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Assay Detail

CHEMBL5113280

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

Binding
Inhibition of human Axl using KKSRGDYMTMQIG as substrate incubated for 40 mins in the presence of [gamma33P]ATP by scintillation counting analysis
41
Total Activities
41
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

Structure-based discovery of potent inhibitors of Axl: design, synthesis, and biological evaluation.
Wu S, Liao M, Li M, Sun M, Xi N, Zeng Y.
RSC Med Chem (2022) 13 : 1246 -1264
PubMed 36325401 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 7.61 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5184642 1 8.30
CHEMBL5185599 1 8.30
CHEMBL5187900 1 8.10
CHEMBL5201640 1 8.05
CHEMBL5171253 1 8.00
CHEMBL5192037 1 8.00
CHEMBL5169760 1 7.96
CHEMBL5187688 1 7.96
CHEMBL5204838 1 7.92
CHEMBL5180366 1 7.92
CHEMBL5197492 1 7.92
CHEMBL5189859 1 7.85
CHEMBL5186349 1 7.85
CHEMBL5209500 1 7.82
CHEMBL2022968 DUBERMATINIB 2.0 1 7.82
CHEMBL5209264 1 7.82
CHEMBL5178768 1 7.80
CHEMBL5199302 1 7.80
CHEMBL5173201 1 7.77
CHEMBL5203409 1 7.75
CHEMBL5179008 1 7.66
CHEMBL5205244 1 7.66
CHEMBL5177979 1 7.64
CHEMBL5187223 1 7.60
CHEMBL5195687 1 7.55
CHEMBL5175081 1 7.52
CHEMBL5207577 1 7.52
CHEMBL5176724 1 7.52
CHEMBL5189203 1 7.44
CHEMBL5173543 1 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5184642 IC50 = 5.0 nM 8.30
CHEMBL5185599 IC50 = 5.0 nM 8.30
CHEMBL5187900 IC50 = 8.0 nM 8.10
CHEMBL5201640 IC50 = 9.0 nM 8.05
CHEMBL5171253 IC50 = 10.0 nM 8.00
CHEMBL5192037 IC50 = 10.0 nM 8.00
CHEMBL5169760 IC50 = 11.0 nM 7.96
CHEMBL5187688 IC50 = 11.0 nM 7.96
CHEMBL5204838 IC50 = 12.0 nM 7.92
CHEMBL5180366 IC50 = 12.0 nM 7.92
CHEMBL5197492 IC50 = 12.0 nM 7.92
CHEMBL5189859 IC50 = 14.0 nM 7.85
CHEMBL5186349 IC50 = 14.0 nM 7.85
CHEMBL5209264 IC50 = 15.0 nM 7.82
CHEMBL2022968 DUBERMATINIB IC50 = 15.0 nM 7.82
CHEMBL5209500 IC50 = 15.0 nM 7.82
CHEMBL5178768 IC50 = 16.0 nM 7.80
CHEMBL5199302 IC50 = 16.0 nM 7.80
CHEMBL5173201 IC50 = 17.0 nM 7.77
CHEMBL5203409 IC50 = 18.0 nM 7.75
CHEMBL5179008 IC50 = 22.0 nM 7.66
CHEMBL5205244 IC50 = 22.0 nM 7.66
CHEMBL5177979 IC50 = 23.0 nM 7.64
CHEMBL5187223 IC50 = 25.0 nM 7.60
CHEMBL5195687 IC50 = 28.0 nM 7.55
CHEMBL5175081 IC50 = 30.0 nM 7.52
CHEMBL5207577 IC50 = 30.0 nM 7.52
CHEMBL5176724 IC50 = 30.0 nM 7.52
CHEMBL5189203 IC50 = 36.0 nM 7.44
CHEMBL5173543 IC50 = 46.0 nM 7.34
CHEMBL5187989 IC50 = 48.0 nM 7.32
CHEMBL5204819 IC50 = 49.0 nM 7.31
CHEMBL5170873 IC50 = 49.0 nM 7.31
CHEMBL5202025 IC50 = 50.0 nM 7.30
CHEMBL5195675 IC50 = 51.0 nM 7.29
CHEMBL5183041 IC50 = 100.0 nM 7.00
CHEMBL5183908 IC50 = 101.0 nM 7.00
CHEMBL5183492 IC50 = 169.0 nM 6.77
CHEMBL5197239 IC50 = 185.0 nM 6.73
CHEMBL5169769 IC50 = 555.0 nM 6.26
CHEMBL5192078 IC50 - -