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Assay Detail

CHEMBL5323117

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Binding
Binding affinity to non-autoinhibited form of CSF1R (unknown origin) assessed as dissociation constant incubated for 1 hr by qPCR based Hill equation analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Macrophage colony-stimulating factor 1 receptor (CHEMBL1844)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Kd 4 7.36 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3813873 PEXIDARTINIB 4.0 1 8.24
CHEMBL5415149 1 7.44
CHEMBL5404686 1 7.10
CHEMBL5407395 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3813873 PEXIDARTINIB Kd = 5.8 nM 8.24
CHEMBL5415149 Kd = 36.0 nM 7.44
CHEMBL5404686 Kd = 80.0 nM 7.10
CHEMBL5407395 Kd = 220.0 nM 6.66