Lead Optimization for Antipsychotics
Ace Therapeutics provides Lead Optimization services for antipsychotic diseases. We have highly trained medicinal chemists and many years of experience in antipsychotic discovery. We can consistently deliver high-quality drug candidates for investigational new drug studies in the shortest possible time. Our clients use our knowledge and capabilities to accelerate their drug discovery programs.
Introduction of Lead Optimization for Antipsychotics
In order to solve the problems of low strength or specificity of action, inappropriate pharmacokinetic properties, high toxic side effects, or chemical and metabolic instability, chemical modification and embellishment of the structures of antipsychotic leads to optimize their physicochemical and biological activities are required. Based on the discovered molecular structures of antipsychotic leads, a series of compounds were prepared based on the principle of similarity and evaluated for their antipsychotic activity, absorption, and structure-activity relationship (SAR).
Lead Optimization Services
Ace Therapeutics provides clients with exclusive antipsychotic lead optimization service solutions based on cutting-edge science. The goal of antipsychotic lead optimization is to generate one or more preclinical antipsychotic candidates. During this phase, we can do the following studies and balance various attributes: efficacy, toxicity, PK/PD, metabolic profile, and chemical stability. Compounds entering the lead optimization phase are evaluated by our integrated team and a strategy is designed to optimize their properties. Involving in vitro and in vivo evaluation of lead properties, the team uses our collaborative approach to ensure full alignment and prioritize or deprioritize lead families as needed.
Antipsychotic Lead Optimization Services We Can Provide
- Binding pattern prediction
- Scaffold hopping
- Binding affinity optimization
- Conformational stability assessment
- Other antipsychotic lead optimization
Antipsychotic Lead Optimization Research Technique
| Antipsychotic lead optimization research technique |
Particulars |
| Conventional optimization method |
Structure optimizations including splitting and splicing to generate twins. |
| Local modifications include switching rings, homologues transformation, the introduction of ene bonds or large groups, change of group electrical properties, etc. |
| Replacement of biological isoplatoon of bioelectrons |
Molecules or groups with similar physical or chemical properties and similar biological activities due to the same number or arrangement of peripheral electrons are called "biological electron isoplatoon". |
| Prodrug design |
The use of prodrug principles in antipsychotic design leads to improvements in the pharmacokinetic properties of antipsychotic leads, but generally doesn't increase their activity. |
| Soft drug design |
The soft drug design approach can reduce the side effects of antipsychotics that accumulate in the body. |
| Quantitative structure and activity relationship (QSAR) |
Research quantitatively the interaction between antipsychotic leads and biomacromolecules as well as their physiological properties such as absorption, distribution, metabolism, and excretion in organisms. |
| Computer-aided antipsychotic drug design |
Accelerating the design of new psychiatrics. |
A Partial List of Guided Lead Optimization Studies
- Target engagement in vitro
- Selectivity profiling and optimization
- Potency distribution showing structure-activity relationship (SAR)
- Solubility profiling and optimization
- Metabolic liabilities profile
- Human plasma protein binding ≤ 99%
- CYP450 inhibition
Ace Therapeutics has many years of laboratory experience and scientific expertise in the field of antipsychotic drug development. Partnering with us can set your program apart from the competition. Our industry-leading lead optimization solutions can increase your likelihood of success while minimizing cost and cycle time. Advance your most promising anti-psychotic compounds and experience cost-effective insights with our late-stage discovery and lead compound optimization services. Please feel free to make an inquiry to learn how we can translate your small and large molecules into preclinical candidates and ultimately into therapeutic agents.
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