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Assay Detail

CHEMBL1286930

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Functional
Antiproliferative activity against human SKOV3 cells expressing MDR1-6/6 by sulforhodamine B assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SK-OV-3
Confidence 1 — Organism
Curated By Autocuration

Target

SK-OV-3 (CHEMBL614925)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and discovery of water-soluble microtubule targeting agents that bind to the colchicine site on tubulin and circumvent Pgp mediated resistance.
Gangjee A, Zhao Y, Lin L, Raghavan S, Roberts EG, Risinger AL, Hamel E, Mooberry SL.
J Med Chem (2010) 53 : 8116 -8128
PubMed 20973488 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.62 8.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1206232 FOSBRETABULIN 3.0 1 8.18
CHEMBL1277064 1 7.35
CHEMBL1275943 1 6.36
CHEMBL299613 2-METHOXYESTRADIOL 2.0 1 5.64
CHEMBL428647 PACLITAXEL 4.0 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1206232 FOSBRETABULIN IC50 = 6.6 nM 8.18
CHEMBL1277064 IC50 = 44.4 nM 7.35
CHEMBL1275943 IC50 = 435.0 nM 6.36
CHEMBL299613 2-METHOXYESTRADIOL IC50 = 2268.0 nM 5.64
CHEMBL428647 PACLITAXEL IC50 = 2600.0 nM 5.58