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
X-165
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.
Search By Structure
- A-1331852
- dotinurad (FYU-981)
- X-165
- “compound 38a”
- HTL22562
- “compound 23”
- MGS0274
- LXE408
- “compound 2”
- AB680
- “compound 18”
- ETX0282
- “compound 6g”
- EC2629
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