Assay Detail
Binding
CHEMBL1811698
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Inhibition of human SGLT2 expressed in african green monkey COS7 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 2 hrs by scintillation counting in presence of 25 % human plasma
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.09 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1807551 | — | — | 1 | 8.74 |
| CHEMBL1808388 | BEXAGLIFLOZIN | 4.0 | 1 | 8.64 |
| CHEMBL1807552 | — | — | 1 | 8.52 |
| CHEMBL1808389 | — | — | 1 | 8.52 |
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 8.49 |
| CHEMBL1808390 | — | — | 1 | 8.40 |
| CHEMBL1807547 | — | — | 1 | 8.36 |
| CHEMBL1808386 | — | — | 1 | 8.22 |
| CHEMBL1807542 | — | — | 1 | 8.10 |
| CHEMBL497971 | — | — | 1 | 8.03 |
| CHEMBL1807548 | — | — | 1 | 8.02 |
| CHEMBL1807544 | — | — | 1 | 8.02 |
| CHEMBL1807550 | — | — | 1 | 8.00 |
| CHEMBL1807541 | — | — | 1 | 8.00 |
| CHEMBL1807546 | — | — | 1 | 7.03 |
| CHEMBL1807540 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1807551 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL1808388 | BEXAGLIFLOZIN | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL1807552 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1808389 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1808390 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1807547 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL1808386 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1807542 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL497971 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL1807548 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL1807544 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL1807550 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1807541 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1807546 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL1807540 | — | IC50 | = | 428.0 | nM | 6.37 |