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A-446

2D structure
Target GLS 
Targeted domain Allosteric site at the dimer‐dimer interface
Mode of action Inhibitor
Control A-426
Recommended cellular usage concentration 100 nM
In vivo use Yes
Donated by Abbvie


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: GAC (GLS) Enzyme activity assay: IC50 = 31 nM
Selectivity within target family: > 30-fold GLS2 Enzyme activity assay: : IC50 > 30 µM (>1000-fold selectivity)
Selectivity outside target family Probe selectivity observed in Proteome Integral Stability Assay. Closest off-targets in Cerep binding assay at 10 μM (percent inhibition of control specific binding): ADORA3 ( agonist radioligand) 76.6 %, CHRM1 (antagonist radioligand) 92.6 %, CHRM2 (antagonist radioligand) 71.5 %
Clean PDSP scan data (44 targets) at 10 µM except for HTR1D (Ki = 6453.57 nM)
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: CTG assay in A549 cells IC50 = 11 nM
Control compound (100 times less potent than the probe) A-426: GAC (GLS) Enzyme activity assay: : IC50 > 30 µM (> 100-fold less active); GLS2 Enzyme activity assay: : IC50 > 30 µM