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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]