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Assay Detail

CHEMBL642967

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Binding
Inhibition of crude aldose reductase of rat lens
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and aldose reductase inhibitory activity of substituted 2-oxoquinoline-1-acetic acid derivatives.
DeRuiter J, Brubaker AN, Whitmer WL, Stein JL.
J Med Chem (1986) 29 : 2024 -2028
PubMed 3093680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.93 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56337 EPALRESTAT 4.0 1 8.00
CHEMBL266497 SORBINIL 3.0 1 7.77
CHEMBL62197 1 6.35
CHEMBL305164 1 6.04
CHEMBL63055 ALRESTATIN 2.0 1 5.82
CHEMBL291659 1 5.62
CHEMBL64312 1 5.48
CHEMBL64455 1 5.22
CHEMBL428495 1 4.50
CHEMBL64552 1 4.48
CHEMBL62329 1 -
CHEMBL59766 1 -
CHEMBL292547 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56337 EPALRESTAT IC50 = 10.0 nM 8.00
CHEMBL266497 SORBINIL IC50 = 17.0 nM 7.77
CHEMBL62197 IC50 = 450.0 nM 6.35
CHEMBL305164 IC50 = 910.0 nM 6.04
CHEMBL63055 ALRESTATIN IC50 = 1500.0 nM 5.82
CHEMBL291659 IC50 = 2400.0 nM 5.62
CHEMBL64312 IC50 = 3300.0 nM 5.48
CHEMBL64455 IC50 = 6000.0 nM 5.22
CHEMBL428495 IC50 = 32000.0 nM 4.50
CHEMBL64552 IC50 = 33000.0 nM 4.48
CHEMBL62329 IC50 = 110000.0 nM -
CHEMBL59766 IC50 = 590000.0 nM -
CHEMBL292547 IC50 = 470000.0 nM -