3
CHEMBL2376487 5ht2a_human Human No 6.0 IC50 = 1000 Funct
Displacement of [3H]-ketanserin from human 5HT2A receptorDisplacement of [3H]-ketanserin from human 5HT2A receptor
257 1 2 3 2.0 CC1=C(C2=C(N1)C=CC(=C2)[N+](=O)[O-])C3=CCNCC3
CHEMBL447733 5ht2a_human Human No 6.0 IC50 = 1000 Funct
Displacement of [3H]ketanserin from 5HT2A receptorDisplacement of [3H]ketanserin from 5HT2A receptor
263 4 0 4 3.5 CN(C)CC1=CC=CC=C1OC2=CC(=C(C=C2)F)F
CHEMBL12177 5ht2a_rat Rat No 6.0 IC50 = 1000 Funct
In vitro inhibitory concentration against radioligand [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cortical membraneIn vitro inhibitory concentration against radioligand [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cortical membrane
432 6 1 9 2.5 CC1=C(SC2=C1C(=O)N(C(=N2)SCCCN3CCN(CC3)C4=NC=CC=N4)N)C
CHEMBL54265 5ht2a_rat Rat No 5.0 IC50 = 10000 Funct
Binding activity against 5-hydroxytryptamine 2C receptor from pig cortex membrane using [3H]mesulergine as radioligand.Binding activity against 5-hydroxytryptamine 2C receptor from pig cortex membrane using [3H]mesulergine as radioligand.
255 4 1 3 1.3 CN(C)CCC1=CNC2=C1C=C(C=C2)N3C=NC=N3
CHEMBL26018 5ht2a_bovin Bovine No 5.0 IC50 = 10000 Funct
Binding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortexBinding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortex
447 11 1 6 4.6 CCCN(CCCCNS(=O)(=O)C1=CC=C(C=C1)C)C2CC3=C(C=CC=C3OC)OC2
CHEMBL300735 5ht2a_bovin Bovine No 5.0 IC50 = 10000 Funct
Binding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortexBinding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortex
447 11 1 6 4.6 CCCN(CCCCNS(=O)(=O)C1=CC=C(C=C1)C)C2CC3=C(C=CC=C3OC)OC2
CHEMBL284912 5ht2a_bovin Bovine No 5.0 IC50 = 10000 Funct
Binding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortexBinding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortex
363 9 0 5 3.3 CCCN(CCCCN1CCOCC1)C2CC3=C(C=CC=C3OC)OC2
CHEMBL49 5ht2a_bovin Bovine Yes 5.0 IC50 = 10000 Funct
Binding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortexBinding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortex
386 6 0 6 2.6 C1CCC2(C1)CC(=O)N(C(=O)C2)CCCCN3CCN(CC3)C4=NC=CC=N4
CHEMBL52438 5ht2a_bovin Bovine No 5.0 IC50 = 10000 Funct
Binding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortexBinding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortex
283 5 0 2 5.1 CCCN(CCC)C1CC2=C(C=CC3=CC=CC=C23)OC1
CHEMBL438755 5ht2a_human Human No 5.0 IC50 = 10000 Funct
Binding affinity towards 5-hydroxytryptamine 2A receptor by displacement of [3H]ketanserinBinding affinity towards 5-hydroxytryptamine 2A receptor by displacement of [3H]ketanserin
318 5 0 4 3.4 CCCN1CCN(C2(C1)CC3=C(C=CC=C3OC)OC2)CCC
CHEMBL1852514 5ht2a_human Human No 6.0 IC50 = 1011 Funct
Binding Assay: For serotonin 5-HT2A binding, an aliquot of human recombinant serotonin 5-HT2A receptor (PerkinElmer Life and Analytical Sciences, USA) expressed in CHO-K1 cells (5 ug/well) and 1 nM [3H]Ketanserin (PerkinElmer) were used in the presence of mianserin (20 uM) as a nonspecific. The reaction mixture was incubated for 60 min at 27° C. using 50 mM Tris-HCl (pH 7.4) buffer containing 4 mM CaCl2 and 0.1% ascorbic acid, and harvested through filtermate A glass fiber filter (Wallac, Finland) presoaked in 0.5% polyethyleneimine (PEI) by microbeta filtermate-96 harvester (PerkinElmer) to terminate the reaction, and then washed with ice cold 50 mM Tris-HCl buffer solution (pH 7.4). The filter was then covered with MeltiLex, sealed in a sample bag, dried in an oven. The radioactivity retained in the filter was finally counted using MicroBeta Plus (Wallac). For serotonin 5-HT2C binding, frozen membranes from stable CHO-K1 cell line expressing the human recombinant 5-HT2C receptor.Binding Assay: For serotonin 5-HT2A binding, an aliquot of human recombinant serotonin 5-HT2A receptor (PerkinElmer Life and Analytical Sciences, USA) expressed in CHO-K1 cells (5 ug/well) and 1 nM [3H]Ketanserin (PerkinElmer) were used in the presence of mianserin (20 uM) as a nonspecific. The reaction mixture was incubated for 60 min at 27° C. using 50 mM Tris-HCl (pH 7.4) buffer containing 4 mM CaCl2 and 0.1% ascorbic acid, and harvested through filtermate A glass fiber filter (Wallac, Finland) presoaked in 0.5% polyethyleneimine (PEI) by microbeta filtermate-96 harvester (PerkinElmer) to terminate the reaction, and then washed with ice cold 50 mM Tris-HCl buffer solution (pH 7.4). The filter was then covered with MeltiLex, sealed in a sample bag, dried in an oven. The radioactivity retained in the filter was finally counted using MicroBeta Plus (Wallac). For serotonin 5-HT2C binding, frozen membranes from stable CHO-K1 cell line expressing the human recombinant 5-HT2C receptor.
