Assay Detail
Binding
CHEMBL1167866
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Inhibition of human SGLT2 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 1.5 hrs by liquid scintillation counting
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
ortho-Substituted C-aryl glucosides as highly potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 8.19 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1164052 | — | — | 1 | 9.52 |
| CHEMBL1165446 | — | — | 1 | 9.05 |
| CHEMBL1163912 | — | — | 1 | 9.05 |
| CHEMBL1165840 | — | — | 1 | 8.92 |
| CHEMBL1163590 | — | — | 1 | 8.80 |
| CHEMBL496138 | — | — | 1 | 8.72 |
| CHEMBL1163593 | — | — | 1 | 8.52 |
| CHEMBL1163532 | — | — | 1 | 8.44 |
| CHEMBL1163754 | — | — | 1 | 8.22 |
| CHEMBL565784 | — | — | 1 | 8.19 |
| CHEMBL1163914 | — | — | 1 | 8.17 |
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 8.17 |
| CHEMBL1165643 | — | — | 1 | 7.92 |
| CHEMBL1163823 | — | — | 1 | 7.80 |
| CHEMBL1164445 | — | — | 1 | 7.28 |
| CHEMBL1163753 | — | — | 1 | 6.96 |
| CHEMBL1163692 | — | — | 1 | 6.89 |
| CHEMBL1163592 | — | — | 1 | 6.77 |
| CHEMBL1163687 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1164052 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1165446 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1163912 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1165840 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1163590 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL496138 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1163593 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1163532 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1163754 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL565784 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL1163914 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL1165643 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1163823 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1164445 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1163753 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1163692 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1163592 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1163687 | — | IC50 | < | 10.0 | nM | - |