PF-670462 [Ligand Id: 9371] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1951415 (PF-670462)
  • 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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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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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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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 human CK1 delta transfected in african green monkey cos7 cells after overnight incubation by whole cell assay B 7.09 pIC50 80.5 nM IC50 J Med Chem (2013) 56: 6819-6828 [PMID:23919824]
ChEMBL Inhibition of CK1delta B 7.1 pIC50 80 nM IC50 Eur J Med Chem (2012) 56: 30-38 [PMID:22944772]
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]
GtoPdb In a biochemical kinase assay. - 7.85 pIC50 14 nM IC50 J Pharmacol Exp Ther (2007) 322: 730-8 [PMID:17502429]
ChEMBL Inhibition of full-length human CK1delta expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL competent cells using PLSRTLpSVASLPGL as substrate incubated for 3 hrs in presence of ATP by Kinase-Glo luminescence assay B 7.85 pIC50 14 nM IC50 Eur J Med Chem (2021) 216: 113331-113331 [PMID:33721670]
ChEMBL Inhibition of human CK1delta in presence of [gamma33P]-ATP B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2019) 181: 111581-111581 [PMID:31400711]
ChEMBL Inhibition of Casein kinase 1 delta B 7.89 pIC50 13 nM IC50 J Med Chem (2012) 55: 10307-10311 [PMID:23106386]
ChEMBL Inhibition of human recombinant CK1delta expressed in Escherichia coli using PLSRTLpSVASLPGL as substrate after 2 hrs by KinaseGlo assay B 8.1 pIC50 8 nM IC50 J Med Chem (2012) 55: 956-960 [PMID:22168824]
ChEMBL Inhibition of CK1 delta (unknown origin) using PLSRTLpSVASLPGL as substrate after 60 mins by microplate reader analysis B 8.11 pIC50 7.8 nM IC50 J Med Chem (2013) 56: 6819-6828 [PMID:23919824]
casein kinase 1 epsilon/Casein kinase I epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
ChEMBL Inhibition of CK1epsilon B 6.89 pIC50 130 nM IC50 Eur J Med Chem (2012) 56: 30-38 [PMID:22944772]
ChEMBL Inhibition of Casein kinase 1 epsilon B 7.1 pIC50 80 nM IC50 J Med Chem (2012) 55: 10307-10311 [PMID:23106386]
ChEMBL Inhibition of human CK1epsilon in presence of [gamma33P]-ATP B 7.1 pIC50 80 nM IC50 Eur J Med Chem (2019) 181: 111581-111581 [PMID:31400711]
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 CK1 epsilon (unknown origin) using PLSRTLpSVASLPGL as substrate after 85 mins by microplate reader analysis B 7.54 pIC50 29 nM IC50 J Med Chem (2013) 56: 6819-6828 [PMID:23919824]
ChEMBL Inhibition of human CK1epsilon expressed in Escherichia coli BL21 using PLSRTLpSVASLPGL as substrate after 3 hrs by KinaseGlo assay B 8.1 pIC50 8 nM IC50 J Med Chem (2012) 55: 956-960 [PMID:22168824]
GtoPdb In a biochemical kinase assay. - 8.11 pIC50 7.7 nM IC50 J Pharmacol Exp Ther (2007) 322: 730-8 [PMID:17502429]
ChEMBL Inhibition of full-length human CK1epsilon expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL competent cells using PLSRTLpSVASLPGL as substrate incubated for 3 hrs in presence of ATP by Kinase-Glo luminescence assay B 8.11 pIC50 7.7 nM IC50 Eur J Med Chem (2021) 216: 113331-113331 [PMID:33721670]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
GtoPdb In a biochemical kinase assay. - 6.82 pIC50 150 nM IC50 J Pharmacol Exp Ther (2007) 322: 730-8 [PMID:17502429]
ChEMBL Inhibition of EGFR B 6.82 pIC50 150 nM IC50 J Med Chem (2012) 55: 956-960 [PMID:22168824]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of [3H]dofetilide from human ERG channel B 4.56 pIC50 27700 nM IC50 J Med Chem (2013) 56: 6819-6828 [PMID:23919824]
ChEMBL Inhibition of human ERG channel by electrophysiological method B 4.57 pIC50 27000 nM IC50 J Med Chem (2013) 56: 6819-6828 [PMID:23919824]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
GtoPdb In a biochemical kinase assay. - 6.72 pIC50 190 nM IC50 J Pharmacol Exp Ther (2007) 322: 730-8 [PMID:17502429]
ChEMBL Inhibition of p38alpha B 6.72 pIC50 190 nM IC50 J Med Chem (2012) 55: 956-960 [PMID:22168824]

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]