Assay Detail
Functional
CHEMBL4052199
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa1-Arg-(pI)DPhe-Xaa4-NH2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 32 | 5.86 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.74 |
| CHEMBL264190 | — | — | 1 | 8.52 |
| CHEMBL4083717 | — | — | 1 | 8.06 |
| CHEMBL4063911 | — | — | 1 | 7.77 |
| CHEMBL4079298 | — | — | 1 | 6.70 |
| CHEMBL4071063 | — | — | 1 | 6.68 |
| CHEMBL4078495 | — | — | 1 | 6.60 |
| CHEMBL4091894 | — | — | 1 | 6.57 |
| CHEMBL4102774 | — | — | 1 | 6.47 |
| CHEMBL4072129 | — | — | 1 | 6.30 |
| CHEMBL4100160 | — | — | 1 | 6.24 |
| CHEMBL4086346 | — | — | 1 | 6.17 |
| CHEMBL4068643 | — | — | 1 | 6.00 |
| CHEMBL4092424 | — | — | 1 | 5.89 |
| CHEMBL4080138 | — | — | 1 | 5.54 |
| CHEMBL4073316 | — | — | 1 | 5.39 |
| CHEMBL4103567 | — | — | 1 | 5.36 |
| CHEMBL4105142 | — | — | 1 | 5.30 |
| CHEMBL4102613 | — | — | 1 | 5.27 |
| CHEMBL4103985 | — | — | 1 | 5.26 |
| CHEMBL4062425 | — | — | 1 | 5.08 |
| CHEMBL4074368 | — | — | 1 | 4.80 |
| CHEMBL4079721 | — | — | 1 | 4.75 |
| CHEMBL4064728 | — | — | 1 | 4.58 |
| CHEMBL4073782 | — | — | 1 | 4.17 |
| CHEMBL4084136 | — | — | 1 | 4.17 |
| CHEMBL4087277 | — | — | 1 | 4.16 |
| CHEMBL4100584 | — | — | 1 | 4.15 |
| CHEMBL4065189 | — | — | 1 | 4.14 |
| CHEMBL4084671 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.18 | nM | 9.74 |
| CHEMBL264190 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4083717 | — | EC50 | = | 8.8 | nM | 8.06 |
| CHEMBL4063911 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4079298 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4071063 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4078495 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4091894 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4102774 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4072129 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4100160 | — | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4086346 | — | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4068643 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4092424 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4080138 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4073316 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4103567 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4105142 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4102613 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4103985 | — | EC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4062425 | — | EC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL4074368 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4079721 | — | EC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4064728 | — | EC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4073782 | — | EC50 | = | 68000.0 | nM | 4.17 |
| CHEMBL4084136 | — | EC50 | = | 67000.0 | nM | 4.17 |
| CHEMBL4087277 | — | EC50 | = | 69000.0 | nM | 4.16 |
| CHEMBL4100584 | — | EC50 | = | 71000.0 | nM | 4.15 |
| CHEMBL4065189 | — | EC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL4084671 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4092849 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4089759 | — | EC50 | > | 100000.0 | nM | - |