Assay Detail
Binding
CHEMBL4616383
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant DPP4 incubated for 15 mins using Gly-Pro-7-AMC substrate
14
Total Activities
14
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
Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.87 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105762 | OMARIGLIPTIN | 4.0 | 1 | 8.51 |
| CHEMBL4641763 | — | — | 1 | 8.41 |
| CHEMBL4646510 | COFROGLIPTIN | 2.0 | 1 | 8.38 |
| CHEMBL4644314 | — | — | 1 | 8.15 |
| CHEMBL4636223 | — | — | 1 | 7.93 |
| CHEMBL4640183 | — | — | 1 | 7.74 |
| CHEMBL4634272 | — | — | 1 | 7.69 |
| CHEMBL4640418 | — | — | 1 | 7.66 |
| CHEMBL4634474 | — | — | 1 | 7.58 |
| CHEMBL4635433 | — | — | 1 | 7.31 |
| CHEMBL4649110 | — | — | 1 | 7.22 |
| CHEMBL4635648 | — | — | 1 | - |
| CHEMBL4633377 | — | — | 1 | - |
| CHEMBL4643841 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105762 | OMARIGLIPTIN | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4641763 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4646510 | COFROGLIPTIN | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4644314 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL4636223 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4640183 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL4634272 | — | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL4640418 | — | IC50 | = | 22.1 | nM | 7.66 |
| CHEMBL4634474 | — | IC50 | = | 26.5 | nM | 7.58 |
| CHEMBL4635433 | — | IC50 | = | 48.9 | nM | 7.31 |
| CHEMBL4649110 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4635648 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4633377 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4643841 | — | IC50 | > | 1000.0 | nM | - |