Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma.

Article Details

Citation

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
DrugTargetPropertyMeasurementpHTemperature (°C)
(S)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLINE)SULFONYL]-HOMOPIPERAZINERho-associated protein kinase 1IC 50 (nM)30N/AN/ADetails