Axcelead offer a comprehensive set of best-in-class capabilities to meet a range of customer needs.


Hit finding

Planning of hit identification strategyTarget assessment
Design of screening cascade
Proposal of compound library
Assay development for screeningMaterial preparation (cDNAs, proteins, cells)
Assay development
(Enzymes, GPCRs, transporters, ion channels, nuclear receptors, etc.)
Biochemical assay
Biophysical assay
Phenotypic assay (Cell line, Primary cells, iPS cells)
Protein-protein interaction; PPI
Electrophysiological assay
High throughput screen (HTS)*

*Various read-outs including also radiometric formats
*Ability to perform HTS under BSL2 conditions
Assay adaptation for HTS (full automation, miniaturization)
Pilot screen (HTS assay validation)
HTS campaign and Data analysisPrimary screening
Counter screening
EC50/IC50 measurement
Purity test
Hit follow up
(Hit expansion, species difference, selectivity, mechanism of action, etc.)

Lead generation/optimization

in vitro evaluation of compounds for hit/lead/IND generation
in vitro profiling and MOA/kinetics analysis
Biochemical analysis
Biophysical analysis(SPR, ASMS, TSA, ITC, NMR)
Structural biology for SBDD and FBDD
Cell-based assay

Compound library management

Compound logisticsCompound storage (Vials, tubes; 96&384 tube, Plates; 96&384&1536 well)
Compound quality control
Powder weighing
Liquid handling and reformatting
Compound information management
Managing, recording and reporting of all manipulation of client samples
Library management(Consulting services)
Facilities and EquipmentLab-automation system
Fully automated storage systems
Compound Logistics IT system
(managing, recording and reporting of all operations of client samples)


Medicinal Chemistry

“All-in-One” Medicinal Chemistry services, from hit compound
identification to selection of IND candidate compounds
Design and synthesis of new compounds for broad ranges of target
diseases and target classes

Peptide chemistry

Candidate-oriented research on lead peptide creation and
Peptide synthetic

Synthetic chemistry

Development of practical synthetic routes
Non-GLP API synthesis (up to 1 kg)
Synthesis of internal standards
Synthesis of labeled compounds
Synthesis and identification of estimated metabolites
Platform technology
High-temperature and/or high-pressure reaction using autoclaves
Micronization by jet-milling

High-throughput synthesis

High-throughput parallel synthesis
Reaction screening

 Analytical chemistry

NMR structural analysis
Quantitative NMR
Fragment screening (ligand-based protein NMR)
X-ray diffraction analysis
HPLC analysis and purification

Computational chemistry

Computer-aided drug discovery (SBDD/LBDD/FBDD)
Molecular design through molecular dynamic simulations
Virtual screening
Design of screening library


Pharmacology studies in oncology

In vitro studies

Cancer cell proliferation assaysCell panel
3D cultures (spheroid culture, soft agar culture)
Combination effect analysis
Cancer immunology-related analysisT cell cytotoxicity assay
Target validation, Mechanism of action analysis, biomarker analysis

in vivo studies

Antitumor efficacy studies
Pharmacology studies by IVIS
Target engagement, pharmacokinetic/pharmacodynamic (PK/PD) analysis: blood, tumor, mouse organs
Tumor-infiltrating lymphocyte (TIL) analysis
Immunodeficient mouse model (xenograft model)Human cancer cell lines / patient-derived tumor (PDx)
Subcutaneous tumor, orthotopic tumor, metastasis, systemic dissemination models
Immunocompetent mouse model (syngeneic model)Mouse cancer cell lines
Subcutaneous tumor, metastasis models

Pharmacology studies in immunological disorders

in vitro studies

Analyses of cytokine production, signal activation, and cell types in primary culture cells and whole blood
Proliferation assays of T cells, B cells, etc.
Th1, Th17, and Treg differentiation assays
Migration and apoptosis assays of splenocytes, thymocytes, B cells, neutrophiles, etc.
Target validation, Mechanism of action analysis, Biomarker analysis

in vivo studies

Target engagement and PK/PD analysis: Cytokine production and intracellular signal activation, etc.
Immune cell phenotyping in blood, lymph nodes, and various other tissues (Flow cytometry using 5-laser BD LSRFortessaTM)
Antibody production assay
Animal modelsModels of inflammatory bowel diseases
Multiple sclerosis model
Rheumatoid arthritis model
Psoriasis models, etc.

