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Assay Detail

CHEMBL4725003

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

Binding
Inhibition of human SGLT1 expressed in COS7 cells assessed as reduction in [14C]-AMG uptake
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium/glucose cotransporter 1 (CHEMBL4979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of remogliflozin etabonate: A potent and highly selective SGLT2 inhibitor.
Shimizu K,Fujikura H,Fushimi N,Nishimura T,Tatani K,Katsuno K,Fujimori Y,Watanabe S,Hiratochi M,Nakabayashi T,Kamada N,Arakawa K,Hikawa H,Azumaya I,Isaji M
Bioorg Med Chem (2021) 34 : 116033 -116033
PubMed 33581390 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.78 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3980689 1 6.96
CHEMBL4765036 1 6.82
CHEMBL3950588 1 6.63
CHEMBL3896936 1 6.49
CHEMBL3907970 1 6.46
CHEMBL3972664 1 6.42
CHEMBL3908950 1 6.39
CHEMBL4795938 1 6.33
CHEMBL3934976 1 6.20
CHEMBL3923809 1 5.99
CHEMBL4793115 1 5.88
CHEMBL4750405 1 5.79
CHEMBL3915296 1 5.79
CHEMBL3969998 1 5.77
CHEMBL3960449 1 5.56
CHEMBL4752053 1 5.06
CHEMBL4787524 1 4.99
CHEMBL4786882 1 4.88
CHEMBL4785821 1 4.87
CHEMBL3958686 REMOGLIFLOZIN -1.0 1 4.78
CHEMBL4791676 1 4.62
CHEMBL4790263 1 4.50
CHEMBL2028665 REMOGLIFLOZIN ETABONATE 2.0 1 -
CHEMBL4760667 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3980689 IC50 = 109.0 nM 6.96
CHEMBL4765036 IC50 = 150.0 nM 6.82
CHEMBL3950588 IC50 = 233.0 nM 6.63
CHEMBL3896936 IC50 = 321.0 nM 6.49
CHEMBL3907970 IC50 = 345.0 nM 6.46
CHEMBL3972664 IC50 = 378.0 nM 6.42
CHEMBL3908950 IC50 = 405.0 nM 6.39
CHEMBL4795938 IC50 = 468.0 nM 6.33
CHEMBL3934976 IC50 = 626.0 nM 6.20
CHEMBL3923809 IC50 = 1030.0 nM 5.99
CHEMBL4793115 IC50 = 1320.0 nM 5.88
CHEMBL4750405 IC50 = 1630.0 nM 5.79
CHEMBL3915296 IC50 = 1630.0 nM 5.79
CHEMBL3969998 IC50 = 1690.0 nM 5.77
CHEMBL3960449 IC50 = 2780.0 nM 5.56
CHEMBL4752053 IC50 = 8710.0 nM 5.06
CHEMBL4787524 IC50 = 10300.0 nM 4.99
CHEMBL4786882 IC50 = 13300.0 nM 4.88
CHEMBL4785821 IC50 = 13600.0 nM 4.87
CHEMBL3958686 REMOGLIFLOZIN IC50 = 16600.0 nM 4.78
CHEMBL4791676 IC50 = 23700.0 nM 4.62
CHEMBL4790263 IC50 = 31500.0 nM 4.50
CHEMBL2028665 REMOGLIFLOZIN ETABONATE IC50 > 100000.0 nM -
CHEMBL4760667 IC50 > 100000.0 nM -