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Assay Detail

CHEMBL1099882

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

Binding
Inhibition of lactase by HPLC
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Lactase/phlorizin hydrolase (CHEMBL1075131)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual-action lipophilic iminosugar improves glycemic control in obese rodents by reduction of visceral glycosphingolipids and buffering of carbohydrate assimilation.
Wennekes T, Meijer AJ, Groen AK, Boot RG, Groener JE, van Eijk M, Ottenhoff R, Bijl N, Ghauharali K, Song H, O'Shea TJ, Liu H, Yew N, Copeland D, van den Berg RJ, van der Marel GA, Overkleeft HS, Aerts JM.
J Med Chem (2010) 53 : 689 -698
PubMed 20000679 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.32 4.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL574645 1 4.46
CHEMBL1561 MIGLITOL 4.0 1 4.30
CHEMBL110458 MIGALASTAT 4.0 1 4.30
CHEMBL307429 DUVOGLUSTAT 2.0 1 4.21
CHEMBL1029 MIGLUSTAT 4.0 1 -
CHEMBL175901 1 -
CHEMBL1076754 1 -
CHEMBL1086996 1 -
CHEMBL1086997 LUCERASTAT 3.0 1 -
CHEMBL1088158 1 -
CHEMBL179409 1 -
CHEMBL1088291 1 -
CHEMBL1088292 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL574645 IC50 = 35000.0 nM 4.46
CHEMBL1561 MIGLITOL IC50 = 50000.0 nM 4.30
CHEMBL110458 MIGALASTAT IC50 = 50000.0 nM 4.30
CHEMBL307429 DUVOGLUSTAT IC50 = 62000.0 nM 4.21
CHEMBL1029 MIGLUSTAT IC50 > 100000.0 nM -
CHEMBL175901 IC50 > 1000000.0 nM -
CHEMBL1076754 IC50 = 1000000.0 nM -
CHEMBL1086996 IC50 > 1000000.0 nM -
CHEMBL1086997 LUCERASTAT IC50 = 1000000.0 nM -
CHEMBL1088158 IC50 = 375000.0 nM -
CHEMBL179409 IC50 = 400000.0 nM -
CHEMBL1088291 IC50 > 1000000.0 nM -
CHEMBL1088292 IC50 > 1000000.0 nM -