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SR-318 | Inhibitor of MAPK14, MAPK11
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (1 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
  • IC50:5 nM
  • IC50:3.7 nM
MAPK11
  • IC50:32 nM
  • IC50:10 nM
Inhibitor
< 100 nM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
NanoBRET
Selectivity Assessment Description:
Closest off-targets found in KinomeScan: DDR1/2, KIT, ZAK, RSK4, MYLK4 show &gt; 200-fold selecti ...

Potency
Cellular
In Vitro

MAPK14

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.9b01227

MAPK11

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.9b01227

Negative Control Compounds

SR-321
Notes: SR-321: IC50 MAPK14 = 13 µM and MAPK11 = 11 µM (NanoBRET), DDR2: IC50 = 220 nM (NanoBRET), but no other kinase activity. Clean GPCR scan except for one off-target: TMEM97 Ki =2887.53 nM

Orthogonal Probes def

Skepinone-L
NEFLAMAPIMOD
FS-694

Chemical Information

Molecular Formula C27H33N5O2
SMILEs Nc1c(C(=O)NCc2ccc(C(=O)NCCCC3CCCCC3)cc2)cnn1-c1ccccc1
InChI InChI=1S/C27H33N5O2/c28-25-24(19-31-32(25)23-11-5-2-6-12-23)27(34)30-18-21-13-15-22(16-14-21)26(33)29-17-7-10-20-8-3-1-4-9-20/h2,5-6,11-16,19-20H,1,3-4,7-10,17-18,28H2,(H,29,33)(H,30,34)
Molecular weight 459.26 Da
AlogP 4.474800000000004
HBond acceptors 7
HBond donors 4
Atoms 67

References

Publications

Cross References

SGC additional analysis

Vendors

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Expert Reviews

by SERP
(on 2 Jun 2020 )
Cellular Use Rating
In Model Organisms
SR-318 displays exquisite selectivity for p38a/b vs other kinases. At 100nM, 90% p38a/b inhibition is observed in cells using NanoBRET while other kinases are basically uninhibited at this concentration....
by SERP
(on 20 Feb 2025 )
Cellular Use Rating
SR-318 is a potent and selective inhibitor of p38α/β. In a cellular NanoBret assay, the probe showed >90% inhibition at 100 nM. For in vivo use the half-life of 2.5 h in human liver microsomes should be...
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