Drug intelligence / Profile preview

compound 39 (Davis et al., 2010)

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Ophthalmic
01

Overview

Compound 39 is a small molecule Rho-associated kinase (ROCK) inhibitor characterized by a benzothiophene scaffold. It was identified through an ultra high-throughput enzymatic activity screen and optimized via structure-activity relationship (SAR) studies at the 2- and 5-positions of the benzothiophene scaffold. The compound targets both ROCK1 and ROCK2 isoforms. In preclinical research, specifically a monkey model of glaucoma-associated ocular hypertension, Compound 39 demonstrated the ability to substantially reduce intraocular pressure. Its mechanism of action involves increasing aqueous humor outflow through the trabecular meshwork, making it a potential therapeutic candidate for the treatment of glaucoma.

Other names
Benzothiophene-based ROCK inhibitor 39Benzothiophene-based ROCK inhibitor 39-Rho-associated kinase-Small molecule-Glaucoma
02

Targets

ROCK1 (Rho-associated coiled-coil containing protein kinase 1)ROCK2 (Rho-associated coiled-coil containing protein kinase 2)

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