Assay Detail
Functional
CHEMBL2073121
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Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | BHK570 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 8.40 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2070245 | — | — | 1 | 10.40 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.85 |
| CHEMBL2070246 | — | — | 1 | 9.82 |
| CHEMBL2070243 | — | — | 1 | 9.77 |
| CHEMBL2070241 | BREMELANOTIDE | 4.0 | 1 | 9.70 |
| CHEMBL2070244 | — | — | 1 | 9.33 |
| CHEMBL2070248 | — | — | 1 | 9.00 |
| CHEMBL2070242 | — | — | 1 | 8.70 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 8.47 |
| CHEMBL2070251 | — | — | 1 | 8.33 |
| CHEMBL2070252 | — | — | 1 | 7.82 |
| CHEMBL2070249 | — | — | 1 | 7.21 |
| CHEMBL2070250 | — | — | 1 | 7.07 |
| CHEMBL2070374 | — | — | 1 | 7.06 |
| CHEMBL2069317 | — | — | 1 | 6.89 |
| CHEMBL2070247 | — | — | 1 | 6.77 |
| CHEMBL2070254 | — | — | 1 | 6.57 |
| CHEMBL2070253 | — | — | 1 | - |
| CHEMBL2070373 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2070245 | — | EC50 | = | 0.04 | nM | 10.40 |
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.14 | nM | 9.85 |
| CHEMBL2070246 | — | EC50 | = | 0.15 | nM | 9.82 |
| CHEMBL2070243 | — | EC50 | = | 0.17 | nM | 9.77 |
| CHEMBL2070241 | BREMELANOTIDE | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL2070244 | — | EC50 | = | 0.47 | nM | 9.33 |
| CHEMBL2070248 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2070242 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL2070251 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL2070252 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2070249 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL2070250 | — | EC50 | = | 85.0 | nM | 7.07 |
| CHEMBL2070374 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL2069317 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2070247 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2070254 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2070253 | — | EC50 | - | — | - | |
| CHEMBL2070373 | — | EC50 | - | — | - |