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Assay Detail

CHEMBL3404066

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

Binding
Induction of microtubule depolymerization in rat A10 cells after 18 hrs by indirect immunofluorescence assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type A10
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
EC50 14 6.52 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67 COMBRETASTATIN A4 -1.0 1 8.01
CHEMBL3403517 1 7.68
CHEMBL3297898 1 6.99
CHEMBL3403519 1 6.74
CHEMBL3403513 1 6.22
CHEMBL3403510 1 5.57
CHEMBL3403509 1 5.52
CHEMBL3403514 1 5.42
CHEMBL3403512 1 -
CHEMBL3403511 1 -
CHEMBL3403515 1 -
CHEMBL3403516 1 -
CHEMBL3403518 1 -
CHEMBL428647 PACLITAXEL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67 COMBRETASTATIN A4 EC50 = 9.8 nM 8.01
CHEMBL3403517 EC50 = 21.0 nM 7.68
CHEMBL3297898 EC50 = 103.0 nM 6.99
CHEMBL3403519 EC50 = 182.0 nM 6.74
CHEMBL3403513 EC50 = 606.0 nM 6.22
CHEMBL3403510 EC50 = 2719.0 nM 5.57
CHEMBL3403509 EC50 = 2994.0 nM 5.52
CHEMBL3403514 EC50 = 3786.0 nM 5.42
CHEMBL3403512 EC50 > 10000.0 nM -
CHEMBL3403511 EC50 > 10000.0 nM -
CHEMBL3403515 EC50 > 10000.0 nM -
CHEMBL3403516 EC50 > 10000.0 nM -
CHEMBL3403518 EC50 > 10000.0 nM -
CHEMBL428647 PACLITAXEL EC50 - -