Assay Detail
Binding
CHEMBL4711280
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Inhibition of DPP4 in human Caco-2 cells using AP-AFC as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 10 mins by fluorescence based analysis
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Caco-2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.65 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4784434 | — | — | 1 | 8.70 |
| CHEMBL376359 | ALOGLIPTIN | 4.0 | 1 | 8.40 |
| CHEMBL4764120 | — | — | 1 | 7.05 |
| CHEMBL4743490 | — | — | 1 | 6.52 |
| CHEMBL4798418 | — | — | 1 | 6.40 |
| CHEMBL4765147 | — | — | 1 | 6.33 |
| CHEMBL4764894 | — | — | 1 | 6.10 |
| CHEMBL4754343 | — | — | 1 | 5.96 |
| CHEMBL4798053 | — | — | 1 | 5.92 |
| CHEMBL4752835 | — | — | 1 | 5.80 |
| CHEMBL4794801 | — | — | 1 | 5.62 |
| CHEMBL4754461 | — | — | 1 | 5.55 |
| CHEMBL4749086 | — | — | 1 | 5.46 |
| CHEMBL4791597 | — | — | 1 | 5.24 |
| CHEMBL4763718 | — | — | 1 | 5.10 |
| CHEMBL4743516 | — | — | 1 | 5.09 |
| CHEMBL4787437 | — | — | 1 | 5.04 |
| CHEMBL4745889 | — | — | 1 | 4.93 |
| CHEMBL4786137 | — | — | 1 | 4.84 |
| CHEMBL4760965 | — | — | 1 | 4.75 |
| CHEMBL4753503 | — | — | 1 | 4.65 |
| CHEMBL4782865 | — | — | 1 | 4.63 |
| CHEMBL4751895 | — | — | 1 | 4.60 |
| CHEMBL4779718 | — | — | 1 | 4.50 |
| CHEMBL4776878 | — | — | 1 | 4.09 |
| CHEMBL4794198 | — | — | 1 | - |
| CHEMBL4751103 | — | — | 1 | - |
| CHEMBL4799877 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4784434 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL376359 | ALOGLIPTIN | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4764120 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4743490 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4798418 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4765147 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4764894 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4754343 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4798053 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4752835 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4794801 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4754461 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4749086 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4791597 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4763718 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL4743516 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL4787437 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL4745889 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL4786137 | — | IC50 | = | 14400.0 | nM | 4.84 |
| CHEMBL4760965 | — | IC50 | = | 17700.0 | nM | 4.75 |
| CHEMBL4753503 | — | IC50 | = | 22200.0 | nM | 4.65 |
| CHEMBL4782865 | — | IC50 | = | 23600.0 | nM | 4.63 |
| CHEMBL4751895 | — | IC50 | = | 25300.0 | nM | 4.60 |
| CHEMBL4779718 | — | IC50 | = | 31800.0 | nM | 4.50 |
| CHEMBL4776878 | — | IC50 | = | 80500.0 | nM | 4.09 |
| CHEMBL4794198 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4751103 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4799877 | — | IC50 | > | 100000.0 | nM | - |