Assay Detail
Binding
CHEMBL4379983
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Inhibition of human DPP4 in pH 7.4 Tris buffer using AP-7-ATFMC as substrate preincubated for 15 mins followed by substrate addition by microplate reader analysis
5
Total Activities
5
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
Synthesis and discovery of triazolo-pyridazine-6-yl-substituted piperazines as effective anti-diabetic drugs; evaluated over dipeptidyl peptidase-4 inhibition mechanism and insulinotropic activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.83 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4454091 | — | — | 1 | 9.12 |
| CHEMBL237500 | LINAGLIPTIN | 4.0 | 1 | 8.90 |
| CHEMBL4460852 | — | — | 1 | 8.76 |
| CHEMBL4547171 | — | — | 1 | 8.70 |
| CHEMBL4529301 | — | — | 1 | 8.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4454091 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL237500 | LINAGLIPTIN | IC50 | = | 1.25 | nM | 8.90 |
| CHEMBL4460852 | — | IC50 | = | 1.75 | nM | 8.76 |
| CHEMBL4547171 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4529301 | — | IC50 | = | 2.25 | nM | 8.65 |