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In Vitro Pharmacology & Receptor Binding Studies

Our in vitro pharmacology studies include radioreceptor binding and a panel of over 230 validated in vitro pharmacological assays covering a broad range of targets including receptors, transporters, enzymes, ion channels, and second messengers to assess pharmacological safety parameters for small molecule drugs. 

Pharmacology studies can be divided into three categories: 

  • primary pharmacodynamic
  • secondary pharmacodynamic
  • safety pharmacology 

Our Approach to DDI & Safety Pharmacology Studies

The objectives of safety pharmacology studies include:

  • identify undesirable pharmacodynamic properties of a substance that may have relevance to its human safety 
  • evaluate adverse pharmacodynamic and/or pathophysiological effects of a substance observed in toxicology and/or clinical studies
  • investigate the mechanism of the adverse pharmacodynamic effects observed and/or suspected.

Through our partner, the Drug Development Solutions Center, we offer a panel of over 230 validated in vitro measurement systems using animal tissue or human protein expression systems, covering a broad range of targets including receptors, transporters, enzymes, ion channels, and second messengers.

These assays help to identify lead compounds, define the mechanism of action and identify off-target activities. All assays are available on a one-off basis and clients can select one or more assays to be tested against any number of compounds at any number of concentrations.

Further investigation, if needed, can be conducted to identify the character and mechanism of action of drug candidates, measuring activities of agonist, antagonist, and inverse-antagonist.

Pharmacology studies in drug development contribute to drug safety evaluation

Our Capabilities for Your In Vitro Pharmacology Studies

Competitive Binding Assay: RadioReceptor Assay (RRA)

Our RadioReceptor Assay (RRA) is a competitive binding assay, evaluating the affinity of a test compound to various receptors by determining the inhibition ratio of the hot ligand binding to the membrane or tissue receptor.

Functional Assay

Our in vitro Functional Assay is a differentiation study to identify agonists, antagonists, and inverse agonists. We can quantitatively characterize by examining the dose-response curve obtained in GPCR or GTPγS functional assays.

Enzyme Inhibition Study

Our in vitro Enzyme Inhibition pharmacological study uses enzymes derived from humans to investigate inhibitory effects a drug compound may have through the determination of inhibition rates of specific enzymes at different concentrations.

Kinase Inhibition Assay

Inhibitory effect of a test drug is analyzed by determining inhibition rates of kinase activity at different concentrations.

Nuclear Receptor Assay

Nuclear receptor inhibition assays assess reactivity and tissue-specific effect of a test drug with various combinations of nuclear receptors, cofactors, or co-repressors.

Options for Ex Vivo Pharmacology Studies

Cell-based Assays

Studies using cells isolated from tissue or commercially available cells are available to study inhibition of cell membrane enzymes, cellular uptake, decomposition, and cytokine production. 

Scatchard Analysis

Various receptors can be characterized by measuring the effect of repeated administration on pharmacological action. 

Image Analysis

Receptor distribution in target tissues is measured using receptor mapping to visualize changes in receptor density in tissue samples.

In Vivo Pharmacology Studies

Enzyme Production Study

Animals are treated with a test compound, followed by measurement of the target enzyme quantity in tissue by the multiplex method in order to clarify the effects on the tissue enzyme production.

Get Details

Find out more about the Drug Development Solutions Center, reliability standards, cell-based assays, and results format

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