Assay Detail
Functional
CHEMBL834412
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
37
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 37 | 7.05 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL359976 | — | — | 1 | 8.54 |
| CHEMBL360716 | — | — | 1 | 8.42 |
| CHEMBL339053 | — | — | 1 | 8.24 |
| CHEMBL349850 | — | — | 1 | 8.15 |
| CHEMBL185035 | — | — | 1 | 7.92 |
| CHEMBL184405 | — | — | 1 | 7.82 |
| CHEMBL125819 | — | — | 1 | 7.82 |
| CHEMBL363925 | — | — | 1 | 7.75 |
| CHEMBL366321 | — | — | 1 | 7.47 |
| CHEMBL184325 | — | — | 1 | 7.44 |
| CHEMBL183890 | — | — | 1 | 7.40 |
| CHEMBL341982 | — | — | 1 | 7.40 |
| CHEMBL360989 | — | — | 1 | 7.29 |
| CHEMBL185417 | — | — | 1 | 7.14 |
| CHEMBL340355 | — | — | 2 | 7.10 |
| CHEMBL360169 | — | — | 1 | 7.05 |
| CHEMBL184068 | — | — | 1 | 7.04 |
| CHEMBL182231 | — | — | 1 | 7.03 |
| CHEMBL365636 | — | — | 1 | 6.86 |
| CHEMBL363074 | — | — | 1 | 6.84 |
| CHEMBL364577 | — | — | 1 | 6.79 |
| CHEMBL185145 | — | — | 1 | 6.76 |
| CHEMBL185583 | — | — | 1 | 6.72 |
| CHEMBL359777 | — | — | 1 | 6.68 |
| CHEMBL433710 | — | — | 1 | 6.62 |
| CHEMBL363684 | — | — | 1 | 6.60 |
| CHEMBL413556 | — | — | 1 | 6.56 |
| CHEMBL183434 | — | — | 1 | 6.56 |
| CHEMBL362880 | — | — | 1 | 6.52 |
| CHEMBL366706 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL359976 | — | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL360716 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL339053 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL349850 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL185035 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL184405 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL125819 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL363925 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL366321 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL184325 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL183890 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL341982 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL360989 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL185417 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL340355 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL360169 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL184068 | — | EC50 | = | 91.0 | nM | 7.04 |
| CHEMBL182231 | — | EC50 | = | 94.0 | nM | 7.03 |
| CHEMBL340355 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL365636 | — | EC50 | = | 138.0 | nM | 6.86 |
| CHEMBL363074 | — | EC50 | = | 146.0 | nM | 6.84 |
| CHEMBL364577 | — | EC50 | = | 164.0 | nM | 6.79 |
| CHEMBL185145 | — | EC50 | = | 174.0 | nM | 6.76 |
| CHEMBL185583 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL359777 | — | EC50 | = | 208.0 | nM | 6.68 |
| CHEMBL433710 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL363684 | — | EC50 | = | 253.0 | nM | 6.60 |
| CHEMBL413556 | — | EC50 | = | 274.0 | nM | 6.56 |
| CHEMBL183434 | — | EC50 | = | 274.0 | nM | 6.56 |
| CHEMBL362880 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL366706 | — | EC50 | = | 357.0 | nM | 6.45 |
| CHEMBL365279 | — | EC50 | = | 460.0 | nM | 6.34 |
| CHEMBL184526 | — | EC50 | = | 487.0 | nM | 6.31 |
| CHEMBL362147 | — | EC50 | = | 577.0 | nM | 6.24 |
| CHEMBL185427 | — | EC50 | = | 632.0 | nM | 6.20 |
| CHEMBL365278 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL185094 | — | EC50 | = | 2060.0 | nM | 5.69 |