8RK64

8RK64 : Covalent Inhibitor of UCHL1

Structure

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Probe 8RK64 is in the process of SERP review.

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Information

UCHL1

Covalent Inhibitor

up to 3 uM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P09936

Target Class: Enzyme

Target SubClass: Peptidase

Potency: IC50

Potency Value: 320 nM

Potency Assay: UCHL1 inhibition assay with Ub-Rho-morpholine as substrate Kinetic profile: kinact = 0.01382 1/s; KI(app) = 164 µM; kinact/KI = 84 * 1/(M*s)

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Ubiquitin carboxyl-terminal hydrolase isozyme L1, ...

DOI Reference: 10.1021/jacs.0c07726

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Within target family No inhibition within UCH family: UCHL3 (IC50 = 216 µM); UCHL5 (IC50 >> 200 µM) (Inhibition assay with Ub-Rho-morpholine as substrate) No inhibition of other deubiquitylating enzymes in activity‐based protein profiling assay (ABPP) experiment Outside target family: 2‐step labelling pull‐down proteomics experiment: One off-target identified in a 2‐step labelling pull‐down proteomics experiment: PARK7 (has a cystein in the active site)

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