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Assay Detail

CHEMBL949274

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Binding
Inhibition of bovine tubulin polymerization after 20 mins
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

Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors.
Romagnoli R, Baraldi PG, Sarkar T, Carrion MD, Cara CL, Cruz-Lopez O, Preti D, Tabrizi MA, Tolomeo M, Grimaudo S, Di Cristina A, Zonta N, Balzarini J, Brancale A, Hsieh HP, Hamel E.
J Med Chem (2008) 51 : 1464 -1468
PubMed 18260616 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.30 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.92
CHEMBL272460 1 5.85
CHEMBL227027 1 5.68
CHEMBL364123 1 5.54
CHEMBL271388 1 5.34
CHEMBL270289 1 5.19
CHEMBL272459 1 5.15
CHEMBL410703 1 5.08
CHEMBL270096 1 5.00
CHEMBL270694 1 4.82
CHEMBL409539 1 4.75
CHEMBL271171 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67 COMBRETASTATIN A4 IC50 = 1200.0 nM 5.92
CHEMBL272460 IC50 = 1400.0 nM 5.85
CHEMBL227027 IC50 = 2100.0 nM 5.68
CHEMBL364123 IC50 = 2900.0 nM 5.54
CHEMBL271388 IC50 = 4600.0 nM 5.34
CHEMBL270289 IC50 = 6400.0 nM 5.19
CHEMBL272459 IC50 = 7100.0 nM 5.15
CHEMBL410703 IC50 = 8400.0 nM 5.08
CHEMBL270096 IC50 = 10000.0 nM 5.00
CHEMBL270694 IC50 = 15000.0 nM 4.82
CHEMBL409539 IC50 = 18000.0 nM 4.75
CHEMBL271171 IC50 > 40000.0 nM -