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Compound class: Synthetic organic
Comment: TAM16 is a benzofuran inhibitor of MTB Pks13 with potent in vitro bactericidal activity against drug-susceptible and drug-resistant clinical isolates of M. tuberculosis. In multiple mouse infection models it showed in vivo efficacy equal to the first-line TB drug isoniazid . There is PDB structure 5V3Y and the compound is example 32 in . Analogues are exemplified with activity data (with some gaps).
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. Aggarwal A, Parai MK, Shetty N, Wallis D, Woolhiser L, Hastings C, Dutta NK, Galaviz S, Dhakal RC, Shrestha R et al.. (2017)
Development of a Novel Lead that Targets M. tuberculosis Polyketide Synthase 13.
Cell, 170 (2): 249-259.e25. [PMID:28669536]
2. Sacchettini, et al.. (2016)
Substituted benzofuran derivatives as novel antimycobacterial agents.
Patent number: WO2016172498. Assignee: Texas A&M University. Priority date: 17/08/2017. Publication date: 27/10/2016.