IC261 [Ligand Id: 5985] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL576349 (IC261) |
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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 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]
