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Assay Detail

CHEMBL837482

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

Functional
Concentration required to inhibit cell proliferation by 50% in KBH5.0 tumor cell line; overexpress BCRP
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KB 3-1
Confidence 1 — Organism
Curated By Intermediate

Target

KB 3-1 (CHEMBL614590)
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 7.09 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL186397 1 8.40
CHEMBL184515 1 7.52
CHEMBL184236 1 7.16
CHEMBL187426 1 6.96
CHEMBL187041 1 6.30
CHEMBL186690 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL186397 IC50 = 4.0 nM 8.40
CHEMBL184515 IC50 = 30.0 nM 7.52
CHEMBL184236 IC50 = 70.0 nM 7.16
CHEMBL187426 IC50 = 110.0 nM 6.96
CHEMBL187041 IC50 = 500.0 nM 6.30
CHEMBL186690 IC50 = 600.0 nM 6.22