Assay Detail
Functional
CHEMBL4835795
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Melanocyte-stimulating hormone receptor (CHEMBL4077) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 29 | 6.13 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.05 |
| CHEMBL438402 | — | — | 1 | 9.19 |
| CHEMBL264190 | — | — | 1 | 7.87 |
| CHEMBL342954 | — | — | 1 | 7.00 |
| CHEMBL4846261 | — | — | 1 | 6.70 |
| CHEMBL4877184 | — | — | 1 | 6.54 |
| CHEMBL4877232 | — | — | 1 | 6.54 |
| CHEMBL4868636 | — | — | 1 | 6.52 |
| CHEMBL4856877 | — | — | 1 | 6.52 |
| CHEMBL4848322 | — | — | 1 | 6.52 |
| CHEMBL4863206 | — | — | 1 | 6.48 |
| CHEMBL4868223 | — | — | 1 | 6.36 |
| CHEMBL4845842 | — | — | 1 | 6.30 |
| CHEMBL4878558 | — | — | 1 | 6.26 |
| CHEMBL4849626 | — | — | 1 | 6.24 |
| CHEMBL4872932 | — | — | 1 | 6.22 |
| CHEMBL4866532 | — | — | 1 | 6.16 |
| CHEMBL4877537 | — | — | 1 | 5.64 |
| CHEMBL4869669 | — | — | 1 | 5.64 |
| CHEMBL4847357 | — | — | 1 | 5.21 |
| CHEMBL4856539 | — | — | 1 | 5.17 |
| CHEMBL4877442 | — | — | 1 | 5.17 |
| CHEMBL4871577 | — | — | 1 | 5.16 |
| CHEMBL4861482 | — | — | 1 | 5.14 |
| CHEMBL4851040 | — | — | 1 | 4.99 |
| CHEMBL4878922 | — | — | 1 | 4.81 |
| CHEMBL4849344 | — | — | 1 | 4.64 |
| CHEMBL4850501 | — | — | 1 | 4.54 |
| CHEMBL4869531 | — | — | 1 | 4.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.09 | nM | 10.05 |
| CHEMBL438402 | — | EC50 | = | 0.64 | nM | 9.19 |
| CHEMBL264190 | — | EC50 | = | 13.4 | nM | 7.87 |
| CHEMBL342954 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4846261 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4877184 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4877232 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4868636 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4856877 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4848322 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4863206 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4868223 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4845842 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4878558 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4849626 | — | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4872932 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4866532 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4877537 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4869669 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4847357 | — | EC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL4856539 | — | EC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4877442 | — | EC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4871577 | — | EC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL4861482 | — | EC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL4851040 | — | EC50 | = | 10220.0 | nM | 4.99 |
| CHEMBL4878922 | — | EC50 | = | 15500.0 | nM | 4.81 |
| CHEMBL4849344 | — | EC50 | = | 22900.0 | nM | 4.64 |
| CHEMBL4850501 | — | EC50 | = | 29100.0 | nM | 4.54 |
| CHEMBL4869531 | — | EC50 | = | 47800.0 | nM | 4.32 |