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Compile Data Set for Download or QSAR

Found 1428 hits of ec50 for UniProtKB: P08908   
Target/Host
(Institution)		LigandTarget/Host
Links		Ligand
Links		Trg + Lig
Links		Ki
nM		ΔG°
kcal/mole		IC50
nM		Kd
nM		EC50/IC50
nM		koff
s-1		kon
M-1s-1		pHTemp
°C
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433523
PNG
(US10562853, Compound 44)
Show SMILES Fc1ccc(cc1Cl)C(=O)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1
Show InChI InChI=1S/C23H24ClF2N3O2/c24-18-14-16(4-5-19(18)25)22(30)29-11-7-23(26,8-12-29)15-27-10-13-31-21-3-1-2-20-17(21)6-9-28-20/h1-6,9,14,27-28H,7-8,10-13,15H2
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n/an/an/an/a 0.0000210n/an/an/an/a


TBA

Assay Description
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-ar...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433476
PNG
(US10562853, Compound 2)
Show SMILES CC(=O)Nc1cccc(OCCNCC2(F)CCN(CC2)C(=O)c2ccc(F)c(Cl)c2)c1
Show InChI InChI=1S/C23H26ClF2N3O3/c1-16(30)28-18-3-2-4-19(14-18)32-12-9-27-15-23(26)7-10-29(11-8-23)22(31)17-5-6-21(25)20(24)13-17/h2-6,13-14,27H,7-12,15H2,1H3,(H,28,30)
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n/an/an/an/a 0.000209n/an/an/an/a


TBA

Assay Description
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-ar...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433499
PNG
(US10562853, Compound 16)
Show SMILES Fc1ccc(cc1Cl)C(=O)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1
Show InChI InChI=1S/C24H24ClF2N3O2/c25-19-15-18(6-7-20(19)26)23(31)30-12-8-24(27,9-13-30)16-28-11-14-32-21-5-1-3-17-4-2-10-29-22(17)21/h1-7,10,15,28H,8-9,11-14,16H2
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n/an/an/an/a 0.00148n/an/an/an/a


TBA

Assay Description
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-ar...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50546857
PNG
(CHEMBL4757755)
Show SMILES Fc1ccc(cc1Cl)C(=O)N1CCC(F)(CNCCOc2cccc3NCCc23)CC1
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n/an/an/an/a 0.00363n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alp...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50546857
PNG
(CHEMBL4757755)
Show SMILES Fc1ccc(cc1Cl)C(=O)N1CCC(F)(CNCCOc2cccc3NCCc23)CC1
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n/an/an/an/a 0.00513n/an/an/an/a


TBA

Assay Description
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-ar...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50180054
PNG
(CHEMBL199824 | [O-methyl-11C]2-{4-[4-(7-methoxynap...)
Show SMILES COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1
Show InChI InChI=1S/C23H29N5O3/c1-25-22(29)17-24-28(23(25)30)11-4-3-10-26-12-14-27(15-13-26)21-7-5-6-18-8-9-19(31-2)16-20(18)21/h5-9,16-17H,3-4,10-15H2,1-2H3
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n/an/an/an/a 0.0100n/an/an/an/a



Columbia University College of Physicians and Surgeons

Curated by ChEMBL


Assay Description
Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation

J Med Chem 49: 125-34 (2006)


Article DOI: 10.1021/jm050725j
BindingDB Entry DOI: 10.7270/Q2R49QBD
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433537
PNG
(US10562853, Compound 60)
Show SMILES CC1(C)Cc2cccc(OCCNCC3(F)CCN(CC3)C(=O)c3ccc(F)c(Cl)c3)c2O1
Show InChI InChI=1S/C25H29ClF2N2O3/c1-24(2)15-18-4-3-5-21(22(18)33-24)32-13-10-29-16-25(28)8-11-30(12-9-25)23(31)17-6-7-20(27)19(26)14-17/h3-7,14,29H,8-13,15-16H2,1-2H3
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n/an/an/an/a 0.0102n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alp...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50546857
PNG
(CHEMBL4757755)
Show SMILES Fc1ccc(cc1Cl)C(=O)N1CCC(F)(CNCCOc2cccc3NCCc23)CC1
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n/an/an/an/a 0.0132n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433476
PNG
(US10562853, Compound 2)
Show SMILES CC(=O)Nc1cccc(OCCNCC2(F)CCN(CC2)C(=O)c2ccc(F)c(Cl)c2)c1
Show InChI InChI=1S/C23H26ClF2N3O3/c1-16(30)28-18-3-2-4-19(14-18)32-12-9-27-15-23(26)7-10-29(11-8-23)22(31)17-5-6-21(25)20(24)13-17/h2-6,13-14,27H,7-12,15H2,1H3,(H,28,30)
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n/an/an/an/a 0.0138n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433477
PNG
(US10562853, Compound 3)
Show SMILES CC(=O)Nc1cccc(OCCNCC2(F)CCN(CC2)C(=O)c2ccc(Cl)c(Cl)c2)c1
Show InChI InChI=1S/C23H26Cl2FN3O3/c1-16(30)28-18-3-2-4-19(14-18)32-12-9-27-15-23(26)7-10-29(11-8-23)22(31)17-5-6-20(24)21(25)13-17/h2-6,13-14,27H,7-12,15H2,1H3,(H,28,30)
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n/an/an/an/a 0.0251n/an/an/an/a


