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UNC1215 | UNC1215 : Inhibitor 2:2 dimer formation of L3MBTL3
RATINGS:
Cellular Use: (3 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
L3MBTL3
  • Kd:120 nM
  • IC50:40 nM
  • EC50:50-100 nM
2:2 dimer formation
100 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - L3MBTL1 2 uM

Potency Assay Off-Target:
UNC1215 is >50-fold selective for L3MBtL3 in an alpha screen against Kme readers proteins. No activi ...
Selectivity Assessment Description:
In an array of 250 chromatin-associated effector proteins (Cador 5.0), UNC1215 bound to 6 protein ...

Potency
Cellular
In Vitro

L3MBTL3

Mode of Action: 2:2 dimer formation

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.1157

Negative Control Compounds

UNC1079

Chemical Information

Molecular Formula C32H43N5O2
SMILEs O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1
InChI InChI=1S/C32H43N5O2/c38-31(36-20-12-27(13-21-36)34-16-4-5-17-34)25-10-11-29(30(24-25)33-26-8-2-1-3-9-26)32(39)37-22-14-28(15-23-37)35-18-6-7-19-35/h1-3,8-11,24,27-28,33H,4-7,12-23H2
Molecular weight 529.34 Da
AlogP 4.831
HBond acceptors 7
HBond donors 1
Atoms 82

Vendors

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Expert Reviews

by SERP
(on 14 Jun 2016 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 22 Jun 2016 )
Cellular Use Rating
This probe seems to have a very nice selectivity towards L3MBTL3. UNC1215 is nontoxic at concentration well above the EC50.
by SERP
(on 23 Jun 2016 )
Cellular Use Rating
In Model Organisms
As of June 2016, this is the first and only potent and selective inhibitor of L3MBTL3 with activity in cells. This looks like a good compound to probe this target's disease relevance and biology. The...
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