Assay Detail
Binding
CHEMBL5366931
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant DPP-4 (1 to 530 residues) using Gly-Pro-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 5 mins by CF assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 8.47 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL237500 | LINAGLIPTIN | 4.0 | 1 | 9.85 |
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | 4.0 | 1 | 8.82 |
| CHEMBL2105762 | OMARIGLIPTIN | 4.0 | 1 | 8.80 |
| CHEMBL376359 | ALOGLIPTIN | 4.0 | 1 | 8.12 |
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | 7.75 |
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 7.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL237500 | LINAGLIPTIN | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2105762 | OMARIGLIPTIN | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL376359 | ALOGLIPTIN | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL1422 | SITAGLIPTIN | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL142703 | VILDAGLIPTIN | IC50 | = | 34.0 | nM | 7.47 |