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Assay Detail

CHEMBL3855896

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

Binding
Inhibition of human Aurora kinase A (E122 to K401 residues) expressed in mammalian expression system by Z'LYTE assay
12
Total Activities
12
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

Discovery of a Series of 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-ones as Selective PI3K-δ/γ Inhibitors.
Ferguson FM, Ni J, Zhang T, Tesar B, Sim T, Kim ND, Deng X, Brown JR, Zhao JJ, Gray NS.
ACS Med Chem Lett (2016) 7 : 908 -912
PubMed 27774127 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.15 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3904942 1 8.68
CHEMBL1673047 1 8.32
CHEMBL3950648 1 7.80
CHEMBL3909068 1 7.64
CHEMBL3926951 1 7.31
CHEMBL3979343 1 7.23
CHEMBL3942643 1 6.96
CHEMBL3959351 1 6.82
CHEMBL3907932 1 6.72
CHEMBL3898901 1 6.57
CHEMBL3889977 1 6.46
CHEMBL3932938 1 5.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3904942 IC50 = 2.1 nM 8.68
CHEMBL1673047 IC50 = 4.8 nM 8.32
CHEMBL3950648 IC50 = 16.0 nM 7.80
CHEMBL3909068 IC50 = 23.0 nM 7.64
CHEMBL3926951 IC50 = 49.0 nM 7.31
CHEMBL3979343 IC50 = 59.0 nM 7.23
CHEMBL3942643 IC50 = 110.0 nM 6.96
CHEMBL3959351 IC50 = 150.0 nM 6.82
CHEMBL3907932 IC50 = 190.0 nM 6.72
CHEMBL3898901 IC50 = 270.0 nM 6.57
CHEMBL3889977 IC50 = 350.0 nM 6.46
CHEMBL3932938 IC50 = 4900.0 nM 5.31