Assay Detail
Binding
CHEMBL714369
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Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
24
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 6.14 | 10.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | — | 1 | 10.06 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.68 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 8.27 |
| CHEMBL357558 | — | — | 1 | 7.80 |
| CHEMBL152612 | — | — | 1 | 7.76 |
| CHEMBL347216 | — | — | 1 | 7.33 |
| CHEMBL151906 | — | — | 1 | 6.84 |
| CHEMBL264190 | — | — | 1 | 6.62 |
| CHEMBL154153 | — | — | 1 | 6.58 |
| CHEMBL154251 | — | — | 1 | 6.00 |
| CHEMBL348901 | — | — | 1 | 5.82 |
| CHEMBL347364 | — | — | 1 | 5.57 |
| CHEMBL2371147 | — | — | 2 | 5.46 |
| CHEMBL346925 | — | — | 1 | 5.27 |
| CHEMBL358833 | — | — | 1 | 5.11 |
| CHEMBL152986 | — | — | 1 | 5.11 |
| CHEMBL349795 | — | — | 1 | 5.09 |
| CHEMBL2096693 | — | — | 1 | 5.07 |
| CHEMBL152555 | — | — | 1 | 4.94 |
| CHEMBL350012 | — | — | 1 | 4.56 |
| CHEMBL433522 | — | — | 1 | 4.52 |
| CHEMBL2096745 | — | — | 1 | 4.41 |
| CHEMBL2371150 | — | — | 1 | 4.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | EC50 | = | 0.087 | nM | 10.06 |
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.21 | nM | 9.68 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 5.37 | nM | 8.27 |
| CHEMBL357558 | — | EC50 | = | 15.8 | nM | 7.80 |
| CHEMBL152612 | — | EC50 | = | 17.2 | nM | 7.76 |
| CHEMBL347216 | — | EC50 | = | 46.2 | nM | 7.33 |
| CHEMBL151906 | — | EC50 | = | 143.0 | nM | 6.84 |
| CHEMBL264190 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL154153 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL154251 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL348901 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL347364 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL2371147 | — | EC50 | = | 3460.0 | nM | 5.46 |
| CHEMBL346925 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL152986 | — | EC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL358833 | — | EC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL349795 | — | EC50 | = | 8120.0 | nM | 5.09 |
| CHEMBL2096693 | — | EC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL2371147 | — | EC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL152555 | — | EC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL350012 | — | EC50 | = | 27600.0 | nM | 4.56 |
| CHEMBL433522 | — | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL2096745 | — | EC50 | = | 39400.0 | nM | 4.41 |
| CHEMBL2371150 | — | EC50 | = | 43700.0 | nM | 4.36 |