High-Throughput Screening

High-throughput screening (HTS) is a cornerstone technology in modern drug discovery, enabling the rapid identification of biologically active compounds from large chemical libraries. At Creative BioMar, we combine target-class expertise with deep knowledge of cell biology to deliver robust and reliable screening solutions. Our HTS platforms integrate advanced assay systems, human primary cells, and disease-relevant models to ensure physiological relevance. With a library of over 850,000 synthetic compounds and the ability to handle client libraries of up to 3 million compounds, we consistently deliver validated hit compounds across diverse therapeutic areas, driving innovation in biomedical and pharmaceutical research.

High-Throughput Screening: Overview

The discovery of novel therapeutics increasingly depends on efficient screening technologies. High-throughput screening allows the systematic evaluation of thousands to millions of compounds against validated biological targets in a short time frame. However, the success of HTS relies heavily on the design of physiologically relevant assay systems, accurate image analysis, and a thorough understanding of disease biology.

At Creative BioMart, we leverage our long-standing expertise in cell line generation, assay development, and screening technologies to provide HTS campaigns that deliver actionable results. By incorporating high-content profiling and advanced imaging algorithms, we not only identify hit compounds but also generate deeper insights into biological mechanisms, ensuring more informed drug At Creative BioMart, we have established advanced expertise in harnessing these advantages for industrial and research applications.

High-Throughput Screening Services

Creative BioMart provides a comprehensive portfolio of HTS services, including:

High-Throughput Screening

of large compound libraries (up to 3 million compounds)

High-Content Profiling

Using standard cell models, human primary cells, and disease-specific cell lines

Custom Assay Development

For target-specific and pathway-specific studies

Compound Screening

For client-supplied libraries, with secure storage for repeat campaigns

Advanced Image Analysis Algorithms

Tailored to complex biological endpoints

End-to-End Project Management

From assay design to validated hit identification

Service Workflow

Service Details

Our expertise spans a wide range of biological readouts, enabling precise evaluation of compound effects across different cellular processes:

• Anchorage independence (3D growth models)
• Apoptosis and cell death
• Autophagy and protein aggregation
• Cell motility and migration
• Cytoskeletal rearrangements
• Epigenetic modifications
• Live imaging (e.g., calcium flux)
• Marker expression analysis
• Neurite outgrowth assays
• Receptor internalization and degradation
• Subcellular localization studies
• Transcription factor translocation
• Viral replication assays

With capabilities to handle single-compound or compressed formats, our HTS platforms deliver efficiency, scalability, and reproducibility across multiple screening campaigns.

Why Partner with Us for HTS Expertise

Comprehensive Expertise: Decades of experience in assay development, screening, and cell biology.

Scalable Capacity: Screening of up to 3 million compounds, with library storage for repeat campaigns.

Physiological Relevance: Use of human primary cells and disease-relevant models for translational insights.

Advanced Analytics: Proprietary image analysis algorithms for high-content, multiparametric profiling.

Proven Track Record: Over 20 HTS campaigns executed annually, consistently delivering validated hit compounds.

Flexible Collaboration: Client-tailored workflows, transparent reporting, and end-to-end scientific support.

Case Studies and Applications

Case 1: High-throughput screening identifies a neuroprotective candidate for Parkinson’s Disease

Antoniou et al., 2022. doi:10.1038/s41531-022-00278-y

Combining high-throughput screening with iPSC-based disease modeling offers a powerful approach to uncover therapies for neurodegenerative disorders. Using iPSC-derived neurons from patients with familial Parkinson’s disease carrying the p.A53T α-synuclein mutation, researchers applied high-content imaging to screen a kinase inhibitor library. The multi-kinase inhibitor BX795 emerged as a promising candidate, restoring disease-associated phenotypes at a single dose. Proteomic profiling revealed its protective effects were mediated through 118 proteins linked to RNA metabolism, protein synthesis, clearance, and stress responses, centered on the mTORC1 pathway. BX795 corrected aberrant protein synthesis and enhanced autophagy, supporting its potential as a therapeutic for Parkinson’s and related protein misfolding disorders.

Figure 1. Scatter plot showing the ratio of TH versus TUJ1 fluorescence intensity in duplicate upon treatment with 273 small molecule kinase inhibitors. The dots inside the green square correspond to the 4 hit compounds showing significant increase of TH versus TUJ1 fluorescence ratio as compared to the DMSO controls (blue dots). The red arrow indicates BX795. (Antoniou et al., 2022)

Case 2: MAPK Crmapk Mediates Mycoparasitism in Clonostachys chloroleuca

Lv et al., 2022. doi:10.1038/s41598-022-13899-3

Clonostachys chloroleuca 67-1 is a promising mycoparasite for controlling plant fungal diseases, with the MAPK gene Crmapk playing a central role in its biocontrol activity. To explore its molecular mechanisms, a high-quality yeast two-hybrid (Y2H) library was constructed, containing 1.6 × 10⁷ clones with a 96% recombination rate. Using a pGBKT7-Crmapk bait vector, 60 interacting proteins were identified, many associated with metabolism, cellular processes, and signal transduction. Integrating bioinformatics and transcriptome analyses of wild-type and ΔCrmapk mutants during parasitism of Sclerotinia sclerotiorum sclerotia revealed 41 differentially expressed genes, highlighting potential targets of the Fus3/Kss1-MAPK pathway and providing key insights into Crmapk-mediated mycoparasitism.

