mPGES1-IN-3

mPGES1-IN-3 : Inhibitor of PTGES

Structure

SERP Rating

Probe mPGES1-IN-3 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

PTGES

Inhibitor

up to 5 uM

In Vitro Validations

Uniprot ID: O14684

Target Class: Enzyme

Target SubClass: Synthase

Potency: IC50

Potency Value: 8 nM

Potency Assay: mPGES-1 enzymatic assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Prostaglandin E synthase, PIG12, PGES, MPGES1, MGS ...

DOI Reference: 10.1016/j.bmcl.2016.10.079

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Profiled in a battery of in vitro and cellular assays to evaluate its selectivity over other prostanoid synthases, mPGES1-IN-3 demonstrated good selectivity (approximately > 1000 fold) over COX-1, COX-2, mPGES-2,cPGES, PGD2, PGI2, and TXA2 synthases. In CEREP safety screen-44 assay (binding assay), mPGES1-IN-3 inhibited benzodiazepine (BzD)-peripheral (63.2%@ 10 µM), A3 (80.2%@ 10 µM) and Clchannel (65%@ 10 µM) activity only. Moreover, mPGES1-IN-3 displayed low to moderate activity in the hERG channel (patch clamp assay, 17% and 46% inhibition at 1 and 10 µM test concentration).

I have extra information to add

SERP ratings and comments

No SERP comments found for mPGES1-IN-3