PF-4800567 [Ligand Id: 8050] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2069623 (PF-4800567)
  • casein kinase 1 delta/Casein kinase I delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
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  • casein kinase 1 epsilon/Casein kinase I epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 1 delta/Casein kinase I delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
ChEMBL Inhibition of CK1delta B 6.15 pIC50 711 nM IC50 Eur J Med Chem (2012) 56: 30-38 [PMID:22944772]
ChEMBL Inhibition of Casein kinase 1 delta B 6.15 pIC50 711 nM IC50 J Med Chem (2012) 55: 10307-10311 [PMID:23106386]
ChEMBL Inhibition of human CK1delta in presence of [gamma33P]-ATP B 6.15 pIC50 711 nM IC50 Eur J Med Chem (2019) 181: 111581-111581 [PMID:31400711]
GtoPdb - - 6.15 pIC50 711 nM IC50 J Pharmacol Exp Ther (2009) 330: 430-9 [PMID:19458106]
ChEMBL Inhibition of human full length CK1delta1 (2 to 415 residues) using PLSRTLpSVASLPGL as substrate after 2 hrs by kinase-glo assay B 7.49 pIC50 32 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
casein kinase 1 epsilon/Casein kinase I epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
GtoPdb - - 7.49 pIC50 32 nM IC50 J Pharmacol Exp Ther (2009) 330: 430-9 [PMID:19458106]
ChEMBL Inhibition of CK1epsilon B 7.49 pIC50 32 nM IC50 Eur J Med Chem (2012) 56: 30-38 [PMID:22944772]
ChEMBL Inhibition of Casein kinase 1 epsilon B 7.49 pIC50 32 nM IC50 J Med Chem (2012) 55: 10307-10311 [PMID:23106386]
ChEMBL Inhibition of human full length polyhistidine-tagged CK1epsilon expressed in Escherichia coli BL21-Codon-Plus (DE3)-RIL using PLSRTLpSVASLPGL as substrate after 2 hrs by kinase-glo assay B 7.49 pIC50 32 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
ChEMBL Inhibition of human CK1epsilon in presence of [gamma33P]-ATP B 7.49 pIC50 32 nM IC50 Eur J Med Chem (2019) 181: 111581-111581 [PMID:31400711]

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]