CK156 | CK156 : Inhibitor of STK17A
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 reviews)
In Vivo
Vendors

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
STK17A
  • IC50:49 nM
  • Kd:21 nM
  • IC50:181 nM
Inhibitor
up to 5 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
The selectivity profile of CK156 was determined with the scanMAX® assay from DiscoverX at 1000 and 1 ...

Potency
Cellular
In Vitro

STK17A

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.2c00173

Negative Control Compounds

CANSAR3550543
Notes: The negative control CKJB71 showed no activity in a DSF assay for 90 kinases and no on-target activity determined by NanoBRET in intact cells and in lysed cells.

Chemical Information

Molecular Formula C21H25N5O3
SMILEs CC(C)(C)NC(=O)c1ccc2cc1OCCOCCNc1ccn3ncc-2c3n1
InChI InChI=1S/C21H25N5O3/c1-21(2,3)25-20(27)15-5-4-14-12-17(15)29-11-10-28-9-7-22-18-6-8-26-19(24-18)16(14)13-23-26/h4-6,8,12-13H,7,9-11H2,1-3H3,(H,22,24)(H,25,27)
Molecular weight 395.20 Da
AlogP 0.0
HBond acceptors 8
HBond donors 2
Atoms 54

Expert Reviews


(on 17 Jun 2024 )
Cellular Use Rating
This is a compound with good in vitro potency Kd = 21 nM (ITC) and IC50 of 49 nM (33PanQuinase), good cellular potency with IC50 of 182 nM and very good selectivity, tested 468 kinases as off-targets....
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