@article {572831,
	title = {Screening for cell migration inhibitors via automated microscopy reveals a Rho-kinase inhibitor.},
	journal = {Chem Biol},
	volume = {12},
	number = {3},
	year = {2005},
	month = {2005 Mar},
	pages = {385-95},
	abstract = {Small-molecule kinase inhibitors are predominantly discovered in pure protein assays. We have discovered an inhibitor of Rho-kinase (ROCK) through an image-based, high-throughput screen of cell monolayer wound healing. Using automated microscopy, we screened a library of approximately 16,000 compounds finding many that affected cell migration or cell morphology as well as compounds that blocked mitotic progression. We tested approximately 200 compounds in a series of subassays and chose one, 3-(4-pyridyl)indole (Rockout), for more detailed characterization. Rockout inhibits blebbing and causes dissolution of actin stress fibers, phenocopying Rho-kinase inhibitors. Testing Rho-kinase activity in vitro, Rockout inhibits with an IC50 of 25 microM ( approximately 5-fold less potent than Y-27632) but has a similar specificity profile. We also profile the wound healing assay with a library of compounds with known bioactivities, revealing multiple pathways involved in the biology.},
	keywords = {Animals, BALB 3T3 Cells, Cell Movement, Dose-Response Relationship, Drug, Intracellular Signaling Peptides and Proteins, Mice, Microscopy, Confocal, Protein Kinase Inhibitors, Protein-Serine-Threonine Kinases, rho-Associated Kinases},
	issn = {1074-5521},
	doi = {10.1016/j.chembiol.2005.01.015},
	author = {Yarrow, Justin C and Totsukawa, Go and Charras, Guillaume T and Mitchison, Timothy J.}
}
