ChEMBL ligand: CHEMBL3675743
GPR4/G-protein coupled receptor 4 in Human [ChEMBL: CHEMBL3638324] [GtoPdb: 84] [UniProtKB: P46093] GPR4/G-protein coupled receptor 4 in Mouse [ChEMBL: CHEMBL4105764] [GtoPdb: 84] [UniProtKB: Q8BUD0] GPR4/G-protein coupled receptor 4 in Rat [ChEMBL: CHEMBL4105950] [GtoPdb: 84] [UniProtKB: Q4KLH9] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] There should be some charts here, you may need to enable JavaScript!
GPR68/Ovarian cancer G-protein coupled receptor 1 in Human [ChEMBL: CHEMBL3713916] [GtoPdb: 114] [UniProtKB: Q15743] There should be some charts here, you may need to enable JavaScript!
GPR65/Psychosine receptor in Human [ChEMBL: CHEMBL3714081] [GtoPdb: 113] [UniProtKB: Q8IYL9] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
GPR4/G-protein coupled receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3638324] [GtoPdb: 84] [UniProtKB: P46093]
ChEMBL	Radio Ligand Binding Assay: Serial dilutions of compounds (stock in 10 mM DMSO) are prepared by first diluting the compounds in DMSO followed by a 1:50 dilution into assay buffer (10 mM HEPES, pH 8.0, 100 mM NaCl, 5 mM MgCl2, 1 mM CaCl2, 0.5% fatty acid-free BSA, 0.05% Tween-20). The radioligand [3H]4 (example 39) (specific activity 1500 GBq/mmol) is diluted directly into the assay buffer immediately before use to obtain a 20 nM solution. The desired amount of membranes (20 μg/well) is diluted with assay buffer. 50 μL of pre-diluted compound and 50 μL of [3H]4 (example 39) is placed into the bottom of a 96-well well plate. 100 μL of the membrane-suspension is added and the plate stirred for 60 minutes. The reaction is stopped by transfer onto the filter of a 96-well GF/C filter plate (soaked for 1 hour in 0.25% PEI) using a cell harvester.	B	7.13	pIC50	74	nM	IC50	US-8748435-B2. Pyrazolo pyrimidine derivatives (2014)
GtoPdb	Measuring antagonism of pH-dependent cAMP release in HELA cells expressing human GPR4.	-	7.15	pIC50	70	nM	IC50	J Med Chem (2017) 60: 3672-3683 [PMID:28445047]
ChEMBL	Antagonist activity at human GPR4 expressed in human HeLa cells assessed as inhibition of IBMX-induced cAMP accumulation after 15 mins by HTRF assay	F	7.15	pIC50	70	nM	IC50	J Med Chem (2017) 60: 3672-3683 [PMID:28445047]
ChEMBL	Antagonist activity at human GPR4 expressed in human HeLa cells assessed as inhibition of IBMX-induced cAMP accumulation after 15 mins in presence of 40% rat plasma by HTRF assay	F	7.17	pIC50	67	nM	IC50	J Med Chem (2017) 60: 3672-3683 [PMID:28445047]
GPR4/G-protein coupled receptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105764] [GtoPdb: 84] [UniProtKB: Q8BUD0]
ChEMBL	Antagonist activity at mouse GPR4 expressed in HEK cells assessed as inhibition of IBMX-induced cAMP accumulation after 15 mins by HTRF assay	F	6.28	pIC50	530	nM	IC50	J Med Chem (2017) 60: 3672-3683 [PMID:28445047]
GPR4/G-protein coupled receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105950] [GtoPdb: 84] [UniProtKB: Q4KLH9]
ChEMBL	Antagonist activity at rat GPR4 expressed in HEK cells assessed as inhibition of IBMX-induced cAMP accumulation after 15 mins by HTRF assay	F	5.74	pIC50	1840	nM	IC50	J Med Chem (2017) 60: 3672-3683 [PMID:28445047]
GtoPdb	Measuring antagonism of pH-dependent cAMP release in HEK cells expressing rat GPR4.	-	5.74	pIC50	1840	nM	IC50	J Med Chem (2017) 60: 3672-3683 [PMID:28445047]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Displacement of [3H]dofetilide from recombinant human ERG expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method	B	4.72	pIC50	19000	nM	IC50	J Med Chem (2017) 60: 3672-3683 [PMID:28445047]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL	Displacement of [3H]-R(-)-alpha-Methyl[imidazole-2.5(n)]histamine from human recombinant histamine H3 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation counting method	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2017) 60: 3672-3683 [PMID:28445047]
GPR68/Ovarian cancer G-protein coupled receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3713916] [GtoPdb: 114] [UniProtKB: Q15743]
ChEMBL	Inhibition of OGR1 (unknown origin) expressed in human HeLa cells assessed as reduction in cAMP accumulation	F	4.7	pIC50	>20000	nM	IC50	J Med Chem (2017) 60: 3672-3683 [PMID:28445047]
GPR65/Psychosine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714081] [GtoPdb: 113] [UniProtKB: Q8IYL9]
ChEMBL	Inhibition of TDAG8 (unknown origin) expressed in human HeLa cells assessed as reduction in cAMP accumulation	F	4.7	pIC50	>20000	nM	IC50	J Med Chem (2017) 60: 3672-3683 [PMID:28445047]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]