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Assay Detail

CHEMBL5381806

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

Functional
Reversal of vinorelbine resistance in human KB cells assessed as reduction in cell viability incubated for 72 hrs in presence of vinorelbine (Rvb = 7.4+/-2.2 nM)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

KB (CHEMBL398)
Type CELL-LINE
Organism Homo sapiens

Publication

Modular Biomimetic Strategy Enabled Discovery of Simplified Pseudo-Natural Macrocyclic P-Glycoprotein Inhibitors Capable of Overcoming Multidrug Resistance.
Liu B, Yu X, Liu L, Wang L, Wang J, Huang Q, Xu Z, Luo C, Lou L, Huang W, Yang W.
J Med Chem (2023) 66 : 2550 -2565
PubMed 36728755 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.72 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5399206 1 9.15
CHEMBL5437817 1 8.66
CHEMBL6966 VERAPAMIL 4.0 1 8.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5399206 IC50 = 0.7 nM 9.15
CHEMBL5437817 IC50 = 2.2 nM 8.66
CHEMBL6966 VERAPAMIL IC50 = 4.4 nM 8.36