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Assay Detail

CHEMBL5323100

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of CSF1-induced CSF1R signalling in mouse BMDM cells assessed as reduction in ERK1/2 phosphorylation preincubated for 30 mins followed by CSF1 addition and measured after 10 mins
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type BMDM
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Macrophage colony-stimulating factor 1 receptor (CHEMBL5570)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

A highly selective purine-based inhibitor of CSF1R potently inhibits osteoclast differentiation.
Aarhus TI, Eickhoff J, Klebl B, Unger A, Boros J, Choidas A, Zischinsky ML, Wolowczyk C, Bjørkøy G, Sundby E, Hoff BH.
Eur J Med Chem (2023) 255 : 115344 -115344
PubMed 37141705 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.99 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5407395 1 7.40
CHEMBL5404686 1 7.08
CHEMBL3813873 PEXIDARTINIB 4.0 1 7.00
CHEMBL5431736 1 7.00
CHEMBL5415149 1 6.97
CHEMBL5413223 1 6.48
CHEMBL5406229 1 -
CHEMBL5401076 1 -
CHEMBL5417420 1 -
CHEMBL5416633 1 -
CHEMBL5424810 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5407395 IC50 = 40.0 nM 7.40
CHEMBL5404686 IC50 = 83.0 nM 7.08
CHEMBL3813873 PEXIDARTINIB IC50 = 100.0 nM 7.00
CHEMBL5431736 IC50 = 100.0 nM 7.00
CHEMBL5415149 IC50 = 106.0 nM 6.97
CHEMBL5413223 IC50 = 330.0 nM 6.48
CHEMBL5406229 IC50 > 300.0 nM -
CHEMBL5401076 IC50 > 300.0 nM -
CHEMBL5417420 IC50 > 300.0 nM -
CHEMBL5416633 IC50 > 300.0 nM -
CHEMBL5424810 IC50 > 300.0 nM -