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Assay Detail

CHEMBL5381802

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

Functional
Reversal of vinorelbine resistance in human KBv200 cells assessed as reduction in cell viability incubated for 72 hrs in presence of vinorelbine (Rvb = 224 to 228.30 nM)
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KBv200
Confidence 1 — Organism
Curated By Autocuration

Target

KBv200 (CHEMBL5465447)
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 33 8.32 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5399206 1 10.70
CHEMBL5399548 1 10.30
CHEMBL5440498 1 9.68
CHEMBL5405970 1 9.52
CHEMBL5411100 1 9.42
CHEMBL5438378 1 9.40
CHEMBL5401184 1 9.38
CHEMBL5414613 1 9.36
CHEMBL5412964 1 9.26
CHEMBL5437817 1 9.13
CHEMBL5423696 1 8.95
CHEMBL5400937 1 8.92
CHEMBL5424930 1 8.91
CHEMBL5415612 1 8.81
CHEMBL5436836 1 8.75
CHEMBL5409040 1 8.45
CHEMBL5440933 1 8.44
CHEMBL5394735 1 8.44
CHEMBL5422705 1 8.43
CHEMBL5401230 1 8.34
CHEMBL6966 VERAPAMIL 4.0 1 8.16
CHEMBL5427928 1 8.06
CHEMBL5394304 1 7.61
CHEMBL5424931 1 7.33
CHEMBL5422663 1 6.90
CHEMBL5439986 1 6.85
CHEMBL5418928 1 6.85
CHEMBL5419588 1 6.82
CHEMBL5436774 1 6.77
CHEMBL5430656 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5399206 IC50 = 0.02 nM 10.70
CHEMBL5399548 IC50 = 0.05 nM 10.30
CHEMBL5440498 IC50 = 0.21 nM 9.68
CHEMBL5405970 IC50 = 0.3 nM 9.52
CHEMBL5411100 IC50 = 0.38 nM 9.42
CHEMBL5438378 IC50 = 0.4 nM 9.40
CHEMBL5401184 IC50 = 0.42 nM 9.38
CHEMBL5414613 IC50 = 0.44 nM 9.36
CHEMBL5412964 IC50 = 0.55 nM 9.26
CHEMBL5437817 IC50 = 0.74 nM 9.13
CHEMBL5423696 IC50 = 1.13 nM 8.95
CHEMBL5400937 IC50 = 1.19 nM 8.92
CHEMBL5424930 IC50 = 1.24 nM 8.91
CHEMBL5415612 IC50 = 1.54 nM 8.81
CHEMBL5436836 IC50 = 1.76 nM 8.75
CHEMBL5409040 IC50 = 3.58 nM 8.45
CHEMBL5440933 IC50 = 3.65 nM 8.44
CHEMBL5394735 IC50 = 3.64 nM 8.44
CHEMBL5422705 IC50 = 3.76 nM 8.43
CHEMBL5401230 IC50 = 4.57 nM 8.34
CHEMBL6966 VERAPAMIL IC50 = 6.96 nM 8.16
CHEMBL5427928 IC50 = 8.63 nM 8.06
CHEMBL5394304 IC50 = 24.48 nM 7.61
CHEMBL5424931 IC50 = 46.64 nM 7.33
CHEMBL5422663 IC50 = 126.6 nM 6.90
CHEMBL5439986 IC50 = 139.9 nM 6.85
CHEMBL5418928 IC50 = 140.4 nM 6.85
CHEMBL5419588 IC50 = 152.3 nM 6.82
CHEMBL5436774 IC50 = 169.4 nM 6.77
CHEMBL5430656 IC50 = 199.0 nM 6.70
CHEMBL5408442 IC50 = 209.5 nM 6.68
CHEMBL5440594 IC50 = 247.8 nM 6.61
CHEMBL5433471 IC50 = 289.2 nM 6.54