ralimetinib [Ligand Id: 7959] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2364626 (LSN-2322600 FREE BASE, LSN2322600 FREE BASE, Ly-2228820, LY-2228820, LY2228820, LY22288220, Ralimetinib)
  • mitogen-activated protein kinase 14 in Human [GtoPdb: 1499] [UniProtKB: Q16539]
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  • mitogen-activated protein kinase 11 in Human [GtoPdb: 1500] [UniProtKB: Q15759]
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  • epidermal growth factor receptor in Human [GtoPdb: 1797] [UniProtKB: P00533]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mitogen-activated protein kinase 14 in Human [GtoPdb: 1499] [UniProtKB: Q16539]
GtoPdb - - 8.15 pIC50 7 nM IC50 Bioorg Med Chem Lett (2008) 18: 179-83 [PMID:18039577]
GtoPdb - - 8.4 pIC50 4 nM IC50 Cell Chem Biol (2023) 30: 1211-1222.e5 [PMID:37827156]
mitogen-activated protein kinase 11 in Human [GtoPdb: 1500] [UniProtKB: Q15759]
GtoPdb - - 9 pIC50 1 nM IC50 Cell Chem Biol (2023) 30: 1211-1222.e5 [PMID:37827156]
epidermal growth factor receptor in Human [GtoPdb: 1797] [UniProtKB: P00533]
GtoPdb Inhibitor potency for EGFR with gatekeeper mutation T790M - 5.22 pIC50 6060 nM IC50 Cell Chem Biol (2023) 30: 1211-1222.e5 [PMID:37827156]
GtoPdb Inhibitor potency for WT EGFR - 6.74 pIC50 180 nM IC50 Cell Chem Biol (2023) 30: 1211-1222.e5 [PMID:37827156]
GtoPdb Inhibitor potency for EGFRG719C - 7.96 pIC50 11 nM IC50 Cell Chem Biol (2023) 30: 1211-1222.e5 [PMID:37827156]

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]