Abstract
The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC50 of ∼3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacology studies showed that 5 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation.
Original language | English (US) |
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Pages (from-to) | 6642-6645 |
Number of pages | 4 |
Journal | Journal of Medicinal Chemistry |
Volume | 51 |
Issue number | 21 |
DOIs | |
State | Published - Nov 13 2008 |
Externally published | Yes |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery