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Assay Detail

CHEMBL3404073

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

Functional
Antiproliferative activity against human SKOV3-MDR1-M6/6 cells overexpressing wild type beta3 tubulin after 48 hrs by sulforhodamine B assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SKOV3-MDR1-M6/6
Confidence 1 — Organism
Curated By Autocuration

Publication

The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
Zhang X, Raghavan S, Ihnat M, Hamel E, Zammiello C, Bastian A, Mooberry SL, Gangjee A.
Bioorg Med Chem (2015) 23 : 2408 -2423
PubMed 25882519 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.00 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67 COMBRETASTATIN A4 -1.0 1 8.52
CHEMBL3403517 1 7.71
CHEMBL3403519 1 7.51
CHEMBL3297898 1 7.20
CHEMBL3403513 1 6.81
CHEMBL3403510 1 6.69
CHEMBL3403509 1 6.32
CHEMBL3403514 1 6.29
CHEMBL428647 PACLITAXEL 4.0 1 5.92
CHEMBL3403512 1 -
CHEMBL3403511 1 -
CHEMBL3403515 1 -
CHEMBL3403516 1 -
CHEMBL3403518 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67 COMBRETASTATIN A4 IC50 = 3.0 nM 8.52
CHEMBL3403517 IC50 = 19.4 nM 7.71
CHEMBL3403519 IC50 = 30.8 nM 7.51
CHEMBL3297898 IC50 = 63.3 nM 7.20
CHEMBL3403513 IC50 = 155.2 nM 6.81
CHEMBL3403510 IC50 = 203.3 nM 6.69
CHEMBL3403509 IC50 = 482.9 nM 6.32
CHEMBL3403514 IC50 = 509.0 nM 6.29
CHEMBL428647 PACLITAXEL IC50 = 1187.2 nM 5.92
CHEMBL3403512 IC50 - -
CHEMBL3403511 IC50 - -
CHEMBL3403515 IC50 - -
CHEMBL3403516 IC50 - -
CHEMBL3403518 IC50 - -