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Assay Detail

CHEMBL1108920

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

Binding
Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of glucose uptake
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

(1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol (TS-071) is a potent, selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for type 2 diabetes treatment.
Kakinuma H, Oi T, Hashimoto-Tsuchiya Y, Arai M, Kawakita Y, Fukasawa Y, Iida I, Hagima N, Takeuchi H, Chino Y, Asami J, Okumura-Kitajima L, Io F, Yamamoto D, Miyata N, Takahashi T, Uchida S, Yamamoto K.
J Med Chem (2010) 53 : 3247 -3261
PubMed 20302302 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.20 8.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1093422 1 8.94
CHEMBL1090821 1 8.86
CHEMBL1090786 1 8.82
CHEMBL1090820 1 8.78
CHEMBL1093777 1 8.77
CHEMBL1090822 1 8.75
CHEMBL1091946 1 8.75
CHEMBL1093423 LUSEOGLIFLOZIN 2.0 1 8.65
CHEMBL1092287 1 8.64
CHEMBL1093778 1 8.57
CHEMBL1091547 1 8.40
CHEMBL1092738 1 8.03
CHEMBL1090560 1 7.97
CHEMBL1091966 1 7.87
CHEMBL1091947 1 7.76
CHEMBL1093013 1 7.73
CHEMBL245067 PHLORIZIN 1 7.56
CHEMBL1091948 1 7.42
CHEMBL1092273 1 7.13
CHEMBL1092274 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1093422 IC50 = 1.16 nM 8.94
CHEMBL1090821 IC50 = 1.37 nM 8.86
CHEMBL1090786 IC50 = 1.51 nM 8.82
CHEMBL1090820 IC50 = 1.68 nM 8.78
CHEMBL1093777 IC50 = 1.71 nM 8.77
CHEMBL1090822 IC50 = 1.78 nM 8.75
CHEMBL1091946 IC50 = 1.77 nM 8.75
CHEMBL1093423 LUSEOGLIFLOZIN IC50 = 2.26 nM 8.65
CHEMBL1092287 IC50 = 2.29 nM 8.64
CHEMBL1093778 IC50 = 2.68 nM 8.57
CHEMBL1091547 IC50 = 4.01 nM 8.40
CHEMBL1092738 IC50 = 9.4 nM 8.03
CHEMBL1090560 IC50 = 10.8 nM 7.97
CHEMBL1091966 IC50 = 13.4 nM 7.87
CHEMBL1091947 IC50 = 17.4 nM 7.76
CHEMBL1093013 IC50 = 18.8 nM 7.73
CHEMBL245067 PHLORIZIN IC50 = 27.8 nM 7.56
CHEMBL1091948 IC50 = 37.9 nM 7.42
CHEMBL1092273 IC50 = 73.6 nM 7.13
CHEMBL1092274 IC50 = 283.0 nM 6.55