Assay Detail
Binding
CHEMBL824628
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Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
25
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Selective, high affinity peptide antagonists of alpha-melanotropin action at human melanocortin receptor 4: their synthesis and biological evaluation in vitro.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 6.86 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL442504 | — | — | 1 | 9.64 |
| CHEMBL385465 | — | — | 1 | 9.02 |
| CHEMBL408843 | — | — | 1 | 8.59 |
| CHEMBL420167 | — | — | 1 | 7.85 |
| CHEMBL2370533 | — | — | 1 | 7.70 |
| CHEMBL331259 | — | — | 1 | 7.70 |
| CHEMBL2370553 | — | — | 1 | 7.60 |
| CHEMBL268851 | — | — | 1 | 7.54 |
| CHEMBL434985 | — | — | 1 | 7.54 |
| CHEMBL124169 | — | — | 1 | 7.33 |
| CHEMBL333178 | — | — | 1 | 7.25 |
| CHEMBL122773 | — | — | 2 | 6.92 |
| CHEMBL266417 | — | — | 1 | 6.85 |
| CHEMBL123938 | — | — | 1 | 6.82 |
| CHEMBL407213 | — | — | 1 | 6.72 |
| CHEMBL433645 | — | — | 1 | 6.38 |
| CHEMBL331728 | — | — | 1 | 5.82 |
| CHEMBL333262 | — | — | 1 | 5.54 |
| CHEMBL334309 | — | — | 1 | 5.52 |
| CHEMBL333263 | — | — | 1 | 5.52 |
| CHEMBL420727 | — | — | 1 | 5.23 |
| CHEMBL332762 | — | — | 1 | 5.23 |
| CHEMBL432407 | — | — | 1 | 5.23 |
| CHEMBL436169 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL442504 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL385465 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL408843 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL420167 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2370533 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL331259 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2370553 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL268851 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL434985 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL124169 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL333178 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL122773 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL266417 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL123938 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL407213 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL122773 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL433645 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL331728 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL333262 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL334309 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL333263 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL420727 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL332762 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL432407 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL436169 | — | Ki | = | 5900.0 | nM | 5.23 |