Assay Detail
Binding
CHEMBL995932
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Binding affinity to glucagon receptor in rat liver membrane by membrane filter assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Human glucagon receptor antagonists with thiazole cores. A novel series with superior pharmacokinetic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.63 | 5.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL471580 | — | — | 1 | 5.85 |
| CHEMBL492813 | — | — | 1 | 5.80 |
| CHEMBL519776 | — | — | 1 | 5.77 |
| CHEMBL455323 | — | — | 1 | 5.75 |
| CHEMBL501628 | — | — | 1 | 5.70 |
| CHEMBL470729 | — | — | 1 | 5.57 |
| CHEMBL446821 | — | — | 1 | 5.36 |
| CHEMBL492605 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL471580 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL492813 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL519776 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL455323 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL501628 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL470729 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL446821 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL492605 | — | IC50 | = | 5400.0 | nM | 5.27 |