Assay Detail
Binding
CHEMBL4014754
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Activation of recombinant human glucokinase assessed as conversion of D-glucose to D-glucose-6-phosphate in presence of 2.5 mM glucose by G6PDH coupled spectrophotometric assay
14
Total Activities
9
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
Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 8.10 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4086782 | — | — | 1 | 8.70 |
| CHEMBL4083339 | — | — | 2 | 8.62 |
| CHEMBL4067028 | — | — | 2 | 8.43 |
| CHEMBL4078915 | — | — | 2 | 8.35 |
| CHEMBL4086771 | — | — | 2 | 8.35 |
| CHEMBL4067037 | — | — | 1 | 8.32 |
| CHEMBL4068048 | — | — | 2 | 8.32 |
| CHEMBL4104680 | — | — | 1 | 8.09 |
| CHEMBL4094511 | — | — | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4086782 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4083339 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4067028 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4067028 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4078915 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4086771 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4067037 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4068048 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4086771 | — | EC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4104680 | — | EC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4094511 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4068048 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4078915 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4083339 | — | EC50 | = | 86.0 | nM | 7.07 |