Assay Detail
Binding
CHEMBL3583541
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Activation of recombinant human glucokinase assessed as formation of glucose-6-phosphate by G6PDH/NADP coupled assay
17
Total Activities
16
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
Optimizing glucokinase activator binding kinetics to lower in vivo hypoglycemia risk
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 7.19 | 8.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3580738 | — | — | 2 | 8.03 |
| CHEMBL3580737 | MK-0941 FREE BASE | 2.0 | 1 | 8.02 |
| CHEMBL3217925 | — | — | 1 | 7.79 |
| CHEMBL3580740 | — | — | 1 | 7.62 |
| CHEMBL3218477 | — | — | 1 | 7.58 |
| CHEMBL3219124 | AZD-1656 | 2.0 | 1 | 7.55 |
| CHEMBL499520 | — | — | 1 | 7.43 |
| CHEMBL3580742 | — | — | 1 | 7.28 |
| CHEMBL608393 | — | — | 1 | 7.10 |
| CHEMBL2204663 | — | — | 1 | 6.94 |
| CHEMBL3580739 | — | — | 1 | 6.92 |
| CHEMBL2165615 | NERIGLIATIN | 2.0 | 1 | 6.76 |
| CHEMBL3580741 | — | — | 1 | 6.72 |
| CHEMBL2165616 | — | — | 1 | 6.68 |
| CHEMBL1783734 | PIRAGLIATIN | 2.0 | 1 | 6.44 |
| CHEMBL2204655 | — | — | 1 | 6.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3580738 | — | EC50 | = | 9.4 | nM | 8.03 |
| CHEMBL3580737 | MK-0941 FREE BASE | EC50 | = | 9.5 | nM | 8.02 |
| CHEMBL3217925 | — | EC50 | = | 16.2 | nM | 7.79 |
| CHEMBL3580740 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3218477 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3219124 | AZD-1656 | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL499520 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3580742 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL608393 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2204663 | — | EC50 | = | 114.0 | nM | 6.94 |
| CHEMBL3580738 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3580739 | — | EC50 | = | 121.0 | nM | 6.92 |
| CHEMBL2165615 | NERIGLIATIN | EC50 | = | 174.0 | nM | 6.76 |
| CHEMBL3580741 | — | EC50 | = | 191.0 | nM | 6.72 |
| CHEMBL2165616 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1783734 | PIRAGLIATIN | EC50 | = | 364.0 | nM | 6.44 |
| CHEMBL2204655 | — | EC50 | = | 391.0 | nM | 6.41 |