Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
10324985 76205 5 None - 1 Human 11.0 pEC50 = 11 Functional
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
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76205 5 None - 1 Human 11.0 pEC50 = 11 Functional
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
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76205 5 None - 1 Human 11.0 pEC50 = 11 Functional
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
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
132257058 180050 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
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
ChEMBL 449 7 2 4 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3c2CCN3)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4757755 180050 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
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
ChEMBL 449 7 2 4 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3c2CCN3)CC1 10.1021/acs.jmedchem.0c00814
132247312 179797 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
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
ChEMBL 465 8 2 4 4.1 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4755058 179797 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
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
ChEMBL 465 8 2 4 4.1 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
24804775 18976 0 None 31 2 Human 10.5 pEC50 = 10.5 Functional
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
ChEMBL 412 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290716 18976 0 None 31 2 Human 10.5 pEC50 = 10.5 Functional
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
ChEMBL 412 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
10324985 76205 5 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76205 5 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76205 5 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
132247307 179554 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 481 8 2 4 4.6 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4752177 179554 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 481 8 2 4 4.6 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
89638711 113558 1 None - 1 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 344 6 0 8 -0.1 Cn1c(=O)cnn(CCCCN2CCN(c3ccccn3)CC2)c1=O 10.1016/j.bmcl.2014.07.048
CHEMBL3330612 113558 1 None - 1 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 344 6 0 8 -0.1 Cn1c(=O)cnn(CCCCN2CCN(c3ccccn3)CC2)c1=O 10.1016/j.bmcl.2014.07.048
132247301 179911 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 447 7 2 3 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4756233 179911 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 447 7 2 3 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4633397 176265 0 None 70 3 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 426 6 0 8 2.8 O=c1n(CCCCN2CCN(c3cccc4scnc34)CC2)nc2c(F)cccn12 10.1016/j.bmcl.2020.127027
CHEMBL4647011 177197 0 None 263 3 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 425 6 0 7 3.5 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2ccc(F)cn12 10.1016/j.bmcl.2020.127027
CHEMBL4648027 177272 0 None 4073 3 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 475 6 0 7 4.6 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(Cl)cc(Cl)cn12 10.1016/j.bmcl.2020.127027
21830793 91177 2 None - 1 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmcl.2014.07.048
CHEMBL2413154 91177 2 None - 1 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmcl.2014.07.048
21830793 91177 2 None - 1 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 91177 2 None - 1 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
132256760 182379 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
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
ChEMBL 437 8 2 4 4.1 CNc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4796345 182379 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
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
ChEMBL 437 8 2 4 4.1 CNc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
4223 3761 82 None 8 15 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2018.04.037
6918314 3761 82 None 8 15 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2018.04.037
7427 3761 82 None 8 15 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2018.04.037
CHEMBL439849 3761 82 None 8 15 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2018.04.037
DB06684 3761 82 None 8 15 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2018.04.037
4223 3761 82 None 8 15 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2019.01.025
6918314 3761 82 None 8 15 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2019.01.025
7427 3761 82 None 8 15 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2019.01.025
CHEMBL439849 3761 82 None 8 15 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2019.01.025
DB06684 3761 82 None 8 15 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2019.01.025
18922713 97820 1 None - 1 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 10.1021/jm000339w
CHEMBL276031 97820 1 None - 1 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 10.1021/jm000339w
132256714 179528 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 438 8 1 4 4.1 COc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4751777 179528 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 438 8 1 4 4.1 COc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
71294258 113562 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 362 6 0 8 0.1 Cn1c(=O)cnn(CCCCN2CCN(c3cccc(F)n3)CC2)c1=O 10.1016/j.bmcl.2014.07.048
CHEMBL3330616 113562 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 362 6 0 8 0.1 Cn1c(=O)cnn(CCCCN2CCN(c3cccc(F)n3)CC2)c1=O 10.1016/j.bmcl.2014.07.048
11948707 165355 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
CHEMBL426317 165355 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
89638708 113549 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 343 6 0 7 0.5 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3)CC2)c1=O 10.1016/j.bmcl.2014.07.048
CHEMBL3330603 113549 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 343 6 0 7 0.5 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3)CC2)c1=O 10.1016/j.bmcl.2014.07.048
132256714 179528 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 438 8 1 4 4.1 COc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4751777 179528 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 438 8 1 4 4.1 COc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
132256724 179889 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 459 7 1 4 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4756041 179889 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 459 7 1 4 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1 10.1021/acs.jmedchem.0c00814
11382841 18067 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 360 9 2 3 4.1 COc1ccc(F)cc1OCCNCCCc1c[nH]c2ccc(F)cc12 10.1021/jm0304010
CHEMBL127171 18067 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 360 9 2 3 4.1 COc1ccc(F)cc1OCCNCCCc1c[nH]c2ccc(F)cc12 10.1021/jm0304010
145961968 160702 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 531 6 2 4 6.1 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(Br)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
CHEMBL4128200 160702 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 531 6 2 4 6.1 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(Br)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
145960843 160595 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4126644 160595 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
5 135 60 None -35 27 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
5202 135 60 None -35 27 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
CHEMBL39 135 60 None -35 27 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
DB08839 135 60 None -35 27 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
CHEMBL4741908 178718 0 None 3 3 Human 9.3 pEC50 = 9.3 Functional
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
ChEMBL 421 6 0 5 4.2 O=C1COc2ccccc2N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2020.112572
145961773 160738 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 464 6 2 5 4.8 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4128689 160738 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 464 6 2 5 4.8 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
145962474 160835 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 467 6 2 4 5.6 Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4130230 160835 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 467 6 2 4 5.6 Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
73346042 91176 1 None - 1 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 91176 1 None - 1 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
132247308 180898 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 451 8 2 4 3.2 NC(=O)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4777581 180898 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 451 8 2 4 3.2 NC(=O)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
5 135 60 None -35 27 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.01.052
5202 135 60 None -35 27 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.01.052
CHEMBL39 135 60 None -35 27 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.01.052
DB08839 135 60 None -35 27 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.01.052
145974939 163887 0 None 11 3 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 442 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sc(F)cc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4217182 163887 0 None 11 3 Human 9.2 pEC50 = 9.2 Functional
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
ChEMBL 442 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sc(F)cc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
145963079 160767 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 471 6 2 4 5.5 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(F)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
CHEMBL4129170 160767 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 471 6 2 4 5.5 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(F)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
10694660 177544 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 445 6 2 4 4.0 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cc[nH]n3)n2)CC1 10.1021/jm9806906
CHEMBL46539 177544 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 445 6 2 4 4.0 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cc[nH]n3)n2)CC1 10.1021/jm9806906
145962581 160668 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 487 6 2 4 6.0 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(Cl)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
CHEMBL4127774 160668 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 487 6 2 4 6.0 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(Cl)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
