Assay Detail
Binding
CHEMBL2424447
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Inhibition of human purified His-tagged DPP-9 assessed as cleavage of substrate using Gly-Pro-AMC chromogenic substrate after 60 mins by fluorescence spectrophotometry
18
Total Activities
18
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 and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.41 | 7.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 7.18 |
| CHEMBL2418633 | — | — | 1 | 6.58 |
| CHEMBL2418627 | — | — | 1 | 6.55 |
| CHEMBL2418630 | — | — | 1 | 6.51 |
| CHEMBL2418631 | — | — | 1 | 6.48 |
| CHEMBL2418624 | — | — | 1 | 6.47 |
| CHEMBL2418628 | — | — | 1 | 6.47 |
| CHEMBL2417563 | — | — | 1 | 6.46 |
| CHEMBL2418625 | — | — | 1 | 6.44 |
| CHEMBL2418632 | — | — | 1 | 6.36 |
| CHEMBL2418626 | — | — | 1 | 6.36 |
| CHEMBL2418639 | — | — | 1 | 6.35 |
| CHEMBL2418629 | — | — | 1 | 6.26 |
| CHEMBL2418634 | — | — | 1 | 6.22 |
| CHEMBL2418637 | — | — | 1 | 6.21 |
| CHEMBL2418636 | — | — | 1 | 6.20 |
| CHEMBL2418638 | — | — | 1 | 5.79 |
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL142703 | VILDAGLIPTIN | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2418633 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2418627 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2418630 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2418631 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2418624 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2418628 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2417563 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL2418625 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL2418632 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2418626 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2418639 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL2418629 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL2418634 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2418637 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL2418636 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL2418638 | — | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL1422 | SITAGLIPTIN | IC50 | = | 130240.0 | nM | - |