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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] |
| ChEMBL | Agonist activity at human GLP-1 expressed in HEK293 cells assessed as reduction in intracellular cAMP accumulation incubated for 60 mins by HTRF assay | F | 8.92 | pEC50 | 1.2 | nM | EC50 | Eur J Med Chem (2024) 275: 116632-116632 [PMID:38959726] |
| ChEMBL |
cAMP Assay: hGLP1R-HEK293 was seeded in 96 well plates at 2.0×104 cells per well and cultured over night. The medium for culturing the cells was changed to 50 μL of Medium A (DMEM, 20 mM HEPES, 0.05% BSA, 0.5 mM 3-isobutyl-1-methylxanthine) the next day, and the cells were incubated at 37° C. for 30 min. Then, 50 μL of Medium B (DMEM, 20 mM HEPES, 0.05% BSA, 0.5 mM 3-isobutyl-1-methylxanthine) containing GLP-1 or the compound was added, and the cells were incubated at 37° C. for an additional 30 min. Then, 100 μL of Assay lysis buffer (Applied Bioscience) was added, and the cells were incubated at 37° C. for 30 min. The cAMP concentration was quantified using cAMP HiRange kit (Cisbio Bioassays). |
B | 8.92 | pEC50 | 1.2 | nM | EC50 | US-10858356-B2. Pyrazolopyridine derivative having GLP-1 receptor agonist effect (2020) |
| 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 36:
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]