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IMP-1710 | Covalent Inhibitor of UCHL1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 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
UCHL1
  • IC50:38 nM
  • IC50:110 nM
100 nM - 1000 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Cross-screening against 20 DUBs demonstrated exquisite selectivity for IMP-1710 for UCHL1. Exquisite ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Selectivity across the proteome was assessed with nanoLC-MS/MS analysis showing marginal enrichment ...

Potency
Cellular
In Vitro

UCHL1

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? No

Negative Control Compounds

cpd 3

Chemical Information

Molecular Formula C23H19N5O
SMILEs C#Cc1cnc2[nH]cc(-c3cccc4c3CCN4C(=O)[C@@H]3CCCN3C#N)c2c1
InChI InChI=1S/C23H19N5O/c1-2-15-11-18-19(13-26-22(18)25-12-15)16-5-3-6-20-17(16)8-10-28(20)23(29)21-7-4-9-27(21)14-24/h1,3,5-6,11-13,21H,4,7-10H2,(H,25,26)/t21-/m0/s1
Molecular weight 381.16 Da
AlogP 3.0457800000000015
HBond acceptors 6
HBond donors 1
Atoms 48

References

Publications

Cross References

ChEMBL PubChem canSAR

Vendors

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Expert Reviews

by SERP
(on 21 Sept 2021)
Cellular Use Rating
This looks like a potent and selective inhibitor of UCHL1. There are still few things to keep in mind when using this compound: 1)The unbiased quantitative chemical proteomic profiling was conducted...
by SERP
(on 6 Oct 2021)
Cellular Use Rating
IMP-1711 (compound 3) is a well-characterized reversible covalent inhibitor of UCHL1 with excellent selectivity and high potency. The probe compound has demonstrated robust cellular target engagement...
by SERP
(on 11 Oct 2021)
Cellular Use Rating
I would recommend 100-200 nM for target engagement or proteomics analysis. Investigation of downstream effects in models such as IPF may need up to 1000 nM of this compound.
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