Assay Detail
Binding
CHEMBL4193353
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Activation of recombinant human liver glucokinase 2 assessed as assessed as reduction in Km for glucose in presence of 5 mM glucose by G6PDH coupled assay
4
Total Activities
4
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
Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 6.90 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4205489 | — | — | 1 | 7.52 |
| CHEMBL4203455 | — | — | 1 | 7.30 |
| CHEMBL4214183 | — | — | 1 | 6.82 |
| CHEMBL2165615 | NERIGLIATIN | 2.0 | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4205489 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4203455 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4214183 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2165615 | NERIGLIATIN | EC50 | = | 1090.0 | nM | 5.96 |