Assay Detail
Functional
CHEMBL4344901
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Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
12
Total Activities
12
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
Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 6.78 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.72 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 9.66 |
| CHEMBL320157 | — | — | 1 | 7.00 |
| CHEMBL4590532 | — | — | 1 | 5.89 |
| CHEMBL50056 | — | — | 1 | 5.82 |
| CHEMBL3287060 | — | — | 1 | 5.52 |
| CHEMBL4465466 | — | — | 1 | 5.40 |
| CHEMBL4574756 | — | — | 1 | 5.22 |
| CHEMBL4554278 | — | — | 1 | - |
| CHEMBL4582657 | — | — | 1 | - |
| CHEMBL4587259 | — | — | 1 | - |
| CHEMBL4558851 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.19 | nM | 9.72 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.22 | nM | 9.66 |
| CHEMBL320157 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4590532 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL50056 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3287060 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4465466 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4574756 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4554278 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4582657 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4587259 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4558851 | — | EC50 | > | 100000.0 | nM | - |