Assay Detail
Binding
CHEMBL903910
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells
64
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 64 | 6.94 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL362985 | — | — | 3 | 8.09 |
| CHEMBL226281 | — | — | 1 | 7.98 |
| CHEMBL226025 | — | — | 1 | 7.95 |
| CHEMBL226176 | — | — | 1 | 7.93 |
| CHEMBL226228 | — | — | 1 | 7.82 |
| CHEMBL226024 | — | — | 1 | 7.75 |
| CHEMBL225966 | — | — | 1 | 7.66 |
| CHEMBL226123 | — | — | 1 | 7.64 |
| CHEMBL226280 | — | — | 1 | 7.63 |
| CHEMBL226227 | — | — | 1 | 7.61 |
| CHEMBL376829 | — | — | 1 | 7.58 |
| CHEMBL226125 | — | — | 1 | 7.57 |
| CHEMBL226177 | — | — | 1 | 7.57 |
| CHEMBL226124 | — | — | 1 | 7.48 |
| CHEMBL226279 | — | — | 1 | 7.43 |
| CHEMBL376609 | — | — | 1 | 7.43 |
| CHEMBL226342 | — | — | 1 | 7.38 |
| CHEMBL427270 | — | — | 1 | 7.37 |
| CHEMBL225968 | — | — | 1 | 7.33 |
| CHEMBL226341 | — | — | 1 | 7.27 |
| CHEMBL433574 | — | — | 1 | 7.24 |
| CHEMBL226497 | — | — | 1 | 7.20 |
| CHEMBL226072 | — | — | 1 | 7.19 |
| CHEMBL375251 | — | — | 1 | 7.14 |
| CHEMBL225967 | — | — | 1 | 7.08 |
| CHEMBL226498 | — | — | 1 | 7.07 |
| CHEMBL389073 | — | — | 1 | 7.03 |
| CHEMBL226391 | — | — | 1 | 7.00 |
| CHEMBL225693 | — | — | 1 | 6.98 |
| CHEMBL226443 | — | — | 1 | 6.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL362985 | — | IC50 | = | 8.13 | nM | 8.09 |
| CHEMBL226281 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL226025 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL226176 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL362985 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL226228 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL226024 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL225966 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL362985 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL226123 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL226280 | — | IC50 | = | 23.6 | nM | 7.63 |
| CHEMBL226227 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL376829 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL226125 | — | IC50 | = | 27.1 | nM | 7.57 |
| CHEMBL226177 | — | IC50 | = | 27.1 | nM | 7.57 |
| CHEMBL226124 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL226279 | — | IC50 | = | 36.8 | nM | 7.43 |
| CHEMBL376609 | — | IC50 | = | 36.8 | nM | 7.43 |
| CHEMBL226342 | — | IC50 | = | 41.8 | nM | 7.38 |
| CHEMBL427270 | — | IC50 | = | 42.6 | nM | 7.37 |
| CHEMBL225968 | — | IC50 | = | 47.2 | nM | 7.33 |
| CHEMBL226341 | — | IC50 | = | 53.2 | nM | 7.27 |
| CHEMBL433574 | — | IC50 | = | 57.3 | nM | 7.24 |
| CHEMBL226497 | — | IC50 | = | 62.8 | nM | 7.20 |
| CHEMBL226072 | — | IC50 | = | 65.1 | nM | 7.19 |
| CHEMBL375251 | — | IC50 | = | 72.3 | nM | 7.14 |
| CHEMBL225967 | — | IC50 | = | 82.8 | nM | 7.08 |
| CHEMBL226498 | — | IC50 | = | 85.9 | nM | 7.07 |
| CHEMBL389073 | — | IC50 | = | 92.5 | nM | 7.03 |
| CHEMBL226391 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL225693 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL226443 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL374176 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL225965 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL225749 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL226073 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL225854 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL225748 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL226023 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL226442 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL226496 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL225909 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL220092 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL225964 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL226444 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL226074 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL225910 | — | IC50 | = | 263.0 | nM | 6.58 |
| CHEMBL225855 | — | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL225692 | — | IC50 | = | 303.0 | nM | 6.52 |
| CHEMBL389956 | — | IC50 | = | 341.0 | nM | 6.47 |