Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL199824 5ht1a_human Human Yes 11.0 EC50 = 0.0 nM Funct
Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulationAgonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation
423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1
CHEMBL2068762 5ht1a_human Human Yes 11.0 EC50 = 0.0 nM Funct
Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulationAgonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation
423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1
CHEMBL4790600 5ht1a_human Human No 11.0 EC50 = 0.0 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
478 7 1 4 4.8 CC1(C)Cc2cccc(OCCNCC3(F)CCN(C(=O)c4ccc(F)c(Cl)c4)CC3)c2O1
CHEMBL4757755 5ht1a_human Human No 10.9 EC50 = 0.0 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
449 7 2 4 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3c2CCN3)CC1
CHEMBL4755058 5ht1a_human Human No 10.9 EC50 = 0.0 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
465 8 2 4 4.1 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL4752177 5ht1a_human Human No 10.6 EC50 = 0.0 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
481 8 2 4 4.6 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1
CHEMBL4756233 5ht1a_human Human No 10.5 EC50 = 0.0 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
447 7 2 3 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1
CHEMBL1290716 5ht1a_human Human No 10.5 EC50 = 0.0 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
412 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)CC3)cccc2n1
CHEMBL199824 5ht1a_human Human Yes 10.3 EC50 = 0.1 nM Funct
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1
CHEMBL2068762 5ht1a_human Human Yes 10.3 EC50 = 0.1 nM Funct
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1
CHEMBL4752177 5ht1a_human Human No 10.2 EC50 = 0.1 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
481 8 2 4 4.6 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1
CHEMBL4796345 5ht1a_human Human No 10.1 EC50 = 0.1 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
437 8 2 4 4.1 CNc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL3330612 5ht1a_human Human Yes 10.1 EC50 = 0.1 nM Funct
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
344 6 0 8 -0.1 Cn1c(=O)cnn(CCCCN2CCN(c3ccccn3)CC2)c1=O
CHEMBL4756233 5ht1a_human Human No 10.1 EC50 = 0.1 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
447 7 2 3 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1
CHEMBL4796345 5ht1a_human Human No 10.1 EC50 = 0.1 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
437 8 2 4 4.1 CNc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL4633397 5ht1a_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
426 6 0 8 2.8 O=c1n(CCCCN2CCN(c3cccc4scnc34)CC2)nc2c(F)cccn12
CHEMBL4647011 5ht1a_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
425 6 0 7 3.5 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2ccc(F)cn12
CHEMBL4648027 5ht1a_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
475 6 0 7 4.6 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(Cl)cc(Cl)cn12
CHEMBL2413154 5ht1a_human Human Yes 10.0 EC50 = 0.1 nM Funct
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1
CHEMBL2413154 5ht1a_human Human Yes 10.0 EC50 = 0.1 nM Funct
Partial agonist activity at human 5HT1A receptor expressed in CHO cells assessed as increase in [35S]GTPgammaS bindingPartial agonist activity at human 5HT1A receptor expressed in CHO cells assessed as increase in [35S]GTPgammaS binding
373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1
CHEMBL4796345 5ht1a_human Human No 10.0 EC50 = 0.1 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
437 8 2 4 4.1 CNc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL439849 5ht1a_human Human Yes 9.9 EC50 = 0.1 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2
CHEMBL439849 5ht1a_human Human Yes 9.9 EC50 = 0.1 nM Funct
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2
CHEMBL276031 5ht1a_human Human Yes 9.9 EC50 = 0.1 nM Funct
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1
CHEMBL4751777 5ht1a_human Human No 9.9 EC50 = 0.1 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
438 8 1 4 4.1 COc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1
CHEMBL4755058 5ht1a_human Human No 9.8 EC50 = 0.2 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
465 8 2 4 4.1 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL4777581 5ht1a_human Human No 9.7 EC50 = 0.2 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
451 8 2 4 3.2 NC(=O)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL3330616 5ht1a_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
362 6 0 8 0.1 Cn1c(=O)cnn(CCCCN2CCN(c3cccc(F)n3)CC2)c1=O
CHEMBL426317 5ht1a_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cellsAgonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cells
373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1
CHEMBL3330603 5ht1a_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
343 6 0 7 0.5 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3)CC2)c1=O
CHEMBL4751777 5ht1a_human Human No 9.5 EC50 = 0.3 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
438 8 1 4 4.1 COc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1
CHEMBL511857 5ht1a_human Human No 9.5 EC50 = 0.3 nM Bind
Agonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assayAgonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assay
351 4 0 4 3.9 COc1cccc([C@H]2CC[C@H](N3CCN(c4ccccn4)CC3)CC2)c1
CHEMBL4790600 5ht1a_human Human No 9.5 EC50 = 0.3 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
478 7 1 4 4.8 CC1(C)Cc2cccc(OCCNCC3(F)CCN(C(=O)c4ccc(F)c(Cl)c4)CC3)c2O1
CHEMBL4756041 5ht1a_human Human No 9.5 EC50 = 0.3 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
459 7 1 4 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1
CHEMBL127171 5ht1a_human Human No 9.5 EC50 = 0.3 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
360 9 2 3 4.1 COc1ccc(F)cc1OCCNCCCc1c[nH]c2ccc(F)cc12
CHEMBL4128200 5ht1a_human Human No 9.5 EC50 = 0.4 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
531 6 2 4 6.1 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(Br)cc56)CC4)c13)CCCC2
CHEMBL4126644 5ht1a_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1
CHEMBL4751777 5ht1a_human Human No 9.4 EC50 = 0.4 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
438 8 1 4 4.1 COc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1
CHEMBL4786067 5ht1a_human Human No 9.4 EC50 = 0.4 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
438 8 1 4 4.1 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL4753328 5ht1a_human Human Yes 9.4 EC50 = 0.4 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
409 7 1 4 3.5 C1CN(CCC1(CNCCOC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL39 5ht1a_human Human Yes 9.3 EC50 = 0.5 nM Funct
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL4756041 5ht1a_human Human No 9.3 EC50 = 0.5 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
459 7 1 4 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1
CHEMBL4741908 5ht1a_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
421 6 0 5 4.2 O=C1COc2ccccc2N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL4128689 5ht1a_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
464 6 2 5 4.8 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCC6)CC3)c2c1
CHEMBL4752177 5ht1a_human Human No 9.2 EC50 = 0.6 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
481 8 2 4 4.6 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1
CHEMBL4130230 5ht1a_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
467 6 2 4 5.6 Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1
CHEMBL2413153 5ht1a_human Human Yes 9.2 EC50 = 0.7 nM Funct
Partial agonist activity at human 5HT1A receptor expressed in CHO cells assessed as increase in [35S]GTPgammaS bindingPartial agonist activity at human 5HT1A receptor expressed in CHO cells assessed as increase in [35S]GTPgammaS binding
405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O
CHEMBL4777581 5ht1a_human Human No 9.2 EC50 = 0.7 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
451 8 2 4 3.2 NC(=O)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL39 5ht1a_human Human Yes 9.2 EC50 = 0.7 nM Funct
Agonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cellsAgonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cells
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL4217182 5ht1a_human Human No 9.2 EC50 = 0.7 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
442 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sc(F)cc34)CC2)ccn1
CHEMBL4129170 5ht1a_human Human No 9.1 EC50 = 0.7 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
471 6 2 4 5.5 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(F)cc56)CC4)c13)CCCC2
CHEMBL46539 5ht1a_human Human No 9.1 EC50 = 0.7 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
445 6 2 4 4.0 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cc[nH]n3)n2)CC1
CHEMBL4127774 5ht1a_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
487 6 2 4 6.0 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(Cl)cc56)CC4)c13)CCCC2
CHEMBL444590 5ht1a_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
365 6 0 4 4.1 COC1=CC=CC2=C1CCCC2CCCN3CCN(CC3)C4=CC=CC=N4
CHEMBL316960 5ht1a_human Human No 9.1 EC50 = 0.8 nM Funct
In vitro potency at human 5-hydroxytryptamine 1A receptor in inhibiting forskolin-stimulated accumulation of intracellular cAMPIn vitro potency at human 5-hydroxytryptamine 1A receptor in inhibiting forskolin-stimulated accumulation of intracellular cAMP
413 5 1 5 2.9 CC1CN(c2cccc3c2OCCO3)CC(C)N1CCNC(=O)c1ccc(F)cc1
CHEMBL81728 5ht1a_human Human No 9.1 EC50 = 0.8 nM Funct
In vitro potency at human 5-hydroxytryptamine 1A receptor in inhibiting forskolin-stimulated accumulation of intracellular cAMPIn vitro potency at human 5-hydroxytryptamine 1A receptor in inhibiting forskolin-stimulated accumulation of intracellular cAMP
385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1
CHEMBL4751542 5ht1a_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
470 6 1 6 3.8 Nc1ccc2c(c1)N(CCCCN1CCN(c3cccc4sccc34)CC1)S(=O)(=O)CC2
CHEMBL511857 5ht1a_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
351 4 0 4 3.9 COc1cccc([C@H]2CC[C@H](N3CCN(c4ccccn4)CC3)CC2)c1
CHEMBL4741857 5ht1a_human Human No 9.1 EC50 = 0.8 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
408 7 1 3 4.1 C1CN(CCC1(CNCCOC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL4741857 5ht1a_human Human No 9.1 EC50 = 0.8 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
408 7 1 3 4.1 C1CN(CCC1(CNCCOC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL3330614 5ht1a_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
362 6 0 8 0.1 Cn1c(=O)cnn(CCCCN2CCN(c3ncccc3F)CC2)c1=O
CHEMBL81728 5ht1a_human Human No 9.1 EC50 = 0.9 nM Funct
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1
CHEMBL4754941 5ht1a_human Human No 9.1 EC50 = 0.9 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
425 7 1 4 4.0 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2ccccn2)CC1
CHEMBL4287980 5ht1a_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
423 6 0 5 3.8 O=C1C2CC=CCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL4214528 5ht1a_human Human No 9.1 EC50 = 0.9 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
436 8 1 5 3.7 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccn1
CHEMBL142862 5ht1a_human Human No 9.0 EC50 = 0.9 nM Funct
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
236 4 1 2 2.4 COc1ccc2[nH]cc(CCN(C)C)c2c1F
CHEMBL81728 5ht1a_human Human No 9.0 EC50 = 1.0 nM Funct
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1
CHEMBL39 5ht1a_human Human Yes 9.0 EC50 = 1 nM Funct
Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulationAgonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL4786067 5ht1a_human Human No 9.0 EC50 = 1.0 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
438 8 1 4 4.1 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL4286905 5ht1a_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
437 6 0 5 4.2 O=C1c2cccc(F)c2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL419240 5ht1a_human Human No 9.0 EC50 = 1.1 nM Bind
Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cellsEffective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells
370 8 2 4 3.7 Fc1ccc2[nH]cc(CCCNCCOc3cccc4c3OCCO4)c2c1
CHEMBL327126 5ht1a_human Human No 9.0 EC50 = 1.1 nM Bind
Stimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cellsStimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells
407 5 1 4 4.2 O[C@H](COc1ccccc1F)CN1CCC2(CC1)OCc1c2ccc2ccccc12
CHEMBL4759331 5ht1a_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
471 6 1 6 3.9 O=S1(=O)CCc2ccc(O)cc2N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL46582 5ht1a_human Human No 9.0 EC50 = 1.1 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
461 6 2 4 4.5 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cc[nH]n3)n2)CC1
CHEMBL4295055 5ht1a_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
453 6 0 5 4.9 O=C1CC2(CCCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL4635414 5ht1a_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
443 6 0 7 3.6 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(F)cc(F)cn12
CHEMBL4126818 5ht1a_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
453 6 2 4 5.3 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccccc56)CC4)c13)CCCC2
CHEMBL149482 5ht1a_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at human 5-HT1AR expressed in HEK293 cells assessed as increase in calcium flux by fluorimetric methodAgonist activity at human 5-HT1AR expressed in HEK293 cells assessed as increase in calcium flux by fluorimetric method
261 6 1 2 3.8 CCCCN(CCC)C1CCc2cccc(O)c2C1
CHEMBL4209188 5ht1a_human Human No 8.9 EC50 = 1.2 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
424 8 1 6 3.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1
CHEMBL326751 5ht1a_human Human No 8.9 EC50 = 1.2 nM Bind
Stimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cellsStimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells
389 5 1 4 4.1 O[C@H](COc1ccccc1)CN1CCC2(CC1)OCc1c2ccc2ccccc12
CHEMBL4286717 5ht1a_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
427 7 0 5 4.4 CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1
CHEMBL139505 5ht1a_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
361 6 0 4 4.0 COC1=CC=CC2=C(C=CC=C21)CCCN3CCN(CC3)C4=CC=CC=N4
CHEMBL2112645 5ht1a_human Human No 8.9 EC50 = 1.3 nM Bind
Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cellsEffective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells
324 9 2 3 3.8 COc1ccccc1OCCNCCCc1c[nH]c2ccccc12
CHEMBL311015 5ht1a_human Human No 8.9 EC50 = 1.3 nM Funct
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
421 6 0 6 2.7 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1
CHEMBL4781985 5ht1a_human Human No 8.9 EC50 = 1.4 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
437 8 2 4 4.1 CNc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1
CHEMBL4638430 5ht1a_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
432 6 0 8 3.2 N#Cc1cccn2c(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)nc12
CHEMBL330827 5ht1a_human Human No 8.9 EC50 = 1.4 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
352 8 3 3 3.8 Fc1ccc2[nH]cc(CCCNCCOc3cccc4[nH]cnc34)c2c1
CHEMBL1926761 5ht1a_human Human Yes 8.8 EC50 = 1.5 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
400 7 1 5 2.6 O=C1c2ccccc2S(=O)(=O)N1CCCCNCC1CCc2ccccc2O1
CHEMBL4649106 5ht1a_human Human No 8.8 EC50 = 1.5 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
443 6 0 7 3.6 O=c1n(CCCCN2CCN(c3cccc4sc(F)cc34)CC2)nc2c(F)cccn12
CHEMBL4125762 5ht1a_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5c(N)c6c(nc45)CCCC6)CC3)c2c1
CHEMBL79161 5ht1a_human Human No 8.8 EC50 = 1.6 nM Funct
Ability to influence the binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptorAbility to influence the binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptor
413 8 1 8 1.9 COc1ccccc1N1CCN(CCCNc2c(C(C)=O)c(C)nn(C)c2=O)CC1
CHEMBL4291215 5ht1a_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
413 6 0 5 4.0 CC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1
CHEMBL331609 5ht1a_human Human No 8.8 EC50 = 1.6 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
334 8 3 3 3.6 c1ccc2c(CCCNCCOc3cccc4[nH]cnc34)c[nH]c2c1
CHEMBL4283546 5ht1a_human Human No 8.8 EC50 = 1.7 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
425 6 0 5 4.0 O=C1C2CCCCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL4638599 5ht1a_human Human No 8.8 EC50 = 1.7 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
407 6 0 7 3.3 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2ccccn12
CHEMBL4644352 5ht1a_human Human No 8.7 EC50 = 1.8 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
425 6 0 7 3.5 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(F)cccn12
