Assay Detail
Binding
CHEMBL2429190
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Inhibition of human DPP-4 using Gly-pro-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins
16
Total Activities
16
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
Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.16 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2425893 | — | — | 1 | 9.40 |
| CHEMBL2425894 | — | — | 1 | 9.15 |
| CHEMBL2425895 | — | — | 1 | 8.92 |
| CHEMBL376359 | ALOGLIPTIN | 4.0 | 1 | 8.82 |
| CHEMBL2425892 | — | — | 1 | 8.72 |
| CHEMBL2425890 | — | — | 1 | 8.70 |
| CHEMBL2425886 | — | — | 1 | 8.51 |
| CHEMBL2425884 | — | — | 1 | 8.47 |
| CHEMBL2425889 | — | — | 1 | 8.18 |
| CHEMBL2425891 | — | — | 1 | 8.04 |
| CHEMBL2425888 | — | — | 1 | 7.97 |
| CHEMBL2425885 | — | — | 1 | 7.66 |
| CHEMBL2425887 | — | — | 1 | 7.50 |
| CHEMBL2424672 | — | — | 1 | 6.70 |
| CHEMBL2425882 | — | — | 1 | 5.66 |
| CHEMBL2425883 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2425893 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL2425894 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL2425895 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL376359 | ALOGLIPTIN | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2425892 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2425890 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2425886 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL2425884 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL2425889 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL2425891 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL2425888 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL2425885 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2425887 | — | IC50 | = | 31.3 | nM | 7.50 |
| CHEMBL2424672 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL2425882 | — | IC50 | = | 2177.5 | nM | 5.66 |
| CHEMBL2425883 | — | IC50 | > | 10000.0 | nM | - |