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Assay Detail

CHEMBL952234

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

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

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4.
Hall JJ, Sriram M, Strecker TE, Tidmore JK, Jelinek CJ, Kumar GD, Hadimani MB, Pettit GR, Chaplin DJ, Trawick ML, Pinney KG.
Bioorg Med Chem Lett (2008) 18 : 5146 -5149
PubMed 18710804 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.65 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.92
CHEMBL217041 1 5.85
CHEMBL330407 1 5.58
CHEMBL506431 1 5.54
CHEMBL191350 1 5.35
CHEMBL496951 1 -
CHEMBL497164 1 -
CHEMBL493948 1 -
CHEMBL496952 1 -
CHEMBL497165 1 -
CHEMBL497166 1 -
CHEMBL495925 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67 COMBRETASTATIN A4 IC50 = 1200.0 nM 5.92
CHEMBL217041 IC50 = 1400.0 nM 5.85
CHEMBL330407 IC50 = 2600.0 nM 5.58
CHEMBL506431 IC50 = 2900.0 nM 5.54
CHEMBL191350 IC50 = 4500.0 nM 5.35
CHEMBL496951 IC50 - -
CHEMBL497164 IC50 - -
CHEMBL493948 IC50 - -
CHEMBL496952 IC50 > 40000.0 nM -
CHEMBL497165 IC50 > 40000.0 nM -
CHEMBL497166 IC50 > 40000.0 nM -
CHEMBL495925 IC50 - -