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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

2,4-DINITROPHENOL	98143	None	45	Human	Binding	EC50	=	31100.00	4.51	-	2	Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis	ChEMBL	184.0	2	1	5	1.21	O=[N+]([O-])c1ccc(O)c([N+](=O)[O-])c1	https://dx.doi.org/10.1039/C2MD20210G
3,5-DINITROCATECHOL (OR-486)	58347	None	41	Human	Binding	EC50	=	22000.00	4.66	-	1	Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis	ChEMBL	200.0	2	2	6	0.91	O=[N+]([O-])c1cc(O)c(O)c([N+](=O)[O-])c1	https://dx.doi.org/10.1039/C2MD20210G
7-DESHYDROXYPYROGALLIN-4-CARBOXYLIC ACID	198382	None	6	Human	Binding	IC50	=	110.00	6.96	-	1	Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins	ChEMBL	248.0	1	4	5	1.01	O=C(O)c1cc(O)c(=O)c2c(O)c(O)ccc2c1	https://dx.doi.org/10.1021/ml2003058
alpha-CYANO-4-HYDROXYCINNAMIC ACID	207442	None	48	Human	Binding	IC50	=	30400.00	4.52	-	1	Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins	ChEMBL	189.0	2	2	3	1.38	N#C/C(=C\c1ccc(O)cc1)C(=O)O	https://dx.doi.org/10.1021/ml2003058
AMLEXANOX	8735	None	73	Human	Binding	EC50	=	4000.00	5.40	-	3	Agonist activity at human GPR35 expressed in CHO-K1 cells after 90 mins by beta-arrestin 2 recruitment assay	ChEMBL	298.1	2	2	5	2.75	CC(C)c1ccc2oc3nc(N)c(C(=O)O)cc3c(=O)c2c1	https://dx.doi.org/10.1021/acs.jmedchem.6b01431
BAICALEIN	208190	None	72	Human	Binding	IC50	=	28200.00	4.55	-	1	Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins	ChEMBL	270.1	1	3	5	2.58	O=c1cc(-c2ccccc2)oc2cc(O)c(O)c(O)c12	https://dx.doi.org/10.1021/ml2003058
CHEMBL107513	5471	None	25	Human	Binding	EC50	=	52600.00	4.28	-	1	Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis	ChEMBL	184.0	2	1	5	1.21	O=[N+]([O-])c1ccc([N+](=O)[O-])c(O)c1	https://dx.doi.org/10.1039/C2MD20210G
CHEMBL1256291	17196	None	28	Human	Binding	EC50	=	54400.00	4.26	-	2	Agonist activity at GPR35 in human U2OS cells assessed as induction of beta-arrestin translocation after 5 hrs by beta-lactamase reporter gene assay	ChEMBL	277.0	3	2	5	2.38	O=C(c1cc(O)c(O)c([N+](=O)[O-])c1)c1ccccc1F	https://dx.doi.org/10.1039/C2MD20210G
CHEMBL1256291	17196	None	28	Human	Binding	EC50	=	8660.00	5.06	-	2	Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis	ChEMBL	277.0	3	2	5	2.38	O=C(c1cc(O)c(O)c([N+](=O)[O-])c1)c1ccccc1F	https://dx.doi.org/10.1039/C2MD20210G
CHEMBL1368962	27526	None	29	Human	Binding	EC50	=	550.00	6.26	-	3	Antagonist activity at human N-terminal HA-tagged GPR35a expressed in human U2OS cells co-expressing GFP-fused beta arrestin-2 assessed as inhibition of agonist induced redistribution of GFP-fused beta arrestin-2 preincubated for 15 mins followed by agonist addition by fluorescence assay	ChEMBL	523.1	6	1	6	5.97	O=C(Nc1ccc2nc(SCc3ccc(Cl)cc3)sc2c1)c1ccccc1C(=O)N1CCOCC1	https://dx.doi.org/10.1016/j.bmcl.2016.12.012
CHEMBL1368962	27526	None	29	Human	Binding	IC50	=	4560.00	5.34	-	3	Antagonist activity at HA tagged GPR35a (unknown origin) expressed in human U2OS cells co-expressing GFP-fused beta arrestin-2 assessed as inhibition of zaprinast induced effect	ChEMBL	523.1	6	1	6	5.97	O=C(Nc1ccc2nc(SCc3ccc(Cl)cc3)sc2c1)c1ccccc1C(=O)N1CCOCC1	https://dx.doi.org/10.1016/j.bmcl.2016.12.012
