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Assay Detail

CHEMBL1686567

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Binding
Inhibition of rat intestinal isomaltase
14
Total Activities
14
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

Sucrase-isomaltase, intestinal (CHEMBL3114)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Isolation, structure identification and SAR studies on thiosugar sulfonium salts, neosalaprinol and neoponkoranol, as potent α-glucosidase inhibitors.
Xie W, Tanabe G, Akaki J, Morikawa T, Ninomiya K, Minematsu T, Yoshikawa M, Wu X, Muraoka O.
Bioorg Med Chem (2011) 19 : 2015 -2022
PubMed 21345683 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.57 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1684162 NEOSALACINOL 1 6.52
CHEMBL1258643 1 6.00
CHEMBL1684166 1 6.00
CHEMBL1208974 SALACINOL 1 5.89
CHEMBL1258529 NEOPONKORANOL 1 5.85
CHEMBL1232371 NEOKOTALANOL 1 5.75
CHEMBL476960 VOGLIBOSE 4.0 1 5.68
CHEMBL1258528 PONKORANOL 1 5.58
CHEMBL1093264 KOTALANOL 1 5.24
CHEMBL1684163 NEOSALAPRINOL 1 5.19
CHEMBL1209027 SALAPRINOL 1 4.82
CHEMBL1684165 1 4.28
CHEMBL1684164 1 -
CHEMBL404271 ACARBOSE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1684162 NEOSALACINOL IC50 = 300.0 nM 6.52
CHEMBL1258643 IC50 = 1000.0 nM 6.00
CHEMBL1684166 IC50 = 1000.0 nM 6.00
CHEMBL1208974 SALACINOL IC50 = 1300.0 nM 5.89
CHEMBL1258529 NEOPONKORANOL IC50 = 1400.0 nM 5.85
CHEMBL1232371 NEOKOTALANOL IC50 = 1800.0 nM 5.75
CHEMBL476960 VOGLIBOSE IC50 = 2100.0 nM 5.68
CHEMBL1258528 PONKORANOL IC50 = 2600.0 nM 5.58
CHEMBL1093264 KOTALANOL IC50 = 5700.0 nM 5.24
CHEMBL1684163 NEOSALAPRINOL IC50 = 6500.0 nM 5.19
CHEMBL1209027 SALAPRINOL IC50 = 15000.0 nM 4.82
CHEMBL1684165 IC50 = 52900.0 nM 4.28
CHEMBL1684164 IC50 > 329000.0 nM -
CHEMBL404271 ACARBOSE IC50 = 155000.0 nM -