Assay Detail
Functional
CHEMBL5522552
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Agonist activity at human RXFP1 expressed in CHO-K1 cells assessed as dynamic mass redistribution (DMR) measured after 60 mins by G-protein coupling DMR assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 | 3 | 8.73 | 10.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5194101 | — | — | 1 | 10.60 |
| CHEMBL5559571 | — | — | 1 | 9.50 |
| CHEMBL3716980 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5194101 | — | EC50 | = | 0.02512 | nM | 10.60 |
| CHEMBL5559571 | — | EC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL3716980 | — | EC50 | = | 794.33 | nM | 6.10 |