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Assay Detail

CHEMBL770794

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

Functional
Cytotoxicity against human lymphoblast tumor cell line RPM18402
10
Total Activities
10
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 Intermediate

Target

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

Publication

Diaza- and triazachrysenes: potent topoisomerase-targeting agents with exceptional antitumor activity against the human tumor xenograft, MDA-MB-435.
Ruchelman AL, Singh SK, Wu X, Ray A, Yang JM, Li TK, Liu A, Liu LF, LaVoie EJ.
Bioorg Med Chem Lett (2002) 12 : 3333 -3336
PubMed 12392745 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.46 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71086 1 9.00
CHEMBL70790 1 8.70
CHEMBL113970 1 8.40
CHEMBL326615 1 8.00
CHEMBL84 TOPOTECAN 4.0 1 7.92
CHEMBL113338 1 6.82
CHEMBL452231 TENIPOSIDE 4.0 1 6.66
CHEMBL113470 1 6.58
CHEMBL321593 1 6.24
CHEMBL331376 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71086 IC50 = 1.0 nM 9.00
CHEMBL70790 IC50 = 2.0 nM 8.70
CHEMBL113970 IC50 = 4.0 nM 8.40
CHEMBL326615 IC50 = 10.0 nM 8.00
CHEMBL84 TOPOTECAN IC50 = 12.0 nM 7.92
CHEMBL113338 IC50 = 150.0 nM 6.82
CHEMBL452231 TENIPOSIDE IC50 = 220.0 nM 6.66
CHEMBL113470 IC50 = 260.0 nM 6.58
CHEMBL321593 IC50 = 570.0 nM 6.24
CHEMBL331376 IC50 = 570.0 nM 6.24