What is Hit to Lead (H2L)?

Hit to lead (H2L) is a key step towards compound optimization in drug discovery. The main purpose of H2L is to find suitable leads along the path to the final clinically active drug. In the H2L phase, researchers refine initial compounds using different screening methods, such as high-throughput screening. The screening process aims to reduce the number of these compounds to fewer and more qualified leads using in vitro and computer-based methods. To assess their efficacy in any in vivo model, the lead must possess sufficient properties. Obtain promising preclinical drug candidates by selecting the most promising hits and leveraging H2L and automated chemical synthesis workflows to speed up experimental screening cycles, reduce duration and hands-on time, thereby reducing overall drug discovery timelines.

Fig. 1. Process of hit-to-lead optimization and drug candidate selection. (Andricopulo AD, et al.,2009)

Services Overview

The hit to lead phase is a critical stage in the drug development process. At this stage, Ace Therapeutics' excellent scientists will screen the different compounds you hit through modern screening platforms (such as comprehensive high-throughput screening activities, virtual screening or NMR screening) to select the safest and most effective candidates for further screening. We provide robust and efficient experimental design and methodology to support our clients through lead optimization.

How Do We Meet Our Customers' Needs?

Ace Therapeutics is committed to the development of small molecule lead compounds in ophthalmology. Here, we provide our customers with customized solutions to support their research. With our scientific and chemical expertise, we can significantly improve the characteristics of small molecules hit by our customers in the previous stage. This will enable them to meet the basic criteria for entering the phase of pilot optimization. We utilize physicochemical characterization, state-of-the-art facilities to assess compound potency, selectivity and off-target effects, thereby advancing our clients' programs, saving time and cost. Our scientists utilize a range of design strategies to design and optimize small molecules down to compounds, including but not limited to.

• Hit Characterization
• Structure-Based Drug Design
• Fragment-Based Drug Design
• Computer-Aided Drug Design
• Chemical Synthesis

Explore Our Capabilities

In order to advance hit molecules into therapeutic small molecule lead compounds, our team of experts with extensive interdisciplinary expertise selects the most promising compounds for the next stage by optimizing numerous attributes of compounds, including solubility, potency, pharmacokinetics, toxicity, etc. During this process, we ensure that each molecule is extensively tested and eligible for lead optimization. What attracts our clients is our superior capabilities in the field of lead optimization, including but not limited to.

• Appropriate in vivo pharmacokinetic data in ocular disease model species.
• Computer analysis of compounds.
• Orthogonal testing to confirm the suitability of promising hit series.
• Computer-aided drug design tools.
• Advanced chemical synthesis for hit amplification of small molecules.
• Drug feasibility assessment based on patent space analysis, SAR and DMPK criteria.
• Initial improvement in ADME performance.
• Biophysical testing and structural characterization.
• Structure-activity relationship (SAR) and structure-property relationship analysis across DMPK analysis.
• A large group of computational chemistry experts specializing in drug design.
• Strong biotechnology platform support.

With broad capabilities across multiple disciplines, including chemistry, in vitro biology, structural biology and custom assay expertise, Ace Therapeutics is committed to helping customers worldwide discover ophthalmologically high-quality small molecule drugs. Our small molecule drug discovery scientists have more than years of comprehensive industry drug discovery experience and can experimentally support the most complex lead projects. You can quickly and efficiently find lead compounds with Ace Therapeutics. If you have any special needs in the field of H2L of ophthalmic small molecule lead compounds, please feel free to contact us. We look forward to working with you in the future.

Reference

1. Andricopulo AD, Salum LB, Abraham DJ. Structure-based drug design strategies in medicinal chemistry. Curr Top Med Chem. 2009;9(9):771-90.

• Target ID and Validation Services for Small Molecule Ophthalmic Drug
• Hit Identification Services for Small Molecule Ophthalmic Drug
• Lead Optimization Services for Small Molecule Ophthalmic Drug

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