Assay Detail
Functional
CHEMBL4309181
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Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 8.98 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4460053 | — | — | 1 | 10.52 |
| CHEMBL4569789 | — | — | 1 | 10.22 |
| CHEMBL3798421 | — | — | 1 | 9.24 |
| CHEMBL3797690 | — | — | 1 | 9.17 |
| CHEMBL4518266 | — | — | 1 | 9.02 |
| CHEMBL3799094 | — | — | 1 | 8.96 |
| CHEMBL3799955 | — | — | 1 | 8.92 |
| CHEMBL264190 | — | — | 1 | 8.74 |
| CHEMBL4466007 | — | — | 1 | 8.72 |
| CHEMBL4573190 | — | — | 1 | 8.72 |
| CHEMBL3799563 | — | — | 1 | 8.70 |
| CHEMBL4569886 | — | — | 1 | 8.33 |
| CHEMBL3798845 | — | — | 1 | 8.26 |
| CHEMBL4467240 | — | — | 1 | 8.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4460053 | — | EC50 | = | 0.03 | nM | 10.52 |
| CHEMBL4569789 | — | EC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3798421 | — | EC50 | = | 0.57 | nM | 9.24 |
| CHEMBL3797690 | — | EC50 | = | 0.67 | nM | 9.17 |
| CHEMBL4518266 | — | EC50 | = | 0.95 | nM | 9.02 |
| CHEMBL3799094 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3799955 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL264190 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4466007 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4573190 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3799563 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4569886 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3798845 | — | EC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4467240 | — | EC50 | = | 5.9 | nM | 8.23 |