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Assay Detail

CHEMBL844302

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Binding
Concentration required for 50% for in vitro activity against human SDH (sorbitol dehydrogenase)
8
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sorbitol dehydrogenase (CHEMBL2275)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A sorbitol dehydrogenase inhibitor of exceptional in vivo potency with a long duration of action: 1-(R)-[4-[4-(4,6-dimethyl[1,3,5]triazin-2-yl)- 2R,6S-dimethylpiperazin-1-yl]pyrimidin-2- yl]ethanol.
Mylari BL, Oates PJ, Zembrowski WJ, Beebe DA, Conn EL, Coutcher JB, O'Gorman MT, Linhares MC, Withbroe GJ.
J Med Chem (2002) 45 : 4398 -4401
PubMed 12238919 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.06 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL136420 1 8.40
CHEMBL136900 1 8.40
CHEMBL136680 2 8.30
CHEMBL136103 1 8.15
CHEMBL342697 1 8.15
CHEMBL435428 1 7.89
CHEMBL139187 1 7.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL136420 IC50 = 4.0 nM 8.40
CHEMBL136900 IC50 = 4.0 nM 8.40
CHEMBL136680 IC50 = 5.0 nM 8.30
CHEMBL136103 IC50 = 7.0 nM 8.15
CHEMBL342697 IC50 = 7.0 nM 8.15
CHEMBL435428 IC50 = 13.0 nM 7.89
CHEMBL136680 IC50 = 16.0 nM 7.80
CHEMBL139187 IC50 = 43.0 nM 7.37