Assay Detail
Binding
CHEMBL912988
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Inhibition of DPP8
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.12 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL94278 | — | — | 1 | 8.40 |
| CHEMBL3085037 | — | — | 1 | 6.96 |
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | 4.0 | 1 | 6.89 |
| CHEMBL95089 | — | — | 1 | 5.91 |
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 5.87 |
| CHEMBL217455 | — | — | 1 | 5.28 |
| CHEMBL96937 | — | — | 1 | 4.91 |
| CHEMBL217252 | — | — | 1 | 4.75 |
| CHEMBL217040 | — | — | 1 | - |
| CHEMBL386654 | — | — | 1 | - |
| CHEMBL385904 | — | — | 1 | - |
| CHEMBL217654 | — | — | 1 | - |
| CHEMBL387297 | — | — | 1 | - |
| CHEMBL386369 | — | — | 1 | - |
| CHEMBL216957 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL94278 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3085037 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL95089 | — | Ki | = | 1218.0 | nM | 5.91 |
| CHEMBL142703 | VILDAGLIPTIN | Ki | = | 1342.0 | nM | 5.87 |
| CHEMBL217455 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL96937 | — | Ki | = | 12360.0 | nM | 4.91 |
| CHEMBL217252 | — | Ki | = | 17700.0 | nM | 4.75 |
| CHEMBL217040 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL386654 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL385904 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL217654 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL387297 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL386369 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL216957 | — | Ki | > | 30000.0 | nM | - |