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Assay Detail

CHEMBL1176994

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

Functional
Cytotoxicity against human HT-29 cells under aerobic condition after 5 days by SRB assay
11
Total Activities
11
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 Autocuration

Target

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

Publication

Hypoxic selectivity and solubility--investigating the properties of A-ring substituted nitro seco-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-ones (nitroCBIs) as hypoxia-activated prodrugs for antitumor therapy.
Tercel M, Yang S, Atwell GJ, Smith E, Gu Y, Anderson RF, Denny WA, Wilson WR, Pruijn FB.
Bioorg Med Chem (2010) 18 : 4997 -5006
PubMed 20580559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.88 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1171845 1 7.62
CHEMBL585201 1 7.46
CHEMBL1172173 1 6.14
CHEMBL1171982 1 5.96
CHEMBL1172175 1 5.89
CHEMBL1172174 1 5.82
CHEMBL1172218 1 5.75
CHEMBL1171844 1 5.57
CHEMBL570414 1 5.34
CHEMBL1172008 1 4.62
CHEMBL1172009 1 4.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1171845 IC50 = 24.0 nM 7.62
CHEMBL585201 IC50 = 35.0 nM 7.46
CHEMBL1172173 IC50 = 730.0 nM 6.14
CHEMBL1171982 IC50 = 1100.0 nM 5.96
CHEMBL1172175 IC50 = 1300.0 nM 5.89
CHEMBL1172174 IC50 = 1500.0 nM 5.82
CHEMBL1172218 IC50 = 1800.0 nM 5.75
CHEMBL1171844 IC50 = 2700.0 nM 5.57
CHEMBL570414 IC50 = 4600.0 nM 5.34
CHEMBL1172008 IC50 = 24000.0 nM 4.62
CHEMBL1172009 IC50 = 31000.0 nM 4.51