Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

miR-1-3p, as a novel diagnostic and prognostic biomarker, aggravates pancreatic acinar cell injury in acute pancreatitis by targeting GNPTAB.

Hereditas·2026
Same author

Bardet-Biedl syndrome in a Chinese patient with a novel homozygous <i>BBS5</i> variant from paternal uniparental disomy.

Ophthalmic genetics·2026
Same author

Predicting 1-Year Renal Outcomes in Patients with Diabetic Kidney Disease in CKD Stages 3 to 4: A Multimodal Machine Learning Approach Fusing Clinical Composites and Pathology Images.

Research (Washington, D.C.)·2026
Same author

Benzo(a)pyrene aggregating lung inflammation via inducing IL1R1 expression in asthma: Insights from network toxicology, single-cell transcriptomics, and Mendelian randomization.

Ecotoxicology and environmental safety·2026
Same author

Eosinophil-derived apoptotic extracellular vesicles accelerate steatotic liver repair after ischemia/reperfusion injury through mitochondria-associated metabolic reprogramming.

Journal of nanobiotechnology·2026
Same author

Application of Community-Based Participatory Research to Support Chinese American Dementia Caregivers.

Journal of gerontological social work·2026

Related Experiment Video

Updated: Jun 26, 2025

A Rapid Screening Workflow to Identify Potential Combination Therapy for GBM using Patient-Derived Glioma Stem Cells
05:29

A Rapid Screening Workflow to Identify Potential Combination Therapy for GBM using Patient-Derived Glioma Stem Cells

Published on: March 28, 2021

2.8K

Identification of Selective Imidazopyridine CSF1R Inhibitors.

John L Kane1, Gary Asmussen1, Joseph Batchelor1

  • 1Integrated Drug Discovery, Sanofi R&D, 350 Water Street, Cambridge, Massachusetts 02141, United States.

ACS Medicinal Chemistry Letters
|May 15, 2024
PubMed
Summary

Researchers developed novel inhibitors targeting the Colony Stimulating Factor-1 Receptor (CSF1R), crucial for immune cell function. Compound 36 shows potent activity and good oral exposure, offering potential for treating CSF1R-related diseases like cancer and neurodegeneration.

More Related Videos

A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 4
06:56

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

13.7K
A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
07:41

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

8.9K

Related Experiment Videos

Last Updated: Jun 26, 2025

A Rapid Screening Workflow to Identify Potential Combination Therapy for GBM using Patient-Derived Glioma Stem Cells
05:29

A Rapid Screening Workflow to Identify Potential Combination Therapy for GBM using Patient-Derived Glioma Stem Cells

Published on: March 28, 2021

2.8K
A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 4
06:56

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

13.7K
A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
07:41

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

8.9K

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Immunology

Background:

  • Colony stimulating factor-1 receptor (CSF1R) is a receptor tyrosine kinase vital for mononuclear phagocyte system (MPS) cells, including macrophages and microglia.
  • Dysregulated CSF1R signaling is implicated in diseases such as cancer, inflammation, and neurodegeneration.

Purpose of the Study:

  • To develop novel inhibitors of CSF1R.
  • To identify a lead compound with potent CSF1R inhibitory activity and favorable pharmacokinetic properties.

Main Methods:

  • Utilized a previously described imidazo[4,5-b]pyridine scaffold.
  • Conducted structure-activity relationship (SAR) studies.
  • Evaluated biochemical and cellular activity, in vitro ADME properties, and oral exposure in rats.

Main Results:

  • Discovered a novel series of CSF1R inhibitors based on the imidazo[4,5-b]pyridine scaffold.
  • Identified compound 36 as a lead compound with potent CSF1R biochemical and cellular activity.
  • Compound 36 demonstrated acceptable in vitro ADME properties and oral exposure in rat models.

Conclusions:

  • Novel imidazo[4,5-b]pyridine-based compounds effectively inhibit CSF1R.
  • Compound 36 represents a promising lead for further development in treating CSF1R-associated diseases.