10474042 169428 0 None -1 4 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 365 6 0 4 4.1 COc1cccc2c1CCCC2CCCN1CCN(c2ccccn2)CC1 10.1016/j.bmc.2015.05.042
CHEMBL444590 169428 0 None -1 4 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 365 6 0 4 4.1 COc1cccc2c1CCCC2CCCN1CCN(c2ccccn2)CC1 10.1016/j.bmc.2015.05.042
44336170 106557 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 413 5 1 5 2.9 CC1CN(c2cccc3c2OCCO3)CC(C)N1CCNC(=O)c1ccc(F)cc1 10.1021/jm960496o
CHEMBL316960 106557 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 413 5 1 5 2.9 CC1CN(c2cccc3c2OCCO3)CC(C)N1CCNC(=O)c1ccc(F)cc1 10.1021/jm960496o
10430183 199197 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/jm960496o
CHEMBL81728 199197 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/jm960496o
CHEMBL4751542 179510 0 None 3 3 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 470 6 1 6 3.8 Nc1ccc2c(c1)N(CCCCN1CCN(c3cccc4sccc34)CC1)S(=O)(=O)CC2 10.1016/j.ejmech.2020.112572
CHEMBL511857 186440 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 351 4 0 4 3.9 COc1cccc([C@H]2CC[C@H](N3CCN(c4ccccn4)CC3)CC2)c1 10.1016/j.bmc.2015.05.042
118713100 113560 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 362 6 0 8 0.1 Cn1c(=O)cnn(CCCCN2CCN(c3ncccc3F)CC2)c1=O 10.1016/j.bmcl.2014.07.048
CHEMBL3330614 113560 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 362 6 0 8 0.1 Cn1c(=O)cnn(CCCCN2CCN(c3ncccc3F)CC2)c1=O 10.1016/j.bmcl.2014.07.048
10430183 199197 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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)
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL81728 199197 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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)
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
145993172 166184 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 423 6 0 5 3.8 O=C1C2CC=CCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4287980 166184 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 423 6 0 5 3.8 O=C1C2CC=CCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
145971556 163688 0 None 29 3 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 436 8 1 5 3.7 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4214528 163688 0 None 29 3 Human 9.1 pEC50 = 9.1 Functional
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
ChEMBL 436 8 1 5 3.7 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccn1 10.1016/j.bmcl.2018.01.038
10082834 34081 1 None 19498 2 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 236 4 1 2 2.4 COc1ccc2[nH]cc(CCN(C)C)c2c1F 10.1021/jm000339w
CHEMBL142862 34081 1 None 19498 2 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 236 4 1 2 2.4 COc1ccc2[nH]cc(CCN(C)C)c2c1F 10.1021/jm000339w
10430183 199197 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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)
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL81728 199197 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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)
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
5 135 60 None -35 27 Human 9.0 pEC50 = 9 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
5202 135 60 None -35 27 Human 9.0 pEC50 = 9 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
CHEMBL39 135 60 None -35 27 Human 9.0 pEC50 = 9 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
DB08839 135 60 None -35 27 Human 9.0 pEC50 = 9 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
138692457 181570 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 438 8 1 4 4.1 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4786067 181570 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 438 8 1 4 4.1 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
145991127 166118 0 None 34 3 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 437 6 0 5 4.2 O=C1c2cccc(F)c2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4286905 166118 0 None 34 3 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 437 6 0 5 4.2 O=C1c2cccc(F)c2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4759331 180172 0 None 16 3 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 471 6 1 6 3.9 O=S1(=O)CCc2ccc(O)cc2N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2020.112572
10813901 177560 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 461 6 2 4 4.5 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cc[nH]n3)n2)CC1 10.1021/jm9806906
CHEMBL46582 177560 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 461 6 2 4 4.5 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cc[nH]n3)n2)CC1 10.1021/jm9806906
145993577 166574 0 None 9 3 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 453 6 0 5 4.9 O=C1CC2(CCCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4295055 166574 0 None 9 3 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 453 6 0 5 4.9 O=C1CC2(CCCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4635414 176372 0 None 22 3 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 443 6 0 7 3.6 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(F)cc(F)cn12 10.1016/j.bmcl.2020.127027
145952639 160607 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 453 6 2 4 5.3 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccccc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
CHEMBL4126818 160607 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 453 6 2 4 5.3 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccccc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
21689040 41542 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 261 6 1 2 3.8 CCCCN(CCC)C1CCc2cccc(O)c2C1 10.1016/j.ejmech.2018.01.002
CHEMBL149482 41542 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 261 6 1 2 3.8 CCCCN(CCC)C1CCc2cccc(O)c2C1 10.1016/j.ejmech.2018.01.002
145966333 163249 0 None 19 6 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4209188 163249 0 None 19 6 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
145993117 166109 0 None 8 6 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 427 7 0 5 4.4 CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
CHEMBL4286717 166109 0 None 8 6 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 427 7 0 5 4.4 CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
11046644 30312 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 361 6 0 4 4.0 COc1cccc2c(CCCN3CCN(c4ccccn4)CC3)cccc12 10.1016/j.bmc.2015.05.042
CHEMBL139505 30312 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 361 6 0 4 4.0 COc1cccc2c(CCCN3CCN(c4ccccn4)CC3)cccc12 10.1016/j.bmc.2015.05.042
10047814 104162 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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)
ChEMBL 421 6 0 6 2.7 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
CHEMBL311015 104162 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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)
ChEMBL 421 6 0 6 2.7 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
CHEMBL4638430 176572 0 None 1 3 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 432 6 0 8 3.2 N#Cc1cccn2c(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)nc12 10.1016/j.bmcl.2020.127027
9798593 112113 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 352 8 3 3 3.8 Fc1ccc2[nH]cc(CCCNCCOc3cccc4[nH]cnc34)c2c1 10.1021/jm0304010
CHEMBL330827 112113 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 352 8 3 3 3.8 Fc1ccc2[nH]cc(CCCNCCOc3cccc4[nH]cnc34)c2c1 10.1021/jm0304010
9822317 68638 2 None - 1 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 400 7 1 5 2.6 O=C1c2ccccc2S(=O)(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926761 68638 2 None - 1 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 400 7 1 5 2.6 O=C1c2ccccc2S(=O)(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL4649106 177330 0 None 7 3 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 443 6 0 7 3.6 O=c1n(CCCCN2CCN(c3cccc4sc(F)cc34)CC2)nc2c(F)cccn12 10.1016/j.bmcl.2020.127027
145963146 160526 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5c(N)c6c(nc45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4125762 160526 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5c(N)c6c(nc45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
10949698 198857 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 413 8 1 8 1.9 COc1ccccc1N1CCN(CCCNc2c(C(C)=O)c(C)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL79161 198857 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 413 8 1 8 1.9 COc1ccccc1N1CCN(CCCNc2c(C(C)=O)c(C)nn(C)c2=O)CC1 10.1021/jm0009336
145988038 166365 0 None 4 3 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 413 6 0 5 4.0 CC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
CHEMBL4291215 166365 0 None 4 3 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 413 6 0 5 4.0 CC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
11232913 112602 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 334 8 3 3 3.6 c1ccc2c(CCCNCCOc3cccc4[nH]cnc34)c[nH]c2c1 10.1021/jm0304010
CHEMBL331609 112602 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 334 8 3 3 3.6 c1ccc2c(CCCNCCOc3cccc4[nH]cnc34)c[nH]c2c1 10.1021/jm0304010
145990126 165940 0 None 2 3 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 425 6 0 5 4.0 O=C1C2CCCCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4283546 165940 0 None 2 3 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 425 6 0 5 4.0 O=C1C2CCCCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4638599 176588 0 None 7 5 Human 8.8 pEC50 = 8.8 Functional
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
ChEMBL 407 6 0 7 3.3 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2ccccn12 10.1016/j.bmcl.2020.127027
CHEMBL4644352 177026 0 None 9 6 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 425 6 0 7 3.5 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(F)cccn12 10.1016/j.bmcl.2020.127027
145973003 163724 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
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
ChEMBL 450 8 0 7 3.9 COc1ccccc1N1CCN(CCCOc2ccc3c(C)cc(=O)oc3c2C(C)=O)CC1 10.1016/j.bmc.2017.12.016
CHEMBL4215022 163724 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
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
ChEMBL 450 8 0 7 3.9 COc1ccccc1N1CCN(CCCOc2ccc3c(C)cc(=O)oc3c2C(C)=O)CC1 10.1016/j.bmc.2017.12.016
11307899 78236 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 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 10.1021/jm0341204
CHEMBL2112882 78236 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 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 10.1021/jm0341204
10411236 100682 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 444 6 1 5 4.7 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3cnco3)n2)CC1 10.1021/jm9806906
CHEMBL297138 100682 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 444 6 1 5 4.7 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3cnco3)n2)CC1 10.1021/jm9806906
