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Assay Detail

CHEMBL3707601

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

Binding
Inhibitory Assay: The method for measuring the in-vitro inhibitory activity of a test compound against Aurora B kinase activity was substantially the same as in the case of Aurora A. A purified recombinant human Aurora B protein was purchased from Carna Biosciences, Inc. The composition of a reaction buffer was 20 mM HEPES (pH 7.4), 2 mM DTT, 0.01% Tween-20, magnesium chloride (final concentration: 1 mM) and ATP (final concentration: 40 μM), and incubation time was set to 60 minutes.
13
Total Activities
13
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 B (CHEMBL2185)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Method for enhancing anti-tumor effect of a microtubule-targeting drug, and a method for treatment of tumor
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.47 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3692218 1 7.05
CHEMBL3692206 TAS-119 1.0 1 6.85
CHEMBL3692210 1 6.75
CHEMBL3692215 1 6.72
CHEMBL3692209 1 6.58
CHEMBL3692207 1 6.47
CHEMBL3692214 1 6.42
CHEMBL3692217 1 6.41
CHEMBL3692216 1 6.35
CHEMBL3692211 1 6.34
CHEMBL3692213 1 6.06
CHEMBL3692212 1 6.05
CHEMBL3692208 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3692218 IC50 = 90.0 nM 7.05
CHEMBL3692206 TAS-119 IC50 = 140.0 nM 6.85
CHEMBL3692210 IC50 = 180.0 nM 6.75
CHEMBL3692215 IC50 = 190.0 nM 6.72
CHEMBL3692209 IC50 = 260.0 nM 6.58
CHEMBL3692207 IC50 = 340.0 nM 6.47
CHEMBL3692214 IC50 = 380.0 nM 6.42
CHEMBL3692217 IC50 = 390.0 nM 6.41
CHEMBL3692216 IC50 = 450.0 nM 6.35
CHEMBL3692211 IC50 = 460.0 nM 6.34
CHEMBL3692213 IC50 = 880.0 nM 6.06
CHEMBL3692212 IC50 = 900.0 nM 6.05
CHEMBL3692208 IC50 = 930.0 nM 6.03