imlunestrant [Ligand Id: 12896] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL5095183 (Imlunestrant, Ly 3484356, LY-3484356, LY3484356) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
| ChEMBL | Binding affinity to ERalpha Y537S mutant (unknown origin) | B | 8.55 | pKi | 2.8 | nM | Ki | J Med Chem (2023) 66: 8339-8381 [PMID:37377342] |
| ChEMBL | Binding affinity to wild type ERalpha (unknown origin) | B | 9.19 | pKi | 0.64 | nM | Ki | J Med Chem (2023) 66: 8339-8381 [PMID:37377342] |
| GtoPdb | Binding affinity for WT hERα | - | 9.51 | pKi | 0.31 | nM | Ki | WO2020014435A1. Selective estrogen receptor degraders (2020) |
| ChEMBL | Induction of ERalpha Y537N mutant degradation in human MCF cells high content imaging assay | B | 8.02 | pIC50 | 9.6 | nM | IC50 | J Med Chem (2023) 66: 8339-8381 [PMID:37377342] |
| ChEMBL | Induction of wild type ERalpha degradation in human MCF cells by high content imaging assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2023) 66: 8339-8381 [PMID:37377342] |
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]
