GPCRdb

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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

acifran	259	None	36	Human	Binding	EC50	=	316.00	6.50	-	2	Agonist activity at HCA3 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA	ChEMBL	218.1	2	1	3	1.47	CC1(c2ccccc2)OC(C(=O)O)=CC1=O	https://dx.doi.org/10.1016/j.bmc.2015.02.018
CHEMBL1224070	16177	None	0	Human	Binding	IC50	=	33000.00	4.48	-	3	Displacement of radioligand from human GPR109B	ChEMBL	331.1	6	1	5	2.82	O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12	https://dx.doi.org/10.1016/j.bmcl.2010.07.108

Showing 1 to 2 of 2 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-(5-bromothiophen-3-yl)-5-methyl-4-oxo-4,5-dihydro-furan-2-carboxylic acid	126	None	0	Human	Functional	EC50	=	1470.00	5.83	-14	2	Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	301.9	2	1	4	2.29	CC1(c2csc(Br)c2)OC(C(=O)O)=CC1=O	https://dx.doi.org/10.1021/jm800896z
(+)-5-(5-bromothiophen-3-yl)-5-methyl-4-oxo-4,5-dihydro-furan-2-carboxylic acid	126	None	0	Human	Functional	EC50	=	370.00	6.43	-14	2	Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation	ChEMBL	301.9	2	1	4	2.29	CC1(c2csc(Br)c2)OC(C(=O)O)=CC1=O	https://dx.doi.org/10.1021/jm070022x
(+)-5-(5-bromothiophen-3-yl)-5-methyl-4-oxo-4,5-dihydro-furan-2-carboxylic acid	126	None	0	Human	Functional	EC50	=	1500.00	5.82	-14	2	Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation	ChEMBL	301.9	2	1	4	2.29	CC1(c2csc(Br)c2)OC(C(=O)O)=CC1=O	https://dx.doi.org/10.1021/jm070022x
2-hydroxyoctanoic acid	67	None	51	Human	Functional	pEC50	=	-	5.40	-	2	Unclassified	Guide to Pharmacology	160.1	6	2	2	1.40	CCCCCCC(O)C(=O)O	https://pubmed.ncbi.nlm.nih.gov/19561068
3-hydroxyoctanoic acid	101	None	0	Human	Functional	pEC50	=	-	5.10	-	1	Unclassified	Guide to Pharmacology	160.1	6	2	2	1.40	CCCCC[C@H](O)CC(=O)O	https://pubmed.ncbi.nlm.nih.gov/19561068
4-(n-propyl)amino-3-nitrobenzoic acid	120	None	29	Human	Functional	pEC50	=	-	7.52	-	1	Unclassified	Guide to Pharmacology	224.1	5	2	4	2.12	CCCNc1ccc(C(=O)O)cc1[N+](=O)[O-]	https://pubmed.ncbi.nlm.nih.gov/17931863
4-(n-propyl)amino-3-nitrobenzoic acid	120	None	29	Human	Functional	EC50	=	29.51	7.53	-	1	Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay	ChEMBL	224.1	5	2	4	2.12	CCCNc1ccc(C(=O)O)cc1[N+](=O)[O-]	https://dx.doi.org/10.1016/j.bmcl.2007.09.058
5-butyl-1H-pyrazole-3-carboxylic acid	131	None	45	Human	Functional	EC50	=	11748.98	4.93	-33	3	Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay	ChEMBL	168.1	4	2	2	1.45	CCCCc1cc(C(=O)O)n[nH]1	https://dx.doi.org/10.1016/j.bmcl.2007.07.101
5-methyl-5-(5-methylthiophen-3-yl)-4-oxo-4,5-dihydrofuran-2-carboxylic acid	143	None	0	Human	Functional	pEC50	None	-	6.70	-1	2	Unclassified	Guide to Pharmacology	238.0	2	1	4	1.84	Cc1cc(C2(C)OC(C(=O)O)=CC2=O)cs1	https://pubmed.ncbi.nlm.nih.gov/17358052
5-methyl-5-(5-methylthiophen-3-yl)-4-oxo-4,5-dihydrofuran-2-carboxylic acid	143	None	0	Human	Functional	EC50	=	5000.00	5.30	-1	2	Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation	ChEMBL	238.0	2	1	4	1.84	Cc1cc(C2(C)OC(C(=O)O)=CC2=O)cs1	https://dx.doi.org/10.1021/jm070022x
5-methyl-5-(5-methylthiophen-3-yl)-4-oxo-4,5-dihydrofuran-2-carboxylic acid	143	None	0	Human	Functional	EC50	=	180.00	6.75	-1	2	Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation	ChEMBL	238.0	2	1	4	1.84	Cc1cc(C2(C)OC(C(=O)O)=CC2=O)cs1	https://dx.doi.org/10.1021/jm070022x
5-methyl-5-(5-methylthiophen-3-yl)-4-oxo-4,5-dihydrofuran-2-carboxylic acid	143	None	0	Human	Functional	EC50	=	180.00	6.75	-1	2	Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation	ChEMBL	238.0	2	1	4	1.84	Cc1cc(C2(C)OC(C(=O)O)=CC2=O)cs1	https://dx.doi.org/10.1021/jm070022x
acifran	259	None	36	Human	Functional	pEC50	None	-	4.95	-4	2	Unclassified	Guide to Pharmacology	218.1	2	1	3	1.47	CC1(c2ccccc2)OC(C(=O)O)=CC1=O	https://pubmed.ncbi.nlm.nih.gov/12522134
acifran	259	None	36	Human	Functional	pEC50	None	-	4.95	-4	2	Unclassified	Guide to Pharmacology	218.1	2	1	3	1.47	CC1(c2ccccc2)OC(C(=O)O)=CC1=O	https://pubmed.ncbi.nlm.nih.gov/16389067
acifran	259	None	36	Human	Functional	pEC50	None	-	4.95	-4	2	Unclassified	Guide to Pharmacology	218.1	2	1	3	1.47	CC1(c2ccccc2)OC(C(=O)O)=CC1=O	https://pubmed.ncbi.nlm.nih.gov/17358052
acifran	259	None	36	Human	Functional	pEC50	None	-	4.95	-4	2	Unclassified	Guide to Pharmacology	218.1	2	1	3	1.47	CC1(c2ccccc2)OC(C(=O)O)=CC1=O	https://pubmed.ncbi.nlm.nih.gov/15929991
acifran	259	None	36	Human	Functional	IC50	=	3000.00	5.52	-4	2	Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	218.1	2	1	3	1.47	CC1(c2ccccc2)OC(C(=O)O)=CC1=O	https://dx.doi.org/10.1021/jm800896z
acifran	259	None	36	Human	Functional	EC50	=	3000.00	5.52	-4	2	Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation	ChEMBL	218.1	2	1	3	1.47	CC1(c2ccccc2)OC(C(=O)O)=CC1=O	https://dx.doi.org/10.1021/jm070022x
acifran	259	None	36	Human	Functional	EC50	=	4200.00	5.38	-4	2	Agonist activity at N-terminal HA-tagged GPR109b receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assay	ChEMBL	218.1	2	1	3	1.47	CC1(c2ccccc2)OC(C(=O)O)=CC1=O	https://dx.doi.org/10.1016/j.bmcl.2009.05.108
acifran	259	None	36	Human	Functional	EC50	=	4200.00	5.38	-4	2	Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	218.1	2	1	3	1.47	CC1(c2ccccc2)OC(C(=O)O)=CC1=O	https://dx.doi.org/10.1021/jm800896z

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Ligand source activities (1 row/activity)