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Assay Detail

CHEMBL4233439

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

Binding
Inhibition of SGLT2 (unknown origin)
6
Total Activities
6
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 2 (CHEMBL3884)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of nitric oxide releasing derivatives of dapagliflozin as potential anti-diabetic and anti-thrombotic agents.
Li Z, Xu X, Deng L, Liao R, Liang R, Zhang B, Zhang L.
Bioorg Med Chem (2018) 26 : 3947 -3952
PubMed 29954682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.54 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429910 DAPAGLIFLOZIN 4.0 1 8.96
CHEMBL2048484 CANAGLIFLOZIN ANHYDROUS 4.0 1 8.66
CHEMBL1093423 LUSEOGLIFLOZIN 2.0 1 8.64
CHEMBL2107830 EMPAGLIFLOZIN 4.0 1 8.51
CHEMBL2110731 TOFOGLIFLOZIN ANHYDROUS 4.0 1 8.40
CHEMBL2018096 IPRAGLIFLOZIN 4.0 1 8.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429910 DAPAGLIFLOZIN IC50 = 1.1 nM 8.96
CHEMBL2048484 CANAGLIFLOZIN ANHYDROUS IC50 = 2.2 nM 8.66
CHEMBL1093423 LUSEOGLIFLOZIN IC50 = 2.3 nM 8.64
CHEMBL2107830 EMPAGLIFLOZIN IC50 = 3.1 nM 8.51
CHEMBL2110731 TOFOGLIFLOZIN ANHYDROUS IC50 = 4.0 nM 8.40
CHEMBL2018096 IPRAGLIFLOZIN IC50 = 8.4 nM 8.08