Assay Detail
Binding
CHEMBL4187777
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DPP4 using A-P-7-amido-4-trifluoromethylcoumarin as substrate pretreated for 10 mins followed by substrate addition measured after 10 mins
14
Total Activities
14
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
Surrogating and redirection of pyrazolo[1,5-a]pyrimidin-7(4H)-one core, a novel class of potent and selective DPP-4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.73 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376359 | ALOGLIPTIN | 4.0 | 1 | 8.40 |
| CHEMBL4205581 | — | — | 1 | 7.31 |
| CHEMBL4204176 | — | — | 1 | 7.10 |
| CHEMBL4212894 | — | — | 1 | 6.40 |
| CHEMBL4213950 | — | — | 1 | 5.92 |
| CHEMBL4215849 | — | — | 1 | 5.89 |
| CHEMBL4207996 | — | — | 1 | 5.70 |
| CHEMBL4208513 | — | — | 1 | 5.60 |
| CHEMBL4216792 | — | — | 1 | 4.98 |
| CHEMBL4212367 | — | — | 1 | 4.94 |
| CHEMBL4217326 | — | — | 1 | 4.76 |
| CHEMBL4210635 | — | — | 1 | 4.67 |
| CHEMBL4203639 | — | — | 1 | 4.33 |
| CHEMBL4205100 | — | — | 1 | 4.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376359 | ALOGLIPTIN | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4205581 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4204176 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4212894 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4213950 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4215849 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4207996 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4208513 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4216792 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL4212367 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL4217326 | — | IC50 | = | 17200.0 | nM | 4.76 |
| CHEMBL4210635 | — | IC50 | = | 21500.0 | nM | 4.67 |
| CHEMBL4203639 | — | IC50 | = | 46500.0 | nM | 4.33 |
| CHEMBL4205100 | — | IC50 | = | 59900.0 | nM | 4.22 |