Assay Detail
Binding
CHEMBL4688063
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Inhibition of recombinant human DPP4 using Gly-Pro-AMC as substrate incubated for 1 hr by fluorogenic assay
11
Total Activities
11
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
Synthesis, in vitro evaluation, and computational simulations studies of 1,2,3-triazole analogues as DPP-4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.94 | 8.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | 8.11 |
| CHEMBL4250492 | — | — | 1 | 7.85 |
| CHEMBL4790735 | — | — | 1 | 7.55 |
| CHEMBL4789426 | — | — | 1 | 6.92 |
| CHEMBL4747721 | — | — | 1 | 6.88 |
| CHEMBL4750352 | — | — | 1 | 6.84 |
| CHEMBL4792546 | — | — | 1 | 6.59 |
| CHEMBL4745231 | — | — | 1 | 6.58 |
| CHEMBL4790799 | — | — | 1 | 6.52 |
| CHEMBL4763110 | — | — | 1 | 6.37 |
| CHEMBL4798357 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1422 | SITAGLIPTIN | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4250492 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4790735 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4789426 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL4747721 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL4750352 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL4792546 | — | IC50 | = | 254.0 | nM | 6.59 |
| CHEMBL4745231 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL4790799 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL4763110 | — | IC50 | = | 427.0 | nM | 6.37 |
| CHEMBL4798357 | — | IC50 | = | 780.0 | nM | 6.11 |