Assay Detail
Binding
CHEMBL717666
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In vitro activation of mouse recombinant Melanocortin-1 receptor.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 6.34 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL386583 | — | — | 1 | 10.70 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.42 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 9.26 |
| CHEMBL264190 | — | — | 1 | 7.70 |
| CHEMBL317968 | — | — | 1 | 6.75 |
| CHEMBL330561 | — | — | 1 | 6.69 |
| CHEMBL94391 | — | — | 1 | 6.54 |
| CHEMBL327479 | — | — | 1 | 6.30 |
| CHEMBL317969 | — | — | 1 | 5.94 |
| CHEMBL330233 | — | — | 1 | 5.75 |
| CHEMBL96871 | — | — | 1 | 5.58 |
| CHEMBL320157 | — | — | 1 | 5.37 |
| CHEMBL431092 | — | — | 1 | 5.36 |
| CHEMBL432201 | — | — | 1 | 5.27 |
| CHEMBL432027 | — | — | 1 | 5.18 |
| CHEMBL329490 | — | — | 1 | 5.15 |
| CHEMBL96531 | — | — | 1 | 5.11 |
| CHEMBL405174 | — | — | 1 | 5.10 |
| CHEMBL94369 | — | — | 1 | 5.02 |
| CHEMBL275303 | — | — | 1 | 4.95 |
| CHEMBL329847 | — | — | 1 | 4.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL386583 | — | EC50 | = | 0.02 | nM | 10.70 |
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.038 | nM | 10.42 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.55 | nM | 9.26 |
| CHEMBL264190 | — | EC50 | = | 20.1 | nM | 7.70 |
| CHEMBL317968 | — | EC50 | = | 176.0 | nM | 6.75 |
| CHEMBL330561 | — | EC50 | = | 203.0 | nM | 6.69 |
| CHEMBL94391 | — | EC50 | = | 289.0 | nM | 6.54 |
| CHEMBL327479 | — | EC50 | = | 503.0 | nM | 6.30 |
| CHEMBL317969 | — | EC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL330233 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL96871 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL320157 | — | EC50 | = | 4250.0 | nM | 5.37 |
| CHEMBL431092 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL432201 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL432027 | — | EC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL329490 | — | EC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL96531 | — | EC50 | = | 7730.0 | nM | 5.11 |
| CHEMBL405174 | — | EC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL94369 | — | EC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL275303 | — | EC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL329847 | — | EC50 | = | 11500.0 | nM | 4.94 |