Functional cell-based uHTS in chemical genomic drug discovery |
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Authors: | Croston Glenn E |
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Institution: | ACADIA Pharmaceuticals, 3911 Sorrento Valley Blvd, San Diego, CA 92121, USA. gcroston@acadia-pharm.com |
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Abstract: | The availability of genomic information significantly increases the number of potential targets available for drug discovery, although the function of many targets and their relationship to disease is unknown. In a chemical genomic research approach, ultra-high throughput screening (uHTS) of genomic targets takes place early in the drug discovery process, before target validation. Target-selective modulators then provide drug leads and pharmacological research tools to validate target function. Effective implementation of a chemical genomic strategy requires assays that can perform uHTS for large numbers of genomic targets. Cell-based functional assays are capable of the uHTS throughput required for chemical genomic research, and their functional nature provides distinct advantages over ligand-binding assays in the identification of target-selective modulators. |
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