Assay Detail
Binding
CHEMBL2424445
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Inhibition of human purified His-tagged DPP-4 assessed as cleavage of substrate using Gly-Pro-AMC chromogenic substrate after 60 mins by fluorescence spectrophotometry
19
Total Activities
19
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 | 19 | 7.92 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 8.52 |
| CHEMBL2418626 | — | — | 1 | 8.42 |
| CHEMBL2418631 | — | — | 1 | 8.36 |
| CHEMBL2418628 | — | — | 1 | 8.22 |
| CHEMBL2418630 | — | — | 1 | 8.12 |
| CHEMBL2418625 | — | — | 1 | 8.12 |
| CHEMBL2418639 | — | — | 1 | 8.08 |
| CHEMBL2418632 | — | — | 1 | 8.07 |
| CHEMBL2418636 | — | — | 1 | 8.03 |
| CHEMBL2418633 | — | — | 1 | 8.00 |
| CHEMBL2417563 | — | — | 1 | 7.98 |
| CHEMBL2418627 | — | — | 1 | 7.82 |
| CHEMBL2418634 | — | — | 1 | 7.80 |
| CHEMBL2418638 | — | — | 1 | 7.75 |
| CHEMBL2418624 | — | — | 1 | 7.71 |
| CHEMBL2418629 | — | — | 1 | 7.68 |
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | 7.61 |
| CHEMBL2418637 | — | — | 1 | 7.59 |
| CHEMBL2418635 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL142703 | VILDAGLIPTIN | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2418626 | — | IC50 | = | 3.79 | nM | 8.42 |
| CHEMBL2418631 | — | IC50 | = | 4.35 | nM | 8.36 |
| CHEMBL2418628 | — | IC50 | = | 6.05 | nM | 8.22 |
| CHEMBL2418630 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL2418625 | — | IC50 | = | 7.56 | nM | 8.12 |
| CHEMBL2418639 | — | IC50 | = | 8.28 | nM | 8.08 |
| CHEMBL2418632 | — | IC50 | = | 8.57 | nM | 8.07 |
| CHEMBL2418636 | — | IC50 | = | 9.39 | nM | 8.03 |
| CHEMBL2418633 | — | IC50 | = | 10.02 | nM | 8.00 |
| CHEMBL2417563 | — | IC50 | = | 10.45 | nM | 7.98 |
| CHEMBL2418627 | — | IC50 | = | 15.24 | nM | 7.82 |
| CHEMBL2418634 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL2418638 | — | IC50 | = | 17.61 | nM | 7.75 |
| CHEMBL2418624 | — | IC50 | = | 19.54 | nM | 7.71 |
| CHEMBL2418629 | — | IC50 | = | 20.84 | nM | 7.68 |
| CHEMBL1422 | SITAGLIPTIN | IC50 | = | 24.83 | nM | 7.61 |
| CHEMBL2418637 | — | IC50 | = | 25.5 | nM | 7.59 |
| CHEMBL2418635 | — | IC50 | = | 265.0 | nM | 6.58 |