Assay Detail
Binding
CHEMBL1763178
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Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting
24
Total Activities
24
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 |
Publication
Discovery of non-glucoside SGLT2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.76 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 8.40 |
| CHEMBL1762504 | — | — | 1 | 8.05 |
| CHEMBL1762505 | — | — | 1 | 8.00 |
| CHEMBL1762500 | — | — | 1 | 7.52 |
| CHEMBL1762499 | — | — | 1 | 7.52 |
| CHEMBL1762498 | — | — | 1 | 7.40 |
| CHEMBL1762502 | — | — | 1 | 7.16 |
| CHEMBL1762492 | — | — | 1 | 7.10 |
| CHEMBL1762490 | — | — | 1 | 7.05 |
| CHEMBL1762495 | — | — | 1 | 6.82 |
| CHEMBL1762491 | — | — | 1 | 6.82 |
| CHEMBL1762501 | — | — | 1 | 6.80 |
| CHEMBL1762497 | — | — | 1 | 6.75 |
| CHEMBL1762488 | — | — | 1 | 6.60 |
| CHEMBL1762484 | — | — | 1 | 6.43 |
| CHEMBL1762493 | — | — | 1 | 6.37 |
| CHEMBL1762494 | — | — | 1 | 6.28 |
| CHEMBL1762496 | — | — | 1 | 6.19 |
| CHEMBL1762486 | — | — | 1 | 5.96 |
| CHEMBL1762485 | — | — | 1 | 5.92 |
| CHEMBL1762483 | — | — | 1 | 5.85 |
| CHEMBL1762503 | — | — | 1 | 5.80 |
| CHEMBL1762489 | — | — | 1 | 5.68 |
| CHEMBL1762487 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1762504 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1762505 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1762500 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1762499 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1762498 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1762502 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1762492 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1762490 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1762495 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1762491 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1762501 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1762497 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1762488 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1762484 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL1762493 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL1762494 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL1762496 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL1762486 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1762485 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1762483 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1762503 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL1762489 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1762487 | — | IC50 | = | 2110.0 | nM | 5.68 |