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Ligand source activities (1 row/activity)

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

(-)-propranolol	3187	None	44	Human	Binding	AC50	=	20610.10	4.69	-	34	Binding affinity towards human AGTR1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1038/s41467-023-40064-9
5-oxo-1-2-4-oxadiazol biphenyl	150	None	0	Rat	Binding	pKi	=	-	8.99	-	1	Unclassified	Guide to Pharmacology	423.2	9	2	5	3.69	CCC[C@@H](C(=O)O)N(Cc1ccc(-c2ccccc2-c2noc(=O)[nH]2)cc1)C(=O)CC	https://pubmed.ncbi.nlm.nih.gov/22410249
[Sar¹,Ala⁸]Ang-II	3479	None	0	Human	Binding	pKd	=	-	9.05	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11901215
[Sar¹,Cha⁴]Ang-II	3480	None	0	Rat	Binding	pKd	=	-	7.12	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11901215
[Sar¹,Cha⁴]Ang-II	3480	None	0	Rat	Binding	pKd	=	-	7.12	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10066768
[Sar¹,Cha⁸]Ang-II	3481	None	0	Rat	Binding	pKd	=	-	9.33	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11901215
[Sar¹,Cha⁸]Ang-II	3481	None	0	Rat	Binding	pKd	=	-	9.33	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10066768
[Sar¹,Gly⁴,Gly⁸]Ang-II	3483	None	0	Human	Binding	pKd	=	-	6.51	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11901215
[Sar¹,Ile⁴,Ile⁸]Ang-II	3484	None	0	Human	Binding	pKd	=	-	6.51	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12949261
[Sar¹,Ile⁸]Ang-II	3485	None	0	Human	Binding	pKd	=	-	9.43	-	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11901215
[Val5] - ANGIOTENSIN II	211801	None	28	Human	Binding	Kd	=	1.60	8.80	-	1	Binding affinity to human AT1 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.8b00435
ALFACALCIDOL	53539	None	37	Human	Binding	AC50	=	8400.00	5.08	-	2	Binding affinity towards human AGTR1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	400.3	6	2	2	6.59	C=C1/C(=C\C=C2/CCC[C@@]3(C)[C@H]2CC[C@@H]3[C@H](C)CCCC(C)C)C[C@@H](O)C[C@@H]1O	https://dx.doi.org/10.1038/s41467-023-40064-9
amisulpride	400	3H-angiotensin II	72	Human	Binding	pKi	=	10000.00	5.00	-4365	53	-	PDSP KiDatabase	369.2	7	2	6	1.28	CCN1CCCC1CNC(=O)c1cc(S(=O)(=O)CC)c(N)cc1OC	-
amitriptyline	401	None	38	Human	Binding	AC50	=	1400.00	5.85	-	51	Binding affinity towards human AGTR1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	277.2	3	0	1	4.17	CN(C)CCC=C1c2ccccc2CCc2ccccc21	https://dx.doi.org/10.1038/s41467-023-40064-9
ANETHOLTRITHION	63103	None	64	Human	Binding	AC50	=	9299.90	5.03	-	10	Binding affinity towards human AGTR1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	240.0	2	0	4	4.21	COc1ccc(-c2cc(=S)ss2)cc1	https://dx.doi.org/10.1038/s41467-023-40064-9
angiotensin A	418	None	0	Human	Binding	pKi	=	-	8.80	1	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/21464395
angiotensin II	419	None	38	Human	Binding	IC50	=	10.20	7.99	-1	5	Displacement of [125-I]-[Sar1, Ile8] from recombinant human AT1R transfected in human HEK293 cells incubated for 2 hrs by liquid scintillation counter analysis	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.bmcl.2021.128086
angiotensin II	419	None	38	Human	Binding	EC50	=	9.70	8.01	-1	5	Agonist activity at human AT1R expressed in HEK293 cells incubated for 60 mins by luminescence based beta-arrestin recruitment assay	ChEMBL	-	-	-	-	-	-	-
angiotensin II	419	None	38	Human	Binding	Ki	=	0.16	9.80	-1	5	Displacement of [3H]-Angiotensin 2 from human placental AT1 receptor expressed in African green monkey COS7 cell membranes after 90 mins by gamma counting	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.5b01495
angiotensin II	419	None	38	Human	Binding	IC50	=	0.72	9.14	-1	5	Displacement of [3H]-Asp-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-ValTyr-Ile-His-Pro-Phe-OH Tris(hydrotrifluoroacetate) from human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ after 2 hrs by liquid scintillation counting	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.5b01495

