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8RK64 | 8RK64 : Covalent Inhibitor of UCHL1
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
UCHL1
  • IC50:320 nM
Covalent Inhibitor
up to 3 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Within target family No inhibition within UCH family: UCHL3 (IC50 = 216 µM); UCHL5 (IC50 >> 200 µM) ...

Potency
Cellular
In Vitro

UCHL1

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jacs.0c07726

In Vivo Validations

Zebrafish embryos
Dose: 5 uM

DOI Reference: 10.1021/jacs.0c07726

Negative Control Compounds

JYQ88
Notes: JYQ88: UCHL1 inhibition assay with Ub-Rho-morpholine as substrate: IC50 = 12.9 µM (45 times less potent); No UCHL1 inhibition observed in ABPP experiment. Binds much better to PARK7 compared to 8RK64. Clean GPCR scan.

Chemical Information

Molecular Formula C14H16N8O2S
SMILEs N#CN1CC[C@H](C(=O)Nc2nc3c(s2)CN(C(=O)CN=[N+]=[N-])CC3)C1
InChI InChI=1S/C14H16N8O2S/c15-8-21-3-1-9(6-21)13(24)19-14-18-10-2-4-22(7-11(10)25-14)12(23)5-17-20-16/h9H,1-7H2,(H,18,19,24)/t9-/m0/s1
Molecular weight 360.11 Da
AlogP 0.0
HBond acceptors 10
HBond donors 1
Atoms 41
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

Expert Reviews

No SERP comments found for 8RK64

Probe 8RK64 is in the process of SERP review.

Please continue to check back for new reviews and commentary.