Assay Detail
Binding
CHEMBL2168593
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Activation of human recombinant glucokinase using 6.5 mM glucose by spectrophotometric analysis
13
Total Activities
13
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
Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 6.46 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2165620 | PF-04991532 | 2.0 | 1 | 7.05 |
| CHEMBL2165619 | — | — | 1 | 6.94 |
| CHEMBL2165615 | NERIGLIATIN | 2.0 | 1 | 6.73 |
| CHEMBL2165616 | — | — | 1 | 6.67 |
| CHEMBL2165626 | — | — | 1 | 6.55 |
| CHEMBL2165627 | — | — | 1 | 6.34 |
| CHEMBL2165623 | — | — | 1 | 6.25 |
| CHEMBL2165617 | — | — | 1 | 5.97 |
| CHEMBL2165624 | — | — | 1 | 5.60 |
| CHEMBL2165618 | — | — | 1 | - |
| CHEMBL2165625 | — | — | 1 | - |
| CHEMBL2165622 | — | — | 1 | - |
| CHEMBL2165621 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2165620 | PF-04991532 | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2165619 | — | EC50 | = | 114.0 | nM | 6.94 |
| CHEMBL2165615 | NERIGLIATIN | EC50 | = | 188.0 | nM | 6.73 |
| CHEMBL2165616 | — | EC50 | = | 212.0 | nM | 6.67 |
| CHEMBL2165626 | — | EC50 | = | 284.0 | nM | 6.55 |
| CHEMBL2165627 | — | EC50 | = | 456.0 | nM | 6.34 |
| CHEMBL2165623 | — | EC50 | = | 565.0 | nM | 6.25 |
| CHEMBL2165617 | — | EC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL2165624 | — | EC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL2165618 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2165625 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2165622 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2165621 | — | EC50 | > | 10000.0 | nM | - |