Assay Detail
Binding
CHEMBL1027304
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Inhibition of human liver glycogen phosphorylase a by coupled kinetic fluorescent intensity assay
21
Total Activities
21
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
Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.68 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL471266 | — | — | 1 | 8.52 |
| CHEMBL458655 | — | — | 1 | 8.52 |
| CHEMBL449986 | — | — | 1 | 8.40 |
| CHEMBL459792 | — | — | 1 | 8.40 |
| CHEMBL506011 | — | — | 1 | 8.40 |
| CHEMBL472292 | — | — | 1 | 8.15 |
| CHEMBL443938 | — | — | 1 | 8.15 |
| CHEMBL479920 | — | — | 1 | 8.10 |
| CHEMBL473486 | — | — | 1 | 8.00 |
| CHEMBL471469 | — | — | 1 | 8.00 |
| CHEMBL512725 | — | — | 1 | 7.89 |
| CHEMBL474098 | — | — | 1 | 7.89 |
| CHEMBL479728 | — | — | 1 | 7.82 |
| CHEMBL474297 | — | — | 1 | 7.72 |
| CHEMBL516918 | — | — | 1 | 7.55 |
| CHEMBL475508 | — | — | 1 | 7.31 |
| CHEMBL474298 | — | — | 1 | 7.06 |
| CHEMBL474705 | — | — | 1 | 6.84 |
| CHEMBL516038 | — | — | 1 | 6.30 |
| CHEMBL516369 | — | — | 1 | 6.27 |
| CHEMBL474706 | — | — | 1 | 5.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL471266 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL458655 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL449986 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL459792 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL506011 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL472292 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL443938 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL479920 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL473486 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL471469 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL512725 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL474098 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL479728 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL474297 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL516918 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL475508 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL474298 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL474705 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL516038 | — | IC50 | = | 506.0 | nM | 6.30 |
| CHEMBL516369 | — | IC50 | = | 542.0 | nM | 6.27 |
| CHEMBL474706 | — | IC50 | = | 1067.0 | nM | 5.97 |