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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 |
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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 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]