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Assay Detail

CHEMBL5342462

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

Binding
Inhibition of CSF1R (unknown origin) in presence of ATP by Z-LYTE based FRET assay
20
Total Activities
20
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

Synthesis and Development of Highly Selective Pyrrolo[2,3-<i>d</i>]pyrimidine CSF1R Inhibitors Targeting the Autoinhibited Form.
Aarhus TI, Bjørnstad F, Wolowczyk C, Larsen KU, Rognstad L, Leithaug T, Unger A, Habenberger P, Wolf A, Bjørkøy G, Pridans C, Eickhoff J, Klebl B, Hoff BH, Sundby E.
J Med Chem (2023) 66 : 6959 -6980
PubMed 37191268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.82 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5439126 1 9.52
CHEMBL5425883 1 9.40
CHEMBL5411617 1 9.40
CHEMBL5405206 1 9.40
CHEMBL5430348 1 9.40
CHEMBL5406924 1 9.30
CHEMBL5404033 1 9.22
CHEMBL5436321 1 9.05
CHEMBL5397490 1 8.85
CHEMBL5435513 1 8.85
CHEMBL5398778 1 8.74
CHEMBL5420485 1 8.57
CHEMBL5397426 1 8.52
CHEMBL5416772 1 8.40
CHEMBL5417719 1 8.31
CHEMBL3813873 PEXIDARTINIB 4.0 1 8.30
CHEMBL5415647 1 8.19
CHEMBL5416379 1 8.11
CHEMBL5431035 1 7.96
CHEMBL5418087 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5439126 IC50 = 0.3 nM 9.52
CHEMBL5425883 IC50 = 0.4 nM 9.40
CHEMBL5411617 IC50 = 0.4 nM 9.40
CHEMBL5405206 IC50 = 0.4 nM 9.40
CHEMBL5430348 IC50 = 0.4 nM 9.40
CHEMBL5406924 IC50 = 0.5 nM 9.30
CHEMBL5404033 IC50 = 0.6 nM 9.22
CHEMBL5436321 IC50 = 0.9 nM 9.05
CHEMBL5397490 IC50 = 1.4 nM 8.85
CHEMBL5435513 IC50 = 1.4 nM 8.85
CHEMBL5398778 IC50 = 1.8 nM 8.74
CHEMBL5420485 IC50 = 2.7 nM 8.57
CHEMBL5397426 IC50 = 3.0 nM 8.52
CHEMBL5416772 IC50 = 4.0 nM 8.40
CHEMBL5417719 IC50 = 4.9 nM 8.31
CHEMBL3813873 PEXIDARTINIB IC50 = 5.0 nM 8.30
CHEMBL5415647 IC50 = 6.4 nM 8.19
CHEMBL5416379 IC50 = 7.7 nM 8.11
CHEMBL5431035 IC50 = 11.0 nM 7.96
CHEMBL5418087 IC50 < 0.3 nM -