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Assay Detail

CHEMBL1035595

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

Binding
Inhibition of tubulin polymerization
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design and synthesis of 2-(3-benzo[b]thienyl)-6,7-methylenedioxyquinolin-4-one analogues as potent antitumor agents that inhibit tubulin assembly.
Chang YH, Hsu MH, Wang SH, Huang LJ, Qian K, Morris-Natschke SL, Hamel E, Kuo SC, Lee KH.
J Med Chem (2009) 52 : 4883 -4891
PubMed 19719238 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.91 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130200 1 6.43
CHEMBL557892 1 6.24
CHEMBL571668 1 6.19
CHEMBL539380 1 6.12
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.92
CHEMBL550284 1 4.57
CHEMBL562621 1 -
CHEMBL550349 1 -
CHEMBL561765 1 -
CHEMBL564802 1 -
CHEMBL560501 1 -
CHEMBL561629 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130200 IC50 = 370.0 nM 6.43
CHEMBL557892 IC50 = 580.0 nM 6.24
CHEMBL571668 IC50 = 640.0 nM 6.19
CHEMBL539380 IC50 = 760.0 nM 6.12
CHEMBL67 COMBRETASTATIN A4 IC50 = 1200.0 nM 5.92
CHEMBL550284 IC50 = 27000.0 nM 4.57
CHEMBL562621 IC50 > 4000.0 nM -
CHEMBL550349 IC50 > 40000.0 nM -
CHEMBL561765 IC50 > 40000.0 nM -
CHEMBL564802 IC50 > 4000.0 nM -
CHEMBL560501 IC50 > 40000.0 nM -
CHEMBL561629 IC50 > 40000.0 nM -