Assay Detail
Functional
CHEMBL4344904
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Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
16
Total Activities
16
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 | 16 | 6.76 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 8.96 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 8.43 |
| CHEMBL264190 | — | — | 1 | 7.68 |
| CHEMBL3287060 | — | — | 1 | 7.05 |
| CHEMBL4590532 | — | — | 1 | 6.57 |
| CHEMBL4465466 | — | — | 1 | 6.30 |
| CHEMBL320157 | — | — | 1 | 6.00 |
| CHEMBL50056 | — | — | 1 | 5.68 |
| CHEMBL4574756 | — | — | 1 | 5.51 |
| CHEMBL4437801 | — | — | 1 | 5.42 |
| CHEMBL4554278 | — | — | 1 | - |
| CHEMBL4513953 | — | — | 1 | - |
| CHEMBL4582657 | — | — | 1 | - |
| CHEMBL4590028 | — | — | 1 | - |
| CHEMBL4587259 | — | — | 1 | - |
| CHEMBL4558851 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL264190 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3287060 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4590532 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4465466 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL320157 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL50056 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4574756 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4437801 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4554278 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4513953 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4582657 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4590028 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4587259 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4558851 | — | EC50 | > | 100000.0 | nM | - |