CHEMBL4760621 5ht1a_human Human No 8.7 EC50 = 1.9 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
422 7 1 3 4.4 Cc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL4215022 5ht1a_rat Rat No 8.7 EC50 = 2.0 nM Funct
Agonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assay
450 8 0 7 3.9 COc1ccccc1N1CCN(CCCOc2ccc3c(C)cc(=O)oc3c2C(C)=O)CC1
CHEMBL2112882 5ht1a_human Human No 8.7 EC50 = 2.0 nM Funct
Binding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-SBinding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-S
597 6 4 6 2.5 CC(C)C[C@H]1C(=O)N[C@@H](Cc2ccccc2)[C@]2(O)O[C@@](C)(NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)C(=O)N12
CHEMBL297138 5ht1a_human Human No 8.7 EC50 = 2.0 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
444 6 1 5 4.7 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3cnco3)n2)CC1
CHEMBL231471 5ht1a_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
446 6 1 5 4.3 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2nccc(-c3ccco3)n2)CC1
CHEMBL595055 5ht1a_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
439 6 2 3 4.0 CCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2c(F)cc3c(c2C1)C(=O)NCC3
CHEMBL218261 5ht1a_human Human Yes 8.0 EC50 = 10 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
363 7 1 3 5.1 CC1(C)Cc2cccc(OCCNCc3cccc(C4=CCCC4)c3)c2O1
CHEMBL39 5ht1a_human Human Yes 8.0 EC50 = 10 nM Funct
Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL42766 5ht1a_human Human No 8.0 EC50 = 10 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
404 6 1 4 3.5 CN(C)c1cccc(CNCC2(F)CCN(C(=O)c3cccc(Cl)c3)CC2)n1
CHEMBL39 5ht1a_rat Rat Yes 8.0 EC50 = 10 nM Funct
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL1259241 5ht1a_human Human No 8.0 EC50 = 10 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1
CHEMBL4102561 5ht1a_human Human No 8.0 EC50 = 10.2 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
420 4 1 7 3.3 Cc1nc2c(O)cccn2c(=O)c1CCN1CCN(c2cccc3sccc23)CC1
CHEMBL4074326 5ht1a_human Human No 8.0 EC50 = 10.2 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
406 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCC=C2
CHEMBL4116465 5ht1a_human Human No 8.0 EC50 = 10.2 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
406 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCC=C2
CHEMBL4797282 5ht1a_human Human No 8.0 EC50 = 10.2 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(Cl)c2)CC1
CHEMBL4741857 5ht1a_human Human No 8.0 EC50 = 10.5 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
408 7 1 3 4.1 C1CN(CCC1(CNCCOC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL4741857 5ht1a_human Human No 8.0 EC50 = 10.5 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
408 7 1 3 4.1 C1CN(CCC1(CNCCOC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL4094825 5ht1a_human Human No 8.0 EC50 = 10.5 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
404 4 0 6 3.6 Cc1nc2ccccn2c(=O)c1CCN1CCN(c2cccc3sccc23)CC1
CHEMBL4280084 5ht1a_human Human No 8.0 EC50 = 10.5 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
457 6 2 7 1.9 O=C1C2CC(O)C(O)CC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL4289238 5ht1a_human Human No 8.0 EC50 = 10.6 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
453 6 0 5 3.8 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sc(F)cc23)CC1
CHEMBL45423 5ht1a_human Human No 8.0 EC50 = 10.7 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
450 6 1 4 4.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(N3CCC3)n2)CC1
CHEMBL56 5ht1a_human Human Yes 8.0 EC50 = 10.9 nM Funct
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL4777098 5ht1a_human Human No 8.0 EC50 = 11.0 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
462 6 0 5 3.9 CN1CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)c2ccccc2C1=O
CHEMBL4438036 5ht1a_human Human No 7.0 EC50 = 100 nM Bind
Agonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assayAgonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assay
354 4 2 4 2.7 C=C[C@H]1CN2CCc3c([nH]c4ccccc34)[C@H]2C[C@@H]1[C@@H](CO)C(=O)OC
CHEMBL4747425 5ht1a_human Human No 7.0 EC50 = 100 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(F)cc2)CC1
CHEMBL1259055 5ht1a_human Human No 7.0 EC50 = 100 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
380 5 2 3 3.6 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc4[nH]ccc4c3)CC2)nc1
CHEMBL592939 5ht1a_human Human No 7.0 EC50 = 101 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
465 7 2 3 4.4 O=C1NCCc2cc(F)c3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3
CHEMBL3805772 5ht1a_human Human No 7.0 EC50 = 101 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
449 9 1 4 4.7 CCNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1
CHEMBL4532185 5ht1a_human Human No 5.0 EC50 = 10100 nM Bind
Agonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assayAgonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assay
398 4 1 6 2.4 C=C[C@H]1CN2CC[C@]3(O[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC)C(=O)Nc1ccccc13
CHEMBL4781985 5ht1a_human Human No 7.0 EC50 = 102.3 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
437 8 2 4 4.1 CNc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1
CHEMBL4463843 5ht1a_human Human Yes 5.0 EC50 = 10200 nM Bind
Agonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assayAgonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assay
544 4 5 11 -0.6 COC(=O)C1=CO[C@@H](O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@H]2[C@@H]1C[C@@]13O[C@H]2CN1CCc1c3[nH]c2ccccc12
CHEMBL519266 5ht1a_human Human Yes 5.0 EC50 = 10300 nM Bind
Agonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assayAgonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assay
384 4 1 5 2.7 CC[C@H]1CN2CC[C@]3(C(=O)Nc4ccccc43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC
CHEMBL4789505 5ht1a_human Human No 7.0 EC50 = 104.7 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
407 7 2 3 4.1 C1CN(CCC1(CNCCNC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL4519938 5ht1a_human Human No 6.0 EC50 = 1050 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding
454 8 3 4 3.7 CCc1cccc(c1Cl)N1CCN(CC1)C[C@@H](CCNC(=O)c1cc2c([nH]1)cccc2)O
CHEMBL4292655 5ht1a_human Human No 7.0 EC50 = 107 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
421 5 0 5 3.2 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCN1CCN(c2cccc3sccc23)CC1
CHEMBL4533184 5ht1a_human Human No 7.0 EC50 = 107 nM Funct
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
449 6 1 4 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4c5c(nc6ccccc46)CCC5)CC3)c2c1
CHEMBL4464476 5ht1a_mouse Mouse No 7.0 EC50 = 107 nM Bind
Agonist activity at mouse 5-HT1A expressed in HEK293 cells after 2 to 5 minsAgonist activity at mouse 5-HT1A expressed in HEK293 cells after 2 to 5 mins
463 6 1 4 5.6 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4c5c(nc6ccccc46)CCCC5)CC3)c2c1
CHEMBL3989558 5ht1a_human Human No 6.0 EC50 = 1075 nM Funct
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1
CHEMBL485253 5ht1a_human Human No 6.0 EC50 = 1075 nM Funct
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1
CHEMBL1774384 5ht1a_human Human No 6.0 EC50 = 1080 nM Funct
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
500 8 1 4 5.3 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1
CHEMBL1259209 5ht1a_human Human No 8.0 EC50 = 11 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
399 5 1 3 4.0 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC(C5)C3)C4)CC2)nc1
CHEMBL4248491 5ht1a_human Human No 8.0 EC50 = 11 nM Funct
Partial agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in cAMP accumulation by chemiluminescence-based assayPartial agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in cAMP accumulation by chemiluminescence-based assay
506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1
CHEMBL4202443 5ht1a_human Human No 8.0 EC50 = 11.3 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4sccc34)CC2)n1
CHEMBL4292254 5ht1a_human Human No 7.9 EC50 = 11.6 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
473 7 0 5 4.4 Cc1ccc(C23CC2C(=O)N(CCCCN2CCN(c4cccc5sccc45)CC2)C3=O)cc1
CHEMBL1926749 5ht1a_human Human No 7.9 EC50 = 11.6 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
334 7 1 5 2.4 O=C1CSC(=O)N1CCCCNCC1CCc2ccccc2O1
CHEMBL1962697 5ht1a_human Human No 7.9 EC50 = 11.6 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
334 7 1 5 2.4 O=C1CSC(=O)N1CCCCNCC1CCc2ccccc2O1
CHEMBL120055 5ht1a_human Human No 7.0 EC50 = 110 nM Funct
Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 110-250Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 110-250
392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1
CHEMBL321818 5ht1a_human Human No 7.0 EC50 = 110 nM Funct
Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 110-250Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 110-250
392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1
CHEMBL4082150 5ht1a_human Human No 6.0 EC50 = 1100 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
504 6 1 7 4.5 Cc1ccc(Sc2ccccc2N2CCN(CCc3c(C)nc4n(c3=O)CCCC4O)CC2)c(C)c1
CHEMBL4117087 5ht1a_human Human No 6.0 EC50 = 1100 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
504 6 1 7 4.5 Cc1ccc(Sc2ccccc2N2CCN(CCc3c(C)nc4n(c3=O)CCCC4O)CC2)c(C)c1
CHEMBL481839 5ht1a_human Human Yes 5.0 EC50 = 11000 nM Bind
Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cellsDisplacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells
323 0 0 5 3.0 CN1[C@H]2Cc3cc4c(cc3[C@@H]1Cc1cc3c(cc12)OCO3)OCO4
CHEMBL221183 5ht1a_human Human No 7.0 EC50 = 112.2 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
363 7 1 3 5.1 CC1(C)COc2c(OCCNCc3cccc(C4=CCCC4)c3)cccc21
CHEMBL4759629 5ht1a_human Human No 7.0 EC50 = 112.2 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
425 7 1 4 4.2 C1CN(CCC1(CNCCSC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL205031 5ht1a_human Human No 6.0 EC50 = 1131 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
345 3 2 3 4.1 C1=C(c2c[nH]c3ccccc23)CCN(CC2CNc3ccccc3O2)C1
CHEMBL4786537 5ht1a_human Human No 6.9 EC50 = 114.8 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
407 7 1 3 4.0 C1CN(CCC1(CNCCCC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL4580078 5ht1a_human Human No 4.9 EC50 = 11400 nM Bind
Agonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assayAgonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assay
370 3 2 4 2.8 C/C=C1\C[N@@+]2([O-])CCc3c([nH]c4ccccc34)[C@@H]2C[C@@H]1[C@H](CO)C(=O)OC
CHEMBL575290 5ht1a_human Human No 5.9 EC50 = 1150 nM Funct
Partial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assayPartial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assay
287 3 1 2 4.6 Clc1cccc(Oc2ccccc2C2CCNCC2)c1
CHEMBL234853 5ht1a_human Human No 6.9 EC50 = 116.2 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4ccc5ncccc5c4C3)c2c1
CHEMBL4211473 5ht1a_human Human No 6.9 EC50 = 117 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3ccc4ccsc4c3)CC2)n1
CHEMBL4797752 5ht1a_human Human No 6.9 EC50 = 117.5 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(Cl)cc2)CC1
CHEMBL4517102 5ht1a_human Human No 6.9 EC50 = 118 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl
CHEMBL4434876 5ht1a_human Human No 5.9 EC50 = 1180 nM Funct
Agonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assay
430 6 1 1 6.9 Fc1ccc(C2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2ccccc2)c1
CHEMBL2431042 5ht1a_human Human No 5.9 EC50 = 1195 nM Funct
Partial agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAPartial agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
359 10 1 4 2.4 CCc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O
CHEMBL3040827 5ht1a_human Human No 5.9 EC50 = 1195 nM Funct
Partial agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAPartial agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
359 10 1 4 2.4 CCc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O
CHEMBL3805165 5ht1a_human Human No 7.9 EC50 = 12 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
447 8 1 6 3.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4c3OC(F)(F)O4)CC2)c1
CHEMBL1259033 5ht1a_human Human No 7.9 EC50 = 12 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
347 5 1 4 3.2 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccsc3)CC2)nc1
CHEMBL56 5ht1a_human Human Yes 7.9 EC50 = 12.0 nM Funct
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL288244 5ht1a_human Human No 7.9 EC50 = 12.0 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
477 6 1 4 5.9 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cccs3)n2)CC1
CHEMBL4636321 5ht1a_human Human No 7.9 EC50 = 12.1 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
441 6 0 7 4.0 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(Cl)cccn12
CHEMBL44159 5ht1a_human Human No 7.9 EC50 = 12.3 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
445 6 1 5 3.8 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2cccc(-n3cccn3)n2)CC1
CHEMBL4786537 5ht1a_human Human No 7.9 EC50 = 12.6 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
407 7 1 3 4.0 C1CN(CCC1(CNCCCC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL45334 5ht1a_human Human No 7.9 EC50 = 12.6 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
408 6 2 4 3.7 CNc1cccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1
CHEMBL81095 5ht1a_human Human No 7.9 EC50 = 12.6 nM Funct
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
413 7 1 5 2.9 O=C(NCCCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1
CHEMBL4214642 5ht1a_human Human No 7.9 EC50 = 12.8 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
443 8 1 7 3.2 CNC(=O)c1cccc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)n1
CHEMBL4759629 5ht1a_human Human No 7.9 EC50 = 12.9 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
425 7 1 4 4.2 C1CN(CCC1(CNCCSC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL3805515 5ht1a_human Human No 6.9 EC50 = 120 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
465 9 1 5 4.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC
CHEMBL26655 5ht1a_human Human Yes 4.9 EC50 = 12000 nM Funct
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
212 1 1 1 2.9 CN1CC=C(c2c[nH]c3ccccc23)CC1
CHEMBL479243 5ht1a_rat Rat No 5.9 EC50 = 1210 nM Funct
Agonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS binding
433 6 1 9 1.8 CCC1=CC2C(=O)N(N)C(SCCCN3CCN(c4ncccn4)CC3)=NC2S1
CHEMBL3805376 5ht1a_human Human No 6.9 EC50 = 122 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
435 8 1 4 4.3 CNC(=O)c1ccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1
CHEMBL3806091 5ht1a_human Human No 6.9 EC50 = 122 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
449 8 1 4 4.6 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C
CHEMBL1926745 5ht1a_human Human No 6.9 EC50 = 123 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
371 7 1 4 1.6 O=C1C2CCCN2C(=O)CN1CCCCNCC1CCc2ccccc2O1
CHEMBL1962804 5ht1a_human Human No 6.9 EC50 = 123 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
371 7 1 4 1.6 O=C1C2CCCN2C(=O)CN1CCCCNCC1CCc2ccccc2O1
CHEMBL4790662 5ht1a_human Human No 6.9 EC50 = 123.0 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
454 8 1 4 4.6 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1
CHEMBL4218720 5ht1a_rat Rat No 6.9 EC50 = 125.9 nM Funct
Antagonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes assessed as inhibition of 8-OH-DPAT-induced receptor activation after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assayAntagonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes assessed as inhibition of 8-OH-DPAT-induced receptor activation after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assay
498 7 0 6 4.7 CC(=O)c1c(OCCCN2CCN(c3ccccc3Br)CC2)ccc2c(C)cc(=O)oc12
CHEMBL39 5ht1a_human Human Yes 6.9 EC50 = 128.8 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht1a_human Human Yes 6.9 EC50 = 128.8 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL312448 5ht1a_human Human Yes 6.9 EC50 = 129 nM Funct
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C
CHEMBL3805518 5ht1a_human Human No 7.9 EC50 = 13 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
443 8 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc1F
CHEMBL3805559 5ht1a_human Human No 7.9 EC50 = 13 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
425 8 1 5 4.4 CNC(=O)c1cccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1
CHEMBL2112645 5ht1a_human Human No 7.9 EC50 = 13 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
324 9 2 3 3.8 COc1ccccc1OCCNCCCc1c[nH]c2ccccc12
CHEMBL1259151 5ht1a_human Human No 7.9 EC50 = 13 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
341 5 1 3 3.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccccc3)CC2)nc1
CHEMBL4754363 5ht1a_human Human No 7.9 EC50 = 13.2 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
406 7 1 2 4.6 C1CN(CCC1(CNCCCC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL288992 5ht1a_human Human No 7.9 EC50 = 13.2 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
