Assay Detail
Functional
CHEMBL4808886
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of Truncated Glucagon Peptides to Achieve Selective, High Potency, Full Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.21 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4857523 | — | — | 1 | 9.37 |
| CHEMBL4867132 | — | — | 1 | 8.16 |
| CHEMBL4876736 | — | — | 1 | 7.92 |
| CHEMBL4853767 | — | — | 1 | 7.88 |
| CHEMBL4849980 | — | — | 1 | 7.40 |
| CHEMBL4875003 | — | — | 1 | 7.36 |
| CHEMBL4870505 | — | — | 1 | 7.32 |
| CHEMBL4876838 | — | — | 1 | 7.15 |
| CHEMBL4865509 | — | — | 1 | 7.13 |
| CHEMBL4861024 | — | — | 1 | 7.10 |
| CHEMBL4860642 | — | — | 1 | 7.09 |
| CHEMBL4876499 | — | — | 1 | 6.89 |
| CHEMBL4869368 | — | — | 1 | 6.72 |
| CHEMBL4870133 | — | — | 1 | 6.57 |
| CHEMBL4875380 | — | — | 1 | 6.56 |
| CHEMBL4850520 | — | — | 1 | 6.46 |
| CHEMBL4873721 | — | — | 1 | 6.40 |
| CHEMBL4876913 | — | — | 1 | 6.33 |
| CHEMBL437471 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4857523 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL4867132 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4876736 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL4853767 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL4849980 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4875003 | — | IC50 | = | 44.1 | nM | 7.36 |
| CHEMBL4870505 | — | IC50 | = | 47.7 | nM | 7.32 |
| CHEMBL4876838 | — | IC50 | = | 71.4 | nM | 7.15 |
| CHEMBL4865509 | — | IC50 | = | 73.2 | nM | 7.13 |
| CHEMBL4861024 | — | IC50 | = | 79.1 | nM | 7.10 |
| CHEMBL4860642 | — | IC50 | = | 81.8 | nM | 7.09 |
| CHEMBL4876499 | — | IC50 | = | 129.8 | nM | 6.89 |
| CHEMBL4869368 | — | IC50 | = | 191.8 | nM | 6.72 |
| CHEMBL4870133 | — | IC50 | = | 267.4 | nM | 6.57 |
| CHEMBL4875380 | — | IC50 | = | 274.9 | nM | 6.56 |
| CHEMBL4850520 | — | IC50 | = | 345.7 | nM | 6.46 |
| CHEMBL4873721 | — | IC50 | = | 397.9 | nM | 6.40 |
| CHEMBL4876913 | — | IC50 | = | 472.2 | nM | 6.33 |
| CHEMBL437471 | — | IC50 | - | — | - |