Assay Detail
Binding
CHEMBL912987
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Inhibition of human DPP4 expressed in Caco-2 cells
27
Total Activities
27
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 | 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 | 27 | 7.76 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | 4.0 | 1 | 9.22 |
| CHEMBL217455 | — | — | 1 | 9.00 |
| CHEMBL386369 | — | — | 1 | 9.00 |
| CHEMBL94278 | — | — | 1 | 9.00 |
| CHEMBL216957 | — | — | 1 | 8.89 |
| CHEMBL387297 | — | — | 1 | 8.52 |
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 8.40 |
| CHEMBL3085037 | — | — | 1 | 8.40 |
| CHEMBL217040 | — | — | 1 | 8.30 |
| CHEMBL217766 | — | — | 1 | 8.10 |
| CHEMBL217252 | — | — | 1 | 8.10 |
| CHEMBL96937 | — | — | 1 | 8.00 |
| CHEMBL95089 | — | — | 1 | 7.96 |
| CHEMBL217654 | — | — | 1 | 7.66 |
| CHEMBL387232 | — | — | 1 | 7.62 |
| CHEMBL385904 | — | — | 1 | 7.60 |
| CHEMBL217032 | — | — | 1 | 7.31 |
| CHEMBL386654 | — | — | 1 | 7.21 |
| CHEMBL217155 | — | — | 1 | 7.10 |
| CHEMBL385247 | — | — | 1 | 7.05 |
| CHEMBL386022 | — | — | 1 | 7.02 |
| CHEMBL217001 | — | — | 1 | 7.01 |
| CHEMBL385483 | — | — | 1 | 6.09 |
| CHEMBL217138 | — | — | 1 | 6.02 |
| CHEMBL385024 | — | — | 1 | 5.42 |
| CHEMBL216900 | — | — | 1 | - |
| CHEMBL216370 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL217455 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL386369 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL94278 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL216957 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL387297 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL142703 | VILDAGLIPTIN | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3085037 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL217040 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL217766 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL217252 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL96937 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL95089 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL217654 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL387232 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL385904 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL217032 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL386654 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL217155 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL385247 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL386022 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL217001 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL385483 | — | Ki | = | 811.0 | nM | 6.09 |
| CHEMBL217138 | — | Ki | = | 959.0 | nM | 6.02 |
| CHEMBL385024 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL216900 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL216370 | — | Ki | > | 30000.0 | nM | - |