Systematic Chemogenetic Library Assembly

Abstract

Chemogenetic libraries, collections of well-defined chemical probes, provide tremendous value to biomedical research but require substantial effort to ensure diversity as well as quality of the contents. We have assembled a chemogenetic library by data mining and crowdsourcing institutional expertise. We are sharing our approach, lessons learned, and disclosing our current collection of 4,185 compounds with their primary annotated gene targets (https://github.com/Novartis/MoaBox). This physical collection is regularly updated and used broadly both within Novartis and in collaboration with external partners. ll

Engineering digitizer circuits for chemical and genetic screens in human cells

“…This library is typically used to study compound mechanism of action (MoA) and can help identify genes that are involved in a pathway of interest. Others have used this well-defined library to study a variety of pathways, and findings from these screens are compiled for collaborative use 23 . We thus used this compound library to test whether drug hits that emerged would corroborate with our PKC-specific AP-1 pathway in both agonist and antagonist screens.…”

Will the chemical probes please stand up?

“…It is regularly updated and used widely both within Novartis and by their external collaborators. 64 …”

Fostering Research Synergies between Chemists in Swiss Academia and at Novartis

“…50'000 non-proprietary compounds containing highly diverse LMW structures 2. 4'200 compounds with defined mode of action (MoA box) [25] 3. ~3000 purified natural products 4.…”