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FS-694 | FS-694 : Inhibitor Type I½ of MAPK14
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MAPK14
  • IC50:0.2 nM
  • Kd:1.5 nM
  • IC50:14.9 nM Alpha; 16.9 nM Beta
Inhibitor
100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Off targets detected in DX screen inactive in cells

Potency
Cellular
In Vitro

MAPK14

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm301539x

Negative Control Compounds

FM-743
Notes: FM-743: IC50 MAPK14/MAPK11 = 11.3/ 16.2 µM (NanoBRET)

Orthogonal Probes def

Skepinone-L
SR-318
NEFLAMAPIMOD

Chemical Information

Molecular Formula C35H33FN4O4
SMILEs O=C(NCCN1CCOCC1)c1ccc2c(c1)C(=O)c1ccc(Nc3ccc(F)c(NC(=O)c4ccccc4)c3)cc1CC2
InChI InChI=1S/C35H33FN4O4/c36-31-13-11-28(22-32(31)39-35(43)24-4-2-1-3-5-24)38-27-10-12-29-25(20-27)8-6-23-7-9-26(21-30(23)33(29)41)34(42)37-14-15-40-16-18-44-19-17-40/h1-5,7,9-13,20-22,38H,6,8,14-19H2,(H,37,42)(H,39,43)
Molecular weight 592.25 Da
AlogP 5.2132
HBond acceptors 8
HBond donors 3
Atoms 77

Vendors

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Expert Reviews

by SERP
(on 24 Sept 2020 )
Cellular Use Rating
FS-694 is a dual active “type 1.5” inhibitor for P38-alpha (MAPK14) and P38-beta (MAPK11). Broad kinase selectivity at 1 µM shows that the compound is extremely selective. Off target activities include...
by SERP+
(on 23 May 2024 )
Cellular Use Rating
According to the literature, the compound is both an efficient probe for the target and has good qualities regarding the observed criteria (potency, selectivity, engagement etc.). However further assays,...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria