Chemical Probes logo
SR-302 | SR-302 : Inhibitor of DDR1, DDR2, MAPK11, MAPK14
RATINGS:
Cellular Use: (1 reviews)

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

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
DDR1
  • IC50:53.3 nM
  • IC50:23 nM
DDR2
  • IC50:0.75 nM
  • IC50:18 nM
MAPK11
  • IC50:45.1 nM
  • IC50:196 nM
MAPK14
  • IC50:6.2 nM
  • IC50:125 nM
Inhibitor
100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Closest off-targets found in KinomeScan: ABL1, RIPK2, RPS6KA5, CHEK2, STK38L; for all IC50 > 25 µM ( ...

Potency
Cellular
In Vitro

DDR1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.1c00868

DDR2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.1c00868

MAPK11

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.1c00868

MAPK14

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.1c00868

Negative Control Compounds

SR-301
Notes: https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c00868

Orthogonal Probes def

Skepinone-L

Chemical Information

Molecular Formula C32H42N6O5S
SMILEs CS(=O)(=O)N1CCCC(NC(=O)[C@H](CCC2CCCCC2)NC(=O)c2ccc(CNC(=O)c3cnc4ccccn34)cc2)C1
InChI InChI=1S/C32H42N6O5S/c1-44(42,43)37-18-7-10-26(22-37)35-31(40)27(17-14-23-8-3-2-4-9-23)36-30(39)25-15-12-24(13-16-25)20-34-32(41)28-21-33-29-11-5-6-19-38(28)29/h5-6,11-13,15-16,19,21,23,26-27H,2-4,7-10,14,17-18,20,22H2,1H3,(H,34,41)(H,35,40)(H,36,39)/t26?,27-/m0/s1
Molecular weight 622.29 Da
AlogP 3.2634000000000016
HBond acceptors 11
HBond donors 3
Atoms 86

Expert Reviews

by SERP+
(on 17 Jun 2024 )
Cellular Use Rating
SR-302 shows good potency for DDR1 and DDR2 in vitro determined by enyzme kinetic assay (IC50 = 53.3 nM and IC50 = 0.75 nM). Activity in cells was investigated via NanoBRET which delivered IC50 = 23 nM...
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