Assay Detail
Functional
CHEMBL5107060
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
31
Total Activities
31
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK2936E |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 26 | 8.63 | 10.21 |
| pEC50 | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | — | 1 | 10.21 |
| CHEMBL5185775 | — | — | 1 | 9.98 |
| CHEMBL5185945 | — | — | 1 | 9.97 |
| CHEMBL3301624 | SETMELANOTIDE | 4.0 | 1 | 9.82 |
| CHEMBL5172738 | — | — | 1 | 9.80 |
| CHEMBL5191309 | — | — | 1 | 9.74 |
| CHEMBL5195641 | — | — | 1 | 9.64 |
| CHEMBL5178164 | — | — | 1 | 9.56 |
| CHEMBL5170533 | — | — | 1 | 9.52 |
| CHEMBL5175487 | — | — | 1 | 9.51 |
| CHEMBL5203986 | — | — | 1 | 9.48 |
| CHEMBL5192329 | — | — | 1 | 9.46 |
| CHEMBL5185405 | — | — | 1 | 9.40 |
| CHEMBL5207936 | — | — | 1 | 9.22 |
| CHEMBL2070241 | BREMELANOTIDE | 4.0 | 1 | 9.17 |
| CHEMBL5190042 | — | — | 1 | 9.16 |
| CHEMBL5179081 | — | — | 1 | 9.02 |
| CHEMBL5187932 | — | — | 1 | 8.59 |
| CHEMBL5199932 | — | — | 1 | 7.40 |
| CHEMBL5177494 | — | — | 1 | 6.79 |
| CHEMBL5182345 | — | — | 1 | 6.72 |
| CHEMBL5175444 | — | — | 1 | 6.71 |
| CHEMBL5208830 | — | — | 1 | 6.53 |
| CHEMBL5196407 | — | — | 1 | 6.42 |
| CHEMBL5195937 | — | — | 1 | 6.34 |
| CHEMBL5181752 | — | — | 1 | 6.30 |
| CHEMBL5175981 | — | — | 1 | - |
| CHEMBL5179373 | — | — | 1 | - |
| CHEMBL5204285 | — | — | 1 | - |
| CHEMBL5181812 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | EC50 | = | 0.06166 | nM | 10.21 |
| CHEMBL5185775 | — | EC50 | = | 0.1047 | nM | 9.98 |
| CHEMBL5185945 | — | EC50 | = | 0.1072 | nM | 9.97 |
| CHEMBL3301624 | SETMELANOTIDE | EC50 | = | 0.1514 | nM | 9.82 |
| CHEMBL5172738 | — | EC50 | = | 0.1585 | nM | 9.80 |
| CHEMBL5191309 | — | EC50 | = | 0.182 | nM | 9.74 |
| CHEMBL5195641 | — | EC50 | = | 0.2291 | nM | 9.64 |
| CHEMBL5178164 | — | EC50 | = | 0.2754 | nM | 9.56 |
| CHEMBL5170533 | — | EC50 | = | 0.302 | nM | 9.52 |
| CHEMBL5175487 | — | EC50 | = | 0.309 | nM | 9.51 |
| CHEMBL5203986 | — | EC50 | = | 0.3311 | nM | 9.48 |
| CHEMBL5192329 | — | EC50 | = | 0.3467 | nM | 9.46 |
| CHEMBL5185405 | — | EC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL5207936 | — | EC50 | = | 0.6026 | nM | 9.22 |
| CHEMBL2070241 | BREMELANOTIDE | EC50 | = | 0.6761 | nM | 9.17 |
| CHEMBL5190042 | — | EC50 | = | 0.6918 | nM | 9.16 |
| CHEMBL5179081 | — | EC50 | = | 0.955 | nM | 9.02 |
| CHEMBL5187932 | — | EC50 | = | 2.57 | nM | 8.59 |
| CHEMBL5199932 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5177494 | — | EC50 | = | 162.18 | nM | 6.79 |
| CHEMBL5182345 | — | EC50 | = | 190.55 | nM | 6.72 |
| CHEMBL5175444 | — | EC50 | = | 194.98 | nM | 6.71 |
| CHEMBL5208830 | — | EC50 | = | 295.12 | nM | 6.53 |
| CHEMBL5196407 | — | EC50 | = | 380.19 | nM | 6.42 |
| CHEMBL5195937 | — | EC50 | = | 457.09 | nM | 6.34 |
| CHEMBL5181752 | — | EC50 | = | 501.19 | nM | 6.30 |
| CHEMBL5175981 | — | pEC50 | - | — | - | |
| CHEMBL5179373 | — | pEC50 | - | — | - | |
| CHEMBL5204285 | — | pEC50 | - | — | - | |
| CHEMBL5181812 | — | pEC50 | - | — | - | |
| CHEMBL5176443 | — | pEC50 | - | — | - |