Assay Detail
Binding
CHEMBL2424448
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Inhibition of human purified His-tagged DPP-8 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 | 6.32 | 6.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2418633 | — | — | 1 | 6.62 |
| CHEMBL2418637 | — | — | 1 | 6.55 |
| CHEMBL2418630 | — | — | 1 | 6.52 |
| CHEMBL2417563 | — | — | 1 | 6.50 |
| CHEMBL2418624 | — | — | 1 | 6.48 |
| CHEMBL2418628 | — | — | 1 | 6.47 |
| CHEMBL2418627 | — | — | 1 | 6.41 |
| CHEMBL2418625 | — | — | 1 | 6.37 |
| CHEMBL2418626 | — | — | 1 | 6.36 |
| CHEMBL2418631 | — | — | 1 | 6.35 |
| CHEMBL2418634 | — | — | 1 | 6.33 |
| CHEMBL2418639 | — | — | 1 | 6.29 |
| CHEMBL2418636 | — | — | 1 | 6.17 |
| CHEMBL2418632 | — | — | 1 | 6.16 |
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 5.96 |
| CHEMBL2418638 | — | — | 1 | 5.95 |
| CHEMBL2418629 | — | — | 1 | 5.92 |
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2418633 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2418637 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2418630 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2417563 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL2418624 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2418628 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2418627 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL2418625 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL2418626 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2418631 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL2418634 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL2418639 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL2418636 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL2418632 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL142703 | VILDAGLIPTIN | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2418638 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL2418629 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL1422 | SITAGLIPTIN | IC50 | = | 114830.0 | nM | - |