TBA

Assay Description
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-ar...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433523
PNG
(US10562853, Compound 44)
Show SMILES Fc1ccc(cc1Cl)C(=O)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1
Show InChI InChI=1S/C23H24ClF2N3O2/c24-18-14-16(4-5-19(18)25)22(30)29-11-7-23(26,8-12-29)15-27-10-13-31-21-3-1-2-20-17(21)6-9-28-20/h1-6,9,14,27-28H,7-8,10-13,15H2
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n/an/an/an/a 0.0295n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alp...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50417427
PNG
(CHEMBL1290716)
Show SMILES Cc1ccc2c(cccc2n1)N1CCN(CCc2cccc3n(C)c(=O)ccc23)CC1
Show InChI InChI=1S/C26H28N4O/c1-19-9-10-22-23(27-19)6-4-8-25(22)30-17-15-29(16-18-30)14-13-20-5-3-7-24-21(20)11-12-26(31)28(24)2/h3-12H,13-18H2,1-2H3
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n/an/an/an/a 0.0316n/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay

Bioorg Med Chem Lett 20: 7092-6 (2010)


Article DOI: 10.1016/j.bmcl.2010.09.085
BindingDB Entry DOI: 10.7270/Q2MC919V
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50180054
PNG
(CHEMBL199824 | [O-methyl-11C]2-{4-[4-(7-methoxynap...)
Show SMILES COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1
Show InChI InChI=1S/C23H29N5O3/c1-25-22(29)17-24-28(23(25)30)11-4-3-10-26-12-14-27(15-13-26)21-7-5-6-18-8-9-19(31-2)16-20(18)21/h5-9,16-17H,3-4,10-15H2,1-2H3
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n/an/an/an/a 0.0500n/an/an/an/a



Columbia University College of Physicians and Surgeons

Curated by ChEMBL


Assay Description
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding

J Med Chem 49: 125-34 (2006)


Article DOI: 10.1021/jm050725j
BindingDB Entry DOI: 10.7270/Q2R49QBD
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433477
PNG
(US10562853, Compound 3)
Show SMILES CC(=O)Nc1cccc(OCCNCC2(F)CCN(CC2)C(=O)c2ccc(Cl)c(Cl)c2)c1
Show InChI InChI=1S/C23H26Cl2FN3O3/c1-16(30)28-18-3-2-4-19(14-18)32-12-9-27-15-23(26)7-10-29(11-8-23)22(31)17-5-6-20(24)21(25)13-17/h2-6,13-14,27H,7-12,15H2,1H3,(H,28,30)
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n/an/an/an/a 0.0661n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433531
PNG
(US10562853, Compound 52)
Show SMILES CNc1cccc(OCCNCC2(F)CCN(CC2)C(=O)c2ccc(F)c(Cl)c2)c1
Show InChI InChI=1S/C22H26ClF2N3O2/c1-26-17-3-2-4-18(14-17)30-12-9-27-15-22(25)7-10-28(11-8-22)21(29)16-5-6-20(24)19(23)13-16/h2-6,13-14,26-27H,7-12,15H2,1H3
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n/an/an/an/a 0.0741n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alp...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50024580
PNG
(CHEMBL3330612)
Show SMILES Cn1c(=O)cnn(CCCCN2CCN(CC2)c2ccccn2)c1=O
Show InChI InChI=1S/C17H24N6O2/c1-20-16(24)14-19-23(17(20)25)9-5-4-8-21-10-12-22(13-11-21)15-6-2-3-7-18-15/h2-3,6-7,14H,4-5,8-13H2,1H3
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n/an/an/an/a 0.0800n/an/an/an/a



