EARO Services

EARO services primarily support projects in the early-stages of the drug discovery process from target discovery and validation, hit identification to early structural analysis of target-hit interaction in a collaborative environment.

Expert consultation for all aspects of drug screening campaigns is available, from selecting the most appropriate assays that combine target-class and cell biology, establishing appropriate quality control parameters for validation to miniaturising and optimising the automation.

The services are not limited to the ones listed below, please write to us for custom-designed assays.

High Throughput Assays

High Throughput Assays

Cell-Based Assays

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A robust & sensitive cell-based assay is crucial for drug discovery campaign to select desirable hits with on target potencies. EARO offers an array of off -the-shelf and custom designed assays to investigate and screen for compounds against your target of interest and disease biology.

Proliferation Assays

Cell proliferation and viability assays provide a fast and effective platform to identify compounds with cytotoxic properties. We have optimised and miniaturised rapid and sensitive Proliferation assays ranging from traditional measurements that detect changes in cellular in ATP/ADP levels to image-based assays using Fluorescent dyes.

Cell Signalling Assays

Determine the mechanism of action of the test compounds using our homogeneous signal transduction assays and monitor receptor mediated modulation of pathways in response to the test compounds.

Reporter Assays

Investigate regulation of gene expression using custom designed and optimised reporter assays.

Protein Interaction Assays

Confirm the affinity of test compounds to the Protein of interest using NanoBRET Assays and/or study Protein-Protein interaction in cells using NanoBiT assays.

Ion Channel Assays

Screen, identify and validate compounds against Ion Channels and GPCR targets using High Throughput homogeneous cell based FLIPR assays.

Biochemical Assays

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Biochemical assays prove a rapid and efficient method to quantify & analyse the binding properties of the target protein and the effect of the compound on the target of interest. Over the years, we have optimised and miniaturised numerous biochemical assays for diverse target classes e.g reductase, methyltransferase , kinases etc. Choose from a range of High Throughput Screening capable biochemical assay technologies for your target specific assay requirements – AlphaLISA, FRET, FP, Oxido-reductase, Methyl-transferase, etc.

High Content Imaging Assays

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In contrast to traditional a single end-point read out of activity, HCI, automated microscope-based measurement of biological activity in 2D and 3D in vitro cultures following treatment with small molecule or genomic libraries in multi-well plates offers the ability to study multiple parameters simultaneously in complex biological systems. Typically, multiple features of the cell or organism are measured with one or more fluorescent dyes, hence the term High Content.

Cell Painting

An information rich multidimensional profiling of biological activity using robust and highly specific dyes to paint multiple cellular organelles to predict drug’s activity, toxicity or mechanism of action to accelerate drug discovery.

3D Tumour Spheroid Modelling

Tumour spheroid models can be used to recapitulate complex tumour microenvironment, which is composed of cells in different proliferative and metabolic states for the development of new anticancer strategies using automated imaging and analysis methods to assess treatment effectiveness with higher predictive value.

Co-culture Modelling

In the context of late-stage cancers investigation, co-culture screening offers a great advantage with identifying therapeutics that selectively kill primary and/or metastatic tumour populations.

High Throughput Screening Libraries

High Throughput Screening Libraries

Small Molecule Libraries

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Over 500,000 high quality small molecules with adequate diversity, lead-likeness, and solubility profile so the resulting hits are worth studying. These molecules can be further categorized into Focused sets with predictive algorithms that increase the chances of finding hits from within a selection from the entire library to accelerate discovery. EARO also hosts a number of diversity sets for discovery biology and libraries of drugs that have cleared at least the 1st phase of clinical trials for target validation and drug re-purposing studies.

Biologics Libraries

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Collection of human whole genome shRNA (TRC 2.0), siRNA, cDNA overexpression, lncRNA, miRNA mimics and inhibitors libraries.

Fragment Libraries

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Smaller fragments of molecules as libraries to reduce size and complexity for more efficient chemical sampling and subsequently combining the fragments towards a mature lead compound.

Protein Production

Protein Production

Construct Design & Optimisation

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Protein targets from various classes including kinases, phosphatases, proteases, transcription factors, decarboxylases and more can be engineered for optimal expression.

Protein Expression

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Small scale version to test for protein expression and large-scale version to upscale protein yield.

Protein Purification

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To obtain target protein of high purity, homogeneity, and also sufficient quantity to meet the standards for biochemical / functional assays, HTS, biophysical analysis or for your protein structure determination. Affinity purification, ion-exchange and gel-purification methods are used for obtaining high purity protein.

Protein Structure & Biophysics

Protein Structure & Biophysics

Protein Quality Control & Ligand Binding Validation

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The purification quality control measures protein homogeneity, concentration and molecular weight which are important before carrying out any further validations.

Crystallisation Screening

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Crystallisation grade protein is formed under different condition and screened for crystal hits with the most optimal conditions are chosen using nanolitre liquid handlers.

Crystal Optimisation

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Crystal hits are further optimised for protein concentration, incubation temperature, precipitants, and additives. Alternatively, seeding techniques and limited proteolysis methods can be used to find the optimal crystal formation conditions.

Protein-Ligand Complex Formation

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Ligands come in many forms – fragment, small-molecule, peptide, protein, DNA, co-factors. Soaking these ligands to form apo crystals and then facilitating protein-ligand complex formation by reverse-soaking ligands with protein crystals.

X-Ray Diffraction Data Acquisition & Processing

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Measurements from diffractometers and synchrotron beamlines are collected to test and improve diffraction quality. Diffraction datasets are created using processed high resolution diffraction images.

Structural Data Analysis

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Crystallography data analysis includes phase determination, structure modelling and refinement, fitting ligands and electron density mapping.

In Silico Biology & Analytics

In Silico Biology & Analytics

High Content Analysis (HCA)

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Extraction of multi-parametric data from cellular/sub-cellular images to quantify phenotypic alterations in cells. Deriving meaningful biological insights from HCA and HCS requires expertise in large-scale cellular imaging, image and statistical analyses. For more complex problems, techniques in Artificial Intelligence/Machine Learning (AI/ML) and multi-dimensional -omics data analytics are essential to model and predict cellular phenotypic behaviours associated with drug treatment.

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