Assay Detail
Binding
CHEMBL1780909
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human DPP-4 assessed as H-Gly-Pro-AMC cleavage after 1 hr by fluorescence assay
27
Total Activities
27
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
Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.75 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1779710 | EVOGLIPTIN | 4.0 | 1 | 9.05 |
| CHEMBL1779714 | — | — | 1 | 8.89 |
| CHEMBL1779708 | — | — | 1 | 8.77 |
| CHEMBL1779709 | — | — | 1 | 8.66 |
| CHEMBL1779707 | — | — | 1 | 8.37 |
| CHEMBL1779713 | — | — | 1 | 8.28 |
| CHEMBL1779706 | — | — | 1 | 8.13 |
| CHEMBL1779704 | — | — | 1 | 8.13 |
| CHEMBL1779712 | — | — | 1 | 7.96 |
| CHEMBL1779705 | — | — | 1 | 7.92 |
| CHEMBL1779695 | — | — | 1 | 7.86 |
| CHEMBL1779711 | — | — | 1 | 7.77 |
| CHEMBL1779702 | — | — | 1 | 7.57 |
| CHEMBL1779703 | — | — | 1 | 7.54 |
| CHEMBL1779701 | — | — | 1 | 7.51 |
| CHEMBL1779700 | — | — | 1 | 7.47 |
| CHEMBL1779699 | — | — | 1 | 7.47 |
| CHEMBL1779694 | — | — | 1 | 7.42 |
| CHEMBL1779698 | — | — | 1 | 7.41 |
| CHEMBL1779691 | — | — | 1 | 7.37 |
| CHEMBL1779690 | — | — | 1 | 7.35 |
| CHEMBL1779696 | — | — | 1 | 7.31 |
| CHEMBL1779697 | — | — | 1 | 7.29 |
| CHEMBL1779693 | — | — | 1 | 7.27 |
| CHEMBL1779688 | — | — | 1 | 7.03 |
| CHEMBL1779692 | — | — | 1 | 6.94 |
| CHEMBL1779689 | — | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1779710 | EVOGLIPTIN | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1779714 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1779708 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1779709 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL1779707 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1779713 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL1779706 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL1779704 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL1779712 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1779705 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1779695 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL1779711 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1779702 | — | IC50 | = | 26.7 | nM | 7.57 |
| CHEMBL1779703 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1779701 | — | IC50 | = | 30.8 | nM | 7.51 |
| CHEMBL1779700 | — | IC50 | = | 33.8 | nM | 7.47 |
| CHEMBL1779699 | — | IC50 | = | 33.9 | nM | 7.47 |
| CHEMBL1779694 | — | IC50 | = | 38.5 | nM | 7.42 |
| CHEMBL1779698 | — | IC50 | = | 38.9 | nM | 7.41 |
| CHEMBL1779691 | — | IC50 | = | 42.7 | nM | 7.37 |
| CHEMBL1779690 | — | IC50 | = | 44.8 | nM | 7.35 |
| CHEMBL1779696 | — | IC50 | = | 48.9 | nM | 7.31 |
| CHEMBL1779697 | — | IC50 | = | 50.7 | nM | 7.29 |
| CHEMBL1779693 | — | IC50 | = | 54.1 | nM | 7.27 |
| CHEMBL1779688 | — | IC50 | = | 92.6 | nM | 7.03 |
| CHEMBL1779692 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL1779689 | — | IC50 | = | 311.0 | nM | 6.51 |