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Assay Detail

CHEMBL3384693

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

Binding
Inhibition of intestinal lactase (unknown origin)
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification and development of biphenyl substituted iminosugars as improved dual glucosylceramide synthase/neutral glucosylceramidase inhibitors.
Ghisaidoobe AT, van den Berg RJ, Butt SS, Strijland A, Donker-Koopman WE, Scheij S, van den Nieuwendijk AM, Koomen GJ, van Loevezijn A, Leemhuis M, Wennekes T, van der Stelt M, van der Marel GA, van Boeckel CA, Aerts JM, Overkleeft HS.
J Med Chem (2014) 57 : 9096 -9104
PubMed 25250725 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 4.45 5.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3354622 1 5.05
CHEMBL3354062 1 4.77
CHEMBL3354025 1 4.70
CHEMBL3354063 1 4.70
CHEMBL3354625 1 4.70
CHEMBL3354630 1 4.60
CHEMBL3354621 1 4.57
CHEMBL3354624 1 4.52
CHEMBL3354623 1 4.46
CHEMBL574645 1 4.46
CHEMBL3354629 1 4.35
CHEMBL3354627 1 4.35
CHEMBL3354626 1 4.30
CHEMBL3354637 NIZUBAGLUSTAT 2.0 1 4.30
CHEMBL3354631 1 4.22
CHEMBL3354636 1 4.22
CHEMBL3354038 1 4.10
CHEMBL3354633 1 4.10
CHEMBL3354635 1 4.00
CHEMBL3354628 1 -
CHEMBL3354620 1 -
CHEMBL3354632 1 -
CHEMBL3354634 1 -
CHEMBL1086996 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3354622 IC50 = 9000.0 nM 5.05
CHEMBL3354062 IC50 = 17000.0 nM 4.77
CHEMBL3354025 IC50 = 20000.0 nM 4.70
CHEMBL3354063 IC50 = 20000.0 nM 4.70
CHEMBL3354625 IC50 = 20000.0 nM 4.70
CHEMBL3354630 IC50 = 25000.0 nM 4.60
CHEMBL3354621 IC50 = 27000.0 nM 4.57
CHEMBL3354624 IC50 = 30000.0 nM 4.52
CHEMBL3354623 IC50 = 35000.0 nM 4.46
CHEMBL574645 IC50 = 35000.0 nM 4.46
CHEMBL3354629 IC50 = 45000.0 nM 4.35
CHEMBL3354627 IC50 = 45000.0 nM 4.35
CHEMBL3354626 IC50 = 50000.0 nM 4.30
CHEMBL3354637 NIZUBAGLUSTAT IC50 = 50000.0 nM 4.30
CHEMBL3354631 IC50 = 60000.0 nM 4.22
CHEMBL3354636 IC50 = 60000.0 nM 4.22
CHEMBL3354038 IC50 = 80000.0 nM 4.10
CHEMBL3354633 IC50 = 80000.0 nM 4.10
CHEMBL3354635 IC50 = 100000.0 nM 4.00
CHEMBL3354628 IC50 > 100000.0 nM -
CHEMBL3354620 IC50 > 100000.0 nM -
CHEMBL3354632 IC50 > 100000.0 nM -
CHEMBL3354634 IC50 = 125000.0 nM -
CHEMBL1086996 IC50 = 200000.0 nM -