Hit-to-Lead & Lead Optimization

Our highly skilled and experienced medicinal chemists make use of a hypothesis-driven multiparameter approach to lead optimization. This involves effective compound design making use of computational chemistry techniques in concert with detailed structure-activity relationship (SAR) data analysis, allied to rapid compound preparation utilizing parallel and accelerated organic synthesis, microwave chemistry and design of experiments methodology.

Hit-to-lead projects are conducted in a rigorous and fast manner, involving hit-confirmation and validation followed by extensive SAR exploration to provide robust lead series. These compound series are then taken forward through the process of rational lead optimization to improve potency, selectivity and ADMET properties to satisfy predefined criteria for a candidate drug to be progressed into development.

Through our hit-to-lead and lead optimization activities, Evotec's medicinal chemists ensure that compounds are designed to answer questions and are made rapidly for biological testing in order to provide new data to help direct the next round of optimization.