molecules of the month


oral BCAT1/2 inhibitor

favorable PK profile in rats

from 788762 cmpd. HTS and SBDD

J. Med. Chem.

Bayer Pharma AG, Berlin, DE

BAY-069 chemical structure oral BCAT1/2 inhibitor - Bayer Pharma AG, Berlin, DE
4 mins read

Context. BAY-069 (Bayer) is a branched-chain amino acid transaminase (BCAT) 1/2 inhibitor. Involved in the synthesis and breakdown of branched-chain amino acids, BCAT1 and BCAT2 have also been implicated in several diseases, including various cancer types, with the ligandability evidenced by the many reported inhibitors. Tool compound BAY-069, a (trifluoromethyl)pyrimidinedione identified in an HTS campaign, is a BCAT1-focused dual BCAT1/2 inhibitor with IC50 values of 31 nM for BCAT1 and 153 nM for BCAT2. Donated by BI as a chemical probe along with an inactive control, it may be helpful to further understand BCAT biology and safety in different settings. The molecule is an interesting example of an oral molecule with an N2-substituted pyrimidinedione. Target. BCATs mediate the catabolism of…

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