zaragozic acid A [Ligand Id: 3057] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL280978
  • farnesyltransferase, CAAX box, beta/farnesyltransferase, CAAX box, alpha/Protein farnesyltransferase in Rat [ChEMBL: CHEMBL2095197] [GtoPdb: 28262825] [UniProtKB: Q02293Q04631]
  • This target only has 0 pki data point
1 CHEMBL280978_lig_chart_1 Protein farnesyltransferase Rat
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  • squalene synthase /Squalene synthetase in Human [ChEMBL: CHEMBL3338] [GtoPdb: 645] [UniProtKB: P37268]
  • squalene synthase /Squalene synthetase in Rat [ChEMBL: CHEMBL3815] [GtoPdb: 645] [UniProtKB: Q02769]
2 CHEMBL280978_lig_chart_2 Squalene synthetase HumanRat
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
farnesyltransferase, CAAX box, beta/farnesyltransferase, CAAX box, alpha/Protein farnesyltransferase in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095197] [GtoPdb: 28262825] [UniProtKB: Q02293Q04631]
ChEMBL Inhibition of Farnesyltransferase B 7.92 pIC50 12 nM IC50 J. Med. Chem. (2002) 45: 1460-1465 [PMID:11906287]
squalene synthase /Squalene synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3338] [GtoPdb: 645] [UniProtKB: P37268]
GtoPdb Human enzyme expressed in yeast, in vitro assay - 9.6 pKi 0.25 nM Ki Arch. Biochem. Biophys. (1995) 316: 713-23 [PMID:7864626]
ChEMBL In vitro inhibitory activity of compound was measured against Candida squalene synthase(SQS) enzyme B 8.3 pIC50 5 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 2541-2546
ChEMBL Inhibition of Candida albicans squalene synthase(SQS) B 8.3 pIC50 5 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 2605-2610
GtoPdb in vitro, soluable microsomal enzymes purified from rat and human liver microsomes - 9.15 pIC50 0.7 nM - Arch. Biochem. Biophys. (1998) 350: 283-90 [PMID:9473303]
squalene synthase /Squalene synthetase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3815] [GtoPdb: 645] [UniProtKB: Q02769]
GtoPdb Compound was tested for inhibition of squalene synthase in rat liver. - 10.11 pKi 0.08 nM Ki Proc. Natl. Acad. Sci. U.S.A. (1993) 90: 80-4 [PMID:8419946]
ChEMBL In vitro inhibitory activity against Squalene synthase from rats B 7.92 pIC50 12 nM IC50 J. Med. Chem. (1996) 39: 1413-1422 [PMID:8691471]
ChEMBL In vitro inhibitory activity measured against rat squalene synthase(SQS) enzyme B 7.92 pIC50 12 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 2541-2546
ChEMBL Inhibitory concentration against mammalian Squalene synthase B 7.92 pIC50 12 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 2683-2688
ChEMBL In vitro inhibitory concentration against squalene synthase from male rat liver microsomes B 7.92 pIC50 12 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 661-666
ChEMBL Inhibition of rat liver squalene synthase(SQS) B 7.92 pIC50 12 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 2605-2610
ChEMBL In vitro inhibition of rat squalene synthase B 7.92 pIC50 12 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 1931-1936
ChEMBL Inhibition of rat liver squalene synthase by liqiud scintillation counting B 9.3 pIC50 0.5 nM IC50 J. Nat. Prod. (1993) 56: 1923-1929 [PMID:8289063]

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]