Synonyms: VX-853 | VX853
Compound class:
Synthetic organic
Comment: Timcodar (VX-853) is a pyridine compound that was developed by Vertex Pharmaceuticals. It acts as a mammalian and bacterial efflux pump inhibitor. It was proposed to enhance activity of antibacterials such as rifampin, by inhibiting their efflux via bacterial efflux pumps [1,3]. It was also investigated for potential to prevent efflux of chemotherapy drugs, to enhance cancer treatment, and has been proposed as a possible antiobesity therapy [2].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Grossman TH, Shoen CM, Jones SM, Jones PL, Cynamon MH, Locher CP. (2015)
The efflux pump inhibitor timcodar improves the potency of antimycobacterial agents. Antimicrob Agents Chemother, 59 (3): 1534-41. [PMID:25534740] |
2. Hinds Jr TD, John K, McBeth L, Trabbic CJ, Sanchez ER. (2016)
Timcodar (VX-853) Is a Non-FKBP12 Binding Macrolide Derivative That Inhibits PPARγ and Suppresses Adipogenesis. PPAR Res, 2016: 6218637. [PMID:27190501] |
3. Mullin S, Mani N, Grossman TH. (2004)
Inhibition of antibiotic efflux in bacteria by the novel multidrug resistance inhibitors biricodar (VX-710) and timcodar (VX-853). Antimicrob Agents Chemother, 48 (11): 4171-6. [PMID:15504837] |