Assay Detail
Binding
CHEMBL719018
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards human Melanocortin 1 receptor (hMC1R)
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 25 | 7.51 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.30 |
| CHEMBL92481 | — | — | 1 | 8.46 |
| CHEMBL432565 | — | — | 1 | 8.22 |
| CHEMBL419307 | — | — | 1 | 8.22 |
| CHEMBL312998 | — | — | 1 | 7.94 |
| CHEMBL89004 | — | — | 1 | 7.76 |
| CHEMBL406276 | — | — | 1 | 7.69 |
| CHEMBL316259 | — | — | 1 | 7.52 |
| CHEMBL88537 | — | — | 1 | 7.47 |
| CHEMBL50056 | — | — | 1 | 7.43 |
| CHEMBL264306 | — | — | 1 | 7.43 |
| CHEMBL313377 | — | — | 1 | 7.40 |
| CHEMBL315356 | — | — | 1 | 7.37 |
| CHEMBL329586 | — | — | 1 | 7.37 |
| CHEMBL407825 | — | — | 1 | 7.32 |
| CHEMBL89270 | — | — | 1 | 7.29 |
| CHEMBL327450 | — | — | 1 | 7.24 |
| CHEMBL328117 | — | — | 1 | 7.21 |
| CHEMBL86573 | — | — | 1 | 7.20 |
| CHEMBL88630 | — | — | 1 | 7.06 |
| CHEMBL315258 | — | — | 1 | 7.04 |
| CHEMBL316038 | — | — | 1 | 6.90 |
| CHEMBL91957 | — | — | 1 | 6.77 |
| CHEMBL88185 | — | — | 1 | 6.58 |
| CHEMBL431801 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL92481 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL432565 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL419307 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL312998 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL89004 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL406276 | — | Ki | = | 20.5 | nM | 7.69 |
| CHEMBL316259 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL88537 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL50056 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL264306 | — | Ki | = | 37.5 | nM | 7.43 |
| CHEMBL313377 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL315356 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL329586 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL407825 | — | Ki | = | 47.5 | nM | 7.32 |
| CHEMBL89270 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL327450 | — | Ki | = | 57.5 | nM | 7.24 |
| CHEMBL328117 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL86573 | — | Ki | = | 63.5 | nM | 7.20 |
| CHEMBL88630 | — | Ki | = | 86.5 | nM | 7.06 |
| CHEMBL315258 | — | Ki | = | 91.5 | nM | 7.04 |
| CHEMBL316038 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL91957 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL88185 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL431801 | — | Ki | = | 0.006 | nM | - |