“compound 2” is a heme-displacing IDO1 inhibitor with a similar binding mode to BMS-986205 with a low projected human dose. A bis-amide hit was generated from a mass-spectrometry based binding screen, and optimized through structure-based drug design. An initial benzamide lead was metabolically unstable due to rapid amide hydrolysis, but this [...]
< 1 minute read
Sep. 18, 2021
Compound 2: A Potent, Oral Heme-Displacing IDO1 Inhibitor
"compound 2"
potent, oral heme-displacing IDO1 inhibitor low predicted human dose (<10 mg QD) from ALIS mass-based binding screen + SBDD ACS Med. Chem. Lett., Jul. 15, 2020 Merck & Co., Boston, MA
Loading...
