GPCRdb

Ligand source activities (1 row/activity)

Affinity
Potency

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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

AR231453	452	None	52	Human	Binding	EC50	=	4.78	8.32	-	1	Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay	ChEMBL	505.2	7	1	11	3.56	CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])CC2)n1	https://dx.doi.org/10.1016/j.bmcl.2019.126707
BMS-903452	114755	None	17	Human	Binding	EC50	=	14.00	7.85	-	1	Agonist activity at human GPR119	ChEMBL	512.0	5	0	8	3.52	CS(=O)(=O)c1ccc(-n2cc(Cl)c(OC3CCN(c4ncc(Cl)cn4)CC3)cc2=O)c(F)c1	https://dx.doi.org/10.1021/jm501175v
CHEMBL1766081	61253	None	0	Human	Binding	Ki	=	23.00	7.64	6	2	Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting	ChEMBL	386.2	5	0	7	3.67	Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C	https://dx.doi.org/10.1021/jm200003p
CHEMBL1766081	61253	None	0	Rat	Binding	Ki	=	140.00	6.85	-6	2	Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation counting	ChEMBL	386.2	5	0	7	3.67	Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C	https://dx.doi.org/10.1021/jm200003p
CHEMBL1766082	61254	None	0	Human	Binding	Ki	=	20.00	7.70	2	2	Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting	ChEMBL	428.2	5	0	8	3.15	Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C	https://dx.doi.org/10.1021/jm200003p
CHEMBL1766082	61254	None	0	Human	Binding	Ki	=	33.00	7.48	2	2	Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting	ChEMBL	428.2	5	0	8	3.15	Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C	https://dx.doi.org/10.1021/jm200003p
CHEMBL1766082	61254	None	0	Rat	Binding	Ki	=	32.00	7.50	-2	2	Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation counting	ChEMBL	428.2	5	0	8	3.15	Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C	https://dx.doi.org/10.1021/jm200003p
CHEMBL1766082	61254	None	0	Rat	Binding	Ki	=	125.00	6.90	-2	2	Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation counting	ChEMBL	428.2	5	0	8	3.15	Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C	https://dx.doi.org/10.1021/jm200003p
CHEMBL1766083	61255	None	0	Human	Binding	Ki	=	1599.00	5.80	-	1	Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting	ChEMBL	414.2	5	0	8	2.90	Cc1ncccc1Oc1ncnc(OC2C3COC2CN(C(=O)OC(C)C)C3)c1C	https://dx.doi.org/10.1021/jm200003p
CHEMBL1766202	61278	None	0	Human	Binding	Ki	=	1176.00	5.93	-	1	Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting	ChEMBL	414.2	5	0	8	2.90	Cc1ncccc1Oc1ncnc(O[C@@H]2[C@H]3CO[C@@H]2CN(C(=O)OC(C)C)C3)c1C	https://dx.doi.org/10.1021/jm200003p
CHEMBL1766203	61279	None	0	Human	Binding	Ki	=	2270.00	5.64	-	1	Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting	ChEMBL	414.2	5	0	8	2.90	Cc1ncccc1Oc1ncnc(O[C@H]2[C@@H]3CO[C@H]2CN(C(=O)OC(C)C)C3)c1C	https://dx.doi.org/10.1021/jm200003p
CHEMBL1951011	70847	None	0	Human	Binding	Ki	=	53.00	7.28	-	2	Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay	ChEMBL	467.2	6	0	8	3.51	Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CCN(C(=O)OC(C)C)CC1	https://dx.doi.org/10.1021/jm301626p
CHEMBL2086650	77418	None	1	Human	Binding	IC50	=	351.00	6.46	-	2	Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis	ChEMBL	448.2	5	0	8	2.52	CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1	https://dx.doi.org/10.1016/j.bmcl.2013.04.006
CHEMBL2086650	77418	None	1	Mouse	Binding	IC50	=	543.00	6.26	-	2	Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis	ChEMBL	448.2	5	0	8	2.52	CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1	https://dx.doi.org/10.1016/j.bmcl.2013.04.006
CHEMBL2086660	77426	None	0	Human	Binding	IC50	=	17.00	7.77	-	2	Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis	ChEMBL	462.2	5	0	8	2.90	C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1	https://dx.doi.org/10.1016/j.bmcl.2013.04.006
CHEMBL2086660	77426	None	0	Mouse	Binding	IC50	=	129.00	6.89	-	2	Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis	ChEMBL	462.2	5	0	8	2.90	C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1	https://dx.doi.org/10.1016/j.bmcl.2013.04.006
CHEMBL2086680	77445	None	0	Human	Binding	IC50	=	10.00	8.00	-	2	Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis	ChEMBL	396.2	4	0	8	2.38	CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1	https://dx.doi.org/10.1016/j.bmcl.2013.04.006
CHEMBL2086680	77445	None	0	Mouse	Binding	IC50	=	507.00	6.29	-	2	Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis	ChEMBL	396.2	4	0	8	2.38	CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1	https://dx.doi.org/10.1016/j.bmcl.2013.04.006
CHEMBL2086684	77448	None	0	Human	Binding	IC50	=	1.00	9.00	-	2	Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis	ChEMBL	410.2	4	0	8	2.77	C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1	https://dx.doi.org/10.1016/j.bmcl.2013.04.006
CHEMBL2086684	77448	None	0	Mouse	Binding	IC50	=	100.00	7.00	-	2	Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis	ChEMBL	410.2	4	0	8	2.77	C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1	https://dx.doi.org/10.1016/j.bmcl.2013.04.006