422 7 2 4 4.0 CCNc1cccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1
CHEMBL4277751 5ht1a_human Human No 7.9 EC50 = 13.3 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
437 6 0 5 4.2 O=C1c2ccc(F)cc2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL4756041 5ht1a_human Human No 7.9 EC50 = 13.5 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
459 7 1 4 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1
CHEMBL1277007 5ht1a_human Human No 7.9 EC50 = 13.7 nM Funct
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
446 6 1 7 2.8 Cc1cc(N2CCN(CCCCc3nc4c(c(=O)n3N)CCCC4)CC2)nc2ccccc12
CHEMBL125902 5ht1a_human Human No 7.9 EC50 = 13.7 nM Bind
Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cellsEffective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells
364 8 2 4 3.9 Fc1ccc2[nH]cc(CCCNCCOc3cccc4nccnc34)c2c1
CHEMBL4285479 5ht1a_human Human No 7.9 EC50 = 13.8 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
407 4 0 5 2.8 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCN1CCN(c2cccc3sccc23)CC1
CHEMBL1259108 5ht1a_human Human No 6.9 EC50 = 130 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
403 5 1 5 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4sccc4s3)CC2)nc1
CHEMBL4062992 5ht1a_human Human No 5.9 EC50 = 1300 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
445 4 0 7 3.4 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2(F)F
CHEMBL128 5ht1a_rat Rat Yes 5.9 EC50 = 1300 nM Funct
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL4753394 5ht1a_human Human No 5.9 EC50 = 1318.3 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
454 8 1 4 4.6 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1
CHEMBL1774385 5ht1a_human Human No 6.9 EC50 = 134 nM Funct
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
425 8 1 5 3.7 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3o2)CC1
CHEMBL441546 5ht1a_human Human No 6.9 EC50 = 134.9 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
337 7 1 4 4.2 C1=C(c2cccc(CNCCOc3cccc4c3OCO4)c2)CCC1
CHEMBL4742122 5ht1a_human Human No 6.9 EC50 = 134.9 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
409 7 1 4 3.5 C1CN(CCC1(CNCCOC2=CN=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL382333 5ht1a_human Human No 6.9 EC50 = 135 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
435 6 1 4 5.1 CCCN1CC(CN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)Oc2c(OC)cccc21
CHEMBL1457510 5ht1a_human Human Yes 4.9 EC50 = 13500 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4
CHEMBL3805434 5ht1a_human Human No 6.9 EC50 = 137 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
477 9 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(C(C)=O)c1
CHEMBL574004 5ht1a_human Human No 6.9 EC50 = 137 nM Funct
Partial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assayPartial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assay
289 3 1 2 4.2 Fc1cccc(Oc2cccc(F)c2C2CCNCC2)c1
CHEMBL473282 5ht1a_human Human No 6.9 EC50 = 138 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
361 6 2 4 4.0 c1ccc2c(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c[nH]c2c1
CHEMBL4760666 5ht1a_human Human No 6.9 EC50 = 138.0 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
451 8 1 4 4.2 CN(C)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL1301276 5ht1a_human Human Yes 4.9 EC50 = 13800 nM Funct
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
245 1 1 2 1.8 C[N+]1=C2CCCCCN2C(O)(c2ccccc2)C1
CHEMBL1616268 5ht1a_human Human Yes 4.9 EC50 = 13800 nM Funct
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
245 1 1 2 1.8 C[N+]1=C2CCCCCN2C(O)(c2ccccc2)C1
CHEMBL381542 5ht1a_human Human No 5.9 EC50 = 1385 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
411 8 2 3 5.2 c1ccc(CN2CC(CNCCCc3c[nH]c4ccccc34)Oc3ccccc32)cc1
CHEMBL4060678 5ht1a_human Human No 5.9 EC50 = 1395 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
425 4 1 8 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2O
CHEMBL4277532 5ht1a_human Human No 7.9 EC50 = 14 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
436 6 0 6 3.0 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2nsc3ccccc23)CC1
CHEMBL56 5ht1a_human Human Yes 7.8 EC50 = 14.5 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL56 5ht1a_human Human Yes 7.8 EC50 = 14.5 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL4756233 5ht1a_human Human No 7.8 EC50 = 14.5 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
447 7 2 3 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1
CHEMBL4786537 5ht1a_human Human No 7.8 EC50 = 14.5 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
407 7 1 3 4.0 C1CN(CCC1(CNCCCC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL4760621 5ht1a_human Human No 7.8 EC50 = 14.8 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
422 7 1 3 4.4 Cc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL3144354 5ht1a_human Human No 7.8 EC50 = 14.8 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
503 11 1 7 5.2 S=c1[nH]ncn1[C@@H]1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)[C@H]1OCc1ccccc1
CHEMBL42042 5ht1a_human Human No 7.8 EC50 = 14.8 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
459 6 1 5 4.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1-n1cccn1
CHEMBL4129917 5ht1a_human Human No 7.8 EC50 = 14.9 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5nc6c(c(N)c5c4)CCCC6)CC3)c2c1
CHEMBL475105 5ht1a_human Human No 6.9 EC50 = 140 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
389 7 2 4 4.6 CC(Nc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1)C1CC1
CHEMBL218217 5ht1a_human Human No 5.9 EC50 = 1412.5 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
361 9 1 3 5.3 CC(C)Oc1ccccc1OCCNCc1cccc(-c2ccccc2)c1
CHEMBL1774534 5ht1a_human Human No 5.8 EC50 = 1430 nM Funct
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
424 8 2 4 3.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3[nH]2)CC1
CHEMBL4130059 5ht1a_human Human No 6.8 EC50 = 146.0 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
492 6 2 5 5.6 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCCC6)CC3)c2c1
CHEMBL371300 5ht1a_human Human Yes 5.8 EC50 = 1460 nM Funct
Agonistic activity at cloned human 5HT1A receptor expressed in CHO cells by inhibition of forskolin-induced cAMP productionAgonistic activity at cloned human 5HT1A receptor expressed in CHO cells by inhibition of forskolin-induced cAMP production
191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21
CHEMBL39 5ht1a_human Human Yes 6.8 EC50 = 147 nM Funct
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL515438 5ht1a_human Human No 6.8 EC50 = 147 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
375 7 2 4 4.2 c1ccc2c(CCN3CCCC(c4ccnc(NCC5CC5)n4)C3)c[nH]c2c1
CHEMBL4760621 5ht1a_human Human No 6.8 EC50 = 147.9 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
422 7 1 3 4.4 Cc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL4544583 5ht1a_human Human No 6.8 EC50 = 149 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
438 8 2 3 4.7 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl
CHEMBL56 5ht1a_human Human Yes 7.8 EC50 = 15 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL1259034 5ht1a_human Human No 7.8 EC50 = 15 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
331 5 1 4 2.7 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccco3)CC2)nc1
CHEMBL49 5ht1a_human Human Yes 7.8 EC50 = 15.1 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL4781985 5ht1a_human Human No 7.8 EC50 = 15.1 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
437 8 2 4 4.1 CNc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1
CHEMBL49 5ht1a_human Human Yes 7.8 EC50 = 15.1 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL39 5ht1a_human Human Yes 7.8 EC50 = 15.3 nM Bind
Agonist activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by Fluo-4 dye based FLIPR assayAgonist activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by Fluo-4 dye based FLIPR assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL419240 5ht1a_human Human No 7.8 EC50 = 15.7 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
370 8 2 4 3.7 Fc1ccc2[nH]cc(CCCNCCOc3cccc4c3OCCO4)c2c1
CHEMBL4739908 5ht1a_human Human No 7.8 EC50 = 15.9 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1
CHEMBL39 5ht1a_human Human Yes 6.8 EC50 = 150 nM Funct
Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL370758 5ht1a_human Human No 6.8 EC50 = 150 nM Funct
Inhibition of forskolin-induced increase in cAMP in human 5-hydroxytryptamine 1A receptor expressed HeLa cellsInhibition of forskolin-induced increase in cAMP in human 5-hydroxytryptamine 1A receptor expressed HeLa cells
378 3 0 4 1.8 O=C1[C@@H]2CCCN2C(=O)CN1CN1CCN(c2cccc3ccccc23)CC1
CHEMBL2312640 5ht1a_human Human No 4.8 EC50 = 15000 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc2ccccc12
CHEMBL4760271 5ht1a_human Human No 6.8 EC50 = 151.4 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2F)CC1
CHEMBL231273 5ht1a_human Human No 6.8 EC50 = 154.9 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
414 5 1 4 3.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ncc(Cl)cn2)CC1
CHEMBL221957 5ht1a_human Human No 5.8 EC50 = 1548.8 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
379 9 1 3 6.0 CC(C)Oc1ccccc1OCCNCc1cccc(C2=CCCCCC2)c1
CHEMBL410273 5ht1a_human Human No 6.8 EC50 = 155 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
325 5 3 3 3.3 Fc1ccc2[nH]cc(CCNCC3CNc4ccccc4O3)c2c1
CHEMBL2312639 5ht1a_human Human No 4.8 EC50 = 15500 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1
CHEMBL4127445 5ht1a_human Human No 5.8 EC50 = 1563.2 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4ccc5nc6c(c(N)c5c4)CCCC6)CC3)c2c1
CHEMBL1926686 5ht1a_human Human No 6.8 EC50 = 157 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
371 8 1 4 2.6 O=C1C2CCCN2C(=O)N1CCCCCNCC1CCc2ccccc2O1
CHEMBL1962913 5ht1a_human Human No 6.8 EC50 = 157 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
371 8 1 4 2.6 O=C1C2CCCN2C(=O)N1CCCCCNCC1CCc2ccccc2O1
CHEMBL1258999 5ht1a_human Human No 7.8 EC50 = 16 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1
CHEMBL1926733 5ht1a_human Human No 7.8 EC50 = 16.3 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
357 7 1 4 2.2 O=C1C2CCCN2C(=O)N1CCCCNCC1CCc2ccccc2O1
CHEMBL1962486 5ht1a_human Human No 7.8 EC50 = 16.3 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
357 7 1 4 2.2 O=C1C2CCCN2C(=O)N1CCCCNCC1CCc2ccccc2O1
CHEMBL4217986 5ht1a_human Human No 7.8 EC50 = 16.5 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
411 8 1 7 2.8 NC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1
CHEMBL4077006 5ht1a_human Human No 7.8 EC50 = 16.9 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
432 4 0 7 2.6 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3OC(F)(F)O4)CC1)CCCC2
CHEMBL4117235 5ht1a_human Human No 7.8 EC50 = 16.9 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
432 4 0 7 2.6 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3OC(F)(F)O4)CC1)CCCC2
CHEMBL4760666 5ht1a_human Human No 7.8 EC50 = 17.0 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
451 8 1 4 4.2 CN(C)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL464099 5ht1a_human Human Yes 6.8 EC50 = 160 nM Bind
Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cellsDisplacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells
341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C
CHEMBL4456720 5ht1a_human Human No 5.8 EC50 = 1600 nM Bind
Agonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assayAgonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assay
546 4 6 11 -0.7 COC(=O)C1=CO[C@@H](O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@H]2[C@@H]1C[C@H]1c3[nH]c4ccccc4c3CCN1C[C@@H]2O
CHEMBL4781985 5ht1a_human Human No 6.8 EC50 = 162.2 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
437 8 2 4 4.1 CNc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1
CHEMBL297208 5ht1a_human Human No 6.8 EC50 = 162.2 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
468 6 1 6 4.1 N#CC1(CNCc2cccc(-n3cccn3)n2)CCN(C(=O)c2ccc(Cl)c(Cl)c2)CC1
CHEMBL494678 5ht1a_human Human No 5.8 EC50 = 1621.8 nM Funct
Agonist activity at 5HT1A receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by GTPgammaS binding assay
294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1
CHEMBL4747083 5ht1a_human Human No 5.8 EC50 = 1621.8 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
438 8 1 4 4.1 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)cc1
CHEMBL2312935 5ht1a_human Human No 5.8 EC50 = 1650 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2c1
CHEMBL377941 5ht1a_human Human No 6.8 EC50 = 167.5 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
339 5 2 3 3.3 CN1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21
CHEMBL473903 5ht1a_human Human No 6.8 EC50 = 169 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
379 6 2 4 4.1 Fc1ccc2[nH]cc(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c2c1
CHEMBL39 5ht1a_human Human Yes 6.8 EC50 = 169.8 nM Bind
Agonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assayAgonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL4793515 5ht1a_human Human No 6.8 EC50 = 169.8 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
424 7 1 3 4.8 C1CN(CCC1(CNCCSC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL3597636 5ht1a_human Human No 7.8 EC50 = 17 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
454 7 2 5 3.7 O=C(NCCC(O)CN1CCN(c2cccc3ccccc23)CC1)c1cnc2ccccc2c1
CHEMBL1259071 5ht1a_human Human No 7.8 EC50 = 17 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1
CHEMBL4746386 5ht1a_human Human No 7.8 EC50 = 17.4 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2Cl)CC1
CHEMBL4740097 5ht1a_human Human No 7.8 EC50 = 17.4 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
408 7 2 4 3.5 C1CN(CCC1(CNCCNC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL4753328 5ht1a_human Human Yes 7.8 EC50 = 17.4 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
409 7 1 4 3.5 C1CN(CCC1(CNCCOC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL4279645 5ht1a_human Human No 7.8 EC50 = 17.4 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
469 6 2 7 1.8 O=C1[C@@H]2[C@H](C(=O)N1CCCCN1CCN(c3cccc4sccc34)CC1)[C@@H]1C[C@H]2[C@@H](O)[C@H]1O
CHEMBL4210637 5ht1a_human Human No 7.8 EC50 = 17.6 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
440 9 1 6 4.2 CCNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1
CHEMBL314213 5ht1a_rat Rat No 6.8 EC50 = 170 nM Funct
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
325 6 2 5 3.3 CN(C)CCc1c[nH]c2ccc(Nc3ncccc3[N+](=O)[O-])cc12
CHEMBL391531 5ht1a_human Human No 6.8 EC50 = 171.6 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4c(ccc5ncccc45)C3)c2c1
CHEMBL4754941 5ht1a_human Human No 6.8 EC50 = 173.8 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
425 7 1 4 4.0 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2ccccn2)CC1
CHEMBL4777207 5ht1a_human Human No 6.8 EC50 = 175.1 nM Funct
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
445 8 0 3 5.1 O=C(c1ccccc1)N(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)CC1CC1
CHEMBL4215048 5ht1a_human Human No 6.8 EC50 = 176 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
443 8 1 7 3.2 CNC(=O)c1ccnc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)c1
CHEMBL39 5ht1a_human Human Yes 7.8 EC50 = 18 nM Funct
Agonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL1259032 5ht1a_human Human No 7.8 EC50 = 18 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
347 5 1 4 3.2 Cc1ccc(CNCC2(F)CCN(C(=O)c3cccs3)CC2)nc1
CHEMBL1259200 5ht1a_human Human No 7.8 EC50 = 18 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
417 5 2 4 3.5 Cc1ccc(CNCC2(O)CC3CCC(C2)N3C(=O)c2ccc(F)c(Cl)c2)nc1
CHEMBL4760271 5ht1a_human Human No 7.7 EC50 = 18.2 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2F)CC1
CHEMBL1926747 5ht1a_human Human No 7.7 EC50 = 18.9 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
375 7 1 5 2.4 O=C1C2CCSN2C(=O)N1CCCCNCC1CCc2ccccc2O1
CHEMBL1962460 5ht1a_human Human No 7.7 EC50 = 18.9 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
375 7 1 5 2.4 O=C1C2CCSN2C(=O)N1CCCCNCC1CCc2ccccc2O1
CHEMBL596885 5ht1a_human Human No 6.8 EC50 = 180 nM Funct
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
289 2 0 2 3.5 C#CCOc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3
CHEMBL3358509 5ht1a_human Human No 5.8 EC50 = 1800 nM Funct
Agonist activity at human 5HT1A receptor (unknown origin) expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human 5HT1A receptor (unknown origin) expressed in CHO cells by [35S]GTPgammaS binding assay
388 7 1 4 3.6 O=C(NCCCCN1CCN(c2ccccc2)CC1)c1ccc2ncccc2c1
CHEMBL39 5ht1a_human Human Yes 5.8 EC50 = 1800 nM Bind
Agonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assayAgonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL2165119 5ht1a_human Human No 5.8 EC50 = 1800 nM Bind
pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).
