Assay Detail
Binding
CHEMBL878355
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Activity in mouse melanocortin-3 receptor (mMC3R) 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 | 5.76 | 10.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.01 |
| CHEMBL430239 | MELATONAN | — | 1 | 9.80 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 9.10 |
| CHEMBL152612 | — | — | 1 | 6.81 |
| CHEMBL357558 | — | — | 1 | 6.13 |
| CHEMBL347216 | — | — | 1 | 5.79 |
| CHEMBL154153 | — | — | 1 | 5.46 |
| CHEMBL151906 | — | — | 1 | 5.43 |
| CHEMBL264190 | — | — | 1 | 5.27 |
| CHEMBL2371147 | — | — | 2 | 5.00 |
| CHEMBL347364 | — | — | 1 | 4.87 |
| CHEMBL154251 | — | — | 1 | 4.82 |
| CHEMBL358833 | — | — | 1 | 4.80 |
| CHEMBL348901 | — | — | 1 | 4.79 |
| CHEMBL346925 | — | — | 1 | 4.66 |
| CHEMBL2096693 | — | — | 1 | 4.63 |
| CHEMBL152986 | — | — | 1 | 4.57 |
| CHEMBL349795 | — | — | 1 | 4.52 |
| CHEMBL152555 | — | — | 1 | 4.27 |
| CHEMBL2371150 | — | — | 1 | - |
| CHEMBL350012 | — | — | 1 | - |
| CHEMBL2096745 | — | — | 1 | - |
| CHEMBL433522 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.098 | nM | 10.01 |
| CHEMBL430239 | MELATONAN | EC50 | = | 0.16 | nM | 9.80 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.79 | nM | 9.10 |
| CHEMBL152612 | — | EC50 | = | 156.0 | nM | 6.81 |
| CHEMBL357558 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL347216 | — | EC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL154153 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL151906 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL264190 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL2371147 | — | EC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL347364 | — | EC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL154251 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL358833 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL348901 | — | EC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL346925 | — | EC50 | = | 21900.0 | nM | 4.66 |
| CHEMBL2096693 | — | EC50 | = | 23200.0 | nM | 4.63 |
| CHEMBL152986 | — | EC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL349795 | — | EC50 | = | 30250.0 | nM | 4.52 |
| CHEMBL2371147 | — | EC50 | = | 33500.0 | nM | 4.47 |
| CHEMBL152555 | — | EC50 | = | 53300.0 | nM | 4.27 |
| CHEMBL350012 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL2371150 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL433522 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL2096745 | — | EC50 | > | 100000.0 | nM | - |