Assay Detail
Functional
CHEMBL972349
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Agonist activity at human GLP1R expressed in CHO cells assessed as increase in cAMP level by cAMP-response element/luciferase activation assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 9.71 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL524907 | — | — | 1 | 11.00 |
| CHEMBL526685 | — | — | 1 | 10.85 |
| CHEMBL526730 | — | — | 1 | 10.72 |
| CHEMBL500447 | — | — | 1 | 10.62 |
| CHEMBL499370 | — | — | 1 | 10.57 |
| CHEMBL507190 | — | — | 1 | 10.11 |
| CHEMBL526684 | — | — | 1 | 9.85 |
| CHEMBL525956 | — | — | 1 | 9.85 |
| CHEMBL524538 | — | — | 1 | 9.35 |
| CHEMBL526893 | — | — | 1 | 9.33 |
| CHEMBL505224 | — | — | 1 | 9.13 |
| CHEMBL504234 | — | — | 1 | 8.74 |
| CHEMBL468769 | — | — | 1 | 8.05 |
| CHEMBL504759 | — | — | 1 | 7.82 |
| CHEMBL499133 | — | — | 1 | - |
| CHEMBL499930 | — | — | 1 | - |
| CHEMBL527077 | — | — | 1 | - |
| CHEMBL507645 | — | — | 1 | - |
| CHEMBL499208 | — | — | 1 | - |
| CHEMBL525934 | — | — | 1 | - |
| CHEMBL414357 | EXENATIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL524907 | — | EC50 | = | 0.01 | nM | 11.00 |
| CHEMBL526685 | — | EC50 | = | 0.014 | nM | 10.85 |
| CHEMBL526730 | — | EC50 | = | 0.019 | nM | 10.72 |
| CHEMBL500447 | — | EC50 | = | 0.024 | nM | 10.62 |
| CHEMBL499370 | — | EC50 | = | 0.027 | nM | 10.57 |
| CHEMBL507190 | — | EC50 | = | 0.077 | nM | 10.11 |
| CHEMBL526684 | — | EC50 | = | 0.14 | nM | 9.85 |
| CHEMBL525956 | — | EC50 | = | 0.14 | nM | 9.85 |
| CHEMBL524538 | — | EC50 | = | 0.45 | nM | 9.35 |
| CHEMBL526893 | — | EC50 | = | 0.47 | nM | 9.33 |
| CHEMBL505224 | — | EC50 | = | 0.74 | nM | 9.13 |
| CHEMBL504234 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL468769 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL504759 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL499133 | — | EC50 | = | 0.008 | nM | - |
| CHEMBL499930 | — | EC50 | = | 0.006 | nM | - |
| CHEMBL527077 | — | EC50 | = | 0.008 | nM | - |
| CHEMBL507645 | — | EC50 | = | 0.004 | nM | - |
| CHEMBL499208 | — | EC50 | = | 0.006 | nM | - |
| CHEMBL525934 | — | EC50 | = | 0.003 | nM | - |
| CHEMBL414357 | EXENATIDE | EC50 | = | 0.004 | nM | - |