Assay Detail
Binding
CHEMBL861585
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell
42
Total Activities
41
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 | Expert |
Target
Melanin-concentrating hormone receptor 1 (CHEMBL344) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of orally efficacious melanin-concentrating hormone receptor-1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 7.83 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL382668 | — | — | 1 | 8.80 |
| CHEMBL380509 | — | — | 1 | 8.74 |
| CHEMBL425410 | — | — | 1 | 8.70 |
| CHEMBL382140 | — | — | 1 | 8.66 |
| CHEMBL206616 | — | — | 1 | 8.64 |
| CHEMBL383340 | — | — | 1 | 8.60 |
| CHEMBL208025 | — | — | 1 | 8.60 |
| CHEMBL205285 | — | — | 1 | 8.57 |
| CHEMBL204881 | — | — | 1 | 8.55 |
| CHEMBL206248 | — | — | 1 | 8.54 |
| CHEMBL382177 | — | — | 1 | 8.48 |
| CHEMBL205838 | — | — | 1 | 8.46 |
| CHEMBL204407 | — | — | 1 | 8.40 |
| CHEMBL206503 | — | — | 1 | 8.39 |
| CHEMBL204212 | — | — | 1 | 8.36 |
| CHEMBL204161 | — | — | 1 | 8.15 |
| CHEMBL382631 | — | — | 1 | 8.15 |
| CHEMBL206831 | — | — | 1 | 8.10 |
| CHEMBL381810 | — | — | 1 | 8.05 |
| CHEMBL378019 | — | — | 1 | 8.05 |
| CHEMBL205979 | — | — | 1 | 8.03 |
| CHEMBL382841 | — | — | 1 | 8.00 |
| CHEMBL190068 | — | — | 1 | 7.94 |
| CHEMBL383432 | — | — | 1 | 7.89 |
| CHEMBL205397 | — | — | 2 | 7.89 |
| CHEMBL381162 | — | — | 1 | 7.89 |
| CHEMBL203166 | — | — | 1 | 7.82 |
| CHEMBL206637 | — | — | 1 | 7.82 |
| CHEMBL203388 | — | — | 1 | 7.82 |
| CHEMBL377955 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL382668 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL380509 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL425410 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL382140 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL206616 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL383340 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL208025 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL205285 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL204881 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL206248 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL382177 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL205838 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL204407 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL206503 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL204212 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL204161 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL382631 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL206831 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL381810 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL378019 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL205979 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL382841 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL190068 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL383432 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL205397 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL381162 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL203166 | — | Ki | = | 15.1 | nM | 7.82 |
| CHEMBL206637 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL203388 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL377955 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL205397 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL206195 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL203445 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL205874 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL380692 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL206498 | — | Ki | = | 394.0 | nM | 6.41 |
| CHEMBL437130 | — | Ki | = | 605.0 | nM | 6.22 |
| CHEMBL204514 | — | Ki | = | 727.0 | nM | 6.14 |
| CHEMBL206825 | — | Ki | = | 974.0 | nM | 6.01 |
| CHEMBL382772 | — | Ki | = | 1615.0 | nM | 5.79 |
| CHEMBL206813 | — | Ki | = | 2190.0 | nM | 5.66 |
| CHEMBL380718 | — | Ki | > | 3000.0 | nM | - |