Assay Detail
Binding
CHEMBL824629
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Binding affinity against human melanocortin receptor 4 (hMC4R) (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 | 8.15 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL442504 | — | — | 1 | 10.22 |
| CHEMBL385465 | — | — | 1 | 10.02 |
| CHEMBL434985 | — | — | 1 | 9.59 |
| CHEMBL331259 | — | — | 1 | 9.55 |
| CHEMBL333178 | — | — | 1 | 9.43 |
| CHEMBL123938 | — | — | 1 | 9.30 |
| CHEMBL408843 | — | — | 1 | 9.24 |
| CHEMBL122773 | — | — | 2 | 9.24 |
| CHEMBL268851 | — | — | 1 | 9.07 |
| CHEMBL124169 | — | — | 1 | 9.06 |
| CHEMBL2370553 | — | — | 1 | 8.82 |
| CHEMBL420167 | — | — | 1 | 8.80 |
| CHEMBL2370533 | — | — | 1 | 8.66 |
| CHEMBL433645 | — | — | 1 | 8.40 |
| CHEMBL407213 | — | — | 1 | 8.37 |
| CHEMBL266417 | — | — | 1 | 7.70 |
| CHEMBL334309 | — | — | 1 | 7.24 |
| CHEMBL331728 | — | — | 1 | 6.96 |
| CHEMBL333262 | — | — | 1 | 6.38 |
| CHEMBL333263 | — | — | 1 | 6.22 |
| CHEMBL332762 | — | — | 1 | 6.02 |
| CHEMBL436169 | — | — | 1 | 5.89 |
| CHEMBL432407 | — | — | 1 | 5.43 |
| CHEMBL420727 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL442504 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL385465 | — | Ki | = | 0.096 | nM | 10.02 |
| CHEMBL434985 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL331259 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL333178 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL123938 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL122773 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL408843 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL268851 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL124169 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL2370553 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL122773 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL420167 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2370533 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL433645 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL407213 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL266417 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL334309 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL331728 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL333262 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL333263 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL332762 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL436169 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL432407 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL420727 | — | Ki | = | 3800.0 | nM | 5.42 |