BAY-069

2D structure
Target BCAT1  BCAT2 
Targeted domain Substrate binding site
Mode of action Inhibitor
Control BAY-771
Recommended cellular usage concentration 1 µM
In vivo use Yes
Donated by Bayer


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: Biochemical assay: BCAT1 IC50 = 27 nM; BCAT2 IC50 = 130 nM
Selectivity within target family: > 30-fold Aspartate transaminase: GOT1 and GOT2: IC50 > 50 μM
Selectivity outside target family Clean panel (Tested 30 kinases, 30 proteases and 77 other targets). One off-target in PDSP scan: GABA/PBR (Ki = 74.19 nM)
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: Cellular mechanistic assay – BCAA measurement: U-87-MG (high BCAT1 expressing) cells: IC50 =358 nM; MDA-MB-231 (high BCAT2 expressing) cells: IC50 = 874 nM
Control compound (100 times less potent than the probe) BAY-771: Biochemical assay: BCAT1 IC50 = 6.5 µM; BCAT2 IC50 = 10.8 µM
Cellular mechanistic assay: U-87-MG (high BCAT1 expressing) cells: IC50 = 6.2 µM (17-fold)