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Assay Detail

CHEMBL1645642

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

Binding
Inhibition of porcine brain tubulin polymerization by microtubule assembly assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Tubulin (CHEMBL2111354)
Type PROTEIN FAMILY
Organism Sus scrofa

Publication

Synthesis and biological evaluation of tubulysin D analogs related to stereoisomers of tubuvaline.
Shibue T, Okamoto I, Morita N, Morita H, Hirasawa Y, Hosoya T, Tamura O.
Bioorg Med Chem Lett (2011) 21 : 431 -434
PubMed 21106374 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.68 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1643765 11-EPI-TUBULYSIN D 1 5.85
CHEMBL159 VINBLASTINE 4.0 1 5.80
CHEMBL1643766 13-EPI-TUBULYSIN D 1 5.77
CHEMBL455213 TUBULYSIN D 1 5.77
CHEMBL1643767 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1643765 11-EPI-TUBULYSIN D IC50 = 1400.0 nM 5.85
CHEMBL159 VINBLASTINE IC50 = 1600.0 nM 5.80
CHEMBL1643766 13-EPI-TUBULYSIN D IC50 = 1700.0 nM 5.77
CHEMBL455213 TUBULYSIN D IC50 = 1700.0 nM 5.77
CHEMBL1643767 IC50 = 6300.0 nM 5.20