High-Throughput Screening of Inhibitors

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Creative Enzymes enjoys an outstanding reputation in the enzyme industries for providing professional technical consultation and advanced technology platforms. To support therapeutic development and industrial applications such as food and chemical processing, we have launched our High-throughput Screening (HTS) service dedicated to enzyme inhibitors and ligands. This service focuses on all enzymology parameters that can reveal binding affinity, activity, and selectivity of candidate molecules.

Our HTS platform is highly customizable and capable of new method development for emerging targets. With extensive pre-built inhibitor libraries and the ability to design custom libraries, Creative Enzymes ensures rapid, precise, and reproducible screening for a broad range of enzyme classes. As testified by many customers, our HTS service stands out in both therapeutic and industrial applications.

Significance of Inhibitor High-Throughput Screening

High-throughput screening has revolutionized the search for enzyme inhibitors by allowing the rapid evaluation of thousands of compounds in parallel. While early screening efforts concentrated on kinases and proteases, today's discovery pipelines demand efficient screening for a much broader set of enzyme families.

At Creative Enzymes, our HTS platform extends to phosphatases, deacetylases, lipases, esterases, transferases, isomerases, reductases, ligases, glycosidases, and convertases, among others. This breadth ensures that both academic and industrial partners can identify high-value inhibitors across diverse enzyme targets.

High-throughput screening of inhibitors

By integrating technical support, customized assay development, inhibitor library construction, and precise activity measurements, we provide end-to-end solutions for inhibitor discovery.

Our Robust Service Offerings

Our High-throughput Screening of Inhibitors service is designed to meet the diverse needs of clients across pharmaceutical, biotechnology, food, and chemical industries. Key service highlights include:

Customizable Screening: Tailored assays and workflows for specific enzyme targets or compound classes.
New Method Development: Establishing novel screening approaches for newly discovered or difficult-to-assay targets.
Pre-built Inhibitor Libraries: Ready-to-use compound collections, all available for purchase.
Custom Library Construction: Designed according to client-specific needs for target enzymes.
Comprehensive Parameter Measurement: Potency, specificity, IC₅₀, K_i, kinetic constants, and binding affinity.
Technical Consultation: Complimentary sessions to refine experimental design and ensure optimal outcomes.

Full-Service from Initial to Verification

To provide more targeted support, our HTS service is divided into four specialized steps:

Service	Features	Price
Computational and Technical Support for High-Throughput Inhibitor Screening	Provides in silico modeling, docking, and technical consultation to optimize library design and screening strategy.	Get a quote
Construction of Inhibitor Libraries for High-Throughput Screening	Offers both pre-built compound collections and fully customized libraries designed to meet specific target requirements.
High-Throughput Inhibitor Assays and Screening	Delivers automated, scalable assay platforms capable of screening thousands of compounds with high accuracy and reproducibility.
Determination and Measurement of Inhibitor Activity	Focuses on detailed follow-up assays to quantify potency, kinetics, specificity, and stability of identified hits.

Service Workflow

High-throughput screening workflow for enzyme inhibitors

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Why Choose Creative Enzymes

Customizable Screening Platforms

Flexible workflows to address novel targets or unique assay requirements.

Comprehensive Enzyme Coverage

From kinases to glycosidases, we provide screening across a wide range of enzyme families.

Advanced Technology Platform

Automated systems ensure rapid, reproducible, and scalable screening.

Pre-built & Custom Libraries

Clients can leverage ready-to-use compound libraries or request tailored collections.

Integrated End-to-End Support

From computational guidance to final activity measurement, we provide a complete service pipeline.

Proven Track Record

Validated by numerous clients, our services have accelerated inhibitor discovery in both therapeutic and industrial contexts.

