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Assay Detail

CHEMBL3887258

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

Binding
Kinase Assay: Axl (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 μM KKSRGDYMTMQIG, 10 mM MgAcetate and [γ-33P-ATP] (specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is 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.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase receptor UFO (CHEMBL4895)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted quinoline compounds and methods of use
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.01 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3920222 1 8.30
CHEMBL3984441 NINGETINIB 2.0 1 7.96
CHEMBL3919169 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3920222 IC50 = 5.0 nM 8.30
CHEMBL3984441 NINGETINIB IC50 = 11.0 nM 7.96
CHEMBL3919169 IC50 = 17.0 nM 7.77