442 8 2 5 3.4 CC1=C(C(=CC=C1)N2CCN(CC2)CC(CNC(=O)C3=C(N(C(=N3)C)CC(C)C)C)O)C
CHEMBL1852514 5ht2a_human Human No 6.0 IC50 = 1011 Funct
BindingDB_Patents: Binding Assay. For serotonin 5-HT2A binding, an aliquot of human recombinant serotonin 5-HT2A receptor (PerkinElmer Life and Analytical Sciences, USA) expressed in CHO-K1 cells (5 ug/well) and 1 nM [3H]Ketanserin (PerkinElmer) were used in the presence of mianserin (20 uM) as a nonspecific. The reaction mixture was incubated for 60 min at 27° C. using 50 mM Tris-HCl (pH 7.4) buffer containing 4 mM CaCl2 and 0.1% ascorbic acid, and harvested through filtermate A glass fiber filter (Wallac, Finland) presoaked in 0.5% polyethyleneimine (PEI) by microbeta filtermate-96 harvester (PerkinElmer) to terminate the reaction, and then washed with ice cold 50 mM Tris-HCl buffer solution (pH 7.4). The filter was then covered with MeltiLex, sealed in a sample bag, dried in an oven. The radioactivity retained in the filter was finally counted using MicroBeta Plus (Wallac). For serotonin 5-HT2C binding, frozen membranes from stable CHO-K1 cell line expressing the human recombinant 5-HT2C receptor.BindingDB_Patents: Binding Assay. For serotonin 5-HT2A binding, an aliquot of human recombinant serotonin 5-HT2A receptor (PerkinElmer Life and Analytical Sciences, USA) expressed in CHO-K1 cells (5 ug/well) and 1 nM [3H]Ketanserin (PerkinElmer) were used in the presence of mianserin (20 uM) as a nonspecific. The reaction mixture was incubated for 60 min at 27° C. using 50 mM Tris-HCl (pH 7.4) buffer containing 4 mM CaCl2 and 0.1% ascorbic acid, and harvested through filtermate A glass fiber filter (Wallac, Finland) presoaked in 0.5% polyethyleneimine (PEI) by microbeta filtermate-96 harvester (PerkinElmer) to terminate the reaction, and then washed with ice cold 50 mM Tris-HCl buffer solution (pH 7.4). The filter was then covered with MeltiLex, sealed in a sample bag, dried in an oven. The radioactivity retained in the filter was finally counted using MicroBeta Plus (Wallac). For serotonin 5-HT2C binding, frozen membranes from stable CHO-K1 cell line expressing the human recombinant 5-HT2C receptor.
