Menu

BAY-885

2D structure
Target MAPK7 
Targeted domain Kinase domain (active site)
Mode of action Inhibitor (type 1.5, ATP competitive)
Control BAY-693
Recommended cellular usage concentration 1 µM
In vivo use No
Donated by Bayer


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: MAPK7 inhibition (@ 250 μM ATP), IC50= 35 nM
Selectivity within target family: > 30-fold Surpasses criterion: Selectivity against Eurofins kinase panel at 1 μM (350 kinases were tested). Residual kinase activity below 50% reported for FER (h): 38%, EPHB3 (h): 42%, EPHA5 (h): 57%. For other kinases, residual activity reported ≥ 80%.
Selectivity outside target family Clean PDSP scan with one exception for SIGMAR1 (Ki = 2502.07 nM)
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: active in cellular mechanistic luciferase assay (IC50 =115 nM) demonstrating on-target cell activity
Control compound (100 times less potent than the probe) Surpasses criterion: BAY-693 with biochemical activity IC50 = 6.4 µM and cellular on target activity IC50 = 11 µM)
Clean PDSP scan with exception for SIGMAR1 (Ki = 2368.65 nM) and TMEM97 (Ki =4903.43 nM)