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Assay Detail

CHEMBL935531

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

Functional
Cytotoxicity against human H460 cells under hypoxic condition after 2 hrs by Alamar blue staining assay
8
Total Activities
8
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 Autocuration

Target

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

Publication

Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
Duan JX, Jiao H, Kaizerman J, Stanton T, Evans JW, Lan L, Lorente G, Banica M, Jung D, Wang J, Ma H, Li X, Yang Z, Hoffman RM, Ammons WS, Hart CP, Matteucci M.
J Med Chem (2008) 51 : 2412 -2420
PubMed 18257544 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.52 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260046 EVOFOSFAMIDE 3.0 1 7.72
CHEMBL260427 1 7.08
CHEMBL404776 1 6.96
CHEMBL408385 1 6.92
CHEMBL261442 1 6.68
CHEMBL72793 1 6.58
CHEMBL403718 1 5.24
CHEMBL50882 TIRAPAZAMINE 3.0 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260046 EVOFOSFAMIDE IC50 = 19.0 nM 7.72
CHEMBL260427 IC50 = 83.0 nM 7.08
CHEMBL404776 IC50 = 110.0 nM 6.96
CHEMBL408385 IC50 = 120.0 nM 6.92
CHEMBL261442 IC50 = 210.0 nM 6.68
CHEMBL72793 IC50 = 260.0 nM 6.58
CHEMBL403718 IC50 = 5700.0 nM 5.24
CHEMBL50882 TIRAPAZAMINE IC50 = 11000.0 nM 4.96