Assay Detail
Binding
CHEMBL1772494
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Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of methyl alpha-D-glucopyranoside uptake after 1 hr
7
Total Activities
7
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 a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.02 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1770244 | — | — | 1 | 6.30 |
| CHEMBL1770246 | — | — | 1 | 6.26 |
| CHEMBL1770245 | — | — | 1 | 6.02 |
| CHEMBL1090058 | — | — | 1 | 5.81 |
| CHEMBL1770248 | ERTUGLIFLOZIN | 4.0 | 1 | 5.71 |
| CHEMBL1770249 | — | — | 1 | - |
| CHEMBL1770247 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1770244 | — | IC50 | = | 506.0 | nM | 6.30 |
| CHEMBL1770246 | — | IC50 | = | 546.0 | nM | 6.26 |
| CHEMBL1770245 | — | IC50 | = | 958.0 | nM | 6.02 |
| CHEMBL1090058 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL1770248 | ERTUGLIFLOZIN | IC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL1770249 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1770247 | — | IC50 | > | 10000.0 | nM | - |