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ChEMBL ligand: CHEMBL311228 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Cell division control protein 28 in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5213] [UniProtKB: P00546] | ||||||||
ChEMBL | Inhibition of yeast W303 cdc28 phosphorylation assessed as [32P] incorporation in histone H1 from [gamma32P]ATP by scintillation counting | B | 5.15 | pIC50 | 7000 | nM | IC50 | Science (1998) 281: 533-538 [PMID:9677190] |
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635] | ||||||||
ChEMBL | Inhibition of human cdc2/cyclin B assessed as [32P] incorporation in histone H1 from [gamma32P]ATP | B | 6.47 | pIC50 | 340 | nM | IC50 | Science (1998) 281: 533-538 [PMID:9677190] |
GtoPdb | CDK1/cyclin B complex | - | 6.47 | pIC50 | 340 | nM | IC50 | Science (1998) 281: 533-8 [PMID:9677190] |
Cyclin-dependent protein kinase PHO85 in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5589] [UniProtKB: P17157] | ||||||||
ChEMBL | Inhibition of yeast W303 Pho85 phosphorylation assessed as [32P] incorporation in histone H1 from [gamma32P]ATP by scintillation counting | B | 5.7 | pIC50 | 2000 | nM | IC50 | Science (1998) 281: 533-538 [PMID:9677190] |
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
ChEMBL | Binding affinity to GSK3-beta | B | 6.9 | pKd | 126 | nM | Kd | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
GtoPdb | - | - | 7.52 | pIC50 | 30 | nM | IC50 | Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363] |
ChEMBL | Inhibition of GSK3-beta | B | 7.52 | pIC50 | 30 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525] | ||||||||
ChEMBL | Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay | B | 4.8 | pIC50 | 16000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4108-4114 [PMID:21632247] |
MER proto-oncogene, tyrosine kinase/Proto-oncogene tyrosine-protein kinase MER in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866] | ||||||||
ChEMBL | Inhibition of Mer kinase | B | 4.95 | pIC50 | 11300 | nM | IC50 | ACS Med Chem Lett (2011) 2: 907-912 [PMID:22247788] |
ChEMBL | Inhibition of MER (588 to 855) (unknown origin) by fluorescence assay | B | 4.95 | pIC50 | 11300 | nM | IC50 | Eur J Med Chem (2013) 61: 2-25 [PMID:22749189] |
ChEMBL | Inhibition of N-terminal His-tagged Mer kinase (588 to 855 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells measured every min by ADP Quest Assay | B | 4.95 | pIC50 | 11300 | nM | IC50 | Bioorg Med Chem (2016) 24: 3083-3092 [PMID:27238842] |
ChEMBL | Inhibition of Mer expressed in Escherichia coli BL21 (DE3) cells using EFPIYDFLPAKKK-CONH2 as substrate after 180 mins by microfluid capillary electrophoresis assay | B | 4.96 | pIC50 | 11000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 129-134 [PMID:22662287] |
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]