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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

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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 public comments)
by SERP
(on 25 Apr 2017)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public 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