D4476 [Ligand Id: 5940] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL410456
  • casein kinase 1 alpha 1/Casein kinase I alpha in Human [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
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  • casein kinase 1 delta/Casein kinase I delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
  • casein kinase 1 delta/Casein kinase I delta in Rat [ChEMBL: CHEMBL4484] [GtoPdb: 1997] [UniProtKB: Q06486]
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  • casein kinase 1 epsilon/Casein kinase I epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
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  • Casein kinase II subunit alpha in Schizosaccharomyces pombe 972h- [ChEMBL: CHEMBL1075255] [UniProtKB: P40231]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • protein kinase D1/Protein kinase C mu in Human [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139]
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  • transforming growth factor beta receptor 1/TGF-beta receptor type I in Human [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 1 alpha 1/Casein kinase I alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
GtoPdb - - 6.52 pIC50 300 nM IC50 Eur J Med Chem (2012) 56: 30-8 [PMID:22944772]
ChEMBL Inhibition of CK1 using KRRRALS(p)VASLPGL as substrate after 40 mins by scintillation counter B 6.52 pIC50 300 nM IC50 Eur J Med Chem (2012) 56: 30-38 [PMID:22944772]
casein kinase 1 delta/Casein kinase I delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
GtoPdb - - 6.52 pIC50 300 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
ChEMBL Inhibition of CK1delta B 6.52 pIC50 300 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of CK1delta in the presence of 100uM ATP B 6.52 pIC50 300 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
ChEMBL Inhibition of human CK1D using KRRRAL[pS]VASLPGL as substrate by [gamma-33P]-ATP assay B 6.77 pIC50 171 nM IC50 Eur J Med Chem (2019) 161: 456-467 [PMID:30384048]
casein kinase 1 delta/Casein kinase I delta in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4484] [GtoPdb: 1997] [UniProtKB: Q06486]
ChEMBL Inhibition of rat CK1delta in presence of 20 uM ATP B 6.45 pIC50 353.3 nM IC50 Bioorg Med Chem Lett (2013) 23: 5578-5585 [PMID:24007918]
ChEMBL Inhibition of GST-fused rat CK1delta expressed in Escherichia coli using phosphorylated peptide TFRPRTSpSNASTIS as substrate B 6.52 pIC50 300 nM IC50 J Med Chem (2009) 52: 7618-7630 [PMID:19591487]
casein kinase 1 epsilon/Casein kinase I epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
ChEMBL Inhibition of human CK1E using KRRRAL[pS]VASLPGL as substrate by [gamma-33P]-ATP assay B 6.47 pIC50 338 nM IC50 Eur J Med Chem (2019) 161: 456-467 [PMID:30384048]
Casein kinase II subunit alpha in Schizosaccharomyces pombe 972h- (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075255] [UniProtKB: P40231]
ChEMBL Inhibition of Schizosaccharomyces pombe CK1 B 6.7 pIC50 200 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibition of p38alpha B 4.92 pIC50 12000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of GST-fused human p38alpha expressed in Escherichia coli B 4.92 pIC50 12000 nM IC50 J Med Chem (2009) 52: 7618-7630 [PMID:19591487]
ChEMBL Inhibition of p38-alpha MAPK in the presence of 50uM ATP B 5.24 pIC50 5800 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
ChEMBL Inhibition of human p38alpha MAPK in presence of 50 uM ATP B 5.38 pIC50 4154 nM IC50 Bioorg Med Chem Lett (2013) 23: 5578-5585 [PMID:24007918]
protein kinase D1/Protein kinase C mu in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139]
ChEMBL Inhibition of PKD1 in the presence of 50uM ATP B 5.04 pIC50 9100 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
transforming growth factor beta receptor 1/TGF-beta receptor type I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
ChEMBL Inhibition of ALK5 B 6.3 pIC50 500 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]

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]