Assay Detail
Functional
CHEMBL691187
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 8.24 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.15 |
| CHEMBL432565 | — | — | 1 | 9.30 |
| CHEMBL406276 | — | — | 1 | 8.70 |
| CHEMBL419307 | — | — | 1 | 8.70 |
| CHEMBL89004 | — | — | 1 | 8.70 |
| CHEMBL329586 | — | — | 1 | 8.46 |
| CHEMBL264306 | — | — | 1 | 8.35 |
| CHEMBL315356 | — | — | 1 | 8.30 |
| CHEMBL86573 | — | — | 1 | 8.19 |
| CHEMBL316259 | — | — | 1 | 8.17 |
| CHEMBL328117 | — | — | 1 | 8.15 |
| CHEMBL316038 | — | — | 1 | 8.15 |
| CHEMBL313377 | — | — | 1 | 8.15 |
| CHEMBL407825 | — | — | 1 | 8.12 |
| CHEMBL312998 | — | — | 1 | 8.10 |
| CHEMBL88630 | — | — | 1 | 8.10 |
| CHEMBL327450 | — | — | 1 | 8.05 |
| CHEMBL315258 | — | — | 1 | 8.02 |
| CHEMBL92481 | — | — | 1 | 8.02 |
| CHEMBL50056 | — | — | 1 | 7.89 |
| CHEMBL88537 | — | — | 1 | 7.86 |
| CHEMBL89270 | — | — | 1 | 7.50 |
| CHEMBL91957 | — | — | 1 | 7.48 |
| CHEMBL88185 | — | — | 1 | 7.06 |
| CHEMBL431801 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.07 | nM | 10.15 |
| CHEMBL432565 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL406276 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL419307 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL89004 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL329586 | — | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL264306 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL315356 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL86573 | — | EC50 | = | 6.5 | nM | 8.19 |
| CHEMBL316259 | — | EC50 | = | 6.8 | nM | 8.17 |
| CHEMBL328117 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL316038 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL313377 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL407825 | — | EC50 | = | 7.5 | nM | 8.12 |
| CHEMBL312998 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL88630 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL327450 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL315258 | — | EC50 | = | 9.5 | nM | 8.02 |
| CHEMBL92481 | — | EC50 | = | 9.5 | nM | 8.02 |
| CHEMBL50056 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL88537 | — | EC50 | = | 13.7 | nM | 7.86 |
| CHEMBL89270 | — | EC50 | = | 31.8 | nM | 7.50 |
| CHEMBL91957 | — | EC50 | = | 33.3 | nM | 7.48 |
| CHEMBL88185 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL431801 | — | EC50 | = | 0.009 | nM | - |