orforglipron [Ligand Id: 12175] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4446782 |
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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 | Quantified by [125I]GLP-1(7-36) competition binding using GLP-1R expressing cell membranes | - | 8.49 | pKi | 3.22 | nM | Ki | Proc Natl Acad Sci U S A (2020) 117: 29959-29967 [PMID:33177239] |
| ChEMBL | Positive allosteric modulator activity at human GLP-1R expressed in PSC-HEK293 cells in presence of EC20 level of GLP1(9-36)NH2 incubated for 30 mins by HTRF cAMP assay | F | 6.22 | pEC50 | 600 | nM | EC50 | J Med Chem (2020) 63: 2292-2307 [PMID:31596080] |
| GLP-1 receptor/Glucagon-like peptide 1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075290] [GtoPdb: 249] [UniProtKB: O35659] | ||||||||
| ChEMBL | Positive allosteric modulator activity at mouse GLP-1R expressed in PSC-HEK293 cells in presence of EC20 level of GLP1(9-36)NH2 incubated for 30 mins by HTRF cAMP assay | F | 6.52 | pEC50 | 300 | nM | EC50 | J Med Chem (2020) 63: 2292-2307 [PMID:31596080] |
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]
