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Assay Detail

CHEMBL3100250

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

Binding
Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition measured for 20 mins by turbidometric analysis
8
Total Activities
8
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

Concise synthesis and biological evaluation of 2-Aroyl-5-amino benzo[b]thiophene derivatives as a novel class of potent antimitotic agents.
Romagnoli R, Baraldi PG, Lopez-Cara C, Preti D, Aghazadeh Tabrizi M, Balzarini J, Bassetto M, Brancale A, Fu XH, Gao Y, Li J, Zhang SZ, Hamel E, Bortolozzi R, Basso G, Viola G.
J Med Chem (2013) 56 : 9296 -9309
PubMed 24164557 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.89 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3099864 1 6.32
CHEMBL3099862 1 6.28
CHEMBL3099863 1 6.17
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.92
CHEMBL3099861 1 5.89
CHEMBL227027 1 5.68
CHEMBL3099860 1 5.50
CHEMBL371795 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3099864 IC50 = 480.0 nM 6.32
CHEMBL3099862 IC50 = 520.0 nM 6.28
CHEMBL3099863 IC50 = 680.0 nM 6.17
CHEMBL67 COMBRETASTATIN A4 IC50 = 1200.0 nM 5.92
CHEMBL3099861 IC50 = 1300.0 nM 5.89
CHEMBL227027 IC50 = 2100.0 nM 5.68
CHEMBL3099860 IC50 = 3200.0 nM 5.50
CHEMBL371795 IC50 = 4200.0 nM 5.38