Ace Therapeutics is committed to helping our clients accurately identify and validate psychiatric disease-related targets to ensure successful downstream drug development. Our phenotype-directed target identification and validation technology allows for the direct matching of genetic variants to disease phenotypes, thereby reducing the risk of early failure.

Introduction of Hit Discovery for Antipsychotics

Material preparation for the creation of new antipsychotic drugs begins with the discovery of antipsychotic drug hits. Antipsychotic drug hits are compounds with initial activity against a specific target or link of action. There are many approaches to discovering antipsychotic drugs, mainly random screening methods (natural product and high-throughput screening compound libraries) and rational approaches (molecular design based on the receptor or ligand structure and mechanism). Fragment-based screening, which is also a combination of instrumental analysis and molecular simulation in recent years, is an effective way to discover antipsychotic drugs and evolve into antipsychotic drug leads.

Fig. 1 Lead classes (bottom) originated and developed from screening hits (top) against β-site amyloid precursor protein cleaving enzyme 1. (Keserü G, et al., 2009)

Hit Discovery Services

Ace Therapeutics has extensive experience in antipsychotic drug discovery and provides such services to some pharmaceutical and biotechnology companies and academic institutions. It is well known that the discovery of effective antipsychotics from target to target is expected to greatly accelerate the process of discovering new antipsychotics. We build on this foundation with attentive service and comprehensive data to provide you with exclusive antipsychotic hit discovery service solutions and the most forward-looking studies.

The antipsychotic hit should meet the following criteria:

• The binding strength of the antipsychotic drug to the target is not less than 10μmol/L.
• Have a certain water solubility, solubility is not less than 10μg/mL.
• It can traverse the cell membrane.
• It can show biological activity at the cellular level.
• It has no cytotoxic.
• It has chemical stability.
• It can be prepared.

Our Hit Discovery Capabilities

• High-throughput screening
• High content screening
• Fragment screening
• Virtual screening
• Artificial Intelligence for difficult targets
• Medicinal chemistry knowledge-based design
• Therapeutic antibody discovery

Antipsychotic Hit Discovery Service We Can Provide

• DNA-encoded library (DEL) screening
• Virtual screening
• Fragment-based antipsychotic hit discovery
• Other antipsychotic hit discovery

Antipsychotic Hit Discovery Process

• Initial screening of antipsychotic drugs was performed using the following technical platforms (Figure 2)
• Confirmation phase testing of psychotropic drugs, including the exclusion of potentially reactive compounds, interference assays or self-aggregation, repeated activity assays, dose-response curve determination, homologous structure-activity relationship studies, target binding reversibility studies, and orthogonal assays.
• Conduct biofunctional assays (agonist/antagonist) or cellular assays to confirm the activity of antipsychotic drugs and perform secondary screening.
• Evaluate the effectiveness and intellectual property of antipsychotic drugs.

Fig. 2 Initial screening of antipsychotic hit discovery process.

Ace Therapeutics has a team experienced in drug development for psychiatric disorders. We regularly evaluate early-stage projects and will advise you on the best drug discovery screening strategy to help you successfully advance to lead studies. If you are interested in this service, please make an inquiry to learn how we can support you in your project.

Reference

1. Keserü G, et al. The influence of lead discovery strategies on the properties of drug candidates. Nature Reviews Drug Discovery. 2009, 8: 203-212.