Download MendeleyDiscovery of Tertiary Amine and Indole Derivatives as Potent ROR gamma t Inverse Agonists.
Yang, T., Liu, Q., Cheng, Y., Cai, W., Ma, Y., Yang, L., Wu, Q., Orband-Miller, L.A., Zhou, L., Xiang, Z., Huxdorf, M., Zhang, W., Zhang, J., Xiang, J.N., Leung, S., Qiu, Y., Zhong, Z., Elliott, J.D., Lin, X., Wang, Y.(2014) ACS Med Chem Lett 5: 65-68
- PubMed: 24900774
- DOI: https://doi.org/10.1021/ml4003875
- Primary Citation of Related Structures:
4NIE - PubMed Abstract:
A novel series of tertiary amines as retinoid-related orphan receptor gamma-t (ROR¦Ăt) inverse agonists was discovered through agonist/inverse agonist conversion. The level of ROR¦Ăt inhibition can be enhanced by modulating the conformational disruption of H12 in ROR¦Ăt LBD. Linker exploration and rational design led to the discovery of more potent indole-based ROR¦Ăt inverse agonists.
Organizational Affiliation:
Research and Development, GlaxoSmithKline , No. 3 Building, 898 Halei Road, Pudong, Shanghai 201203, China.
