IC261 [Ligand Id: 5985] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL576349 (IC261)
  • casein kinase 1 alpha 1/Casein kinase I alpha in Human [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
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  • casein kinase 1 delta/Casein kinase I delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
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  • casein kinase 1 gamma 1/Casein kinase I gamma 1 in Human [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0]
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  • casein kinase 1 epsilon in Human [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 alpha 1/Casein kinase I alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
GtoPdb - - 4.8 pIC50 16000 nM IC50 J Biol Chem (2000) 275: 20052-60 [PMID:10749871]
ChEMBL Inhibition of CK1alpha B 5.91 pIC50 1240 nM IC50 Bioorg Med Chem Lett (2008) 18: 5672-5675 [PMID:18799313]
ChEMBL Inhibition of CK1 using KRRRALS(p)VASLPGL as substrate after 40 mins by scintillation counter B 6 pIC50 1000 nM IC50 Eur J Med Chem (2012) 56: 30-38 [PMID:22944772]
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 5.59 pIC50 2570 nM IC50 Bioorg Med Chem Lett (2008) 18: 5672-5675 [PMID:18799313]
ChEMBL Inhibition of human CK1delta expressed in simian genome expressing mouse 3T3 cells B 5.59 pIC50 2570 nM IC50 Bioorg Med Chem Lett (2010) 20: 2958-2963 [PMID:20350806]
GtoPdb - - 6 pIC50 1000 nM IC50 J Biol Chem (2000) 275: 20052-60 [PMID:10749871]
ChEMBL Inhibition of human CK1delta B 6 pIC50 1000 nM IC50 J Med Chem (2009) 52: 7618-7630 [PMID:19591487]
ChEMBL Inhibition of human recombinant CK-1delta using casein as substrate after 60 mins by Kinase-Glo assay B 6 pIC50 1000 nM IC50 J Med Chem (2014) 57: 2755-2772 [PMID:24592867]
casein kinase 1 gamma 1/Casein kinase I gamma 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0]
ChEMBL Inhibition of CK1gamma1 B 4.4 pIC50 >40000 nM IC50 Bioorg Med Chem Lett (2008) 18: 5672-5675 [PMID:18799313]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
casein kinase 1 epsilon in Human [GtoPdb: 1998] [UniProtKB: P49674]
GtoPdb - - 6 pIC50 1000 nM IC50 J Biol Chem (2000) 275: 20052-60 [PMID:10749871]

ChEMBL data shown on this page come from version 32:

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]