GPR4 antagonist 3b [Ligand Id: 10207] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3810385
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  • GPR68/Ovarian cancer G-protein coupled receptor 1 in Human [ChEMBL: CHEMBL3713916] [GtoPdb: 114] [UniProtKB: Q15743]
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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]
GtoPdb - - 7.17 pIC50 67 nM IC50 ACS Med Chem Lett (2016) 7: 493-7 [PMID:27190599]
ChEMBL Antagonist activity at N-terminal HA-tagged GPR4 (unknown origin) expressed in HEK293 cells assessed as inhibition of pH dependent cAMP response element-driven transcriptional activity at pH 7.2 incubated for 6 hrs by dual luciferase reporter gene assay F 7.17 pIC50 67 nM IC50 ACS Med Chem Lett (2016) 7: 493-497 [PMID:27190599]
GPR68/Ovarian cancer G-protein coupled receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3713916] [GtoPdb: 114] [UniProtKB: Q15743]
ChEMBL Antagonist activity at N-terminal HA-tagged OGR1 (unknown origin) expressed in HEK293 cells assessed as inhibition of pH dependent nuclear factor of activated T-cell activity at pH 7.2 incubated for 6 hrs by dual luciferase reporter gene assay B 5 pIC50 >10000 nM IC50 ACS Med Chem Lett (2016) 7: 493-497 [PMID:27190599]
GPR65/Psychosine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714081] [GtoPdb: 113] [UniProtKB: Q8IYL9]
ChEMBL Antagonist activity at N-terminal HA-tagged TDAG8 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of pH dependent cAMP response element-driven transcriptional activity at pH 7.2 incubated for 6 hrs by dual luciferase reporter gene assay F 5 pIC50 >10000 nM IC50 ACS Med Chem Lett (2016) 7: 493-497 [PMID:27190599]

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]