Assay Detail
Binding
CHEMBL863646
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Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
25
Total Activities
24
Compounds Tested
2
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
Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.39 | 8.52 |
| Ki | 1 | 8.70 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216192 | — | — | 2 | 8.70 |
| CHEMBL386247 | — | — | 1 | 8.52 |
| CHEMBL215418 | — | — | 1 | 8.30 |
| CHEMBL214322 | — | — | 1 | 8.22 |
| CHEMBL216010 | — | — | 1 | 8.15 |
| CHEMBL214280 | — | — | 1 | 7.85 |
| CHEMBL215819 | — | — | 1 | 7.55 |
| CHEMBL386117 | — | — | 1 | 7.48 |
| CHEMBL385831 | — | — | 1 | 7.40 |
| CHEMBL215958 | — | — | 1 | 6.77 |
| CHEMBL424720 | — | — | 1 | 6.60 |
| CHEMBL373886 | — | — | 1 | 6.58 |
| CHEMBL214442 | — | — | 1 | 6.50 |
| CHEMBL214535 | — | — | 1 | 6.27 |
| CHEMBL373887 | — | — | 1 | 6.21 |
| CHEMBL215279 | — | — | 1 | - |
| CHEMBL216561 | — | — | 1 | - |
| CHEMBL265132 | — | — | 1 | - |
| CHEMBL214177 | — | — | 1 | - |
| CHEMBL215841 | — | — | 1 | - |
| CHEMBL384247 | — | — | 1 | - |
| CHEMBL384626 | — | — | 1 | - |
| CHEMBL386968 | — | — | 1 | - |
| CHEMBL385215 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216192 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL216192 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL386247 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL215418 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL214322 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL216010 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL214280 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL215819 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL386117 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL385831 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL215958 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL424720 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL373886 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL214442 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL214535 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL373887 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL216561 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL265132 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL215279 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL214177 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL215841 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL384247 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL384626 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL386968 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL385215 | — | IC50 | > | 1000.0 | nM | - |