Stony Brook University

Curated by ChEMBL


Assay Description
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry

Bioorg Med Chem Lett 24: 4759-62 (2014)


Article DOI: 10.1016/j.bmcl.2014.07.048
BindingDB Entry DOI: 10.7270/Q2NZ896M
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433523
PNG
(US10562853, Compound 44)
Show SMILES Fc1ccc(cc1Cl)C(=O)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1
Show InChI InChI=1S/C23H24ClF2N3O2/c24-18-14-16(4-5-19(18)25)22(30)29-11-7-23(26,8-12-29)15-27-10-13-31-21-3-1-2-20-17(21)6-9-28-20/h1-6,9,14,27-28H,7-8,10-13,15H2
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n/an/an/an/a 0.0871n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433531
PNG
(US10562853, Compound 52)
Show SMILES CNc1cccc(OCCNCC2(F)CCN(CC2)C(=O)c2ccc(F)c(Cl)c2)c1
Show InChI InChI=1S/C22H26ClF2N3O2/c1-26-17-3-2-4-18(14-17)30-12-9-27-15-22(25)7-10-28(11-8-22)21(29)16-5-6-20(24)19(23)13-16/h2-6,13-14,26-27H,7-12,15H2,1H3
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n/an/an/an/a 0.0891n/an/an/an/a


TBA

Assay Description
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-ar...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50542266
PNG
(CHEMBL4633397)
Show SMILES Fc1cccn2c1nn(CCCCN1CCN(CC1)c1cccc3scnc13)c2=O
Show InChI InChI=1S/C21H23FN6OS/c22-16-5-4-9-27-20(16)24-28(21(27)29)10-2-1-8-25-11-13-26(14-12-25)17-6-3-7-18-19(17)23-15-30-18/h3-7,9,15H,1-2,8,10-14H2
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n/an/an/an/a 0.100n/an/an/an/a



University of Chinese Academy of Sciences

Curated by ChEMBL


Assay Description
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay

Bioorg Med Chem Lett 30: (2020)


Article DOI: 10.1016/j.bmcl.2020.127027
BindingDB Entry DOI: 10.7270/Q2VD731V
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50542256
PNG
(CHEMBL4648027)
Show SMILES Clc1cc(Cl)c2nn(CCCCN3CCN(CC3)c3cccc4sccc34)c(=O)n2c1
Show InChI InChI=1S/C22H23Cl2N5OS/c23-16-14-18(24)21-25-29(22(30)28(21)15-16)8-2-1-7-26-9-11-27(12-10-26)19-4-3-5-20-17(19)6-13-31-20/h3-6,13-15H,1-2,7-12H2
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n/an/an/an/a 0.100n/an/an/an/a



University of Chinese Academy of Sciences

Curated by ChEMBL


Assay Description
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay

Bioorg Med Chem Lett 30: (2020)


Article DOI: 10.1016/j.bmcl.2020.127027
BindingDB Entry DOI: 10.7270/Q2VD731V
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50542251
PNG
(CHEMBL4647011)
Show SMILES Fc1ccc2nn(CCCCN3CCN(CC3)c3cccc4sccc34)c(=O)n2c1
Show InChI InChI=1S/C22H24FN5OS/c23-17-6-7-21-24-28(22(29)27(21)16-17)10-2-1-9-25-11-13-26(14-12-25)19-4-3-5-20-18(19)8-15-30-20/h3-8,15-16H,1-2,9-14H2
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n/an/an/an/a 0.100n/an/an/an/a



University of Chinese Academy of Sciences

Curated by ChEMBL


Assay Description
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay

Bioorg Med Chem Lett 30: (2020)


Article DOI: 10.1016/j.bmcl.2020.127027
BindingDB Entry DOI: 10.7270/Q2VD731V
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM86757
PNG
(CAS_0 | NSC_11603174 | [11C]MMP)
Show SMILES COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1
Show InChI InChI=1S/C19H27N5O3/c1-21-18(25)15-20-24(19(21)26)10-6-5-9-22-11-13-23(14-12-22)16-7-3-4-8-17(16)27-2/h3-4,7-8,15H,5-6,9-14H2,1-2H3
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n/an/an/an/a 0.100n/an/an/an/a



Stony Brook University

Curated by ChEMBL


Assay Description
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry

Bioorg Med Chem Lett 24: 4759-62 (2014)


