Assay Detail
Binding
CHEMBL4057936
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Agonist activity at SUR in Wistar rat pancreatic islets assessed as increase in insulin secretion at 5 to 20 uM incubated for 1 hr followed by glucose addition for 30 mins by quantitative sandwich enzyme immunoassay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis, molecular modeling and anti-hyperglycemic evaluation of quinazolin-4(3H)-one derivatives as potential PPARγ and SUR agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 5.80 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1481 | GLIMEPIRIDE | 4.0 | 1 | 6.10 |
| CHEMBL4068985 | — | — | 1 | 6.01 |
| CHEMBL4069917 | — | — | 1 | 6.00 |
| CHEMBL4088467 | — | — | 1 | 5.94 |
| CHEMBL4085687 | — | — | 1 | 5.88 |
| CHEMBL4093428 | — | — | 1 | 5.82 |
| CHEMBL4104828 | — | — | 1 | 5.78 |
| CHEMBL4080597 | — | — | 1 | 5.60 |
| CHEMBL4097121 | — | — | 1 | 5.57 |
| CHEMBL4089408 | — | — | 1 | 5.54 |
| CHEMBL4072706 | — | — | 1 | 5.51 |
| CHEMBL4067207 | — | — | 1 | - |
| CHEMBL4061252 | — | — | 1 | - |
| CHEMBL4090062 | — | — | 1 | - |
| CHEMBL4103939 | — | — | 1 | - |
| CHEMBL4086021 | — | — | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1481 | GLIMEPIRIDE | EC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4068985 | — | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4069917 | — | EC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4088467 | — | EC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL4085687 | — | EC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL4093428 | — | EC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL4104828 | — | EC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL4080597 | — | EC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL4097121 | — | EC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL4089408 | — | EC50 | = | 2910.0 | nM | 5.54 |
| CHEMBL4072706 | — | EC50 | = | 3090.0 | nM | 5.51 |
| CHEMBL4067207 | — | EC50 | - | — | - | |
| CHEMBL4061252 | — | EC50 | - | — | - | |
| CHEMBL4090062 | — | EC50 | - | — | - | |
| CHEMBL4103939 | — | EC50 | - | — | - | |
| CHEMBL4086021 | — | EC50 | - | — | - | |
| CHEMBL121 | ROSIGLITAZONE | EC50 | - | — | - |