Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma.
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Davis RL, Kahraman M, Prins TJ, Beaver Y, Cook TG, Cramp J, Cayanan CS, Gardiner EM, McLaughlin MA, Clark AF, Hellberg MR, Shiau AK, Noble SA, Borchardt AJ
Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma.
Bioorg Med Chem Lett. 2010 Jun 1;20(11):3361-6. doi: 10.1016/j.bmcl.2010.04.020. Epub 2010 Apr 11.
- PubMed ID
- 20434334 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) (S)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLINE)SULFONYL]-HOMOPIPERAZINE Rho-associated protein kinase 1 IC 50 (nM) 30 N/A N/A Details