442 8 2 5 3.4 CC1=C(C(=CC=C1)N2CCN(CC2)CC(CNC(=O)C3=C(N(C(=N3)C)CC(C)C)C)O)C
CHEMBL61177 5ht2a_rat Rat No 6.0 IC50 = 1012 Funct
In vitro binding affinity towards serotonin 5-HT2A receptor by the displacement of [3H]spiperone from rat cortical membranesIn vitro binding affinity towards serotonin 5-HT2A receptor by the displacement of [3H]spiperone from rat cortical membranes
398 6 1 7 3.5 C1CN(CCN1CCCC(C2=CC=C(C3=CC=CC=C32)F)O)C4=NC=C(C=N4)F
CHEMBL1933398 5ht2a_human Human Yes 6.0 IC50 = 1019 Funct
Displacement of [3H]Ketanserin from human recombinant 5HT2A receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Ketanserin from human recombinant 5HT2A receptor expressed in CHOK1 cells after 60 mins
268 3 0 4 1.7 CN1CCC(CC1)N(C)S(=O)(=O)C2=CC=CC=C2
CHEMBL1933398 5ht2a_human Human Yes 6.0 IC50 = 1019 Funct
Displacement of [3H]Ketanserin from human recombinant 5HT2A receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Ketanserin from human recombinant 5HT2A receptor expressed in CHOK1 cells after 60 mins
268 3 0 4 1.7 CN1CCC(CC1)N(C)S(=O)(=O)C2=CC=CC=C2
CHEMBL2158706 5ht2a_rat Rat No 6.0 IC50 = 1020 Funct
Displacement of [3H]-ketanserin from 5HT2A receptor in rat cortical membraneDisplacement of [3H]-ketanserin from 5HT2A receptor in rat cortical membrane
339 7 1 4 3.1 C1CN(CCN1CCC(C2=CC=CC=C2)OC(=O)N)C3=CC=CC=C3
CHEMBL2158706 5ht2a_rat Rat No 6.0 IC50 = 1020 Funct
Displacement of [3H]-ketanserin from 5HT2A receptor in rat cortical membraneDisplacement of [3H]-ketanserin from 5HT2A receptor in rat cortical membrane
339 7 1 4 3.1 C1CN(CCN1CCC(C2=CC=CC=C2)OC(=O)N)C3=CC=CC=C3
CHEMBL595133 5ht2a_human Human No 6.0 IC50 = 1025 Funct
Antagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assay
328 6 2 3 3.0 CCNCCC1=C2C(=CC=C1)NC=C2S(=O)(=O)C3=CC=CC=C3
CHEMBL595133 5ht2a_human Human No 6.0 IC50 = 1025 Funct
Antagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assay
328 6 2 3 3.0 CCNCCC1=C2C(=CC=C1)NC=C2S(=O)(=O)C3=CC=CC=C3
CHEMBL116735 5ht2a_human Human No 6.0 IC50 = 1030 Funct
Inhibition of human 5-hydroxytryptamine 2A receptorInhibition of human 5-hydroxytryptamine 2A receptor
481 9 0 5 5.8 C1CN(CCN1CCCC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)C(=O)CCC4=CC=C(C=C4)F
CHEMBL232997 5ht2a_rat Rat No 7.0 IC50 = 104 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
277 4 2 5 -1.1 CC(CC1=C2C(=C(C3=C1CCO3)CC(=O)O)CCO2)N
CHEMBL1080711 5ht2a_human Human No 7.0 IC50 = 104 Funct
Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cells after 60 minsDisplacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cells after 60 mins
528 10 1 3 6.4 CCCN1C(=C(C=C1C2=CC=CC=C2)C(=O)NCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl)C
CHEMBL232997 5ht2a_rat Rat No 7.0 IC50 = 104 Funct
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortexDisplacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
277 4 2 5 -1.1 CC(CC1=C2C(=C(C3=C1CCO3)CC(=O)O)CCO2)N
CHEMBL1080711 5ht2a_human Human No 7.0 IC50 = 104 Funct
Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cells after 60 minsDisplacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cells after 60 mins
528 10 1 3 6.4 CCCN1C(=C(C=C1C2=CC=CC=C2)C(=O)NCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl)C
CHEMBL54 5ht2a_rat Rat Yes 7.0 IC50 = 104 Funct
Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptorInhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor
376 6 1 4 3.2 C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CCCC(=O)C3=CC=C(C=C3)F
CHEMBL44 5ht2a_human Human Yes 5.0 IC50 = 10469 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
270 1 3 5 2.7 C1=CC(=CC=C1C2=COC3=CC(=CC(=C3C2=O)O)O)O
CHEMBL44 5ht2a_human Human Yes 5.0 IC50 = 10469 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
270 1 3 5 2.7 C1=CC(=CC=C1C2=COC3=CC(=CC(=C3C2=O)O)O)O
CHEMBL53416 5ht2a_bovin Bovine No 5.0 IC50 = 10471.3 Funct
Binding affinity against 5-hydroxytryptamine 2A receptor was measured using [3H]ketanserin as radioligandBinding affinity against 5-hydroxytryptamine 2A receptor was measured using [3H]ketanserin as radioligand
342 3 0 3 4.6 C1CN(CCN1CC2=CC=CC=C2)C3=NC4=CC=CC=C4N5C3=CC=C5
CHEMBL1852617 5ht2a_human Human No 7.0 IC50 = 105 Funct
