Assay Detail
Binding
CHEMBL1027305
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Inhibition of human glycogen phosphorylase a in HepG2 cells assessed as inhibition of forskolin-stimulated glycogenolysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| 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 | 6.55 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL471266 | — | — | 1 | 7.47 |
| CHEMBL472292 | — | — | 1 | 7.06 |
| CHEMBL479728 | — | — | 1 | 6.98 |
| CHEMBL479920 | — | — | 1 | 6.96 |
| CHEMBL471469 | — | — | 1 | 6.90 |
| CHEMBL459792 | — | — | 1 | 6.88 |
| CHEMBL506011 | — | — | 1 | 6.87 |
| CHEMBL458655 | — | — | 1 | 6.84 |
| CHEMBL473486 | — | — | 1 | 6.83 |
| CHEMBL449986 | — | — | 1 | 6.81 |
| CHEMBL512725 | — | — | 1 | 6.77 |
| CHEMBL443938 | — | — | 1 | 6.74 |
| CHEMBL474297 | — | — | 1 | 6.64 |
| CHEMBL516918 | — | — | 1 | 6.45 |
| CHEMBL474098 | — | — | 1 | 6.42 |
| CHEMBL474298 | — | — | 1 | 6.29 |
| CHEMBL475508 | — | — | 1 | 6.14 |
| CHEMBL474705 | — | — | 1 | 5.99 |
| CHEMBL516369 | — | — | 1 | 5.78 |
| CHEMBL516038 | — | — | 1 | 5.74 |
| CHEMBL474706 | — | — | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL471266 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL472292 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL479728 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL479920 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL471469 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL459792 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL506011 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL458655 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL473486 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL449986 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL512725 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL443938 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL474297 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL516918 | — | IC50 | = | 353.0 | nM | 6.45 |
| CHEMBL474098 | — | IC50 | = | 384.0 | nM | 6.42 |
| CHEMBL474298 | — | IC50 | = | 513.0 | nM | 6.29 |
| CHEMBL475508 | — | IC50 | = | 716.0 | nM | 6.14 |
| CHEMBL474705 | — | IC50 | = | 1026.0 | nM | 5.99 |
| CHEMBL516369 | — | IC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL516038 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL474706 | — | IC50 | = | 8260.0 | nM | 5.08 |