Assay Detail
Functional
CHEMBL1027401
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Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
27
Total Activities
27
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 | Autocuration |
Publication
Discovery of orally bioavailable 1,3,4-trisubstituted 2-oxopiperazine-based melanocortin-4 receptor agonists as potential antiobesity agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 8.09 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL446757 | — | — | 1 | 9.10 |
| CHEMBL443396 | — | — | 1 | 9.05 |
| CHEMBL442829 | — | — | 1 | 9.05 |
| CHEMBL448410 | — | — | 1 | 9.05 |
| CHEMBL453734 | — | — | 1 | 8.92 |
| CHEMBL506762 | — | — | 1 | 8.89 |
| CHEMBL504349 | — | — | 1 | 8.77 |
| CHEMBL506272 | — | — | 1 | 8.70 |
| CHEMBL213566 | — | — | 1 | 8.66 |
| CHEMBL452710 | — | — | 1 | 8.57 |
| CHEMBL466380 | — | — | 1 | 8.52 |
| CHEMBL449131 | — | — | 1 | 8.30 |
| CHEMBL449050 | — | — | 1 | 8.30 |
| CHEMBL507876 | — | — | 1 | 8.10 |
| CHEMBL450236 | — | — | 1 | 8.05 |
| CHEMBL447117 | — | — | 1 | 8.00 |
| CHEMBL463047 | — | — | 1 | 7.92 |
| CHEMBL448337 | — | — | 1 | 7.60 |
| CHEMBL460138 | — | — | 1 | 7.55 |
| CHEMBL460349 | — | — | 1 | 7.51 |
| CHEMBL517108 | — | — | 1 | 7.43 |
| CHEMBL453300 | — | — | 1 | 7.43 |
| CHEMBL214770 | — | — | 1 | 7.35 |
| CHEMBL451694 | — | — | 1 | 7.33 |
| CHEMBL460142 | — | — | 1 | 7.08 |
| CHEMBL445009 | — | — | 1 | 6.78 |
| CHEMBL468252 | — | — | 1 | 6.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL446757 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL443396 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL442829 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL448410 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL453734 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL506762 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL504349 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL506272 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL213566 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL452710 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL466380 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL449131 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL449050 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL507876 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL450236 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL447117 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL463047 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL448337 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL460138 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL460349 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL517108 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL453300 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL214770 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL451694 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL460142 | — | EC50 | = | 83.0 | nM | 7.08 |
| CHEMBL445009 | — | EC50 | = | 167.0 | nM | 6.78 |
| CHEMBL468252 | — | EC50 | = | 391.0 | nM | 6.41 |