MK-7246

Antagonist of PTGDR2

Structure

SERP Rating

Probe MK-7246 is in the process of SERP review.

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Information

PTGDR2

Antagonist

100 nM, up to 1 uM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: Q9Y5Y4

Target Class: GPCR

Target SubClass: Prostaglandin D2 receptor

Potency: Ki

Potency Value: 2.5 nM

Potency Assay: Prostanoid receptor binding assay (PTGDR2)

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

Target aliases:

Prostaglandin D2 receptor 2, GPR44, DL1R, CRTH2, P ...

DOI Reference: 10.1016/j.bmcl.2010.11.015

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

> 100-fold against related receptors; Hits in the GPCR scan are SLC6A3 (Ki = 283 nM), GABA/PBR (Ki = 1115 nM) and DRD2 (Ki = 3746 nM); Prostanoid receptor binding assay: TBXA2R (Ki = 3804 nM)

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SERP ratings and comments

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