Assay Detail
Functional
CHEMBL4835804
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
39
Total Activities
39
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 |
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 | 39 | 6.44 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL342954 | — | — | 1 | 9.31 |
| CHEMBL438402 | — | — | 1 | 9.15 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 8.59 |
| CHEMBL264190 | — | — | 1 | 8.38 |
| CHEMBL4868636 | — | — | 1 | 6.85 |
| CHEMBL4848322 | — | — | 1 | 6.82 |
| CHEMBL4868223 | — | — | 1 | 6.75 |
| CHEMBL4863206 | — | — | 1 | 6.47 |
| CHEMBL4877184 | — | — | 1 | 6.42 |
| CHEMBL4878922 | — | — | 1 | 6.36 |
| CHEMBL4858724 | — | — | 1 | 6.33 |
| CHEMBL4863711 | — | — | 1 | 6.32 |
| CHEMBL4872932 | — | — | 1 | 6.31 |
| CHEMBL4849626 | — | — | 1 | 6.30 |
| CHEMBL4877232 | — | — | 1 | 6.29 |
| CHEMBL4864094 | — | — | 1 | 6.28 |
| CHEMBL4845842 | — | — | 1 | 6.28 |
| CHEMBL4862172 | — | — | 1 | 6.27 |
| CHEMBL4866151 | — | — | 1 | 6.25 |
| CHEMBL4856539 | — | — | 1 | 6.25 |
| CHEMBL4856877 | — | — | 1 | 6.24 |
| CHEMBL4878558 | — | — | 1 | 6.23 |
| CHEMBL4846261 | — | — | 1 | 6.22 |
| CHEMBL4850501 | — | — | 1 | 6.22 |
| CHEMBL4871577 | — | — | 1 | 6.21 |
| CHEMBL4861482 | — | — | 1 | 6.20 |
| CHEMBL4869531 | — | — | 1 | 6.18 |
| CHEMBL4866532 | — | — | 1 | 6.13 |
| CHEMBL4878201 | — | — | 1 | 6.09 |
| CHEMBL4869669 | — | — | 1 | 6.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL342954 | — | EC50 | = | 0.49 | nM | 9.31 |
| CHEMBL438402 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL264190 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4868636 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4848322 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4868223 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4863206 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4877184 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4878922 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4858724 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4863711 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4872932 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4849626 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4877232 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4864094 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4845842 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4862172 | — | EC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4856539 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4866151 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4856877 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4878558 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4846261 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4850501 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4871577 | — | EC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4861482 | — | EC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4869531 | — | EC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4866532 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4878201 | — | EC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4869669 | — | EC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4867949 | — | EC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL4864765 | — | EC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL4851040 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4847357 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4877537 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4848447 | — | EC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL4849344 | — | EC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL4863313 | — | EC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL4877442 | — | EC50 | = | 6600.0 | nM | 5.18 |