Assay Detail
Functional
CHEMBL3386599
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Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay
27
Total Activities
27
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
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 7.80 | 10.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3184840 | — | — | 1 | 10.91 |
| CHEMBL3338689 | — | — | 1 | 8.57 |
| CHEMBL3338686 | — | — | 1 | 7.67 |
| CHEMBL3338677 | — | — | 1 | 7.47 |
| CHEMBL3338681 | — | — | 1 | 7.38 |
| CHEMBL3338687 | — | — | 1 | 7.02 |
| CHEMBL3338680 | — | — | 1 | 6.70 |
| CHEMBL3338699 | — | — | 1 | 6.65 |
| CHEMBL3338685 | — | — | 1 | - |
| CHEMBL3338684 | — | — | 1 | - |
| CHEMBL3338683 | — | — | 1 | - |
| CHEMBL3338682 | — | — | 1 | - |
| CHEMBL3338690 | — | — | 1 | - |
| CHEMBL3338693 | — | — | 1 | - |
| CHEMBL3338679 | — | — | 1 | - |
| CHEMBL3338678 | — | — | 1 | - |
| CHEMBL3338691 | — | — | 1 | - |
| CHEMBL3338688 | — | — | 1 | - |
| CHEMBL3338700 | — | — | 1 | - |
| CHEMBL3338698 | — | — | 1 | - |
| CHEMBL3337468 | — | — | 1 | - |
| CHEMBL3338697 | — | — | 1 | - |
| CHEMBL3338696 | — | — | 1 | - |
| CHEMBL3338695 | — | — | 1 | - |
| CHEMBL3338694 | — | — | 1 | - |
| CHEMBL3338692 | — | — | 1 | - |
| CHEMBL3338701 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3184840 | — | EC50 | = | 0.0122 | nM | 10.91 |
| CHEMBL3338689 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3338686 | — | EC50 | = | 21.5 | nM | 7.67 |
| CHEMBL3338677 | — | EC50 | = | 33.7 | nM | 7.47 |
| CHEMBL3338681 | — | EC50 | = | 41.3 | nM | 7.38 |
| CHEMBL3338687 | — | EC50 | = | 95.7 | nM | 7.02 |
| CHEMBL3338680 | — | EC50 | = | 198.6 | nM | 6.70 |
| CHEMBL3338699 | — | EC50 | = | 225.5 | nM | 6.65 |
| CHEMBL3338685 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338684 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338683 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338682 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338690 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338693 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338679 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338678 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338691 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338688 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338700 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338698 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3337468 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338697 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338696 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338695 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338694 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338692 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3338701 | — | EC50 | > | 30000.0 | nM | - |