Assay Detail
Binding
CHEMBL2329663
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SGLT1 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 | 6.68 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2323684 | — | — | 1 | 8.00 |
| CHEMBL2323695 | — | — | 1 | 7.96 |
| CHEMBL2323692 | — | — | 1 | 7.92 |
| CHEMBL2323683 | — | — | 1 | 7.82 |
| CHEMBL2323409 | — | — | 1 | 7.64 |
| CHEMBL2323405 | — | — | 1 | 7.60 |
| CHEMBL2323693 | — | — | 1 | 7.35 |
| CHEMBL2323694 | — | — | 1 | 7.30 |
| CHEMBL2323407 | — | — | 1 | 7.16 |
| CHEMBL2323408 | — | — | 1 | 6.99 |
| CHEMBL2323406 | — | — | 1 | 6.91 |
| CHEMBL2323417 | — | — | 1 | 6.77 |
| CHEMBL2159106 | — | — | 1 | 6.68 |
| CHEMBL2323415 | — | — | 1 | 6.66 |
| CHEMBL2323413 | — | — | 1 | 6.46 |
| CHEMBL2323686 | — | — | 1 | 6.41 |
| CHEMBL2323685 | — | — | 1 | 6.38 |
| CHEMBL2323691 | — | — | 1 | 6.35 |
| CHEMBL2323416 | — | — | 1 | 6.29 |
| CHEMBL2323687 | — | — | 1 | 6.14 |
| CHEMBL2160193 | — | — | 1 | 6.13 |
| CHEMBL2323418 | — | — | 1 | 6.11 |
| CHEMBL2323690 | — | — | 1 | 6.08 |
| CHEMBL2323689 | — | — | 1 | 6.03 |
| CHEMBL2323414 | — | — | 1 | 5.99 |
| CHEMBL2323410 | — | — | 1 | 5.83 |
| CHEMBL2323688 | — | — | 1 | 5.82 |
| CHEMBL2323412 | — | — | 1 | 5.70 |
| CHEMBL2323411 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2323684 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2323695 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2323692 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2323683 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2323409 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2323405 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2323693 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2323694 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2323407 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2323408 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL2323406 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL2323417 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2159106 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL2323415 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL2323413 | — | IC50 | = | 351.0 | nM | 6.46 |
| CHEMBL2323686 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL2323685 | — | IC50 | = | 422.0 | nM | 6.38 |
| CHEMBL2323691 | — | IC50 | = | 446.0 | nM | 6.35 |
| CHEMBL2323416 | — | IC50 | = | 517.0 | nM | 6.29 |
| CHEMBL2323687 | — | IC50 | = | 724.0 | nM | 6.14 |
| CHEMBL2160193 | — | IC50 | = | 738.0 | nM | 6.13 |
| CHEMBL2323418 | — | IC50 | = | 772.0 | nM | 6.11 |
| CHEMBL2323690 | — | IC50 | = | 831.0 | nM | 6.08 |
| CHEMBL2323689 | — | IC50 | = | 931.0 | nM | 6.03 |
| CHEMBL2323414 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL2323410 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL2323688 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2323412 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL2323411 | — | IC50 | = | 6170.0 | nM | 5.21 |