Assay Detail
Binding
CHEMBL1008755
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| IC50 | 12 | 8.23 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376756 | KISSPEPTIN-10 | 3.0 | 1 | 10.15 |
| CHEMBL472833 | — | — | 1 | 9.92 |
| CHEMBL453956 | — | — | 1 | 9.62 |
| CHEMBL388586 | — | — | 1 | 9.15 |
| CHEMBL444664 | — | — | 1 | 8.92 |
| CHEMBL501043 | — | — | 1 | 8.34 |
| CHEMBL503052 | — | — | 1 | 8.24 |
| CHEMBL450923 | — | — | 1 | 7.50 |
| CHEMBL448207 | — | — | 1 | 7.50 |
| CHEMBL507796 | — | — | 1 | 6.62 |
| CHEMBL478053 | — | — | 1 | 6.42 |
| CHEMBL444522 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376756 | KISSPEPTIN-10 | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL472833 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL453956 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL388586 | — | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL444664 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL501043 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL503052 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL450923 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL448207 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL507796 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL478053 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL444522 | — | IC50 | = | 460.0 | nM | 6.34 |