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Assay Detail

CHEMBL4266274

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

Binding
Inhibition of Aurora A kinase (unknown origin)
11
Total Activities
11
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

Aurora kinase A (CHEMBL4722)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies.
Borisa AC, Bhatt HG.
Eur J Med Chem (2017) 140 : 1 -19
PubMed 28918096 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.97 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL572878 TOZASERTIB 2.0 1 9.22
CHEMBL483158 ALISERTIB 3.0 1 8.92
CHEMBL502124 1 8.47
CHEMBL259084 MLN-8054 1.0 1 8.40
CHEMBL2140408 AMG-900 1.0 1 8.30
CHEMBL4277690 1 8.05
CHEMBL402548 DANUSERTIB 2.0 1 7.89
CHEMBL482968 ENMD-2076 2.0 1 7.85
CHEMBL383899 ANILINOPYRIMIDINE1 1 7.38
CHEMBL202721 1 6.96
CHEMBL272125 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL572878 TOZASERTIB IC50 = 0.6 nM 9.22
CHEMBL483158 ALISERTIB IC50 = 1.2 nM 8.92
CHEMBL502124 IC50 = 3.4 nM 8.47
CHEMBL259084 MLN-8054 IC50 = 4.0 nM 8.40
CHEMBL2140408 AMG-900 IC50 = 5.0 nM 8.30
CHEMBL4277690 IC50 = 9.0 nM 8.05
CHEMBL402548 DANUSERTIB IC50 = 13.0 nM 7.89
CHEMBL482968 ENMD-2076 IC50 = 14.0 nM 7.85
CHEMBL383899 ANILINOPYRIMIDINE1 IC50 = 42.0 nM 7.38
CHEMBL202721 IC50 = 110.0 nM 6.96
CHEMBL272125 IC50 = 560.0 nM 6.25