Assay Detail
Binding
CHEMBL990114
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Activation of GST fused human liver glucokinase assessed as generation of NADPH by G6PDH coupled assay
13
Total Activities
13
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
SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: discovery of PSN-GK1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 5.93 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL480725 | — | — | 1 | 7.16 |
| CHEMBL499520 | — | — | 1 | 6.89 |
| CHEMBL519273 | — | — | 1 | 6.85 |
| CHEMBL516458 | — | — | 1 | 6.25 |
| CHEMBL479947 | — | — | 1 | 6.24 |
| CHEMBL517534 | — | — | 1 | 6.24 |
| CHEMBL479948 | — | — | 1 | 5.84 |
| CHEMBL481166 | — | — | 1 | 5.64 |
| CHEMBL481167 | — | — | 1 | 5.46 |
| CHEMBL519934 | — | — | 1 | 5.05 |
| CHEMBL479974 | — | — | 1 | 4.97 |
| CHEMBL480180 | — | — | 1 | 4.58 |
| CHEMBL479753 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL480725 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL499520 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL519273 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL516458 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL479947 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL517534 | — | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL479948 | — | EC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL481166 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL481167 | — | EC50 | = | 3470.0 | nM | 5.46 |
| CHEMBL519934 | — | EC50 | = | 8930.0 | nM | 5.05 |
| CHEMBL479974 | — | EC50 | = | 10770.0 | nM | 4.97 |
| CHEMBL480180 | — | EC50 | = | 26010.0 | nM | 4.58 |
| CHEMBL479753 | — | EC50 | > | 10000.0 | nM | - |