Assay Detail
Binding
CHEMBL2329661
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SGLT2 expressed in COS7 cells assessed as inhibition [14C]-AMG cellular uptake
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and structure-activity relationships of a series of 4-benzyl-5-isopropyl-1H-pyrazol-3-yl β-D-glycopyranosides substituted with novel hydrophilic groups as highly potent inhibitors of sodium glucose co-transporter 1 (SGLT1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.30 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2323692 | — | — | 1 | 8.10 |
| CHEMBL2323684 | — | — | 1 | 7.75 |
| CHEMBL2323683 | — | — | 1 | 7.70 |
| CHEMBL2323405 | — | — | 1 | 7.38 |
| CHEMBL2323409 | — | — | 1 | 7.34 |
| CHEMBL2323693 | — | — | 1 | 7.10 |
| CHEMBL2323406 | — | — | 1 | 7.01 |
| CHEMBL2323407 | — | — | 1 | 6.82 |
| CHEMBL2323408 | — | — | 1 | 6.68 |
| CHEMBL2159106 | — | — | 1 | 6.54 |
| CHEMBL2323417 | — | — | 1 | 6.50 |
| CHEMBL2323416 | — | — | 1 | 6.45 |
| CHEMBL2323695 | — | — | 1 | 6.43 |
| CHEMBL2323414 | — | — | 1 | 6.34 |
| CHEMBL2323415 | — | — | 1 | 6.22 |
| CHEMBL2323689 | — | — | 1 | 6.03 |
| CHEMBL2323418 | — | — | 1 | 5.98 |
| CHEMBL2323413 | — | — | 1 | 5.97 |
| CHEMBL2323685 | — | — | 1 | 5.80 |
| CHEMBL2323694 | — | — | 1 | 5.76 |
| CHEMBL2160193 | — | — | 1 | 5.70 |
| CHEMBL2323410 | — | — | 1 | 5.61 |
| CHEMBL2323412 | — | — | 1 | 5.59 |
| CHEMBL2323686 | — | — | 1 | 5.51 |
| CHEMBL2323688 | — | — | 1 | 5.40 |
| CHEMBL2323690 | — | — | 1 | 5.33 |
| CHEMBL2323687 | — | — | 1 | 5.29 |
| CHEMBL2323691 | — | — | 1 | 5.25 |
| CHEMBL2323411 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2323692 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2323684 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2323683 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2323405 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2323409 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL2323693 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2323406 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL2323407 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL2323408 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL2159106 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL2323417 | — | IC50 | = | 319.0 | nM | 6.50 |
| CHEMBL2323416 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL2323695 | — | IC50 | = | 371.0 | nM | 6.43 |
| CHEMBL2323414 | — | IC50 | = | 457.0 | nM | 6.34 |
| CHEMBL2323415 | — | IC50 | = | 608.0 | nM | 6.22 |
| CHEMBL2323689 | — | IC50 | = | 936.0 | nM | 6.03 |
| CHEMBL2323418 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL2323413 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL2323685 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL2323694 | — | IC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL2160193 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL2323410 | — | IC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL2323412 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL2323686 | — | IC50 | = | 3090.0 | nM | 5.51 |
| CHEMBL2323688 | — | IC50 | = | 3980.0 | nM | 5.40 |
| CHEMBL2323690 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL2323687 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL2323691 | — | IC50 | = | 5620.0 | nM | 5.25 |
| CHEMBL2323411 | — | IC50 | = | 9950.0 | nM | 5.00 |