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Assay Detail

CHEMBL1004565

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Binding
Inhibition of tubulin polymerization
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-6-substituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives as antimitotic agents and inhibitors of tubulin polymerization.
Romagnoli R, Baraldi PG, Carrion MD, Cruz-Lopez O, Cara CL, Tolomeo M, Grimaudo S, Di Cristina A, Pipitone MR, Balzarini J, Kandil S, Brancale A, Sarkar T, Hamel E.
Bioorg Med Chem Lett (2008) 18 : 5041 -5045
PubMed 18725179 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.87 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL496320 1 6.22
CHEMBL524986 1 6.22
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.92
CHEMBL447202 1 5.72
CHEMBL189355 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL496320 IC50 = 600.0 nM 6.22
CHEMBL524986 IC50 = 600.0 nM 6.22
CHEMBL67 COMBRETASTATIN A4 IC50 = 1200.0 nM 5.92
CHEMBL447202 IC50 = 1900.0 nM 5.72
CHEMBL189355 IC50 = 5400.0 nM 5.27