Assay Detail
Binding
CHEMBL902716
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Inhibition of human DPP4 in Caco-2 cells by fluorescene assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Caco-2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.63 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL237289 | — | — | 1 | 9.00 |
| CHEMBL237500 | LINAGLIPTIN | 4.0 | 1 | 9.00 |
| CHEMBL391089 | — | — | 1 | 8.70 |
| CHEMBL237067 | — | — | 1 | 8.52 |
| CHEMBL237499 | — | — | 1 | 8.52 |
| CHEMBL237287 | — | — | 1 | 8.40 |
| CHEMBL429450 | — | — | 1 | 8.40 |
| CHEMBL365000 | — | — | 1 | 8.30 |
| CHEMBL237488 | — | — | 1 | 8.22 |
| CHEMBL391307 | — | — | 1 | 8.10 |
| CHEMBL237288 | — | — | 1 | 8.05 |
| CHEMBL237279 | — | — | 1 | 7.46 |
| CHEMBL237281 | — | — | 1 | 7.25 |
| CHEMBL399216 | — | — | 1 | 7.09 |
| CHEMBL237280 | — | — | 1 | 7.06 |
| CHEMBL235792 | — | — | 1 | 6.70 |
| CHEMBL391634 | — | — | 1 | 6.55 |
| CHEMBL235352 | — | — | 1 | 6.24 |
| CHEMBL235134 | — | — | 1 | 5.55 |
| CHEMBL235133 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL237289 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL237500 | LINAGLIPTIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL391089 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL237067 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL237499 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL237287 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL429450 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL365000 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL237488 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL391307 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL237288 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL237279 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL237281 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL399216 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL237280 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL235792 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL391634 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL235352 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL235134 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL235133 | — | IC50 | = | 3900.0 | nM | 5.41 |