molecules of the month


selective RORgt inverse agonist

entered clinical dev. (psoriasis), discontinued

from HTS and SBDD

ACS Med. Chem. Lett., Apr. 10, 2020

Bristol Myers Squibb, Princeton, NJ

1 min read

BMS-986251 is an inverse agonist of RORgt, a hot target in inflammation for a significant period. Unfortunately it looks like development hit a wall in this space, and several publications of various company’s RORgt modulators have appeared in the last several months. Chemically, 251 is interesting with 5 stereocenters, none of which look particularly easy to set. Looking forward to the process paper on this one!

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