Assay Detail
Binding
CHEMBL4368093
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Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition measured at 60 secs interval for 20 mins by fluorometic method
22
Total Activities
22
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
Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.47 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4448186 | — | — | 1 | 10.00 |
| CHEMBL4465482 | — | — | 1 | 9.74 |
| CHEMBL4461587 | — | — | 1 | 9.66 |
| CHEMBL4588692 | — | — | 1 | 9.36 |
| CHEMBL4536341 | — | — | 1 | 9.14 |
| CHEMBL4544024 | — | — | 1 | 8.98 |
| CHEMBL4452518 | — | — | 1 | 8.70 |
| CHEMBL4446618 | — | — | 1 | 8.66 |
| CHEMBL4528994 | — | — | 1 | 8.63 |
| CHEMBL4464069 | — | — | 1 | 8.61 |
| CHEMBL4435383 | — | — | 1 | 8.54 |
| CHEMBL4458949 | — | — | 1 | 8.41 |
| CHEMBL376359 | ALOGLIPTIN | 4.0 | 1 | 8.35 |
| CHEMBL4590999 | — | — | 1 | 8.30 |
| CHEMBL4458152 | — | — | 1 | 8.25 |
| CHEMBL4458832 | — | — | 1 | 8.22 |
| CHEMBL4441220 | — | — | 1 | 7.99 |
| CHEMBL4567320 | — | — | 1 | 7.69 |
| CHEMBL4465374 | — | — | 1 | 7.66 |
| CHEMBL4465448 | — | — | 1 | 7.29 |
| CHEMBL4468590 | — | — | 1 | 7.13 |
| CHEMBL4528149 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4448186 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4465482 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL4461587 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL4588692 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL4536341 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL4544024 | — | IC50 | = | 1.05 | nM | 8.98 |
| CHEMBL4452518 | — | IC50 | = | 1.98 | nM | 8.70 |
| CHEMBL4446618 | — | IC50 | = | 2.19 | nM | 8.66 |
| CHEMBL4528994 | — | IC50 | = | 2.35 | nM | 8.63 |
| CHEMBL4464069 | — | IC50 | = | 2.43 | nM | 8.61 |
| CHEMBL4435383 | — | IC50 | = | 2.91 | nM | 8.54 |
| CHEMBL4458949 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL376359 | ALOGLIPTIN | IC50 | = | 4.46 | nM | 8.35 |
| CHEMBL4590999 | — | IC50 | = | 5.06 | nM | 8.30 |
| CHEMBL4458152 | — | IC50 | = | 5.61 | nM | 8.25 |
| CHEMBL4458832 | — | IC50 | = | 5.99 | nM | 8.22 |
| CHEMBL4441220 | — | IC50 | = | 10.21 | nM | 7.99 |
| CHEMBL4567320 | — | IC50 | = | 20.48 | nM | 7.69 |
| CHEMBL4465374 | — | IC50 | = | 22.09 | nM | 7.66 |
| CHEMBL4465448 | — | IC50 | = | 50.9 | nM | 7.29 |
| CHEMBL4468590 | — | IC50 | = | 74.43 | nM | 7.13 |
| CHEMBL4528149 | — | IC50 | = | 85.48 | nM | 7.07 |