Assay Detail
Binding
CHEMBL5366934
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant DPP-4 expressed in human Caco-2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate measured after 1 hrs by fluorescence based assay
6
Total Activities
6
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 | Autocuration |
Publication
Development of Long-Acting Dipeptidyl Peptidase-4 Inhibitors: Structural Evolution and Long-Acting Determinants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.85 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL237500 | LINAGLIPTIN | 4.0 | 1 | 9.00 |
| CHEMBL1650443 | TRELAGLIPTIN | 4.0 | 1 | 8.27 |
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | 7.72 |
| CHEMBL376359 | ALOGLIPTIN | 4.0 | 1 | 7.62 |
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | 4.0 | 1 | 7.30 |
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL237500 | LINAGLIPTIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1650443 | TRELAGLIPTIN | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL1422 | SITAGLIPTIN | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL376359 | ALOGLIPTIN | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL142703 | VILDAGLIPTIN | IC50 | = | 62.0 | nM | 7.21 |