Assay Detail
Binding
CHEMBL5366901
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Inhibition of DPP-4 (unknown origin)
18
Total Activities
16
Compounds Tested
2
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 | 16 | 7.37 | 9.00 |
| EC50 | 2 | 8.56 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL237500 | LINAGLIPTIN | 4.0 | 2 | 9.00 |
| CHEMBL2105762 | OMARIGLIPTIN | 4.0 | 2 | 8.80 |
| CHEMBL5408495 | — | — | 1 | 8.66 |
| CHEMBL5418259 | — | — | 1 | 8.60 |
| CHEMBL5432172 | — | — | 1 | 8.40 |
| CHEMBL376359 | ALOGLIPTIN | 4.0 | 1 | 8.15 |
| CHEMBL4297435 | RETAGLIPTIN | 3.0 | 1 | 7.92 |
| CHEMBL183207 | — | — | 1 | 7.85 |
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | 7.75 |
| CHEMBL184636 | — | — | 1 | 7.72 |
| CHEMBL363319 | — | — | 1 | 6.92 |
| CHEMBL184040 | — | — | 1 | 6.87 |
| CHEMBL184738 | — | — | 1 | 5.72 |
| CHEMBL184262 | — | — | 1 | 5.52 |
| CHEMBL37980 | — | — | 1 | 5.00 |
| CHEMBL186032 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL237500 | LINAGLIPTIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2105762 | OMARIGLIPTIN | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5408495 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL2105762 | OMARIGLIPTIN | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5418259 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL237500 | LINAGLIPTIN | EC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5432172 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL376359 | ALOGLIPTIN | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4297435 | RETAGLIPTIN | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL183207 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1422 | SITAGLIPTIN | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL184636 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL363319 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL184040 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL184738 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL184262 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL37980 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL186032 | — | IC50 | = | 11000.0 | nM | 4.96 |