Assay Detail
Binding
CHEMBL856320
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Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells
60
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Propionylpiperazines as human melanocortin-4 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 60 | 6.52 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL378327 | — | — | 1 | 8.23 |
| CHEMBL425261 | — | — | 1 | 8.19 |
| CHEMBL214886 | — | — | 1 | 8.09 |
| CHEMBL212180 | — | — | 1 | 8.06 |
| CHEMBL215066 | — | — | 1 | 8.04 |
| CHEMBL213721 | — | — | 1 | 7.92 |
| CHEMBL377231 | — | — | 1 | 7.85 |
| CHEMBL385274 | — | — | 1 | 7.80 |
| CHEMBL386771 | — | — | 1 | 7.70 |
| CHEMBL213122 | — | — | 1 | 7.60 |
| CHEMBL386259 | — | — | 1 | 7.58 |
| CHEMBL425962 | — | — | 1 | 7.51 |
| CHEMBL215617 | — | — | 1 | 7.51 |
| CHEMBL213469 | — | — | 1 | 7.44 |
| CHEMBL214551 | — | — | 1 | 7.42 |
| CHEMBL212451 | — | — | 1 | 7.33 |
| CHEMBL215905 | — | — | 1 | 7.22 |
| CHEMBL385003 | — | — | 1 | 7.17 |
| CHEMBL215906 | — | — | 1 | 7.17 |
| CHEMBL215106 | — | — | 1 | 7.15 |
| CHEMBL212779 | — | — | 1 | 7.10 |
| CHEMBL386707 | — | — | 1 | 7.04 |
| CHEMBL214799 | — | — | 1 | 6.92 |
| CHEMBL212802 | — | — | 2 | 6.92 |
| CHEMBL215481 | — | — | 1 | 6.85 |
| CHEMBL386162 | — | — | 1 | 6.80 |
| CHEMBL378448 | — | — | 1 | 6.70 |
| CHEMBL378913 | — | — | 1 | 6.64 |
| CHEMBL378425 | — | — | 1 | 6.62 |
| CHEMBL438275 | — | — | 1 | 6.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL378327 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL425261 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL214886 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL212180 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL215066 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL213721 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL377231 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL385274 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL386771 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL213122 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL386259 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL215617 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL425962 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL213469 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL214551 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL212451 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL215905 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL385003 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL215906 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL215106 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL212779 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL386707 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL212802 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL214799 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL215481 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL386162 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL378448 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL378913 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL378425 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL438275 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL380018 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL215519 | — | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL215609 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL212664 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL212802 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL212882 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL379200 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL215531 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL215502 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL214559 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL214582 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL213153 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL215332 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL378671 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL213152 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL215290 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL384852 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL214560 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL214155 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL213214 | — | Ki | = | 4000.0 | nM | 5.40 |