Assay Detail
Functional
CHEMBL5582336
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Agonist activity at human GLP-1R expressed in HEK293 cells assessed as accumulation of cAMP preincubated for 30 mins followed by d2-labeled cAMP addition and anti-cAMP cryptate addition measured after 60 mins by HTRF assay
24
Total Activities
24
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
Design and Evaluation of 3-Phenyloxetane Derivative Agonists of the Glucagon-Like Peptide-1 Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 8.80 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5590455 | — | — | 1 | 10.52 |
| CHEMBL5594743 | — | — | 1 | 10.52 |
| CHEMBL5591135 | — | — | 1 | 10.15 |
| CHEMBL5591054 | — | — | 1 | 10.10 |
| CHEMBL5595973 | — | — | 1 | 10.10 |
| CHEMBL4518483 | DANUGLIPRON | 2.0 | 1 | 9.92 |
| CHEMBL5592770 | — | — | 1 | 9.27 |
| CHEMBL5592386 | — | — | 1 | 9.15 |
| CHEMBL5590471 | — | — | 1 | 9.12 |
| CHEMBL5594276 | — | — | 1 | 9.07 |
| CHEMBL5593096 | — | — | 1 | 9.02 |
| CHEMBL5592184 | — | — | 1 | 8.85 |
| CHEMBL5594583 | — | — | 1 | 8.55 |
| CHEMBL5595501 | — | — | 1 | 8.51 |
| CHEMBL5594044 | — | — | 1 | 7.62 |
| CHEMBL5591875 | — | — | 1 | 7.48 |
| CHEMBL5594618 | — | — | 1 | 7.41 |
| CHEMBL5590511 | — | — | 1 | 7.12 |
| CHEMBL5591847 | — | — | 1 | 6.84 |
| CHEMBL5594876 | — | — | 1 | 6.75 |
| CHEMBL5592842 | — | — | 1 | - |
| CHEMBL5593681 | — | — | 1 | - |
| CHEMBL5593962 | — | — | 1 | - |
| CHEMBL5591858 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5590455 | — | EC50 | = | 0.03 | nM | 10.52 |
| CHEMBL5594743 | — | EC50 | = | 0.03 | nM | 10.52 |
| CHEMBL5591135 | — | EC50 | = | 0.07 | nM | 10.15 |
| CHEMBL5591054 | — | EC50 | = | 0.08 | nM | 10.10 |
| CHEMBL5595973 | — | EC50 | = | 0.08 | nM | 10.10 |
| CHEMBL4518483 | DANUGLIPRON | EC50 | = | 0.12 | nM | 9.92 |
| CHEMBL5592770 | — | EC50 | = | 0.54 | nM | 9.27 |
| CHEMBL5592386 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5590471 | — | EC50 | = | 0.75 | nM | 9.12 |
| CHEMBL5594276 | — | EC50 | = | 0.85 | nM | 9.07 |
| CHEMBL5593096 | — | EC50 | = | 0.95 | nM | 9.02 |
| CHEMBL5592184 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5594583 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5595501 | — | EC50 | = | 3.08 | nM | 8.51 |
| CHEMBL5594044 | — | EC50 | = | 23.69 | nM | 7.62 |
| CHEMBL5591875 | — | EC50 | = | 33.17 | nM | 7.48 |
| CHEMBL5594618 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5590511 | — | EC50 | = | 75.88 | nM | 7.12 |
| CHEMBL5591847 | — | EC50 | = | 145.45 | nM | 6.84 |
| CHEMBL5594876 | — | EC50 | = | 179.2 | nM | 6.75 |
| CHEMBL5592842 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5593681 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5593962 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5591858 | — | EC50 | > | 1000.0 | nM | - |