Assay Detail
Binding
CHEMBL3873254
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Competitive inhibition of His6-tagged human liver glycogen phosphorylase-a expressed in Escherichia coli BL21 Gold (DE3) assessed as release of inorganic phosphate using varying levels of glucose-1-phosphate and constant concentration of AMP and glycogen measured after 1 min by Dixon plot method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Liver |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthetic, enzyme kinetic, and protein crystallographic studies of C-β-d-glucopyranosyl pyrroles and imidazoles reveal and explain low nanomolar inhibition of human liver glycogen phosphorylase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.20 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3770455 | — | — | 1 | 7.58 |
| CHEMBL3770514 | — | — | 1 | 6.81 |
| CHEMBL3936229 | — | — | 1 | - |
| CHEMBL3954904 | — | — | 1 | - |
| CHEMBL3921272 | — | — | 1 | - |
| CHEMBL3946226 | — | — | 1 | - |
| CHEMBL3968658 | — | — | 1 | - |
| CHEMBL3937338 | — | — | 1 | - |
| CHEMBL423707 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3770455 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL3770514 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL3936229 | — | Ki | - | — | - | |
| CHEMBL3954904 | — | Ki | - | — | - | |
| CHEMBL3921272 | — | Ki | - | — | - | |
| CHEMBL3946226 | — | Ki | - | — | - | |
| CHEMBL3968658 | — | Ki | - | — | - | |
| CHEMBL3937338 | — | Ki | - | — | - | |
| CHEMBL423707 | — | Ki | = | 4280000.0 | nM | - |