Assay Detail
Binding
CHEMBL995928
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Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BHK |
| 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 | 30 | 6.98 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464663 | — | — | 1 | 7.47 |
| CHEMBL506800 | — | — | 1 | 7.44 |
| CHEMBL444126 | — | — | 1 | 7.32 |
| CHEMBL455323 | — | — | 1 | 7.30 |
| CHEMBL471580 | — | — | 1 | 7.12 |
| CHEMBL451288 | — | — | 1 | 7.11 |
| CHEMBL442651 | — | — | 1 | 7.11 |
| CHEMBL492813 | — | — | 1 | 7.10 |
| CHEMBL448584 | — | — | 1 | 7.09 |
| CHEMBL519776 | — | — | 1 | 7.09 |
| CHEMBL446821 | — | — | 1 | 7.07 |
| CHEMBL492605 | — | — | 1 | 7.07 |
| CHEMBL443971 | — | — | 1 | 7.07 |
| CHEMBL470729 | — | — | 1 | 7.04 |
| CHEMBL501628 | — | — | 1 | 7.04 |
| CHEMBL448561 | — | — | 1 | 7.03 |
| CHEMBL491920 | — | — | 1 | 7.02 |
| CHEMBL493020 | — | — | 1 | 7.01 |
| CHEMBL491352 | — | — | 1 | 7.00 |
| CHEMBL450411 | — | — | 1 | 6.93 |
| CHEMBL523847 | — | — | 1 | 6.92 |
| CHEMBL501392 | — | — | 1 | 6.92 |
| CHEMBL521650 | — | — | 1 | 6.89 |
| CHEMBL502694 | — | — | 1 | 6.88 |
| CHEMBL493019 | — | — | 1 | 6.82 |
| CHEMBL504260 | — | — | 1 | 6.65 |
| CHEMBL505685 | — | — | 1 | 6.58 |
| CHEMBL493233 | — | — | 1 | 6.50 |
| CHEMBL472586 | — | — | 1 | 6.38 |
| CHEMBL494248 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464663 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL506800 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL444126 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL455323 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL471580 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL451288 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL442651 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL492813 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL448584 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL519776 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL446821 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL492605 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL443971 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL470729 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL501628 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL448561 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL491920 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL493020 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL491352 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL450411 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL523847 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL501392 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL521650 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL502694 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL493019 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL504260 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL505685 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL493233 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL472586 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL494248 | — | IC50 | = | 531.0 | nM | 6.28 |