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Assay Detail

CHEMBL683167

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

Functional
Inhibitory activity against drug resistant H69/LX4 line overexpressing P-glycoprotein
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H69
Confidence 1 — Organism
Curated By Expert

Target

NCI-H69 (CHEMBL614805)
Type CELL-LINE
Organism Homo sapiens

Publication

Structure-activity relationships for pyrido-, imidazo-, pyrazolo-, pyrazino-, and pyrrolophenazinecarboxamides as topoisomerase-targeted anticancer agents.
Gamage SA, Spicer JA, Rewcastle GW, Milton J, Sohal S, Dangerfield W, Mistry P, Vicker N, Charlton PA, Denny WA.
J Med Chem (2002) 45 : 740 -743
PubMed 11806725 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 8.72 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL162885 1 9.19
CHEMBL162739 1 9.04
CHEMBL353127 1 9.02
CHEMBL350147 1 8.98
CHEMBL355827 1 8.92
CHEMBL162781 1 8.92
CHEMBL349474 1 8.92
CHEMBL351740 1 8.92
CHEMBL162987 1 8.92
CHEMBL165348 1 8.92
CHEMBL163525 1 8.89
CHEMBL162451 1 8.85
CHEMBL163577 1 8.82
CHEMBL351239 1 8.77
CHEMBL162112 1 8.72
CHEMBL163072 1 8.68
CHEMBL163609 1 8.49
CHEMBL433703 1 8.35
CHEMBL351244 1 8.28
CHEMBL53463 DOXORUBICIN 4.0 1 6.86
CHEMBL163314 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL162885 IC50 = 0.64 nM 9.19
CHEMBL162739 IC50 = 0.92 nM 9.04
CHEMBL353127 IC50 = 0.95 nM 9.02
CHEMBL350147 IC50 = 1.05 nM 8.98
CHEMBL355827 IC50 = 1.2 nM 8.92
CHEMBL162781 IC50 = 1.2 nM 8.92
CHEMBL349474 IC50 = 1.2 nM 8.92
CHEMBL351740 IC50 = 1.2 nM 8.92
CHEMBL162987 IC50 = 1.2 nM 8.92
CHEMBL165348 IC50 = 1.2 nM 8.92
CHEMBL163525 IC50 = 1.3 nM 8.89
CHEMBL162451 IC50 = 1.4 nM 8.85
CHEMBL163577 IC50 = 1.5 nM 8.82
CHEMBL351239 IC50 = 1.7 nM 8.77
CHEMBL162112 IC50 = 1.9 nM 8.72
CHEMBL163072 IC50 = 2.1 nM 8.68
CHEMBL163609 IC50 = 3.2 nM 8.49
CHEMBL433703 IC50 = 4.5 nM 8.35
CHEMBL351244 IC50 = 5.2 nM 8.28
CHEMBL53463 DOXORUBICIN IC50 = 137.0 nM 6.86
CHEMBL163314 IC50 > 4.0 nM -