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Assay Detail

CHEMBL3862725

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

Binding
Inhibition of Aurora-B/INCENP (unknown origin) using biotinylated STK2 substrate incubated for 30 mins by HTRF assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Aurora kinase B/Inner centromere protein (CHEMBL3430907)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening.
Kilchmann F, Marcaida MJ, Kotak S, Schick T, Boss SD, Awale M, Gönczy P, Reymond JL.
J Med Chem (2016) 59 : 7188 -7211
PubMed 27391133 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.26 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483158 ALISERTIB 3.0 1 8.96
CHEMBL3600873 MK-5108 1.0 1 8.83
CHEMBL3921246 1 6.82
CHEMBL3903187 1 6.08
CHEMBL3985313 1 5.85
CHEMBL3904239 1 5.81
CHEMBL3915550 1 5.77
CHEMBL3975102 1 5.58
CHEMBL3932394 1 5.57
CHEMBL3924918 1 5.00
CHEMBL3941377 1 4.64
CHEMBL3983087 1 -
CHEMBL3913242 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483158 ALISERTIB IC50 = 1.1 nM 8.96
CHEMBL3600873 MK-5108 IC50 = 1.49 nM 8.83
CHEMBL3921246 IC50 = 150.0 nM 6.82
CHEMBL3903187 IC50 = 830.0 nM 6.08
CHEMBL3985313 IC50 = 1400.0 nM 5.85
CHEMBL3904239 IC50 = 1540.0 nM 5.81
CHEMBL3915550 IC50 = 1700.0 nM 5.77
CHEMBL3975102 IC50 = 2600.0 nM 5.58
CHEMBL3932394 IC50 = 2700.0 nM 5.57
CHEMBL3924918 IC50 = 10000.0 nM 5.00
CHEMBL3941377 IC50 = 23000.0 nM 4.64
CHEMBL3983087 IC50 - -
CHEMBL3913242 IC50 - -