Assay Detail
Binding
CHEMBL3223666
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Activation of recombinant human glucokinase assessed as formation of glucose-6-phosphate by G6PDH/NADP coupled assay
32
Total Activities
32
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
Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 32 | 6.59 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3218477 | — | — | 1 | 7.57 |
| CHEMBL499520 | — | — | 1 | 7.43 |
| CHEMBL3218488 | — | — | 1 | 7.19 |
| CHEMBL1783735 | — | — | 1 | 7.18 |
| CHEMBL3218487 | — | — | 1 | 7.07 |
| CHEMBL3218478 | — | — | 1 | 7.06 |
| CHEMBL3218482 | — | — | 1 | 7.04 |
| CHEMBL575726 | — | — | 1 | 6.91 |
| CHEMBL3218497 | — | — | 1 | 6.90 |
| CHEMBL3218485 | — | — | 1 | 6.82 |
| CHEMBL3218498 | — | — | 1 | 6.78 |
| CHEMBL2165615 | NERIGLIATIN | 2.0 | 1 | 6.73 |
| CHEMBL2165616 | — | — | 1 | 6.67 |
| CHEMBL3218499 | — | — | 1 | 6.59 |
| CHEMBL3218489 | — | — | 1 | 6.58 |
| CHEMBL1096435 | Ro-281675 | — | 1 | 6.48 |
| CHEMBL3218500 | — | — | 1 | 6.48 |
| CHEMBL1783734 | PIRAGLIATIN | 2.0 | 1 | 6.44 |
| CHEMBL3218490 | — | — | 1 | 6.41 |
| CHEMBL3218496 | — | — | 1 | 6.41 |
| CHEMBL3218483 | — | — | 1 | 6.32 |
| CHEMBL3218495 | — | — | 1 | 6.32 |
| CHEMBL3218491 | — | — | 1 | 6.15 |
| CHEMBL3218480 | — | — | 1 | 6.06 |
| CHEMBL3218494 | — | — | 1 | 5.66 |
| CHEMBL3218481 | — | — | 1 | 5.51 |
| CHEMBL3218479 | — | — | 1 | 5.18 |
| CHEMBL3218501 | — | — | 1 | - |
| CHEMBL3218493 | — | — | 1 | - |
| CHEMBL3218492 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3218477 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL499520 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3218488 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1783735 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3218487 | — | EC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3218478 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3218482 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL575726 | — | EC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3218497 | — | EC50 | = | 127.0 | nM | 6.90 |
| CHEMBL3218485 | — | EC50 | = | 153.0 | nM | 6.82 |
| CHEMBL3218498 | — | EC50 | = | 167.0 | nM | 6.78 |
| CHEMBL2165615 | NERIGLIATIN | EC50 | = | 188.0 | nM | 6.73 |
| CHEMBL2165616 | — | EC50 | = | 212.0 | nM | 6.67 |
| CHEMBL3218499 | — | EC50 | = | 254.0 | nM | 6.59 |
| CHEMBL3218489 | — | EC50 | = | 261.0 | nM | 6.58 |
| CHEMBL3218500 | — | EC50 | = | 331.0 | nM | 6.48 |
| CHEMBL1096435 | Ro-281675 | EC50 | = | 334.0 | nM | 6.48 |
| CHEMBL1783734 | PIRAGLIATIN | EC50 | = | 364.0 | nM | 6.44 |
| CHEMBL3218490 | — | EC50 | = | 393.0 | nM | 6.41 |
| CHEMBL3218496 | — | EC50 | = | 391.0 | nM | 6.41 |
| CHEMBL3218483 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3218495 | — | EC50 | = | 477.0 | nM | 6.32 |
| CHEMBL3218491 | — | EC50 | = | 705.0 | nM | 6.15 |
| CHEMBL3218480 | — | EC50 | = | 870.0 | nM | 6.06 |
| CHEMBL3218494 | — | EC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL3218481 | — | EC50 | = | 3061.0 | nM | 5.51 |
| CHEMBL3218479 | — | EC50 | = | 6610.0 | nM | 5.18 |
| CHEMBL3218501 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3218493 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL3218492 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL3218486 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL3218484 | — | EC50 | > | 20.0 | nM | - |