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Assay Detail

CHEMBL2045967

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

Binding
Inhibition of recombinant AKR1B10 assessed as NADP+ dependent reduction of DL-glyceraldehyde by fluorescence assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Aldo-keto reductase family 1 member B10 (CHEMBL5983)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17β-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships.
Adeniji AO, Twenter BM, Byrns MC, Jin Y, Chen M, Winkler JD, Penning TM.
J Med Chem (2012) 55 : 2311 -2323
PubMed 22263837 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.74 5.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10372 ZOPOLRESTAT 2.0 1 5.63
CHEMBL1682205 1 4.82
CHEMBL2041554 1 4.79
CHEMBL1682201 1 4.43
CHEMBL2041556 1 4.41
CHEMBL1682200 1 4.34
CHEMBL1682202 1 -
CHEMBL1682203 1 -
CHEMBL1682204 1 -
CHEMBL2041555 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10372 ZOPOLRESTAT IC50 = 2360.0 nM 5.63
CHEMBL1682205 IC50 = 15000.0 nM 4.82
CHEMBL2041554 IC50 = 16200.0 nM 4.79
CHEMBL1682201 IC50 = 37100.0 nM 4.43
CHEMBL2041556 IC50 = 39300.0 nM 4.41
CHEMBL1682200 IC50 = 46000.0 nM 4.34
CHEMBL1682202 IC50 > 50000.0 nM -
CHEMBL1682203 IC50 - -
CHEMBL1682204 IC50 > 50000.0 nM -
CHEMBL2041555 IC50 - -