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SGC707

Allosteric Inhibitor of PRMT3

Structure

Information

  • PRMT3
  • Allosteric Inhibitor
  • 10 nM - 10 uM

In Vitro Validations

Uniprot ID: O60678
Target Class: Epigenetic
Target SubClass: Protein methyltransferase
Potency: Kd
Potency Value: 53 nM
Potency Assay: ITC
PDB ID for probe-target interaction (3D structure): 4RYL
Structure-activity relationship: Yes
Target aliases:
Protein arginine N-methyltransferase 3, HRMT1L3, P ...

DOI Reference: 10.1002/anie.201412154

Uniprot ID: O60678
Target Class: Epigenetic
Target SubClass: Protein methyltransferase
Potency: Kd
Potency Value: 85n M
Potency Assay: SPR
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Protein arginine N-methyltransferase 3, HRMT1L3, P ...

DOI Reference: 10.1002/anie.201412154

Uniprot ID: O60678
Target Class: Epigenetic
Target SubClass: Protein methyltransferase
Potency: IC50
Potency Value: 31 nM
Potency Assay: Scintillation proximity assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Protein arginine N-methyltransferase 3, HRMT1L3, P ...

DOI Reference: 10.1002/anie.201412154

Uniprot ID: O60678
Target Class: Epigenetic
Target SubClass: Protein methyltransferase
Potency: IC50
Potency Value: 66 nM
Potency Assay: LC-MS detection assay under balanced conditions.
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Protein arginine N-methyltransferase 3, HRMT1L3, P ...

DOI Reference: 10.1002/anie.201412154

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selective for PRMT3 over 31 DNA, RNA and protein methyltransferases.
Probe Selectivity in Vitro:

Selective for PRMT3 over 250 kinases, GPCRs, ion channels and transporters. Modest off-target activity was noted at 10,000 nM SGC707: 69% inhibition of HTR2B (Ki > 15,000 nM); 56% inhibition of BRSK1; 60% inhibition of DLK1; 55% inhibition of RPS6KA4; 58% inhibition of PRKG2, and 61% inhibition of PRKX.

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SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 10 Jun 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 25 Apr 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

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 biochemical and cellular potency should be further explored.

(last updated: 27 Apr 2017 )