Assay Detail
Functional
CHEMBL3803379
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
15
Total Activities
15
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 |
Target
Melanocyte-stimulating hormone receptor (CHEMBL4077) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 15 | 7.79 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.52 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 9.82 |
| CHEMBL4299619 | — | — | 1 | 8.36 |
| CHEMBL4299612 | — | — | 1 | 8.24 |
| CHEMBL3798421 | — | — | 1 | 8.19 |
| CHEMBL3799955 | — | — | 1 | 7.90 |
| CHEMBL264190 | — | — | 1 | 7.85 |
| CHEMBL3799094 | — | — | 1 | 7.79 |
| CHEMBL3799563 | — | — | 1 | 7.60 |
| CHEMBL3797690 | — | — | 1 | 7.58 |
| CHEMBL103817 | — | — | 1 | 7.01 |
| CHEMBL3799408 | — | — | 1 | 6.95 |
| CHEMBL3798912 | — | — | 1 | 6.86 |
| CHEMBL3798768 | — | — | 1 | 6.25 |
| CHEMBL405282 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.03 | nM | 10.52 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.15 | nM | 9.82 |
| CHEMBL4299619 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4299612 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3798421 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL3799955 | — | EC50 | = | 12.6 | nM | 7.90 |
| CHEMBL264190 | — | EC50 | = | 14.1 | nM | 7.85 |
| CHEMBL3799094 | — | EC50 | = | 16.4 | nM | 7.79 |
| CHEMBL3799563 | — | EC50 | = | 24.9 | nM | 7.60 |
| CHEMBL3797690 | — | EC50 | = | 26.2 | nM | 7.58 |
| CHEMBL103817 | — | EC50 | = | 98.4 | nM | 7.01 |
| CHEMBL3799408 | — | EC50 | = | 112.0 | nM | 6.95 |
| CHEMBL3798912 | — | EC50 | = | 139.0 | nM | 6.86 |
| CHEMBL3798768 | — | EC50 | = | 563.0 | nM | 6.25 |
| CHEMBL405282 | — | EC50 | = | 1090.0 | nM | 5.96 |