Assay Detail
Binding
CHEMBL861265
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Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
19
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Melanin-concentrating hormone receptor 1 (CHEMBL4730) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 18 | 7.01 | 8.30 |
| Ki | 1 | 8.48 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216192 | — | — | 2 | 8.48 |
| CHEMBL214280 | — | — | 1 | 8.15 |
| CHEMBL215418 | — | — | 1 | 7.55 |
| CHEMBL215958 | — | — | 1 | 6.64 |
| CHEMBL214535 | — | — | 1 | 6.47 |
| CHEMBL373886 | — | — | 1 | 6.40 |
| CHEMBL373887 | — | — | 1 | 6.34 |
| CHEMBL424720 | — | — | 1 | 6.21 |
| CHEMBL385215 | — | — | 1 | - |
| CHEMBL386968 | — | — | 1 | - |
| CHEMBL384626 | — | — | 1 | - |
| CHEMBL384247 | — | — | 1 | - |
| CHEMBL215841 | — | — | 1 | - |
| CHEMBL214177 | — | — | 1 | - |
| CHEMBL215279 | — | — | 1 | - |
| CHEMBL216561 | — | — | 1 | - |
| CHEMBL265132 | — | — | 1 | - |
| CHEMBL214442 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216192 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL216192 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL214280 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL215418 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL215958 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL214535 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL373886 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL373887 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL424720 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL214442 | — | IC50 | - | — | - | |
| CHEMBL265132 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL216561 | — | 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 | - |