molecules of the month


in vitro ATAD2 inhibitor

Preclinical, oncology

from 1.8 million compound HTS and opt.

J. Med. Chem.


in vitro ATAD2 inhibitor - AstraZeneca
2 mins read

Context. AZ13824374 (AstraZeneca) is an in vitro ATAD2 inhibitor. Reviewer and nominator Julien Lefranc says, “several ATAD2 probes have been published in the past (including GSK 8814, GSCK388, and BAY-850), but so far no compounds have reached clinical trials.” ATAD2 is a bromodomain-containing, chromatin-binding target that is overexpressed in many cancers due to c-Myc coamplification. While ATAD2 inhibition is supported by siRNA target modulation, there is limited pharmacological evidence to support it as a bona fide cancer target.  Prior literature molecules showed limited cellular activity, or activity that is confounded by potential off-target activities. This tool compound is the first to demonstrate significant cellular ATAD2 activity while also being highly selective against BRD4 and other bromodomains, which could confound interpretation…

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