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Assay Detail

CHEMBL694339

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

Functional
Concentration required to kill hypoxic HT-29 human colon carcinoma cells in vitro
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-29
Confidence 1 — Organism
Curated By Intermediate

Target

HT-29 (CHEMBL384)
Type CELL-LINE
Organism Homo sapiens

Publication

DNA-targeted 1,2,4-benzotriazine 1,4-dioxides: potent analogues of the hypoxia-selective cytotoxin tirapazamine.
Hay MP, Pruijn FB, Gamage SA, Liyanage HD, Kovacs MS, Patterson AV, Wilson WR, Brown JM, Denny WA.
J Med Chem (2004) 47 : 475 -488
PubMed 14711317 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.80 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL436403 1 7.80
CHEMBL144115 1 7.75
CHEMBL344761 1 7.37
CHEMBL423373 1 7.19
CHEMBL143167 1 7.10
CHEMBL342956 1 7.02
CHEMBL144407 1 6.96
CHEMBL145788 1 6.92
CHEMBL144802 1 6.75
CHEMBL144932 1 6.23
CHEMBL144526 1 5.24
CHEMBL50882 TIRAPAZAMINE 3.0 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL436403 IC50 = 16.0 nM 7.80
CHEMBL144115 IC50 = 18.0 nM 7.75
CHEMBL344761 IC50 = 43.0 nM 7.37
CHEMBL423373 IC50 = 65.0 nM 7.19
CHEMBL143167 IC50 = 79.0 nM 7.10
CHEMBL342956 IC50 = 95.0 nM 7.02
CHEMBL144407 IC50 = 110.0 nM 6.96
CHEMBL145788 IC50 = 120.0 nM 6.92
CHEMBL144802 IC50 = 180.0 nM 6.75
CHEMBL144932 IC50 = 590.0 nM 6.23
CHEMBL144526 IC50 = 5700.0 nM 5.24
CHEMBL50882 TIRAPAZAMINE IC50 = 6200.0 nM 5.21