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Assay Detail

CHEMBL3299992

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Functional
Antiproliferative activity against human HeLa cells expressing beta3-tubulin
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HeLa
Confidence 1 — Organism
Curated By Autocuration

Target

HeLa (CHEMBL399)
Type CELL-LINE
Organism Homo sapiens

Publication

The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
Zhang X, Raghavan S, Ihnat M, Thorpe JE, Disch BC, Bastian A, Bailey-Downs LC, Dybdal-Hargreaves NF, Rohena CC, Hamel E, Mooberry SL, Gangjee A.
Bioorg Med Chem (2014) 22 : 3753 -3772
PubMed 24890652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.80 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL428647 PACLITAXEL 4.0 1 8.00
CHEMBL3297898 1 7.57
CHEMBL3298000 1 7.35
CHEMBL3297899 1 6.69
CHEMBL3297900 1 5.82
CHEMBL3297999 1 5.39
CHEMBL3297998 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL428647 PACLITAXEL IC50 = 10.0 nM 8.00
CHEMBL3297898 IC50 = 27.2 nM 7.57
CHEMBL3298000 IC50 = 44.7 nM 7.35
CHEMBL3297899 IC50 = 205.6 nM 6.69
CHEMBL3297900 IC50 = 1500.0 nM 5.82
CHEMBL3297999 IC50 = 4070.0 nM 5.39
CHEMBL3297998 IC50 > 10000.0 nM -