BAY-9835

2D structure
Target ADAMTS7  ADAMTS12 
Targeted domain Protease domain
Mode of action Inhibitor
Control BAY-1880
Recommended cellular usage concentration 100 nM
In vivo use Yes
Donated by Bayer


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: Biochemical enzymatic assay IC50 [nM]: hADAMTS7: (6), mADAMTS7: (8), rADAMTS7: (27), hADAMTS12: (30 )
Selectivity within target family: > 30-fold Protease panel IC50 [µM]: hADAMTS4 (6.726), hADAMTS5 (9.924), hADAM8 (2.25), hADAM10 (32.802), hADAM17 (5.772), hMMP12 (5.376), hMMP15 (78.474), hMMP2, hMMP14, CAPN1 (Calpain 1), CASP3 (Caspase3), CTSB (Cathepsin B), CTSS (Cathepsin S), MALT1 all > 10 µM
Selectivity outside target family Eurofins Panlabs panel (77 targets) at 10 µM: clean
In-house kinase panel (12): all IC50 > 20 µM
On target cell activity for secreted targets Close analogue Cpd 29 significantly inhibits mADAMTS7 at 100 nM in Fibulin-3 cellular cleavage assay
Control compound (100 times less potent than the probe) BAY-1880: Biochemical enzymatic assay IC50: hADAMTS7 (23.4 µM), hADAMTS4 (> 50 µM); hADAMTS12 (n.d.)
In-house kinase panel (14): all IC50 > 20 µM