SGC707

Allosteric Inhibitor of PRMT3

Structure

SERP Rating

In Cells

(4 ratings)

In Model Organisms

(3 ratings)

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.

Information

Protein target names: PRMT3

Mechanism of action: Allosteric Inhibitor

Recommended in-cell concentration:

10 nM - 10 uM

Primary References:

DOI - 10.1002/anie.201412154

Probe Availability:

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 and comments

SERP Ratings

In Cell Rating

(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

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 )