Assay Detail
Functional
CHEMBL5522565
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human RXFP1 expressed in HEK293 cells coexpressing GRK2 assessed as beta-arrestin internalization by BRET assay relative to control
3
Total Activities
3
Compounds Tested
2
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
Discovery of Clinical Candidate AZD5462, a Selective Oral Allosteric RXFP1 Agonist for Treatment of Heart Failure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 8.00 | 8.82 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5194101 | — | — | 1 | 8.82 |
| CHEMBL5559571 | — | — | 1 | 7.18 |
| CHEMBL3716980 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5194101 | — | EC50 | = | 1.514 | nM | 8.82 |
| CHEMBL5559571 | — | EC50 | = | 66.07 | nM | 7.18 |
| CHEMBL3716980 | — | Activity | - | — | - |