zaragozic acid A [Ligand Id: 3057] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL280978 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| farnesyltransferase, CAAX box, subunit beta/farnesyltransferase, CAAX box, subunit alpha/Protein farnesyltransferase in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095197] [GtoPdb: 2826, 2825] [UniProtKB: Q02293, Q04631] | ||||||||
| 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 USA (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 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]