23625537 85825 0 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 446 6 1 5 4.3 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2nccc(-c3ccco3)n2)CC1 10.1021/jm070714l
CHEMBL231471 85825 0 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 446 6 1 5 4.3 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2nccc(-c3ccco3)n2)CC1 10.1021/jm070714l
15980895 193561 0 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 439 6 2 3 4.0 CCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2c(F)cc3c(c2C1)C(=O)NCC3 10.1016/j.bmcl.2009.10.134
CHEMBL595055 193561 0 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 439 6 2 3 4.0 CCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2c(F)cc3c(c2C1)C(=O)NCC3 10.1016/j.bmcl.2009.10.134
10248159 82519 2 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 363 7 1 3 5.1 CC1(C)Cc2cccc(OCCNCc3cccc(C4=CCCC4)c3)c2O1 10.1021/jm061180b
CHEMBL218261 82519 2 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 363 7 1 3 5.1 CC1(C)Cc2cccc(OCCNCc3cccc(C4=CCCC4)c3)c2O1 10.1021/jm061180b
5 135 60 None -35 27 Human 8.0 pEC50 = 8 Functional
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.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00101a032
5202 135 60 None -35 27 Human 8.0 pEC50 = 8 Functional
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.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00101a032
CHEMBL39 135 60 None -35 27 Human 8.0 pEC50 = 8 Functional
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.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00101a032
DB08839 135 60 None -35 27 Human 8.0 pEC50 = 8 Functional
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.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00101a032
10549236 165575 0 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 404 6 1 4 3.5 CN(C)c1cccc(CNCC2(F)CCN(C(=O)c3cccc(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL42766 165575 0 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 404 6 1 4 3.5 CN(C)c1cccc(CNCC2(F)CCN(C(=O)c3cccc(Cl)c3)CC2)n1 10.1021/jm9806906
5 135 60 None -19 27 Rat 8.0 pEC50 = 8 Functional
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00042a003
5202 135 60 None -19 27 Rat 8.0 pEC50 = 8 Functional
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00042a003
CHEMBL39 135 60 None -19 27 Rat 8.0 pEC50 = 8 Functional
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00042a003
DB08839 135 60 None -19 27 Rat 8.0 pEC50 = 8 Functional
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00042a003
42606339 17579 0 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1259241 17579 0 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
137657949 158737 0 None 2 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 420 4 1 7 3.3 Cc1nc2c(O)cccn2c(=O)c1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.bmc.2017.07.040
CHEMBL4102561 158737 0 None 2 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 420 4 1 7 3.3 Cc1nc2c(O)cccn2c(=O)c1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.bmc.2017.07.040
129186563 160228 0 None -1 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 406 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCC=C2 10.1016/j.bmc.2017.07.040
CHEMBL4074326 160228 0 None -1 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 406 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCC=C2 10.1016/j.bmc.2017.07.040
CHEMBL4116465 160228 0 None -1 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 406 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCC=C2 10.1016/j.bmc.2017.07.040
137653567 158037 0 None -3 6 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 404 4 0 6 3.6 Cc1nc2ccccn2c(=O)c1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.bmc.2017.07.040
CHEMBL4094825 158037 0 None -3 6 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 404 4 0 6 3.6 Cc1nc2ccccn2c(=O)c1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.bmc.2017.07.040
145982353 165773 0 None -1 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 457 6 2 7 1.9 O=C1C2CC(O)C(O)CC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4280084 165773 0 None -1 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 457 6 2 7 1.9 O=C1C2CC(O)C(O)CC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
145987942 166250 0 None -4 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 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 10.1016/j.ejmech.2017.12.099
CHEMBL4289238 166250 0 None -4 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 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 10.1016/j.ejmech.2017.12.099
10789756 173155 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 450 6 1 4 4.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(N3CCC3)n2)CC1 10.1021/jm9806906
CHEMBL45423 173155 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 450 6 1 4 4.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(N3CCC3)n2)CC1 10.1021/jm9806906
1220 182 39 None -1 9 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
31 182 39 None -1 9 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
7 182 39 None -1 9 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
CHEMBL56 182 39 None -1 9 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
CHEMBL4777098 180867 0 None 3 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 462 6 0 5 3.9 CN1CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)c2ccccc2C1=O 10.1016/j.ejmech.2020.112572
132257061 179173 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4747425 179173 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c00814
49782389 17517 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 380 5 2 3 3.6 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc4[nH]ccc4c3)CC2)nc1 10.1021/jm100835q
CHEMBL1259055 17517 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 380 5 2 3 3.6 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc4[nH]ccc4c3)CC2)nc1 10.1021/jm100835q
15980854 193252 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 465 7 2 3 4.4 O=C1NCCc2cc(F)c3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL592939 193252 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 465 7 2 3 4.4 O=C1NCCc2cc(F)c3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
127051039 139493 0 None 1 3 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 449 9 1 4 4.7 CCNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805772 139493 0 None 1 3 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 449 9 1 4 4.7 CCNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
132257265 181248 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 437 8 2 4 4.1 CNc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4781985 181248 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 437 8 2 4 4.1 CNc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
138692456 181841 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 407 7 2 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCNc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4789505 181841 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 407 7 2 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCNc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
11288 3227 0 None -56 2 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 454 8 3 4 3.7 CCc1cccc(c1Cl)N1CCN(CC1)C[C@@H](CCNC(=O)c1cc2c([nH]1)cccc2)O 10.1021/acs.jmedchem.9b00607
130431314 3227 0 None -56 2 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 454 8 3 4 3.7 CCc1cccc(c1Cl)N1CCN(CC1)C[C@@H](CCNC(=O)c1cc2c([nH]1)cccc2)O 10.1021/acs.jmedchem.9b00607
CHEMBL4519938 3227 0 None -56 2 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 454 8 3 4 3.7 CCc1cccc(c1Cl)N1CCN(CC1)C[C@@H](CCNC(=O)c1cc2c([nH]1)cccc2)O 10.1021/acs.jmedchem.9b00607
145987659 166438 0 None -3 3 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 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 10.1016/j.ejmech.2017.12.099
CHEMBL4292655 166438 0 None -3 3 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 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 10.1016/j.ejmech.2017.12.099
155547346 172757 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 449 6 1 4 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4c5c(nc6ccccc46)CCC5)CC3)c2c1 10.1016/j.bmc.2019.01.025
CHEMBL4533184 172757 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 449 6 1 4 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4c5c(nc6ccccc46)CCC5)CC3)c2c1 10.1016/j.bmc.2019.01.025
6540428 183621 0 None 37 2 Human 6.0 pEC50 = 6.0 Functional
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 ]
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 nan
CHEMBL3989558 183621 0 None 37 2 Human 6.0 pEC50 = 6.0 Functional
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 ]
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 nan
CHEMBL485253 183621 0 None 37 2 Human 6.0 pEC50 = 6.0 Functional
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 ]
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 nan
53248159 61454 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 500 8 1 4 5.3 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm200288r
CHEMBL1774384 61454 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 500 8 1 4 5.3 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm200288r
49781933 17570 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 399 5 1 3 4.0 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC(C5)C3)C4)CC2)nc1 10.1021/jm100835q
CHEMBL1259209 17570 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 399 5 1 3 4.0 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC(C5)C3)C4)CC2)nc1 10.1021/jm100835q
118626142 165008 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4248491 165008 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
145976732 162697 0 None 7 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4sccc34)CC2)n1 10.1016/j.bmcl.2018.01.038
CHEMBL4202443 162697 0 None 7 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4sccc34)CC2)n1 10.1016/j.bmcl.2018.01.038
145989183 166419 0 None 7 3 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 473 7 0 5 4.4 Cc1ccc(C23CC2C(=O)N(CCCCN2CCN(c4cccc5sccc45)CC2)C3=O)cc1 10.1016/j.ejmech.2017.12.099
CHEMBL4292254 166419 0 None 7 3 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 473 7 0 5 4.4 Cc1ccc(C23CC2C(=O)N(CCCCN2CCN(c4cccc5sccc45)CC2)C3=O)cc1 10.1016/j.ejmech.2017.12.099
56850665 70942 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 334 7 1 5 2.4 O=C1CSC(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926749 70942 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 334 7 1 5 2.4 O=C1CSC(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962697 70942 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 334 7 1 5 2.4 O=C1CSC(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
10385855 14136 0 None -181 3 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1 10.1016/0960-894X(95)00091-7
CHEMBL120055 14136 0 None -181 3 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1 10.1016/0960-894X(95)00091-7
CHEMBL321818 14136 0 None -181 3 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1 10.1016/0960-894X(95)00091-7
