Assay Detail
Functional
CHEMBL1008757
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Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of novel G-protein-coupled receptor 54 agonists with resistance to degradation by matrix metalloproteinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 9.02 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376756 | KISSPEPTIN-10 | 3.0 | 1 | 9.62 |
| CHEMBL472833 | — | — | 1 | 9.52 |
| CHEMBL453956 | — | — | 1 | 9.44 |
| CHEMBL388586 | — | — | 1 | 9.35 |
| CHEMBL444664 | — | — | 1 | 8.60 |
| CHEMBL503052 | — | — | 1 | 8.37 |
| CHEMBL501043 | — | — | 1 | 8.27 |
| CHEMBL507796 | — | — | 1 | - |
| CHEMBL450923 | — | — | 1 | - |
| CHEMBL478053 | — | — | 1 | - |
| CHEMBL444522 | — | — | 1 | - |
| CHEMBL448207 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376756 | KISSPEPTIN-10 | EC50 | = | 0.24 | nM | 9.62 |
| CHEMBL472833 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL453956 | — | EC50 | = | 0.36 | nM | 9.44 |
| CHEMBL388586 | — | EC50 | = | 0.45 | nM | 9.35 |
| CHEMBL444664 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL503052 | — | EC50 | = | 4.3 | nM | 8.37 |
| CHEMBL501043 | — | EC50 | = | 5.4 | nM | 8.27 |
| CHEMBL507796 | — | EC50 | - | — | - | |
| CHEMBL450923 | — | EC50 | - | — | - | |
| CHEMBL478053 | — | EC50 | - | — | - | |
| CHEMBL444522 | — | EC50 | - | — | - | |
| CHEMBL448207 | — | EC50 | - | — | - |