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Assay Detail

CHEMBL818979

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

Functional
Inhibition of glutamate-dependent tubulin polymerization at 30 degrees C(0.25 mM MgCl2)
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Bos taurus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Tubulin (CHEMBL2094134)
Type PROTEIN FAMILY
Organism Bos taurus

Publication

Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions.
Getahun Z, Jurd L, Chu PS, Lin CM, Hamel E.
J Med Chem (1992) 35 : 1058 -1067
PubMed 1552500 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.58 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18981 THIOCOLCHICINE 1 6.19
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.96
CHEMBL10519 1 5.92
CHEMBL10557 1 5.80
CHEMBL10144 1 5.75
CHEMBL10642 1 5.72
CHEMBL274212 1 5.70
CHEMBL10121 1 5.64
CHEMBL10703 1 5.60
CHEMBL275976 1 5.57
CHEMBL10215 1 5.52
CHEMBL273261 1 5.42
CHEMBL10686 1 5.42
CHEMBL10559 1 5.41
CHEMBL10127 1 5.36
CHEMBL10405 1 5.27
CHEMBL10185 1 5.12
CHEMBL269215 1 5.06
CHEMBL10255 1 -
CHEMBL10653 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18981 THIOCOLCHICINE IC50 = 640.0 nM 6.19
CHEMBL67 COMBRETASTATIN A4 IC50 = 1100.0 nM 5.96
CHEMBL10519 IC50 = 1200.0 nM 5.92
CHEMBL10557 IC50 = 1600.0 nM 5.80
CHEMBL10144 IC50 = 1800.0 nM 5.75
CHEMBL10642 IC50 = 1900.0 nM 5.72
CHEMBL274212 IC50 = 2000.0 nM 5.70
CHEMBL10121 IC50 = 2300.0 nM 5.64
CHEMBL10703 IC50 = 2500.0 nM 5.60
CHEMBL275976 IC50 = 2700.0 nM 5.57
CHEMBL10215 IC50 = 3000.0 nM 5.52
CHEMBL273261 IC50 = 3800.0 nM 5.42
CHEMBL10686 IC50 = 3800.0 nM 5.42
CHEMBL10559 IC50 = 3900.0 nM 5.41
CHEMBL10127 IC50 = 4400.0 nM 5.36
CHEMBL10405 IC50 = 5400.0 nM 5.27
CHEMBL10185 IC50 = 7500.0 nM 5.12
CHEMBL269215 IC50 = 8800.0 nM 5.06
CHEMBL10255 IC50 > 40000.0 nM -
CHEMBL10653 IC50 > 40000.0 nM -