D4476 [Ligand Id: 5940] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL410456 |
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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]
