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Substituted Indoles as Selective Protease Activated Receptor 4 (PAR-4) Antagonists: Discovery and SAR of ML354

Substituted Indoles as Selective Protease Activated Receptor 4 (PAR-4) Antagonists: Discovery and SAR of ML354

Wandong Wen, Summer E Young, Matthew T Duvernay, Michael L Schulte, Kellie D Nance, Bruce J Melancon, Julie Engers, Charles W Locuson 2nd, Michael R Wood, J Scott Daniels, Wenjun Wu, Craig W Lindsley, Heidi E Hamm, etc.

Bioorg Med Chem Lett. 2014 Oct 1;24(19):4708-4713.

PMID: 25176330

Abstract:

Herein we report the discovery and SAR of an indole-based protease activated receptor-4 (PAR-4) antagonist scaffold derived from a similarity search of the Vanderbilt HTS collection, leading to MLPCN probe ML354 (VU0099704). Using a novel PAC-1 fluorescent αIIbβ3 activation assay this probe molecule antagonist was found to have an IC50 of 140nM for PAR-4 with 71-fold selectivity versus PAR-1 (PAR-1IC50=10μM).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP89159604	ML354		89159-60-4	Price

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