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Assay Detail

CHEMBL4343613

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

Binding
Inhibition of human SGLT2
10
Total Activities
10
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

Synthetic strategy and SAR studies of C-glucoside heteroaryls as SGLT2 inhibitor: A review.
Haider K, Pathak A, Rohilla A, Haider MR, Ahmad K, Yar MS.
Eur J Med Chem (2019) 184 : 111773 -111773
PubMed 31630053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.57 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3125150 1 9.17
CHEMBL1770248 ERTUGLIFLOZIN 4.0 1 9.06
CHEMBL429910 DAPAGLIFLOZIN 4.0 1 8.95
CHEMBL3039507 SOTAGLIFLOZIN 4.0 1 8.82
CHEMBL1093423 LUSEOGLIFLOZIN 2.0 1 8.65
CHEMBL2110731 TOFOGLIFLOZIN ANHYDROUS 4.0 1 8.54
CHEMBL4521016 1 8.51
CHEMBL2048484 CANAGLIFLOZIN ANHYDROUS 4.0 1 8.36
CHEMBL2018096 IPRAGLIFLOZIN 4.0 1 8.13
CHEMBL245067 PHLORIZIN 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3125150 IC50 = 0.67 nM 9.17
CHEMBL1770248 ERTUGLIFLOZIN IC50 = 0.877 nM 9.06
CHEMBL429910 DAPAGLIFLOZIN IC50 = 1.12 nM 8.95
CHEMBL3039507 SOTAGLIFLOZIN IC50 = 1.5 nM 8.82
CHEMBL1093423 LUSEOGLIFLOZIN IC50 = 2.26 nM 8.65
CHEMBL2110731 TOFOGLIFLOZIN ANHYDROUS IC50 = 2.9 nM 8.54
CHEMBL4521016 IC50 = 3.1 nM 8.51
CHEMBL2048484 CANAGLIFLOZIN ANHYDROUS IC50 = 4.4 nM 8.36
CHEMBL2018096 IPRAGLIFLOZIN IC50 = 7.38 nM 8.13
CHEMBL245067 PHLORIZIN IC50 = 34.6 nM 7.46