FR-49175 [Ligand Id: 3150] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1088981 (3R,10Ar-Dithiomethyl Gliotoxin A)
  • farnesyl diphosphate synthase/Farnesyl diphosphate synthase in Human [ChEMBL: CHEMBL1782] [GtoPdb: 644] [UniProtKB: P14324]
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  • euchromatic histone lysine methyltransferase 2/Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 in Human [ChEMBL: CHEMBL6032] [GtoPdb: 2652] [UniProtKB: Q96KQ7]
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  • Rhodesain in Trypanosoma brucei rhodesiense [ChEMBL: CHEMBL4188] [UniProtKB: Q95PM0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
farnesyl diphosphate synthase/Farnesyl diphosphate synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1782] [GtoPdb: 644] [UniProtKB: P14324]
ChEMBL Inhibition of farnesyl protein transferase B 4 pIC50 >100000 nM IC50 Bioorg Med Chem (2010) 18: 2566-2574 [PMID:20303767]
euchromatic histone lysine methyltransferase 2/Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6032] [GtoPdb: 2652] [UniProtKB: Q96KQ7]
ChEMBL Inhibition of HMT-G9a using S-adenosylmethionine and biotinylated H3 peptide after 1 hr B 4 pIC50 >100000 nM IC50 J Nat Prod (2012) 75: 111-114 [PMID:22148349]
Rhodesain in Trypanosoma brucei rhodesiense (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4188] [UniProtKB: Q95PM0]
ChEMBL Inhibition of Trypanosoma brucei brucei recombinant rhodesain after 5 mins by spectrofluorimetry B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem (2010) 18: 2566-2574 [PMID:20303767]

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]