Assay Detail
Binding
CHEMBL893404
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Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Melanin-concentrating hormone receptor 1 (CHEMBL1075228) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 8.21 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL185271 | SNAP-7941 | — | 1 | 9.60 |
| CHEMBL388440 | — | — | 1 | 9.22 |
| CHEMBL429464 | — | — | 1 | 9.21 |
| CHEMBL243338 | — | — | 1 | 8.85 |
| CHEMBL243355 | — | — | 1 | 8.74 |
| CHEMBL396234 | — | — | 1 | 8.72 |
| CHEMBL390679 | — | — | 1 | 8.72 |
| CHEMBL243138 | — | — | 1 | 8.72 |
| CHEMBL243128 | — | — | 1 | 8.62 |
| CHEMBL243578 | — | — | 1 | 8.54 |
| CHEMBL242689 | — | — | 1 | 8.52 |
| CHEMBL244370 | — | — | 1 | 8.42 |
| CHEMBL242902 | — | — | 1 | 8.12 |
| CHEMBL243507 | — | — | 1 | 8.07 |
| CHEMBL394793 | — | — | 1 | 8.00 |
| CHEMBL242901 | — | — | 1 | 7.85 |
| CHEMBL244369 | — | — | 1 | 7.55 |
| CHEMBL243129 | — | — | 1 | 7.54 |
| CHEMBL242053 | — | — | 1 | 7.47 |
| CHEMBL242054 | — | — | 1 | 7.43 |
| CHEMBL243354 | — | — | 1 | 7.33 |
| CHEMBL243139 | — | — | 1 | 7.30 |
| CHEMBL388234 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL185271 | SNAP-7941 | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL388440 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL429464 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL243338 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL243355 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL396234 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL390679 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL243138 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL243128 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL243578 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL242689 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL244370 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL242902 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL243507 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL394793 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL242901 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL244369 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL243129 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL242053 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL242054 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL243354 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL243139 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL388234 | — | Ki | = | 500.0 | nM | 6.30 |