462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl
CHEMBL425936 5ht1a_human Human No 6.7 EC50 = 181.5 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
355 6 3 4 3.3 COc1ccc2c(c1)OC(CNCCc1c[nH]c3ccc(F)cc13)CN2
CHEMBL234853 5ht1a_human Human No 6.7 EC50 = 181.8 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4ccc5ncccc5c4C3)c2c1
CHEMBL1309229 5ht1a_human Human Yes 5.7 EC50 = 1815 nM Funct
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
216 5 2 1 3.0 CCCCc1ccc2[nH]cc(CCN)c2c1
CHEMBL1616674 5ht1a_human Human Yes 5.7 EC50 = 1815 nM Funct
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
216 5 2 1 3.0 CCCCc1ccc2[nH]cc(CCN)c2c1
CHEMBL1277281 5ht1a_human Human No 6.7 EC50 = 182 nM Funct
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
450 6 1 8 2.7 Nn1c(SCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2c(c1=O)CCCC2
CHEMBL49 5ht1a_human Human Yes 6.7 EC50 = 186.2 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL49 5ht1a_human Human Yes 6.7 EC50 = 186.2 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL4789505 5ht1a_human Human No 6.7 EC50 = 186.2 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
407 7 2 3 4.1 C1CN(CCC1(CNCCNC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL2431051 5ht1a_human Human No 7.7 EC50 = 19 nM Funct
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
375 11 1 5 2.3 CCOc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O
CHEMBL3040382 5ht1a_human Human No 7.7 EC50 = 19 nM Funct
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
375 11 1 5 2.3 CCOc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O
CHEMBL596297 5ht1a_human Human No 7.7 EC50 = 19 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
454 8 2 4 4.3 N#Cc1ccc2[nH]cc(CCCCN(CC3CC3)C3COc4ccc5c(c4C3)C(=O)NC5)c2c1
CHEMBL39 5ht1a_human Human Yes 7.7 EC50 = 19 nM Funct
Agonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL191971 5ht1a_human Human Yes 7.7 EC50 = 19.1 nM Funct
Binding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-SBinding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-S
497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1
CHEMBL4797282 5ht1a_human Human No 7.7 EC50 = 19.5 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(Cl)c2)CC1
CHEMBL1926759 5ht1a_human Human No 7.7 EC50 = 19.9 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
362 9 1 5 3.2 O=C1CSC(=O)N1CCCCCCNCC1CCc2ccccc2O1
CHEMBL1962491 5ht1a_human Human No 7.7 EC50 = 19.9 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
362 9 1 5 3.2 O=C1CSC(=O)N1CCCCCCNCC1CCc2ccccc2O1
CHEMBL4752833 5ht1a_human Human No 7.7 EC50 = 20.0 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
442 7 1 3 4.7 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1
CHEMBL448891 5ht1a_human Human Yes 6.7 EC50 = 190 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2
CHEMBL1806874 5ht1a_human Human No 6.7 EC50 = 190 nM Funct
Agonist activity at 5-HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 minsAgonist activity at 5-HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins
467 8 0 5 6.8 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)CCCCC2CCSS2)c1-3
CHEMBL203018 5ht1a_human Human No 6.7 EC50 = 190 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
407 4 1 4 4.3 COc1cccc2c1OC(CN1CC=C(c3c[nH]c4ccc(F)cc34)CC1)CN2C
CHEMBL383446 5ht1a_human Human No 6.7 EC50 = 190.5 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
367 6 2 3 4.1 CC(C)N1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21
CHEMBL413777 5ht1a_human Human No 6.7 EC50 = 195.0 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
353 9 1 3 5.3 CC(C)Oc1ccccc1OCCNCc1cccc(C2CCCC2)c1
CHEMBL230963 5ht1a_human Human Yes 6.7 EC50 = 195.0 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F
CHEMBL230963 5ht1a_human Human Yes 6.7 EC50 = 195.0 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F
CHEMBL382179 5ht1a_human Human No 6.7 EC50 = 196.5 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
349 7 2 3 4.0 CCCN1CC(CNCCc2c[nH]c3ccccc23)Oc2ccccc21
CHEMBL1645600 5ht1a_human Human No 6.7 EC50 = 197 nM Funct
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
311 4 1 3 3.8 Fc1cccc(Cl)c1Oc1cccc(F)c1OC1CNC1
CHEMBL7257 5ht1a_human Human Yes 6.7 EC50 = 197 nM Funct
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL4789505 5ht1a_human Human No 5.7 EC50 = 1995.3 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
407 7 2 3 4.1 C1CN(CCC1(CNCCNC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL4634009 5ht1a_human Human No 8.7 EC50 = 2 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
437 7 0 8 3.3 COc1cccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n12
CHEMBL126424 5ht1a_human Human No 8.7 EC50 = 2 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
351 8 3 2 4.4 Fc1ccc2[nH]cc(CCCNCCOc3cccc4[nH]ccc34)c2c1
CHEMBL4750444 5ht1a_human Human No 8.7 EC50 = 2.1 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
451 8 2 4 3.2 NC(=O)c1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1
CHEMBL2107510 5ht1a_human Human Yes 8.7 EC50 = 2.1 nM Bind
Partial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assayPartial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assay
369 5 1 5 1.9 O=C(NCCN1CCN(c2ncccn2)CC1)C12CC3CC(CC(C3)C1)C2
CHEMBL2111138 5ht1a_human Human Yes 8.7 EC50 = 2.1 nM Bind
Partial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assayPartial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assay
369 5 1 5 1.9 O=C(NCCN1CCN(c2ncccn2)CC1)C12CC3CC(CC(C3)C1)C2
CHEMBL45422 5ht1a_human Human Yes 8.7 EC50 = 2.1 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
422 6 2 4 4.0 CNc1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ccc1C
CHEMBL4644500 5ht1a_human Human No 8.7 EC50 = 2.2 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
437 7 0 8 3.3 COc1cccn2c(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)nc12
CHEMBL4213342 5ht1a_human Human No 8.7 EC50 = 2.2 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
425 8 1 7 3.0 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1
CHEMBL4786067 5ht1a_human Human No 8.6 EC50 = 2.3 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
438 8 1 4 4.1 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL4739908 5ht1a_human Human No 8.6 EC50 = 2.3 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1
CHEMBL4278581 5ht1a_human Human No 8.6 EC50 = 2.4 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
435 6 0 5 3.6 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3ccsc23)CC1
CHEMBL1277558 5ht1a_human Human No 8.6 EC50 = 2.5 nM Funct
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
549 6 1 10 2.9 CC(=O)N1CCc2c(sc3nc(SCCCN4CCN(c5ccc6ccccc6n5)CC4)n(N)c(=O)c23)C1
CHEMBL78874 5ht1a_human Human No 8.6 EC50 = 2.5 nM Funct
Ability to influence the binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptorAbility to influence the binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptor
475 9 1 8 3.3 CCC(=O)c1c(-c2ccccc2)nn(C)c(=O)c1NCCN1CCN(c2ccccc2OC)CC1
CHEMBL56 5ht1a_human Human Yes 8.6 EC50 = 2.6 nM Funct
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL221920 5ht1a_human Human No 8.6 EC50 = 2.6 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
362 7 1 4 4.3 C1=C(c2cncc(CNCCOc3cccc4c3OC3(CC3)C4)c2)CCC1
CHEMBL43146 5ht1a_human Human No 8.6 EC50 = 2.6 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
461 6 1 4 5.4 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3ccco3)n2)CC1
CHEMBL4749223 5ht1a_human Human No 8.6 EC50 = 2.7 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
448 7 0 7 4.2 COc1ccc2ncc(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)c2c1
CHEMBL3805099 5ht1a_human Human No 8.6 EC50 = 2.7 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
442 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccc1F
CHEMBL42545 5ht1a_human Human No 8.6 EC50 = 2.8 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
459 6 2 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1-c1cc[nH]n1
CHEMBL4635890 5ht1a_human Human No 8.6 EC50 = 2.8 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
408 6 0 8 2.7 O=c1n(CCCCN2CCN(c3cccc4scnc34)CC2)nc2ccccn12
CHEMBL4777581 5ht1a_human Human No 8.6 EC50 = 2.8 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
451 8 2 4 3.2 NC(=O)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL542671 5ht1a_human Human No 8.6 EC50 = 2.8 nM Funct
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1
CHEMBL82215 5ht1a_human Human No 8.6 EC50 = 2.8 nM Funct
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1
CHEMBL384657 5ht1a_human Human No 8.5 EC50 = 2.9 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
364 7 1 4 4.5 CC1(C)Cc2cccc(OCCNCc3cncc(C4=CCCC4)c3)c2O1
CHEMBL542671 5ht1a_human Human No 8.5 EC50 = 2.9 nM Funct
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1
CHEMBL82215 5ht1a_human Human No 8.5 EC50 = 2.9 nM Funct
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1
CHEMBL126407 5ht1a_human Human No 8.5 EC50 = 2.9 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
352 8 2 3 4.7 Fc1ccc2[nH]cc(CCCNCCOc3cccc4ccoc34)c2c1
CHEMBL140406 5ht1a_human Human No 8.5 EC50 = 3.0 nM Funct
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
363 5 0 4 4.0 COC1=CC=CC\2=C1CCC/C2=C\CCN3CCN(CC3)C4=CC=CC=N4
CHEMBL46971 5ht1a_human Human No 8.5 EC50 = 3.0 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
438 6 1 4 4.2 CN(C)c1cccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1
CHEMBL209821 5ht1a_human Human Yes 7.7 EC50 = 20 nM Funct
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
450 10 2 5 3.0 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)CC3CCCCC3)CC2)c1
CHEMBL210537 5ht1a_human Human No 7.7 EC50 = 20 nM Funct
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
444 9 2 5 2.8 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)c3ccc(C)cc3)CC2)c1
CHEMBL1259087 5ht1a_human Human No 7.7 EC50 = 20 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3sccc3Br)CC2)nc1
CHEMBL1259107 5ht1a_human Human No 7.7 EC50 = 20 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
361 5 1 4 3.5 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(C)cs3)CC2)nc1
CHEMBL4644742 5ht1a_human Human No 7.7 EC50 = 20.2 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
432 6 0 8 3.2 N#Cc1cccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n12
CHEMBL4790662 5ht1a_human Human No 7.7 EC50 = 20.4 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
454 8 1 4 4.6 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1
CHEMBL42994 5ht1a_human Human No 7.7 EC50 = 20.4 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
420 6 1 4 4.1 CN(C)c1cccc(CNCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1
CHEMBL423181 5ht1a_human Human No 7.7 EC50 = 20.9 nM Funct
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
351 5 0 4 3.4 COC1=CC2=C(CCC(C2)CCN3CCN(CC3)C4=CC=CC=N4)C=C1
CHEMBL4753328 5ht1a_human Human Yes 7.7 EC50 = 20.9 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
409 7 1 4 3.5 C1CN(CCC1(CNCCOC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL4747083 5ht1a_human Human No 7.7 EC50 = 20.9 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
438 8 1 4 4.1 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)cc1
CHEMBL4753414 5ht1a_human Human No 7.7 EC50 = 20.9 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
410 7 1 5 2.9 C1CN(CCC1(CNCCOC2=NC=CN=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL47013 5ht1a_human Human No 7.7 EC50 = 20.9 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
409 5 1 3 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)nc1
CHEMBL582945 5ht1a_human Human No 6.7 EC50 = 200 nM Funct
Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
624 12 2 9 5.2 COc1ccccc1N1CCN(CCCn2cc(CCCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1
CHEMBL2104993 5ht1a_human Human Yes 6.7 EC50 = 200 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1
CHEMBL480521 5ht1a_human Human Yes 5.7 EC50 = 2000 nM Bind
Agonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assayAgonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assay
384 4 1 5 2.7 CC[C@H]1CN2CC[C@@]3(C(=O)Nc4ccccc43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC
CHEMBL230425 5ht1a_human Human No 5.7 EC50 = 2041.7 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
409 6 2 4 3.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(CO)cn2)CC1
CHEMBL4483569 5ht1a_human Human No 5.7 EC50 = 2060 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding
454 8 3 4 3.7 CCc1cccc(N2CCN(C[C@@H](O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl
CHEMBL209324 5ht1a_human Human Yes 7.7 EC50 = 21 nM Funct
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
417 9 1 5 2.9 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(C)cc2)CC1
CHEMBL323441 5ht1a_human Human No 7.7 EC50 = 21 nM Bind
Stimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cellsStimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells
407 5 1 4 4.2 O[C@@H](COc1ccccc1F)CN1CCC2(CC1)OCc1c2ccc2ccccc12
CHEMBL4294797 5ht1a_human Human Yes 7.7 EC50 = 21.3 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
419 6 0 5 4.1 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL1926751 5ht1a_human Human No 7.7 EC50 = 21.8 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
385 9 1 4 3.0 O=C1C2CCCN2C(=O)N1CCCCCCNCC1CCc2ccccc2O1
CHEMBL1962585 5ht1a_human Human No 7.7 EC50 = 21.8 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
385 9 1 4 3.0 O=C1C2CCCN2C(=O)N1CCCCCCNCC1CCc2ccccc2O1
CHEMBL56 5ht1a_human Human Yes 7.7 EC50 = 21.9 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL4755058 5ht1a_human Human No 7.7 EC50 = 21.9 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
465 8 2 4 4.1 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL44904 5ht1a_human Human No 7.7 EC50 = 21.9 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
406 6 2 4 4.1 CNc1cccc(CNCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1
CHEMBL1774535 5ht1a_human Human No 5.7 EC50 = 2140 nM Funct
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1
CHEMBL475694 5ht1a_human Human No 6.7 EC50 = 216 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
379 6 2 4 4.1 Fc1cccc2c(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c[nH]c12
CHEMBL583752 5ht1a_human Human No 6.7 EC50 = 219 nM Funct
Partial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assayPartial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assay
271 3 1 2 4.1 Fc1cccc(Oc2ccccc2C2CCNCC2)c1
CHEMBL606864 5ht1a_human Human No 7.7 EC50 = 22 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
386 5 3 4 2.8 N#Cc1ccc2[nH]cc(CCCNC3COc4ccc5c(c4C3)C(=O)NC5)c2c1
CHEMBL342986 5ht1a_human Human Yes 7.7 EC50 = 22 nM Funct
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
246 6 1 2 3.1 CCN(CC)CCc1c[nH]c2ccc(OC)cc12
CHEMBL1278088 5ht1a_human Human Yes 7.7 EC50 = 22.3 nM Funct
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
432 6 1 7 2.5 Nn1c(CCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2c(c1=O)CCCC2
CHEMBL4800109 5ht1a_human Human No 7.6 EC50 = 22.8 nM Funct
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
366 7 0 4 3.1 CC(C)N(CCCN1CCN(c2ccccn2)CC1)C(=O)c1ccccc1
CHEMBL46512 5ht1a_human Human No 7.6 EC50 = 22.9 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
478 6 1 5 5.2 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3nccs3)n2)CC1
CHEMBL84107 5ht1a_rat Rat No 6.7 EC50 = 220 nM Funct
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
337 5 3 5 3.5 O=[N+]([O-])c1cccnc1Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1
CHEMBL4583944 5ht1a_human Human No 5.7 EC50 = 2200 nM Bind
Agonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assayAgonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assay
356 4 2 4 2.9 CC[C@H]1CN2CCc3c([nH]c4ccccc34)[C@H]2C[C@@H]1[C@@H](CO)C(=O)OC
CHEMBL275628 5ht1a_human Human Yes 5.7 EC50 = 2219 nM Funct
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2
CHEMBL4797282 5ht1a_human Human No 6.7 EC50 = 223.9 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(Cl)c2)CC1
CHEMBL1645601 5ht1a_human Human No 6.7 EC50 = 225 nM Funct
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
291 4 1 3 3.4 Cc1cccc(F)c1Oc1cccc(F)c1OC1CNC1
CHEMBL39 5ht1a_human Human Yes 6.6 EC50 = 229.1 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL394530 5ht1a_human Human No 6.6 EC50 = 229.1 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
411 6 1 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(CF)cn2)CC1
CHEMBL2431048 5ht1a_human Human No 7.6 EC50 = 23 nM Funct
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
361 10 1 5 1.9 COc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O
CHEMBL3040882 5ht1a_human Human No 7.6 EC50 = 23 nM Funct
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
361 10 1 5 1.9 COc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O
CHEMBL1926750 5ht1a_human Human No 7.6 EC50 = 23.3 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
