SGC707

Allosteric Inhibitor of PRMT3

Structure

Information

Protein target names: PRMT3

Mechanism of action: Allosteric Inhibitor

Recommended in-cell concentration:
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

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SERP Ratings

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(last updated: 10 Jun 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 6 Sept 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 25 Apr 2017 )

SERP Ratings

In Cell Rating
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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 )