IRAK4 inhibitor 4b [PMID: 18474425] [Ligand Id: 8080] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL256713
  • interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617]
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  • interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617]
ChEMBL Inhibition of truncated human N-terminal GST-fusion tagged IRAK1 (194 to 712 residues) expressed in baculovirus expression system using FAM-labelled peptide as substrate preincubated for 10 mins followed by substrate addition and further incubated for 1 hr in presence of ATP at Km concentration by caliper mobility shift assay B 7.64 pIC50 23 nM IC50 J Med Chem (2021) 64: 10878-10889 [PMID:34279092]
ChEMBL Inhibition of wild-type human partial length IRAK1 (R194 to S712 residues) expressed in mammalian expression system by Kinomescan method B 8.05 pIC50 9 nM IC50 ACS Med Chem Lett (2020) 11: 2238-2243 [PMID:33214835]
interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3]
ChEMBL Inhibition of full length human N-terminal GST-fusion tagged IRAK4 expressed in baculovirus expression system using FAM-labelled peptide as substrate preincubated for 10 mins followed by substrate addition and further incubated for 1 hr in presence of ATP at Km concentration by caliper mobility shift assay B 7.62 pIC50 24 nM IC50 J Med Chem (2021) 64: 10878-10889 [PMID:34279092]
ChEMBL Inhibition of IRAK4 B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2008) 18: 3211-3214 [PMID:18474425]
GtoPdb - - 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2008) 18: 3211-4 [PMID:18474425]
ChEMBL Inhibition of wild-type human partial length IRAK4 (M1 to S460 residues) expressed in mammalian expression system by Kinomescan method B 7.77 pIC50 17 nM IC50 ACS Med Chem Lett (2020) 11: 2238-2243 [PMID:33214835]

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]