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Assay Detail

CHEMBL4770232

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

Binding
Inhibition of bovine brain tubulin polymerisation preincubated with compound followed by GTP addition and measured after 20 mins by turbidimetry based spectrophotometric method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis, in vitro and in vivo biological evaluation of 2-amino-3-aroylbenzo[b]furan derivatives as highly potent tubulin polymerization inhibitors.
Oliva P,Romagnoli R,Manfredini S,Brancale A,Ferla S,Hamel E,Ronca R,Maccarinelli F,Giacomini A,Rruga F,Mariotto E,Viola G,Bortolozzi R
Eur J Med Chem (2020) 200 : 112448 -112448
PubMed 32417696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.31 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4784348 1 6.43
CHEMBL4795215 1 6.41
CHEMBL4786045 1 6.32
CHEMBL4795928 1 6.30
CHEMBL4786603 1 6.29
CHEMBL67 COMBRETASTATIN A4 -1.0 1 6.27
CHEMBL4782713 1 6.24
CHEMBL1823159 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4784348 IC50 = 370.0 nM 6.43
CHEMBL4795215 IC50 = 390.0 nM 6.41
CHEMBL4786045 IC50 = 480.0 nM 6.32
CHEMBL4795928 IC50 = 500.0 nM 6.30
CHEMBL4786603 IC50 = 510.0 nM 6.29
CHEMBL67 COMBRETASTATIN A4 IC50 = 540.0 nM 6.27
CHEMBL4782713 IC50 = 570.0 nM 6.24
CHEMBL1823159 IC50 = 590.0 nM 6.23