GPCRdb

Ligand source activities (1 row/activity)

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Ligands (move mouse cursor over ligand name to see structure)					Receptor	Activity									Chemical information
Sel. page	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
	10169886	175654	None	31	Human	Functional	pIC50	=	9.5	9.5	-	1	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	175654	None	31	Human	Functional	pIC50	=	9.5	9.5	-	1	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	529	None	38	Human	Functional	pIC50	=	7.7	7.7	2	2	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	529	None	38	Human	Functional	pIC50	=	7.7	7.7	2	2	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	529	None	38	Human	Functional	pIC50	=	7.7	7.7	2	2	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	2466	None	0	Rat	Functional	pEC50	=	4.4	4.4	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	16336942
	7038	2466	None	0	Rat	Functional	pEC50	=	4.4	4.4	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	16336942
	155817499	888	None	0	Human	Functional	pEC50	=	6	6.0	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	18854305
	155817499	888	None	0	Human	Functional	pEC50	=	6	6.0	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	20479330
	7040	888	None	0	Human	Functional	pEC50	=	6	6.0	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	18854305
	7040	888	None	0	Human	Functional	pEC50	=	6	6.0	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	20479330
	155817500	887	None	0	Human	Functional	pEC50	=	6.2	6.2	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	18854305
	155817500	887	None	0	Human	Functional	pEC50	=	6.2	6.2	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	20479330
	7041	887	None	0	Human	Functional	pEC50	=	6.2	6.2	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	18854305
	7041	887	None	0	Human	Functional	pEC50	=	6.2	6.2	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	20479330
	7039	454	None	0	Rat	Functional	pEC50	=	6.3	6.3	-1	2	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	454	None	0	Rat	Functional	pEC50	=	6.3	6.3	-1	2	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	454	None	0	Human	Functional	pEC50	=	6.3	6.3	1	2	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	454	None	0	Human	Functional	pEC50	=	6.3	6.3	1	2	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	2791	None	21	Mouse	Functional	pEC50	=	6.4	6.4	-9	4	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11551509
	1479	2791	None	21	Mouse	Functional	pEC50	=	6.4	6.4	-9	4	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11551509
	CHEMBL429731	2791	None	21	Mouse	Functional	pEC50	=	6.4	6.4	-9	4	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11551509
	11279	453	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	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	453	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	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	456	None	0	Human	Functional	pEC50	=	8	8.0	-	1	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	456	None	0	Human	Functional	pEC50	=	8	8.0	-	1	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	455	None	0	Rat	Functional	pIC50	=	6.5	6.5	-1	2	UnclassifiedUnclassified	Guide to Pharmacology	416	4	0	2	5.2	C=CCCN1CCC2(CC1)CN(c1c2cc(Cl)cc1)C(=O)c1c(F)cccc1F	22003054
	7042	455	None	0	Rat	Functional	pIC50	=	6.5	6.5	-1	2	UnclassifiedUnclassified	Guide to Pharmacology	416	4	0	2	5.2	C=CCCN1CCC2(CC1)CN(c1c2cc(Cl)cc1)C(=O)c1c(F)cccc1F	22003054
	7043	457	None	0	Rat	Functional	pIC50	=	6.5	6.5	-1	2	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	22003054
	59004159	455	None	0	Human	Functional	pIC50	=	6.7	6.7	1	2	UnclassifiedUnclassified	Guide to Pharmacology	416	4	0	2	5.2	C=CCCN1CCC2(CC1)CN(c1c2cc(Cl)cc1)C(=O)c1c(F)cccc1F	22003054
	7042	455	None	0	Human	Functional	pIC50	=	6.7	6.7	1	2	UnclassifiedUnclassified	Guide to Pharmacology	416	4	0	2	5.2	C=CCCN1CCC2(CC1)CN(c1c2cc(Cl)cc1)C(=O)c1c(F)cccc1F	22003054
	7043	457	None	0	Human	Functional	pIC50	=	6.8	6.8	1	2	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	22003054
	5579	529	None	38	Mouse	Functional	pIC50	=	7.3	7.3	-2	2	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	529	None	38	Mouse	Functional	pIC50	=	7.3	7.3	-2	2	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	529	None	38	Mouse	Functional	pIC50	=	7.3	7.3	-2	2	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	417	None	0	Mouse	Functional	pIC50	=	8.2	8.2	35	2	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	123805.0	417	None	0	Mouse	Functional	pIC50	=	8.2	8.2	35	2	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	46878481	417	None	0	Mouse	Functional	pIC50	=	8.2	8.2	35	2	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	5578	417	None	0	Mouse	Functional	pIC50	=	8.2	8.2	35	2	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	582	417	None	0	Mouse	Functional	pIC50	=	8.2	8.2	35	2	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	CHEMBL3545347	417	None	0	Mouse	Functional	pIC50	=	8.2	8.2	35	2	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	DB11720	417	None	0	Mouse	Functional	pIC50	=	8.2	8.2	35	2	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	6081	1311	None	0	Mouse	Functional	pIC50	=	9.5	9.5	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792

Get vendors

Ligands (move mouse cursor over ligand name to see structure)					Receptor	Activity									Chemical information
Sel. page	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
	123805	417	None	0	Mouse	Binding	pKd	=	9.1	9.1	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	123805.0	417	None	0	Mouse	Binding	pKd	=	9.1	9.1	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	46878481	417	None	0	Mouse	Binding	pKd	=	9.1	9.1	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	5578	417	None	0	Mouse	Binding	pKd	=	9.1	9.1	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	582	417	None	0	Mouse	Binding	pKd	=	9.1	9.1	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	CHEMBL3545347	417	None	0	Mouse	Binding	pKd	=	9.1	9.1	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	DB11720	417	None	0	Mouse	Binding	pKd	=	9.1	9.1	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12829792
	123805	417	None	0	Mouse	Binding	pKi	=	7.3	7.3	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420
	123805.0	417	None	0	Mouse	Binding	pKi	=	7.3	7.3	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420
	46878481	417	None	0	Mouse	Binding	pKi	=	7.3	7.3	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420
	5578	417	None	0	Mouse	Binding	pKi	=	7.3	7.3	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420
	582	417	None	0	Mouse	Binding	pKi	=	7.3	7.3	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420
	CHEMBL3545347	417	None	0	Mouse	Binding	pKi	=	7.3	7.3	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420
	DB11720	417	None	0	Mouse	Binding	pKi	=	7.3	7.3	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420
	6081	1311	None	0	Mouse	Binding	pKi	=	8.3	8.3	-	1	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	21670420

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Ligand source activities (1 row/activity)