Assay Detail
Binding
CHEMBL711699
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Activity in mouse melanocortin-5 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 | 6.75 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.15 |
| CHEMBL430239 | MELATONAN | — | 1 | 9.80 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 9.36 |
| CHEMBL152612 | — | — | 1 | 8.40 |
| CHEMBL357558 | — | — | 1 | 8.31 |
| CHEMBL347216 | — | — | 1 | 7.92 |
| CHEMBL154153 | — | — | 1 | 7.48 |
| CHEMBL264190 | — | — | 1 | 7.45 |
| CHEMBL151906 | — | — | 1 | 7.32 |
| CHEMBL347364 | — | — | 1 | 7.00 |
| CHEMBL348901 | — | — | 1 | 6.82 |
| CHEMBL2371147 | — | — | 2 | 6.75 |
| CHEMBL154251 | — | — | 1 | 6.33 |
| CHEMBL2096693 | — | — | 1 | 6.16 |
| CHEMBL346925 | — | — | 1 | 6.12 |
| CHEMBL349795 | — | — | 1 | 6.07 |
| CHEMBL152986 | — | — | 1 | 6.05 |
| CHEMBL152555 | — | — | 1 | 5.15 |
| CHEMBL358833 | — | — | 1 | 5.13 |
| CHEMBL433522 | — | — | 1 | 4.84 |
| CHEMBL2096745 | — | — | 1 | 4.61 |
| CHEMBL350012 | — | — | 1 | 4.44 |
| CHEMBL2371150 | — | — | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.071 | nM | 10.15 |
| CHEMBL430239 | MELATONAN | EC50 | = | 0.16 | nM | 9.80 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.44 | nM | 9.36 |
| CHEMBL152612 | — | EC50 | = | 3.96 | nM | 8.40 |
| CHEMBL357558 | — | EC50 | = | 4.86 | nM | 8.31 |
| CHEMBL347216 | — | EC50 | = | 12.1 | nM | 7.92 |
| CHEMBL154153 | — | EC50 | = | 33.1 | nM | 7.48 |
| CHEMBL264190 | — | EC50 | = | 35.3 | nM | 7.45 |
| CHEMBL151906 | — | EC50 | = | 47.7 | nM | 7.32 |
| CHEMBL347364 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL348901 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2371147 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL154251 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL2096693 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL346925 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL349795 | — | EC50 | = | 850.0 | nM | 6.07 |
| CHEMBL152986 | — | EC50 | = | 890.0 | nM | 6.05 |
| CHEMBL2371147 | — | EC50 | = | 960.0 | nM | 6.02 |
| CHEMBL152555 | — | EC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL358833 | — | EC50 | = | 7440.0 | nM | 5.13 |
| CHEMBL433522 | — | EC50 | = | 14500.0 | nM | 4.84 |
| CHEMBL2096745 | — | EC50 | = | 24800.0 | nM | 4.61 |
| CHEMBL350012 | — | EC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL2371150 | — | EC50 | = | 38400.0 | nM | 4.42 |