GPCRdb

Ligand source activities (1 row/activity)

Potency
Affinity

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Ligands					Receptor			Assay information							Chemical information
Sel. page	Common 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
	10169886	182329	33	None	-	1	Human	9.5	pIC50	=	9.5	Functional	Antagonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells by cAMP accumulation based assayAntagonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells by cAMP accumulation based assay	ChEMBL	872	26	14	12	-2.3	CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C)C(=O)O	10.1021/acs.jmedchem.9b01780
	CHEMBL4578721	182329	33	None	-	1	Human	9.5	pIC50	=	9.5	Functional	Antagonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells by cAMP accumulation based assayAntagonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells by cAMP accumulation based assay	ChEMBL	872	26	14	12	-2.3	CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C)C(=O)O	10.1021/acs.jmedchem.9b01780
	5579	7317	49	None	2	2	Human	7.7	pIC50	=	7.7	Functional	Agonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulationAgonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation	ChEMBL	580	11	2	8	5.4	CCNC(=O)NS(=O)(=O)c1sc(cc1c1ccc(cc1)Cn1c(nc(c1C=O)OC)c1ccccc1)CC(C)C	10.1021/acs.jmedchem.9b01780
	9851724	7317	49	None	2	2	Human	7.7	pIC50	=	7.7	Functional	Agonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulationAgonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation	ChEMBL	580	11	2	8	5.4	CCNC(=O)NS(=O)(=O)c1sc(cc1c1ccc(cc1)Cn1c(nc(c1C=O)OC)c1ccccc1)CC(C)C	10.1021/acs.jmedchem.9b01780
	CHEMBL4303593	7317	49	None	2	2	Human	7.7	pIC50	=	7.7	Functional	Agonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulationAgonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation	ChEMBL	580	11	2	8	5.4	CCNC(=O)NS(=O)(=O)c1sc(cc1c1ccc(cc1)Cn1c(nc(c1C=O)OC)c1ccccc1)CC(C)C	10.1021/acs.jmedchem.9b01780
	155817498	9244	0	None	-	1	Rat	4.4	pEC50	=	4.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	16336942
	7038	9244	0	None	-	1	Rat	4.4	pEC50	=	4.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	16336942
	155817499	7675	0	None	-	1	Human	6.0	pEC50	=	6	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	18854305
	155817499	7675	0	None	-	1	Human	6.0	pEC50	=	6	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	20479330
	7040	7675	0	None	-	1	Human	6.0	pEC50	=	6	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	18854305
	7040	7675	0	None	-	1	Human	6.0	pEC50	=	6	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	20479330
	155817500	7674	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	18854305
	155817500	7674	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	20479330
	7041	7674	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	18854305
	7041	7674	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	20479330
	7039	7242	0	None	-1	2	Rat	6.3	pEC50	=	6.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	555	8	0	8	3.4	COc1cc(ccc1S(=O)(=O)N1CC(C(C1)c1cccc(c1)F)CN1CCN(CC1)c1ccccn1)[N+](=O)[O-]	22003054
	89560738	7242	0	None	-1	2	Rat	6.3	pEC50	=	6.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	555	8	0	8	3.4	COc1cc(ccc1S(=O)(=O)N1CC(C(C1)c1cccc(c1)F)CN1CCN(CC1)c1ccccn1)[N+](=O)[O-]	22003054
	7039	7242	0	None	1	2	Human	6.3	pEC50	=	6.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	555	8	0	8	3.4	COc1cc(ccc1S(=O)(=O)N1CC(C(C1)c1cccc(c1)F)CN1CCN(CC1)c1ccccn1)[N+](=O)[O-]	22003054
	89560738	7242	0	None	1	2	Human	6.3	pEC50	=	6.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	555	8	0	8	3.4	COc1cc(ccc1S(=O)(=O)N1CC(C(C1)c1cccc(c1)F)CN1CCN(CC1)c1ccccn1)[N+](=O)[O-]	22003054
	123797	9567	25	None	-10	3	Mouse	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11551509
	1479	9567	25	None	-10	3	Mouse	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11551509
	CHEMBL429731	9567	25	None	-10	3	Mouse	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11551509
	11279	7241	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	572	8	0	7	4.1	COc1cc(ccc1S(=O)(=O)N1CC(C(C1)c1cccc(c1)F)CN1CCN(CC1)c1ccc(cc1)F)[N+](=O)[O-]	29928987
