Assay Detail
Binding
CHEMBL1788085
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Activation of human recombinant glucokinase using 6.5 mM glucose by spectrophotometry
33
Total Activities
33
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
Pyridones as glucokinase activators: identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 33 | 6.36 | 7.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL205627 | — | — | 1 | 7.35 |
| CHEMBL1783740 | — | — | 1 | 7.22 |
| CHEMBL1783745 | — | — | 1 | 7.16 |
| CHEMBL1783739 | — | — | 1 | 6.96 |
| CHEMBL1783753 | — | — | 1 | 6.85 |
| CHEMBL1783744 | — | — | 1 | 6.80 |
| CHEMBL1783748 | — | — | 1 | 6.80 |
| CHEMBL499520 | — | — | 1 | 6.75 |
| CHEMBL1783738 | — | — | 1 | 6.64 |
| CHEMBL1783747 | — | — | 1 | 6.62 |
| CHEMBL1783743 | — | — | 1 | 6.58 |
| CHEMBL1783760 | — | — | 1 | 6.58 |
| CHEMBL1783752 | — | — | 1 | 6.48 |
| CHEMBL1783742 | — | — | 1 | 6.36 |
| CHEMBL1783741 | — | — | 1 | 6.32 |
| CHEMBL1783737 | — | — | 1 | 6.30 |
| CHEMBL1783727 | — | — | 1 | 6.29 |
| CHEMBL1783736 | — | — | 1 | 6.25 |
| CHEMBL1783755 | — | — | 1 | 6.23 |
| CHEMBL1783751 | — | — | 1 | 6.22 |
| CHEMBL1783735 | — | — | 1 | 6.21 |
| CHEMBL1783746 | — | — | 1 | 6.17 |
| CHEMBL1096435 | Ro-281675 | — | 1 | 6.16 |
| CHEMBL1783756 | — | — | 1 | 6.16 |
| CHEMBL1783757 | — | — | 1 | 6.14 |
| CHEMBL1783758 | — | — | 1 | 6.04 |
| CHEMBL1783754 | — | — | 1 | 5.89 |
| CHEMBL1783761 | — | — | 1 | 5.89 |
| CHEMBL1783734 | PIRAGLIATIN | 2.0 | 1 | 5.85 |
| CHEMBL1783749 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL205627 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1783740 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1783745 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1783739 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1783753 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1783744 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1783748 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL499520 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1783738 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1783747 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1783743 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1783760 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1783752 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL1783742 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1783741 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL1783737 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1783727 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL1783736 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL1783755 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1783751 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL1783735 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL1783746 | — | EC50 | = | 670.0 | nM | 6.17 |
| CHEMBL1096435 | Ro-281675 | EC50 | = | 690.0 | nM | 6.16 |
| CHEMBL1783756 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1783757 | — | EC50 | = | 720.0 | nM | 6.14 |
| CHEMBL1783758 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL1783754 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1783761 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1783734 | PIRAGLIATIN | EC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL1783749 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1783759 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1783750 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL1270959 | — | EC50 | = | 3500.0 | nM | 5.46 |