137630811 160299 0 None -1 3 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 504 6 1 7 4.5 Cc1ccc(Sc2ccccc2N2CCN(CCc3c(C)nc4n(c3=O)CCCC4O)CC2)c(C)c1 10.1016/j.bmc.2017.07.040
CHEMBL4082150 160299 0 None -1 3 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 504 6 1 7 4.5 Cc1ccc(Sc2ccccc2N2CCN(CCc3c(C)nc4n(c3=O)CCCC4O)CC2)c(C)c1 10.1016/j.bmc.2017.07.040
CHEMBL4117087 160299 0 None -1 3 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 504 6 1 7 4.5 Cc1ccc(Sc2ccccc2N2CCN(CCc3c(C)nc4n(c3=O)CCCC4O)CC2)c(C)c1 10.1016/j.bmc.2017.07.040
16109488 83619 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 363 7 1 3 5.1 CC1(C)COc2c(OCCNCc3cccc(C4=CCCC4)c3)cccc21 10.1021/jm061180b
CHEMBL221183 83619 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 363 7 1 3 5.1 CC1(C)COc2c(OCCNCc3cccc(C4=CCCC4)c3)cccc21 10.1021/jm061180b
132257069 180195 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 425 7 1 4 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCSc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4759629 180195 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 425 7 1 4 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCSc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
9928161 75342 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 345 3 2 3 4.1 C1=C(c2c[nH]c3ccccc23)CCN(CC2CNc3ccccc3O2)C1 10.1016/j.bmcl.2005.11.054
CHEMBL205031 75342 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 345 3 2 3 4.1 C1=C(c2c[nH]c3ccccc23)CCN(CC2CNc3ccccc3O2)C1 10.1016/j.bmcl.2005.11.054
45483512 191821 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 287 3 1 2 4.6 Clc1cccc(Oc2ccccc2C2CCNCC2)c1 10.1016/j.bmcl.2009.10.014
CHEMBL575290 191821 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 287 3 1 2 4.6 Clc1cccc(Oc2ccccc2C2CCNCC2)c1 10.1016/j.bmcl.2009.10.014
9799764 87688 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4ccc5ncccc5c4C3)c2c1 10.1016/j.bmcl.2007.03.049
CHEMBL234853 87688 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4ccc5ncccc5c4C3)c2c1 10.1016/j.bmcl.2007.03.049
145965041 163445 0 None 3 3 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3ccc4ccsc4c3)CC2)n1 10.1016/j.bmcl.2018.01.038
CHEMBL4211473 163445 0 None 3 3 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3ccc4ccsc4c3)CC2)n1 10.1016/j.bmcl.2018.01.038
130431317 172119 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4517102 172119 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
155510732 168694 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 430 6 1 1 6.9 Fc1ccc(C2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2ccccc2)c1 10.1016/j.bmcl.2019.126703
CHEMBL4434876 168694 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 430 6 1 1 6.9 Fc1ccc(C2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2ccccc2)c1 10.1016/j.bmcl.2019.126703
11667626 101887 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 359 10 1 4 2.4 CCc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
CHEMBL2431042 101887 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 359 10 1 4 2.4 CCc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
CHEMBL3040827 101887 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 359 10 1 4 2.4 CCc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
127049163 139443 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 447 8 1 6 3.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4c3OC(F)(F)O4)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805165 139443 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 447 8 1 6 3.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4c3OC(F)(F)O4)CC2)c1 10.1016/j.bmcl.2016.04.087
42606222 17508 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 347 5 1 4 3.2 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccsc3)CC2)nc1 10.1021/jm100835q
CHEMBL1259033 17508 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 347 5 1 4 3.2 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccsc3)CC2)nc1 10.1021/jm100835q
1220 182 39 None -1 9 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmc.2015.05.042
31 182 39 None -1 9 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmc.2015.05.042
7 182 39 None -1 9 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmc.2015.05.042
CHEMBL56 182 39 None -1 9 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmc.2015.05.042
10719425 99505 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 477 6 1 4 5.9 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cccs3)n2)CC1 10.1021/jm9806906
CHEMBL288244 99505 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 477 6 1 4 5.9 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cccs3)n2)CC1 10.1021/jm9806906
CHEMBL4636321 176441 0 None 7 3 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 441 6 0 7 4.0 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(Cl)cccn12 10.1016/j.bmcl.2020.127027
10718220 168486 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 445 6 1 5 3.8 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
CHEMBL44159 168486 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 445 6 1 5 3.8 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
11795765 172769 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 408 6 2 4 3.7 CNc1cccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL45334 172769 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 408 6 2 4 3.7 CNc1cccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm9806906
44461162 199121 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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)
ChEMBL 413 7 1 5 2.9 O=C(NCCCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL81095 199121 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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)
ChEMBL 413 7 1 5 2.9 O=C(NCCCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
145972513 163696 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 443 8 1 7 3.2 CNC(=O)c1cccc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)n1 10.1016/j.bmcl.2018.01.038
CHEMBL4214642 163696 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 443 8 1 7 3.2 CNC(=O)c1cccc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)n1 10.1016/j.bmcl.2018.01.038
127048533 139469 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 465 9 1 5 4.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1016/j.bmcl.2016.04.087
CHEMBL3805515 139469 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 465 9 1 5 4.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1016/j.bmcl.2016.04.087
152215 96325 39 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 ]
ChEMBL 212 1 1 1 2.9 CN1CC=C(c2c[nH]c3ccccc23)CC1 nan
CHEMBL26655 96325 39 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 ]
ChEMBL 212 1 1 1 2.9 CN1CC=C(c2c[nH]c3ccccc23)CC1 nan
44578448 182050 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
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
ChEMBL 433 6 1 9 1.8 CCC1=CC2C(=O)N(N)C(SCCCN3CCN(c4ncccn4)CC3)=NC2S1 10.1021/jm800176x
CHEMBL479243 182050 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
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
ChEMBL 433 6 1 9 1.8 CCC1=CC2C(=O)N(N)C(SCCCN3CCN(c4ncccn4)CC3)=NC2S1 10.1021/jm800176x
127049861 139458 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 435 8 1 4 4.3 CNC(=O)c1ccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmcl.2016.04.087
CHEMBL3805376 139458 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 435 8 1 4 4.3 CNC(=O)c1ccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmcl.2016.04.087
127049516 139521 0 None 6 3 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 449 8 1 4 4.6 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2016.04.087
CHEMBL3806091 139521 0 None 6 3 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 449 8 1 4 4.6 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2016.04.087
56850658 70957 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 371 7 1 4 1.6 O=C1C2CCCN2C(=O)CN1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926745 70957 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 371 7 1 4 1.6 O=C1C2CCCN2C(=O)CN1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962804 70957 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 371 7 1 4 1.6 O=C1C2CCCN2C(=O)CN1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
145969406 164019 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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
ChEMBL 498 7 0 6 4.7 CC(=O)c1c(OCCCN2CCN(c3ccccc3Br)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.bmc.2017.12.016
CHEMBL4218720 164019 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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
ChEMBL 498 7 0 6 4.7 CC(=O)c1c(OCCCN2CCN(c3ccccc3Br)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.bmc.2017.12.016
3658 3874 41 None 2 4 Human 6.9 pEC50 = 6.9 Functional
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 ]
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C nan
517 3874 41 None 2 4 Human 6.9 pEC50 = 6.9 Functional
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 ]
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C nan
5709 3874 41 None 2 4 Human 6.9 pEC50 = 6.9 Functional
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 ]
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C nan
CHEMBL312448 3874 41 None 2 4 Human 6.9 pEC50 = 6.9 Functional
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 ]
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C nan
DB06694 3874 41 None 2 4 Human 6.9 pEC50 = 6.9 Functional
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 ]
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C nan
127049863 139470 0 None 1 6 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 443 8 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
CHEMBL3805518 139470 0 None 1 6 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 443 8 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
127049862 139475 0 None -1 6 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 425 8 1 5 4.4 CNC(=O)c1cccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805559 139475 0 None -1 6 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 425 8 1 5 4.4 CNC(=O)c1cccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2016.04.087
11381753 78137 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 324 9 2 3 3.8 COc1ccccc1OCCNCCCc1c[nH]c2ccccc12 10.1021/jm0304010
CHEMBL2112645 78137 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 324 9 2 3 3.8 COc1ccccc1OCCNCCCc1c[nH]c2ccccc12 10.1021/jm0304010
49780599 17551 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 341 5 1 3 3.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccccc3)CC2)nc1 10.1021/jm100835q
CHEMBL1259151 17551 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 341 5 1 3 3.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccccc3)CC2)nc1 10.1021/jm100835q
