Assay Detail
Functional
CHEMBL5356871
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mouse MC1R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
21
Total Activities
21
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
Discovery of a Pan-Melanocortin Receptor Antagonist [Ac-DPhe(pI)-Arg-Nal(2')-Orn-NH<sub>2</sub>] at the MC1R, MC3R, MC4R, and MC5R that Mediates an Increased Feeding Response in Mice and a 40-Fold Selective MC1R Antagonist [Ac-DPhe(pI)-DArg-Nal(2')-Arg-NH<sub>2</sub>].
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 21 | 6.61 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4865888 | — | — | 1 | 7.70 |
| CHEMBL5405613 | — | — | 1 | 7.30 |
| CHEMBL5421355 | — | — | 1 | 7.20 |
| CHEMBL5435335 | — | — | 1 | 7.10 |
| CHEMBL5397260 | — | — | 1 | 7.00 |
| CHEMBL5438129 | — | — | 1 | 6.70 |
| CHEMBL5406385 | — | — | 1 | 6.70 |
| CHEMBL5419394 | — | — | 1 | 6.70 |
| CHEMBL5417913 | — | — | 1 | 6.60 |
| CHEMBL5413452 | — | — | 1 | 6.60 |
| CHEMBL5408661 | — | — | 1 | 6.50 |
| CHEMBL5414015 | — | — | 1 | 6.50 |
| CHEMBL5403689 | — | — | 1 | 6.50 |
| CHEMBL5421386 | — | — | 1 | 6.40 |
| CHEMBL5397668 | — | — | 1 | 6.20 |
| CHEMBL5409282 | — | — | 1 | 6.20 |
| CHEMBL5413381 | — | — | 1 | 6.20 |
| CHEMBL4866219 | — | — | 1 | 6.20 |
| CHEMBL5413535 | — | — | 1 | 5.90 |
| CHEMBL5397924 | — | — | 1 | 5.90 |
| CHEMBL5396157 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4865888 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL5405613 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL5421355 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL5435335 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL5397260 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL5438129 | — | Kd | = | 199.53 | nM | 6.70 |
| CHEMBL5406385 | — | Kd | = | 199.53 | nM | 6.70 |
| CHEMBL5419394 | — | Kd | = | 199.53 | nM | 6.70 |
| CHEMBL5417913 | — | Kd | = | 251.19 | nM | 6.60 |
| CHEMBL5413452 | — | Kd | = | 251.19 | nM | 6.60 |
| CHEMBL5408661 | — | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL5414015 | — | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL5403689 | — | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL5421386 | — | Kd | = | 398.11 | nM | 6.40 |
| CHEMBL5397668 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL5409282 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL5413381 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL4866219 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL5413535 | — | Kd | = | 1258.93 | nM | 5.90 |
| CHEMBL5397924 | — | Kd | = | 1258.93 | nM | 5.90 |
| CHEMBL5396157 | — | Kd | > | 3162.28 | nM | - |