orforglipron [Ligand Id: 12175] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4446782 (Ly3502970, LY-3502970, LY3502970, Orforglipron) |
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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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