Pharmacology studies in central nervous system diseases

in vitro studies

Protein and gene expression analysis in primary central nervous system cells

in vivo studies

Behavioral test(Psychiatric-disease-related)Prepulse inhibition test
3-chamber sociability test
Psychostimulant-induced hyperactivity
Behavioral test(Motor function)
Grip strength test
Running wheel test
Behavioral test(Cognitive function)Novel object recognition test
8-Arm radial maze test
Target engagement and PK/PD analysisMicrodialysis
Sleep EEG
Pathological analysis
Collection of cerebrospinal fluid (CSF)
Animal modelsCognitive dysfunction models (scopolamine, MK-801)
Valproic acid-induced autism model
Poly (I:C) model of schizophrenia
Development of animal models by intracerebral injection

Pharmacology studies in cardiovascular diseases

in vitro studies

Hypertrophy, apoptosis, and cell signaling assay in primary cardiomyocyte
Isolated perfused rat heart (Langendorff perfused heart)
Aortic ring preparation
Target validation, Mechanism of action analysis, Biomarker analysis

in vivo studies

Target engagement and PK/PD analysis
CV safety (blood pressure, cardiac function, and electro-cardiogram, etc.)
Animal modelsIschemia/reperfusion model
Heart failure modelsHeart failure models (Small animals): MI model, TAC model etc.
Heart failure models (Large animals):Ischemia/reperfusion Heart failure models, MI model
Cardiac function measurement by cardiac catheterization
Cardiac function measurement by echocardiography
Hypertension models
Pulmonary hypertension model
Renal disease models (Alport syndrome mouse etc.)

Pharmacology studies in metabolic diseases

in vitro studies

Fibrosis evaluation in co-culture of hepatic stellate cell and hepatocyte
MOA analysis of lowering/increasing blood glucose, body weight loss/gain
Glucose metabolism / lipid metabolism assay in primary hepatocyte, cell lines of hepatocyte, pancreatic β cell, and adipocyte
Lipid metabolism assay in isolated skeletal muscle
Target validation, Mechanism of action analysis, Biomarker analysis

in vivo studies

Target engagement and PK/PD analysis
Animal modelsNon-alcoholic steatohepatitis (NASH) models(MC4R-KO mice fed western diet、Choline-deficient high-fat fed mice、Drug-induced fibrosis model etc.)
Diabetes models(Small animals)Glucose tolerance test
insulin tolerance test
Glucose clamp technique
Diabetes models (Large animals)
Obesity modelsBody composition analysis (Echo-MRI and X-ray CT)
Energy expenditure analysis (Open-circuit indirect calorimeter)

Pharmacology studies in gastrointestinal motility disorders

in vitro studies

Magnus test

in vivo studies

Defecation studies
Bead expulsion assay
Colonic manometry test

Pharmacology studies for cell therapy using large animals

in vivo studies

Immunosuppressed models Immunosuppressed porcine model
Immunosuppressed monkey modelCell engraftment evaluation
Disease modelsHeart failure porcine/monkey model
Type 1 diabetes porcine model


MetabolomicsPathway analysis
Analytical method development for target metabolites
LipidomicsNon-target analysis covering over 20 lipid classes
ProteomicsProtein turnover analysis
Protein-protein interaction analysis
Post-translational modification profiling


Data analysisMoA analysis using global omics data
Annotations (gene functions, mutation, etc.)
Data visualization
Gene mutation analysis
Single-cell RNA-seq data analysis
Biomarker discovery
GenomicsTarget re-sequencing
16S rRNA sequencing for microbiome analysis
Consultation on omics data acquisition and validation study plan

Genetically modified animals (mice)

Generation of knock-out (KO) rodents
Generation of transgenic (Tg) rodents
Generation of knock-in (KI) rodents
Creation of humanized rodents
Additional gene modification to rodent disease models
Cleaning to SPF grade and breeding(Rodents introduction from outside organizations)
Cryopreservation of embryos and sperm of rodents
gRNA design and vector construction for genome


ADME Screening

ADME ScreeningPurity
Kinetic solubility
log D
MDR1 substrate screening (using NIH MDR1-MDCK cell)
Metabolic stability
CYP inhibition
CYP3A time-dependent inhibition (TDI)
CYP induction
Plasma protein binding
Cassette dosing (rodents)

