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Assay Detail

CHEMBL4143387

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 reduction in [14C]AMG uptake after 1 hr by microbeta counting method
29
Total Activities
29
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

Identification of an oxime-containing C-glucosylarene as a potential inhibitor of sodium-dependent glucose co-transporter 2.
Yuan MC, Yeh TK, Chen CT, Song JS, Huang YC, Hsieh TC, Huang CY, Huang YL, Wang MH, Wu SH, Yao CH, Chao YS, Lee JC.
Eur J Med Chem (2018) 143 : 611 -620
PubMed 29216560 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 29 6.69 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429910 DAPAGLIFLOZIN 4.0 1 8.70
CHEMBL4164934 1 7.42
CHEMBL4176765 1 7.34
CHEMBL4173627 1 7.20
CHEMBL4168847 1 7.19
CHEMBL245067 PHLORIZIN 1 7.10
CHEMBL4172842 1 7.06
CHEMBL4166140 1 7.04
CHEMBL4169906 1 7.02
CHEMBL4161587 1 6.89
CHEMBL4176991 1 6.82
CHEMBL4165421 1 6.76
CHEMBL4176700 1 6.76
CHEMBL4160788 1 6.71
CHEMBL4165004 1 6.69
CHEMBL4165713 1 6.68
CHEMBL4173333 1 6.68
CHEMBL4161979 1 6.52
CHEMBL4171400 1 6.47
CHEMBL4170248 1 6.43
CHEMBL4171709 1 6.40
CHEMBL4172198 1 6.40
CHEMBL4161107 1 6.37
CHEMBL4175624 1 6.37
CHEMBL4159626 1 6.34
CHEMBL4164519 1 6.17
CHEMBL4176218 1 5.71
CHEMBL4168361 1 5.65
CHEMBL4175153 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429910 DAPAGLIFLOZIN EC50 = 2.0 nM 8.70
CHEMBL4164934 EC50 = 38.0 nM 7.42
CHEMBL4176765 EC50 = 46.0 nM 7.34
CHEMBL4173627 EC50 = 63.0 nM 7.20
CHEMBL4168847 EC50 = 65.0 nM 7.19
CHEMBL245067 PHLORIZIN EC50 = 79.0 nM 7.10
CHEMBL4172842 EC50 = 88.0 nM 7.06
CHEMBL4166140 EC50 = 92.0 nM 7.04
CHEMBL4169906 EC50 = 95.0 nM 7.02
CHEMBL4161587 EC50 = 130.0 nM 6.89
CHEMBL4176991 EC50 = 151.0 nM 6.82
CHEMBL4165421 EC50 = 175.0 nM 6.76
CHEMBL4176700 EC50 = 173.0 nM 6.76
CHEMBL4160788 EC50 = 194.0 nM 6.71
CHEMBL4165004 EC50 = 204.0 nM 6.69
CHEMBL4165713 EC50 = 211.0 nM 6.68
CHEMBL4173333 EC50 = 208.0 nM 6.68
CHEMBL4161979 EC50 = 301.0 nM 6.52
CHEMBL4171400 EC50 = 335.0 nM 6.47
CHEMBL4170248 EC50 = 370.0 nM 6.43
CHEMBL4171709 EC50 = 396.0 nM 6.40
CHEMBL4172198 EC50 = 395.0 nM 6.40
CHEMBL4161107 EC50 = 431.0 nM 6.37
CHEMBL4175624 EC50 = 429.0 nM 6.37
CHEMBL4159626 EC50 = 457.0 nM 6.34
CHEMBL4164519 EC50 = 678.0 nM 6.17
CHEMBL4176218 EC50 = 1953.0 nM 5.71
CHEMBL4168361 EC50 = 2251.0 nM 5.65
CHEMBL4175153 EC50 = 8541.0 nM 5.07