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Assay Detail

CHEMBL5144623

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

Binding
Inhibition of human SGLT2 expressed in CHO cells by methyl-alpha-D-glucopyranoside assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium/glucose cotransporter 2 (CHEMBL3884)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of GCC5694A: A potent and selective sodium glucose co-transporter 2 inhibitor for the treatment of type 2 diabetes.
Kong YK, Song KS, Jung ME, Kang M, Kim HJ, Kim MJ.
Bioorg Med Chem Lett (2022) 56 : 128466 -128466
PubMed 34813882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.94 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3703920 1 9.43
CHEMBL3703785 1 9.36
CHEMBL3703921 ENAVOGLIFLOZIN 3.0 1 9.34
CHEMBL429910 DAPAGLIFLOZIN 4.0 1 9.31
CHEMBL3703789 1 9.17
CHEMBL3703800 1 9.14
CHEMBL3703791 1 9.10
CHEMBL3703930 1 9.10
CHEMBL3703797 1 9.01
CHEMBL3654929 1 8.94
CHEMBL3703936 1 8.93
CHEMBL3654892 1 8.91
CHEMBL5208827 1 8.84
CHEMBL3703804 1 8.82
CHEMBL3703799 1 8.81
CHEMBL3703801 1 8.76
CHEMBL3703790 1 8.69
CHEMBL3703906 1 8.68
CHEMBL3703916 1 8.38
CHEMBL5205876 1 8.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3703920 IC50 = 0.37 nM 9.43
CHEMBL3703785 IC50 = 0.44 nM 9.36
CHEMBL3703921 ENAVOGLIFLOZIN IC50 = 0.46 nM 9.34
CHEMBL429910 DAPAGLIFLOZIN IC50 = 0.49 nM 9.31
CHEMBL3703789 IC50 = 0.68 nM 9.17
CHEMBL3703800 IC50 = 0.72 nM 9.14
CHEMBL3703791 IC50 = 0.79 nM 9.10
CHEMBL3703930 IC50 = 0.79 nM 9.10
CHEMBL3703797 IC50 = 0.98 nM 9.01
CHEMBL3654929 IC50 = 1.16 nM 8.94
CHEMBL3703936 IC50 = 1.17 nM 8.93
CHEMBL3654892 IC50 = 1.22 nM 8.91
CHEMBL5208827 IC50 = 1.44 nM 8.84
CHEMBL3703804 IC50 = 1.52 nM 8.82
CHEMBL3703799 IC50 = 1.53 nM 8.81
CHEMBL3703801 IC50 = 1.72 nM 8.76
CHEMBL3703790 IC50 = 2.03 nM 8.69
CHEMBL3703906 IC50 = 2.09 nM 8.68
CHEMBL3703916 IC50 = 4.22 nM 8.38
CHEMBL5205876 IC50 = 7.44 nM 8.13