Fueling Open-Source Drug Discovery: 177 Small-Molecule Leads against Tuberculosis Articles uri icon

publication date

  • January 2013

start page

  • 313

end page

  • 321


  • 2


  • 8

International Standard Serial Number (ISSN)

  • 1860-7179

Electronic International Standard Serial Number (EISSN)

  • 1860-7187


  • With the aim of fuelling open-source, translational, early-stage drug discovery activities, the results of the recently completed antimycobacterial phenotypic screening campaign against Mycobacterium bovis BCG with hit confirmation in M. tuberculosis H37Rv were made publicly accessible. A set of 177 potent non-cytotoxic H37Rv hits was identified and will be made available to maximize the potential impact of the compounds toward a chemical genetics/proteomics exercise, while at the same time providing a plethora of potential starting points for new synthetic lead-generation activities. Two additional drug-discovery-relevant datasets are included a drug-like property analysis reflecting the latest lead-like guidelines and an early lead-generation package of the most promising hits within the clusters identified.


  • drug discovery; high throughput screening; open innovation; tuberculosis