Assay Detail
Functional
CHEMBL4379990
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Antidiabetic activity in glucose-treated rat INS1(832/13) cells assessed as increase in insulin release in presence of 3 mM glucose measured after 2 hrs by radioimmunoassay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | INS1(832/13) |
| Confidence | 1 — Organism |
| 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 | 8.00 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4529301 | — | — | 1 | 8.82 |
| CHEMBL4454091 | — | — | 1 | 8.55 |
| CHEMBL4547171 | — | — | 1 | 8.41 |
| CHEMBL4460852 | — | — | 1 | 8.32 |
| CHEMBL1272 | REPAGLINIDE | 4.0 | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4529301 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4454091 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4547171 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4460852 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL1272 | REPAGLINIDE | IC50 | = | 1250.0 | nM | 5.90 |