danuglipron [Ligand Id: 12064] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4518483 (Danuglipron, Pf-06882961, PF-06882961)
  • GLP-1 receptor/Glucagon-like peptide 1 receptor in Human [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GLP-1 receptor/Glucagon-like peptide 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220]
GtoPdb Binding affinity of danuglipron evaluated in a competition binding assay with radiolabeled GLP-1 as tracer - 6.44 pKi 360 nM Ki J Med Chem (2022) 65: 8208-8226 [PMID:35647711]
ChEMBL Displacement of [125I]GLP-1 from human GLP-1R (7 to 36 residues) expressed in HEK293 or CHO cell membranes after 120 mins by radioligand binding assay B 7.92 pEC50 12 nM EC50 J Med Chem (2020) 63: 5031-5073 [PMID:31930920]

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]