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ChEMBL ligand: CHEMBL4650281 (Cln 081, Cln-081, CLN-081, CLN081, TAS-6417, TAS6417, TPC-064, TPC064, Zipalertinib) |
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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 WT hEGFR in a biochemical enzyme assay | - | 8.1 | pIC50 | 8 | nM | IC50 | Mol Cancer Ther (2018) 17: 1648-1658 [PMID:29748209] |
GtoPdb | Inhibition of hEGFR with D770_N771insNPG insertion in a biochemical enzyme assay | - | 8.13 | pIC50 | 7.4 | nM | IC50 | Mol Cancer Ther (2018) 17: 1648-1658 [PMID:29748209] |
GtoPdb | Inhibition of hEGFR with T790M/L858R mutation in a biochemical enzyme assay | - | 8.7 | pIC50 | 2 | nM | IC50 | Mol Cancer Ther (2018) 17: 1648-1658 [PMID:29748209] |
ChEMBL | Inhibition of wild type EGFR (unknown origin) | B | 8.96 | pIC50 | 1.1 | nM | IC50 | RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498] |
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]