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Assay Detail

CHEMBL962087

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

Binding
Inhibition of human recombinant Aurora A
10
Total Activities
10
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

Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.
Peifer C, Selig R, Kinkel K, Ott D, Totzke F, Schächtele C, Heidenreich R, Röcken M, Schollmeyer D, Laufer S.
J Med Chem (2008) 51 : 3814 -3824
PubMed 18529047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.89 5.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL509435 1 5.50
CHEMBL521201 1 5.50
CHEMBL201511 MALEIMIDE 1 5.27
CHEMBL488811 1 5.19
CHEMBL452812 1 4.80
CHEMBL529663 1 4.80
CHEMBL529217 1 4.54
CHEMBL488646 1 4.52
CHEMBL488645 1 4.48
CHEMBL453593 1 4.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL509435 IC50 = 3200.0 nM 5.50
CHEMBL521201 IC50 = 3200.0 nM 5.50
CHEMBL201511 MALEIMIDE IC50 = 5400.0 nM 5.27
CHEMBL488811 IC50 = 6500.0 nM 5.19
CHEMBL452812 IC50 = 16000.0 nM 4.80
CHEMBL529663 IC50 = 16000.0 nM 4.80
CHEMBL529217 IC50 = 29000.0 nM 4.54
CHEMBL488646 IC50 = 30000.0 nM 4.52
CHEMBL488645 IC50 = 33000.0 nM 4.48
CHEMBL453593 IC50 = 47000.0 nM 4.33