Assay Detail
Binding
CHEMBL1811699
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Inhibition of human SGLT1 expressed in human 293 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 1.5 hrs by scintillation counting in presence of 25 % human plasma
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Cell Type | HEK293 |
| 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 | 27 | 5.49 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1807551 | — | — | 1 | 6.22 |
| CHEMBL1807547 | — | — | 1 | 6.17 |
| CHEMBL497971 | — | — | 1 | 6.01 |
| CHEMBL1807548 | — | — | 1 | 5.85 |
| CHEMBL1807552 | — | — | 1 | 5.60 |
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 5.51 |
| CHEMBL1808386 | — | — | 1 | 5.44 |
| CHEMBL1808388 | BEXAGLIFLOZIN | 4.0 | 1 | 5.25 |
| CHEMBL1807542 | — | — | 1 | 5.24 |
| CHEMBL1808390 | — | — | 1 | 5.16 |
| CHEMBL1807546 | — | — | 1 | 5.05 |
| CHEMBL1808389 | — | — | 1 | 4.42 |
| CHEMBL1807726 | — | — | 1 | - |
| CHEMBL1807553 | — | — | 1 | - |
| CHEMBL1807550 | — | — | 1 | - |
| CHEMBL1807549 | — | — | 1 | - |
| CHEMBL1807545 | — | — | 1 | - |
| CHEMBL1807544 | — | — | 1 | - |
| CHEMBL1807543 | — | — | 1 | - |
| CHEMBL1807541 | — | — | 1 | - |
| CHEMBL1807540 | — | — | 1 | - |
| CHEMBL1808394 | — | — | 1 | - |
| CHEMBL1808393 | — | — | 1 | - |
| CHEMBL1808392 | — | — | 1 | - |
| CHEMBL1808391 | — | — | 1 | - |
| CHEMBL1808387 | — | — | 1 | - |
| CHEMBL1808385 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1807551 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL1807547 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL497971 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL1807548 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1807552 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1808386 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1808388 | BEXAGLIFLOZIN | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL1807542 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL1808390 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL1807546 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL1808389 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL1807726 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1807553 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1807550 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1807549 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1807545 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1807544 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1807543 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1807541 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1807540 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1808394 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1808393 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1808392 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1808391 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1808387 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1808385 | — | IC50 | > | 100000.0 | nM | - |