Article DOI: 10.1016/j.bmcl.2014.07.048
BindingDB Entry DOI: 10.7270/Q2NZ896M
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433531
PNG
(US10562853, Compound 52)
Show SMILES CNc1cccc(OCCNCC2(F)CCN(CC2)C(=O)c2ccc(F)c(Cl)c2)c1
Show InChI InChI=1S/C22H26ClF2N3O2/c1-26-17-3-2-4-18(14-17)30-12-9-27-15-22(25)7-10-28(11-8-22)21(29)16-5-6-20(24)19(23)13-16/h2-6,13-14,26-27H,7-12,15H2,1H3
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n/an/an/an/a 0.112n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50151982
PNG
(5-{4-[4-(5-Cyano-1H-indol-3-yl)-butyl]-piperazin-1...)
Show SMILES NC(=O)c1cc2cc(ccc2o1)N1CCN(CCCCc2c[nH]c3ccc(cc23)C#N)CC1
Show InChI InChI=1S/C26H27N5O2/c27-16-18-4-6-23-22(13-18)19(17-29-23)3-1-2-8-30-9-11-31(12-10-30)21-5-7-24-20(14-21)15-25(33-24)26(28)32/h4-7,13-15,17,29H,1-3,8-12H2,(H2,28,32)
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n/an/an/an/a 0.120n/an/an/an/a



East China University of Science and Technology

Curated by ChEMBL


Assay Description
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay

Bioorg Med Chem 26: 3117-3125 (2018)


Article DOI: 10.1016/j.bmc.2018.04.037
BindingDB Entry DOI: 10.7270/Q28P631Z
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50151982
PNG
(5-{4-[4-(5-Cyano-1H-indol-3-yl)-butyl]-piperazin-1...)
Show SMILES NC(=O)c1cc2cc(ccc2o1)N1CCN(CCCCc2c[nH]c3ccc(cc23)C#N)CC1
Show InChI InChI=1S/C26H27N5O2/c27-16-18-4-6-23-22(13-18)19(17-29-23)3-1-2-8-30-9-11-31(12-10-30)21-5-7-24-20(14-21)15-25(33-24)26(28)32/h4-7,13-15,17,29H,1-3,8-12H2,(H2,28,32)
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n/an/an/an/a 0.120n/an/an/an/a



CSIR-Central Drug Research Institute

Curated by ChEMBL


Assay Description
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay

Bioorg Med Chem 27: 895-930 (2019)


Article DOI: 10.1016/j.bmc.2019.01.025
BindingDB Entry DOI: 10.7270/Q2N87F3N
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50094670
PNG
(1-(4-Dipropylamino-1,3,4,5-tetrahydro-benzo[cd]ind...)
Show SMILES CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(C1)c23
Show InChI InChI=1S/C19H26N2O/c1-4-8-21(9-5-2)15-10-14-12-20-18-7-6-16(13(3)22)17(11-15)19(14)18/h6-7,12,15,20H,4-5,8-11H2,1-3H3
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n/an/an/an/a 0.130n/an/an/an/a



Purdue University

Curated by ChEMBL


Assay Description
EC50 for inhibition of 50 microM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor

J Med Chem 43: 4701-10 (2001)


BindingDB Entry DOI: 10.7270/Q2HT2NM7
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433480
PNG
(US10562853, Compound 6)
Show SMILES COc1ccccc1OCCNCC1(F)CCN(CC1)C(=O)c1ccc(F)c(Cl)c1
Show InChI InChI=1S/C22H25ClF2N2O3/c1-29-19-4-2-3-5-20(19)30-13-10-26-15-22(25)8-11-27(12-9-22)21(28)16-6-7-18(24)17(23)14-16/h2-7,14,26H,8-13,15H2,1H3
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n/an/an/an/a 0.138n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50272610
PNG
(CHEMBL4129019)
Show SMILES COC(=O)c1ccc2[nH]cc(CCCCN3CCN(CC3)c3cccc4nc5CCCCc5c(N)c34)c2c1
Show InChI InChI=1S/C31H37N5O2/c1-38-31(37)21-12-13-25-24(19-21)22(20-33-25)7-4-5-14-35-15-17-36(18-16-35)28-11-6-10-27-29(28)30(32)23-8-2-3-9-26(23)34-27/h6,10-13,19-20,33H,2-5,7-9,14-18H2,1H3,(H2,32,34)
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n/an/an/an/a<0.140n/an/an/an/a



