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Assay Detail

CHEMBL832762

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

Binding
Inhibition of tubulin polymerization upon incubation for 20 min at 30 degree C
19
Total Activities
19
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

Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
Pettit GR, Rhodes MR, Herald DL, Hamel E, Schmidt JM, Pettit RK.
J Med Chem (2005) 48 : 4087 -4099
PubMed 15943482 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.19 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL192860 1 5.96
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.92
CHEMBL192224 1 5.58
CHEMBL371487 1 5.55
CHEMBL192841 1 5.19
CHEMBL540358 1 5.12
CHEMBL195287 1 4.85
CHEMBL536726 1 4.70
CHEMBL191624 1 4.51
CHEMBL36455 E-COMBRETASTATIN A-4 1 4.48
CHEMBL535375 1 -
CHEMBL541122 1 -
CHEMBL537854 1 -
CHEMBL537189 1 -
CHEMBL536497 1 -
CHEMBL535601 1 -
CHEMBL195691 1 -
CHEMBL195219 1 -
CHEMBL192166 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL192860 IC50 = 1100.0 nM 5.96
CHEMBL67 COMBRETASTATIN A4 IC50 = 1200.0 nM 5.92
CHEMBL192224 IC50 = 2600.0 nM 5.58
CHEMBL371487 IC50 = 2800.0 nM 5.55
CHEMBL192841 IC50 = 6500.0 nM 5.19
CHEMBL540358 IC50 = 7600.0 nM 5.12
CHEMBL195287 IC50 = 14000.0 nM 4.85
CHEMBL536726 IC50 = 20000.0 nM 4.70
CHEMBL191624 IC50 = 31000.0 nM 4.51
CHEMBL36455 E-COMBRETASTATIN A-4 IC50 = 33000.0 nM 4.48
CHEMBL535375 IC50 > 40000.0 nM -
CHEMBL541122 IC50 > 40000.0 nM -
CHEMBL537854 IC50 > 40000.0 nM -
CHEMBL537189 IC50 > 40000.0 nM -
CHEMBL536497 IC50 > 40000.0 nM -
CHEMBL535601 IC50 > 40000.0 nM -
CHEMBL195691 IC50 > 40000.0 nM -
CHEMBL195219 IC50 > 40000.0 nM -
CHEMBL192166 IC50 > 40000.0 nM -