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 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]