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Assay Detail

CHEMBL4180707

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

Functional
Cytotoxicity against human NCI-H460 cells after 24 hrs under hypoxic condition by luminescence-based Cell-Titer Glo assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H460
Confidence 1 — Organism
Curated By Intermediate

Target

NCI-H460 (CHEMBL396)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of pyrrolobenzodiazepine-containing hypoxia-activated prodrugs.
Dragovich PS, Broccatelli F, Chen J, Fan P, Le H, Mao W, Pillow TH, Polson AG, Wai J, Xu Z, Yao H, Zhang D.
Bioorg Med Chem Lett (2017) 27 : 5300 -5304
PubMed 29079474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.89 10.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16932 1 10.21
CHEMBL1165777 1 9.27
CHEMBL4216973 1 8.96
CHEMBL260046 EVOFOSFAMIDE 3.0 1 8.03
CHEMBL4209698 1 7.77
CHEMBL54905 1 6.56
CHEMBL4209619 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16932 IC50 = 0.062 nM 10.21
CHEMBL1165777 IC50 = 0.54 nM 9.27
CHEMBL4216973 IC50 = 1.1 nM 8.96
CHEMBL260046 EVOFOSFAMIDE IC50 = 9.3 nM 8.03
CHEMBL4209698 IC50 = 17.0 nM 7.77
CHEMBL54905 IC50 = 273.0 nM 6.56
CHEMBL4209619 IC50 = 35000.0 nM 4.46