Binding Assay: For serotonin 5-HT2A binding, an aliquot of human recombinant serotonin 5-HT2A receptor (PerkinElmer Life and Analytical Sciences, USA) expressed in CHO-K1 cells (5 ug/well) and 1 nM [3H]Ketanserin (PerkinElmer) were used in the presence of mianserin (20 uM) as a nonspecific. The reaction mixture was incubated for 60 min at 27° C. using 50 mM Tris-HCl (pH 7.4) buffer containing 4 mM CaCl2 and 0.1% ascorbic acid, and harvested through filtermate A glass fiber filter (Wallac, Finland) presoaked in 0.5% polyethyleneimine (PEI) by microbeta filtermate-96 harvester (PerkinElmer) to terminate the reaction, and then washed with ice cold 50 mM Tris-HCl buffer solution (pH 7.4). The filter was then covered with MeltiLex, sealed in a sample bag, dried in an oven. The radioactivity retained in the filter was finally counted using MicroBeta Plus (Wallac). For serotonin 5-HT2C binding, frozen membranes from stable CHO-K1 cell line expressing the human recombinant 5-HT2C receptor.Binding Assay: For serotonin 5-HT2A binding, an aliquot of human recombinant serotonin 5-HT2A receptor (PerkinElmer Life and Analytical Sciences, USA) expressed in CHO-K1 cells (5 ug/well) and 1 nM [3H]Ketanserin (PerkinElmer) were used in the presence of mianserin (20 uM) as a nonspecific. The reaction mixture was incubated for 60 min at 27° C. using 50 mM Tris-HCl (pH 7.4) buffer containing 4 mM CaCl2 and 0.1% ascorbic acid, and harvested through filtermate A glass fiber filter (Wallac, Finland) presoaked in 0.5% polyethyleneimine (PEI) by microbeta filtermate-96 harvester (PerkinElmer) to terminate the reaction, and then washed with ice cold 50 mM Tris-HCl buffer solution (pH 7.4). The filter was then covered with MeltiLex, sealed in a sample bag, dried in an oven. The radioactivity retained in the filter was finally counted using MicroBeta Plus (Wallac). For serotonin 5-HT2C binding, frozen membranes from stable CHO-K1 cell line expressing the human recombinant 5-HT2C receptor.
474 8 1 4 5.6 CC1=C(C(=CC=C1)N2CCN(CC2)CCCNC(=O)C3=C(N(C(=N3)C(C)C)C4=CC=CC=C4)C)C
CHEMBL500329 5ht2a_human Human No 7.0 IC50 = 105 Funct
Displacement of [3H]ketanserin from 5HT2A receptorDisplacement of [3H]ketanserin from 5HT2A receptor
312 5 1 3 4.0 CNCC1=C(C=C(C=C1)OC)OC2=CC(=C(C=C2)Cl)Cl
CHEMBL1852617 5ht2a_human Human No 7.0 IC50 = 105 Funct
BindingDB_Patents: Binding Assay. For serotonin 5-HT2A binding, an aliquot of human recombinant serotonin 5-HT2A receptor (PerkinElmer Life and Analytical Sciences, USA) expressed in CHO-K1 cells (5 ug/well) and 1 nM [3H]Ketanserin (PerkinElmer) were used in the presence of mianserin (20 uM) as a nonspecific. The reaction mixture was incubated for 60 min at 27° C. using 50 mM Tris-HCl (pH 7.4) buffer containing 4 mM CaCl2 and 0.1% ascorbic acid, and harvested through filtermate A glass fiber filter (Wallac, Finland) presoaked in 0.5% polyethyleneimine (PEI) by microbeta filtermate-96 harvester (PerkinElmer) to terminate the reaction, and then washed with ice cold 50 mM Tris-HCl buffer solution (pH 7.4). The filter was then covered with MeltiLex, sealed in a sample bag, dried in an oven. The radioactivity retained in the filter was finally counted using MicroBeta Plus (Wallac). For serotonin 5-HT2C binding, frozen membranes from stable CHO-K1 cell line expressing the human recombinant 5-HT2C receptor.BindingDB_Patents: Binding Assay. For serotonin 5-HT2A binding, an aliquot of human recombinant serotonin 5-HT2A receptor (PerkinElmer Life and Analytical Sciences, USA) expressed in CHO-K1 cells (5 ug/well) and 1 nM [3H]Ketanserin (PerkinElmer) were used in the presence of mianserin (20 uM) as a nonspecific. The reaction mixture was incubated for 60 min at 27° C. using 50 mM Tris-HCl (pH 7.4) buffer containing 4 mM CaCl2 and 0.1% ascorbic acid, and harvested through filtermate A glass fiber filter (Wallac, Finland) presoaked in 0.5% polyethyleneimine (PEI) by microbeta filtermate-96 harvester (PerkinElmer) to terminate the reaction, and then washed with ice cold 50 mM Tris-HCl buffer solution (pH 7.4). The filter was then covered with MeltiLex, sealed in a sample bag, dried in an oven. The radioactivity retained in the filter was finally counted using MicroBeta Plus (Wallac). For serotonin 5-HT2C binding, frozen membranes from stable CHO-K1 cell line expressing the human recombinant 5-HT2C receptor.
