Ace Therapeutics provides comprehensive anti-psychotic drug discovery services, and our lead optimization scientists work with our target identification, hit identification, and hit-to-lead teams to provide seamless solutions for our clients.

Introduction of Lead Discovery for Antipsychotics

After evaluation of different models and refinement of activity intensity criteria for antipsychotic leads obtained through activity screening, antipsychotic leads are identified by considering various factors such as the structure type and intellectual property of the compound, which is known as antipsychotic lead discovery. Antipsychotic leads are newly discovered compounds with well-defined pharmacological activities and chemical structures for specific targets and models. An antipsychotic lead may be a known compound, but its activity should be newly discovered. Certainly, the chemical structure of the antipsychotic lead should preferably be new. At this stage, more detailed ADME characterization and cytotoxicity testing of the antipsychotic leads should be performed.

Fig. 1 2D interactions of the lead compound with the receptor. (Olasupo SB, et al., 2021)

Lead Discovery Services

Ace Therapeutics provides our clients with exclusive solutions for antipsychotic lead discovery services through advanced technology. The goal of our antipsychotic lead discovery services is to optimize antipsychotic drugs with enhanced activity and selectivity, as well as appropriate pharmacokinetic properties, to a level that allows for in vivo animal testing. Our team combines experienced leadership and project scientists with a wide range of resources, such as parallel synthesis and purification, supported by our computational chemistry and in vitro ADME platforms. This combination of expertise and infrastructure allows for rapid multi-parameter scale-up and optimization of compound families. Our efficient research platform enables rapid, high-quality screening of antipsychotic drug leads with novel structures and high potency.

Antipsychotic Lead Discovery Service We Can Provide

• Optimization of antipsychotic hits based on DEL
• Structure-based compounds design
• Fragment library filtering
• Parallel synthesis of antipsychotic lead
• Rapid pharmacokinetic screening of multi-compound combinations
• Other antipsychotic lead discovery

Antipsychotic Lead Discovery Process

• Many potential compounds are screened to identify a large number of tightly bound compounds that lead to antipsychotic hits.
• These antipsychotic hits need to undergo rounds of rigorous screening to determine their suitability as antipsychotic leads (Figure 2).
• Biological activity studies of antipsychotic leads include biochemical assays, biophysical assays, and cellular assays.

Fig. 2 The process of antipsychotic lead discovery.

Ace Therapeutics has been conducting anti-psychotic drug development and lead discovery for many years. Our experts work diligently with a variety of clients in early-stage drug discovery programs. From inhibitor screening to the mechanism of action studies, we are committed to providing high-quality data to accelerate your project. If you are interested in this service, please make an inquiry to learn how we can support you in your project.

Reference

1. Olasupo SB, et al. Computer-aided drug design and in silico pharmacokinetics predictions of some potential antipsychotic agents. Scientific African. 2021, 12: e00734.