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Assay Detail

CHEMBL2027232

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Binding
Inhibition of AXL kinase
9
Total Activities
9
Compounds Tested
2
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

Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors.
Mollard A, Warner SL, Call LT, Wade ML, Bearss JJ, Verma A, Sharma S, Vankayalapati H, Bearss DJ.
ACS Med Chem Lett (2011) 2 : 907 -912
PubMed 22247788 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.69 8.96
INH 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL460702 BMS-777607 2.0 1 8.96
CHEMBL254702 1 8.19
CHEMBL2023349 R428 1 7.85
CHEMBL2023351 1 7.80
CHEMBL2023350 1 7.52
CHEMBL2023352 1 7.00
CHEMBL601719 CRIZOTINIB 4.0 1 6.52
CHEMBL2023353 1 -
CHEMBL2023354 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL460702 BMS-777607 IC50 = 1.1 nM 8.96
CHEMBL254702 IC50 = 6.4 nM 8.19
CHEMBL2023349 R428 IC50 = 14.0 nM 7.85
CHEMBL2023351 IC50 = 16.0 nM 7.80
CHEMBL2023350 IC50 = 30.0 nM 7.52
CHEMBL2023352 IC50 = 100.0 nM 7.00
CHEMBL601719 CRIZOTINIB IC50 = 300.0 nM 6.52
CHEMBL2023353 INH = 33.0 uM -
CHEMBL2023354 INH = 47.0 uM -