Assay Detail
Binding
CHEMBL684120
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Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
33
Total Activities
33
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 | 33 | 6.27 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL158548 | — | — | 1 | 6.96 |
| CHEMBL160287 | — | — | 1 | 6.89 |
| CHEMBL156458 | — | — | 1 | 6.85 |
| CHEMBL155686 | — | — | 1 | 6.77 |
| CHEMBL351772 | — | — | 1 | 6.77 |
| CHEMBL158676 | — | — | 1 | 6.75 |
| CHEMBL347663 | — | — | 1 | 6.70 |
| CHEMBL158535 | — | — | 1 | 6.58 |
| CHEMBL348555 | — | — | 1 | 6.57 |
| CHEMBL347462 | — | — | 1 | 6.54 |
| CHEMBL157529 | — | — | 1 | 6.46 |
| CHEMBL160550 | — | — | 1 | 6.42 |
| CHEMBL345863 | — | — | 1 | 6.40 |
| CHEMBL158477 | — | — | 1 | 6.35 |
| CHEMBL348401 | — | — | 1 | 6.31 |
| CHEMBL345834 | — | — | 1 | 6.30 |
| CHEMBL160380 | — | — | 1 | 6.30 |
| CHEMBL346698 | — | — | 1 | 6.30 |
| CHEMBL328126 | — | — | 1 | 6.10 |
| CHEMBL160490 | — | — | 1 | 6.09 |
| CHEMBL160561 | — | — | 1 | 6.04 |
| CHEMBL160638 | — | — | 1 | 6.02 |
| CHEMBL160281 | — | — | 1 | 6.00 |
| CHEMBL351104 | — | — | 1 | 5.89 |
| CHEMBL155694 | — | — | 1 | 5.80 |
| CHEMBL350255 | — | — | 1 | 5.77 |
| CHEMBL160289 | — | — | 1 | 5.66 |
| CHEMBL436022 | — | — | 1 | 5.64 |
| CHEMBL159198 | — | — | 1 | 5.64 |
| CHEMBL158989 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL158548 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL160287 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL156458 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL155686 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL351772 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL158676 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL347663 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL158535 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL348555 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL347462 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL157529 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL160550 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL345863 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL158477 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL348401 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL160380 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL346698 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL345834 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL328126 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL160490 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL160561 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL160638 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL160281 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL351104 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL155694 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL350255 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL160289 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL436022 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL159198 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL158989 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL160372 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL160735 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL160314 | — | IC50 | > | 3000.0 | nM | - |