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Assay Detail

CHEMBL2026545

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

Binding
Inhibition of bovine brain tubulin polymerization by thermostatic spectrophotometer
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
Yamazaki Y, Tanaka K, Nicholson B, Deyanat-Yazdi G, Potts B, Yoshida T, Oda A, Kitagawa T, Orikasa S, Kiso Y, Yasui H, Akamatsu M, Chinen T, Usui T, Shinozaki Y, Yakushiji F, Miller BR, Neuteboom S, Palladino M, Kanoh K, Lloyd GK, Hayashi Y.
J Med Chem (2012) 55 : 1056 -1071
PubMed 22185476 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.03 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2024544 1 6.29
CHEMBL2022198 1 6.26
CHEMBL67 COMBRETASTATIN A4 -1.0 1 6.26
CHEMBL2024561 1 6.12
CHEMBL1096380 PLINABULIN 3.0 1 5.88
CHEMBL107 COLCHICINE 4.0 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2024544 IC50 = 510.0 nM 6.29
CHEMBL2022198 IC50 = 550.0 nM 6.26
CHEMBL67 COMBRETASTATIN A4 IC50 = 550.0 nM 6.26
CHEMBL2024561 IC50 = 760.0 nM 6.12
CHEMBL1096380 PLINABULIN IC50 = 1310.0 nM 5.88
CHEMBL107 COLCHICINE IC50 = 4120.0 nM 5.38