darizmetinib [Ligand Id: 12376] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4795907
  • mitogen-activated protein kinase kinase 4/Dual specificity mitogen-activated protein kinase kinase 4 in Human [ChEMBL: CHEMBL2897] [GtoPdb: 2065] [UniProtKB: P45985]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mitogen-activated protein kinase kinase 4/Dual specificity mitogen-activated protein kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2897] [GtoPdb: 2065] [UniProtKB: P45985]
GtoPdb Binned value from patent data - 6.3 pIC50 <500 nM IC50 WO2019149738A1. Protein kinase mkk4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death (2019)
ChEMBL Inhibition of MKK4/(unknown origin) using JNK1 as substrate in presence of [gamma-33P]-ATP by scintillation counter assay B 6.3 pIC50 <500 nM IC50 WO-2019149738-A1. Protein kinase mkk4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death (null)

ChEMBL data shown on this page come from version 33:

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]