The present invention provides novel chemical compounds characterized as Rhokinase (ROCK) inhibitors, methods for their discovery, and their therapeutic,research, anddiagnostic use. In particular, the present invention provides 1,4-benzodiazepine-2,5-dionecompounds and related compounds having ROCK inhibitory activity, and methodsof usingsuch compounds as therapeutic agents to treat a number of conditionsassociated with ROCKactivity. Representative compounds of this invention have a structure as shownin thefollowing formula.(see above formula)