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SGC707 | SGC707 : Allosteric inhibitor of PRMT3
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (2 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
PRMT3
  • Kd:53 nM
  • Kd:85n M
  • IC50:31 nM
  • IC50:66 nM
  • EC50:1300 nM
Allosteric
10 nM - 10 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selective for PRMT3 over 31 DNA, RNA and protein methyltransferases.
Selectivity Assessment Description:
Selective for PRMT3 over 250 kinases, GPCRs, ion channels and transporters. Modest off-target act ...

Potency
Cellular
In Vitro

PRMT3

Mode of Action: Allosteric

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1002/anie.201412154

In Vivo Validations

Mouse
Dose: 30 mg/mL
Route of delivery: Intraperitoneal

DOI Reference: 10.1002/anie.201412154

Negative Control Compounds

XY1

Orthogonal Probes def

MS023

Chemical Information

Molecular Formula C16H18N4O2
SMILEs O=C(NCC(=O)N1CCCC1)Nc1ccc2cnccc2c1
InChI InChI=1S/C16H18N4O2/c21-15(20-7-1-2-8-20)11-18-16(22)19-14-4-3-13-10-17-6-5-12(13)9-14/h3-6,9-10H,1-2,7-8,11H2,(H2,18,19,22)
Molecular weight 298.14 Da
AlogP 1.9786999999999995
HBond acceptors 6
HBond donors 2
Atoms 40

References

Publications

Cross References

Vendors

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Expert Reviews

by SERP
(on 10 Jun 2016 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 25 Apr 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 27 Apr 2017 )
Cellular Use Rating
In Model Organisms
SGC707 displays excellent biochemical inhibition, with promising target selectivity. Cellular potency values were ranging and assay-dependent, but support use at 1-10 uM doses. The offset observed between...
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