Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4430163

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

Binding
Inhibition of AKR1C3 in human KG1a cells assessed as potentiation of etoposide-induced cytotoxicity by measuring etoposide IC50 cotreated at 72 hrs by MTS assay (Rvb = 6.70 uM)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aldo-keto reductase family 1 member C3 (CHEMBL4681)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective AKR1C3 Inhibitors Potentiate Chemotherapeutic Activity in Multiple Acute Myeloid Leukemia (AML) Cell Lines.
Verma K, Zang T, Gupta N, Penning TM, Trippier PC.
ACS Med Chem Lett (2016) 7 : 774 -779
PubMed 27563402 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.71 5.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4457540 1 5.97
CHEMBL4470997 1 5.61
CHEMBL4441387 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4457540 IC50 = 1080.0 nM 5.97
CHEMBL4470997 IC50 = 2470.0 nM 5.61
CHEMBL4441387 IC50 = 2880.0 nM 5.54