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Assay Detail

CHEMBL4276355

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

Binding
Inhibition of N-terminal GST-tagged human AXL cytoplasmic domain (464 to 885 end residues) expressed in baculovirus expression system using fluorecence-labeled substrate by MCE assay
2
Total Activities
2
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

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

Publication

Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.
Zhao J, Zhang D, Zhang W, Stashko MA, DeRyckere D, Vasileiadi E, Parker RE, Hunter D, Liu Q, Zhang Y, Norris-Drouin J, Li B, Drewry DH, Kireev D, Graham DK, Earp HS, Frye SV, Wang X.
J Med Chem (2018) 61 : 10242 -10254
PubMed 30347155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.35 8.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3326006 1 8.78
CHEMBL4283353 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3326006 IC50 = 1.65 nM 8.78
CHEMBL4283353 IC50 = 12.1 nM 7.92