Assay Detail
Functional
CHEMBL4052189
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
30
Total Activities
30
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 | 30 | 6.20 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.05 |
| CHEMBL4083717 | — | — | 1 | 7.80 |
| CHEMBL4063911 | — | — | 1 | 7.40 |
| CHEMBL4072129 | — | — | 1 | 7.24 |
| CHEMBL264190 | — | — | 1 | 7.14 |
| CHEMBL4071063 | — | — | 1 | 6.80 |
| CHEMBL4091894 | — | — | 1 | 6.34 |
| CHEMBL4102774 | — | — | 1 | 6.27 |
| CHEMBL4078495 | — | — | 1 | 6.22 |
| CHEMBL4079298 | — | — | 1 | 6.21 |
| CHEMBL4092424 | — | — | 1 | 6.03 |
| CHEMBL4086346 | — | — | 1 | 5.96 |
| CHEMBL4102613 | — | — | 1 | 5.82 |
| CHEMBL4103985 | — | — | 1 | 5.64 |
| CHEMBL4079721 | — | — | 1 | 5.60 |
| CHEMBL4073316 | — | — | 1 | 5.60 |
| CHEMBL4103567 | — | — | 1 | 5.52 |
| CHEMBL4100160 | — | — | 1 | 5.41 |
| CHEMBL4084671 | — | — | 1 | 5.40 |
| CHEMBL4065669 | — | — | 1 | 5.30 |
| CHEMBL4064728 | — | — | 1 | 5.05 |
| CHEMBL4074368 | — | — | 1 | 4.89 |
| CHEMBL4062425 | — | — | 1 | 4.85 |
| CHEMBL4073480 | — | — | 1 | - |
| CHEMBL4089759 | — | — | 1 | - |
| CHEMBL4098164 | — | — | 1 | - |
| CHEMBL4100584 | — | — | 1 | - |
| CHEMBL4092849 | — | — | 1 | - |
| CHEMBL4069415 | — | — | 1 | - |
| CHEMBL4090448 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.09 | nM | 10.05 |
| CHEMBL4083717 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4063911 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4072129 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL264190 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4071063 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4091894 | — | EC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4102774 | — | EC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4078495 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4079298 | — | EC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4092424 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4086346 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4102613 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4103985 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4079721 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4073316 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4103567 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4100160 | — | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4084671 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4065669 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4064728 | — | EC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL4074368 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4062425 | — | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4073480 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4089759 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4098164 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4100584 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4092849 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4069415 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4090448 | — | EC50 | > | 100000.0 | nM | - |