Abstract
We identified a new benzothiophene containing Rho kinase inhibitor scaffold in an ultra high-throughput enzymatic activity screen. SAR studies, driven by a novel label-free cellular impedance assay, were used to derive 39, which substantially reduced intraocular pressure in a monkey model of glaucoma-associated ocular hypertension.
Original language | English |
---|---|
Pages (from-to) | 3361-3366 |
Number of pages | 6 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 20 |
Issue number | 11 |
DOIs | |
State | Published - 1 Jun 2010 |
Keywords
- ATP competitive
- Adhesion
- Benzothiophene
- Glaucoma
- Impedance
- Inhibitor
- Kinase
- ROCK
- Rho