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Related Experiment Video

Updated: May 11, 2026

A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 4
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A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 4

Published on: March 10, 2018

Chemokine receptor antagonist development.

Alexandre Garin1, Zoë Johnson, Aurelie Hermant

  • 1Geneva Research Centre, Division of Autoimmune and Inflammatory Diseases, Merck Serono, Geneva, Switzerland.

Methods in Molecular Biology (Clifton, N.J.)
|April 30, 2013
PubMed
Summary
This summary is machine-generated.

This study details assays for characterizing drug compounds from high-throughput screening. It assesses compound potency, whole blood effects, and establishes pharmacokinetic/pharmacodynamic relationships in rodents.

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Published on: February 20, 2018

Area of Science:

  • Drug discovery and development
  • Medicinal chemistry
  • Pharmacology

Background:

  • High-throughput screening (HTS) campaigns identify numerous potential drug candidates.
  • Characterization of these hits is crucial for advancing drug discovery programs.
  • Understanding compound behavior in biological matrices and in vivo is essential.

Purpose of the Study:

  • To describe robust assays for characterizing compounds from HTS.
  • To evaluate compound potency and stability in different environments.
  • To establish the pharmacokinetic/pharmacodynamic (PK/PD) relationship in a preclinical model.

Main Methods:

  • Assays to determine compound potency in buffer solutions.
  • Evaluation of compound activity in the presence of whole blood.
  • In vivo studies to establish PK/PD relationships in rodent models.

Main Results:

  • Established methods for assessing compound potency.
  • Demonstrated the impact of whole blood on compound efficacy.
  • Characterized the PK/PD profiles of selected compounds in rodents.

Conclusions:

  • The described assays provide a comprehensive approach to drug candidate characterization.
  • Understanding in vitro and in vivo compound behavior is critical for successful drug development.
  • This work facilitates the progression of HTS hits into viable drug leads.