Assay Detail
Binding
CHEMBL4413686
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Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.92 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4446618 | — | — | 1 | 8.77 |
| CHEMBL4558007 | — | — | 1 | 8.60 |
| CHEMBL376359 | ALOGLIPTIN | 4.0 | 1 | 8.57 |
| CHEMBL4516959 | — | — | 1 | 8.46 |
| CHEMBL4562685 | — | — | 1 | 8.41 |
| CHEMBL4581959 | — | — | 1 | 8.40 |
| CHEMBL4527363 | — | — | 1 | 8.34 |
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | 8.16 |
| CHEMBL4538597 | — | — | 1 | 8.12 |
| CHEMBL4438210 | — | — | 1 | 8.12 |
| CHEMBL4530011 | — | — | 1 | 7.25 |
| CHEMBL4436620 | — | — | 1 | 7.13 |
| CHEMBL4468423 | — | — | 1 | 7.05 |
| CHEMBL4453917 | — | — | 1 | 7.03 |
| CHEMBL4445783 | — | — | 1 | 6.40 |
| CHEMBL4537845 | — | — | 1 | - |
| CHEMBL4585574 | — | — | 1 | - |
| CHEMBL4559809 | — | — | 1 | - |
| CHEMBL4571572 | — | — | 1 | - |
| CHEMBL4437931 | — | — | 1 | - |
| CHEMBL4540469 | — | — | 1 | - |
| CHEMBL4440121 | — | — | 1 | - |
| CHEMBL4581624 | — | — | 1 | - |
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4446618 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4558007 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL376359 | ALOGLIPTIN | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4516959 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4562685 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4581959 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4527363 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL1422 | SITAGLIPTIN | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4538597 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL4438210 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4530011 | — | IC50 | = | 56.6 | nM | 7.25 |
| CHEMBL4436620 | — | IC50 | = | 74.6 | nM | 7.13 |
| CHEMBL4468423 | — | IC50 | = | 89.8 | nM | 7.05 |
| CHEMBL4453917 | — | IC50 | = | 93.2 | nM | 7.03 |
| CHEMBL4445783 | — | IC50 | = | 395.0 | nM | 6.40 |
| CHEMBL4537845 | — | IC50 | - | — | - | |
| CHEMBL4585574 | — | IC50 | - | — | - | |
| CHEMBL4559809 | — | IC50 | - | — | - | |
| CHEMBL4571572 | — | IC50 | - | — | - | |
| CHEMBL4437931 | — | IC50 | - | — | - | |
| CHEMBL4540469 | — | IC50 | - | — | - | |
| CHEMBL4440121 | — | IC50 | - | — | - | |
| CHEMBL4581624 | — | IC50 | - | — | - | |
| CHEMBL142703 | VILDAGLIPTIN | IC50 | - | — | - |