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ChEMBL ligand: CHEMBL1951415 (PF-670462) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]