10812183 99588 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 422 7 2 4 4.0 CCNc1cccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL288992 99588 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 422 7 2 4 4.0 CCNc1cccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm9806906
145984151 165635 0 None 16 3 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 437 6 0 5 4.2 O=C1c2ccc(F)cc2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4277751 165635 0 None 16 3 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 437 6 0 5 4.2 O=C1c2ccc(F)cc2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
132256724 179889 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 459 7 1 4 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4756041 179889 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 459 7 1 4 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1 10.1021/acs.jmedchem.0c00814
23155650 18304 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 446 6 1 7 2.8 Cc1cc(N2CCN(CCCCc3nc4c(c(=O)n3N)CCCC4)CC2)nc2ccccc12 10.1021/jm1002292
CHEMBL1277007 18304 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 446 6 1 7 2.8 Cc1cc(N2CCN(CCCCc3nc4c(c(=O)n3N)CCCC4)CC2)nc2ccccc12 10.1021/jm1002292
145991746 166039 0 None 6 3 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 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 10.1016/j.ejmech.2017.12.099
CHEMBL4285479 166039 0 None 6 3 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 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 10.1016/j.ejmech.2017.12.099
42606340 17537 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 403 5 1 5 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4sccc4s3)CC2)nc1 10.1021/jm100835q
CHEMBL1259108 17537 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 403 5 1 5 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4sccc4s3)CC2)nc1 10.1021/jm100835q
137635294 155297 0 None -245 3 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 445 4 0 7 3.4 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2(F)F 10.1016/j.bmc.2017.07.040
CHEMBL4062992 155297 0 None -245 3 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 445 4 0 7 3.4 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2(F)F 10.1016/j.bmc.2017.07.040
2543 3495 56 None -19 12 Rat 5.9 pEC50 = 5.9 Functional
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00042a003
5358 3495 56 None -19 12 Rat 5.9 pEC50 = 5.9 Functional
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00042a003
54 3495 56 None -19 12 Rat 5.9 pEC50 = 5.9 Functional
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00042a003
CHEMBL128 3495 56 None -19 12 Rat 5.9 pEC50 = 5.9 Functional
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00042a003
DB00669 3495 56 None -19 12 Rat 5.9 pEC50 = 5.9 Functional
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00042a003
132256814 179662 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 454 8 1 4 4.6 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1021/acs.jmedchem.0c00814
CHEMBL4753394 179662 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 454 8 1 4 4.6 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1021/acs.jmedchem.0c00814
53248208 61455 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 425 8 1 5 3.7 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm200288r
CHEMBL1774385 61455 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 425 8 1 5 3.7 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm200288r
16109510 168481 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 337 7 1 4 4.2 C1=C(c2cccc(CNCCOc3cccc4c3OCO4)c2)CCC1 10.1021/jm061180b
CHEMBL441546 168481 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 337 7 1 4 4.2 C1=C(c2cccc(CNCCOc3cccc4c3OCO4)c2)CCC1 10.1021/jm061180b
9932697 140191 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 435 6 1 4 5.1 CCCN1CC(CN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)Oc2c(OC)cccc21 10.1016/j.bmcl.2005.11.054
CHEMBL382333 140191 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 435 6 1 4 5.1 CCCN1CC(CN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)Oc2c(OC)cccc21 10.1016/j.bmcl.2005.11.054
3246443 37274 2 None -13 3 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL1457510 37274 2 None -13 3 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
127049849 139464 0 None -3 3 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 477 9 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(C(C)=O)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805434 139464 0 None -3 3 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 477 9 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(C(C)=O)c1 10.1016/j.bmcl.2016.04.087
45375938 191638 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 289 3 1 2 4.2 Fc1cccc(Oc2cccc(F)c2C2CCNCC2)c1 10.1016/j.bmcl.2009.10.014
CHEMBL574004 191638 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 289 3 1 2 4.2 Fc1cccc(Oc2cccc(F)c2C2CCNCC2)c1 10.1016/j.bmcl.2009.10.014
44591228 178454 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 361 6 2 4 4.0 c1ccc2c(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2008.12.087
CHEMBL473282 178454 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 361 6 2 4 4.0 c1ccc2c(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2008.12.087
132247311 180279 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 451 8 1 4 4.2 CN(C)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4760666 180279 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 451 8 1 4 4.2 CN(C)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
2998814 54534 2 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 ]
ChEMBL 245 1 1 2 1.8 C[N+]1=C2CCCCCN2C(O)(c2ccccc2)C1 nan
CHEMBL1301276 54534 2 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 ]
ChEMBL 245 1 1 2 1.8 C[N+]1=C2CCCCCN2C(O)(c2ccccc2)C1 nan
CHEMBL1616268 54534 2 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 ]
ChEMBL 245 1 1 2 1.8 C[N+]1=C2CCCCCN2C(O)(c2ccccc2)C1 nan
9909555 139906 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 411 8 2 3 5.2 c1ccc(CN2CC(CNCCCc3c[nH]c4ccccc34)Oc3ccccc32)cc1 10.1016/j.bmcl.2005.11.054
CHEMBL381542 139906 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 411 8 2 3 5.2 c1ccc(CN2CC(CNCCCc3c[nH]c4ccccc34)Oc3ccccc32)cc1 10.1016/j.bmcl.2005.11.054
15057516 155107 0 None -269 3 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 425 4 1 8 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
CHEMBL4060678 155107 0 None -269 3 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 425 4 1 8 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
10550893 165629 0 None -3 3 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 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 10.1016/j.ejmech.2017.12.099
CHEMBL4277532 165629 0 None -3 3 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 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 10.1016/j.ejmech.2017.12.099
132247301 179911 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 447 7 2 3 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4756233 179911 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 447 7 2 3 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1 10.1021/acs.jmedchem.0c00814
132256713 181607 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 407 7 1 3 4.0 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCCc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4786537 181607 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 407 7 1 3 4.0 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCCc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
132256749 180272 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 422 7 1 3 4.4 Cc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4760621 180272 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 422 7 1 3 4.4 Cc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
21797090 106053 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 503 11 1 7 5.2 S=c1[nH]ncn1[C@@H]1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9806906
CHEMBL3144354 106053 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 503 11 1 7 5.2 S=c1[nH]ncn1[C@@H]1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9806906
10647621 162837 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 459 6 1 5 4.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1-n1cccn1 10.1021/jm9806906
CHEMBL42042 162837 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 459 6 1 5 4.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1-n1cccn1 10.1021/jm9806906
145963710 160811 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5nc6c(c(N)c5c4)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4129917 160811 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5nc6c(c(N)c5c4)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
44591230 179456 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 389 7 2 4 4.6 CC(Nc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1)C1CC1 10.1016/j.bmcl.2008.12.087
CHEMBL475105 179456 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 389 7 2 4 4.6 CC(Nc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1)C1CC1 10.1016/j.bmcl.2008.12.087
16109481 82512 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 361 9 1 3 5.3 CC(C)Oc1ccccc1OCCNCc1cccc(-c2ccccc2)c1 10.1021/jm061180b
CHEMBL218217 82512 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 361 9 1 3 5.3 CC(C)Oc1ccccc1OCCNCc1cccc(-c2ccccc2)c1 10.1021/jm061180b
53248212 61498 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 424 8 2 4 3.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm200288r
CHEMBL1774534 61498 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 424 8 2 4 3.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm200288r
145962678 160824 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 492 6 2 5 5.6 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4130059 160824 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 492 6 2 5 5.6 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
135453290 132834 14 None -724 8 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL371300 132834 14 None -724 8 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
5 135 60 None -35 27 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm9015763
5202 135 60 None -35 27 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm9015763
CHEMBL39 135 60 None -35 27 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm9015763
DB08839 135 60 None -35 27 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm9015763
44591229 186860 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 375 7 2 4 4.2 c1ccc2c(CCN3CCCC(c4ccnc(NCC5CC5)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2008.12.087
CHEMBL515438 186860 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 375 7 2 4 4.2 c1ccc2c(CCN3CCCC(c4ccnc(NCC5CC5)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2008.12.087
132256749 180272 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 422 7 1 3 4.4 Cc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4760621 180272 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 422 7 1 3 4.4 Cc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