East China University of Science and Technology

Curated by ChEMBL


Assay Description
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay

Bioorg Med Chem 26: 3117-3125 (2018)


Article DOI: 10.1016/j.bmc.2018.04.037
BindingDB Entry DOI: 10.7270/Q28P631Z
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50272735
PNG
(CHEMBL4126958)
Show SMILES COc1ccc2[nH]cc(CCCCN3CCN(CC3)c3cccc4nc5CCCCc5c(N)c34)c2c1
Show InChI InChI=1S/C30H37N5O/c1-36-22-12-13-25-24(19-22)21(20-32-25)7-4-5-14-34-15-17-35(18-16-34)28-11-6-10-27-29(28)30(31)23-8-2-3-9-26(23)33-27/h6,10-13,19-20,32H,2-5,7-9,14-18H2,1H3,(H2,31,33)
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n/an/an/an/a<0.140n/an/an/an/a



East China University of Science and Technology

Curated by ChEMBL


Assay Description
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay

Bioorg Med Chem 26: 3117-3125 (2018)


Article DOI: 10.1016/j.bmc.2018.04.037
BindingDB Entry DOI: 10.7270/Q28P631Z
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433476
PNG
(US10562853, Compound 2)
Show SMILES CC(=O)Nc1cccc(OCCNCC2(F)CCN(CC2)C(=O)c2ccc(F)c(Cl)c2)c1
Show InChI InChI=1S/C23H26ClF2N3O3/c1-16(30)28-18-3-2-4-19(14-18)32-12-9-27-15-23(26)7-10-29(11-8-23)22(31)17-5-6-21(25)20(24)13-17/h2-6,13-14,27H,7-12,15H2,1H3,(H,28,30)
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n/an/an/an/a 0.178n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alp...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433526
PNG
(US10562853, Compound 47)
Show SMILES NC(=O)c1cccc(OCCNCC2(F)CCN(CC2)C(=O)c2ccc(F)c(Cl)c2)c1
Show InChI InChI=1S/C22H24ClF2N3O3/c23-18-13-16(4-5-19(18)24)21(30)28-9-6-22(25,7-10-28)14-27-8-11-31-17-3-1-2-15(12-17)20(26)29/h1-5,12-13,27H,6-11,14H2,(H2,26,29)
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n/an/an/an/a 0.182n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alp...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50024574
PNG
(CHEMBL3330616)
Show SMILES Cn1c(=O)cnn(CCCCN2CCN(CC2)c2cccc(F)n2)c1=O
Show InChI InChI=1S/C17H23FN6O2/c1-21-16(25)13-19-24(17(21)26)8-3-2-7-22-9-11-23(12-10-22)15-6-4-5-14(18)20-15/h4-6,13H,2-3,7-12H2,1H3
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n/an/an/an/a 0.200n/an/an/an/a



Stony Brook University

Curated by ChEMBL


Assay Description
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry

Bioorg Med Chem Lett 24: 4759-62 (2014)


Article DOI: 10.1016/j.bmcl.2014.07.048
BindingDB Entry DOI: 10.7270/Q2NZ896M
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM319716
PNG
(6-(2-(4-(benzo[b]thiophen-4-yl)piperidin-1-yl)ethy...)
Show SMILES O=C1COc2ccc(CCN3CCC(CC3)c3cccc4sccc34)cc2N1
Show InChI InChI=1S/C23H24N2O2S/c26-23-15-27-21-5-4-16(14-20(21)24-23)6-10-25-11-7-17(8-12-25)18-2-1-3-22-19(18)9-13-28-22/h1-5,9,13-14,17H,6-8,10-12,15H2,(H,24,26)
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US Patent
n/an/an/an/a 0.223n/an/an/an/a



SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES; SUZHOU VIGONVITA LIFE SCIENCES CO., LTD.; TOPHARMAN SHANDONG CO., LTD.

US Patent


Assay Description
The 5-HT1A receptor agonism activity test (The agonism activity of test compounds on 5-HT1A receptor expressing human recombinant 5-HT1A receptor in ...

