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Assay Detail

CHEMBL911786

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Functional
Inhibition of tubulin polymerization
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Tubulin (CHEMBL2095182)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors.
Romagnoli R, Baraldi PG, Remusat V, Carrion MD, Cara CL, Preti D, Fruttarolo F, Pavani MG, Tabrizi MA, Tolomeo M, Grimaudo S, Balzarini J, Jordan MA, Hamel E.
J Med Chem (2006) 49 : 6425 -6428
PubMed 17034150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.96 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426514 1 6.19
CHEMBL380060 1 6.10
CHEMBL212515 1 6.07
CHEMBL387263 1 6.01
CHEMBL210239 1 5.96
CHEMBL217134 1 5.96
CHEMBL218188 1 5.96
CHEMBL217797 1 5.96
CHEMBL209011 1 5.92
CHEMBL217256 1 5.92
CHEMBL410661 1 5.92
CHEMBL217472 1 5.92
CHEMBL379867 1 5.89
CHEMBL217301 1 5.89
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.85
CHEMBL217297 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426514 IC50 = 640.0 nM 6.19
CHEMBL380060 IC50 = 800.0 nM 6.10
CHEMBL212515 IC50 = 860.0 nM 6.07
CHEMBL387263 IC50 = 970.0 nM 6.01
CHEMBL210239 IC50 = 1100.0 nM 5.96
CHEMBL217134 IC50 = 1100.0 nM 5.96
CHEMBL218188 IC50 = 1100.0 nM 5.96
CHEMBL217797 IC50 = 1100.0 nM 5.96
CHEMBL209011 IC50 = 1200.0 nM 5.92
CHEMBL217256 IC50 = 1200.0 nM 5.92
CHEMBL410661 IC50 = 1200.0 nM 5.92
CHEMBL217472 IC50 = 1200.0 nM 5.92
CHEMBL379867 IC50 = 1300.0 nM 5.89
CHEMBL217301 IC50 = 1300.0 nM 5.89
CHEMBL67 COMBRETASTATIN A4 IC50 = 1400.0 nM 5.85
CHEMBL217297 IC50 = 1500.0 nM 5.82