MBX-2982 [Ligand Id: 10166] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3260505 (Mbx-2982)
  • GPR119/Glucose-dependent insulinotropic receptor in Human [ChEMBL: CHEMBL5652] [GtoPdb: 126] [UniProtKB: Q8TDV5]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GPR119/Glucose-dependent insulinotropic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5652] [GtoPdb: 126] [UniProtKB: Q8TDV5]
GtoPdb - - 5.3 pEC50 5000 nM EC50 Bioorg Med Chem Lett (2014) 24: 2383-7 [PMID:24751443]
ChEMBL Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay F 5.3 pEC50 5000 nM EC50 Bioorg Med Chem Lett (2014) 24: 2383-2387 [PMID:24751443]
ChEMBL Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay F 7.06 pEC50 87 nM EC50 Bioorg Med Chem Lett (2017) 27: 5213-5220 [PMID:29103971]
ChEMBL Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay F 8.41 pEC50 3.9 nM EC50 Bioorg Med Chem Lett (2020) 30: 126855-126855 [PMID:31898998]

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]