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Assay Detail

CHEMBL4392979

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

Functional
Cytotoxicity against human MDA-MB-468 cells incubated for 4 hrs under hypoxic condition followed by compound washout and measured after 5 days by SRB assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-MB-468
Confidence 1 — Organism
Curated By Autocuration

Target

MDA-MB-468 (CHEMBL614335)
Type CELL-LINE
Organism Homo sapiens

Publication

Prototyping kinase inhibitor-cytotoxin anticancer mutual prodrugs activated by tumour hypoxia: A chemical proof of concept study.
Sansom GN, Kirk NS, Guise CP, Anderson RF, Smaill JB, Patterson AV, Kelso MJ.
Bioorg Med Chem Lett (2019) 29 : 1215 -1219
PubMed 30885680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.93 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260046 EVOFOSFAMIDE 3.0 1 8.21
CHEMBL852 MELPHALAN 4.0 1 6.09
CHEMBL50882 TIRAPAZAMINE 3.0 1 5.88
CHEMBL4471736 1 5.13
CHEMBL917 FLOXURIDINE 4.0 1 4.34
CHEMBL4591106 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260046 EVOFOSFAMIDE IC50 = 6.2 nM 8.21
CHEMBL852 MELPHALAN IC50 = 810.0 nM 6.09
CHEMBL50882 TIRAPAZAMINE IC50 = 1304.0 nM 5.88
CHEMBL4471736 IC50 = 7380.0 nM 5.13
CHEMBL917 FLOXURIDINE IC50 = 45530.0 nM 4.34
CHEMBL4591106 IC50 = 247960.0 nM -