Assay Detail
Binding
CHEMBL4140929
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Inhibition of human DPP4 using Gly-Pro-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 5 to 10 mins
23
Total Activities
23
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
Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.74 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4176578 | — | — | 1 | 9.27 |
| CHEMBL4164470 | — | — | 1 | 9.27 |
| CHEMBL4169845 | — | — | 1 | 9.21 |
| CHEMBL4175111 | — | — | 1 | 9.14 |
| CHEMBL4165967 | — | — | 1 | 9.12 |
| CHEMBL4162971 | — | — | 1 | 9.11 |
| CHEMBL4172793 | — | — | 1 | 9.11 |
| CHEMBL4169403 | — | — | 1 | 9.10 |
| CHEMBL4164893 | — | — | 1 | 8.90 |
| CHEMBL1650443 | TRELAGLIPTIN | 4.0 | 1 | 8.85 |
| CHEMBL4173673 | — | — | 1 | 8.84 |
| CHEMBL4161924 | — | — | 1 | 8.80 |
| CHEMBL4173272 | — | — | 1 | 8.79 |
| CHEMBL4161474 | — | — | 1 | 8.78 |
| CHEMBL4165359 | — | — | 1 | 8.77 |
| CHEMBL4162340 | — | — | 1 | 8.64 |
| CHEMBL4169618 | — | — | 1 | 8.62 |
| CHEMBL4177478 | — | — | 1 | 8.17 |
| CHEMBL4174924 | — | — | 1 | 7.82 |
| CHEMBL4162532 | — | — | 1 | 7.75 |
| CHEMBL4173215 | — | — | 1 | 7.58 |
| CHEMBL4165788 | — | — | 1 | - |
| CHEMBL4173013 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4176578 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL4164470 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL4169845 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL4175111 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL4165967 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL4162971 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL4172793 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL4169403 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL4164893 | — | IC50 | = | 1.25 | nM | 8.90 |
| CHEMBL1650443 | TRELAGLIPTIN | IC50 | = | 1.43 | nM | 8.85 |
| CHEMBL4173673 | — | IC50 | = | 1.45 | nM | 8.84 |
| CHEMBL4161924 | — | IC50 | = | 1.58 | nM | 8.80 |
| CHEMBL4173272 | — | IC50 | = | 1.61 | nM | 8.79 |
| CHEMBL4161474 | — | IC50 | = | 1.67 | nM | 8.78 |
| CHEMBL4165359 | — | IC50 | = | 1.69 | nM | 8.77 |
| CHEMBL4162340 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4169618 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4177478 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4174924 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL4162532 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4173215 | — | IC50 | = | 26.6 | nM | 7.58 |
| CHEMBL4165788 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4173013 | — | IC50 | > | 100.0 | nM | - |