High-Throughput Compound Screening
High-Throughput Compound Screening
Services
Online Inquiry

High-Throughput Compound Screening

Accelerate Hit Discovery

Rapidly evaluate hundreds of thousands of compounds against your target using fully automated robotic workflows.

  • Automated G3 Explorer suite processing compounds per week
  • Broad assay menu: biochemical, binding, cell-based with diverse readouts
  • Seamless integration from hit finding through lead optimization
  • Custom assay development with in-house protein and cell line support

Why Choose Our HTS Service?

Our platform combines state-of-the-art automation, broad compound libraries, and deep assay expertise to deliver screens you can trust.

  • Fully automated robotic handling for consistent, reproducible results
  • Flexible plate formats (96-, 384-, 1536-well) tailored to your assay
  • Comprehensive readout options: fluorescence, luminescence, high-content imaging, and more
  • Fast turnaround from study initiation to hit list delivery
Reproducible
Automated
Integrated
Our Approach

From Assay Design to Validated Hits

We execute high-throughput screening as a fully integrated service, combining miniaturized assay development, robotic automation, and data-driven hit validation to support your drug discovery pipeline. High-throughput screening leverages automated systems to test large compound libraries in parallel, enabling rapid hit identification.

Automated Compound Screening Pipeline

Our fully automated platform (Revvity G3 Explorer) handles compound plate preparation, liquid handling, incubation, and multi-mode detection in an enclosed robotic suite. This enables consistent, walk-away screening of large libraries with minimal manual intervention.

  • Robotic plate transport with two-arm system for high throughput
  • Supports biochemical, binding, and cell-based assays across 96/384/1536-well formats
  • We offer multi-mode readouts including fluorescence, polarization, HTRF, AlphaLISA, luminescence, and high-content imaging

Integrated Hit Identification & Validation

We combine primary screening with robust hit confirmation and triage, using dose-response curves, counter-screens, and AI-driven validation to quickly distinguish true hits from artifacts.

  • Automated primary data QC (Z' factor, plate normalization, controls)
  • Hit selection via statistical cutoffs and activity thresholds
  • Orthogonal confirmation assays and IC50/EC50 determination

Quality & Reproducibility

Rigorous quality control at every step—from assay robustness metrics (Z' typical) to replicate consistency—ensures that data from our automated system is highly reproducible.

Statistical Rigor

We apply well-established hit-calling methods, including plate-wise normalization, outlier detection, and multiple testing correction, to reduce false positives and deliver reliable hit lists.

Biological Interpretability

Results are contextualized with target engagement, pathway relevance, and selectivity data from counter-screens and secondary assays, helping you prioritize compounds with the highest translational potential.

Deliverables

What You Receive

Every HTS project delivers a comprehensive package of raw data, analysis reports, and validated hit lists to support your next discovery decision.

Data Deliverables

  • Raw plate reader data (fluorescence, luminescence, imaging) in standard formats
  • Quality control metrics (Z' factor, signal-to-background, replicate CV)
  • Primary hit list with compound IDs, activity values, and statistical scores
  • Dose-response curves and IC50/EC50 for confirmed hits

Reporting & Support

  • Detailed project report with methods, results, and interpretation
  • Compound management documentation (library source, plate maps, storage)
  • Follow-up consultation for hit triage and lead optimization strategy
Service Scope

Configurable Parameters for Your Campaign

Each HTS project is scoped to your specific target, library, and assay needs. Typical parameters are customized during consultation.

ParameterTypical Project Scope
Library SizeThroughput is measured in compounds per week, scoped per project based on library size and assay complexity.
Plate Format96-, 384-, 1,536-well (scoped per project)
Assay TypeBiochemical, binding, cell-based (viability, reporter, phenotypic)
Readout ModeFluorescence intensity/polarization, HTRF, AlphaLISA, luminescence, high-content imaging
Replication StrategySingle or duplicate screening; dose-response triplicates (scoped per project)
Hit ConfirmationDose-response, counter-screen (e.g., autofluorescence, aggregation), orthogonal assay
Data AnalysisAutomated QC, normalization, hit calling, IC50/EC50 fitting, heatmaps, and summary tables
Compound LibrariesClient-supplied, third-party, or our diversity/fragment/kinase inhibitor libraries
Workflow

Five Steps to High-Confidence Hits

Our standardized HTS workflow moves rapidly from assay development to validated results, with quality checks at every stage.

Assay Development & Miniaturization

We design and optimize your biochemical, binding, or cell-based assay for automation, confirming robustness in 384- or 1536-well format and establishing a Z' factor ≥ 0.5.

