The presentation covers a project based on in vivo phenotypic screening using SmartCube®, a state-of-the-art behavioral platform developed by PsychoGenics Inc. This platform provides signatures of molecules in mice allowing for the discovery of new potential treatments for psychiatric indications. It has been validated by &gt; 400 reference molecules or drugs commonly in use for psychiatric indications.<br/>SmartCube® was used as the starting point for an exploratory phenotypic screening approach in that we did not put any a priori biological constraints on screening candidates. Instead, the criteria for compound selection were CNS drug-like properties, manual selection by experienced CNS chemists, freedom to operate with respect to patentability and availability of sufficient high grade powder from our compound library.<br/>Testing for any behavioral activity in SmartCube® gave a hit rate of about 20% of compounds. One of these hits was identified as a starting point for a program based on its attractive in vivo profile in SmartCube® (antipsychotic-like without associated side-effects) and absence of effects on known targets for antipsychotics. From this hit, a lead compound was derived by using SmartCube® as the primary screen to further optimize for antipsychotic-like and pharmacokinetic properties.

<i>In vivo</i> phenotypic screening and optimization for antipsychotic drug candidates

251st National Meeting (2016)

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In vivo phenotypic screening and optimization for antipsychotic drug candidates