- Guide to PHARMACOLOGY
Synonyms: compound 2 [PMID: 10098671] | XR-9576 | XR9576
Compound class: Synthetic organic
Comment: Tariquidar (XR9576) is a third generation inhibitor of the ATP-binding cassette transporter P-glycoprotein (P-gp; ABCB1) . P-gp is a drug transporter that can promote resistance to drugs, including chemotherapeutics. Pharmacologic inhibition of P-gp is an established strategy that is being investigated to block this resistance mechanism in cancers .
Ligand Activity Visualisation Charts
These 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.✖
1. Fox E, Bates SE. (2007)
Tariquidar (XR9576): a P-glycoprotein drug efflux pump inhibitor.
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2. Lai JI, Tseng YJ, Chen MH, Huang CF, Chang PM. (2020)
Clinical Perspective of FDA Approved Drugs With P-Glycoprotein Inhibition Activities for Potential Cancer Therapeutics.
Front Oncol, 10: 561936. [PMID:33312947]
3. Roe M, Folkes A, Ashworth P, Brumwell J, Chima L, Hunjan S, Pretswell I, Dangerfield W, Ryder H, Charlton P. (1999)
Reversal of P-glycoprotein mediated multidrug resistance by novel anthranilamide derivatives.
Bioorg Med Chem Lett, 9 (4): 595-600. [PMID:10098671]