Showing 1 to 20 of 3,273 entries

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

5-butyl-methyl immidazole carboxylate 30	132	None	0	Human	Functional	pIC50	=	-	8.50	-	1	Unclassified	Guide to Pharmacology	348.2	7	1	3	4.95	CCCCc1cnc(C(=O)O)n1Cc1ccc(-c2ccccc2C)cc1	https://pubmed.ncbi.nlm.nih.gov/22889560
5-butyl-methyl immidazole carboxylate 30	132	None	0	Human	Functional	pA2	=	-	7.83	-	1	Unclassified	Guide to Pharmacology	348.2	7	1	3	4.95	CCCCc1cnc(C(=O)O)n1Cc1ccc(-c2ccccc2C)cc1	https://pubmed.ncbi.nlm.nih.gov/22889560
5-oxo-1-2-4-oxadiazol biphenyl	150	None	0	Rat	Functional	pIC50	=	-	8.80	-	1	Unclassified	Guide to Pharmacology	423.2	9	2	5	3.69	CCC[C@@H](C(=O)O)N(Cc1ccc(-c2ccccc2-c2noc(=O)[nH]2)cc1)C(=O)CC	https://pubmed.ncbi.nlm.nih.gov/22410249
[Sar¹,Ile⁸]Ang-II	3485	None	0	Rat	Functional	pEC50	=	-	8.82	-	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/7499361
A77636	208	None	8	Human	Functional	IC50	=	3130.24	5.50	-1047	27	GPCR PRESTO-Tango dose-response in antagonist mode with target: AGTR1	ChEMBL	329.2	2	3	4	3.25	NC[C@@H]1O[C@H](C23CC4CC(CC(C4)C2)C3)Cc2c1ccc(O)c2O	https://dx.doi.org/10.6019/CHEMBL5442687
angiotensin A	418	None	0	Human	Functional	pEC50	=	-	8.17	-56	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/21464395
angiotensin A	418	None	0	Rat	Functional	pIC50	=	-	9.54	-2	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/17138938
angiotensin II	419	None	38	Human	Functional	pIC50	=	-	9.15	-5	5	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10193788
angiotensin II	419	None	38	Human	Functional	pIC50	=	9.30	8.03	-5	5	None	Drug Central	-	-	-	-	-	-	-
angiotensin II	419	None	38	Human	Functional	EC50	=	2.60	8.59	-5	5	Agonist activity at human AT1R expressed in HEK293 cells incubated for 30 mins by IP1 accumulation assay	ChEMBL	-	-	-	-	-	-	-
angiotensin II	419	None	38	Human	Functional	EC50	=	0.49	9.31	-5	5	Agonist activity at human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ assessed as induction of intracellular Ca2+ mobilization by bioluminescence assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.5b01495
angiotensin II	419	None	38	Human	Functional	EC50	=	0.52	9.28	-5	5	Agonist activity at human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ assessed as induction of intracellular Ca2+ mobilization by bioluminescence assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.5b01495
angiotensin II	419	None	38	Rat	Functional	EC50	=	1.30	8.89	-6	5	Agonist activity at rat AT1aR expressed in HEK293 cells incubated for 30 mins by IP1 accumulation assay	ChEMBL	-	-	-	-	-	-	-
angiotensin III	420	None	0	Human	Functional	pIC50	=	-	8.45	-2	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	-
angiotensin IV	421	None	29	Human	Functional	pEC50	=	-	5.90	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12006574
ANGIOTENSIN-II	212873	None	5	Rat	Functional	EC50	=	7.30	8.14	-50	3	Agonist activity at rat AT1aR expressed in HEK293 cells incubated for 30 mins by IP1 accumulation assay	ChEMBL	-	-	-	-	-	-	-
ANGUSTIBALIN	185576	None	17	Human	Functional	IC50	=	21974.00	4.66	-4	2	PUBCHEM_BIOASSAY: Dose Response screen for antagonists of Angiotensin II Receptor Type 1 to assess selectivity of uHTS small molecule antagonists hits of the APJ receptor. (Class of assay: confirmatory) [Related pubchem assays: 2569, 2521 ]	ChEMBL	304.1	1	0	5	1.82	C=C1C(=O)O[C@@H]2C[C@@H](C)[C@@H]3C=CC(=O)[C@@]3(C)[C@@H](OC(C)=O)[C@H]12	-
azilsartan	560	None	64	Human	Functional	pIC50	=	-	8.11	53	2	Unclassified	Guide to Pharmacology	456.1	7	2	7	4.19	CCOc1nc2cccc(C(=O)O)c2n1Cc1ccc(-c2ccccc2-c2nc(=O)o[nH]2)cc1	https://pubmed.ncbi.nlm.nih.gov/24742498
azilsartan	560	None	64	Human	Functional	pIC50	=	-	8.11	53	2	Unclassified	Guide to Pharmacology	456.1	7	2	7	4.19	CCOc1nc2cccc(C(=O)O)c2n1Cc1ccc(-c2ccccc2-c2nc(=O)o[nH]2)cc1	https://pubmed.ncbi.nlm.nih.gov/24739538
azilsartan medoxomil	220221	None	0	Human	Functional	pIC50	=	8.13	8.09	-1	2	None	Drug Central	568.2	9	1	11	4.71	CCOc1nc2cccc(C(=O)OCc3oc(=O)oc3C)c2n1Cc1ccc(-c2ccccc2-c2noc(=O)[nH]2)cc1	-

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Ligand source activities (1 row/activity)