Assay Detail
Binding
CHEMBL2174353
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
10
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Growth hormone secretagogue receptor type 1 (CHEMBL4616) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
An aromatic region to induce a switch between agonism and inverse agonism at the ghrelin receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.62 | 9.15 |
| IC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL500468 | GHRELIN | 3.0 | 1 | 9.15 |
| CHEMBL2170781 | — | — | 1 | 8.31 |
| CHEMBL2170701 | — | — | 1 | 7.66 |
| CHEMBL2170693 | — | — | 1 | 7.50 |
| CHEMBL2170694 | — | — | 1 | 7.46 |
| CHEMBL2170779 | — | — | 1 | 6.63 |
| CHEMBL2170780 | — | — | 1 | 6.61 |
| CHEMBL2170692 | — | — | 1 | - |
| CHEMBL2170691 | — | — | 1 | - |
| CHEMBL2170690 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL500468 | GHRELIN | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2170781 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL2170701 | — | Ki | = | 22.1 | nM | 7.66 |
| CHEMBL2170693 | — | Ki | = | 31.3 | nM | 7.50 |
| CHEMBL2170694 | — | Ki | = | 34.9 | nM | 7.46 |
| CHEMBL2170779 | — | Ki | = | 234.2 | nM | 6.63 |
| CHEMBL2170780 | — | Ki | = | 247.2 | nM | 6.61 |
| CHEMBL2170692 | — | IC50 | >= | 1000.0 | nM | - |
| CHEMBL2170691 | — | IC50 | >= | 1000.0 | nM | - |
| CHEMBL2170690 | — | IC50 | >= | 1000.0 | nM | - |