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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 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]