Lead optimization determines preclinical drug candidates and is the most rigorous segment in the small molecule drug development. Conventional lead optimization involves a four-step cycle of design, synthesis, testing, and analysis until the ideal candidate is obtained. Compared to the hit-to-lead phase, the design and optimization of this phase are more targeted. It needs to be optimized and improved for the aspects where lead is lacking, such as easily metabolized, toxic, and low in selectivity. In addition, it needs to retain the good biological activity and properties of the lead.
Ace Therapeutics provides lead optimization services for H. pylori small molecule drug development. Our lead optimization team is an integrated team of H. pylori experts, computer molecular simulation and design experts, chemists, and ADMET scientists. We can provide a meticulous design of screening funnels to obtain the most promising preclinical candidates. To help obtain successful H. pylori drug candidates, we not only optimize H. pylori lead from the perspective of conventional drugs but also fully consider the specificity of H. pylori drugs. The following is our service information and our unique advantages of optimizing small molecule drugs for H. pylori.
How our staff offer lead optimization services
A clear division of labor and cooperation makes us more efficient in lead optimization. In lead synthesis, our chemists have extensive experience in chemical synthesis and can handle the synthesis of various chemical molecules. In the lead testing phase, our ADMET scientists are skilled in ADMET testing and can efficiently perform testing with the help of advanced laboratory equipment. In the lead analysis and design phase, our H. pylori experts, chemists, and computer molecular simulation and design experts work together to further analyze testing results and redesign lead through 3D quantitative structure-activity relationships (3D-QSAR), 3D pharmacophore methods, and target-based structure design.
Part of our optimization tools
- Multiple sets of proven lead optimization solutions
- More than two screenings to evaluate primary potency and selectivity by using in vitro cell and enzyme assays
- Structure-activity relationship (SAR)-based design optimization
- In vivo studies in rodents infected or uninfected with H. pylori, including PK studies, PD studies, toxicity studies
- In vitro and in vivo assessment of off-target activity
- In vitro and in vivo assessment of drug metabolism
- Structure identification using nuclear magnetic resonance (NMR)
- Chemical synthesis support
- Automated purification systems
- Efficient synthesis of analogues
How we collaborate with our clients to achieve lead optimization
Overall, we work with the client at a high level of collaboration to complete the optimization of the lead. Once we know the background of the lead, we take the initiative to propose a reasonable solution and project progress strategy and interact with the client at each lead optimization stage to ensure that the client is aware of the progress of the lead optimization. In terms of payment, we offer a payment strategy based on the number of cycles of the lead optimization process.
Contact us
Ace Therapeutics has professional staff, skilled technical means, and a service process of multiple communication to provide efficient service for the optimization of H. pylori leads. If you have any questions about H. pylori lead optimization, please do not hesitate to contact us.
※ All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.
