Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1831435

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

Binding
Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting
34
Total Activities
34
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

Novel thiophenyl C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents.
Lee SH, Song KS, Kim JY, Kang M, Lee JS, Cho SH, Park HJ, Kim J, Lee J.
Bioorg Med Chem (2011) 19 : 5813 -5832
PubMed 21906953 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.41 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429910 DAPAGLIFLOZIN 4.0 1 9.31
CHEMBL1830353 1 8.35
CHEMBL1830357 1 8.06
CHEMBL1830354 1 7.99
CHEMBL1830356 1 7.94
CHEMBL1830349 1 7.92
CHEMBL1829088 1 7.91
CHEMBL1830347 1 7.89
CHEMBL1829080 1 7.68
CHEMBL1829086 1 7.61
CHEMBL1829079 1 7.56
CHEMBL1829090 1 7.53
CHEMBL1830870 1 7.46
CHEMBL1830348 1 7.32
CHEMBL1829078 1 7.30
CHEMBL1829089 1 7.30
CHEMBL1830873 1 7.26
CHEMBL1830350 1 7.24
CHEMBL1830352 1 7.22
CHEMBL1829087 1 7.22
CHEMBL1830872 1 7.19
CHEMBL1829082 1 7.16
CHEMBL1829085 1 7.16
CHEMBL1829081 1 7.15
CHEMBL1830346 1 7.15
CHEMBL1830869 1 7.06
CHEMBL1829084 1 7.05
CHEMBL1830355 1 7.04
CHEMBL1830344 1 7.03
CHEMBL1830874 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429910 DAPAGLIFLOZIN IC50 = 0.49 nM 9.31
CHEMBL1830353 IC50 = 4.47 nM 8.35
CHEMBL1830357 IC50 = 8.73 nM 8.06
CHEMBL1830354 IC50 = 10.3 nM 7.99
CHEMBL1830356 IC50 = 11.5 nM 7.94
CHEMBL1830349 IC50 = 11.9 nM 7.92
CHEMBL1829088 IC50 = 12.4 nM 7.91
CHEMBL1830347 IC50 = 12.8 nM 7.89
CHEMBL1829080 IC50 = 21.1 nM 7.68
CHEMBL1829086 IC50 = 24.8 nM 7.61
CHEMBL1829079 IC50 = 27.5 nM 7.56
CHEMBL1829090 IC50 = 29.3 nM 7.53
CHEMBL1830870 IC50 = 34.6 nM 7.46
CHEMBL1830348 IC50 = 48.4 nM 7.32
CHEMBL1829089 IC50 = 49.5 nM 7.30
CHEMBL1829078 IC50 = 50.2 nM 7.30
CHEMBL1830873 IC50 = 54.6 nM 7.26
CHEMBL1830350 IC50 = 57.2 nM 7.24
CHEMBL1830352 IC50 = 60.2 nM 7.22
CHEMBL1829087 IC50 = 59.8 nM 7.22
CHEMBL1830872 IC50 = 65.0 nM 7.19
CHEMBL1829082 IC50 = 68.9 nM 7.16
CHEMBL1829085 IC50 = 69.6 nM 7.16
CHEMBL1829081 IC50 = 71.4 nM 7.15
CHEMBL1830346 IC50 = 70.7 nM 7.15
CHEMBL1830869 IC50 = 86.5 nM 7.06
CHEMBL1829084 IC50 = 88.3 nM 7.05
CHEMBL1830355 IC50 = 91.3 nM 7.04
CHEMBL1830344 IC50 = 94.0 nM 7.03
CHEMBL1830874 IC50 = 111.0 nM 6.96
CHEMBL1830345 IC50 = 115.0 nM 6.94
CHEMBL1830871 IC50 = 140.0 nM 6.85
CHEMBL1830351 IC50 = 162.0 nM 6.79
CHEMBL1829083 IC50 = 451.0 nM 6.35