474 8 1 4 5.6 CC1=C(C(=CC=C1)N2CCN(CC2)CCCNC(=O)C3=C(N(C(=N3)C(C)C)C4=CC=CC=C4)C)C
CHEMBL500329 5ht2a_human Human No 7.0 IC50 = 105 Funct
Displacement of [3H]ketanserin from 5HT2A receptorDisplacement of [3H]ketanserin from 5HT2A receptor
312 5 1 3 4.0 CNCC1=C(C=C(C=C1)OC)OC2=CC(=C(C=C2)Cl)Cl
CHEMBL3805600 5ht2a_human Human No 6.0 IC50 = 1050 Funct
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
436 8 1 4 4.7 CC(=O)NC1=CC(=CC=C1)OCCCCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL488242 5ht2a_human Human Yes 6.0 IC50 = 1050 Funct
Displacement of [3H]ketanserin from 5HT2A receptorDisplacement of [3H]ketanserin from 5HT2A receptor
248 4 1 2 3.4 CNCC1=CC=CC=C1OC2=CC=C(C=C2)Cl
CHEMBL3805600 5ht2a_human Human No 6.0 IC50 = 1050 Funct
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
436 8 1 4 4.7 CC(=O)NC1=CC(=CC=C1)OCCCCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL488242 5ht2a_human Human Yes 6.0 IC50 = 1050 Funct
Displacement of [3H]ketanserin from 5HT2A receptorDisplacement of [3H]ketanserin from 5HT2A receptor
248 4 1 2 3.4 CNCC1=CC=CC=C1OC2=CC=C(C=C2)Cl
CHEMBL342518 5ht2a_rat Rat No 7.0 IC50 = 106 Funct
Binding affinity towards rat 5-hydroxytryptamine 2A receptor was evaluated using [3H]- ketanserin as radioligandBinding affinity towards rat 5-hydroxytryptamine 2A receptor was evaluated using [3H]- ketanserin as radioligand
348 5 0 3 4.4 COC1=CC2=C(CCC(=C2)CCN3CCN(CC3)C4=CC=CC=C4)C=C1
CHEMBL325516 5ht2a_human Human No 6.0 IC50 = 1060 Funct
Inhibition of human 5-hydroxytryptamine 2A receptorInhibition of human 5-hydroxytryptamine 2A receptor
497 10 0 6 6.3 C1CN(CCN1CCCC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)C(=O)OCCC4=CC=C(C=C4)F
CHEMBL1081303 5ht2a_human Human No 6.0 IC50 = 1067 Funct
Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cells after 60 minsDisplacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cells after 60 mins
533 9 1 3 6.9 CC1=C(C=C(N1CC2CCCCC2)C3=CC=CC=C3)C(=O)NCCCN4CCN(CC4)C5=CC(=CC=C5)Cl
CHEMBL1081303 5ht2a_human Human No 6.0 IC50 = 1067 Funct
Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cells after 60 minsDisplacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cells after 60 mins
533 9 1 3 6.9 CC1=C(C=C(N1CC2CCCCC2)C3=CC=CC=C3)C(=O)NCCCN4CCN(CC4)C5=CC(=CC=C5)Cl
CHEMBL3600801 5ht2a_human Human No 7.0 IC50 = 107 Funct
Inhibition of 5HT2A receptor (unknown origin)Inhibition of 5HT2A receptor (unknown origin)
419 7 1 2 5.7 C1CCN(C1)CC2=CC=C(C=C2)CCNC(=O)C3=CC=C(C=C3)C4=CC=C(C=C4)Cl
CHEMBL3600801 5ht2a_human Human No 7.0 IC50 = 107 Funct
Inhibition of 5HT2A receptor (unknown origin)Inhibition of 5HT2A receptor (unknown origin)
419 7 1 2 5.7 C1CCN(C1)CC2=CC=C(C=C2)CCNC(=O)C3=CC=C(C=C3)C4=CC=C(C=C4)Cl
CHEMBL2158794 5ht2a_rat Rat Yes 6.0 IC50 = 1070 Funct
Displacement of [3H]-ketanserin from 5HT2A receptor in rat cortical membraneDisplacement of [3H]-ketanserin from 5HT2A receptor in rat cortical membrane
294 5 0 3 3.2 C1CN(CCN1CCC(=O)C2=CC=CC=C2)C3=CC=CC=C3
CHEMBL2158794 5ht2a_rat Rat Yes 6.0 IC50 = 1070 Funct
Displacement of [3H]-ketanserin from 5HT2A receptor in rat cortical membraneDisplacement of [3H]-ketanserin from 5HT2A receptor in rat cortical membrane
294 5 0 3 3.2 C1CN(CCN1CCC(=O)C2=CC=CC=C2)C3=CC=CC=C3
CHEMBL64948 5ht2a_bovin Bovine No 6.0 IC50 = 1071.5 Funct
Binding affinity towards 5-hydroxytryptamine 2A receptorBinding affinity towards 5-hydroxytryptamine 2A receptor
300 3 0 4 4.0 CCCN1CCN(CC1)C2=NC3=C(N4C2=CC=C4)SC=C3
CHEMBL606150 5ht2a_human Human No 6.0 IC50 = 1078 Funct
Antagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assay
342 7 2 3 3.6 CCCNCCC1=C2C(=CC=C1)NC=C2S(=O)(=O)C3=CC=CC=C3
CHEMBL606150 5ht2a_human Human No 6.0 IC50 = 1078 Funct
Antagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assay
342 7 2 3 3.6 CCCNCCC1=C2C(=CC=C1)NC=C2S(=O)(=O)C3=CC=CC=C3