Showing 1 to 20 of 181 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

(R)-N-oleoyltyrosinol	3337	None	0	Human	Functional	pEC50	=	-	6.30	-	1	Unclassified	Guide to Pharmacology	431.3	19	3	3	6.45	CCCCCCCC/C=C/CCCCCCCC(=O)N[C@@H](CO)Cc1ccc(O)cc1	https://pubmed.ncbi.nlm.nih.gov/19901198
(S)-N-oleoyltyrosinol	3635	None	0	Human	Functional	pEC50	=	-	6.20	-	1	Unclassified	Guide to Pharmacology	431.3	19	3	3	6.45	CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](CO)Cc1ccc(O)cc1	https://pubmed.ncbi.nlm.nih.gov/19901198
1-oleoyl glycerol	37	None	0	Human	Functional	pEC50	=	-	5.60	-	1	Unclassified	Guide to Pharmacology	356.3	18	2	4	4.92	CCCCCCCC/C=C\CCCCCCCC(=O)OCC(O)CO	https://pubmed.ncbi.nlm.nih.gov/21778222
1-palmitoyl-lysophosphatidylcholine	38	None	0	Human	Functional	pEC50	=	-	5.80	-	1	Unclassified	Guide to Pharmacology	495.3	23	1	7	4.58	CCCCCCCCCCCCCCCC(=O)OC[C@H](O)COP(=O)([O-])OCC[N+](C)(C)C	https://pubmed.ncbi.nlm.nih.gov/15607732
1-stearoyl-lysophosphatidylcholine	40	None	0	Human	Functional	pEC50	=	-	5.50	-	1	Unclassified	Guide to Pharmacology	523.4	25	1	7	5.36	CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)([O-])OCC[N+](C)(C)C	https://pubmed.ncbi.nlm.nih.gov/15607732
2-oleoyl glycerol	84	None	0	Human	Functional	pEC50	=	-	5.60	-	1	Unclassified	Guide to Pharmacology	356.3	18	2	4	4.92	CCCCCCCC/C=C\CCCCCCCC(=O)OC(CO)CO	https://pubmed.ncbi.nlm.nih.gov/21778222
A77636	208	None	8	Human	Functional	IC50	=	1865.75	5.73	-616	27	GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR119	ChEMBL	329.2	2	3	4	3.25	NC[C@@H]1O[C@H](C23CC4CC(CC(C4)C2)C3)Cc2c1ccc(O)c2O	https://dx.doi.org/10.6019/CHEMBL5442687
APD668	436	None	50	Human	Functional	EC50	=	1444.63	5.84	1	2	GPCR PRESTO-Tango dose-response in agonist mode with target: GPR119	ChEMBL	477.1	5	0	9	2.75	CC(C)OC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2F)CC1	https://dx.doi.org/10.6019/CHEMBL5442687
APD668	436	None	50	Human	Functional	EC50	=	23.00	7.64	1	2	Agonist activity at human GPR119 expressed in human HEK293 cells assessed as increase in adenylate cyclase activation	ChEMBL	477.1	5	0	9	2.75	CC(C)OC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2F)CC1	https://dx.doi.org/10.1016/j.bmcl.2011.03.007
APD668	436	None	50	Human	Functional	EC50	=	2.70	8.57	1	2	Agonist activity at human GPR119 by melanophore assay	ChEMBL	477.1	5	0	9	2.75	CC(C)OC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2F)CC1	https://dx.doi.org/10.1016/j.bmcl.2011.03.007
