D. Chemistry CoreThe BCSC chemistry team has a strong record of performing effective follow-up chemistry in order to increasethe value of small-molecule hits uncovered in screens, and we offer strong 'hit-to-probe' optimization chemistrysupport for the MLPCN. This team will perform cheminformatics, synthetic medicinal chemistry and limitedpharmacology to optimize active compounds discovered in the HTS Core. The extensive medicinal chemistryand drug development experience of the team will ensure that all chemical probes are well characterized,reliable and capable of providing valid information on their activity against the target of interest. The probecompounds will be produced at our facility on multi-gram scale to ensure that they are usable by the researchcommunity for in vitro and/or in vivo studies. The chemistry team has decades of experience converting initialscreening hits into pharmaceutically relevant leads by tuning properties such as affinity, specificity, andsolubility. Since hit optimization is a collaborative effort, co-localization of the screening center with thechemistry team will increase the efficiency of probe production. The Compound Probe Development Plan(CPDP) will include input from the assay development and counter-screen development teams. Our team,which includes 19 professional staff chemists (16 Ph.D.'s) and outstanding infrastructure, will enable us togenerate 100-300 analogs within each CPDP, although it is our hope that our knowledge and experience willallow us to optimize any compound with even fewer analogs.
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