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Assay Detail

CHEMBL972587

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

Functional
Decrease in histone H3 phosphorylation in human HCT116 cells after 16 hrs by Western blot
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of a potent and selective aurora kinase inhibitor.
Oslob JD, Romanowski MJ, Allen DA, Baskaran S, Bui M, Elling RA, Flanagan WM, Fung AD, Hanan EJ, Harris S, Heumann SA, Hoch U, Jacobs JW, Lam J, Lawrence CE, McDowell RS, Nannini MA, Shen W, Silverman JA, Sopko MM, Tangonan BT, Teague J, Yoburn JC, Yu CH, Zhong M, Zimmerman KM, O'Brien T, Lew W.
Bioorg Med Chem Lett (2008) 18 : 4880 -4884
PubMed 18678489 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.65 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL486850 1 7.80
CHEMBL486877 1 7.80
CHEMBL505037 1 7.80
CHEMBL519728 1 7.20
CHEMBL472193 1 -
CHEMBL520053 1 -
CHEMBL518051 SNS-314 MESYLATE 1 -
CHEMBL512184 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL486850 EC50 = 16.0 nM 7.80
CHEMBL486877 EC50 = 16.0 nM 7.80
CHEMBL505037 EC50 = 16.0 nM 7.80
CHEMBL519728 EC50 = 63.0 nM 7.20
CHEMBL472193 EC50 < 16.0 nM -
CHEMBL520053 EC50 < 16.0 nM -
CHEMBL518051 SNS-314 MESYLATE EC50 < 16.0 nM -
CHEMBL512184 EC50 < 16.0 nM -