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Assay Detail

CHEMBL882165

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Binding
Concentration required for 50% in vitro inhibition in sheep liver sorbitol dehydrogenase (s-SDH)
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Ovis aries
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Sorbitol dehydrogenase (CHEMBL2275)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Orally-effective, long-acting sorbitol dehydrogenase inhibitors: synthesis, structure-activity relationships, and in vivo evaluations of novel heterocycle-substituted piperazino-pyrimidines.
Chu-Moyer MY, Ballinger WE, Beebe DA, Berger R, Coutcher JB, Day WW, Li J, Mylari BL, Oates PJ, Weekly RM.
J Med Chem (2002) 45 : 511 -528
PubMed 11784155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.89 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL146805 1 6.48
CHEMBL151268 1 6.46
CHEMBL357712 1 6.39
CHEMBL358327 1 6.37
CHEMBL423753 1 6.32
CHEMBL148935 1 6.31
CHEMBL151605 1 6.23
CHEMBL148647 1 6.13
CHEMBL148822 1 6.05
CHEMBL151753 1 5.96
CHEMBL348663 1 5.96
CHEMBL148835 1 5.89
CHEMBL147407 1 5.64
CHEMBL148585 1 5.58
CHEMBL151033 1 5.52
CHEMBL151806 1 5.50
CHEMBL148648 1 5.50
CHEMBL357720 1 5.32
CHEMBL341857 1 5.19
CHEMBL422143 1 5.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL146805 IC50 = 330.0 nM 6.48
CHEMBL151268 IC50 = 350.0 nM 6.46
CHEMBL357712 IC50 = 410.0 nM 6.39
CHEMBL358327 IC50 = 430.0 nM 6.37
CHEMBL423753 IC50 = 480.0 nM 6.32
CHEMBL148935 IC50 = 490.0 nM 6.31
CHEMBL151605 IC50 = 590.0 nM 6.23
CHEMBL148647 IC50 = 740.0 nM 6.13
CHEMBL148822 IC50 = 890.0 nM 6.05
CHEMBL151753 IC50 = 1100.0 nM 5.96
CHEMBL348663 IC50 = 1100.0 nM 5.96
CHEMBL148835 IC50 = 1300.0 nM 5.89
CHEMBL147407 IC50 = 2300.0 nM 5.64
CHEMBL148585 IC50 = 2600.0 nM 5.58
CHEMBL151033 IC50 = 3000.0 nM 5.52
CHEMBL151806 IC50 = 3200.0 nM 5.50
CHEMBL148648 IC50 = 3200.0 nM 5.50
CHEMBL357720 IC50 = 4800.0 nM 5.32
CHEMBL341857 IC50 = 6500.0 nM 5.19
CHEMBL422143 IC50 = 9400.0 nM 5.03