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]
  • This target only has 0 pki data point
1 CHEMBL1088981_lig_chart_1 Farnesyl diphosphate synthase Human
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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]
  • This target only has 0 pki data point
2 CHEMBL1088981_lig_chart_2 Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 Human
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  • Rhodesain in Trypanosoma brucei rhodesiense [ChEMBL: CHEMBL4188] [UniProtKB: Q95PM0]
  • This target only has 0 pki data point
3 CHEMBL1088981_lig_chart_3 Rhodesain Trypanosoma brucei rhodesiense
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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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]