Assay Detail
Functional
CHEMBL4151408
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
20
Total Activities
20
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 |
Publication
Synergistic Multiresidue Substitutions of a Macrocyclic c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Agouti-Related Protein (AGRP) Scaffold Yield Potent and >600-Fold MC4R versus MC3R Selective Melanocortin Receptor Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 20 | 8.92 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4166449 | — | — | 1 | 9.60 |
| CHEMBL4163787 | — | — | 1 | 9.50 |
| CHEMBL4164111 | — | — | 1 | 9.50 |
| CHEMBL4174761 | — | — | 1 | 9.20 |
| CHEMBL4166050 | — | — | 1 | 9.20 |
| CHEMBL4162603 | — | — | 1 | 9.10 |
| CHEMBL4173301 | — | — | 1 | 9.10 |
| CHEMBL4172753 | — | — | 1 | 9.10 |
| CHEMBL4169872 | — | — | 1 | 9.10 |
| CHEMBL4164846 | — | — | 1 | 9.10 |
| CHEMBL4170160 | — | — | 1 | 9.00 |
| CHEMBL4159229 | — | — | 1 | 9.00 |
| CHEMBL4175108 | — | — | 1 | 8.90 |
| CHEMBL4171666 | — | — | 1 | 8.80 |
| CHEMBL4167239 | — | — | 1 | 8.80 |
| CHEMBL4176668 | — | — | 1 | 8.60 |
| CHEMBL4174361 | — | — | 1 | 8.60 |
| CHEMBL4159541 | — | — | 1 | 8.50 |
| CHEMBL4168324 | — | — | 1 | 6.80 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4166449 | — | Kd | = | 0.2512 | nM | 9.60 |
| CHEMBL4163787 | — | Kd | = | 0.3162 | nM | 9.50 |
| CHEMBL4164111 | — | Kd | = | 0.3162 | nM | 9.50 |
| CHEMBL4174761 | — | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL4166050 | — | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL4162603 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL4173301 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL4172753 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL4169872 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL4164846 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL4170160 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL4159229 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL4175108 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL4171666 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL4167239 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL4176668 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL4174361 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL4159541 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL4168324 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL441738 | AFAMELANOTIDE | Kd | = | 229086765.28 | nM | - |