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Assay Detail

CHEMBL5737741

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

Binding
Human c-Fms Protein Kinase Assay (gamma-33P-ATP Format): c-fms(h) was incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 μM KKKSPGEYVNIEFG, 10 mM MgAcetate and [γ-33P-ATP] (specific activity approx. 500 cpm/pmol, concentration as required). The reaction was initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction was stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction was then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting.
9
Total Activities
3
Compounds Tested
3
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

Substituted pyridine derivatives useful as C-FMS kinase inhibitors
(2022)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.90 8.00
kon 3 - -
k_off 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6027874 3 8.00
CHEMBL5986778 3 7.96
CHEMBL3674570 EDICOTINIB 2.0 3 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6027874 IC50 = 10.0 nM 8.00
CHEMBL5986778 IC50 = 11.0 nM 7.96
CHEMBL3674570 EDICOTINIB IC50 = 18.0 nM 7.75
CHEMBL5986778 kon = - -
CHEMBL5986778 k_off = - s-1 -
CHEMBL6027874 kon = - -
CHEMBL6027874 k_off = - s-1 -
CHEMBL3674570 EDICOTINIB kon = - -
CHEMBL3674570 EDICOTINIB k_off = - s-1 -