Assay Detail
Functional
CHEMBL894439
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.17 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL243338 | — | — | 1 | 7.89 |
| CHEMBL243138 | — | — | 1 | 7.60 |
| CHEMBL394793 | — | — | 1 | 7.58 |
| CHEMBL242689 | — | — | 1 | 7.57 |
| CHEMBL429464 | — | — | 1 | 7.57 |
| CHEMBL388440 | — | — | 1 | 7.57 |
| CHEMBL243355 | — | — | 1 | 7.47 |
| CHEMBL244370 | — | — | 1 | 7.36 |
| CHEMBL390679 | — | — | 1 | 7.24 |
| CHEMBL244369 | — | — | 1 | 7.19 |
| CHEMBL242053 | — | — | 1 | 7.17 |
| CHEMBL242054 | — | — | 1 | 6.89 |
| CHEMBL242902 | — | — | 1 | 6.85 |
| CHEMBL242901 | — | — | 1 | 6.72 |
| CHEMBL396234 | — | — | 1 | 6.72 |
| CHEMBL243129 | — | — | 1 | 6.22 |
| CHEMBL243139 | — | — | 1 | 6.21 |
| CHEMBL388234 | — | — | 1 | - |
| CHEMBL243578 | — | — | 1 | - |
| CHEMBL243507 | — | — | 1 | - |
| CHEMBL243128 | — | — | 1 | - |
| CHEMBL243354 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL243338 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL243138 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL394793 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL242689 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL429464 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL388440 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL243355 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL244370 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL390679 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL244369 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL242053 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL242054 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL242902 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL242901 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL396234 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL243129 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL243139 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL388234 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL243578 | — | IC50 | - | — | - | |
| CHEMBL243507 | — | IC50 | - | — | - | |
| CHEMBL243128 | — | IC50 | - | — | - | |
| CHEMBL243354 | — | IC50 | - | — | - |