	154733032	7241	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	572	8	0	7	4.1	COc1cc(ccc1S(=O)(=O)N1CC(C(C1)c1cccc(c1)F)CN1CCN(CC1)c1ccc(cc1)F)[N+](=O)[O-]	29928987
	11280	7244	0	None	-	1	Human	8.0	pEC50	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	480	3	0	2	6.2	Fc1cccc(c1C(=O)N1CC2(c3c1ccc(c3)C(C)(C)C)CCN(CC2)CCC(F)(F)F)F	29928987
	15983171	7244	0	None	-	1	Human	8.0	pEC50	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	480	3	0	2	6.2	Fc1cccc(c1C(=O)N1CC2(c3c1ccc(c3)C(C)(C)C)CCN(CC2)CCC(F)(F)F)F	29928987
	59004159	7243	0	None	-1	2	Rat	6.5	pIC50	=	6.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	416	4	0	2	5.2	C=CCCN1CCC2(CC1)CN(c1c2cc(Cl)cc1)C(=O)c1c(F)cccc1F	22003054
	7042	7243	0	None	-1	2	Rat	6.5	pIC50	=	6.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	416	4	0	2	5.2	C=CCCN1CCC2(CC1)CN(c1c2cc(Cl)cc1)C(=O)c1c(F)cccc1F	22003054
	7043	7245	0	None	-1	2	Rat	6.5	pIC50	=	6.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	22003054
	59004159	7243	0	None	1	2	Human	6.7	pIC50	=	6.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	416	4	0	2	5.2	C=CCCN1CCC2(CC1)CN(c1c2cc(Cl)cc1)C(=O)c1c(F)cccc1F	22003054
	7042	7243	0	None	1	2	Human	6.7	pIC50	=	6.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	416	4	0	2	5.2	C=CCCN1CCC2(CC1)CN(c1c2cc(Cl)cc1)C(=O)c1c(F)cccc1F	22003054
	7043	7245	0	None	1	2	Human	6.8	pIC50	=	6.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	22003054
	5579	7317	49	None	-2	2	Mouse	7.3	pIC50	=	7.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	580	11	2	8	5.4	CCNC(=O)NS(=O)(=O)c1sc(cc1c1ccc(cc1)Cn1c(nc(c1C=O)OC)c1ccccc1)CC(C)C	15326087
	9851724	7317	49	None	-2	2	Mouse	7.3	pIC50	=	7.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	580	11	2	8	5.4	CCNC(=O)NS(=O)(=O)c1sc(cc1c1ccc(cc1)Cn1c(nc(c1C=O)OC)c1ccccc1)CC(C)C	15326087
	CHEMBL4303593	7317	49	None	-2	2	Mouse	7.3	pIC50	=	7.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	580	11	2	8	5.4	CCNC(=O)NS(=O)(=O)c1sc(cc1c1ccc(cc1)Cn1c(nc(c1C=O)OC)c1ccccc1)CC(C)C	15326087
	123805	7205	0	None	35	2	Mouse	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	46878481	7205	0	None	35	2	Mouse	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	5578	7205	0	None	35	2	Mouse	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	582	7205	0	None	35	2	Mouse	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	CHEMBL3545347	7205	0	None	35	2	Mouse	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	DB11720	7205	0	None	35	2	Mouse	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	6081	8093	0	None	-	1	Mouse	9.5	pIC50	=	9.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792

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Ligands					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity (Affinity)	# tested GPCRs (Affinity)	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
	123805	7205	0	None	-	1	Mouse	9.1	pKd	=	9.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	46878481	7205	0	None	-	1	Mouse	9.1	pKd	=	9.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	5578	7205	0	None	-	1	Mouse	9.1	pKd	=	9.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	582	7205	0	None	-	1	Mouse	9.1	pKd	=	9.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	CHEMBL3545347	7205	0	None	-	1	Mouse	9.1	pKd	=	9.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	DB11720	7205	0	None	-	1	Mouse	9.1	pKd	=	9.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	123805	7205	0	None	-	1	Mouse	7.3	pKi	=	7.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420
	46878481	7205	0	None	-	1	Mouse	7.3	pKi	=	7.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420
	5578	7205	0	None	-	1	Mouse	7.3	pKi	=	7.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420
	582	7205	0	None	-	1	Mouse	7.3	pKi	=	7.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420
	CHEMBL3545347	7205	0	None	-	1	Mouse	7.3	pKi	=	7.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420
	DB11720	7205	0	None	-	1	Mouse	7.3	pKi	=	7.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420
	6081	8093	0	None	-	1	Mouse	8.3	pKi	=	8.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420

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Ligand source activities (1 row/activity)