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Assay Detail

CHEMBL4015645

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

Binding
Inhibition of human SGLT1 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method
8
Total Activities
8
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

Sodium/glucose cotransporter 1 (CHEMBL4979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor (HSK0935) for the Treatment of Type 2 Diabetes.
Li Y, Shi Z, Chen L, Zheng S, Li S, Xu B, Liu Z, Liu J, Deng C, Ye F.
J Med Chem (2017) 60 : 4173 -4184
PubMed 28447791 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.44 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3039507 SOTAGLIFLOZIN 4.0 1 7.46
CHEMBL4070727 1 6.63
CHEMBL2048484 CANAGLIFLOZIN ANHYDROUS 4.0 1 6.58
CHEMBL1770248 ERTUGLIFLOZIN 4.0 1 6.41
CHEMBL4076289 1 6.34
CHEMBL429910 DAPAGLIFLOZIN 4.0 1 6.20
CHEMBL4070322 1 5.97
CHEMBL4082283 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3039507 SOTAGLIFLOZIN IC50 = 34.6 nM 7.46
CHEMBL4070727 IC50 = 235.0 nM 6.63
CHEMBL2048484 CANAGLIFLOZIN ANHYDROUS IC50 = 265.0 nM 6.58
CHEMBL1770248 ERTUGLIFLOZIN IC50 = 392.0 nM 6.41
CHEMBL4076289 IC50 = 453.0 nM 6.34
CHEMBL429910 DAPAGLIFLOZIN IC50 = 629.0 nM 6.20
CHEMBL4070322 IC50 = 1082.0 nM 5.97
CHEMBL4082283 IC50 = 1096.0 nM 5.96