CHEMBL63790 5ht2a_bovin Bovine No 5.0 IC50 = 10964.8 Funct
Binding affinity towards 5-hydroxytryptamine 2A receptorBinding affinity towards 5-hydroxytryptamine 2A receptor
392 3 0 6 4.4 C1CN(CCN1CC2=CC3=C(C=C2)OCO3)C4=NC5=C(N6C4=CC=C6)SC=C5
CHEMBL565745 5ht2a_human Human No 8.0 IC50 = 11 Funct
Displacement of [125I]DOI from human cloned 5HT2A receptor expressed in CHO cellsDisplacement of [125I]DOI from human cloned 5HT2A receptor expressed in CHO cells
336 4 1 4 1.7 C1=CC(=CC(=C1)Cl)S(=O)(=O)C2=CN(C3=C2C=CC=N3)CCN
CHEMBL375369 5ht2a_human Human No 8.0 IC50 = 11 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
257 3 2 2 2.4 CC1=CC=C(C=C1)C2=CC(=NCCN2)NC(C)(C)C
CHEMBL221297 5ht2a_human Human No 8.0 IC50 = 11 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
279 3 2 4 2.3 CC(C)(C)NC1=NCCNC(=C1)C2=C(C=C(C=C2)F)F
CHEMBL565745 5ht2a_human Human No 8.0 IC50 = 11 Funct
Displacement of [125I]DOI from human cloned 5HT2A receptor expressed in CHO cellsDisplacement of [125I]DOI from human cloned 5HT2A receptor expressed in CHO cells
336 4 1 4 1.7 C1=CC(=CC(=C1)Cl)S(=O)(=O)C2=CN(C3=C2C=CC=N3)CCN
CHEMBL375369 5ht2a_human Human No 8.0 IC50 = 11 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
257 3 2 2 2.4 CC1=CC=C(C=C1)C2=CC(=NCCN2)NC(C)(C)C
CHEMBL221297 5ht2a_human Human No 8.0 IC50 = 11 Funct
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cellsDisplacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells
279 3 2 4 2.3 CC(C)(C)NC1=NCCNC(=C1)C2=C(C=C(C=C2)F)F
CHEMBL153626 5ht2a_rat Rat No 8.0 IC50 = 11.3 Funct
Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptorInhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor
436 6 0 7 4.4 CC1=COC2=C(C1=O)C=CC(=C2)OCCCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F
CHEMBL412876 5ht2a_rat Rat Yes 7.9 IC50 = 11.5 Funct
In vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortexIn vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex
244 3 1 2 2.7 CN(C)CCC1=CNC2=C1C3=C(C=C2)OCCC3
CHEMBL600210 5ht2a_human Human No 7.9 IC50 = 11.6 Funct
Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in avCHO-K1 cellsDisplacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in avCHO-K1 cells
536 10 0 6 6.6 COC1=CC=CC=C1N2CCN(CC2)CCCN(CC3CCCCC3)S(=O)(=O)C4=CC5=CC=CC=C5C=C4
CHEMBL600210 5ht2a_human Human No 7.9 IC50 = 11.6 Funct
Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in avCHO-K1 cellsDisplacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in avCHO-K1 cells
536 10 0 6 6.6 COC1=CC=CC=C1N2CCN(CC2)CCCN(CC3CCCCC3)S(=O)(=O)C4=CC5=CC=CC=C5C=C4
CHEMBL2158716 5ht2a_rat Rat No 7.0 IC50 = 110 Funct
Binding Assay: 6-week-old Sprague-Dawley (SD) rats were anesthetized in an ether container for 5 minutes, brains were separated from rats, and cortical regions were then separated from the brains of the rats. The cortical regions of the rats were put into a Tris-HCl buffer solution (50 mM, pH 7.7) and homogenized, and the homogenate was centrifuged twice at 4 C. at a rotary speed of 50,000 g to obtain a precipitate (membrane protein). The precipitate was put into a buffer solution, and homogenized, which was used later as a protein source. 0.5 nM [3H]-Ketanserin was used as a radioactive isotope, and 10 uM serotonin was used to remove non-specific bindings. 25 ul of the compound, 100 ul of an aqueous radioactive isotope solution, and 100 ul of the protein source were put together, and kept at 25 C. for 1 hour. The resulting mixture was filtered with a membrane filter in a 96-well harvester when the 96-well plate reaction was completed.Binding Assay: 6-week-old Sprague-Dawley (SD) rats were anesthetized in an ether container for 5 minutes, brains were separated from rats, and cortical regions were then separated from the brains of the rats. The cortical regions of the rats were put into a Tris-HCl buffer solution (50 mM, pH 7.7) and homogenized, and the homogenate was centrifuged twice at 4 C. at a rotary speed of 50,000 g to obtain a precipitate (membrane protein). The precipitate was put into a buffer solution, and homogenized, which was used later as a protein source. 