Assay Detail
Functional
CHEMBL1027399
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
22
Total Activities
22
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 |
Target
Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 22 | 6.60 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL506762 | — | — | 1 | 8.00 |
| CHEMBL450236 | — | — | 1 | 7.36 |
| CHEMBL447117 | — | — | 1 | 7.32 |
| CHEMBL504349 | — | — | 1 | 7.30 |
| CHEMBL448410 | — | — | 1 | 7.16 |
| CHEMBL446757 | — | — | 1 | 7.10 |
| CHEMBL452710 | — | — | 1 | 7.01 |
| CHEMBL506272 | — | — | 1 | 6.98 |
| CHEMBL453734 | — | — | 1 | 6.84 |
| CHEMBL442829 | — | — | 1 | 6.77 |
| CHEMBL463047 | — | — | 1 | 6.71 |
| CHEMBL449050 | — | — | 1 | 6.51 |
| CHEMBL448337 | — | — | 1 | 6.41 |
| CHEMBL449131 | — | — | 1 | 6.37 |
| CHEMBL451694 | — | — | 1 | 6.13 |
| CHEMBL507876 | — | — | 1 | 6.10 |
| CHEMBL453300 | — | — | 1 | 6.06 |
| CHEMBL466380 | — | — | 1 | 5.97 |
| CHEMBL460138 | — | — | 1 | 5.82 |
| CHEMBL460142 | — | — | 1 | 5.82 |
| CHEMBL460349 | — | — | 1 | 5.77 |
| CHEMBL517108 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL506762 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL450236 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL447117 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL504349 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL448410 | — | EC50 | = | 69.0 | nM | 7.16 |
| CHEMBL446757 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL452710 | — | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL506272 | — | EC50 | = | 104.0 | nM | 6.98 |
| CHEMBL453734 | — | EC50 | = | 145.0 | nM | 6.84 |
| CHEMBL442829 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL463047 | — | EC50 | = | 193.0 | nM | 6.71 |
| CHEMBL449050 | — | EC50 | = | 308.0 | nM | 6.51 |
| CHEMBL448337 | — | EC50 | = | 392.0 | nM | 6.41 |
| CHEMBL449131 | — | EC50 | = | 432.0 | nM | 6.37 |
| CHEMBL451694 | — | EC50 | = | 734.0 | nM | 6.13 |
| CHEMBL507876 | — | EC50 | = | 796.0 | nM | 6.10 |
| CHEMBL453300 | — | EC50 | = | 878.0 | nM | 6.06 |
| CHEMBL466380 | — | EC50 | = | 1076.0 | nM | 5.97 |
| CHEMBL460138 | — | EC50 | = | 1505.0 | nM | 5.82 |
| CHEMBL460142 | — | EC50 | = | 1523.0 | nM | 5.82 |
| CHEMBL460349 | — | EC50 | = | 1697.0 | nM | 5.77 |
| CHEMBL517108 | — | EC50 | = | 2300.0 | nM | 5.64 |