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Assay Detail

CHEMBL4370288

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

Binding
Inhibition of bovine brain tubulin polymerization after 20 mins
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tubulin (CHEMBL2094134)
Type PROTEIN FAMILY
Organism Bos taurus

Publication

Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.
Romagnoli R, Prencipe F, Oliva P, Baraldi S, Baraldi PG, Schiaffino Ortega S, Chayah M, Kimatrai Salvador M, Lopez-Cara LC, Brancale A, Ferla S, Hamel E, Ronca R, Bortolozzi R, Mariotto E, Mattiuzzo E, Viola G.
J Med Chem (2019) 62 : 1274 -1290
PubMed 30633509 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.51 6.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4569885 1 6.15
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.92
CHEMBL4473768 1 5.60
CHEMBL4572443 1 5.60
CHEMBL4546122 1 5.55
CHEMBL4552482 1 5.48
CHEMBL4541014 1 5.00
CHEMBL4460381 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4569885 IC50 = 710.0 nM 6.15
CHEMBL67 COMBRETASTATIN A4 IC50 = 1200.0 nM 5.92
CHEMBL4473768 IC50 = 2500.0 nM 5.60
CHEMBL4572443 IC50 = 2500.0 nM 5.60
CHEMBL4546122 IC50 = 2800.0 nM 5.55
CHEMBL4552482 IC50 = 3300.0 nM 5.48
CHEMBL4541014 IC50 = 10000.0 nM 5.00
CHEMBL4460381 IC50 = 18000.0 nM 4.75