Discovery DMPK Studies

Bioanalysis (including method development)
In vitro studiesCYP phenotyping studies
CYP3A time-dependent inhibition (TDI)
CYP induction
Non-CYP metabolism studies
Hepatocyte metabolic clearance
Metabolite structural analysis (in vitro/in vivo)
Blood/plasma concentration ratio
Substrate specificity studies using various transporter-expressing cells
Inhibition studies using various transporter-expressing cells
Plasma protein binding
Skin permeability studies
GSH/CN trapping studies
Pharmacokinetic studies in various animal speciesCassette dosing (non-rodents)
Tissue distribution, urinary/biliary excretion
Parenteral administration (transdermal, intranasal, pulmonary, sublingual, intrarectal, etc.)
Compound optimization / translational researchStructure-property relationship
DDI risk assessment
Human PK, effective concentrations, and effective doses prediction
PK/PD/E analysis, TK/TD analysis, modelling & simulation (Business partnership with Leiden Advanced PK/PD)

Physicochemistry and Preformulation Studies

Physicochemical property profilingPurity
Crystal form / crystallinity
Thermal property
Particle size
Thermodynamic solubility, etc.
Development form selection
Formulation for animal experiments
Stability (solid, solution, dosing formulation)

Pre-clinical development

Consulting on development strategy and individual issues
Design of customized nonclinical data package for IND/NDA
Evaluation of the risk of drug-drug interaction at early development stage
Development of entire strategy for metabolites
Modeling & simulation from nonclinical to clinical stages in cooperation with LAP&P


In vitro Exploratory Safety Studies

CytotoxicityGlu/Gal cytotoxicity assay(HepG2 cell)
PhospholipidosisPhospholipidosis assay(HepG2 cell)
Cardiotoxicity ( QT/Proarrhythmic potential assessment )hERG, Nav1.5 peak, Cav1.2 automated patch clamp
Microelectrode array(MEA)assay(hiPS-cardiomyocytes)
Off-targetReceptor binding/enzyme assay
Genotoxicityumu microtest(TA1535/pSK1002)
Ames test(TA100, TA98)
Micro-Ames test(TA100, TA98)
In vitro micronucleus test(TK6 cell)
Multi-Flow DNA damage assay(γH2AX/pHH3/p53/polyploidy(TK6 cell))
PhototoxicityUV/Vis absorption spectra
In vitro 3T3 NRU phototoxicity test

In vivo Exploratory Safety Studies

TK/tolerability studies in rodents and non-rodents
Preliminary range-finding repeated-dose toxicity studies (including TK studies)TK/tolerability studies
Cardiovascular safety pharmacology study (including TK studies; possible in conscious or anesthetized condition)  rodents
Preliminary embryo-fetal development toxicity study in rodents and rabbits (including TK studies)
In vivo photo toxicity studies in rodents
Improvement of oral absorption for insoluble drugs due to nanoparticle preparation technology
In vivo micronucleus tests in rodents

IND/NDA enabling

In vivo definitive safety studies for investigational new drug (IND) application*

Repeated-dose toxicity studies in rodents and non-rodents
Safety pharmacology studies
Genotoxicity studies

*: GLP-compliant (including partly subcontract)

In vivo definitive safety studies for new drug application (NDA)*

Reproductive and developmental toxicity studies
Long-term Repeated-dose toxicity studies
Carcinogenicity studies
Juvenile animal toxicity studies in rodents

*: GLP-compliant (including partly subcontract)

Toxicity mechanism studies / Target validation / Efficacy Studies

Preliminary toxicity evaluation in pharmacology studies
Characterization of disease models and Tg/KO animals
Neuro-electrophysiological examinations due to compound muscle action potentials (CMAPs) or motor evoked potentials (MEPs) in rodents
Pharmacology studies of regenerative medicines in immunosuppressed animals
Ocular function evaluation and mechanistic studies of ocular toxicity (ex. quantitative determination of cataract, ERG, cornea histological examination in life and cotton yarn/Schirmer tear test in rodent)
Histology services (Special staining, immunohistochemistry, and in situ hybridization)
Whole slide image analysis / Morphometry (Fibrosis, G-ratio, etc.)
Electron microscopic examinations
Clinical pathology (Hematology, Blood chemistry, Blood coagulation test, Blood compatibility test, Hemolysis test, Urinalysis)
Exploratory tumorigenesis studies for development of regenerative medicine products
Exploratory carcinogenicity/tumorigenicity studies of regenerative medicines in immunodeficient mice
Laser capture microdissection

Consulting services

Non-clinical safety consultation in various developmental phases (screening phase, candidate nomination, candidate selection, IND, NDA)
Consultation on issues inquired from the regulatory authorities