Assay Detail
Binding
CHEMBL4014758
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Activation of glucokinase in rat INS-1 cells assessed as increase in D-2-deoxyglucose-6-phosphate level in presence of D-2-deoxyglucose by HILIC LC-MS method
14
Total Activities
9
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
Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 7.68 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4067028 | — | — | 2 | 9.05 |
| CHEMBL4086782 | — | — | 1 | 8.77 |
| CHEMBL4083339 | — | — | 2 | 8.60 |
| CHEMBL4068048 | — | — | 2 | 8.41 |
| CHEMBL4078915 | — | — | 2 | 8.14 |
| CHEMBL4104680 | — | — | 1 | 8.11 |
| CHEMBL4086771 | — | — | 2 | 7.68 |
| CHEMBL4067037 | — | — | 1 | 7.66 |
| CHEMBL4094511 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4067028 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4086782 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4083339 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4068048 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4078915 | — | EC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4104680 | — | EC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4086771 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4067037 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4067028 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4086771 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4068048 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4078915 | — | EC50 | = | 247.0 | nM | 6.61 |
| CHEMBL4083339 | — | EC50 | = | 375.0 | nM | 6.43 |
| CHEMBL4094511 | — | EC50 | = | 2111.0 | nM | 5.68 |