Figure 2. Analysis of the quality of the primary C. chloroleuca 67-1 library. (a) Determination of storage capacity. (b) Determination of recombination rate using primers pGADT7-F/R. (c) Determination of the mean length of inserted fragments from fungal colonies randomly selected by PCR amplification with primers pGADT7-F/R. (Lv et al., 2022)

Client Success Stories in High-Throughput Screening

“We engaged Creative BioMart to perform a high-throughput screen against our proprietary kinase target. Their team quickly developed a physiologically relevant cell-based assay and screened over 850,000 compounds with impressive precision. The validated hit series they identified not only showed strong selectivity but also translated well in our in-house secondary assays. Their deep expertise in assay development gave us confidence at every stage.”

— Director of Oncology Research | Global Pharmaceutical Company

“Our lab collaborated with Creative BioMart to evaluate compound effects on neurite outgrowth and protein aggregation in a neuronal disease model. Their high-content imaging and custom algorithm analysis provided multiparametric readouts far beyond what we could achieve internally. The insights we gained allowed us to prioritize compounds with genuine neuroprotective potential, and their detailed data sets were instrumental in our successful grant renewal.”

— Principal Investigator | Academic Medical Center

“We entrusted Creative BioMart with screening our 1.2 million compound libraries against an infectious disease target. Their ability to manage and securely store our library for multiple campaigns was invaluable. They delivered high-quality, reproducible results within the agreed timeline, and the validated hits they provided became the basis for two ongoing lead optimization programs. Their professionalism and scalability exceeded our expectations.”

— VP of Drug Discovery | Mid-Sized Biotech Firm

“We turned to Creative BioMart when we needed a complex, physiologically relevant assay for epigenetic modification studies. Their scientists designed the assay from the ground up, validated its robustness, and ran a focused HTS campaign using our candidate library. The detailed hit validation reports, including dose-response data, were of exceptional quality. Their ability to integrate assay design, screening, and analysis under one roof saved us months of internal development time.”

— Senior Scientist, Translational Biology | Industrial Biotech Company

FAQs About HTS Services

• Q: What types of assays can you support in high-throughput screening?

  A: We provide a broad range of assays, including cell-based, biochemical, and high-content imaging assays. Our expertise covers complex biological readouts such as apoptosis, autophagy, neurite outgrowth, receptor internalization, transcription factor translocation, and viral replication, among others.

• Q: How large a compound library can you screen?

  A: We can screen up to 1 million compounds in single-compound format and up to 3 million in compressed formats. Additionally, we offer secure storage for client-supplied libraries, enabling multiple campaigns without the need for repeated shipments.

• Q: How do you ensure physiological relevance in your screening assays?

  A: Our team leverages extensive experience in cell line generation and assay development to design systems that closely mimic in vivo conditions. We use standard cell models, human primary cells, and disease-relevant cell lines to ensure results translate effectively to biological and clinical settings.

• Q: What sets your data analysis apart from other screening providers?

  A: We have in-house expertise in image analysis algorithm design and high-content profiling, allowing us to capture multiparametric readouts. This advanced analysis provides deeper insights into compound mechanisms beyond simple activity readouts, increasing the value of your screening campaign.

• Q: Can you assist with both hit identification and validation?

  A: Yes. We don’t stop at primary screening. Our workflow includes secondary assays, dose-response testing, and robust hit validation to ensure that identified compounds are reliable and ready for lead optimization.

• Q: Why should we choose you over other HTS providers?

  A: We combine scientific expertise with scalability and flexibility. With over 20 HTS campaigns executed annually, a proprietary compound library of 850,000 compounds, advanced analytics, and the ability to handle client-specific needs, we deliver validated hits with efficiency, reliability, and translational relevance.

References:

1. Antoniou N, Prodromidou K, Kouroupi G, et al, High content screening and proteomic analysis identify a kinase inhibitor that rescues pathological phenotypes in a patient-derived model of Parkinson’s disease. npj Parkinsons Dis. 2022;8(1):15. doi:10.1038/s41531-022-00278-y
2. Lv B, Fan L, Li S, Sun M. Screening and characterisation of proteins interacting with the mitogen-activated protein kinase Crmapk in the fungus Clonostachys chloroleuca. Sci Rep. 2022;12(1):9997. doi:10.1038/s41598-022-13899-3