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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]