130431337 173253 0 None -15 2 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 438 8 2 3 4.7 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4544583 173253 0 None -15 2 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 438 8 2 3 4.7 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
1220 182 39 None -1 9 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.ejmech.2012.11.042
31 182 39 None -1 9 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.ejmech.2012.11.042
7 182 39 None -1 9 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.ejmech.2012.11.042
CHEMBL56 182 39 None -1 9 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.ejmech.2012.11.042
42606459 17509 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 331 5 1 4 2.7 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccco3)CC2)nc1 10.1021/jm100835q
CHEMBL1259034 17509 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 331 5 1 4 2.7 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccco3)CC2)nc1 10.1021/jm100835q
132257265 181248 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 437 8 2 4 4.1 CNc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4781985 181248 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 437 8 2 4 4.1 CNc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
9885700 162549 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 370 8 2 4 3.7 Fc1ccc2[nH]cc(CCCNCCOc3cccc4c3OCCO4)c2c1 10.1021/jm0304010
CHEMBL419240 162549 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 370 8 2 4 3.7 Fc1ccc2[nH]cc(CCCNCCOc3cccc4c3OCCO4)c2c1 10.1021/jm0304010
138692460 178542 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4739908 178542 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1 10.1021/acs.jmedchem.0c00814
5 135 60 None -35 27 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2009.06.019
5202 135 60 None -35 27 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2009.06.019
CHEMBL39 135 60 None -35 27 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2009.06.019
DB08839 135 60 None -35 27 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2009.06.019
11291892 132741 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 378 3 0 4 1.8 O=C1[C@@H]2CCCN2C(=O)CN1CN1CCN(c2cccc3ccccc23)CC1 10.1021/jm048999e
CHEMBL370758 132741 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 378 3 0 4 1.8 O=C1[C@@H]2CCCN2C(=O)CN1CN1CCN(c2cccc3ccccc23)CC1 10.1021/jm048999e
71574204 85615 0 None -18 2 Human 4.8 pEC50 = 4.8 Functional
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
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc2ccccc12 10.1016/j.ejmech.2012.11.042
CHEMBL2312640 85615 0 None -18 2 Human 4.8 pEC50 = 4.8 Functional
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
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc2ccccc12 10.1016/j.ejmech.2012.11.042
132257139 180251 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2F)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4760271 180251 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2F)CC1 10.1021/acs.jmedchem.0c00814
23625383 85628 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 414 5 1 4 3.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ncc(Cl)cn2)CC1 10.1021/jm070714l
CHEMBL231273 85628 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 414 5 1 4 3.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ncc(Cl)cn2)CC1 10.1021/jm070714l
16109508 83745 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 379 9 1 3 6.0 CC(C)Oc1ccccc1OCCNCc1cccc(C2=CCCCCC2)c1 10.1021/jm061180b
CHEMBL221957 83745 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 379 9 1 3 6.0 CC(C)Oc1ccccc1OCCNCc1cccc(C2=CCCCCC2)c1 10.1021/jm061180b
44408946 158757 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 325 5 3 3 3.3 Fc1ccc2[nH]cc(CCNCC3CNc4ccccc4O3)c2c1 10.1016/j.bmcl.2005.11.054
CHEMBL410273 158757 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 325 5 3 3 3.3 Fc1ccc2[nH]cc(CCNCC3CNc4ccccc4O3)c2c1 10.1016/j.bmcl.2005.11.054
71574306 85614 0 None -2 2 Human 4.8 pEC50 = 4.8 Functional
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
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 10.1016/j.ejmech.2012.11.042
CHEMBL2312639 85614 0 None -2 2 Human 4.8 pEC50 = 4.8 Functional
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
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 10.1016/j.ejmech.2012.11.042
145960879 160641 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4ccc5nc6c(c(N)c5c4)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4127445 160641 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4ccc5nc6c(c(N)c5c4)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
56850796 70969 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 371 8 1 4 2.6 O=C1C2CCCN2C(=O)N1CCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926686 70969 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 371 8 1 4 2.6 O=C1C2CCCN2C(=O)N1CCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962913 70969 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 371 8 1 4 2.6 O=C1C2CCCN2C(=O)N1CCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
42606573 17494 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1258999 17494 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
56850390 70921 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 357 7 1 4 2.2 O=C1C2CCCN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926733 70921 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 357 7 1 4 2.2 O=C1C2CCCN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962486 70921 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 357 7 1 4 2.2 O=C1C2CCCN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
145968927 163957 0 None 2 3 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 411 8 1 7 2.8 NC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4217986 163957 0 None 2 3 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 411 8 1 7 2.8 NC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
137629633 160323 0 None 2 3 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 432 4 0 7 2.6 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3OC(F)(F)O4)CC1)CCCC2 10.1016/j.bmc.2017.07.040
CHEMBL4077006 160323 0 None 2 3 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 432 4 0 7 2.6 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3OC(F)(F)O4)CC1)CCCC2 10.1016/j.bmc.2017.07.040
CHEMBL4117235 160323 0 None 2 3 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 432 4 0 7 2.6 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3OC(F)(F)O4)CC1)CCCC2 10.1016/j.bmc.2017.07.040
132247311 180279 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 451 8 1 4 4.2 CN(C)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4760666 180279 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 451 8 1 4 4.2 CN(C)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
10528303 100694 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 468 6 1 6 4.1 N#CC1(CNCc2cccc(-n3cccn3)n2)CCN(C(=O)c2ccc(Cl)c(Cl)c2)CC1 10.1021/jm9806906
CHEMBL297208 100694 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 468 6 1 6 4.1 N#CC1(CNCc2cccc(-n3cccn3)n2)CCN(C(=O)c2ccc(Cl)c(Cl)c2)CC1 10.1021/jm9806906
25130235 184922 0 None -13 3 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 184922 0 None -13 3 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
71574212 85632 0 None 4 2 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312935 85632 0 None 4 2 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2c1 10.1016/j.ejmech.2012.11.042
44408888 137926 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 339 5 2 3 3.3 CN1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
CHEMBL377941 137926 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 339 5 2 3 3.3 CN1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
44591246 178528 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 379 6 2 4 4.1 Fc1ccc2[nH]cc(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c2c1 10.1016/j.bmcl.2008.12.087
CHEMBL473903 178528 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 379 6 2 4 4.1 Fc1ccc2[nH]cc(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c2c1 10.1016/j.bmcl.2008.12.087
122183764 121475 0 None 1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 454 7 2 5 3.7 O=C(NCCC(O)CN1CCN(c2cccc3ccccc23)CC1)c1cnc2ccccc2c1 10.1021/acs.jmedchem.5b00776
CHEMBL3597636 121475 0 None 1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 454 7 2 5 3.7 O=C(NCCC(O)CN1CCN(c2cccc3ccccc23)CC1)c1cnc2ccccc2c1 10.1021/acs.jmedchem.5b00776
42605994 17522 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
CHEMBL1259071 17522 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
132256735 179654 4 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 409 7 1 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4753328 179654 4 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 409 7 1 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
145978965 165746 0 None -1 3 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 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 10.1016/j.ejmech.2017.12.099
CHEMBL4279645 165746 0 None -1 3 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 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 10.1016/j.ejmech.2017.12.099
145967359 163371 0 None 2 3 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 440 9 1 6 4.2 CCNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4210637 163371 0 None 2 3 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 440 9 1 6 4.2 CCNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
10381677 105858 0 None -24 2 Rat 6.8 pEC50 = 6.8 Functional
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 325 6 2 5 3.3 CN(C)CCc1c[nH]c2ccc(Nc3ncccc3[N+](=O)[O-])cc12 10.1021/jm00042a003
CHEMBL314213 105858 0 None -24 2 Rat 6.8 pEC50 = 6.8 Functional
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 325 6 2 5 3.3 CN(C)CCc1c[nH]c2ccc(Nc3ncccc3[N+](=O)[O-])cc12 10.1021/jm00042a003
11188024 144792 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4c(ccc5ncccc45)C3)c2c1 10.1016/j.bmcl.2007.03.049
CHEMBL391531 144792 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4c(ccc5ncccc45)C3)c2c1 10.1016/j.bmcl.2007.03.049
CHEMBL4777207 180875 0 None 2 3 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 445 8 0 3 5.1 O=C(c1ccccc1)N(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)CC1CC1 10.1016/j.ejmech.2020.112214
145974143 163726 0 None -3 3 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 443 8 1 7 3.2 CNC(=O)c1ccnc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2018.01.038
CHEMBL4215048 163726 0 None -3 3 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 443 8 1 7 3.2 CNC(=O)c1ccnc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2018.01.038
5 135 60 None -35 27 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2019.126703
5202 135 60 None -35 27 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2019.126703
CHEMBL39 135 60 None -35 27 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2019.126703
