Assay Detail
Functional
CHEMBL4737528
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Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins in presence of 2 % HSA by HTRF assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | OVCAR-5 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of Potent and Long-Acting Single-Chain Peptide Mimetics of Human Relaxin-2 for Cardiovascular Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 7.46 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4799907 | — | — | 1 | 8.05 |
| CHEMBL4795810 | — | — | 1 | 7.74 |
| CHEMBL4745611 | — | — | 1 | 7.70 |
| CHEMBL4786789 | — | — | 1 | 7.61 |
| CHEMBL4797641 | — | — | 1 | 7.51 |
| CHEMBL4764326 | — | — | 1 | 7.06 |
| CHEMBL4793799 | — | — | 1 | 6.57 |
| CHEMBL4797258 | — | — | 1 | - |
| CHEMBL4752287 | — | — | 1 | - |
| CHEMBL4796713 | — | — | 1 | - |
| CHEMBL4746080 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4799907 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4795810 | — | EC50 | = | 18.4 | nM | 7.74 |
| CHEMBL4745611 | — | EC50 | = | 19.8 | nM | 7.70 |
| CHEMBL4786789 | — | EC50 | = | 24.5 | nM | 7.61 |
| CHEMBL4797641 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4764326 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4793799 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4797258 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL4752287 | — | EC50 | - | — | - | |
| CHEMBL4796713 | — | EC50 | > | 2000.0 | nM | - |
| CHEMBL4746080 | — | EC50 | > | 2000.0 | nM | - |