Document Report Card

ID: ALA3108708

Journal: ACS Med Chem Lett

Title: Discovery of Tertiary Amine and Indole Derivatives as Potent RORγt Inverse Agonists.

Authors: Yang T, Liu Q, Cheng Y, Cai W, Ma Y, Yang L, Wu Q, Orband-Miller LA, Zhou L, Xiang Z, Huxdorf M, Zhang W, Zhang J, Xiang JN, Leung S, Qiu Y, Zhong Z, Elliott JD, Lin X, Wang Y.

Abstract: A novel series of tertiary amines as retinoid-related orphan receptor gamma-t (RORγt) inverse agonists was discovered through agonist/inverse agonist conversion. The level of RORγt inhibition can be enhanced by modulating the conformational disruption of H12 in RORγt LBD. Linker exploration and rational design led to the discovery of more potent indole-based RORγt inverse agonists.

CiteXplore: 24900774

DOI: 10.1021/ml4003875