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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 public 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