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Assay Detail

CHEMBL5117698

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

Binding
Inhibition of tubulin polymerization in human HeLa cells assessed as microtubule network polymerization after 30 mins by immunofluorescence analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tubulin (CHEMBL2095182)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
Hauguel C, Ducellier S, Provot O, Ibrahim N, Lamaa D, Balcerowiak C, Letribot B, Nascimento M, Blanchard V, Askenatzis L, Levaique H, Bignon J, Baschieri F, Bauvais C, Bollot G, Renko D, Deroussent A, Prost B, Laisne MC, Michallet S, Lafanechère L, Papot S, Montagnac G, Tran C, Alami M, Apcher S, Hamze A.
Eur J Med Chem (2022) 240 : 114573 -114573
PubMed 35797900 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.15 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67 COMBRETASTATIN A4 -1.0 1 8.52
CHEMBL498271 1 8.22
CHEMBL5183440 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67 COMBRETASTATIN A4 IC50 = 3.0 nM 8.52
CHEMBL498271 IC50 = 6.0 nM 8.22
CHEMBL5183440 IC50 = 20.0 nM 7.70