Compound Library Management & Preparation

Compound plates are prepared from your library or our in-house collections using automated liquid handlers, with barcode tracking and controlled storage to ensure integrity.

Automated High-Throughput Screening

The G3 Explorer robotic system performs plate transport, reagent addition, incubation, and detection in a fully enclosed suite, processing up to 200 plates per day.

Primary Data Processing & QC

Raw data are normalized, corrected for plate effects, and evaluated with standard metrics (Z' factor, signal-to-background, replicate CV). Failed plates are flagged for re-run.

Hit Identification & Validation

Compounds exceeding a statistically defined activity threshold are cherry-picked for dose-response testing and orthogonal counter-screens, delivering a validated hit list with IC50/EC50 values.

Applications

Screening Strategies for Diverse Therapeutic Needs

Our HTS platform supports multiple screening modalities, from classic target-based to complex phenotypic and imaging-based approaches.

Directly Measure Target Modulation

Ideal for well-characterized targets, we run biochemical or binding assays (e.g., enzyme activity, protein–protein interaction, receptor binding) to identify compounds that modulate activity with high potency.

  • Fluorescence, luminescence, or AlphaLISA readouts for high sensitivity
  • Selectivity panels and mechanism-of-action studies

Functional Activity in Living Cells

Cell-based assays (viability, reporter, signaling pathway, or phenotypic) capture compound effects in a physiologically relevant context, including toxicity and off-target cues.

  • Reporter gene, cell viability (ATP), and second-messenger assays
  • 2D and 3D cell models including organoids (where applicable)

Multiparametric Phenotypic Readouts

Automated microscopy and image analysis extract multiple cellular features (morphology, translocation, neurite outgrowth) per well, enabling rich phenotypic profiling.

  • Nuclear, cytoplasmic, and membrane stains for compartmental analysis
  • Quantitative image features used for hit prioritization
FAQ

High-Throughput Screening — Common Questions

Find answers about our HTS service, from assay format to data delivery.

  • We support biochemical (enzyme activity, binding), cell-based (viability, reporter, signaling), and high-content imaging assays. The optimal assay type is determined during consultation based on your target and desired readout.

  • Our robotic system minimizes manual variability, and every plate is evaluated with standard QC metrics (Z' factor, signal-to-background ratio, replicate CV). Runs failing quality thresholds are repeated before data release.

  • Yes, client-supplied libraries are accepted and handled under controlled conditions. We also offer access to our hand-selected diversity collection, fragment library, and kinase inhibitor library.

  • Primary hits are tested in dose-response to generate IC50/EC50 curves and assessed with counter-screens (e.g., autofluorescence, aggregation) to remove false positives. Confirmed hits are delivered with full data packages.

  • Project scope—including library size, assay type, plate format, replication, and timeline—is defined during a free consultation. No two projects are identical, and we tailor every step accordingly.

Scientific Literature

References

  1. Kang SY, Joshi P, Lee MY. High-Throughput Screening of Compound Neurotoxicity Using 3D-Cultured Neural Stem Cells on a 384-Pillar Plate. Current protocols. 2021;1(4):e107. View on PubMed
  2. Lo YH, Kolahi KS, Du Y, et al. A CRISPR/Cas9-Engineered ARID1A-Deficient Human Gastric Cancer Organoid Model Reveals Essential and Nonessential Modes of Oncogenic Transformation. Cancer discovery. 2021;11(6):1562-1581. View on PubMed
  3. Feng L, Zhong Y, Li L, et al. Leucokinin VIII acetate mitigates asthma severity by targeting ADCK5-induced cellular senescence. International immunopharmacology. 2025;165:115426. View on PubMed
  4. Hu C, Lu CH, Zheng J, et al. Anti-EGFR therapy can overcome acquired resistance to the third-generation ALK-tyrosine kinase inhibitor lorlatinib mediated by activation of EGFR. Acta pharmacologica Sinica. 2025;46(8):2267-2281. View on PubMed
  5. Nakamura K, Ortuste Quiroga HP, Horii N, et al. Iron supplementation alleviates pathologies in a mouse model of facioscapulohumeral muscular dystrophy. The Journal of clinical investigation. 2025;135(17). View on PubMed
  6. Shu W, Dong K, Shen X, et al. Inhibition of PRMT5 triggers synthetic lethality in ARID1A-deficient endometrial cancer by promoting aberrant R-loop accumulation. Molecular cancer. 2026;25(1). View on PubMed

Please kindly note that our products and services are for research use only.