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, LY2228820, LY-2228820, 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 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]