molecules of the month


potent, bioavailable autotaxin inhibitor

orally active in fibrosis mod., Ph. I IND cleared

from 225M cmpd DNA-encoded library + opt.

J. Med. Chem., Jul. 23, 2020

X-Chem, Waltham, MA

Structure of X-165, a highly potent and selective small molecule inhibitor of Autotaxin
1 min read

X-165 is an autotaxin inhibitor clinical candidate for idiopathic pulmonary fibrosis discovered using a 3-cycle DEL screen of 225M compounds derived from amide couplings. An unusual spirocyclic amine building block was responsible for most of their non-phosphonate-containing high-enrichment hits. The initially resynthesized hits had single-digit nanomolar potencies in an enzymatic assay, and optimization for ADME properties while maintaining potency led to X-165.

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