Assay Detail
Binding
CHEMBL717664
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Activity in mouse melanocortin-1 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 |
Target
Melanocyte-stimulating hormone receptor (CHEMBL4077) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 6.83 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | — | 1 | 10.70 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.42 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 9.26 |
| CHEMBL357558 | — | — | 1 | 7.75 |
| CHEMBL152612 | — | — | 1 | 7.70 |
| CHEMBL2096693 | — | — | 1 | 7.37 |
| CHEMBL347364 | — | — | 1 | 7.29 |
| CHEMBL151906 | — | — | 1 | 7.10 |
| CHEMBL347216 | — | — | 1 | 6.90 |
| CHEMBL264190 | — | — | 1 | 6.85 |
| CHEMBL348901 | — | — | 1 | 6.51 |
| CHEMBL152986 | — | — | 1 | 6.28 |
| CHEMBL2371147 | — | — | 2 | 6.17 |
| CHEMBL358833 | — | — | 1 | 6.17 |
| CHEMBL154153 | — | — | 1 | 6.14 |
| CHEMBL346925 | — | — | 1 | 6.12 |
| CHEMBL2096745 | — | — | 1 | 5.82 |
| CHEMBL433522 | — | — | 1 | 5.65 |
| CHEMBL152555 | — | — | 1 | 5.64 |
| CHEMBL154251 | — | — | 1 | 5.60 |
| CHEMBL349795 | — | — | 1 | 5.56 |
| CHEMBL350012 | — | — | 1 | 5.42 |
| CHEMBL2371150 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | EC50 | = | 0.02 | nM | 10.70 |
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.038 | nM | 10.42 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.55 | nM | 9.26 |
| CHEMBL357558 | — | EC50 | = | 17.9 | nM | 7.75 |
| CHEMBL152612 | — | EC50 | = | 20.1 | nM | 7.70 |
| CHEMBL2096693 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL347364 | — | EC50 | = | 51.9 | nM | 7.29 |
| CHEMBL151906 | — | EC50 | = | 79.9 | nM | 7.10 |
| CHEMBL347216 | — | EC50 | = | 127.0 | nM | 6.90 |
| CHEMBL264190 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL348901 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL152986 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL2371147 | — | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL358833 | — | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL2371147 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL154153 | — | EC50 | = | 730.0 | nM | 6.14 |
| CHEMBL346925 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL2096745 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL433522 | — | EC50 | = | 2240.0 | nM | 5.65 |
| CHEMBL152555 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL154251 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL349795 | — | EC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL350012 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL2371150 | — | EC50 | = | 4400.0 | nM | 5.36 |