Chemical Probes logo
PRMT1-Deg-4 | PRMT1-Deg-4 : Degrader (PROTAC) of PRMT1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PRMT1
  • IC50:185.7 nM
  • DC50:770 nM
  • DC50:650 nM
  • DC50:520 nM
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

Molecular Formula C43H56N6O6
SMILEs CNCCN(C)Cc1ccccc1Oc1ccc(C(=O)NCCCCCCCCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)cc1
InChI InChI=1S/C43H56N6O6/c1-44-28-29-48(2)30-32-16-11-12-19-37(32)55-33-22-20-31(21-23-33)40(51)46-27-14-10-8-6-4-3-5-7-9-13-26-45-35-18-15-17-34-39(35)43(54)49(42(34)53)36-24-25-38(50)47-41(36)52/h11-12,15-23,36,44-45H,3-10,13-14,24-30H2,1-2H3,(H,46,51)(H,47,50,52)
Molecular weight 752.43 Da
AlogP 6.274200000000006
HBond acceptors 12
HBond donors 4
Atoms 111

References

Publications

Cross References

canSAR: 7719226 canSAR: 32

Expert Reviews

by SERP
(on 14 Apr 2026)
Cellular Use Rating
This compound should be considered as a weak, slow degrader of PRMT1. No negative controls are shown, either which do not bind E3 or PRMT1 and it is difficult to be certain that effects are driven via...
by SERP
(on 25 Jun 2026)
Cellular Use Rating
In Model Organisms
This compound was shown to induce the degradation of PRMT1 with a reasonable DC50 and selectively over other type I PRMT proteins in cellular models. Pharmacokinetic studies suggest it could be used in...
If you would like to explore AI-generated evaluations, you may wish to visit the page for this compound on our collaborator website
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