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Assay Detail

CHEMBL4180642

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

Binding
Inhibition of ALR1 in Wistar rat kidney assessed as reduction in NADPH consumption preincubated for 1 min followed by substrate addition measured after 4 mins by spectrophotometric analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aldo-keto reductase family 1 member B1 (CHEMBL2622)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure optimization of tetrahydropyridoindole-based aldose reductase inhibitors improved their efficacy and selectivity.
Majekova M, Ballekova J, Prnova M, Stefek M.
Bioorg Med Chem (2017) 25 : 6353 -6360
PubMed 29074349 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.82 5.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4219003 1 5.32
CHEMBL4216153 1 5.12
CHEMBL4206601 1 5.00
CHEMBL4207775 1 4.95
CHEMBL1897400 1 4.93
CHEMBL2391535 1 4.66
CHEMBL4207499 1 4.36
CHEMBL109 VALPROIC ACID 4.0 1 4.25
CHEMBL4202616 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4219003 IC50 = 4840.0 nM 5.32
CHEMBL4216153 IC50 = 7540.0 nM 5.12
CHEMBL4206601 IC50 = 9980.0 nM 5.00
CHEMBL4207775 IC50 = 11200.0 nM 4.95
CHEMBL1897400 IC50 = 11800.0 nM 4.93
CHEMBL2391535 IC50 = 21900.0 nM 4.66
CHEMBL4207499 IC50 = 43800.0 nM 4.36
CHEMBL109 VALPROIC ACID IC50 = 56100.0 nM 4.25
CHEMBL4202616 IC50 > 100000.0 nM -