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Drug Discovery

Integrated Solutions Driving Innovation in Drug Discovery


Drug discovery is a complex scientific endeavor centered around identifying, designing, and developing bioactive compounds with therapeutic potential. Along with identifying and validating target molecules associated with diseases, drug discovery progresses through stages such as high-throughput screening, hit-to-lead optimization, and preclinical testing. Successful drug discovery culminates in developing a therapeutic agent that undergoes rigorous clinical trials before reaching the market.

Enzo provides a comprehensive array of products and services to expedite your drug discovery program across various stages. Whether you are working with mall molecules or biologics, our offerings cover everything from target discovery and validation to formulation and manufacturing.

Empower your drug development journey with Enzo's cutting-edge tools. Experience enhanced efficiency, cost savings, and overall success in the drug discovery process. By choosing Enzo's products and services, you gain the ability to streamline operations, making drug development more accessible. Join us in advancing pharmaceutical research to new heights.


Integrated Solutions Driving Innovation in Drug Discovery

Target Identification

Identifying a biological target, especially disease associated genes, proteins, enzymes or pathways, is crucial in drug discovery. Various methods, including genetic, biochemical, and phenotypic screening, are employed for this purpose

Target Validation

Target validation, a crucial step, involves functional studies to test the biological activity and role of the target to determine its suitability for drug development.

High Throughput Screening

High throughput screening (HTS) is a powerful technique in drug discovery, allowing rapid screening of numerous compounds for their interaction with a specific target or pathway.

Mechanism of Action Studies

Understanding a drug candidate’s mechanism of action (MoA) help optimize drug development and predict therapeutic outcomes.

Toxicity and Integrity Assessment

Protein aggregation in drug discovery poses risks, affecting efficacy, safety, and bioavailability, with concerns about toxicity.

Target Identification

Target identification is a crucial step in the drug discovery process, which aims to identify a biological target for a specific disease or condition. There are several approaches to target identification, including genetic approaches, biochemical approaches, and phenotypic screening.



To address the challenges of target identification and gene expression in Drug Discovery, the AMPIVIEW™ RNA probes, powered by Enzo’s LoopRNA ISH™ technology, provide visualization of the spatial localization of target genes in their tissue context without disrupting cell morphology.

  • Detection of unique nucleic acid targets (DNA/RNA or RNA) down to a single cell level
  • Simple protocols of 2-hour hybridization and one-step amplification
  • Adaptable products ready for any workflow (Manual or Automated)

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AMPIVIEW™ RNA Probes Deliver Superior Sensitivity and Specificity

AMPIVIEW™ RNA probes workflow diagram. Detection of epidermal growth factor receptor (EGFR) in prostate tissue with A. AMPIVIEW™ EGFR (AS) Dig RNA probes and B. AMPIVIEW™ NSP Dig RNA probes, amplified with DIGX® anti-digoxigenin, detected with POLYVIEW® PLUS AP combined with HIGHDEF® Red AP chromogen and hematoxylin.


Target Validation

Once a potential target has been identified, it must be further evaluated to determine if it is a suitable candidate for drug development. One of the key methods used for target validation is functional studies, which involve testing the biological activity of the target and its role in disease processes.


FLUOR DE LYS® HDAC Fluorometric Activity Assay Kit

Our portfolio of scalable enzyme activity assays is anchored by our FLUOR DE LYS® deacetylase assay platform, featuring kits for screening HDAC and Sirtuin activity modulators. We also offer FRET-based assays for matrix metalloproteinases (MMPs) and caspase activity and phospho-specific antibody-based kinase assays.

  • QUALITY: High activity, high purity recombinant enzymes for high-quality hits
  • FLEXIBILITY: Bulk enzymes and substrates available for postscreening studies
  • INNOVATIVE: Patented substrate/developer chemistries in a variety of readout formats

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FLUOR DE LYS® HDAC Fluorometric Activity Assay Kit
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MMP Inhibitor Profiling Kit, Fluorometric
Matrix Metalloproteinase-2 (MMP-2) Fluorometric Drug Discovery Kit, RED
Akt Kinase Activity Kit
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Reaction Scheme of the HDAC Fluorescent Activity Assay

Reaction Scheme of the HDAC Fluorescent Activity Assay. Deacetylation of the substrate sensitizes it to the developer, which then generates a fluorophore (symbol). The fluorophore is excited with 360 nm light and the emitted light (460 nm) is detected on a fluorometric plate reader


High-Throughput Screening

High throughput screening (HTS) is a powerful technique used in drug discovery. It enables the rapid screening of large numbers of compounds for their ability to interact with a specific target or pathway.


SCREEN-WELL® Compound Libraries

Enzo Life Sciences has a long and successful track record in identifying, synthesizing, and commercializing valuable known bioactives for use as research tools. Our long-standing, flagship SCREEN-WELL® Compound Library product family offers an easy, ready-to-use method for compound screening. Our unique offering of focused compound libraries includes FDA-approved drugs, natural products, receptor de-orphaning, chemical genomics, and pathway targeting.

