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Assay Detail

CHEMBL936594

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Binding
Inhibition of human recombinant aldose reductase
9
Total Activities
9
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 B1 (CHEMBL1900)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibition of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) by aldose reductase inhibitors.
Dhagat U, Endo S, Hara A, El-Kabbani O.
Bioorg Med Chem (2008) 16 : 3245 -3254
PubMed 18165015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.47 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL84446 FIDARESTAT 2.0 1 8.05
CHEMBL10372 ZOPOLRESTAT 2.0 1 7.52
CHEMBL436 TOLRESTAT 4.0 1 7.40
CHEMBL273910 MINALRESTAT 2.0 1 7.16
CHEMBL82242 QUERCITRIN 1 6.82
CHEMBL266497 SORBINIL 3.0 1 6.04
CHEMBL50 QUERCETIN 3.0 1 5.66
CHEMBL117 CHRYSIN 1 5.07
CHEMBL164 MYRICETIN 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL84446 FIDARESTAT IC50 = 9.0 nM 8.05
CHEMBL10372 ZOPOLRESTAT IC50 = 30.0 nM 7.52
CHEMBL436 TOLRESTAT IC50 = 40.0 nM 7.40
CHEMBL273910 MINALRESTAT IC50 = 70.0 nM 7.16
CHEMBL82242 QUERCITRIN IC50 = 150.0 nM 6.82
CHEMBL266497 SORBINIL IC50 = 910.0 nM 6.04
CHEMBL50 QUERCETIN IC50 = 2200.0 nM 5.66
CHEMBL117 CHRYSIN IC50 = 8500.0 nM 5.07
CHEMBL164 MYRICETIN IC50 = 29000.0 nM 4.54