Chemical Probes logo
EI1 | EI1 : SAM competitive inhibitor of EZH2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
EZH2
  • Ki:13 nM
  • IC50:15 nM
  • IC50:13 nM
SAM competitive
Up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
EI1 is 90-fold selective for EZH2 over EZH1 and >10,000-fold selective for the remainder of protein ...
Selectivity Assessment Description:
Not available

Potency
Cellular
In Vitro

EZH2

Mode of Action: SAM competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1073/pnas.1210371110

Orthogonal Probes def

GSK343
CPI-360
EPZ-6438

Chemical Information

Molecular Formula C23H26N4O2
SMILEs CCC(CC)n1ccc2c(C(=O)NCc3c(C)cc(C)[nH]c3=O)cc(C#N)cc21
InChI InChI=1S/C23H26N4O2/c1-5-17(6-2)27-8-7-18-19(10-16(12-24)11-21(18)27)22(28)25-13-20-14(3)9-15(4)26-23(20)29/h7-11,17H,5-6,13H2,1-4H3,(H,25,28)(H,26,29)
Molecular weight 390.21 Da
AlogP 4.109220000000002
HBond acceptors 6
HBond donors 2
Atoms 55

References

Publications

Cross References

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 9 Sept 2016 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 9 Sept 2016 )
Cellular Use Rating
In Model Organisms
El1 is a promising inhibitor with good potency as a SAM competitive inhibitor against EZH2 at 13 nM. El1 was obtained from an initial high-throughput screen to identify the chemotype with the best properties....
by SERP
(on 10 Dec 2016 )
Cellular Use Rating
In Model Organisms
Cell-based activity is oberved at 3.3 uM.
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