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ChEMBL ligand: CHEMBL4761468 (Almonertinib, Ameile, Amerol, Aumolertinib, Egfr t790m inhibitor hs-10296, EQ-143, EQ143, HS-10206, Hs 10296, Hs-10296, HS-10296) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
GtoPdb | Inhibition of wild type EGFR enzyme activity in a TR-FRET assay | - | 8.72 | pIC50 | 1.89 | nM | IC50 | WO2016054987A1. Egfr inhibitor, and preparation and application thereof (2016) |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged EGFR T790M/L858R double mutant using biotinylated TK peptide as substrate measured after 30 mins by HTRF assay | B | 9.74 | pIC50 | 0.18 | nM | IC50 | Bioorg Med Chem (2021) 36: 116094-116094 [PMID:33667898] |
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]