IC50: 140 nM

ML-354 is an indole-based, proteinase-activated receptor (PAR) 4 antagonist with good potency and reasonable selectivity versus PAR1. PARs are a family of four G-protein-coupled receptors GPCRs (PAR1-PAR4) with several unique attributes, which are activated by serine proteases. The activation of PARs needs a unique mechanism which requiring proteolysis unmasking their extracellular N-terminal domain. PAR4 is a thrombin receptor found on human platelets and represents a potential therapeutic target for the treatment of thrombotic disorders [1].

In vitro: Up to now, in vitro study of ML-354 is still in the development stage.

In vivo: Up to now, in vivo study of ML-354 is still in the development stage.

Reference:
[1].  Wen, W., Young, S., Duvernay, M., Schulte, M., Nance, K., & Melancon, B. et al. Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354. Bioorganic & Medicinal Chemistry Letters. 2014; 24(19): 4708-4713.