Assay Detail
Binding
CHEMBL5610152
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Displacement of [125I]MCH from rat MCHR1 extracted from HEK293 cell membrane assessed as inhibition constant by competitive binding assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Melanin-concentrating hormone receptor 1 (CHEMBL1075228) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Exploring monocyclic core: Discovery of pyrrol-2-one derivatives as a new series of potent MCHR1 antagonists with in vivo efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 9.03 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214957 | — | — | 1 | 9.47 |
| CHEMBL5613278 | — | — | 1 | 9.28 |
| CHEMBL5611933 | — | — | 1 | 9.26 |
| CHEMBL5612007 | — | — | 1 | 9.21 |
| CHEMBL5613243 | — | — | 1 | 9.20 |
| CHEMBL5612188 | — | — | 1 | 9.19 |
| CHEMBL5612296 | — | — | 1 | 9.18 |
| CHEMBL5613768 | — | — | 1 | 9.17 |
| CHEMBL5613131 | — | — | 1 | 9.16 |
| CHEMBL5613208 | — | — | 1 | 9.14 |
| CHEMBL5612395 | — | — | 1 | 9.14 |
| CHEMBL5614297 | — | — | 1 | 9.12 |
| CHEMBL5612906 | — | — | 1 | 9.11 |
| CHEMBL5612929 | — | — | 1 | 9.10 |
| CHEMBL5614124 | — | — | 1 | 9.09 |
| CHEMBL5613587 | — | — | 1 | 9.07 |
| CHEMBL5614058 | — | — | 1 | 8.99 |
| CHEMBL5614007 | — | — | 1 | 8.97 |
| CHEMBL5613259 | — | — | 1 | 8.96 |
| CHEMBL5613960 | — | — | 1 | 8.93 |
| CHEMBL5612410 | — | — | 1 | 8.89 |
| CHEMBL5613133 | — | — | 1 | 8.66 |
| CHEMBL5611987 | — | — | 1 | 8.24 |
| CHEMBL5613713 | — | — | 1 | 8.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214957 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL5613278 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL5611933 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL5612007 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL5613243 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL5612188 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL5612296 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL5613768 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL5613131 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL5613208 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL5612395 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL5614297 | — | Ki | = | 0.76 | nM | 9.12 |
| CHEMBL5612906 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL5612929 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL5614124 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL5613587 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL5614058 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL5614007 | — | Ki | = | 1.08 | nM | 8.97 |
| CHEMBL5613259 | — | Ki | = | 1.11 | nM | 8.96 |
| CHEMBL5613960 | — | Ki | = | 1.18 | nM | 8.93 |
| CHEMBL5612410 | — | Ki | = | 1.29 | nM | 8.89 |
| CHEMBL5613133 | — | Ki | = | 2.17 | nM | 8.66 |
| CHEMBL5611987 | — | Ki | = | 5.72 | nM | 8.24 |
| CHEMBL5613713 | — | Ki | = | 6.15 | nM | 8.21 |