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.

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