CHEMBL1384502	29474	None	32	Human	Binding	IC50	=	522.00	6.28	-	2	Antagonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay	ChEMBL	482.1	8	3	6	4.66	CC(/C=C1\SC(=S)N(CCCC(=O)Nc2ccc(C(=O)O)c(O)c2)C1=O)=C\c1ccccc1	https://dx.doi.org/10.1021/jm4009373
CHEMBL1384502	29474	None	32	Human	Binding	Ki	=	8.76	8.06	-	2	Displacement of [3H]PSB-13253 from human recombinant GPR35 exprssed in CHO cells by liquid scintillation counting analysis	ChEMBL	482.1	8	3	6	4.66	CC(/C=C1\SC(=S)N(CCCC(=O)Nc2ccc(C(=O)O)c(O)c2)C1=O)=C\c1ccccc1	https://dx.doi.org/10.1021/jm4009373
CHEMBL1384502	29474	None	32	Human	Binding	IC50	=	27.00	7.57	-	2	Antagonist activity at human Gal4-VP16 fused GPR35 expressed in human U2OS cells assessed as beta arrestin translocation by reporter gene assay	ChEMBL	482.1	8	3	6	4.66	CC(/C=C1\SC(=S)N(CCCC(=O)Nc2ccc(C(=O)O)c(O)c2)C1=O)=C\c1ccccc1	https://dx.doi.org/10.1021/jm4009373
CHEMBL1384502	29474	None	32	Human	Binding	Ki	=	4.00	8.40	-	2	Competitive binding affinity to Nluc-fused human GPR35 expressed in CHO-K1 cells assessed as inhibition constant using furimazine as substrate incubated for 30 mins followed by substrate addition by in presence of 10-(4-(2-(4-(4-((2,8-dicarboxy-6-hydroxy-10-methylpyrido[3,2-g]quinolin-4-yl)oxy)butyl)-1H-1,2,3-triazol-1-yl)ethoxy)phenyl)-5,5-difluoro-2,7,9-trimethyl-5H-imidazo[1,2-c]pyrrolo[2,1-f][1,3,2]diazaborinin-6-ium-5-uide	ChEMBL	482.1	8	3	6	4.66	CC(/C=C1\SC(=S)N(CCCC(=O)Nc2ccc(C(=O)O)c(O)c2)C1=O)=C\c1ccccc1	https://dx.doi.org/10.1021/acsmedchemlett.2c00461
CHEMBL1384502	29474	None	32	Human	Binding	IC50	=	27.00	7.57	-	2	Antagonist activity at GPR-35 (unknown origin) by beta-arrestin assay	ChEMBL	482.1	8	3	6	4.66	CC(/C=C1\SC(=S)N(CCCC(=O)Nc2ccc(C(=O)O)c(O)c2)C1=O)=C\c1ccccc1	https://dx.doi.org/10.1021/acsmedchemlett.2c00461
CHEMBL1414071	32788	None	45	Human	Binding	EC50	=	13520.00	4.87	-	1	Agonist activity at GPR35 in human HT-29 cells by DMR assay	ChEMBL	224.0	1	1	3	2.15	O=C(O)c1cc2cc(Cl)ccc2oc1=O	https://dx.doi.org/10.1021/acs.jmedchem.6b01431
CHEMBL1414071	32788	None	45	Human	Binding	IC50	=	13240.00	4.88	-	1	Agonist activity at GPR35 in human HT-29 cells assessed as induction of cell desensitization to 1 uM zaprinast preincubated for 1 hr followed by zaprinast stimulation measured after 8 minutes by DMR assay	ChEMBL	224.0	1	1	3	2.15	O=C(O)c1cc2cc(Cl)ccc2oc1=O	https://dx.doi.org/10.1021/acs.jmedchem.6b01431
CHEMBL1490915	41511	None	4	Human	Binding	IC50	=	7230.00	5.14	-	2	Antagonist activity at HA tagged GPR35a (unknown origin) expressed in human U2OS cells co-expressing GFP-fused beta arrestin-2 assessed as inhibition of zaprinast induced effect	ChEMBL	489.1	6	1	6	5.31	O=C(Nc1ccc2nc(SCc3ccccc3)sc2c1)c1ccccc1C(=O)N1CCOCC1	https://dx.doi.org/10.1016/j.bmcl.2016.12.012
CHEMBL1600989	53468	None	35	Human	Binding	IC50	=	2300.00	5.64	-	1	Agonist activity at GPR35 in human HT-29 cells assessed as induction of cell desensitization to 1 uM zaprinast preincubated for 1 hr followed by zaprinast stimulation measured after 8 minutes by DMR assay	ChEMBL	257.9	1	1	3	2.80	O=C(O)c1cc2cc(Cl)cc(Cl)c2oc1=O	https://dx.doi.org/10.1021/acs.jmedchem.6b01431

Showing 1 to 20 of 396 entries

	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

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Ligand source activities (1 row/activity)