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Assay Detail

CHEMBL824947

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

Functional
Concentration required to inhibit cell proliferation in KBV-1 tumor cell line; overexpress MDR1
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

KB (CHEMBL398)
Type CELL-LINE
Organism Homo sapiens

Publication

Dimethoxybenzo[i]phenanthridine-12-carboxylic acid derivatives and 6H-dibenzo[c,h][2,6]naphthyridin-5-ones with potent topoisomerase I-targeting activity and cytotoxicity.
Ruchelman AL, Zhu S, Zhou N, Liu A, Liu LF, LaVoie EJ.
Bioorg Med Chem Lett (2004) 14 : 5585 -5589
PubMed 15482929 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.79 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70790 1 8.30
CHEMBL361041 1 8.22
CHEMBL187471 1 8.15
CHEMBL186260 1 8.00
CHEMBL65 CAMPTOTHECIN -1.0 1 7.70
CHEMBL84 TOPOTECAN 4.0 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70790 IC50 = 5.0 nM 8.30
CHEMBL361041 IC50 = 6.0 nM 8.22
CHEMBL187471 IC50 = 7.0 nM 8.15
CHEMBL186260 IC50 = 10.0 nM 8.00
CHEMBL65 CAMPTOTHECIN IC50 = 20.0 nM 7.70
CHEMBL84 TOPOTECAN IC50 = 440.0 nM 6.36