APD668	436	None	50	Human	Functional	pEC50	=	-	8.57	1	2	Determined in a melanophore assay (Xenopus oocytes expressing GPR119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.	Guide to Pharmacology	477.1	5	0	9	2.75	CC(C)OC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2F)CC1	https://pubmed.ncbi.nlm.nih.gov/21444206
APD668	436	None	50	Rat	Functional	pEC50	=	-	7.48	-1	2	Determined in a melanophore assay (Xenopus oocytes expressing rGpr119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.	Guide to Pharmacology	477.1	5	0	9	2.75	CC(C)OC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2F)CC1	https://pubmed.ncbi.nlm.nih.gov/21444206
APD668	436	None	50	Rat	Functional	EC50	=	33.00	7.48	-1	2	Agonist activity at rat GPR119 by melanophore assay	ChEMBL	477.1	5	0	9	2.75	CC(C)OC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2F)CC1	https://dx.doi.org/10.1016/j.bmcl.2011.03.007
AR231453	452	None	52	Human	Functional	pEC50	=	-	8.20	-	1	Unclassified	Guide to Pharmacology	505.2	7	1	11	3.56	CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])CC2)n1	https://pubmed.ncbi.nlm.nih.gov/17289847
AR231453	452	None	52	Human	Functional	EC50	=	0.68	9.17	-	1	Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation	ChEMBL	505.2	7	1	11	3.56	CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])CC2)n1	https://dx.doi.org/10.1021/jm8006867
AR231453	452	None	52	Human	Functional	EC50	=	0.65	9.19	-	1	Agonist activity at human GPR119 by melanophore assay	ChEMBL	505.2	7	1	11	3.56	CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])CC2)n1	https://dx.doi.org/10.1016/j.bmcl.2011.03.007
AR231453	452	None	52	Human	Functional	EC50	=	6.00	8.22	-	1	Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay	ChEMBL	505.2	7	1	11	3.56	CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])CC2)n1	https://dx.doi.org/10.1016/j.bmc.2021.116071
AR231453	452	None	52	Human	Functional	EC50	=	640.00	6.19	-	1	Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay	ChEMBL	505.2	7	1	11	3.56	CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])CC2)n1	https://dx.doi.org/10.1016/j.ejmech.2019.112017
AR231453	452	None	52	Human	Functional	EC50	=	700.00	6.16	-	1	Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay	ChEMBL	505.2	7	1	11	3.56	CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])CC2)n1	https://dx.doi.org/10.1016/j.ejmech.2016.08.023
AR231453	452	None	52	Human	Functional	EC50	=	3000.00	5.52	-	1	Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay	ChEMBL	505.2	7	1	11	3.56	CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])CC2)n1	https://dx.doi.org/10.1016/j.bmcl.2014.03.023

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Ligand source activities (1 row/activity)