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Assay Detail

CHEMBL4142928

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

Binding
Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition measured after 20 mins by spectrophotometric analysis
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

Targeting tubulin polymerization by novel 7-aryl-pyrroloquinolinones: Synthesis, biological activity and SARs.
Bortolozzi R, Mattiuzzo E, Dal Pra M, Sturlese M, Moro S, Hamel E, Carta D, Viola G, Ferlin MG.
Eur J Med Chem (2018) 143 : 244 -258
PubMed 29197729 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.78 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67 COMBRETASTATIN A4 -1.0 1 6.19
CHEMBL4163970 1 6.08
CHEMBL4173408 1 6.00
CHEMBL4162100 1 5.96
CHEMBL4159445 1 5.21
CHEMBL4167349 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67 COMBRETASTATIN A4 IC50 = 640.0 nM 6.19
CHEMBL4163970 IC50 = 840.0 nM 6.08
CHEMBL4173408 IC50 = 990.0 nM 6.00
CHEMBL4162100 IC50 = 1100.0 nM 5.96
CHEMBL4159445 IC50 = 6200.0 nM 5.21
CHEMBL4167349 IC50 = 6200.0 nM 5.21