343 6 1 4 1.8 O=C1C2CCCN2C(=O)N1CCCNCC1CCc2ccccc2O1
CHEMBL1962912 5ht1a_human Human No 7.6 EC50 = 23.3 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
343 6 1 4 1.8 O=C1C2CCCN2C(=O)N1CCCNCC1CCc2ccccc2O1
CHEMBL45305 5ht1a_human Human Yes 7.6 EC50 = 23.4 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1
CHEMBL4207328 5ht1a_human Human No 7.6 EC50 = 23.6 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
436 8 1 5 3.7 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1
CHEMBL4742122 5ht1a_human Human No 7.6 EC50 = 24.0 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
409 7 1 4 3.5 C1CN(CCC1(CNCCOC2=CN=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL230327 5ht1a_human Human No 6.6 EC50 = 239.9 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
429 6 1 3 4.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(C(F)F)cn2)CC1
CHEMBL607419 5ht1a_human Human No 7.6 EC50 = 24 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
433 7 2 3 4.2 O=C1NCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3
CHEMBL1112 5ht1a_human Human Yes 7.6 EC50 = 24 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL3805077 5ht1a_human Human No 7.6 EC50 = 24 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
435 8 1 4 4.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1
CHEMBL4079251 5ht1a_human Human No 7.6 EC50 = 24.2 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
442 4 0 6 4.2 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2Cl
CHEMBL219486 5ht1a_human Human No 7.6 EC50 = 24.6 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
365 7 1 4 4.9 CC1(C)Oc2cccc(OCCNCc3cccc(C4=CCCC4)c3)c2O1
CHEMBL4760271 5ht1a_human Human No 7.6 EC50 = 24.6 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2F)CC1
CHEMBL4787394 5ht1a_human Human No 7.6 EC50 = 24.9 nM Funct
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
378 8 0 4 3.1 O=C(c1ccccc1)N(CCCN1CCN(c2ccccn2)CC1)CC1CC1
CHEMBL1259051 5ht1a_human Human No 6.6 EC50 = 240 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
331 5 1 4 2.7 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccoc3)CC2)nc1
CHEMBL1259242 5ht1a_human Human No 6.6 EC50 = 240 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccccc4s3)CC2)nc1
CHEMBL230963 5ht1a_human Human Yes 6.6 EC50 = 245.5 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F
CHEMBL4793515 5ht1a_human Human No 5.6 EC50 = 2454.7 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
424 7 1 3 4.8 C1CN(CCC1(CNCCSC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL606149 5ht1a_human Human No 7.6 EC50 = 25 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
393 5 3 3 3.1 O=C1NCCc2ccc3c(c21)CC(NCCCc1c[nH]c2ccc(F)cc12)CO3
CHEMBL4753414 5ht1a_human Human No 7.6 EC50 = 25.1 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
410 7 1 5 2.9 C1CN(CCC1(CNCCOC2=NC=CN=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL4746386 5ht1a_human Human No 7.6 EC50 = 25.7 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2Cl)CC1
CHEMBL4789505 5ht1a_human Human No 7.6 EC50 = 25.7 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
407 7 2 3 4.1 C1CN(CCC1(CNCCNC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL45305 5ht1a_human Human Yes 7.6 EC50 = 25.7 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1
CHEMBL338587 5ht1a_human Human No 7.6 EC50 = 25.8 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
347 9 3 2 4.6 c1ccc2c(CCCCNCCOc3cccc4[nH]ccc34)c[nH]c2c1
CHEMBL1926760 5ht1a_human Human No 7.6 EC50 = 25.9 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
390 11 1 5 4.0 O=C1CSC(=O)N1CCCCCCCCNCC1CCc2ccccc2O1
CHEMBL1962492 5ht1a_human Human No 7.6 EC50 = 25.9 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
390 11 1 5 4.0 O=C1CSC(=O)N1CCCCCCCCNCC1CCc2ccccc2O1
CHEMBL3597643 5ht1a_human Human No 6.6 EC50 = 250 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
426 7 2 3 4.7 O=C(NCCCCN1CCN(c2cccc3ccccc23)CC1)c1cc2ccccc2[nH]1
CHEMBL2165126 5ht1a_human Human No 5.6 EC50 = 2500 nM Bind
pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).
461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl
CHEMBL4797282 5ht1a_human Human No 6.6 EC50 = 251.2 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(Cl)c2)CC1
CHEMBL311976 5ht1a_human Human No 6.6 EC50 = 251.2 nM Funct
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
429 4 0 7 1.4 O=C1c2ccccc2S(=O)(=O)N1CCN1CCN(c2cccc3c2OCCO3)CC1
CHEMBL4753394 5ht1a_human Human No 5.6 EC50 = 2511.9 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
454 8 1 4 4.6 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1
CHEMBL592951 5ht1a_human Human No 6.6 EC50 = 252 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
435 6 2 3 4.2 CC(C)N(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NCC3
CHEMBL56 5ht1a_human Human Yes 7.6 EC50 = 26 nM Funct
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL604063 5ht1a_human Human No 7.6 EC50 = 26 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
407 5 2 3 3.5 CN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NCC3
CHEMBL3804943 5ht1a_human Human No 7.6 EC50 = 26 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
465 9 1 5 4.3 CNC(=O)c1ccc(OC)c(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1
CHEMBL3806169 5ht1a_human Human No 7.6 EC50 = 26 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
421 8 1 4 4.1 NC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1
CHEMBL75642 5ht1a_human Human No 7.6 EC50 = 26 nM Funct
Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pigCompound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pig
355 3 1 4 4.0 CN1CCC[C@@H]1Cc1c[nH]c2ccc(-n3cnc4cc(C#N)ccc43)cc12
CHEMBL1259210 5ht1a_human Human No 7.6 EC50 = 26 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
387 5 1 3 4.2 Cc1ccc(CNCC2(F)CCN(C(=O)C34CCCC(CCC3)C4)CC2)nc1
CHEMBL4100152 5ht1a_human Human No 7.6 EC50 = 26.2 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
448 4 1 8 2.1 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3OC(F)(F)O4)CC1)CCCC2O
CHEMBL4740097 5ht1a_human Human No 6.6 EC50 = 263.0 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
408 7 2 4 3.5 C1CN(CCC1(CNCCNC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL43097 5ht1a_human Human No 6.6 EC50 = 269.2 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
441 6 1 5 4.1 O=C(c1ccc(Cl)c(Cl)c1)N1CC=C(CNCc2cccc(-n3cccn3)n2)CC1
CHEMBL500 5ht1a_human Human Yes 7.6 EC50 = 27 nM Bind
Stimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cellsStimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells
248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C
CHEMBL39 5ht1a_human Human Yes 7.6 EC50 = 27.5 nM Funct
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL4469777 5ht1a_human Human No 7.6 EC50 = 27.7 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
238 2 0 2 2.7 CCc1cccc(N2CCN(C)CC2)c1Cl
CHEMBL3084757 5ht1a_human Human No 6.6 EC50 = 270 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
365 5 2 4 2.7 Cc1ccc(CNC[C@]2(O)C[C@@H]3CC[C@H](C2)N3C(=O)c2ccccc2)nc1
CHEMBL4740430 5ht1a_human Human No 6.6 EC50 = 275.4 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
476 7 1 3 5.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(C(F)(F)F)c2)CC1
CHEMBL4746734 5ht1a_human Human No 5.6 EC50 = 2754.2 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
424 7 1 5 3.2 CC1=CN=C(N=C1)OCCNCC2(CCN(CC2)C(=O)C3=CC(=C(C=C3)F)Cl)F
CHEMBL592029 5ht1a_human Human No 7.6 EC50 = 28 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
407 6 2 3 3.8 CCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NC3
CHEMBL4212622 5ht1a_human Human No 7.6 EC50 = 28.1 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
452 9 1 6 4.3 O=C(NC1CC1)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1
CHEMBL56 5ht1a_human Human Yes 7.6 EC50 = 28.2 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL440854 5ht1a_human Human No 7.6 EC50 = 28.2 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
461 6 1 5 4.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-n3cccn3)n2)CC1
CHEMBL4239823 5ht1a_human Human No 7.6 EC50 = 28.3 nM Funct
Partial agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in cAMP accumulation by chemiluminescence-based assayPartial agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in cAMP accumulation by chemiluminescence-based assay
506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1
CHEMBL4087246 5ht1a_human Human No 7.5 EC50 = 28.6 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
426 4 1 7 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3CCS4)CC1)CCCC2O
CHEMBL4129051 5ht1a_human Human No 7.5 EC50 = 28.8 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(N)c6c(nc5c4)CCCC6)CC3)c2c1
CHEMBL4753414 5ht1a_human Human No 7.5 EC50 = 28.8 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
410 7 1 5 2.9 C1CN(CCC1(CNCCOC2=NC=CN=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL45048 5ht1a_human Human No 7.5 EC50 = 28.8 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
464 8 1 4 4.8 CCN(CC)c1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ccc1C
CHEMBL595622 5ht1a_human Human No 6.6 EC50 = 284 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
393 6 3 3 3.5 O=C1NCc2ccc3c(c21)CC(NCCCCc1c[nH]c2ccc(F)cc12)CO3
CHEMBL1112 5ht1a_human Human Yes 6.5 EC50 = 285 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL284092 5ht1a_human Human Yes 6.5 EC50 = 288 nM Funct
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
359 6 0 6 1.6 CC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1
CHEMBL4759629 5ht1a_human Human No 6.5 EC50 = 288.4 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
425 7 1 4 4.2 C1CN(CCC1(CNCCSC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL437314 5ht1a_human Human Yes 5.5 EC50 = 2890 nM Funct
Agonistic activity at cloned human 5HT1A receptor expressed in CHO cells by inhibition of forskolin-induced cAMP productionAgonistic activity at cloned human 5HT1A receptor expressed in CHO cells by inhibition of forskolin-induced cAMP production
191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21
CHEMBL4750444 5ht1a_human Human No 7.5 EC50 = 29.5 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
451 8 2 4 3.2 NC(=O)c1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1
CHEMBL475090 5ht1a_human Human No 6.5 EC50 = 290 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
362 6 1 4 4.0 c1ccc2c(c1)CC(CCN1CCCC(c3ccnc(NC4CC4)n3)C1)C2
CHEMBL39 5ht1a_human Human Yes 8.5 EC50 = 3 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL340705 5ht1a_human Human No 8.5 EC50 = 3 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
345 8 2 3 4.3 c1cnc2c(OCCNCCCc3c[nH]c4ccccc34)cccc2c1
CHEMBL45101 5ht1a_human Human No 8.5 EC50 = 3.0 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
443 6 2 4 4.4 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3cc[nH]n3)n2)CC1
CHEMBL4290309 5ht1a_human Human No 8.5 EC50 = 3.1 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
553 8 0 9 2.9 CC(=O)O[C@H]1[C@H]2C[C@H]([C@@H]3C(=O)N(CCCCN4CCN(c5cccc6sccc56)CC4)C(=O)[C@H]23)[C@H]1OC(C)=O
CHEMBL4287752 5ht1a_human Human No 8.5 EC50 = 3.3 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
436 6 0 6 3.0 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3scnc23)CC1
CHEMBL111065 5ht1a_human Human No 8.5 EC50 = 3.3 nM Bind
Stimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cellsStimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells
417 6 1 4 4.7 CCc1cccc(OC[C@@H](O)CN2CCC3(CC2)OCc2c3ccc3ccccc23)c1
CHEMBL4777475 5ht1a_human Human No 8.5 EC50 = 3.4 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
434 6 1 6 3.5 O=c1[nH]c(=O)n(CCCCN2CCN(c3cccc4sccc34)CC2)c2ccccc12
CHEMBL42393 5ht1a_human Human No 8.5 EC50 = 3.5 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
445 6 1 4 4.9 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3ccco3)n2)CC1
CHEMBL111713 5ht1a_human Human No 8.5 EC50 = 3.5 nM Bind
Stimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cellsStimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells
461 5 1 5 4.4 O=C1CCc2c(F)ccc(OCC(O)CN3CCC4(CC3)OCc3c4ccc4ccccc34)c21
CHEMBL423181 5ht1a_human Human No 8.5 EC50 = 3.5 nM Bind
Agonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assayAgonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assay
351 5 0 4 3.4 COC1=CC2=C(CCC(C2)CCN3CCN(CC3)C4=CC=CC=N4)C=C1
CHEMBL4757755 5ht1a_human Human No 8.5 EC50 = 3.5 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
449 7 2 4 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3c2CCN3)CC1
CHEMBL207220 5ht1a_human Human No 8.4 EC50 = 3.6 nM Funct
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
464 10 1 5 3.4 CC(=O)Nc1cccc(N2CCN(CCCCN(C)S(=O)(=O)CC3CCCCC3)CC2)c1
CHEMBL4277101 5ht1a_human Human No 8.4 EC50 = 3.6 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
435 6 0 5 3.6 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL4285839 5ht1a_human Human No 8.4 EC50 = 3.6 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
437 6 0 6 2.2 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1
CHEMBL360319 5ht1a_human Human No 8.4 EC50 = 3.6 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
422 6 1 4 3.7 CN(C)c1cccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1
CHEMBL39 5ht1a_human Human Yes 8.4 EC50 = 3.7 nM Bind
Tested for functional response on CHO cells expressing cloned human 5-hydroxytryptamine 1A receptorTested for functional response on CHO cells expressing cloned human 5-hydroxytryptamine 1A receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL45336 5ht1a_human Human No 8.4 EC50 = 3.7 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
436 6 1 4 4.0 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1N(C)C
CHEMBL39 5ht1a_human Human Yes 8.4 EC50 = 3.8 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL1259072 5ht1a_human Human No 7.5 EC50 = 30 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(Br)s3)CC2)nc1
CHEMBL1259139 5ht1a_human Human No 7.5 EC50 = 30 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
381 5 1 4 3.8 Cc1ccc(CNCC2(F)CCN(C(=O)c3sccc3Cl)CC2)nc1
CHEMBL1277651 5ht1a_human Human No 7.5 EC50 = 30.7 nM Funct
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
428 6 1 7 2.8 Nn1c(CCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2ccccc2c1=O
CHEMBL4067506 5ht1a_human Human No 7.5 EC50 = 30.8 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
430 4 1 8 3.0 Cc1nc2n(c(=O)c1CCN1CCN(c3csc4ccsc34)CC1)CCCC2O
CHEMBL39 5ht1a_human Human Yes 7.5 EC50 = 30.9 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht1a_human Human Yes 7.5 EC50 = 30.9 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL295025 5ht1a_human Human No 7.5 EC50 = 30.9 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
443 6 1 5 4.2 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-n3cccn3)n2)CC1
CHEMBL4061068 5ht1a_human Human No 6.5 EC50 = 300 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
439 4 1 8 2.5 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2(C)O
CHEMBL3805046 5ht1a_human Human No 6.5 EC50 = 301 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
453 8 1 4 4.5 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1F
CHEMBL233591 5ht1a_human Human No 6.5 EC50 = 301.2 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
417 7 1 3 5.5 CCCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3ncccc3c2C1
CHEMBL473902 5ht1a_human Human No 6.5 EC50 = 302 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
363 7 2 4 4.2 CCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1
CHEMBL230963 5ht1a_human Human Yes 6.5 EC50 = 302 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F
CHEMBL3804954 5ht1a_human Human No 6.5 EC50 = 309 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
435 8 1 4 4.3 CNC(=O)c1ccccc1OCCCCN1CCN(c2cccc(Cl)c2Cl)CC1
CHEMBL231373 5ht1a_human Human No 6.5 EC50 = 309.0 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
409 6 2 5 3.0 CNc1ccnc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1
CHEMBL45094 5ht1a_human Human No 6.5 EC50 = 309.0 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
475 7 1 5 4.6 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CF)(CNCc2cccc(-n3cccn3)n2)CC1
CHEMBL4476699 5ht1a_human Human No 7.5 EC50 = 31 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
439 8 1 4 5.0 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1Cl
CHEMBL114452 5ht1a_human Human No 7.5 EC50 = 31 nM Bind
Stimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cellsStimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells
403 6 1 4 4.2 OC(COCc1ccccc1)CN1CCC2(CC1)OCc1c2ccc2ccccc12
CHEMBL1926748 5ht1a_human Human No 7.5 EC50 = 31.5 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
375 7 1 5 2.1 O=C1C2CSCN2C(=O)N1CCCCNCC1CCc2ccccc2O1
CHEMBL1962696 5ht1a_human Human No 7.5 EC50 = 31.5 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
