Assay Detail
Functional
CHEMBL3803380
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Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
11
Total Activities
11
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
An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 7.83 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.62 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 9.12 |
| CHEMBL3798421 | — | — | 1 | 8.00 |
| CHEMBL4299619 | — | — | 1 | 7.70 |
| CHEMBL3799955 | — | — | 1 | 7.64 |
| CHEMBL3799094 | — | — | 1 | 7.57 |
| CHEMBL3799563 | — | — | 1 | 7.51 |
| CHEMBL405282 | — | — | 1 | 7.46 |
| CHEMBL3797690 | — | — | 1 | 7.32 |
| CHEMBL264190 | — | — | 1 | 7.26 |
| CHEMBL4299612 | — | — | 1 | 6.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.24 | nM | 9.62 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.76 | nM | 9.12 |
| CHEMBL3798421 | — | EC50 | = | 10.1 | nM | 8.00 |
| CHEMBL4299619 | — | EC50 | = | 20.2 | nM | 7.70 |
| CHEMBL3799955 | — | EC50 | = | 22.7 | nM | 7.64 |
| CHEMBL3799094 | — | EC50 | = | 27.2 | nM | 7.57 |
| CHEMBL3799563 | — | EC50 | = | 30.9 | nM | 7.51 |
| CHEMBL405282 | — | EC50 | = | 34.6 | nM | 7.46 |
| CHEMBL3797690 | — | EC50 | = | 47.4 | nM | 7.32 |
| CHEMBL264190 | — | EC50 | = | 55.5 | nM | 7.26 |
| CHEMBL4299612 | — | EC50 | = | 107.0 | nM | 6.97 |