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Lead Optimization

Lead Optimization Center

GenScript's seasoned biologists, in alliance with partner medicinal chemists, offer both exploratory and full medicinal chemistry services, and discovery biology services for assessing structure-activity relationships (SAR). The integrated services include custom organic synthesis, peptide synthesis, intermediate and active drug substance production, high-value focused library design and synthesis, primary and secondary assays, bioavailability, and toxicity assessment for advancing compounds from hit to lead, and lead optimization.

Lead Optimization Service

Medicinal Chemistry:

With an experienced team in custom organic synthesis, custom peptide synthesis, intermediate and active drug substances under GMP requirements, library design and synthesis, and medicinal chemistry, GenScript can provide cost efficient alternatives for hit-to-lead and lead optimization in drug discovery. Our libraries can be designed based on small molecular modeling and multi-parameter optimization, covering biochemical potency, efficacy, pharmacokinetics and pharmacodynamics, and toxicity. Our services include, but are not limited to:

  • Hit-to-Lead:
    • Analyze hit compounds
    • Design and synthesize focused libraries around the hits
    • Perform bioassay on library compounds
    • Analyze screening results, generate SAR, and report in standard or client-specified format

  • Lead Optimization:
    • Analyze SAR and propose optimization plan
    • Apply molecular modeling & quantitative SAR for data analysis & drug design
    • Multiparameter optimization: Biochemical & cellular potency, efficacy, PK/PD, selectivity and toxicity (hERG Safety Testing, e.g.)
    • High-value library compounds for screening against targets
    • Traditional medicinal chemistry
Discovery Biology:

GenScript's bio-assay center incorporates specific and secondary assays. Our assay services cover major classes of drug targets from GPCR and ion channels to enzymes (kinases, proteases, etc). GenScript's lead optimization strategies are further validated by our secondary assays. At this stage, more sophisticated and reproducible readouts are performed by more than 200 routine assays (cell-based or biochemical). In addition, we can work with our partners to develop tailored assays aiming at rapidly turning hits into drug candidates.

Quotations and Ordering

Orders can be placed by phone, email, fax, or online with a formal PO (Purchase Order). We recommend that you submit your service requests and orders via our Secure Online Ordering System.

For questions and quotation requests, please use our Secure Web Server. Our customer service representatives are available 24 hours, Monday through Friday to assist you. However, you may also contact us by email, phone, or fax.

Email: japanmarket@genscript.com
Phone: 03-6803-0843
Fax:03-3836-0371, 03-4496-5000(only for order)