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Assay Detail

CHEMBL5046623

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

Binding
Inhibition of NanoLuc-fused CSF1R (unknown origin) expressed in HEK293 cells incubated for 2 hrs by NanoBRET assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
Drewry DH, Annor-Gyamfi JK, Wells CI, Pickett JE, Dederer V, Preuss F, Mathea S, Axtman AD.
J Med Chem (2022) 65 : 1313 -1328
PubMed 34333981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.52 7.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5416410 DASATINIB 4.0 1 7.74
CHEMBL5089987 1 5.30
CHEMBL5072178 1 -
CHEMBL5087006 1 -
CHEMBL4446892 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5416410 DASATINIB IC50 = 18.3 nM 7.74
CHEMBL5089987 IC50 = 5060.0 nM 5.30
CHEMBL5072178 IC50 > 10000.0 nM -
CHEMBL5087006 IC50 > 10000.0 nM -
CHEMBL4446892 IC50 > 10000.0 nM -