DB08839 135 60 None -35 27 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2019.126703
25265257 17507 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 347 5 1 4 3.2 Cc1ccc(CNCC2(F)CCN(C(=O)c3cccs3)CC2)nc1 10.1021/jm100835q
CHEMBL1259032 17507 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 347 5 1 4 3.2 Cc1ccc(CNCC2(F)CCN(C(=O)c3cccs3)CC2)nc1 10.1021/jm100835q
52948486 17568 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 417 5 2 4 3.5 Cc1ccc(CNCC2(O)CC3CCC(C2)N3C(=O)c2ccc(F)c(Cl)c2)nc1 10.1021/jm100835q
CHEMBL1259200 17568 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 417 5 2 4 3.5 Cc1ccc(CNCC2(O)CC3CCC(C2)N3C(=O)c2ccc(F)c(Cl)c2)nc1 10.1021/jm100835q
132257139 180251 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2F)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4760271 180251 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2F)CC1 10.1021/acs.jmedchem.0c00814
57397588 70916 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 375 7 1 5 2.4 O=C1C2CCSN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926747 70916 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 375 7 1 5 2.4 O=C1C2CCSN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962460 70916 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 375 7 1 5 2.4 O=C1C2CCSN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
46180256 193826 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 289 2 0 2 3.5 C#CCOc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm9015763
CHEMBL596885 193826 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 289 2 0 2 3.5 C#CCOc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm9015763
24769156 115489 0 None -6 3 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 388 7 1 4 3.6 O=C(NCCCCN1CCN(c2ccccc2)CC1)c1ccc2ncccc2c1 10.1021/jm501119j
CHEMBL3358509 115489 0 None -6 3 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 388 7 1 4 3.6 O=C(NCCCCN1CCN(c2ccccc2)CC1)c1ccc2ncccc2c1 10.1021/jm501119j
44408784 165285 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 355 6 3 4 3.3 COc1ccc2c(c1)OC(CNCCc1c[nH]c3ccc(F)cc13)CN2 10.1016/j.bmcl.2005.11.054
CHEMBL425936 165285 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 355 6 3 4 3.3 COc1ccc2c(c1)OC(CNCCc1c[nH]c3ccc(F)cc13)CN2 10.1016/j.bmcl.2005.11.054
9799764 87688 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4ccc5ncccc5c4C3)c2c1 10.1016/j.bmcl.2007.03.049
CHEMBL234853 87688 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4ccc5ncccc5c4C3)c2c1 10.1016/j.bmcl.2007.03.049
187811 54586 11 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 ]
ChEMBL 216 5 2 1 3.0 CCCCc1ccc2[nH]cc(CCN)c2c1 nan
CHEMBL1309229 54586 11 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 ]
ChEMBL 216 5 2 1 3.0 CCCCc1ccc2[nH]cc(CCN)c2c1 nan
CHEMBL1616674 54586 11 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 ]
ChEMBL 216 5 2 1 3.0 CCCCc1ccc2[nH]cc(CCN)c2c1 nan
23155625 18330 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 450 6 1 8 2.7 Nn1c(SCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2c(c1=O)CCCC2 10.1021/jm1002292
CHEMBL1277281 18330 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 450 6 1 8 2.7 Nn1c(SCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2c(c1=O)CCCC2 10.1021/jm1002292
138692456 181841 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 407 7 2 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCNc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4789505 181841 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 407 7 2 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCNc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
11646498 101807 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 375 11 1 5 2.3 CCOc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
CHEMBL2431051 101807 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 375 11 1 5 2.3 CCOc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
CHEMBL3040382 101807 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 375 11 1 5 2.3 CCOc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
46225309 193736 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 454 8 2 4 4.3 N#Cc1ccc2[nH]cc(CCCCN(CC3CC3)C3COc4ccc5c(c4C3)C(=O)NC5)c2c1 10.1016/j.bmcl.2009.10.134
CHEMBL596297 193736 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 454 8 2 4 4.3 N#Cc1ccc2[nH]cc(CCCCN(CC3CC3)C3COc4ccc5c(c4C3)C(=O)NC5)c2c1 10.1016/j.bmcl.2009.10.134
5 135 60 None -35 27 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
5202 135 60 None -35 27 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
CHEMBL39 135 60 None -35 27 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
DB08839 135 60 None -35 27 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
75 3312 2 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1021/jm0341204
9870500 3312 2 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1021/jm0341204
CHEMBL191971 3312 2 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1021/jm0341204
132256730 182450 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4797282 182450 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
56850926 70926 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 362 9 1 5 3.2 O=C1CSC(=O)N1CCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926759 70926 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 362 9 1 5 3.2 O=C1CSC(=O)N1CCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962491 70926 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 362 9 1 5 3.2 O=C1CSC(=O)N1CCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
161665 171754 25 None 28 3 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL448891 171754 25 None 28 3 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
46176231 63424 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 467 8 0 5 6.8 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)CCCCC2CCSS2)c1-3 10.1021/jm200347t
CHEMBL1806874 63424 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 467 8 0 5 6.8 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)CCCCC2CCSS2)c1-3 10.1021/jm200347t
9844300 74108 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 407 4 1 4 4.3 COc1cccc2c1OC(CN1CC=C(c3c[nH]c4ccc(F)cc34)CC1)CN2C 10.1016/j.bmcl.2005.11.054
CHEMBL203018 74108 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 407 4 1 4 4.3 COc1cccc2c1OC(CN1CC=C(c3c[nH]c4ccc(F)cc34)CC1)CN2C 10.1016/j.bmcl.2005.11.054
44408681 140534 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 367 6 2 3 4.1 CC(C)N1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
CHEMBL383446 140534 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 367 6 2 3 4.1 CC(C)N1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
16109485 160933 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 353 9 1 3 5.3 CC(C)Oc1ccccc1OCCNCc1cccc(C2CCCC2)c1 10.1021/jm061180b
CHEMBL413777 160933 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 353 9 1 3 5.3 CC(C)Oc1ccccc1OCCNCc1cccc(C2CCCC2)c1 10.1021/jm061180b
44408702 140121 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 349 7 2 3 4.0 CCCN1CC(CNCCc2c[nH]c3ccccc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
CHEMBL382179 140121 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 349 7 2 3 4.0 CCCN1CC(CNCCc2c[nH]c3ccccc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
45102635 56626 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
ChEMBL 311 4 1 3 3.8 Fc1cccc(Cl)c1Oc1cccc(F)c1OC1CNC1 10.1016/j.bmcl.2010.11.066
CHEMBL1645600 56626 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
ChEMBL 311 4 1 3 3.8 Fc1cccc(Cl)c1Oc1cccc(F)c1OC1CNC1 10.1016/j.bmcl.2010.11.066
145 136 46 None -4 11 Human 6.7 pEC50 = 6.7 Functional
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 ]
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
1832 136 46 None -4 11 Human 6.7 pEC50 = 6.7 Functional
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 ]
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
CHEMBL7257 136 46 None -4 11 Human 6.7 pEC50 = 6.7 Functional
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 ]
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
DB14010 136 46 None -4 11 Human 6.7 pEC50 = 6.7 Functional
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 ]
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
CHEMBL4634009 176309 0 None 6 3 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 437 7 0 8 3.3 COc1cccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n12 10.1016/j.bmcl.2020.127027
11428089 17675 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 351 8 3 2 4.4 Fc1ccc2[nH]cc(CCCNCCOc3cccc4[nH]ccc34)c2c1 10.1021/jm0304010
CHEMBL126424 17675 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 351 8 3 2 4.4 Fc1ccc2[nH]cc(CCCNCCOc3cccc4[nH]ccc34)c2c1 10.1021/jm0304010
9802369 173151 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 422 6 2 4 4.0 CNc1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ccc1C 10.1021/jm9806906
CHEMBL45422 173151 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 422 6 2 4 4.0 CNc1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ccc1C 10.1021/jm9806906
CHEMBL4644500 177034 0 None 38 3 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 437 7 0 8 3.3 COc1cccn2c(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)nc12 10.1016/j.bmcl.2020.127027
145963961 163593 0 None 5 6 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 425 8 1 7 3.0 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4213342 163593 0 None 5 6 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 425 8 1 7 3.0 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
145981408 165687 0 None 2 3 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 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 10.1016/j.ejmech.2017.12.099
CHEMBL4278581 165687 0 None 2 3 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 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 10.1016/j.ejmech.2017.12.099
49837354 18363 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 549 6 1 10 2.9 CC(=O)N1CCc2c(sc3nc(SCCCN4CCN(c5ccc6ccccc6n5)CC4)n(N)c(=O)c23)C1 10.1021/jm1002292
CHEMBL1277558 18363 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 549 6 1 10 2.9 CC(=O)N1CCc2c(sc3nc(SCCCN4CCN(c5ccc6ccccc6n5)CC4)n(N)c(=O)c23)C1 10.1021/jm1002292
10005161 198819 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 475 9 1 8 3.3 CCC(=O)c1c(-c2ccccc2)nn(C)c(=O)c1NCCN1CCN(c2ccccc2OC)CC1 10.1021/jm0009336
CHEMBL78874 198819 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 475 9 1 8 3.3 CCC(=O)c1c(-c2ccccc2)nn(C)c(=O)c1NCCN1CCN(c2ccccc2OC)CC1 10.1021/jm0009336
1220 182 39 None -1 9 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
31 182 39 None -1 9 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
7 182 39 None -1 9 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
CHEMBL56 182 39 None -1 9 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
16109489 83736 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 362 7 1 4 4.3 C1=C(c2cncc(CNCCOc3cccc4c3OC3(CC3)C4)c2)CCC1 10.1021/jm061180b
