Assay Detail
Functional
CHEMBL854911
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Functional antagonism of MCH-R1 expressed in HEK293 cells
14
Total Activities
14
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
Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.85 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL217637 | — | — | 1 | 7.96 |
| CHEMBL450942 | — | — | 1 | 7.82 |
| CHEMBL408198 | — | — | 1 | 7.66 |
| CHEMBL216280 | — | — | 1 | 7.64 |
| CHEMBL217861 | — | — | 1 | 7.11 |
| CHEMBL217605 | — | — | 1 | 7.09 |
| CHEMBL217196 | — | — | 1 | 6.83 |
| CHEMBL216242 | — | — | 1 | 6.64 |
| CHEMBL425445 | — | — | 1 | 6.30 |
| CHEMBL217351 | — | — | 1 | 6.20 |
| CHEMBL384546 | — | — | 1 | 5.61 |
| CHEMBL217140 | — | — | 1 | 5.28 |
| CHEMBL385340 | — | — | 1 | - |
| CHEMBL384492 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL217637 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL450942 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL408198 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL216280 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL217861 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL217605 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL217196 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL216242 | — | Ki | = | 228.0 | nM | 6.64 |
| CHEMBL425445 | — | Ki | = | 497.0 | nM | 6.30 |
| CHEMBL217351 | — | Ki | = | 625.0 | nM | 6.20 |
| CHEMBL384546 | — | Ki | = | 2482.0 | nM | 5.61 |
| CHEMBL217140 | — | Ki | = | 5294.0 | nM | 5.28 |
| CHEMBL385340 | — | Ki | - | — | - | |
| CHEMBL384492 | — | Ki | - | — | - |