Assay Detail
Binding
CHEMBL680807
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Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Potent, orally absorbed glucagon receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.63 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL156458 | — | — | 1 | 7.52 |
| CHEMBL351772 | — | — | 1 | 7.43 |
| CHEMBL160287 | — | — | 1 | 7.31 |
| CHEMBL155686 | — | — | 1 | 7.30 |
| CHEMBL160735 | — | — | 1 | 7.22 |
| CHEMBL158548 | — | — | 1 | 7.22 |
| CHEMBL158676 | — | — | 1 | 7.10 |
| CHEMBL347663 | — | — | 1 | 6.82 |
| CHEMBL328126 | — | — | 1 | 6.70 |
| CHEMBL160490 | — | — | 1 | 6.66 |
| CHEMBL158989 | — | — | 1 | 6.64 |
| CHEMBL155694 | — | — | 1 | 6.62 |
| CHEMBL158535 | — | — | 1 | 6.57 |
| CHEMBL346698 | — | — | 1 | 6.47 |
| CHEMBL345834 | — | — | 1 | 6.47 |
| CHEMBL160638 | — | — | 1 | 6.47 |
| CHEMBL160380 | — | — | 1 | 6.40 |
| CHEMBL157529 | — | — | 1 | 6.37 |
| CHEMBL348555 | — | — | 1 | 6.36 |
| CHEMBL160281 | — | — | 1 | 6.34 |
| CHEMBL345863 | — | — | 1 | 6.30 |
| CHEMBL347462 | — | — | 1 | 6.17 |
| CHEMBL160561 | — | — | 1 | 6.16 |
| CHEMBL160372 | — | — | 1 | 6.16 |
| CHEMBL351104 | — | — | 1 | 6.10 |
| CHEMBL158671 | — | — | 1 | 5.57 |
| CHEMBL348401 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL156458 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL351772 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL160287 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL155686 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL160735 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL158548 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL158676 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL347663 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL328126 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL160490 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL158989 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL155694 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL158535 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL346698 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL345834 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL160638 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL160380 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL157529 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL348555 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL160281 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL345863 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL347462 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL160561 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL160372 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL351104 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL158671 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL348401 | — | IC50 | > | 1000.0 | nM | - |