Assay Detail
Binding
CHEMBL4841115
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Inhibition of human recombinant DPP8 using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by fluorescence based microplate reader assay
18
Total Activities
18
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
Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.73 | 8.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 8.73 |
| CHEMBL376359 | ALOGLIPTIN | 4.0 | 1 | - |
| CHEMBL4876933 | — | — | 1 | - |
| CHEMBL4863102 | — | — | 1 | - |
| CHEMBL4857729 | — | — | 1 | - |
| CHEMBL4875769 | — | — | 1 | - |
| CHEMBL4856337 | — | — | 1 | - |
| CHEMBL4860737 | — | — | 1 | - |
| CHEMBL4873862 | — | — | 1 | - |
| CHEMBL4865204 | — | — | 1 | - |
| CHEMBL4846335 | — | — | 1 | - |
| CHEMBL4876894 | — | — | 1 | - |
| CHEMBL4852700 | — | — | 1 | - |
| CHEMBL4851477 | — | — | 1 | - |
| CHEMBL4863369 | — | — | 1 | - |
| CHEMBL4856255 | — | — | 1 | - |
| CHEMBL4845890 | — | — | 1 | - |
| CHEMBL4871141 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL142703 | VILDAGLIPTIN | IC50 | = | 1.85 | nM | 8.73 |
| CHEMBL376359 | ALOGLIPTIN | IC50 | > | 100.0 | nM | - |
| CHEMBL4876933 | — | IC50 | - | — | - | |
| CHEMBL4863102 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4857729 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4875769 | — | IC50 | - | — | - | |
| CHEMBL4856337 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4860737 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4873862 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4865204 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4846335 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4876894 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4852700 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4851477 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4863369 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4856255 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4845890 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4871141 | — | IC50 | > | 100.0 | nM | - |