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Assay Detail

CHEMBL1825458

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

Binding
Inhibition of Aurora kinase A assessed as phosphorylation of Lats2 substrate at 0.017 to 30 nM by FRET assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).
Zhang L, Fan J, Chong JH, Cesena A, Tam BY, Gilson C, Boykin C, Wang D, Aivazian D, Marcotte D, Xiao G, Le Brazidec JY, Piao J, Lundgren K, Hong K, Vu K, Nguyen K, Gan LS, Silvian L, Ling L, Teng M, Reff M, Takeda N, Timple N, Wang Q, Morena R, Khan S, Zhao S, Li T, Lee WC, Taveras AG, Chao J.
Bioorg Med Chem Lett (2011) 21 : 5633 -5637
PubMed 21798738 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.48 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1825090 1 8.30
CHEMBL1825092 1 8.30
CHEMBL1825091 1 8.22
CHEMBL1825095 1 8.05
CHEMBL1821761 1 7.89
CHEMBL1825089 1 7.85
CHEMBL1825096 1 7.77
CHEMBL1825093 1 7.70
CHEMBL1825094 1 7.52
CHEMBL1825102 1 7.02
CHEMBL1825100 1 6.96
CHEMBL1825097 1 6.82
CHEMBL1825101 1 6.75
CHEMBL1825099 1 6.58
CHEMBL1825098 1 6.46
CHEMBL1825103 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1825090 IC50 = 5.0 nM 8.30
CHEMBL1825092 IC50 = 5.0 nM 8.30
CHEMBL1825091 IC50 = 6.0 nM 8.22
CHEMBL1825095 IC50 = 9.0 nM 8.05
CHEMBL1821761 IC50 = 13.0 nM 7.89
CHEMBL1825089 IC50 = 14.0 nM 7.85
CHEMBL1825096 IC50 = 17.0 nM 7.77
CHEMBL1825093 IC50 = 20.0 nM 7.70
CHEMBL1825094 IC50 = 30.0 nM 7.52
CHEMBL1825102 IC50 = 95.0 nM 7.02
CHEMBL1825100 IC50 = 110.0 nM 6.96
CHEMBL1825097 IC50 = 150.0 nM 6.82
CHEMBL1825101 IC50 = 180.0 nM 6.75
CHEMBL1825099 IC50 = 260.0 nM 6.58
CHEMBL1825098 IC50 = 350.0 nM 6.46
CHEMBL1825103 IC50 > 10000.0 nM -