GproteinDb

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
	6433	3796	0	None	-10	2	Human	5.9	pIC50	=	5.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	563	10	4	9	2.2	COc1ccc(cc1)Cn1c(NCCNC(=N)NC(=O)c2ccc(cc2)F)nc(=O)n(c1=O)Cc1ccc(cc1)F	21421710
	73755221	3796	0	None	-10	2	Human	5.9	pIC50	=	5.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	563	10	4	9	2.2	COc1ccc(cc1)Cn1c(NCCNC(=N)NC(=O)c2ccc(cc2)F)nc(=O)n(c1=O)Cc1ccc(cc1)F	21421710
	1866	3129	0	None	1	2	Human	7.2	pIC50	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12054613
	1866	3129	0	None	1	2	Human	7.2	pIC50	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	15772293
	16122905	3086	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	438	7	0	5	3.7	CC(CN(C(=O)C1OCCN(C1)Cc1ccccc1)Cc1ccc2c(c1)OCCCO2)C	22431614
	6066	3086	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	438	7	0	5	3.7	CC(CN(C(=O)C1OCCN(C1)Cc1ccccc1)Cc1ccc2c(c1)OCCCO2)C	22431614
	1867	3130	0	None	-1	2	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12054613
	1867	3130	0	None	-1	2	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	15772293
	1865	2507	0	None	6	2	Human	9.2	pIC50	=	9.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12054613
	1868	3132	0	None	-31	2	Human	6.0	pIC50	>	6	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	15772293

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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
	11951384	3795	0	None	-74	2	Human	5.8	pKi	=	5.8	Binding	Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane	ChEMBL	451	10	3	8	0.8	CCc1ccc(cc1)Cn1c(=O)nc(n(c1=O)Cc1ccc(cc1)OC)NCCN=C(N)N	10.1021/jm800854e
	6064	3795	0	None	-74	2	Human	5.8	pKi	=	5.8	Binding	Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane	ChEMBL	451	10	3	8	0.8	CCc1ccc(cc1)Cn1c(=O)nc(n(c1=O)Cc1ccc(cc1)OC)NCCN=C(N)N	10.1021/jm800854e
	CHEMBL457515	3795	0	None	-74	2	Human	5.8	pKi	=	5.8	Binding	Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane	ChEMBL	451	10	3	8	0.8	CCc1ccc(cc1)Cn1c(=O)nc(n(c1=O)Cc1ccc(cc1)OC)NCCN=C(N)N	10.1021/jm800854e
	25138121	189031	0	None	-53	2	Human	4.6	pKi	=	4.6	Binding	Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane	ChEMBL	409	9	2	8	1.4	CCc1ccc(Cn2c(=O)nc(NCCN)n(Cc3ccc(OC)cc3)c2=O)cc1	10.1021/jm800854e
	CHEMBL514895	189031	0	None	-53	2	Human	4.6	pKi	=	4.6	Binding	Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane	ChEMBL	409	9	2	8	1.4	CCc1ccc(Cn2c(=O)nc(NCCN)n(Cc3ccc(OC)cc3)c2=O)cc1	10.1021/jm800854e
	25138122	175525	0	None	-15	2	Human	4.2	pKi	=	4.2	Binding	Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane	ChEMBL	477	10	3	10	1.0	CCc1ccc(Cn2c(=O)nc(NCCNC3=NCCN3)n(Cc3ccc(OC)cc3)c2=O)cc1	10.1021/jm800854e
	CHEMBL459142	175525	0	None	-15	2	Human	4.2	pKi	=	4.2	Binding	Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane	ChEMBL	477	10	3	10	1.0	CCc1ccc(Cn2c(=O)nc(NCCNC3=NCCN3)n(Cc3ccc(OC)cc3)c2=O)cc1	10.1021/jm800854e
	11951384	3795	0	None	-74	2	Human	5.8	pKi	=	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	451	10	3	8	0.8	CCc1ccc(cc1)Cn1c(=O)nc(n(c1=O)Cc1ccc(cc1)OC)NCCN=C(N)N	19006379
	6064	3795	0	None	-74	2	Human	5.8	pKi	=	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	451	10	3	8	0.8	CCc1ccc(cc1)Cn1c(=O)nc(n(c1=O)Cc1ccc(cc1)OC)NCCN=C(N)N	19006379
	CHEMBL457515	3795	0	None	-74	2	Human	5.8	pKi	=	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	451	10	3	8	0.8	CCc1ccc(cc1)Cn1c(=O)nc(n(c1=O)Cc1ccc(cc1)OC)NCCN=C(N)N	19006379