Medicilon’s Lead Optimization in Drug Discovery

Medicilon’s medicinal chemistry involves the application of a number of specialized disciplinary approaches all focused on the ultimate goal of drug discovery. Drug target identification and validation, rational (target-based) drug design, structural biology, computational-based drug design, methods development (chemical, biochemical and computational), and “Hit-to-lead” development are all aspects of medicinal chemistry. The techniques and approaches of chemical biology, synthetic organic chemistry, combinatorial (bio)chemistry, mechanistic enzymology, computational chemistry, chemical genomics and high-throughput screening are all used and applied by medicinal chemists towards drug discovery.

Lead Optimization

Medicilon has completed dozens of drug research projects for clients and successfully identified several drug candidates for clinical trials. Our team provides the following services:more details

Target Assessment – Drug Targets
HITs Identification
Lead Optimization
Clinical Candidate Nomination
Computer Aided Drug Design
SAR Study

Lead optimization strategy

From early phase chemistry, through in vitro toxicity screening and metabolism profiling, to establishing in vivo bioavailability; we put facilities and expertise, state-of-the-art equipment and high quality accommodations at your disposal. No “standard” strategy exists that is suitable for the lead optimization of developmental drugs. Therefore,our first focus in assisting you with lead optimization is not to screen a high number of compounds with as many screening studies as possible,but to start designing your most efficient and effective drug screening strategy that addresses major aspects of ADMET.

Lead Optimization

Lead optimization is an operationally diverse stage of the drug discovery process in which the chemical structures of compounds or biologics are modified to improve target specificity and selectivity, plus pharmacodynamic, pharmacokinetic and toxicological properties to produce a preclinical drug candidate. This process requires detailed characterization of lead compound series and lead biologics, including data related to toxicity, efficacy, stability and bioavailability.

Lead optimization (LO) is one of the most expensive and time-consuming stages of the drug development process. Multiple factors make it more challenging given the need to improve the probability of technical success:

• The number of LO programs running simultaneously
• The number of molecules within each of those programs
• The need for integrated safety and efficacy endpoints
• The need for reproducible, decision-driving data

When you partner with Medicilon, you will work collaboratively with a dedicated team of experts assigned specifically to your project—sharing information,identifying and interpreting findings and providing you with the critical information you need to move forward with a successful candidate while prioritizing your lead optimization pipeline. This strong and productive relationship will continue until our team enables you to achieve your goal: the selection of a successful candidate for further development.

Contact us

Email : marketing@medicilon.com
Tel : +86 021 58591500

Tips : Above is part of Lead Optimization Services and Lead Optimization in Drug Discovery. You can also CONTACT US with any question or enquiry you may have. We will be happy to discuss your needs in detail and design an appropriate plan of action.

What is preclinical testing?

In the process of preclinical testing of a compound or biological agent into a drug, the compound involved must go through the testing phase. First, we need to identify potential targets that can treat the disease. Then, a variety of compounds or preparations are screened out. Any compound that has shown potential as a drug for the treatment of this disease needs to be tested for toxicity before clinical testing to reduce the possibility of injury. preclinical testing What is the basis of preclinical testing? According to US Food and Drug Administration (FDA) regulations, a series of tests are required before a new drug is approved for use. In the first stage, basic research determines a hypothetical target for the treatment of a certain disease, and then screens small molecules or biological compounds to discover any substance with the potential to treat the disease. Then, a preclinical research phase followed, before which, as described above, the potential toxicity of the compou

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Inventory of the three major in vitro pharmacokinetic research methods

The metabolic properties of a compound are an essential factor in whether or not it can be used as a drug in the clinical setting, so pharmacokinetic studies of newly synthesized compounds are required in drug development. In vitro incubation with liver microsomes, recombinant CYP450 enzyme lines, and in vitro incubation with hepatocytes are some of the more common in vitro drug metabolism methods. 1. In vitro incubation method with liver microsomes The metabolic stability and metabolic phenotypes of candidate compounds in different species of liver microsomes are good predictors of the metabolic properties of compounds in vivo. They are practical tools for evaluating candidate compounds in the pre-development phase of drug development. Liver microsomes include rat liver microsomes, human liver microsomes, canine liver microsomes, monkey liver microsomes, and mouse liver microsomes. In in vitro incubation of the liver, microsomes are the "gold standard" for in vitro d

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Enzyme Activity Assay Service

Enzymatic assay Lance Assay Alphascreen Assay Z’-LYTE Assay Adapta Assay Kinase-Glo Assay ADP-Glo Assay Ligand Binding Assay ELISA Assay HTRF Assay Enzyme activity assays are laboratory methods for measuring enzymatic activity. They are vital for the study of enzyme kinetics and enzyme inhibition. Enzyme units : Amounts of enzymes can either be expressed as molar amounts, as with any other chemical, or measured in terms of activity, in enzyme units. Medicilon provides various enzyme activity assays for kinases , phosphatases, proteinases, deacetylase, peptidase, esterase, and other enzymes. Our line of well-characterized immunoassays and biochemical kits ensures accurate and reproducible results. Enzyme is a large category of bio-molecules that catalyze various biological processes including metabolic processes, cellular signaling and regulation, cell division and apoptosis. Enzymatic reactions convert substrate molecules into chemically modified molecules products with high sp

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