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ChEMBL ligand: CHEMBL256713 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]