0.5 nM [3H]-Ketanserin was used as a radioactive isotope, and 10 uM serotonin was used to remove non-specific bindings. 25 ul of the compound, 100 ul of an aqueous radioactive isotope solution, and 100 ul of the protein source were put together, and kept at 25 C. for 1 hour. The resulting mixture was filtered with a membrane filter in a 96-well harvester when the 96-well plate reaction was completed.
357 7 1 5 3.2 C1CN(CCN1CCC(C2=CC=CC=C2)OC(=O)N)C3=CC=CC=C3F
CHEMBL2158716 5ht2a_rat Rat No 7.0 IC50 = 110 Funct
Displacement of [3H]-ketanserin from 5HT2A receptor in rat cortical membraneDisplacement of [3H]-ketanserin from 5HT2A receptor in rat cortical membrane
357 7 1 5 3.2 C1CN(CCN1CCC(C2=CC=CC=C2)OC(=O)N)C3=CC=CC=C3F
CHEMBL1154 5ht2a_rat Rat Yes 7.0 IC50 = 110 Funct
Binding affinity against rat 5-hydroxytryptamine 2 receptor in rat cerebral cortex tissue using [3H]spiperone as radioligandBinding affinity against rat 5-hydroxytryptamine 2 receptor in rat cerebral cortex tissue using [3H]spiperone as radioligand
219 1 1 4 2.1 C1CN(CCN1)C2=NSC3=CC=CC=C32
CHEMBL332385 5ht2a_rat Rat No 7.0 IC50 = 110 Funct
Binding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranesBinding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranes
429 8 1 3 4.0 CN(CCCCN1CCNC1=O)CC2=CN(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F
CHEMBL73589 5ht2a_rat Rat No 7.0 IC50 = 110 Funct
Binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligandBinding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligand
457 3 0 9 3.7 CN1CCN(CC1)C2=NC3=CC=CC=C3SC4=C2C=C(C=C4)OS(=O)(=O)C(F)(F)F
CHEMBL2158716 5ht2a_rat Rat No 7.0 IC50 = 110 Funct
BindingDB_Patents: Binding Assay. 6-week-old Sprague-Dawley (SD) rats were anesthetized in an ether container for 5 minutes, brains were separated from rats, and cortical regions were then separated from the brains of the rats. The cortical regions of the rats were put into a Tris-HCl buffer solution (50 mM, pH 7.7) and homogenized, and the homogenate was centrifuged twice at 4 C. at a rotary speed of 50,000 g to obtain a precipitate (membrane protein). The precipitate was put into a buffer solution, and homogenized, which was used later as a protein source. 0.5 nM [3H]-Ketanserin was used as a radioactive isotope, and 10 uM serotonin was used to remove non-specific bindings. 25 ul of the compound, 100 ul of an aqueous radioactive isotope solution, and 100 ul of the protein source were put together, and kept at 25 C. for 1 hour. The resulting mixture was filtered with a membrane filter in a 96-well harvester when the 96-well plate reaction was completed.BindingDB_Patents: Binding Assay. 6-week-old Sprague-Dawley (SD) rats were anesthetized in an ether container for 5 minutes, brains were separated from rats, and cortical regions were then separated from the brains of the rats. The cortical regions of the rats were put into a Tris-HCl buffer solution (50 mM, pH 7.7) and homogenized, and the homogenate was centrifuged twice at 4 C. at a rotary speed of 50,000 g to obtain a precipitate (membrane protein). The precipitate was put into a buffer solution, and homogenized, which was used later as a protein source. 0.5 nM [3H]-Ketanserin was used as a radioactive isotope, and 10 uM serotonin was used to remove non-specific bindings. 25 ul of the compound, 100 ul of an aqueous radioactive isotope solution, and 100 ul of the protein source were put together, and kept at 25 C. for 1 hour. The resulting mixture was filtered with a membrane filter in a 96-well harvester when the 96-well plate reaction was completed.
