Assay Detail
Functional
CHEMBL854912
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Functional antagonism of MCH-R1 expressed in HEK293 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Melanin-concentrating hormone receptor 1 (CHEMBL344) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists--Increasing selectivity over hERG.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.90 | 8.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216821 | — | — | 1 | 8.13 |
| CHEMBL215278 | — | — | 1 | 7.96 |
| CHEMBL217820 | — | — | 1 | 7.92 |
| CHEMBL216741 | — | — | 1 | 7.75 |
| CHEMBL215660 | — | — | 1 | 7.70 |
| CHEMBL214432 | — | — | 1 | 7.62 |
| CHEMBL261964 | — | — | 1 | 6.99 |
| CHEMBL216406 | — | — | 1 | 6.93 |
| CHEMBL437728 | — | — | 1 | 6.89 |
| CHEMBL267320 | — | — | 1 | 6.85 |
| CHEMBL424895 | — | — | 1 | 6.84 |
| CHEMBL214178 | — | — | 1 | 6.84 |
| CHEMBL216314 | — | — | 1 | 6.74 |
| CHEMBL213771 | — | — | 1 | 6.52 |
| CHEMBL268848 | — | — | 1 | 6.14 |
| CHEMBL217860 | — | — | 1 | 6.12 |
| CHEMBL216187 | — | — | 1 | 6.05 |
| CHEMBL216050 | — | — | 1 | 5.61 |
| CHEMBL216429 | — | — | 1 | 5.46 |
| CHEMBL217501 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216821 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL215278 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL217820 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL216741 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL215660 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL214432 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL261964 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL216406 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL437728 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL267320 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL424895 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL214178 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL216314 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL213771 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL268848 | — | Ki | = | 727.0 | nM | 6.14 |
| CHEMBL217860 | — | Ki | = | 755.0 | nM | 6.12 |
| CHEMBL216187 | — | Ki | = | 890.0 | nM | 6.05 |
| CHEMBL216050 | — | Ki | = | 2480.0 | nM | 5.61 |
| CHEMBL216429 | — | Ki | = | 3465.0 | nM | 5.46 |
| CHEMBL217501 | — | Ki | - | — | - |