Assay Detail
Functional
CHEMBL5320169
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Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Flp-In-293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Targeting Melanocortin Receptors Using S<sub><i>N</i></sub>Ar-Type Macrocyclization: A Doubly Orthogonal Route to Cyclic Peptide Conjugates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 8.43 | 9.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5414451 | — | — | 1 | 9.87 |
| CHEMBL430239 | MELATONAN | — | 1 | 9.70 |
| CHEMBL5432868 | — | — | 1 | 9.56 |
| CHEMBL5399539 | — | — | 1 | 9.35 |
| CHEMBL5398659 | — | — | 1 | 9.30 |
| CHEMBL5416095 | — | — | 2 | 9.01 |
| CHEMBL5421885 | — | — | 1 | 9.00 |
| CHEMBL5426684 | — | — | 1 | 8.80 |
| CHEMBL5421108 | — | — | 1 | 8.30 |
| CHEMBL5432664 | — | — | 1 | 8.20 |
| CHEMBL5405038 | — | — | 1 | 7.70 |
| CHEMBL5438253 | — | — | 1 | 7.20 |
| CHEMBL5413092 | — | — | 1 | 7.05 |
| CHEMBL5438629 | — | — | 1 | 6.50 |
| CHEMBL504986 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5414451 | — | EC50 | = | 0.1349 | nM | 9.87 |
| CHEMBL430239 | MELATONAN | EC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL5432868 | — | EC50 | = | 0.2754 | nM | 9.56 |
| CHEMBL5399539 | — | EC50 | = | 0.4467 | nM | 9.35 |
| CHEMBL5398659 | — | EC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL5416095 | — | EC50 | = | 0.98 | nM | 9.01 |
| CHEMBL5421885 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5416095 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5426684 | — | EC50 | = | 1.585 | nM | 8.80 |
| CHEMBL5421108 | — | EC50 | = | 5.012 | nM | 8.30 |
| CHEMBL5432664 | — | EC50 | = | 6.31 | nM | 8.20 |
| CHEMBL5405038 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5438253 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5413092 | — | EC50 | = | 89.13 | nM | 7.05 |
| CHEMBL5438629 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL504986 | — | EC50 | = | 501.19 | nM | 6.30 |