fbpx

molecules of the month

compound 28

potent MAT2A inhibitor in vivo tool

efficacy in MTAP-mut. xenograft (50 mpk SC)

from fragment-based DD (frag. merging)

J. Med. Chem., Apr. 26, 2021

AstraZeneca, Cambridge, UK

compound-28
1 min read

The AstraZeneca MAT2a allosteric inhibitor, compound 28, is a remarkably potent (25 nM in cells) in vivo tool compound generated from merging of two weak fragments (Kd = 250 μM and 6.2 μM). The molecule binds in the same site as AG-270 (above) and has a relatively uncommon quinazolinone core, which makes several polar interactions in the binding site. The identification of this highly efficient inhibitor is a great case study for fragment-based lead generation.


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: