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Assay Detail

CHEMBL4339405

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

Binding
Inhibition of recombinant human AKR1C3 expressed in Escherichia coli BL21 (D3) using oracin as substrate measured after 30 mins in presence of NADPH generating system by HPLC method
1
Total Activities
1
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

Potent and Highly Selective Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors Act as Chemotherapeutic Potentiators in Acute Myeloid Leukemia and T-Cell Acute Lymphoblastic Leukemia.
Verma K, Zang T, Penning TM, Trippier PC.
J Med Chem (2019) 62 : 3590 -3616
PubMed 30836001 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.52 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75897 2'-HYDROXY-FLAVANONE 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75897 2'-HYDROXY-FLAVANONE IC50 = 300.0 nM 6.52