Assay Detail
Binding
CHEMBL860343
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Inhibitory activity against DPP8
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.51 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL307636 | — | — | 1 | 7.57 |
| CHEMBL372746 | — | — | 1 | 6.70 |
| CHEMBL371480 | — | — | 1 | 6.07 |
| CHEMBL371057 | — | — | 1 | 5.85 |
| CHEMBL203084 | — | — | 1 | 5.77 |
| CHEMBL381530 | — | — | 1 | 5.67 |
| CHEMBL383841 | — | — | 1 | 5.67 |
| CHEMBL98408 | — | — | 1 | 5.64 |
| CHEMBL203032 | — | — | 1 | 5.62 |
| CHEMBL201544 | — | — | 1 | 5.59 |
| CHEMBL424854 | — | — | 1 | 5.48 |
| CHEMBL201753 | — | — | 1 | 5.47 |
| CHEMBL200103 | — | — | 1 | 5.45 |
| CHEMBL371907 | — | — | 1 | 5.38 |
| CHEMBL77538 | — | — | 1 | 5.34 |
| CHEMBL425585 | — | — | 1 | 5.27 |
| CHEMBL382847 | — | — | 1 | 5.26 |
| CHEMBL201158 | — | — | 1 | 5.08 |
| CHEMBL382907 | — | — | 1 | 4.97 |
| CHEMBL372391 | — | — | 1 | 4.89 |
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 4.85 |
| CHEMBL201695 | — | — | 1 | 4.66 |
| CHEMBL201398 | — | — | 1 | 4.38 |
| CHEMBL201424 | — | — | 1 | - |
| CHEMBL380902 | — | — | 1 | - |
| CHEMBL425756 | — | — | 1 | - |
| CHEMBL201644 | — | — | 1 | - |
| CHEMBL202711 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL307636 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL372746 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL371480 | — | IC50 | = | 855.0 | nM | 6.07 |
| CHEMBL371057 | — | IC50 | = | 1407.0 | nM | 5.85 |
| CHEMBL203084 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL381530 | — | IC50 | = | 2121.0 | nM | 5.67 |
| CHEMBL383841 | — | IC50 | = | 2117.0 | nM | 5.67 |
| CHEMBL98408 | — | IC50 | = | 2283.0 | nM | 5.64 |
| CHEMBL203032 | — | IC50 | = | 2387.0 | nM | 5.62 |
| CHEMBL201544 | — | IC50 | = | 2592.0 | nM | 5.59 |
| CHEMBL424854 | — | IC50 | = | 3340.0 | nM | 5.48 |
| CHEMBL201753 | — | IC50 | = | 3416.0 | nM | 5.47 |
| CHEMBL200103 | — | IC50 | = | 3583.0 | nM | 5.45 |
| CHEMBL371907 | — | IC50 | = | 4169.0 | nM | 5.38 |
| CHEMBL77538 | — | IC50 | = | 4573.0 | nM | 5.34 |
| CHEMBL425585 | — | IC50 | = | 5346.0 | nM | 5.27 |
| CHEMBL382847 | — | IC50 | = | 5532.0 | nM | 5.26 |
| CHEMBL201158 | — | IC50 | = | 8338.0 | nM | 5.08 |
| CHEMBL382907 | — | IC50 | = | 10744.0 | nM | 4.97 |
| CHEMBL372391 | — | IC50 | = | 12847.0 | nM | 4.89 |
| CHEMBL142703 | VILDAGLIPTIN | IC50 | = | 14219.0 | nM | 4.85 |
| CHEMBL201695 | — | IC50 | = | 21961.0 | nM | 4.66 |
| CHEMBL201398 | — | IC50 | = | 41859.0 | nM | 4.38 |
| CHEMBL201424 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL380902 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL425756 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL201644 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL202711 | — | IC50 | > | 100000.0 | nM | - |