Assay Detail
Binding
CHEMBL3737791
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Inhibition of C-terminal His-tagged DPP8 (unknown origin) expressed in COS7 cells using H-Ala-Pro-pNA substrate preincubated for 15 mins
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 4.30 | 4.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3736511 | — | — | 1 | 4.60 |
| CHEMBL3736067 | — | — | 1 | 4.57 |
| CHEMBL3735843 | — | — | 1 | 4.39 |
| CHEMBL3736423 | — | — | 1 | 4.39 |
| CHEMBL3735852 | — | — | 1 | 4.36 |
| CHEMBL3735925 | — | — | 1 | 4.33 |
| CHEMBL3735129 | — | — | 1 | 4.26 |
| CHEMBL3735917 | — | — | 1 | 4.22 |
| CHEMBL3736085 | — | — | 1 | 4.22 |
| CHEMBL3736137 | — | — | 1 | 4.21 |
| CHEMBL3734828 | — | — | 1 | 4.05 |
| CHEMBL3734999 | — | — | 1 | 4.04 |
| CHEMBL3735865 | — | — | 1 | - |
| CHEMBL3736190 | — | — | 1 | - |
| CHEMBL3735329 | — | — | 1 | - |
| CHEMBL3645492 | — | — | 1 | - |
| CHEMBL3735281 | — | — | 1 | - |
| CHEMBL3736188 | — | — | 1 | - |
| CHEMBL2105762 | OMARIGLIPTIN | 4.0 | 1 | - |
| CHEMBL3736135 | — | — | 1 | - |
| CHEMBL3734912 | — | — | 1 | - |
| CHEMBL3734769 | — | — | 1 | - |
| CHEMBL3735461 | — | — | 1 | - |
| CHEMBL3735433 | — | — | 1 | - |
| CHEMBL3735694 | — | — | 1 | - |
| CHEMBL2425070 | — | — | 1 | - |
| CHEMBL3734964 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3736511 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL3736067 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL3735843 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL3736423 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL3735852 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL3735925 | — | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL3735129 | — | IC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL3735917 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL3736085 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL3736137 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL3734828 | — | IC50 | = | 89000.0 | nM | 4.05 |
| CHEMBL3734999 | — | IC50 | = | 91000.0 | nM | 4.04 |
| CHEMBL3735865 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3736190 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3735329 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3645492 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3735281 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3736188 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2105762 | OMARIGLIPTIN | IC50 | > | 100000.0 | nM | - |
| CHEMBL3736135 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3734912 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3734769 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3735461 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3735433 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3735694 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2425070 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3734964 | — | IC50 | > | 100000.0 | nM | - |