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Assay Detail

CHEMBL657453

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

Functional
Cytotoxic activity against human lymphoblast tumor cell line CPT-K5 after 4 days of treatment
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Nitro and amino substitution in the D-ring of 5-(2-dimethylaminoethyl)- 2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-ones: effect on topoisomerase-I targeting activity and cytotoxicity.
Singh SK, Ruchelman AL, Li TK, Liu A, Liu LF, LaVoie EJ.
J Med Chem (2003) 46 : 2254 -2257
PubMed 12747798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.90 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL452231 TENIPOSIDE 4.0 1 6.55
CHEMBL72772 1 6.48
CHEMBL72223 1 6.42
CHEMBL71086 1 6.22
CHEMBL70790 1 6.05
CHEMBL415117 1 6.02
CHEMBL309352 1 6.00
CHEMBL309355 1 5.55
CHEMBL72726 1 5.50
CHEMBL65 CAMPTOTHECIN -1.0 1 4.21
CHEMBL424421 1 -
CHEMBL73950 1 -
CHEMBL481 IRINOTECAN 4.0 1 -
CHEMBL306476 1 -
CHEMBL304505 1 -
CHEMBL84 TOPOTECAN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL452231 TENIPOSIDE IC50 = 280.0 nM 6.55
CHEMBL72772 IC50 = 330.0 nM 6.48
CHEMBL72223 IC50 = 380.0 nM 6.42
CHEMBL71086 IC50 = 600.0 nM 6.22
CHEMBL70790 IC50 = 900.0 nM 6.05
CHEMBL415117 IC50 = 950.0 nM 6.02
CHEMBL309352 IC50 = 1000.0 nM 6.00
CHEMBL309355 IC50 = 2800.0 nM 5.55
CHEMBL72726 IC50 = 3200.0 nM 5.50
CHEMBL65 CAMPTOTHECIN IC50 = 61000.0 nM 4.21
CHEMBL424421 IC50 > 10000.0 nM -
CHEMBL73950 IC50 > 10000.0 nM -
CHEMBL481 IRINOTECAN IC50 > 100000.0 nM -
CHEMBL306476 IC50 > 10000.0 nM -
CHEMBL304505 IC50 > 10000.0 nM -
CHEMBL84 TOPOTECAN IC50 > 50000.0 nM -