Case Studies and Real-World Applications

Case 1: High-Throughput Screening Identifies Thimerosal as a Potent TrxR1 Inhibitor

Thioredoxin reductase 1 (TrxR1) is a key anticancer target whose inhibition induces ROS-mediated apoptosis. To identify novel inhibitors, researchers developed and optimized an enzyme kinetics–based high-throughput screening (HTS) assay and tested 2,500 compounds from an in-house library. Thimerosal, a common vaccine preservative, emerged as a potent and reversible competitive TrxR1 inhibitor (IC₅₀ = 24.08 nM). It also suppressed A549 lung cancer cell proliferation (GI₅₀ = 6.81 μM), showing greater potency than auranofin. Flow cytometry confirmed thimerosal elevated ROS levels in cancer cells. This study demonstrates the assay's utility and highlights thimerosal as a novel TrxR1 inhibitor.

Thimerosal identified as a potent competitive TrxR1 inhibitor via high-throughput screening Figure 1. Development and optimization of the TrxR1 activity assay. (A) Principle of high-throughput screening for TrxR1 inhibitors. (B–E) Effects of TrxR1, NADPH, DTNB, and DMSO concentrations on reaction rate or activity. (F) IC₅₀ of auranofin against TrxR1 activity. (Ni et al., 2023)

Case 2: Multitarget Screening of Chitinolytic Enzyme Inhibitors for Insecticides

Small-molecule inhibitors of insect chitinolytic enzymes are promising insecticides, but single-target inhibitors often show limited activity. Using a multitarget high-throughput screening strategy, researchers evaluated a natural product library against four chitinolytic enzymes from the Asian corn borer (OfChtI, OfChtII, OfChi-h, and OfHex1). Several phytochemicals, including shikonin and wogonin, inhibited all four enzymes by binding the −1 substrate subsite and forming polar interactions with key catalytic residues. These compounds also exhibited significant insecticidal activity against lepidopteran pests. This study demonstrates the effectiveness of multitarget HTS in discovering natural product–based insecticide leads targeting chitin biodegradation during molting.

Discovery of multitarget natural product inhibitors of insect chitinolytic enzymes using high-throughput screening Figure 2. Primary screen of the TargetMol library containing 1680 natural products for inhibitors against Of ChtI (A), Of ChtII (B), Of Chi-h (C), and Of Hex1 (D). (Li et al., 2021)

FAQs About Inhibitor High-Throughput Screening

Q: Which enzyme classes are supported for high-throughput screening?

A: Our HTS services cover kinases, proteases, phosphatases, deacetylases, lipases, esterases, transferases, isomerases, reductases, ligases, glycosidases, convertases, and more. We also develop customized assays for novel enzyme targets.
Q: Can I use my own inhibitor library?

A: Yes. Clients may supply their own libraries, or we can integrate them with our pre-built or custom-constructed libraries for screening.
Q: What types of assay readouts are available?

A: We offer spectrophotometric, fluorescence, luminescence, HPLC, and MS-based assays, depending on the enzyme target and screening needs.
Q: How many compounds can be screened in a typical project?

A: Our HTS platform supports thousands of compounds per run, with the exact number tailored to client objectives and library size.
Q: How are results delivered?

A: Clients receive a complete dataset with ranked inhibitors, potency measurements (IC₅₀, K_i), specificity profiles, and recommendations for follow-up validation or optimization.
Q: What is the typical project timeline?

A: Project duration depends on library size and assay complexity. Standard HTS projects typically require 4–8 weeks, while custom assay development may extend timelines.

References:

Li W, Ding Y, Qi H, Liu T, Yang Q. Discovery of natural products as multitarget inhibitors of insect chitinolytic enzymes through high-throughput screening. J Agric Food Chem. 2021;69(37):10830-10837. doi:10.1021/acs.jafc.1c03629
Ni Y, Luo Z, Lv Y, Ma S, Luo C, Du D. Thimerosal, a competitive thioredoxin reductase 1 (TrxR1) inhibitor discovered via high-throughput screening. Biochemical and Biophysical Research Communications. 2023;650:117-122. doi:10.1016/j.bbrc.2023.02.014

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