Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.
Article Details
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Wu F, Buttner FH, Chen R, Hickey E, Jakes S, Kaplita P, Kashem MA, Kerr S, Kugler S, Paw Z, Prokopowicz A, Shih CK, Snow R, Young E, Cywin CL
Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.
Bioorg Med Chem Lett. 2010 Jun 1;20(11):3235-9. doi: 10.1016/j.bmcl.2010.04.070. Epub 2010 Apr 22.
- PubMed ID
- 20462760 [ View in PubMed]
- Abstract
Two closely related scaffolds were identified through an uHTS campaign as desirable starting points for the development of Rho-Kinase (ROCK) inhibitors. Here, we describe our hit-to-lead evaluation process which culminated in the rapid discovery of potent leads such as 22 which successfully demonstrated an early in vivo proof of concept for anti-hypertensive activity.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Fasudil Rho-associated protein kinase 1 IC 50 (nM) 660 N/A N/A Details