US Patent US10174011 (2019)


BindingDB Entry DOI: 10.7270/Q2VH5QX7
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM319709
PNG
(5-(2-(4-(6-fluorobenzo[b]thiophen-4-yl)piperazin-1...)
Show SMILES Fc1cc(N2CCN(CCc3ccc4NC(=O)Cc4c3)CC2)c2ccsc2c1
Show InChI InChI=1S/C22H22FN3OS/c23-17-13-20(18-4-10-28-21(18)14-17)26-8-6-25(7-9-26)5-3-15-1-2-19-16(11-15)12-22(27)24-19/h1-2,4,10-11,13-14H,3,5-9,12H2,(H,24,27)
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n/an/an/an/a 0.235n/an/an/an/a



SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES; SUZHOU VIGONVITA LIFE SCIENCES CO., LTD.; TOPHARMAN SHANDONG CO., LTD.

US Patent


Assay Description
The 5-HT1A receptor agonism activity test (The agonism activity of test compounds on 5-HT1A receptor expressing human recombinant 5-HT1A receptor in ...

US Patent US10174011 (2019)


BindingDB Entry DOI: 10.7270/Q2VH5QX7
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50024605
PNG
(CHEMBL3330603 | US9290463, E)
Show SMILES Cn1c(=O)cnn(CCCCN2CCN(CC2)c2ccccc2)c1=O
Show InChI InChI=1S/C18H25N5O2/c1-20-17(24)15-19-23(18(20)25)10-6-5-9-21-11-13-22(14-12-21)16-7-3-2-4-8-16/h2-4,7-8,15H,5-6,9-14H2,1H3
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n/an/an/an/a 0.300n/an/an/an/a



Stony Brook University

Curated by ChEMBL


Assay Description
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry

Bioorg Med Chem Lett 24: 4759-62 (2014)


Article DOI: 10.1016/j.bmcl.2014.07.048
BindingDB Entry DOI: 10.7270/Q2NZ896M
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50182020
PNG
(2-(4-(4-(3-methoxyphenyl)piperazin-1-yl)butyl)-4-m...)
Show SMILES COc1cccc(c1)N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1
Show InChI InChI=1S/C19H27N5O3/c1-21-18(25)15-20-24(19(21)26)9-4-3-8-22-10-12-23(13-11-22)16-6-5-7-17(14-16)27-2/h5-7,14-15H,3-4,8-13H2,1-2H3
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n/an/an/an/a 0.300n/an/an/an/a



Columbia University College of Physicians and Surgeons

Curated by ChEMBL


Assay Description
Agonist activity assessed by stimulation of [35S]GTPgammaS binding to human 5HT1A receptor expressed in CHO cells

Bioorg Med Chem Lett 16: 2101-4 (2006)


Article DOI: 10.1016/j.bmcl.2006.01.052
BindingDB Entry DOI: 10.7270/Q2ZC82FS
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433480
PNG
(US10562853, Compound 6)
Show SMILES COc1ccccc1OCCNCC1(F)CCN(CC1)C(=O)c1ccc(F)c(Cl)c1
Show InChI InChI=1S/C22H25ClF2N2O3/c1-29-19-4-2-3-5-20(19)30-13-10-26-15-22(25)8-11-27(12-9-22)21(28)16-6-7-18(24)17(23)14-16/h2-7,14,26H,8-13,15H2,1H3
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n/an/an/an/a 0.302n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobiliz...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433537
PNG
(US10562853, Compound 60)
Show SMILES CC1(C)Cc2cccc(OCCNCC3(F)CCN(CC3)C(=O)c3ccc(F)c(Cl)c3)c2O1
Show InChI InChI=1S/C25H29ClF2N2O3/c1-24(2)15-18-4-3-5-21(22(18)33-24)32-13-10-29-16-25(28)8-11-30(12-9-25)23(31)17-6-7-20(27)19(26)14-17/h3-7,14,29H,8-13,15-16H2,1-2H3
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n/an/an/an/a 0.324n/an/an/an/a


TBA

Assay Description
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-ar...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50274835
PNG
(CHEMBL511857 | trans-1-(4-(3-methoxyphenyl)cyclohe...)
Show SMILES COc1cccc(c1)[C@H]1CC[C@@H](CC1)N1CCN(CC1)c1ccccn1 |r,wU:8.8,wD:11.15,(1.87,-39.15,;3.2,-38.38,;3.2,-36.84,;1.87,-36.07,;1.87,-34.53,;3.2,-33.76,;4.53,-34.52,;4.54,-36.07,;5.86,-33.74,;5.85,-32.21,;7.19,-31.43,;8.53,-32.2,;8.52,-33.74,;7.2,-34.51,;9.85,-31.43,;11.19,-32.21,;12.52,-31.44,;12.52,-29.9,;11.19,-29.13,;9.85,-29.9,;13.86,-29.14,;13.86,-27.61,;15.19,-26.84,;16.53,-27.61,;16.52,-29.15,;15.19,-29.92,)|
Show InChI InChI=1S/C22H29N3O/c1-26-21-6-4-5-19(17-21)18-8-10-20(11-9-18)24-13-15-25(16-14-24)22-7-2-3-12-23-22/h2-7,12,17-18,20H,8-11,13-16H2,1H3/t18-,20-
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n/an/an/an/a 0.324n/an/an/an/a



Karolinska Institute and Karolinska University Hospital

Curated by ChEMBL


Assay Description
Agonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assay

Bioorg Med Chem 23: 4824-30 (2015)


Article DOI: 10.1016/j.bmc.2015.05.042
BindingDB Entry DOI: 10.7270/Q21R6S8W
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433499
PNG
(US10562853, Compound 16)
Show SMILES Fc1ccc(cc1Cl)C(=O)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1
Show InChI InChI=1S/C24H24ClF2N3O2/c25-19-15-18(6-7-20(19)26)23(31)30-12-8-24(27,9-13-30)16-28-11-14-32-21-5-1-3-17-4-2-10-29-22(17)21/h1-7,10,15,28H,8-9,11-14,16H2
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n/an/an/an/a 0.339n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50150086
PNG
(CHEMBL127171 | [3-(5-Fluoro-1H-indol-3-yl)-propyl]...)
Show SMILES COc1ccc(F)cc1OCCNCCCc1c[nH]c2ccc(F)cc12
Show InChI InChI=1S/C20H22F2N2O2/c1-25-19-7-5-16(22)12-20(19)26-10-9-23-8-2-3-14-13-24-18-6-4-15(21)11-17(14)18/h4-7,11-13,23-24H,2-3,8-10H2,1H3
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n/an/an/an/a 0.340n/an/an/an/a



Wyeth Research

Curated by ChEMBL


Assay Description
Effective concentration against binding of radioligand [35]GTPgammaS in CHO cells expressing human 5-hydroxytryptamine 1A receptor

J Med Chem 47: 3823-42 (2004)


Article DOI: 10.1021/jm0304010
BindingDB Entry DOI: 10.7270/Q2S46RDW
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50272617
PNG
(CHEMBL4128200)
Show SMILES Nc1c2CCCCc2nc2cccc(N3CCN(CCCCc4c[nH]c5ccc(Br)cc45)CC3)c12
Show InChI InChI=1S/C29H34BrN5/c30-21-11-12-24-23(18-21)20(19-32-24)6-3-4-13-34-14-16-35(17-15-34)27-10-5-9-26-28(27)29(31)22-7-1-2-8-25(22)33-26/h5,9-12,18-19,32H,1-4,6-8,13-17H2,(H2,31,33)
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n/an/an/an/a 0.350n/an/an/an/a



East China University of Science and Technology

Curated by ChEMBL


Assay Description
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay

Bioorg Med Chem 26: 3117-3125 (2018)


Article DOI: 10.1016/j.bmc.2018.04.037
BindingDB Entry DOI: 10.7270/Q28P631Z
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50272627
PNG
(CHEMBL4126644)
Show SMILES Nc1c2CCCCc2nc2cccc(N3CCN(CCCCc4c[nH]c5ccc(cc45)C#N)CC3)c12
Show InChI InChI=1S/C30H34N6/c31-19-21-11-12-25-24(18-21)22(20-33-25)6-3-4-13-35-14-16-36(17-15-35)28-10-5-9-27-29(28)30(32)23-7-1-2-8-26(23)34-27/h5,9-12,18,20,33H,1-4,6-8,13-17H2,(H2,32,34)
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n/an/an/an/a 0.360n/an/an/an/a



East China University of Science and Technology

Curated by ChEMBL


Assay Description
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay

Bioorg Med Chem 26: 3117-3125 (2018)


Article DOI: 10.1016/j.bmc.2018.04.037
BindingDB Entry DOI: 10.7270/Q28P631Z
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433480
PNG
(US10562853, Compound 6)
Show SMILES COc1ccccc1OCCNCC1(F)CCN(CC1)C(=O)c1ccc(F)c(Cl)c1
Show InChI InChI=1S/C22H25ClF2N2O3/c1-29-19-4-2-3-5-20(19)30-13-10-26-15-22(25)8-11-27(12-9-22)21(28)16-6-7-18(24)17(23)14-16/h2-7,14,26H,8-13,15H2,1H3
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n/an/an/an/a 0.372n/an/an/an/a


