Assay Detail
Binding
CHEMBL969605
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Displacement of [125I]MCH from human MCHR1 expressed in CHO cells
18
Total Activities
17
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 |
Target
Melanin-concentrating hormone receptor 1 (CHEMBL344) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.43 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL468099 | — | — | 1 | 10.05 |
| CHEMBL511542 | — | — | 1 | 9.82 |
| CHEMBL466425 | — | — | 2 | 9.34 |
| CHEMBL494016 | — | — | 1 | 9.00 |
| CHEMBL493962 | — | — | 1 | 8.77 |
| CHEMBL493967 | — | — | 1 | 8.72 |
| CHEMBL494009 | — | — | 1 | 8.68 |
| CHEMBL522037 | — | — | 1 | 8.68 |
| CHEMBL511747 | — | — | 1 | 8.57 |
| CHEMBL494155 | — | — | 1 | 8.54 |
| CHEMBL523882 | — | — | 1 | 8.02 |
| CHEMBL494156 | — | — | 1 | 8.00 |
| CHEMBL523697 | — | — | 1 | 7.72 |
| CHEMBL468299 | — | — | 1 | 7.38 |
| CHEMBL468509 | — | — | 1 | 7.38 |
| CHEMBL468298 | — | — | 1 | 7.27 |
| CHEMBL467668 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL468099 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL511542 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL466425 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL494016 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL466425 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL493962 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL493967 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL494009 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL522037 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL511747 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL494155 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL523882 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL494156 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL523697 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL468299 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL468509 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL468298 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL467668 | — | IC50 | = | 125.0 | nM | 6.90 |