GDC-0134 [Ligand Id: 11506] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3732012 (Gdc-0134, Rg-6000)
  • mitogen-activated protein kinase kinase kinase 12/Mitogen-activated protein kinase kinase kinase 12 in Human [ChEMBL: CHEMBL1908389] [GtoPdb: 2072] [UniProtKB: Q12852]
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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 kinase 12/Mitogen-activated protein kinase kinase kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908389] [GtoPdb: 2072] [UniProtKB: Q12852]
GtoPdb Inhibition of human DLK catalytic domain activity (1 to 520 amino acids) in a TR-FRET assay. - 8.35 pKi 4.48 nM Ki WO2014177060A1. Biheteroaryl compounds and uses thereof (2014)
ChEMBL Inhibition of N-terminally GST-tagged human DLK catalytic domain (1 to 520 amino acids) using N- terminal His-tagged MKK4 K131M substrate incubated for 60 mins by TR-FRET assay B 9 pKi 1 nM Ki WO-2014177060-A1. Biheteroaryl compounds and uses thereof (2014)

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]