375 7 1 5 2.1 O=C1C2CSCN2C(=O)N1CCCCNCC1CCc2ccccc2O1
CHEMBL56 5ht1a_human Human Yes 7.5 EC50 = 31.6 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL56 5ht1a_human Human Yes 7.5 EC50 = 31.6 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL81095 5ht1a_human Human No 7.5 EC50 = 31.6 nM Funct
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
413 7 1 5 2.9 O=C(NCCCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1
CHEMBL1259017 5ht1a_human Human No 6.5 EC50 = 310 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
381 5 1 5 2.8 Cc1ccc(CNCC2(F)CCN(C(=O)c3cnn4ccccc34)CC2)nc1
CHEMBL4790662 5ht1a_human Human No 6.5 EC50 = 316.2 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
454 8 1 4 4.6 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1
CHEMBL1084132 5ht1a_human Human No 5.5 EC50 = 3162.3 nM Bind
Binding affinity to 5HT1A receptorBinding affinity to 5HT1A receptor
245 3 1 3 1.9 c1ccc(N2CCN(CC3CCCCN3)C2)cc1
CHEMBL207478 5ht1a_human Human No 7.5 EC50 = 32 nM Funct
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
424 10 1 5 2.5 CC(=O)Nc1cccc(N2CCN(CCCCN(C)S(=O)(=O)CC(C)C)CC2)c1
CHEMBL1259184 5ht1a_human Human No 7.5 EC50 = 32 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
371 5 2 5 2.7 Cc1ccc(CNCC2(O)CC3CCC(C2)N3C(=O)c2ccsc2)nc1
CHEMBL56 5ht1a_human Human Yes 7.5 EC50 = 32.4 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL221131 5ht1a_human Human No 7.5 EC50 = 32.4 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
377 8 1 3 5.5 CCC1(C)Cc2cccc(OCCNCc3cccc(C4=CCCC4)c3)c2O1
CHEMBL4796345 5ht1a_human Human No 7.5 EC50 = 32.4 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
437 8 2 4 4.1 CNc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL4103509 5ht1a_human Human No 7.5 EC50 = 32.9 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
422 4 0 7 3.1 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2=O
CHEMBL39 5ht1a_rat Rat Yes 6.5 EC50 = 323 nM Funct
Agonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS binding
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL478413 5ht1a_rat Rat No 6.5 EC50 = 323 nM Funct
Agonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS binding
370 6 0 6 4.0 c1ccc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1
CHEMBL218166 5ht1a_human Human Yes 6.5 EC50 = 323.6 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
385 4 1 4 4.1 O=c1[nH]c2cccc(N3CCN(Cc4cccc(-c5ccccc5)c4)CC3)c2o1
CHEMBL203282 5ht1a_human Human No 6.5 EC50 = 329 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
381 7 2 3 4.4 CC(C)CN1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21
CHEMBL204331 5ht1a_human Human No 6.5 EC50 = 329 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
363 7 2 3 4.4 CC(C)N1CC(CNCCCc2c[nH]c3ccccc23)Oc2ccccc21
CHEMBL39 5ht1a_human Human Yes 7.5 EC50 = 33.1 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht1a_human Human Yes 7.5 EC50 = 33.1 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL296289 5ht1a_human Human No 7.5 EC50 = 33.1 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
436 6 1 4 4.0 Cc1cc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc(N(C)C)c1
CHEMBL203067 5ht1a_human Human No 7.5 EC50 = 33.6 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
321 5 2 3 3.2 CN1CC(CNCCc2c[nH]c3ccccc23)Oc2ccccc21
CHEMBL218313 5ht1a_human Human No 7.5 EC50 = 33.9 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
361 7 1 3 4.9 C1=C(c2cccc(CNCCOc3cccc4c3OC3(CC3)C4)c2)CCC1
CHEMBL574700 5ht1a_human Human No 6.5 EC50 = 330 nM Funct
Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
610 11 2 9 4.8 COc1ccccc1N1CCN(CCCc2cn(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1
CHEMBL4753394 5ht1a_human Human No 6.5 EC50 = 331.1 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
454 8 1 4 4.6 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1
CHEMBL391531 5ht1a_human Human No 6.5 EC50 = 332.4 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4c(ccc5ncccc45)C3)c2c1
CHEMBL382857 5ht1a_human Human No 6.5 EC50 = 336 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
373 5 2 3 4.0 CN1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2cc(Cl)ccc21
CHEMBL140406 5ht1a_human Human No 5.5 EC50 = 3388.4 nM Bind
Agonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assayAgonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assay
363 5 0 4 4.0 COC1=CC=CC\2=C1CCC/C2=C\CCN3CCN(CC3)C4=CC=CC=N4
CHEMBL592953 5ht1a_human Human No 7.5 EC50 = 34 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
435 7 2 3 4.2 CCCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NCC3
CHEMBL1259016 5ht1a_human Human No 7.5 EC50 = 34 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccccc4o3)CC2)nc1
CHEMBL4094926 5ht1a_human Human No 7.5 EC50 = 34.1 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
423 4 1 6 4.0 Cc1nc2n(c(=O)c1CCN1CCC(c3cccc4sccc34)CC1)CCCC2O
CHEMBL1926758 5ht1a_human Human No 7.5 EC50 = 34.2 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
348 8 1 5 2.8 O=C1CSC(=O)N1CCCCCNCC1CCc2ccccc2O1
CHEMBL1962806 5ht1a_human Human No 7.5 EC50 = 34.2 nM Funct
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
348 8 1 5 2.8 O=C1CSC(=O)N1CCCCCNCC1CCc2ccccc2O1
CHEMBL3806224 5ht1a_human Human No 7.5 EC50 = 34.4 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
469 8 1 4 5.0 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1Cl
CHEMBL4739908 5ht1a_human Human No 7.5 EC50 = 34.7 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1
CHEMBL4126486 5ht1a_human Human No 7.5 EC50 = 35.0 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4cccc5c(N)c6c(nc45)CCCC6)CC3)c2c1
CHEMBL3597649 5ht1a_human Human No 6.5 EC50 = 340 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
434 8 2 6 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cnc3ccccc3c2)CC1
CHEMBL598346 5ht1a_human Human No 6.5 EC50 = 341 nM Funct
Agonist activity at 5HT1A receptor by GTPgammaS assayAgonist activity at 5HT1A receptor by GTPgammaS assay
289 3 1 2 4.2 Fc1ccccc1Oc1cccc(F)c1C1CCNCC1
CHEMBL598346 5ht1a_human Human No 6.5 EC50 = 341 nM Funct
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
289 3 1 2 4.2 Fc1ccccc1Oc1cccc(F)c1C1CCNCC1
CHEMBL1523325 5ht1a_human Human Yes 4.5 EC50 = 34800 nM Funct
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
314 5 3 2 2.7 O=C(O)C1CCCCC1C(=O)NCCc1c[nH]c2ccccc12
CHEMBL137485 5ht1a_human Human No 7.5 EC50 = 35 nM Funct
Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.
244 3 1 2 2.8 COc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1
CHEMBL126536 5ht1a_human Human No 7.5 EC50 = 35 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
363 8 2 3 4.5 Fc1ccc2[nH]cc(CCCNCCOc3cccc4ncccc34)c2c1
CHEMBL1259122 5ht1a_human Human No 7.5 EC50 = 35 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
361 5 1 4 3.5 Cc1ccc(CNCC2(F)CCN(C(=O)c3sccc3C)CC2)nc1
CHEMBL591561 5ht1a_human Human No 6.5 EC50 = 350 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
433 6 2 3 4.3 O=C1NCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)C1CCC1)CO3
CHEMBL4553059 5ht1a_human Human No 6.5 EC50 = 351 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding
457 8 1 4 4.9 CCc1cccc(N2CCN(CC(F)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl
CHEMBL593865 5ht1a_human Human No 7.4 EC50 = 36 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
447 7 2 3 4.2 O=C1NCCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3
CHEMBL1259036 5ht1a_human Human No 7.4 EC50 = 36 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
495 5 1 3 3.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccccc4[te]3)CC2)nc1
CHEMBL3805262 5ht1a_human Human No 6.4 EC50 = 361 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
453 8 1 4 4.5 CNC(=O)c1cc(F)cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1
CHEMBL231272 5ht1a_human Human No 5.4 EC50 = 3630.8 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
430 6 1 4 3.9 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ncc(C(F)F)cn2)CC1
CHEMBL4793515 5ht1a_human Human No 5.4 EC50 = 3630.8 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
424 7 1 3 4.8 C1CN(CCC1(CNCCSC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL114453 5ht1a_human Human No 7.4 EC50 = 37 nM Bind
Stimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cellsStimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells
387 5 1 3 4.7 OC(CCc1ccccc1)CN1CCC2(CC1)OCc1c2ccc2ccccc12
CHEMBL444612 5ht1a_human Human Yes 5.4 EC50 = 3700 nM Funct
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
234 5 1 1 3.2 CCN(CC)CCc1c[nH]c2cc(F)ccc12
CHEMBL4777749 5ht1a_human Human No 6.4 EC50 = 373.8 nM Funct
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
380 7 0 5 2.1 O=C(c1ccccc1)N(CCCN1CCN(c2ccccn2)CC1)C1COC1
CHEMBL275854 5ht1a_human Human Yes 6.4 EC50 = 378 nM Bind
Tested for functional response on CHO cells expressing cloned human 5-hydroxytryptamine 1A receptorTested for functional response on CHO cells expressing cloned human 5-hydroxytryptamine 1A receptor
190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N
CHEMBL49 5ht1a_human Human Yes 7.4 EC50 = 38.0 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL4777581 5ht1a_human Human No 7.4 EC50 = 38.0 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
451 8 2 4 3.2 NC(=O)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL4754941 5ht1a_human Human No 7.4 EC50 = 38.9 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
425 7 1 4 4.0 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2ccccn2)CC1
CHEMBL383688 5ht1a_human Human No 6.4 EC50 = 386 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
393 4 2 4 4.3 COc1cccc2c1OC(CN1CC=C(c3c[nH]c4ccc(F)cc34)CC1)CN2
CHEMBL230963 5ht1a_human Human Yes 6.4 EC50 = 389.1 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F
CHEMBL39 5ht1a_human Human Yes 7.4 EC50 = 39 nM Bind
Agonist activity at 5HT1A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL1259109 5ht1a_human Human No 7.4 EC50 = 39 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
403 5 1 5 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccsc4s3)CC2)nc1
CHEMBL4218720 5ht1a_rat Rat No 7.4 EC50 = 39.8 nM Funct
Agonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assay
498 7 0 6 4.7 CC(=O)c1c(OCCCN2CCN(c3ccccc3Br)CC2)ccc2c(C)cc(=O)oc12
CHEMBL4752833 5ht1a_human Human No 7.4 EC50 = 39.8 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
442 7 1 3 4.7 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1
CHEMBL44841 5ht1a_human Human No 7.4 EC50 = 39.8 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
459 6 2 6 3.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(O)(CNCc2cccc(-n3cccn3)n2)CC1
CHEMBL236518 5ht1a_human Human No 6.4 EC50 = 394 nM Funct
Antagonist activity at human 5HT1A expressed in mouse LM(tK-) cells assessed as 5-HT-stimulated [35S]GTPgammaS bindingAntagonist activity at human 5HT1A expressed in mouse LM(tK-) cells assessed as 5-HT-stimulated [35S]GTPgammaS binding
302 7 3 3 3.2 OC(CCNC1CCCCC1)COc1cccc2[nH]ccc12
CHEMBL595744 5ht1a_human Human No 8.4 EC50 = 4 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
411 5 3 3 3.3 O=C1NCCc2cc(F)c3c(c21)CC(NCCCc1c[nH]c2ccc(F)cc12)CO3
CHEMBL340301 5ht1a_human Human No 8.4 EC50 = 4 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
333 8 3 2 4.3 c1ccc2c(CCCNCCOc3cccc4[nH]ccc34)c[nH]c2c1
CHEMBL4763837 5ht1a_human Human No 8.4 EC50 = 4.1 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
466 6 1 5 3.7 O=C1NCC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)c2cc(F)ccc21
CHEMBL3805860 5ht1a_human Human No 8.4 EC50 = 4.3 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3nsc4ccccc34)CC2)c1
CHEMBL126484 5ht1a_human Human No 8.4 EC50 = 4.3 nM Bind
Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cellsEffective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells
342 9 2 3 3.9 COc1ccccc1OCCNCCCc1c[nH]c2ccc(F)cc12
CHEMBL4083333 5ht1a_human Human No 8.3 EC50 = 4.6 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
408 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2
CHEMBL230963 5ht1a_human Human Yes 8.3 EC50 = 4.7 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F
CHEMBL230963 5ht1a_human Human Yes 8.3 EC50 = 4.7 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F
CHEMBL338982 5ht1a_human Human No 8.3 EC50 = 4.7 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
354 8 2 3 3.8 Fc1ccc2[nH]cc(CCCNCCOc3cccc4c3OCC4)c2c1
CHEMBL127171 5ht1a_human Human No 8.3 EC50 = 4.7 nM Bind
Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cellsEffective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells
360 9 2 3 4.1 COc1ccc(F)cc1OCCNCCCc1c[nH]c2ccc(F)cc12
CHEMBL4753414 5ht1a_human Human No 8.3 EC50 = 4.9 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
410 7 1 5 2.9 C1CN(CCC1(CNCCOC2=NC=CN=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL515573 5ht1a_human Human No 7.4 EC50 = 40.7 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
379 8 2 5 3.4 COCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1
CHEMBL4741857 5ht1a_human Human No 7.4 EC50 = 40.7 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
408 7 1 3 4.1 C1CN(CCC1(CNCCOC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL431332 5ht1a_human Human No 6.4 EC50 = 407.4 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
407 6 1 3 4.2 CCc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1
CHEMBL49 5ht1a_human Human Yes 7.4 EC50 = 41 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL126484 5ht1a_human Human No 7.4 EC50 = 41.6 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
342 9 2 3 3.9 COc1ccccc1OCCNCCCc1c[nH]c2ccc(F)cc12
CHEMBL203726 5ht1a_human Human No 6.4 EC50 = 418 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
421 5 1 4 4.7 CCN1CC(CN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)Oc2c(OC)cccc21
CHEMBL1259121 5ht1a_human Human No 7.4 EC50 = 42 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
361 5 1 4 3.5 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(C)s3)CC2)nc1
CHEMBL4205326 5ht1a_human Human No 7.4 EC50 = 42.3 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
443 8 1 7 3.2 CNC(=O)c1cncc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)c1
CHEMBL396062 5ht1a_human Human No 7.4 EC50 = 42.7 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
443 6 2 5 3.7 CNc1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ncc1Cl
CHEMBL4747425 5ht1a_human Human No 7.4 EC50 = 42.7 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(F)cc2)CC1
CHEMBL3597637 5ht1a_human Human No 7.4 EC50 = 43 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
452 8 1 5 4.2 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cnc3ccccc3c2)CC1
CHEMBL39 5ht1a_human Human Yes 7.4 EC50 = 43 nM Funct
Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pigCompound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pig
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL4752177 5ht1a_human Human No 7.4 EC50 = 43.7 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
481 8 2 4 4.6 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1
CHEMBL593281 5ht1a_human Human No 6.4 EC50 = 436 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
483 6 2 3 4.6 O=C1NCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)C(=O)c1ccccc1)CO3
CHEMBL124818 5ht1a_human Human No 7.4 EC50 = 44 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
338 10 2 3 4.2 COc1ccccc1OCCNCCCCc1c[nH]c2ccccc12
CHEMBL1774538 5ht1a_human Human No 6.4 EC50 = 440 nM Funct
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
441 8 1 5 4.2 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3s2)CC1
CHEMBL231372 5ht1a_human Human No 6.4 EC50 = 446.7 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
410 6 1 5 3.0 COc1ccnc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1
CHEMBL4754363 5ht1a_human Human No 6.4 EC50 = 446.7 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
406 7 1 2 4.6 C1CN(CCC1(CNCCCC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL2431038 5ht1a_human Human No 7.4 EC50 = 45 nM Funct
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
381 9 1 4 3.0 O=C1C2CCCN2C(=O)N1CCCCNCCOc1cccc2ccccc12
CHEMBL3040400 5ht1a_human Human No 7.4 EC50 = 45 nM Funct
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
381 9 1 4 3.0 O=C1C2CCCN2C(=O)N1CCCCNCCOc1cccc2ccccc12
CHEMBL39 5ht1a_human Human Yes 7.3 EC50 = 45.3 nM Bind
Partial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assayPartial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL4742122 5ht1a_human Human No 7.3 EC50 = 45.7 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
409 7 1 4 3.5 C1CN(CCC1(CNCCOC2=CN=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL4097395 5ht1a_human Human No 6.4 EC50 = 450 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
425 4 1 8 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3nccc4sccc34)CC1)CCCC2O
CHEMBL1112 5ht1a_human Human Yes 6.4 EC50 = 450 nM Bind
pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).