CHEMBL221920 83736 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 362 7 1 4 4.3 C1=C(c2cncc(CNCCOc3cccc4c3OC3(CC3)C4)c2)CCC1 10.1021/jm061180b
10718870 167108 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 461 6 1 4 5.4 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3ccco3)n2)CC1 10.1021/jm9806906
CHEMBL43146 167108 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 461 6 1 4 5.4 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3ccco3)n2)CC1 10.1021/jm9806906
CHEMBL4749223 179324 0 None 7 3 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 448 7 0 7 4.2 COc1ccc2ncc(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)c2c1 10.1016/j.ejmech.2020.112572
127049865 139436 0 None 4 3 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 442 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
CHEMBL3805099 139436 0 None 4 3 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 442 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
10647622 165201 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 459 6 2 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1-c1cc[nH]n1 10.1021/jm9806906
CHEMBL42545 165201 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 459 6 2 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1-c1cc[nH]n1 10.1021/jm9806906
CHEMBL4635890 176407 0 None 41 3 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 408 6 0 8 2.7 O=c1n(CCCCN2CCN(c3cccc4scnc34)CC2)nc2ccccn12 10.1016/j.bmcl.2020.127027
10474089 199250 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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)
ChEMBL 366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1 10.1016/s0960-894x(98)00406-5
CHEMBL542671 199250 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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)
ChEMBL 366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1 10.1016/s0960-894x(98)00406-5
CHEMBL82215 199250 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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)
ChEMBL 366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1 10.1016/s0960-894x(98)00406-5
10067360 140744 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 364 7 1 4 4.5 CC1(C)Cc2cccc(OCCNCc3cncc(C4=CCCC4)c3)c2O1 10.1021/jm061180b
CHEMBL384657 140744 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 364 7 1 4 4.5 CC1(C)Cc2cccc(OCCNCc3cncc(C4=CCCC4)c3)c2O1 10.1021/jm061180b
10474089 199250 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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)
ChEMBL 366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1 10.1016/s0960-894x(98)00406-5
CHEMBL542671 199250 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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)
ChEMBL 366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1 10.1016/s0960-894x(98)00406-5
CHEMBL82215 199250 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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)
ChEMBL 366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1 10.1016/s0960-894x(98)00406-5
9928432 17672 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 352 8 2 3 4.7 Fc1ccc2[nH]cc(CCCNCCOc3cccc4ccoc34)c2c1 10.1021/jm0304010
CHEMBL126407 17672 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 352 8 2 3 4.7 Fc1ccc2[nH]cc(CCCNCCOc3cccc4ccoc34)c2c1 10.1021/jm0304010
10248163 31173 0 None -288 3 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 363 5 0 4 4.0 COc1cccc2c1CCC/C2=C\CCN1CCN(c2ccccn2)CC1 10.1016/j.bmc.2015.05.042
CHEMBL140406 31173 0 None -288 3 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 363 5 0 4 4.0 COc1cccc2c1CCC/C2=C\CCN1CCN(c2ccccn2)CC1 10.1016/j.bmc.2015.05.042
10789182 178019 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 438 6 1 4 4.2 CN(C)c1cccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL46971 178019 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 438 6 1 4 4.2 CN(C)c1cccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
11430856 77445 17 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 450 10 2 5 3.0 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)CC3CCCCC3)CC2)c1 10.1021/jm0508641
CHEMBL209821 77445 17 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 450 10 2 5 3.0 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)CC3CCCCC3)CC2)c1 10.1021/jm0508641
10343434 77611 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 444 9 2 5 2.8 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm0508641
CHEMBL210537 77611 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 444 9 2 5 2.8 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm0508641
42605993 17528 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3sccc3Br)CC2)nc1 10.1021/jm100835q
CHEMBL1259087 17528 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3sccc3Br)CC2)nc1 10.1021/jm100835q
42606104 17536 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 361 5 1 4 3.5 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(C)cs3)CC2)nc1 10.1021/jm100835q
CHEMBL1259107 17536 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 361 5 1 4 3.5 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(C)cs3)CC2)nc1 10.1021/jm100835q
CHEMBL4644742 177050 0 None 2 3 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 432 6 0 8 3.2 N#Cc1cccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n12 10.1016/j.bmcl.2020.127027
132256796 181935 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 454 8 1 4 4.6 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4790662 181935 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 454 8 1 4 4.6 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
10550097 166656 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 420 6 1 4 4.1 CN(C)c1cccc(CNCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL42994 166656 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 420 6 1 4 4.1 CN(C)c1cccc(CNCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
10948133 164468 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 351 5 0 4 3.4 COc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)CC2 10.1016/j.bmc.2015.05.042
CHEMBL423181 164468 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 351 5 0 4 3.4 COc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)CC2 10.1016/j.bmc.2015.05.042
132257264 179664 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 410 7 1 5 2.9 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cnccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4753414 179664 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 410 7 1 5 2.9 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cnccn2)CC1 10.1021/acs.jmedchem.9b00062
10835365 178067 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 409 5 1 3 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)nc1 10.1021/jm9806906
CHEMBL47013 178067 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 409 5 1 3 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)nc1 10.1021/jm9806906
44537925 192346 0 None 7 3 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 624 12 2 9 5.2 COc1ccccc1N1CCN(CCCn2cc(CCCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL582945 192346 0 None 7 3 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 624 12 2 9 5.2 COc1ccccc1N1CCN(CCCn2cc(CCCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
4806 3777 80 None -1 3 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 3777 80 None -1 3 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 3777 80 None -1 3 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 3777 80 None -1 3 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 3777 80 None -1 3 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
23625239 85352 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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
ChEMBL 409 6 2 4 3.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(CO)cn2)CC1 10.1021/jm070714l
CHEMBL230425 85352 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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
ChEMBL 409 6 2 4 3.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(CO)cn2)CC1 10.1021/jm070714l
130431319 171691 0 None -11 2 Human 5.7 pEC50 = 5.7 Functional
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
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(C[C@@H](O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.9b00607
CHEMBL4483569 171691 0 None -11 2 Human 5.7 pEC50 = 5.7 Functional
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
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(C[C@@H](O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.9b00607
398712 77293 5 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 417 9 1 5 2.9 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm0508641
CHEMBL209324 77293 5 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 417 9 1 5 2.9 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm0508641
91242334 166560 2 None 6 3 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 419 6 0 5 4.1 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4294797 166560 2 None 6 3 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 419 6 0 5 4.1 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
11395034 70936 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 385 9 1 4 3.0 O=C1C2CCCN2C(=O)N1CCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926751 70936 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 385 9 1 4 3.0 O=C1C2CCCN2C(=O)N1CCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962585 70936 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 385 9 1 4 3.0 O=C1C2CCCN2C(=O)N1CCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
1220 182 39 None -1 9 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.0c00814
31 182 39 None -1 9 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.0c00814
7 182 39 None -1 9 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.0c00814
CHEMBL56 182 39 None -1 9 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.0c00814
132247312 179797 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 465 8 2 4 4.1 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4755058 179797 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 465 8 2 4 4.1 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
10787547 171768 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 406 6 2 4 4.1 CNc1cccc(CNCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL44904 171768 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 406 6 2 4 4.1 CNc1cccc(CNCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
53248213 61499 0 None -2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
CHEMBL1774535 61499 0 None -2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
44591261 179971 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 379 6 2 4 4.1 Fc1cccc2c(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c[nH]c12 10.1016/j.bmcl.2008.12.087
CHEMBL475694 179971 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 379 6 2 4 4.1 Fc1cccc2c(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c[nH]c12 10.1016/j.bmcl.2008.12.087