HTS（High Throughput Screening）

HTS (High-throughput screening) is a drug discovery process to identify hit compounds as chemical starting points through compound library screening.

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Our HTS platforms and services for your drug discovery

Seamless services from assay development through hit/lead finding with well-experienced and high expertise
HTS platform covering a wide range of target classes and phenotypes
Pharma-origin vast library with high quality and diverse structure
One-stop Hit follow-up service

Seamless screening platform from assay development
through HTS with well-experienced and high expertise professionals

Axcelead offers an integrated screening platform including material preparation, assay development, and HTS.
Axcelead proposes promising flexible screening plans and strategies based on customer needs.

Axcelead provides hit compounds including high-value information.

■ Compound profiles based on Axcelead original data.

Cytotoxicity data (only for compounds tested in-house so far)
Biological annotations of hit compounds

■ Review of hit compounds by medicinal chemists in Axcelead

Clustering of hit compounds by Axcelead original algorithm
Comments on structural characteristics of each cluster

■ Drug-like properties (QED, HBA/HBD, AlogP, tPSA, number of aromatic ring, Fsp3 etc.)

Assay development and high-throughput screening platforms
covering a wide range of target classes

Platforms are available for all major target classes and phenotypes.

Axcelead proposes and conducts suitable material preparation (recombinant proteins and stable cell lines) for your HTS.

Major Axcelead assay platforms

GPCRs
Enzymes
Ion channels/Transporters
Nuclear receptors
PPI (protein-protein interaction)
Nucleic acids (RNA targeted drugs etc.)
High-throughput Affinity Selection Mass Spectrometry (ASMS) for screening
Phenotypic screening
e.g.) High content screening, Reporter gene assay,Gene expression analysis

Vast compound libraries with high quality and diverse structure

Axcelead proposes the optimal compound libraries for your HTS.

■Diversity libraries

Single library 220,000 compounds
Pooled library 500,000 compounds
(Standard 320,000 cpds)

You can choose either or both of pooled and single libraries that pursue lead-likeness and diversity. CNS focused, Fragment, and low cytotoxic compounds for cell-based screening libraries are available

■Focused libraries

Libraries for target classes (Kinase, GPCR, Protease, PPI, etc.)
Macrocyclic
Molecular Glue
RNA
Covalent
Extended rule of 5
Natural product
Annotation

Biologically annotated library for phenotypic screening is available

High quality compound library

One-stop post HTS service
Hit expansion, Orthogonal assay, ADMET profiling

Axcelead supports to generate Advanced Hit compounds with several approaches including orthogonal assay.

Axcelead biophysical analysis

Affinity selection-mass spectrometry (AS-MS)
Thermal shift assay (TSA)
Nuclear Magnetic Resonance (NMR)
Isothermal titration calorimetry (ITC)
Surface plasmon resonance (SPR)
X-ray crystallography

Solutions for your unique needs and challenges

Utilizing our accumulated expertise and high-quality compound library, we will identify promising hit compounds that contribute to the success of LG/LO. Please refer to the following for tailored solutions and examples that align with your challenges.

New Chemical Modality

HTS assay design and development

Challenging targets

Phenotypic drug discovery

We can also support Target Validation. Please feel free to contact us.