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Assay Detail

CHEMBL2173308

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

Binding
Inhibition of Aurora B kinase-mediated histone H3 phosphorylation at Ser10 in human MDA-MB-468 cells after 2 hrs by Western blot analysis
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-468
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.
Lawrence HR, Martin MP, Luo Y, Pireddu R, Yang H, Gevariya H, Ozcan S, Zhu JY, Kendig R, Rodriguez M, Elias R, Cheng JQ, Sebti SM, Schonbrunn E, Lawrence NJ.
J Med Chem (2012) 55 : 7392 -7416
PubMed 22803810 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.00 6.00
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2170590 1 6.00
CHEMBL2170591 1 6.00
CHEMBL2170404 1 6.00
CHEMBL2170407 1 6.00
CHEMBL2170418 1 6.00
CHEMBL2170417 1 -
CHEMBL2169893 1 -
CHEMBL2170416 1 -
CHEMBL2170415 1 -
CHEMBL2170414 1 -
CHEMBL2170413 1 -
CHEMBL2170412 1 -
CHEMBL2170411 1 -
CHEMBL2170410 1 -
CHEMBL2170409 1 -
CHEMBL2170408 1 -
CHEMBL2170406 1 -
CHEMBL2170405 1 -
CHEMBL2170442 1 -
CHEMBL2170419 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2170590 IC50 = 1000.0 nM 6.00
CHEMBL2170591 IC50 = 1000.0 nM 6.00
CHEMBL2170404 IC50 = 1000.0 nM 6.00
CHEMBL2170407 IC50 = 1000.0 nM 6.00
CHEMBL2170418 IC50 = 1000.0 nM 6.00
CHEMBL2170417 IC50 > 10000.0 nM -
CHEMBL2169893 IC50 > 10000.0 nM -
CHEMBL2170416 IC50 > 10000.0 nM -
CHEMBL2170415 IC50 > 10000.0 nM -
CHEMBL2170414 IC50 < 1000.0 nM -
CHEMBL2170413 IC50 < 1000.0 nM -
CHEMBL2170412 IC50 < 1000.0 nM -
CHEMBL2170411 IC50 < 1000.0 nM -
CHEMBL2170410 IC50 < 1000.0 nM -
CHEMBL2170409 IC50 < 1000.0 nM -
CHEMBL2170408 IC50 > 10000.0 nM -
CHEMBL2170406 IC50 > 10000.0 nM -
CHEMBL2170405 IC50 > 10000.0 nM -
CHEMBL2170442 IC50 < 1000.0 nM -
CHEMBL2170419 Inhibition - % -