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Assay Detail

CHEMBL1828322

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

Functional
Antiproliferative activity against MDR-1 overexpressing human 786-0 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type 786-0
Confidence 1 — Organism
Curated By Autocuration

Target

786-0 (CHEMBL613102)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
Flynn BL, Gill GS, Grobelny DW, Chaplin JH, Paul D, Leske AF, Lavranos TC, Chalmers DK, Charman SA, Kostewicz E, Shackleford DM, Morizzi J, Hamel E, Jung MK, Kremmidiotis G.
J Med Chem (2011) 54 : 6014 -6027
PubMed 21774499 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.13 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1823147 1 9.24
CHEMBL159 VINBLASTINE 4.0 1 8.35
CHEMBL428647 PACLITAXEL 4.0 1 7.51
CHEMBL90555 VINCRISTINE 4.0 1 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1823147 IC50 = 0.58 nM 9.24
CHEMBL159 VINBLASTINE IC50 = 4.5 nM 8.35
CHEMBL428647 PACLITAXEL IC50 = 31.0 nM 7.51
CHEMBL90555 VINCRISTINE IC50 = 37.0 nM 7.43