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Assay Detail

CHEMBL876479

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

Binding
Inhibition of tubulin polymerization
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Tubulin beta-1 chain (CHEMBL1915)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents.
Liou JP, Chang YL, Kuo FM, Chang CW, Tseng HY, Wang CC, Yang YN, Chang JY, Lee SJ, Hsieh HP.
J Med Chem (2004) 47 : 4247 -4257
PubMed 15293996 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.65 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL363063 1 6.05
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.69
CHEMBL364123 1 5.66
CHEMBL189189 1 5.57
CHEMBL186106 1 5.48
CHEMBL363956 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL363063 IC50 = 900.0 nM 6.05
CHEMBL67 COMBRETASTATIN A4 IC50 = 2030.0 nM 5.69
CHEMBL364123 IC50 = 2180.0 nM 5.66
CHEMBL189189 IC50 = 2690.0 nM 5.57
CHEMBL186106 IC50 = 3310.0 nM 5.48
CHEMBL363956 IC50 = 3760.0 nM 5.42