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Assay Detail

CHEMBL3705104

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

Binding
In Vitro Assay: The inhibitory activity of the compounds of this invention against the SGLT-1 or SGLT-2 transporters.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

SGLT-2 inhibitors, methods of making them, and uses thereof
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.82 7.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3660003 1 7.94
CHEMBL3639588 1 7.63
CHEMBL3288752 1 7.44
CHEMBL3288738 1 7.09
CHEMBL3288737 1 7.08
CHEMBL3288744 1 7.04
CHEMBL3288739 1 7.02
CHEMBL3288745 1 6.96
CHEMBL3288740 1 6.89
CHEMBL3288741 1 6.84
CHEMBL3660004 1 6.83
CHEMBL3659998 1 6.77
CHEMBL3288742 1 6.65
CHEMBL3659997 1 6.65
CHEMBL3660000 1 6.65
CHEMBL3288746 1 6.56
CHEMBL3659996 1 6.50
CHEMBL3660002 1 6.48
CHEMBL3659999 1 6.33
CHEMBL3660005 1 6.31
CHEMBL3660001 1 6.27
CHEMBL3288743 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3660003 IC50 = 11.4 nM 7.94
CHEMBL3639588 IC50 = 23.6 nM 7.63
CHEMBL3288752 IC50 = 36.6 nM 7.44
CHEMBL3288738 IC50 = 81.1 nM 7.09
CHEMBL3288737 IC50 = 82.8 nM 7.08
CHEMBL3288744 IC50 = 91.0 nM 7.04
CHEMBL3288739 IC50 = 94.8 nM 7.02
CHEMBL3288745 IC50 = 109.0 nM 6.96
CHEMBL3288740 IC50 = 129.0 nM 6.89
CHEMBL3288741 IC50 = 145.0 nM 6.84
CHEMBL3660004 IC50 = 148.0 nM 6.83
CHEMBL3659998 IC50 = 170.0 nM 6.77
CHEMBL3288742 IC50 = 222.0 nM 6.65
CHEMBL3659997 IC50 = 223.0 nM 6.65
CHEMBL3660000 IC50 = 226.0 nM 6.65
CHEMBL3288746 IC50 = 273.0 nM 6.56
CHEMBL3659996 IC50 = 316.0 nM 6.50
CHEMBL3660002 IC50 = 329.0 nM 6.48
CHEMBL3659999 IC50 = 463.0 nM 6.33
CHEMBL3660005 IC50 = 489.0 nM 6.31
CHEMBL3660001 IC50 = 542.0 nM 6.27
CHEMBL3288743 IC50 = 991.0 nM 6.00