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Sep. 17, 2021

CPI-1612: An EP300/CBP histone acetyltransferase (HAT) inhibitor tool compound

CPI-1612

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

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Drug Hunter Team

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

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