Assay Detail
Functional
CHEMBL996771
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Inhibition of glucagon-stimulated glucose production in human primary hepatocytes preincubated for 10 mins before glucagon addition by NADH-linked hexokinase assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Hepatocyte |
| Confidence | 1 — Organism |
| 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 | 5.48 | 6.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL455323 | — | — | 1 | 6.16 |
| CHEMBL471580 | — | — | 1 | 5.57 |
| CHEMBL519776 | — | — | 1 | 5.55 |
| CHEMBL501628 | — | — | 1 | 5.44 |
| CHEMBL492813 | — | — | 1 | 5.40 |
| CHEMBL470729 | — | — | 1 | 5.17 |
| CHEMBL446821 | — | — | 1 | 5.07 |
| CHEMBL492605 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL455323 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL471580 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL519776 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL501628 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL492813 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL470729 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL446821 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL492605 | — | IC50 | < | 20000.0 | nM | - |