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BAY-3827

2D structure
Target PRKAA1  RPS6KA1 
Targeted domain Kinase domain (active site)
Mode of action Inhibitor (type 1, ATP competitive)
Control BAY-974
Recommended cellular usage concentration 150 nM
In vivo use No
Donated by Bayer


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd>/sub>) Surpasses criterion: High potency in biochemical PRKAA1 assay with IC50 = 1.4 nM @ 10 µM ATP; 15 nM @ 2 mM ATP (Bayer in house); IC50 = 7 nM (Eurofins @ 1 µM)
RPS6KA1(h): IC50 = 9.1 nM (Eurofins @ 1 µM)
Selectivity within target family: > 30-fold Surpasses criterion: Selectivity > 500 fold against 322 out of 329 off-kinases tested; Most potent off-kinases @ 1µM: RPS6KA3 (IC50 = 52 nM (Eurofins)), RPS6KA2 (IC50 = 24 nM (Eurofins)), RPS6KA6 (IC50 = 36 ± 8 nM (n=6, Bayer in house)), FLT3 (IC50 = 124 ± 140 nM (n=6, Bayer in house)), RPS6KA5 (IC50 = 43 nM (Eurofins)), MST3 (IC50 = 94 nM (Eurofins))
Selectivity outside target family Shows off-target activity in the PDSP scan: the closest hits are GABA/PBR (Ki = 222.4 nM) and DRD1 (Ki = 634.31 nM)
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: Active in cellular mechanistic assay (150 nM) demonstrating cellular target engagement
Additional proof for on target activity: ATP-competitive binding mode demonstrated (X-ray available)
Control compound (100 times less potent than the probe) Surpasses criterion: BAY-974 inactive (IC50 > 30 µM); Shows off-target activity in the PDSP scan for GABA/PBR (Ki = 20.99 nM) and TMEM97 (Ki =4470.95 nM)