447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL4745192 5ht1a_human Human No 6.3 EC50 = 451.6 nM Funct
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
433 8 0 3 5.1 CCCN(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)C(=O)c1ccccc1
CHEMBL125902 5ht1a_human Human No 7.3 EC50 = 46 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
364 8 2 4 3.9 Fc1ccc2[nH]cc(CCCNCCOc3cccc4nccnc34)c2c1
CHEMBL1259138 5ht1a_human Human No 7.3 EC50 = 46 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
381 5 1 4 3.8 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)s3)CC2)nc1
CHEMBL4752859 5ht1a_human Human No 7.3 EC50 = 46.1 nM Funct
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
433 7 0 3 5.1 CC(C)N(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)C(=O)c1ccccc1
CHEMBL221743 5ht1a_human Human No 7.3 EC50 = 46.8 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
365 9 1 3 5.6 CC(C)Oc1ccccc1OCCNCc1cccc(C2=CCCCC2)c1
CHEMBL4786537 5ht1a_human Human No 7.3 EC50 = 46.8 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
407 7 1 3 4.0 C1CN(CCC1(CNCCCC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL80189 5ht1a_human Human No 6.3 EC50 = 460 nM Funct
Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pigCompound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pig
305 4 1 4 3.0 CN(C)CCc1c[nH]c2ccc(-n3cnc4cccnc43)cc12
CHEMBL3805826 5ht1a_human Human No 6.3 EC50 = 464 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
491 12 1 4 5.9 CCCCCNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1
CHEMBL83597 5ht1a_rat Rat Yes 7.3 EC50 = 47 nM Funct
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
351 5 2 5 3.9 CN1CCC[C@@H]1Cc1c[nH]c2ccc(Nc3ncccc3[N+](=O)[O-])cc12
CHEMBL1259223 5ht1a_human Human No 7.3 EC50 = 47 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
385 5 1 3 3.6 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC3C5)C4)CC2)nc1
CHEMBL4753394 5ht1a_human Human No 7.3 EC50 = 47.9 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
454 8 1 4 4.6 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1
CHEMBL4742122 5ht1a_human Human No 7.3 EC50 = 47.9 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
409 7 1 4 3.5 C1CN(CCC1(CNCCOC2=CN=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL46379 5ht1a_human Human No 7.3 EC50 = 47.9 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
436 6 1 4 4.0 Cc1ccc(N(C)C)nc1CNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1
CHEMBL4283369 5ht1a_human Human No 7.3 EC50 = 47.9 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
453 6 0 5 4.8 O=C1c2ccc(Cl)cc2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL4797752 5ht1a_human Human No 6.3 EC50 = 478.6 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(Cl)cc2)CC1
CHEMBL4471669 5ht1a_human Human No 7.3 EC50 = 48 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
280 5 0 2 3.8 CCCCN1CCN(c2cccc(CC)c2Cl)CC1
CHEMBL1259224 5ht1a_human Human No 7.3 EC50 = 48 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
433 5 1 3 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC(Cl)(C5)C3)C4)CC2)nc1
CHEMBL4101115 5ht1a_human Human No 6.3 EC50 = 488 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
443 4 0 7 3.6 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2Cl
CHEMBL589141 5ht1a_human Human No 7.3 EC50 = 49 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
447 8 2 3 4.6 O=C1NCc2ccc3c(c21)CC(N(CCCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3
CHEMBL4647189 5ht1a_human Human No 5.3 EC50 = 4966 nM Bind
Partial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assayPartial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assay
566 9 0 5 6.9 c1ccc(CS/C(=N/CC[N+]2(Cc3ccccc3)CCN(c3ncccn3)CC2)C23CC4CC(CC(C4)C2)C3)cc1
CHEMBL4650861 5ht1a_human Human No 5.3 EC50 = 4966 nM Bind
Partial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assayPartial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assay
566 9 0 5 6.9 c1ccc(CS/C(=N/CC[N+]2(Cc3ccccc3)CCN(c3ncccn3)CC2)C23CC4CC(CC(C4)C2)C3)cc1
CHEMBL46467 5ht1a_human Human No 8.3 EC50 = 5.0 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
460 6 1 5 5.2 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3nccs3)n2)CC1
CHEMBL3805704 5ht1a_human Human No 8.3 EC50 = 5.1 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
423 8 1 5 4.2 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4sccc34)CC2)c1
CHEMBL42294 5ht1a_human Human No 8.3 EC50 = 5.2 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
443 6 1 4 5.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3ccco3)n2)CC1
CHEMBL543377 5ht1a_human Human No 8.3 EC50 = 5.2 nM Funct
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
384 6 0 5 3.4 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1
CHEMBL81118 5ht1a_human Human No 8.3 EC50 = 5.2 nM Funct
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
384 6 0 5 3.4 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1
CHEMBL39 5ht1a_human Human Yes 8.3 EC50 = 5.6 nM Bind
Agonist activity at human recombinant 5-HT1A receptor expressed in CHOK1 cells measured after 1 hr by microbeta2 scintillation counterAgonist activity at human recombinant 5-HT1A receptor expressed in CHOK1 cells measured after 1 hr by microbeta2 scintillation counter
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht1a_human Human Yes 8.2 EC50 = 5.7 nM Funct
Agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in calcium flux by fluorimetric methodAgonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in calcium flux by fluorimetric method
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL4747425 5ht1a_human Human No 8.2 EC50 = 5.8 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(F)cc2)CC1
CHEMBL4760271 5ht1a_human Human No 8.2 EC50 = 5.8 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2F)CC1
CHEMBL311015 5ht1a_human Human No 8.2 EC50 = 5.8 nM Funct
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
421 6 0 6 2.7 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1
CHEMBL295662 5ht1a_human Human No 8.2 EC50 = 5.8 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
418 6 1 4 3.8 Cc1ccc(C(=O)N2CCC(F)(CNCc3cccc(N(C)C)n3)CC2)cc1Cl
CHEMBL42618 5ht1a_human Human No 8.2 EC50 = 5.8 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
459 6 1 4 5.8 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3cccs3)n2)CC1
CHEMBL4288388 5ht1a_human Human No 8.2 EC50 = 5.8 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
453 6 0 5 4.8 O=C1c2cccc(Cl)c2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL39 5ht1a_human Human Yes 8.2 EC50 = 5.8 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT1A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL56 5ht1a_human Human Yes 8.2 EC50 = 5.8 nM Funct
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL221692 5ht1a_human Human Yes 8.2 EC50 = 5.9 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1
CHEMBL4751170 5ht1a_human Human Yes 8.2 EC50 = 5.9 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1
CHEMBL4648979 5ht1a_human Human No 8.2 EC50 = 5.9 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
432 6 0 8 3.2 N#Cc1ccn2c(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)nc2c1
CHEMBL421064 5ht1a_human Human No 7.3 EC50 = 50 nM Funct
Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 50-550Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 50-550
378 6 2 4 2.4 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(c4ccccc4)CC3)cc12
CHEMBL1259198 5ht1a_human Human No 7.3 EC50 = 50 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
411 6 1 5 3.8 COc1c(C(=O)N2CCC(F)(CNCc3ccc(C)cn3)CC2)csc1Cl
CHEMBL1802360 5ht1a_human Human Yes 7.3 EC50 = 50.1 nM Bind
Activity at 5HT1A receptorActivity at 5HT1A receptor
369 6 1 4 3.6 O=c1[nH]c2ccccc2n1C1CCN(CCCOc2ccc(F)cc2)CC1
CHEMBL39 5ht1a_human Human Yes 7.3 EC50 = 50.1 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL56 5ht1a_human Human Yes 7.3 EC50 = 51.3 nM Bind
Agonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assayAgonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assay
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL475502 5ht1a_human Human No 7.3 EC50 = 51.4 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
379 8 3 5 3.2 OCCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1
CHEMBL348588 5ht1a_human Human Yes 5.3 EC50 = 5100 nM Funct
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
174 3 2 1 1.9 CNCCc1c[nH]c2ccccc12
CHEMBL4125732 5ht1a_human Human No 7.3 EC50 = 52 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
464 5 2 5 4.8 N#Cc1ccc2[nH]cc(CCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1
CHEMBL1259181 5ht1a_human Human No 7.3 EC50 = 52 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
391 5 1 3 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc4ccccc4c3)CC2)nc1
CHEMBL206130 5ht1a_human Human No 7.3 EC50 = 52.2 nM Funct
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
355 6 3 4 3.3 COc1cccc2c1OC(CNCCc1c[nH]c3ccc(F)cc13)CN2
CHEMBL4746734 5ht1a_human Human No 7.3 EC50 = 52.5 nM Bind
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
424 7 1 5 3.2 CC1=CN=C(N=C1)OCCNCC2(CCN(CC2)C(=O)C3=CC(=C(C=C3)F)Cl)F
CHEMBL119455 5ht1a_rat Rat No 5.3 EC50 = 5200 nM Funct
Ability to inhibit 5-HT sensitive,forskolin-stimulated adenylyl cyclase(FSC) activity in rat hippocampal membranes mediated through 5-hydroxytryptamine 1A receptorAbility to inhibit 5-HT sensitive,forskolin-stimulated adenylyl cyclase(FSC) activity in rat hippocampal membranes mediated through 5-hydroxytryptamine 1A receptor
251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3
CHEMBL4797752 5ht1a_human Human No 5.3 EC50 = 5248.1 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(Cl)cc2)CC1
CHEMBL4760621 5ht1a_human Human No 7.3 EC50 = 53.7 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
422 7 1 3 4.4 Cc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL4790600 5ht1a_human Human No 7.3 EC50 = 53.7 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
478 7 1 4 4.8 CC1(C)Cc2cccc(OCCNCC3(F)CCN(C(=O)c4ccc(F)c(Cl)c4)CC3)c2O1
CHEMBL594357 5ht1a_human Human No 7.3 EC50 = 54 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
447 6 2 3 4.4 O=C1NCCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)C1CCC1)CO3
CHEMBL1259153 5ht1a_human Human No 7.3 EC50 = 54 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
393 6 1 5 3.9 CSc1ccc(C(=O)N2CCC(F)(CNCc3ccc(C)cn3)CC2)s1
CHEMBL4754651 5ht1a_human Human No 7.3 EC50 = 54.5 nM Funct
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
366 8 0 4 3.1 CCCN(CCCN1CCN(c2ccccn2)CC1)C(=O)c1ccccc1
CHEMBL4740097 5ht1a_human Human No 7.3 EC50 = 55.0 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
408 7 2 4 3.5 C1CN(CCC1(CNCCNC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL4452084 5ht1a_human Human No 4.3 EC50 = 54400 nM Bind
Agonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assayAgonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assay
354 4 2 4 2.7 C=C[C@H]1CN2CCc3c([nH]c4ccccc34)[C@H]2C[C@@H]1[C@H](CO)C(=O)OC
CHEMBL4746386 5ht1a_human Human No 6.3 EC50 = 549.5 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2Cl)CC1
CHEMBL53510 5ht1a_rat Rat Yes 7.3 EC50 = 55 nM Funct
Ability to inhibit 5-HT sensitive,forskolin-stimulated adenylyl cyclase(FSC) activity in rat hippocampal membranes mediated through 5-hydroxytryptamine 1A receptorAbility to inhibit 5-HT sensitive,forskolin-stimulated adenylyl cyclase(FSC) activity in rat hippocampal membranes mediated through 5-hydroxytryptamine 1A receptor
265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3
CHEMBL608728 5ht1a_human Human No 7.3 EC50 = 56 nM Funct
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
291 3 0 2 4.0 C=CCOc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3
CHEMBL4463030 5ht1a_human Human No 7.3 EC50 = 56 nM Funct
Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assayAgonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay
495 8 0 5 4.2 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1
CHEMBL340895 5ht1a_human Human No 7.3 EC50 = 56 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
370 8 2 3 4.8 Fc1cc(OCCNCCCc2c[nH]c3ccc(F)cc23)c2occc2c1
CHEMBL39 5ht1a_human Human Yes 7.3 EC50 = 56.2 nM Bind
Agonist activity at human recombinant 5-HT1A receptor expressed in CHOK1 cells measured after 1 hr by microbeta2 scintillation counterAgonist activity at human recombinant 5-HT1A receptor expressed in CHOK1 cells measured after 1 hr by microbeta2 scintillation counter
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL4740430 5ht1a_human Human No 7.3 EC50 = 56.2 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
476 7 1 3 5.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(C(F)(F)F)c2)CC1
CHEMBL4747083 5ht1a_human Human No 6.3 EC50 = 562.3 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
438 8 1 4 4.1 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)cc1
CHEMBL31115 5ht1a_human Human Yes 6.3 EC50 = 564 nM Bind
Tested for functional response on CHO cells expressing cloned human 5-hydroxytryptamine 1A receptorTested for functional response on CHO cells expressing cloned human 5-hydroxytryptamine 1A receptor
204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1
CHEMBL4127877 5ht1a_human Human No 6.3 EC50 = 567 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4ccc5c(N)c6c(nc5c4)CCCC6)CC3)c2c1
CHEMBL39 5ht1a_human Human Yes 7.2 EC50 = 58.9 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL4800286 5ht1a_human Human No 6.2 EC50 = 583.2 nM Funct
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
447 7 0 4 4.0 O=C(c1ccccc1)N(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1COC1
CHEMBL1259123 5ht1a_human Human No 7.2 EC50 = 59 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
437 5 1 5 5.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3sc4sccc4c3Cl)CC2)nc1
CHEMBL3344459 5ht1a_human Human No 6.2 EC50 = 590 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assay
343 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)C)cc3CN1CC2
CHEMBL56 5ht1a_human Human Yes 8.2 EC50 = 6 nM Funct
Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assayAgonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL3805649 5ht1a_human Human No 8.2 EC50 = 6 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
