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Assay Detail

CHEMBL913147

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

Binding
Displacement of [3H]colchicine from bovine brain tubulin at 1 uM
10
Total Activities
10
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

Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization.
Romagnoli R, Baraldi PG, Carrion MD, Lopez Cara C, Preti D, Fruttarolo F, Pavani MG, Tabrizi MA, Tolomeo M, Grimaudo S, Di Cristina A, Balzarini J, Hadfield JA, Brancale A, Hamel E.
J Med Chem (2007) 50 : 2273 -2277
PubMed 17419607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.41 4.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371795 1 4.82
CHEMBL223057 1 4.80
CHEMBL227835 1 4.72
CHEMBL189355 1 4.60
CHEMBL227027 1 4.41
CHEMBL227987 1 4.22
CHEMBL190320 1 4.22
CHEMBL227656 1 4.18
CHEMBL67 COMBRETASTATIN A4 -1.0 1 4.07
CHEMBL387717 1 4.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371795 IC50 = 15000.0 nM 4.82
CHEMBL223057 IC50 = 16000.0 nM 4.80
CHEMBL227835 IC50 = 19000.0 nM 4.72
CHEMBL189355 IC50 = 25000.0 nM 4.60
CHEMBL227027 IC50 = 39000.0 nM 4.41
CHEMBL227987 IC50 = 60000.0 nM 4.22
CHEMBL190320 IC50 = 60000.0 nM 4.22
CHEMBL227656 IC50 = 66000.0 nM 4.18
CHEMBL67 COMBRETASTATIN A4 IC50 = 86000.0 nM 4.07
CHEMBL387717 IC50 = 91000.0 nM 4.04