TBA

Assay Description
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-ar...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM319733
PNG
(5-(2-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)ethy...)
Show SMILES Nc1nc2cc(CCN3CCN(CC3)c3cccc4sccc34)ccc2s1
Show InChI InChI=1S/C21H22N4S2/c22-21-23-17-14-15(4-5-20(17)27-21)6-8-24-9-11-25(12-10-24)18-2-1-3-19-16(18)7-13-26-19/h1-5,7,13-14H,6,8-12H2,(H2,22,23)
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US Patent
n/an/an/an/a 0.379n/an/an/an/a



SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES; SUZHOU VIGONVITA LIFE SCIENCES CO., LTD.; TOPHARMAN SHANDONG CO., LTD.

US Patent


Assay Description
The 5-HT1A receptor agonism activity test (The agonism activity of test compounds on 5-HT1A receptor expressing human recombinant 5-HT1A receptor in ...

US Patent US10174011 (2019)


BindingDB Entry DOI: 10.7270/Q2VH5QX7
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM319734
PNG
(7-(2-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)ethy...)
Show SMILES Nc1nc2cccc(CCN3CCN(CC3)c3cccc4sccc34)c2s1
Show InChI InChI=1S/C21H22N4S2/c22-21-23-17-4-1-3-15(20(17)27-21)7-9-24-10-12-25(13-11-24)18-5-2-6-19-16(18)8-14-26-19/h1-6,8,14H,7,9-13H2,(H2,22,23)
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n/an/an/an/a 0.397n/an/an/an/a



SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES; SUZHOU VIGONVITA LIFE SCIENCES CO., LTD.; TOPHARMAN SHANDONG CO., LTD.

US Patent


Assay Description
The 5-HT1A receptor agonism activity test (The agonism activity of test compounds on 5-HT1A receptor expressing human recombinant 5-HT1A receptor in ...

US Patent US10174011 (2019)


BindingDB Entry DOI: 10.7270/Q2VH5QX7
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433483
PNG
(US10562853, Compound 8)
Show SMILES COc1cccc(OCCNCC2(F)CCN(CC2)C(=O)c2ccc(F)c(Cl)c2)c1
Show InChI InChI=1S/C22H25ClF2N2O3/c1-29-17-3-2-4-18(14-17)30-12-9-26-15-22(25)7-10-27(11-8-22)21(28)16-5-6-20(24)19(23)13-16/h2-6,13-14,26H,7-12,15H2,1H3
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n/an/an/an/a 0.398n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alp...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433501
PNG
(US10562853, Compound 18)
Show SMILES Fc1ccc(cc1Cl)C(=O)N1CCC(F)(CNCCOc2ccccn2)CC1
Show InChI InChI=1S/C20H22ClF2N3O2/c21-16-13-15(4-5-17(16)22)19(27)26-10-6-20(23,7-11-26)14-24-9-12-28-18-3-1-2-8-25-18/h1-5,8,13,24H,6-7,9-12,14H2
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n/an/an/an/a 0.427n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels i...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.9b00062
BindingDB Entry DOI: 10.7270/Q23F4T9H
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM433499
PNG
(US10562853, Compound 16)
Show SMILES Fc1ccc(cc1Cl)C(=O)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1
Show InChI InChI=1S/C24H24ClF2N3O2/c25-19-15-18(6-7-20(19)26)23(31)30-12-8-24(27,9-13-30)16-28-11-14-32-21-5-1-3-17-4-2-10-29-22(17)21/h1-7,10,15,28H,8-9,11-14,16H2
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n/an/an/an/a 0.501n/an/an/an/a


TBA

Assay Description
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alp...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00814
BindingDB Entry DOI: 10.7270/Q24T6NZT
More data for this
Ligand-Target Pair
5-hydroxytryptamine receptor 1A


(Homo sapiens (Human))		BDBM50555884
PNG
(CHEMBL4741908)
Show SMILES O=C1COc2ccccc2N1CCCCN1CCN(CC1)c1cccc2sccc12
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n/an/an/an/a 0.510n/an/an/an/a


TBA

Assay Description
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 rea...

Citation and Details

Article DOI: 10.1016/j.ejmech.2020.112572
BindingDB Entry DOI: 10.7270/Q20K2D7B
More data for this
Ligand-Target Pair
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