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PRMT1-Deg-4 | PRMT1-Deg-4 : Degrader (PROTAC) of PRMT1
RATINGS:
Cellular Use: (0 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
PRMT1
  • IC50:185.7 nM
  • DC50:770 nM
  • DC50:650 nM
  • DC50:520 nM
Degrader (PROTAC)
up to 5 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within family
Selectivity Assessment Description:
AlphaLISA enzymatic inhibition assays confrimed that Cpd 4 retained its potency as a pan inhibitor o ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family
Selectivity Assessment Description:
Selectivity for type I PRMT degradation, other I type PRMT proteins levels, including PRMT3, -4, -6, ...

Potency
Cellular
In Vitro

PRMT1

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5c03030

In Vivo Validations

Mouse
Dose: 20 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 7.03 h
Cmax: 1257 ng/mL
Tmax: 0.667 h
Area Under the Curve:: 5292 h*ng/mL

DOI Reference: 10.1021/acs.jmedchem.5c03030

Chemical Information

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References

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Expert Reviews

No SERP comments found for PRMT1-Deg-4

Probe PRMT1-Deg-4 is in the process of SERP review.

Please continue to check back for new reviews and commentary.