441 8 1 5 4.4 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccc1F
CHEMBL4760666 5ht1a_human Human No 8.2 EC50 = 6.0 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
451 8 1 4 4.2 CN(C)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL4750444 5ht1a_human Human No 8.2 EC50 = 6.0 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
451 8 2 4 3.2 NC(=O)c1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1
CHEMBL311275 5ht1a_human Human No 8.2 EC50 = 6.0 nM Funct
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
352 6 0 4 3.6 c1ccc(CCCCN2CCN(c3cccc4c3OCCO4)CC2)cc1
CHEMBL543139 5ht1a_human Human No 8.2 EC50 = 6.0 nM Funct
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
352 6 0 4 3.6 c1ccc(CCCCN2CCN(c3cccc4c3OCCO4)CC2)cc1
CHEMBL4293718 5ht1a_human Human No 8.2 EC50 = 6.1 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
459 6 0 6 2.7 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3c2OC(F)(F)O3)CC1
CHEMBL4202871 5ht1a_human Human No 8.2 EC50 = 6.2 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
451 9 1 7 3.6 O=C(NC1CC1)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1
CHEMBL375297 5ht1a_human Human No 8.2 EC50 = 6.5 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
351 7 1 4 4.2 C1=C(c2cccc(CNCCOc3cccc4c3OCCO4)c2)CCC1
CHEMBL1259155 5ht1a_human Human No 8.2 EC50 = 6.6 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
391 5 2 4 2.9 Cc1ccc(CNCC2(O)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1
CHEMBL4790600 5ht1a_human Human No 8.2 EC50 = 6.6 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
478 7 1 4 4.8 CC1(C)Cc2cccc(OCCNCC3(F)CCN(C(=O)c4ccc(F)c(Cl)c4)CC3)c2O1
CHEMBL1742477 5ht1a_human Human Yes 8.2 EC50 = 6.6 nM Funct
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cellsCompound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells
415 6 2 6 1.5 OC[C@H]1COc2c(O1)cccc2N1CCN(CC1)CCNC(=O)c1ccc(cc1)F
CHEMBL44118 5ht1a_human Human No 8.2 EC50 = 6.6 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
424 6 2 4 4.2 CNc1cccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1
CHEMBL4637409 5ht1a_human Human No 8.2 EC50 = 6.7 nM Bind
Partial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assayPartial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assay
385 5 1 5 2.7 S=C(NCCN1CCN(c2ncccn2)CC1)C12CC3CC(CC(C3)C1)C2
CHEMBL311275 5ht1a_human Human No 8.2 EC50 = 6.8 nM Funct
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
352 6 0 4 3.6 c1ccc(CCCCN2CCN(c3cccc4c3OCCO4)CC2)cc1
CHEMBL543139 5ht1a_human Human No 8.2 EC50 = 6.8 nM Funct
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
352 6 0 4 3.6 c1ccc(CCCCN2CCN(c3cccc4c3OCCO4)CC2)cc1
CHEMBL4284346 5ht1a_human Human No 8.2 EC50 = 6.9 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL379984 5ht1a_human Human No 7.2 EC50 = 60 nM Funct
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
410 10 2 5 2.1 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)CC(C)C)CC2)c1
CHEMBL4760666 5ht1a_human Human No 7.2 EC50 = 60.3 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
451 8 1 4 4.2 CN(C)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL230963 5ht1a_human Human Yes 7.2 EC50 = 60.3 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F
CHEMBL230963 5ht1a_human Human Yes 7.2 EC50 = 60.3 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F
CHEMBL126253 5ht1a_human Human No 7.2 EC50 = 60.8 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
344 8 2 2 4.9 c1ccc2c(OCCNCCCc3c[nH]c4ccccc34)cccc2c1
CHEMBL1774532 5ht1a_human Human No 6.2 EC50 = 600 nM Funct
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
455 9 1 6 3.7 COc1ccc2oc(C(=O)NCCC(F)CN3CCN(c4ccccc4OC)CC3)cc2c1
CHEMBL1258996 5ht1a_human Human No 6.2 EC50 = 600 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
415 5 2 4 3.1 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC(O)(C5)C3)C4)CC2)nc1
CHEMBL4079365 5ht1a_human Human No 6.2 EC50 = 607 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
409 4 0 7 2.9 Cc1nc2n(c(=O)c1CCN1CCN(c3nccc4sccc34)CC1)CCCC2
CHEMBL4752833 5ht1a_human Human No 6.2 EC50 = 616.6 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
442 7 1 3 4.7 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1
CHEMBL4747083 5ht1a_human Human No 6.2 EC50 = 616.6 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
438 8 1 4 4.1 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)cc1
CHEMBL594829 5ht1a_human Human No 7.2 EC50 = 62 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
379 5 3 3 3.1 O=C1NCc2ccc3c(c21)CC(NCCCc1c[nH]c2ccc(F)cc12)CO3
CHEMBL1255610 5ht1a_human Human No 7.2 EC50 = 62 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
455 6 1 5 4.0 COc1c(C(=O)N2CCC(F)(CNCc3ccc(C)cn3)CC2)csc1Br
CHEMBL4128838 5ht1a_human Human No 7.2 EC50 = 62.4 nM Funct
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1
CHEMBL233591 5ht1a_human Human No 6.2 EC50 = 628.6 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
417 7 1 3 5.5 CCCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3ncccc3c2C1
CHEMBL1259090 5ht1a_human Human No 7.2 EC50 = 63 nM Funct
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
483 5 1 6 3.7 Cc1ccc(CNCC2(F)CCN(C(=O)c3sc(Br)c4c3OCCO4)CC2)nc1
CHEMBL4741857 5ht1a_human Human No 7.2 EC50 = 63.1 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
408 7 1 3 4.1 C1CN(CCC1(CNCCOC2=CC=CC=C2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL231068 5ht1a_human Human Yes 6.2 EC50 = 631.0 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2
CHEMBL4215022 5ht1a_rat Rat No 6.2 EC50 = 631.0 nM Funct
Antagonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes assessed as inhibition of 8-OH-DPAT-induced receptor activation after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assayAntagonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes assessed as inhibition of 8-OH-DPAT-induced receptor activation after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assay
450 8 0 7 3.9 COc1ccccc1N1CCN(CCCOc2ccc3c(C)cc(=O)oc3c2C(C)=O)CC1
CHEMBL311976 5ht1a_human Human No 6.2 EC50 = 631.0 nM Funct
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
429 4 0 7 1.4 O=C1c2ccccc2S(=O)(=O)N1CCN1CCN(c2cccc3c2OCCO3)CC1
CHEMBL4752833 5ht1a_human Human No 6.2 EC50 = 645.7 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
442 7 1 3 4.7 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1
CHEMBL474090 5ht1a_human Human No 7.2 EC50 = 65 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
393 9 2 5 3.8 COCCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1
CHEMBL4759629 5ht1a_human Human No 7.2 EC50 = 66.1 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
425 7 1 4 4.2 C1CN(CCC1(CNCCSC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL386988 5ht1a_human Human No 7.2 EC50 = 67.6 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
367 9 1 4 5.4 CC(C)Oc1ccccc1OCCNCc1cccc(-c2ccsc2)c1
CHEMBL8412 5ht1a_human Human Yes 7.2 EC50 = 67.6 nM Funct
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cellsCompound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells
401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL4074373 5ht1a_human Human No 6.2 EC50 = 680 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
427 4 0 7 3.3 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2F
CHEMBL142936 5ht1a_human Human Yes 6.2 EC50 = 680 nM Funct
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
216 5 1 1 3.1 CCN(CC)CCc1c[nH]c2ccccc12
CHEMBL39 5ht1a_human Human Yes 7.2 EC50 = 69.2 nM Funct
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL425833 5ht1a_human Human No 7.2 EC50 = 69.2 nM Funct
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
413 5 1 3 4.3 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(Cl)cn2)CC1
CHEMBL220809 5ht1a_human Human No 7.2 EC50 = 69.2 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
351 9 1 3 5.2 CC(C)Oc1ccccc1OCCNCc1cccc(C2=CCCC2)c1
CHEMBL4739908 5ht1a_human Human No 7.2 EC50 = 69.2 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1
CHEMBL4105102 5ht1a_human Human No 7.2 EC50 = 69.7 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
425 4 1 8 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4scnc34)CC1)CCCC2O
CHEMBL4640409 5ht1a_human Human No 8.2 EC50 = 7 nM Funct
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
485 6 0 7 4.1 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(Br)cccn12
CHEMBL4790303 5ht1a_human Human Yes 8.2 EC50 = 7 nM Funct
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
476 8 1 3 5.2 O=C(CN1CCN(CCCc2c[nH]c3ccc(F)cc23)CC1)N(c1ccccc1)C1CCCCC1
CHEMBL4790303 5ht1a_human Human Yes 8.2 EC50 = 7 nM Funct
Agonist activity at recombinant 5HT1A receptor (unknown origin) expressed in CHO cell membrane assessed as [35S]GTPgammaS binding by liquid scintillation counting methodAgonist activity at recombinant 5HT1A receptor (unknown origin) expressed in CHO cell membrane assessed as [35S]GTPgammaS binding by liquid scintillation counting method
476 8 1 3 5.2 O=C(CN1CCN(CCCc2c[nH]c3ccc(F)cc23)CC1)N(c1ccccc1)C1CCCCC1
CHEMBL298260 5ht1a_human Human No 8.2 EC50 = 7.1 nM Funct
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
432 6 1 4 4.2 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(N3CCC3)n2)CC1
CHEMBL4087132 5ht1a_human Human No 8.2 EC50 = 7.1 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
444 4 0 6 4.0 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2(F)F
CHEMBL4116744 5ht1a_human Human No 8.2 EC50 = 7.1 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
444 4 0 6 4.0 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2(F)F
CHEMBL31354 5ht1a_human Human Yes 8.2 EC50 = 7.1 nM Funct
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1
CHEMBL31354 5ht1a_human Human Yes 8.2 EC50 = 7.1 nM Bind
Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cellsEffective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells
422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1
CHEMBL4104261 5ht1a_human Human No 8.1 EC50 = 7.2 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
426 4 0 6 3.9 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2F
CHEMBL3805884 5ht1a_human Human No 8.1 EC50 = 7.2 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
453 8 1 4 4.5 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1F
CHEMBL4790662 5ht1a_human Human No 8.1 EC50 = 7.2 nM Bind
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
454 8 1 4 4.6 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1
CHEMBL543377 5ht1a_human Human No 8.1 EC50 = 7.4 nM Funct
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
384 6 0 5 3.4 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1
CHEMBL81118 5ht1a_human Human No 8.1 EC50 = 7.4 nM Funct
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
384 6 0 5 3.4 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1
CHEMBL19215 5ht1a_human Human Yes 8.1 EC50 = 7.5 nM Bind
Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cellsDisplacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells
403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C
CHEMBL4294617 5ht1a_human Human No 8.1 EC50 = 7.7 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
439 6 0 5 4.5 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL762 5ht1a_human Human Yes 7.2 EC50 = 70 nM Funct
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C
CHEMBL4786067 5ht1a_human Human No 7.2 EC50 = 70.8 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
438 8 1 4 4.1 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1
CHEMBL1774383 5ht1a_human Human No 7.1 EC50 = 71.6 nM Funct
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
462 9 1 5 4.0 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1
CHEMBL49 5ht1a_human Human Yes 7.1 EC50 = 72.4 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL49 5ht1a_human Human Yes 7.1 EC50 = 72.4 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL4740430 5ht1a_human Human No 6.1 EC50 = 724.4 nM Bind
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assayBiased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
476 7 1 3 5.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(C(F)(F)F)c2)CC1
CHEMBL4740430 5ht1a_human Human No 6.1 EC50 = 724.4 nM Funct
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
476 7 1 3 5.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(C(F)(F)F)c2)CC1
CHEMBL3805120 5ht1a_human Human No 7.1 EC50 = 74 nM Funct
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
449 8 1 4 4.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1C
CHEMBL4740097 5ht1a_human Human No 7.1 EC50 = 74.1 nM Funct
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
408 7 2 4 3.5 C1CN(CCC1(CNCCNC2=CC=CC=N2)F)C(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL2312934 5ht1a_human Human No 5.1 EC50 = 7400 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1
CHEMBL592028 5ht1a_human Human No 7.1 EC50 = 75 nM Funct
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
393 5 2 3 3.4 CN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NC3
CHEMBL2431146 5ht1a_human Human No 7.1 EC50 = 76 nM Funct
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
331 9 1 4 1.9 O=C1C2CCCN2C(=O)N1CCCCNCCOc1ccccc1
CHEMBL3040401 5ht1a_human Human No 7.1 EC50 = 76 nM Funct
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
331 9 1 4 1.9 O=C1C2CCCN2C(=O)N1CCCCNCCOc1ccccc1
CHEMBL4078409 5ht1a_human Human No 7.1 EC50 = 76.2 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
407 4 0 5 4.5 Cc1nc2n(c(=O)c1CCN1CCC(c3cccc4sccc34)CC1)CCCC2
CHEMBL4117823 5ht1a_human Human No 7.1 EC50 = 76.2 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
407 4 0 5 4.5 Cc1nc2n(c(=O)c1CCN1CCC(c3cccc4sccc34)CC1)CCCC2
CHEMBL4441358 5ht1a_human Human No 7.1 EC50 = 77 nM Funct
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
224 2 1 2 2.3 CCc1cccc(N2CCNCC2)c1Cl
CHEMBL1645617 5ht1a_human Human No 7.1 EC50 = 77 nM Funct
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
325 4 1 3 4.2 Fc1cccc(Cl)c1Oc1cccc(F)c1O[C@@H]1CCNC1
CHEMBL220808 5ht1a_human Human Yes 7.1 EC50 = 77.6 nM Funct
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S b