Abstract

Screening throughput is an important requirement in the early phases of a drug discovery program because it determines the ability to evaluate a large number of compounds and, thereby, the discovery of new pharmaceuticals. The dominant drug discovery paradigm for synthetic drugs is the mechanism-based screening using in-vitro tests for the lead identification. This approach is a superior strategy for well-validated targets with defined mechanism of action, but has limitations for the development of symptomatic treatments in indications with an unclear or multifactorial aetiology. In this cases a screening approach, based on biological efficacy in a disease model, seems to be more rewarding because it can identify compounds with novel or unknown modes of action. However, the limitation of this strategy is the low screening capacity because most of the disease models are time consuming in-vivo tests.

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