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Assay Detail

CHEMBL861403

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

Functional
Cytotoxicity against HEK293 cells transfected with recombinant AOR by MTT assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Prostaglandin reductase 1 (CHEMBL4166)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Investigating the role of stereochemistry in the activity of anticancer acylfulvenes: synthesis, reductase-mediated bioactivation, and cellular toxicity.
Gong J, Neels JF, Yu X, Kensler TW, Peterson LA, Sturla SJ.
J Med Chem (2006) 49 : 2593 -2599
PubMed 16610802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.36 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118218 IROFULVEN 3.0 1 7.26
CHEMBL121987 ACYLFULVENE 1 7.02
CHEMBL380919 1 5.85
CHEMBL205439 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118218 IROFULVEN IC50 = 55.0 nM 7.26
CHEMBL121987 ACYLFULVENE IC50 = 95.0 nM 7.02
CHEMBL380919 IC50 = 1420.0 nM 5.85
CHEMBL205439 IC50 = 5000.0 nM 5.30