  • A unique collection of small molecules including inhibitors, activators and/or inducers
  • Complete documentation set that highlights activity descriptions, plate positions, physical information and a structural database (SD) file
  • The ability to re-supply individual bulk compounds, custom libraries, or hard to source compound

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Activates adenylate cyclase by directly interacting with the catalytic unit of the enzyme leading to an increase in the intracellular concentration of cAMP. Inhibits ion channels by a mechanism that does not involve cAMP. Non-competitive inhibitor of nicotinic acetylcholine receptors. Induces neuronal differentiation in stem cells and several neuroblastoma.


Mechanism of Action Studies

Cell-based assays play a crucial role in drug discovery by providing a relevant and predictive model for evaluating the efficacy, safety, and potential mechanisms of action of drug candidates. This knowledge is invaluable for refining drug design and advancing the development of more potent and efficacious therapeutics.



Our CELLESTIAL® portfolio of fluorescent probes and assay kits for cellular analysis provides a complete set of tools for monitoring cell viability, proliferation, death, oxidative stress, and toxicology. Our dye-based assays have been optimized for the most demanding imaging applications, including confocal microscopy, wide-field fluorescence microscopy, flow cytometry, and high content screening, where consistency and reproducibility are essential.

  • Increased photostability reduces photobleaching
  • Reduce false positives by eliminating non-specific dye-associated artifacts
  • Compatible with common dyes and fluorescent markers (i.e., GFP) for multiplex analysis

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Quantify Autophagic Vacuoles Without Transfection

CYTO-ID® Autophagy Detection Kit 2.0 (ENZ-KIT175) was used to detect autophagy in HeLa cells cultured in (A) media under normal conditions, (B) starvation media (EBSS) treated with 40uM Chloroquine for 4 hours. Starved cells show a higher quantity of autophagic vacuoles compared to cells under normal conditions (fluorescent green).


Toxicity Assessment

Cytotoxicity, or the quality of being toxic to cells, is a cellular regulator that can result in various cell fates. Most often, it results in various types of cell death – including necrosis, where the cell dies due to cell lysis; apoptosis, a form of programmed cell death; or other fates. Enzo provides a variety of assays to quantify cytotoxicity in cells, including an LDH Cytotoxicity WST Assay and Cell Counting Kit 8.


GFP-CERTIFIED® Apoptosis/Necrosis Detection Kit

Distinguishing between apoptosis and necrosis provides valuable insights into the specific pathways through which a drug induces cell death, aiding researchers in assessing the safety and efficacy of potential drug candidates.

  • Suitable for death pathway analysis and drug/toxin studies
  • Readily distinguishes between healthy, early apoptotic, late apoptotic, and necrotic cells
  • Optimized for both fluorescence microscopy and flow cytometry applications

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LDH Cytotoxicity WST Assay
LYSO-ID® Red Cytotoxicity Kit
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Multiplex Healthy, Early Apoptotic, Late Apoptotic, and Necrotic Cells

GFP-CERTIFIED® Apoptosis/Necrosis Detection Kit (ENZ-51002) detects four distinct cell states. Mitochondrial GFP-expressing HeLa cells were treated with 2μM Staurosporine for 4 hours. The apoptosis detection reagent (gold) and necrosis detection reagent (red) specifically detect cell states with clear spectral separation from mitochondria-associated GFP signal. Healthy cells (A), cells undergoing apoptosis (B), cells undergoing late-stage apoptosis (C), and necrotic cells (D).


Integrity Assessment

The reliability of the drug product, from its inception in the laboratory to its application in clinical settings, is a determining factor in the journey of therapeutic development. Robust product integrity and stability are the foundation upon which efficacy, safety, and the ultimate success of emerging therapeutics hinge. Protein aggregation poses substantial risks during drug discovery, impacting therapeutic efficacy and safety.


PROTEOSTAT® Protein Aggregation Assay

Aggregated proteins may lose biological activity, induce immunogenicity, and alter pharmacokinetics, raising concerns about toxicity and reduced bioavailability. Formulation challenges, clinical relevance, and manufacturing hurdles further compound these issues. Addressing aggregation risks is crucial, and innovative solutions like the PROTEOSTAT® protein aggregation assays offer valuable insights.

  • One-step, ready-to-use solution with no radioisotopes
  • High sensitivity that correlates with the [3H]-thymidine incorporation assay
  • High-throughput screening without a solubilization step

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PROTEOSTAT® Protein Aggregation Assay
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PROTEOSTAT® Dye Yields Much Brighter Signal

Signal intensity of PROTEOSTAT® aggregate sensing dye compared to other dyes.


Enabling Your Drug Discovery Program

With over 45 years of innovation and technical expertise, Enzo provides you with the leverage you need to accelerate your Drug Discovery. The development of a single drug, whether it is a new chemical entity or a biologic therapeutic, requires a significant investment of resources. Each step of the process from early discovery through production and delivery, must be fully explored, characterized, and understood.

From target discovery and validation to formulation and manufacturing, Enzo offers a line of products and services that can accelerate your drug discovery program. Choose from an extensive range of assay kits, enzymes, substrates, and compound libraries for primary and secondary screening, immunodetection assays for reliable biomarker detection, and cytotoxicity assays for in vitro drug safety assessment. Our aim is to deliver innovative tools that make drug development more efficient, cost-effective and successful.

Our Technological Depth is our Strength


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