Drug Discovery

RTI's drug discovery group has more than 50 years of history in drug discovery and development of preclinical drug candidates. This history includes natural products discovery and hit generation from libraries, as well as medicinal chemistry–driven lead optimization campaigns to convert weak potency and liabilities into preclinical candidates that can enter IND-enabling studies. Our staff of principal investigators are highly skilled and experienced in a significant portion of the drug discovery and development pipeline.

Drug Discovery Capabilities

Academic Collaboration Opportunities

RTI welcomes and encourages academic collaboration, and our group has a strong track record of academic funding and collaboration. The drug discovery group can provide key services for NIH-style proposals including cheminformatics, in vivo pharmacokinetics, and in vitro preclinical assays. We also have funds available to transition novel biological assays into high-throughput screening formats and screen chemical libraries for hit generation to be used as preliminary data.

Industry and Government Collaboration Opportunities

Our team has worked extensively with industry and government collaborators, including big pharmaceutical companies, small biotech firms, and government agencies. We have functioned as a contract laboratory, as well as in a co-development role. We can provide unique drug discovery services such as isotopic labeling and cheminformatics. We also have an intellectual property portfolio and actively seek out licensing partners for its development.

Drug Discovery Successes

Recent Publications

Wu, H.X., Wacker, D., Mileni, M., Katritch, V., Han, G.W., Vardy, E., Liu, W., Thompson, A.A., Huang, X.P., Carroll, F.I., Mascarella, S.W., et al. (2012). Structure of the human kappa-opioid receptor in complex with JDTic. Nature, 485 (7398):327-332.

Hassler, C., Zhang, Y., Gilmour, B., Graf, T., Fennell, T., Snyder, R., Deschamps, J.R., Reinscheid, R.K., Garau, C., & Runyon, S.P. (2014). Identification of Neuropeptide S Antagonists: Structure-Activity Relationship Studies, X-ray Crystallography, and in Vivo EvaluationACS Chemical Neuroscience, 5 (8):731-744.

Reith, M.E., Blough, B.E., Hong, W.C., Jones, K.T., Schmitt, K.C., Baumann, M.H., et al. (2015). Behavioral, biological, and chemical perspectives on atypical agents targeting the dopamine transporterDrug and Alcohol Dependence, 147:1-19.

Thomas, J.B., Giddings, A.M., Wiethe, R.W., Olepu, S., Warner, K.R., Sarret, P., Gendron, L., Longpre, J.M., Zhang, Y., Runyon, S.P., & Gilmour, B.P. (2014). Identification of N-[(5-{[(4-Methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl] -l-leucine (NTRC-824), a Neurotensin-like Nonpeptide Compound Selective for the Neurotensin Receptor Type 2Journal of Medicinal Chemistry, 57 (17):7472-7477.