357 7 1 5 3.2 C1CN(CCN1CCC(C2=CC=CC=C2)OC(=O)N)C3=CC=CC=C3F
CHEMBL2158716 5ht2a_rat Rat No 7.0 IC50 = 110 Funct
Displacement of [3H]-ketanserin from 5HT2A receptor in rat cortical membraneDisplacement of [3H]-ketanserin from 5HT2A receptor in rat cortical membrane
357 7 1 5 3.2 C1CN(CCN1CCC(C2=CC=CC=C2)OC(=O)N)C3=CC=CC=C3F
CHEMBL3805077 5ht2a_human Human No 6.0 IC50 = 1100 Funct
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
436 8 1 4 4.8 CNC(=O)C1=CC(=CC=C1)OCCCCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3806169 5ht2a_human Human No 6.0 IC50 = 1100 Funct
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
422 8 1 4 4.4 C1CN(CCN1CCCCOC2=CC=CC(=C2)C(=O)N)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3805826 5ht2a_human Human No 6.0 IC50 = 1100 Funct
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
492 12 1 4 6.6 CCCCCNC(=O)C1=CC(=CC=C1)OCCCCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL259415 5ht2a_human Human No 6.0 IC50 = 1100 Funct
Binding affinity at 5HT2A receptorBinding affinity at 5HT2A receptor
510 8 1 5 4.4 CC1=C(C(=CC=C1)N2CCN(CC2)CCCC(=O)NCC3=NC4=CC=CC=C4C(=O)N3C5=CC=CC=C5)C
CHEMBL60447 5ht2a_bovin Bovine No 6.0 IC50 = 1100 Funct
Affinity towards 5-hydroxytryptamine 2A receptor in membranes from bovine frontal cortex using [3H]ketanserinAffinity towards 5-hydroxytryptamine 2A receptor in membranes from bovine frontal cortex using [3H]ketanserin
369 4 1 5 3.4 CN1C2=C(C=C(C=C2)CCN3CCN(CC3)C4=CC=CC=C4O)SC1=O
CHEMBL3805077 5ht2a_human Human No 6.0 IC50 = 1100 Funct
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
436 8 1 4 4.8 CNC(=O)C1=CC(=CC=C1)OCCCCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3806169 5ht2a_human Human No 6.0 IC50 = 1100 Funct
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
422 8 1 4 4.4 C1CN(CCN1CCCCOC2=CC=CC(=C2)C(=O)N)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3805826 5ht2a_human Human No 6.0 IC50 = 1100 Funct
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
492 12 1 4 6.6 CCCCCNC(=O)C1=CC(=CC=C1)OCCCCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL259415 5ht2a_human Human No 6.0 IC50 = 1100 Funct
Binding affinity at 5HT2A receptorBinding affinity at 5HT2A receptor
510 8 1 5 4.4 CC1=C(C(=CC=C1)N2CCN(CC2)CCCC(=O)NCC3=NC4=CC=CC=C4C(=O)N3C5=CC=CC=C5)C
CHEMBL343282 5ht2a_rat Rat No 6.0 IC50 = 1100 Funct
Binding affinity for 5-hydroxytryptamine 2A receptor, activity is expressed as IC50 values.Binding affinity for 5-hydroxytryptamine 2A receptor, activity is expressed as IC50 values.
347 2 1 3 3.9 CC1(CN(CCN1)C2CC(C3=C2C=C(C=C3)Cl)C4=CSC=C4)C
CHEMBL313714 5ht2a_human Human Yes 6.0 IC50 = 1100 Funct
Compound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 2A receptor stably expressed in CHO cellsCompound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 2A receptor stably expressed in CHO cells
463 9 3 6 2.9 C1CN(CCC1NC(CO)C2=CC=C(C=C2)F)CCCC3=CNC4=C3C=C(C=C4)N5C=NN=C5
CHEMBL593527 5ht2a_human Human No 6.0 IC50 = 1105 Funct
Antagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assay
314 5 2 3 2.7 CNCCC1=C2C(=CC=C1)NC=C2S(=O)(=O)C3=CC=CC=C3
CHEMBL593527 5ht2a_human Human No 6.0 IC50 = 1105 Funct
Antagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilizati