Assay Detail
Functional
CHEMBL4052196
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
42
Total Activities
42
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 |
Target
Melanocyte-stimulating hormone receptor (CHEMBL4077) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 42 | 6.60 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.70 |
| CHEMBL4083717 | — | — | 1 | 9.29 |
| CHEMBL4063911 | — | — | 1 | 9.15 |
| CHEMBL4078495 | — | — | 1 | 8.15 |
| CHEMBL4079298 | — | — | 1 | 8.10 |
| CHEMBL264190 | — | — | 1 | 7.70 |
| CHEMBL4103567 | — | — | 1 | 7.27 |
| CHEMBL4102774 | — | — | 1 | 7.26 |
| CHEMBL4071063 | — | — | 1 | 7.25 |
| CHEMBL4091894 | — | — | 1 | 7.16 |
| CHEMBL4073316 | — | — | 1 | 7.14 |
| CHEMBL4086346 | — | — | 1 | 7.04 |
| CHEMBL4100160 | — | — | 1 | 7.03 |
| CHEMBL4068643 | — | — | 1 | 6.68 |
| CHEMBL4084671 | — | — | 1 | 6.68 |
| CHEMBL4072129 | — | — | 1 | 6.55 |
| CHEMBL4092424 | — | — | 1 | 6.48 |
| CHEMBL4080138 | — | — | 1 | 6.46 |
| CHEMBL4074368 | — | — | 1 | 6.36 |
| CHEMBL4102613 | — | — | 1 | 6.34 |
| CHEMBL4089759 | — | — | 1 | 6.27 |
| CHEMBL4101856 | — | — | 1 | 6.22 |
| CHEMBL4083857 | — | — | 1 | 6.12 |
| CHEMBL4066083 | — | — | 1 | 6.11 |
| CHEMBL4060738 | — | — | 1 | 6.00 |
| CHEMBL4099096 | — | — | 1 | 5.92 |
| CHEMBL4094121 | — | — | 1 | 5.92 |
| CHEMBL4079721 | — | — | 1 | 5.75 |
| CHEMBL4064881 | — | — | 1 | 5.58 |
| CHEMBL4103985 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.02 | nM | 10.70 |
| CHEMBL4083717 | — | EC50 | = | 0.51 | nM | 9.29 |
| CHEMBL4063911 | — | EC50 | = | 0.71 | nM | 9.15 |
| CHEMBL4078495 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4079298 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL264190 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4103567 | — | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4102774 | — | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4071063 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4091894 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4073316 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4086346 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4100160 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4068643 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4084671 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4072129 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4092424 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4080138 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4074368 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4102613 | — | EC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4089759 | — | EC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4101856 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4083857 | — | EC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4066083 | — | EC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4060738 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4099096 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4094121 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4079721 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4064881 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4103985 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4073480 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4065669 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4082615 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4079580 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4068777 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4087093 | — | EC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4062425 | — | EC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL4069415 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4087277 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4092849 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4065189 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4084136 | — | EC50 | > | 100000.0 | nM | - |