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Assay Detail

CHEMBL2162525

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

Binding
Inhibition of rat SGLT2 expressed in COS7 cells assessed as reduction of [14C]-AMG uptake
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium/glucose cotransporter 2 (CHEMBL4316)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationship studies of 4-benzyl-1H-pyrazol-3-yl β-d-glucopyranoside derivatives as potent and selective sodium glucose co-transporter 1 (SGLT1) inhibitors with therapeutic activity on postprandial hyperglycemia.
Fushimi N, Fujikura H, Shiohara H, Teranishi H, Shimizu K, Yonekubo S, Ohno K, Miyagi T, Itoh F, Shibazaki T, Tomae M, Ishikawa-Takemura Y, Nakabayashi T, Kamada N, Ozawa T, Kobayashi S, Isaji M.
Bioorg Med Chem (2012) 20 : 6598 -6612
PubMed 23062824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.22 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL245067 PHLORIZIN 1 7.02
CHEMBL2159101 1 5.36
CHEMBL2159102 1 5.33
CHEMBL2159094 1 4.39
CHEMBL2159091 1 4.00
CHEMBL2160193 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL245067 PHLORIZIN IC50 = 96.0 nM 7.02
CHEMBL2159101 IC50 = 4370.0 nM 5.36
CHEMBL2159102 IC50 = 4650.0 nM 5.33
CHEMBL2159094 IC50 = 40800.0 nM 4.39
CHEMBL2159091 IC50 = 100000.0 nM 4.00
CHEMBL2160193 IC50 - -