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 CK1delta (unknown origin) B 7.85 pIC50 14 nM IC50 J Med Chem (2023) 66: 7162-7178 [PMID:37204207]
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 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 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 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 Casein kinase 1 epsilon B 7.1 pIC50 80 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 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 CK1epsilon (unknown origin) B 8.1 pIC50 8 nM IC50 J Med Chem (2023) 66: 7162-7178 [PMID:37204207]
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 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]