Assay Detail
Binding
CHEMBL3223667
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Activation of rat glucokinase
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 6.82 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL499520 | — | — | 1 | 7.30 |
| CHEMBL3218477 | — | — | 1 | 7.30 |
| CHEMBL1783734 | PIRAGLIATIN | 2.0 | 1 | 7.00 |
| CHEMBL3218478 | — | — | 1 | 6.73 |
| CHEMBL1096435 | Ro-281675 | — | 1 | 6.63 |
| CHEMBL575726 | — | — | 1 | 6.41 |
| CHEMBL2165615 | NERIGLIATIN | 2.0 | 1 | 6.39 |
| CHEMBL1783735 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL499520 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3218477 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1783734 | PIRAGLIATIN | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3218478 | — | EC50 | = | 187.0 | nM | 6.73 |
| CHEMBL1096435 | Ro-281675 | EC50 | = | 235.0 | nM | 6.63 |
| CHEMBL575726 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL2165615 | NERIGLIATIN | EC50 | = | 407.0 | nM | 6.39 |
| CHEMBL1783735 | — | EC50 | - | — | - |