molecules of the month


bioavailable EP300/CBP HAT inhibitor

brain penetrant, orally efficacious in xeno.

from HTS and SBDD

ACS Med. Chem. Lett., Apr. 27, 2020

Constellation Pharma., Cambridge, MA

1 min read

CPI-1612 is a pretty efficient-looking EP300/CBP histone acetyltransferase (HAT) inhibitor tool compound with demonstrated activity in a xenograft model and good higher species PK. While epigenetics targets like HATs have been hot this decade, many programs have run into tolerability challenges and/or difficulty identifying activity biomarkers. It doesn’t look like CPI-1612 entered development so it’s likely the program encountered similar issues. While irrelevant for a tool compound, it’s interesting that they were able to abrogate in vitro hERG activity in an early indole series by switching to the 2-amidopyridine scaffold in CPI-1612.

request a trial

You don’t have time to read everything, but you can’t afford to fall behind.

Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples.

Get ahead now by requesting a trial.

already a member? log in: