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Assay Detail

CHEMBL861926

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Binding
Inhibition of Aurora A kinase activity
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
Jung FH, Pasquet G, Lambert-van der Brempt C, Lohmann JJ, Warin N, Renaud F, Germain H, De Savi C, Roberts N, Johnson T, Dousson C, Hill GB, Mortlock AA, Heron N, Wilkinson RW, Wedge SR, Heaton SP, Odedra R, Keen NJ, Green S, Brown E, Thompson K, Brightwell S.
J Med Chem (2006) 49 : 955 -970
PubMed 16451062 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.45 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201297 1 9.00
CHEMBL202567 1 9.00
CHEMBL201197 1 8.70
CHEMBL373013 1 8.30
CHEMBL201655 1 8.22
CHEMBL382054 1 7.92
CHEMBL201654 1 7.37
CHEMBL202026 1 7.26
CHEMBL383448 1 6.97
CHEMBL201263 1 6.96
CHEMBL424850 1 6.80
CHEMBL203039 1 6.34
CHEMBL202502 1 6.33
CHEMBL203422 1 6.32
CHEMBL382804 1 6.24
CHEMBL202370 1 -
CHEMBL202241 1 -
CHEMBL380478 1 -
CHEMBL201953 1 -
CHEMBL202198 1 -
CHEMBL377289 1 -
CHEMBL381721 1 -
CHEMBL201307 1 -
CHEMBL202593 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201297 IC50 = 1.0 nM 9.00
CHEMBL202567 IC50 = 1.0 nM 9.00
CHEMBL201197 IC50 = 2.0 nM 8.70
CHEMBL373013 IC50 = 5.0 nM 8.30
CHEMBL201655 IC50 = 6.0 nM 8.22
CHEMBL382054 IC50 = 12.0 nM 7.92
CHEMBL201654 IC50 = 43.0 nM 7.37
CHEMBL202026 IC50 = 55.0 nM 7.26
CHEMBL383448 IC50 = 106.0 nM 6.97
CHEMBL201263 IC50 = 111.0 nM 6.96
CHEMBL424850 IC50 = 158.0 nM 6.80
CHEMBL203039 IC50 = 452.0 nM 6.34
CHEMBL202502 IC50 = 472.0 nM 6.33
CHEMBL203422 IC50 = 483.0 nM 6.32
CHEMBL382804 IC50 = 578.0 nM 6.24
CHEMBL202370 IC50 > 1000.0 nM -
CHEMBL202241 IC50 < 1.0 nM -
CHEMBL380478 IC50 < 1.0 nM -
CHEMBL201953 IC50 < 1.0 nM -
CHEMBL202198 IC50 < 1.0 nM -
CHEMBL377289 IC50 < 1.0 nM -
CHEMBL381721 IC50 < 1.0 nM -
CHEMBL201307 IC50 < 1.0 nM -
CHEMBL202593 IC50 < 1.0 nM -