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Assay Detail

CHEMBL856404

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

Binding
Inhibition of human recombinant Aurora B
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Aurora kinase B (CHEMBL2185)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.
Mortlock AA, Foote KM, Heron NM, Jung FH, Pasquet G, Lohmann JJ, Warin N, Renaud F, De Savi C, Roberts NJ, Johnson T, Dousson CB, Hill GB, Perkins D, Hatter G, Wilkinson RW, Wedge SR, Heaton SP, Odedra R, Keen NJ, Crafter C, Brown E, Thompson K, Brightwell S, Khatri L, Brady MC, Kearney S, McKillop D, Rhead S, Parry T, Green S.
J Med Chem (2007) 50 : 2213 -2224
PubMed 17373783 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 8.50 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215275 1 9.00
CHEMBL386253 1 9.00
CHEMBL424899 1 9.00
CHEMBL385049 1 9.00
CHEMBL217804 1 8.70
CHEMBL405120 1 6.29
CHEMBL215203 1 -
CHEMBL215495 1 -
CHEMBL215152 DEFOSBARASERTIB 2.0 1 -
CHEMBL215022 1 -
CHEMBL214637 1 -
CHEMBL215322 1 -
CHEMBL216053 1 -
CHEMBL214849 1 -
CHEMBL214848 1 -
CHEMBL214940 1 -
CHEMBL214601 1 -
CHEMBL386310 1 -
CHEMBL214842 1 -
CHEMBL384054 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215275 Ki = 1.0 nM 9.00
CHEMBL386253 Ki = 1.0 nM 9.00
CHEMBL424899 Ki = 1.0 nM 9.00
CHEMBL385049 Ki = 1.0 nM 9.00
CHEMBL217804 Ki = 2.0 nM 8.70
CHEMBL405120 Ki = 510.0 nM 6.29
CHEMBL215203 Ki < 1.0 nM -
CHEMBL215495 Ki < 1.0 nM -
CHEMBL215152 DEFOSBARASERTIB Ki < 1.0 nM -
CHEMBL215022 Ki < 1.0 nM -
CHEMBL214637 Ki < 1.0 nM -
CHEMBL215322 Ki < 1.0 nM -
CHEMBL216053 Ki < 1.0 nM -
CHEMBL214849 Ki < 1.0 nM -
CHEMBL214848 Ki < 1.0 nM -
CHEMBL214940 Ki < 1.0 nM -
CHEMBL214601 Ki < 1.0 nM -
CHEMBL386310 Ki < 1.0 nM -
CHEMBL214842 Ki < 1.0 nM -
CHEMBL384054 Ki < 1.0 nM -