Assay Detail
Binding
CHEMBL3803372
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Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| IC50 | 13 | 7.37 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 8.96 |
| CHEMBL3798421 | — | — | 1 | 8.00 |
| CHEMBL3798768 | — | — | 1 | 7.98 |
| CHEMBL3799408 | — | — | 1 | 7.97 |
| CHEMBL3798912 | — | — | 1 | 7.66 |
| CHEMBL103817 | — | — | 1 | 7.58 |
| CHEMBL4299619 | — | — | 1 | 7.48 |
| CHEMBL3799955 | — | — | 1 | 7.27 |
| CHEMBL3797690 | — | — | 1 | 7.08 |
| CHEMBL264190 | — | — | 1 | 6.67 |
| CHEMBL3799094 | — | — | 1 | 6.59 |
| CHEMBL3799563 | — | — | 1 | 6.54 |
| CHEMBL4299612 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | IC50 | = | 1.09 | nM | 8.96 |
| CHEMBL3798421 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL3798768 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL3799408 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL3798912 | — | IC50 | = | 21.8 | nM | 7.66 |
| CHEMBL103817 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4299619 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3799955 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3797690 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL264190 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL3799094 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL3799563 | — | IC50 | = | 292.0 | nM | 6.54 |
| CHEMBL4299612 | — | IC50 | = | 841.0 | nM | 6.08 |