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Assay Detail

CHEMBL770850

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

Functional
Cytotoxic activity against human lymphoblast tumor cell line RPMI8402 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
Cell Type RPMI 8402
Confidence 1 — Organism
Curated By Expert

Target

RPMI 8402 (CHEMBL612517)
Type CELL-LINE
Organism Homo sapiens

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 7.24 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71086 1 9.00
CHEMBL70790 1 8.70
CHEMBL309355 1 8.70
CHEMBL72772 1 8.52
CHEMBL65 CAMPTOTHECIN -1.0 1 8.30
CHEMBL84 TOPOTECAN 4.0 1 7.92
CHEMBL309352 1 7.60
CHEMBL415117 1 7.22
CHEMBL72223 1 7.10
CHEMBL452231 TENIPOSIDE 4.0 1 6.66
CHEMBL73950 1 6.62
CHEMBL72726 1 6.47
CHEMBL481 IRINOTECAN 4.0 1 6.24
CHEMBL306476 1 5.90
CHEMBL304505 1 5.52
CHEMBL424421 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71086 IC50 = 1.0 nM 9.00
CHEMBL70790 IC50 = 2.0 nM 8.70
CHEMBL309355 IC50 = 2.0 nM 8.70
CHEMBL72772 IC50 = 3.0 nM 8.52
CHEMBL65 CAMPTOTHECIN IC50 = 5.0 nM 8.30
CHEMBL84 TOPOTECAN IC50 = 12.0 nM 7.92
CHEMBL309352 IC50 = 25.0 nM 7.60
CHEMBL415117 IC50 = 60.0 nM 7.22
CHEMBL72223 IC50 = 80.0 nM 7.10
CHEMBL452231 TENIPOSIDE IC50 = 220.0 nM 6.66
CHEMBL73950 IC50 = 240.0 nM 6.62
CHEMBL72726 IC50 = 340.0 nM 6.47
CHEMBL481 IRINOTECAN IC50 = 570.0 nM 6.24
CHEMBL306476 IC50 = 1250.0 nM 5.90
CHEMBL304505 IC50 = 3000.0 nM 5.52
CHEMBL424421 IC50 = 4800.0 nM 5.32