IRAK4 inhibitor rac-45 [PMID: 18501603] [Ligand Id: 8081] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL401633
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  • 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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  • fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NRAS/GTPase NRas in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2079845] [GtoPdb: 2823] [UniProtKB: P01111]
ChEMBL AlphaLISA Assay: AlphaScreen SureFire STAT5 (pTyr694;Tyr699) Assay kit (Perkin Elmer). Assay was performed according to manufacturer protocol. B 5.75 pIC50 1760 nM IC50 US-11254667-B2. Substituted imidazo[1,2-A]pyridines as IRAK 1/4 and flt3 inhibitors (2022)
ChEMBL IC50 Kinase Assays: Table 8-10: Compounds were tested in 10-dose IC50 mode with 3-fold serial dilution starting at 10 uM, and are relative to DMSO, the negative control. The positive control, Staurosporine, was tested in a 10-dose IC50 mode with 4-fold serial dilution starting at 20 uM. Reactions were carried out at 10 uM ATP. Curve fits were performed to determine IC50 where the enzyme activities at the highest concentration of compounds were less than 65%. B 5.75 pIC50 1760 nM IC50 US-11542261-B2. Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors (2023)
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 IRAK1 B 4.64 pIC50 23000 nM IC50 Bioorg Med Chem Lett (2008) 18: 3656-3660 [PMID:18501603]
interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3]
GtoPdb - - 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2008) 18: 3656-60 [PMID:18501603]
ChEMBL Inhibition of IRAK4 B 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2008) 18: 3656-3660 [PMID:18501603]
fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL AlphaLISA Assay: AlphaScreen SureFire STAT5 (pTyr694;Tyr699) Assay kit (Perkin Elmer). Assay was performed according to manufacturer protocol. B 7.52 pIC50 30 nM IC50 US-11254667-B2. Substituted imidazo[1,2-A]pyridines as IRAK 1/4 and flt3 inhibitors (2022)

ChEMBL data shown on this page come from version 36:

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]