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Assay Detail

CHEMBL4254604

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

Binding
Inhibition of pig brain tubulin polymerization measured every 1 min for 20 mins by spectrophotometric method
6
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
Zhou P, Liang Y, Zhang H, Jiang H, Feng K, Xu P, Wang J, Wang X, Ding K, Luo C, Liu M, Wang Y.
Eur J Med Chem (2018) 144 : 817 -842
PubMed 29306206 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.44 5.77
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4285846 2 5.77
CHEMBL4285231 1 5.46
CHEMBL4293724 2 5.46
CHEMBL107 COLCHICINE 4.0 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4285846 IC50 = 1700.0 nM 5.77
CHEMBL4285231 IC50 = 3500.0 nM 5.46
CHEMBL4293724 IC50 = 3500.0 nM 5.46
CHEMBL107 COLCHICINE IC50 = 8600.0 nM 5.07
CHEMBL4293724 Inhibition - % -
CHEMBL4285846 Inhibition - % -