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Assay Detail

CHEMBL5366576

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

Binding
Inhibition of SGLT1 (unknown origin)
11
Total Activities
11
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

Design, Synthesis, and Biological Evaluation of Thioglucoside Analogues of Gliflozin as Potent New Gliflozin Drugs.
Feng GJ, Guo YF, Tang Y, Li M, Jia Y, Li Z, Wang S, Liu H, Wu Y, Dong H.
J Med Chem (2023) 66 : 12536 -12543
PubMed 37608596 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.88 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL245067 PHLORIZIN 1 6.72
CHEMBL183937 1 6.58
CHEMBL5432424 1 6.24
CHEMBL2048484 CANAGLIFLOZIN ANHYDROUS 4.0 1 6.15
CHEMBL429910 DAPAGLIFLOZIN 4.0 1 5.85
CHEMBL5423158 1 5.82
CHEMBL270766 SERGLIFLOZIN A 1 5.68
CHEMBL450044 SERGLIFLOZIN ETABONATE 2.0 1 5.68
CHEMBL5397667 1 5.56
CHEMBL5410593 1 5.28
CHEMBL2107830 EMPAGLIFLOZIN 4.0 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL245067 PHLORIZIN IC50 = 190.0 nM 6.72
CHEMBL183937 IC50 = 260.0 nM 6.58
CHEMBL5432424 IC50 = 571.0 nM 6.24
CHEMBL2048484 CANAGLIFLOZIN ANHYDROUS IC50 = 710.0 nM 6.15
CHEMBL429910 DAPAGLIFLOZIN IC50 = 1400.0 nM 5.85
CHEMBL5423158 IC50 = 1499.0 nM 5.82
CHEMBL270766 SERGLIFLOZIN A IC50 = 2100.0 nM 5.68
CHEMBL450044 SERGLIFLOZIN ETABONATE IC50 = 2100.0 nM 5.68
CHEMBL5397667 IC50 = 2766.0 nM 5.56
CHEMBL5410593 IC50 = 5287.0 nM 5.28
CHEMBL2107830 EMPAGLIFLOZIN IC50 = 8300.0 nM 5.08