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Assay Detail

CHEMBL4339404

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

Binding
Inhibition of recombinant full-length human N-terminal His6-tagged AKR1C3 expressed in Escherichia coli BL21 (DE3) using phenanthrenequinone as substrate in presence of NADPH generating system
2
Total Activities
2
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
Ki 2 4.62 4.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL449572 JASMONIC ACID 1 4.62
CHEMBL2139332 (-)-JASMONIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL449572 JASMONIC ACID Ki = 24000.0 nM 4.62
CHEMBL2139332 (-)-JASMONIC ACID Ki = 153000.0 nM -