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Assay Detail

CHEMBL3815263

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

Binding
Inhibition of rat small intestinal sucrase using sucrose as substrate incubated for 30 mins by glucose-oxidase method
11
Total Activities
11
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

Hydrophobic substituents increase the potency of salacinol, a potent α-glucosidase inhibitor from Ayurvedic traditional medicine 'Salacia'.
Tanabe G, Xie W, Balakishan G, Amer MF, Tsutsui N, Takemura H, Nakamura S, Akaki J, Ninomiya K, Morikawa T, Nakanishi I, Muraoka O.
Bioorg Med Chem (2016) 24 : 3705 -3715
PubMed 27325449 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.51 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3814496 1 7.38
CHEMBL3814988 1 7.05
CHEMBL3815109 1 7.05
CHEMBL3814838 1 6.92
CHEMBL3814911 1 6.62
CHEMBL1561 MIGLITOL 4.0 1 6.37
CHEMBL3814747 1 6.34
CHEMBL3814555 1 6.30
CHEMBL3814264 1 5.89
CHEMBL1182462 1 5.89
CHEMBL239249 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3814496 IC50 = 42.0 nM 7.38
CHEMBL3814988 IC50 = 90.0 nM 7.05
CHEMBL3815109 IC50 = 90.0 nM 7.05
CHEMBL3814838 IC50 = 120.0 nM 6.92
CHEMBL3814911 IC50 = 240.0 nM 6.62
CHEMBL1561 MIGLITOL IC50 = 430.0 nM 6.37
CHEMBL3814747 IC50 = 460.0 nM 6.34
CHEMBL3814555 IC50 = 500.0 nM 6.30
CHEMBL3814264 IC50 = 1300.0 nM 5.89
CHEMBL1182462 IC50 = 1300.0 nM 5.89
CHEMBL239249 IC50 = 1600.0 nM 5.80