Assay Detail
Binding
CHEMBL910341
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human MC4R
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.92 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL385000 | — | — | 1 | 9.40 |
| CHEMBL379054 | — | — | 1 | 9.22 |
| CHEMBL212614 | — | — | 1 | 9.10 |
| CHEMBL215833 | — | — | 1 | 8.96 |
| CHEMBL214410 | — | — | 1 | 8.89 |
| CHEMBL384176 | — | — | 1 | 8.89 |
| CHEMBL384774 | — | — | 1 | 8.30 |
| CHEMBL215576 | — | — | 1 | 8.28 |
| CHEMBL211975 | — | — | 1 | 8.24 |
| CHEMBL215895 | — | — | 1 | 8.22 |
| CHEMBL378837 | — | — | 1 | 8.15 |
| CHEMBL213566 | — | — | 1 | 7.96 |
| CHEMBL211699 | — | — | 1 | 7.54 |
| CHEMBL202699 | — | — | 1 | 6.98 |
| CHEMBL214770 | — | — | 1 | 6.72 |
| CHEMBL212332 | — | — | 1 | 6.65 |
| CHEMBL213284 | — | — | 1 | 6.58 |
| CHEMBL212855 | — | — | 1 | 6.44 |
| CHEMBL387246 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL385000 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL379054 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL212614 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL215833 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL214410 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL384176 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL384774 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL215576 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL211975 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL215895 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL378837 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL213566 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL211699 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL202699 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL214770 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL212332 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL213284 | — | Ki | = | 261.0 | nM | 6.58 |
| CHEMBL212855 | — | Ki | = | 365.0 | nM | 6.44 |
| CHEMBL387246 | — | Ki | = | 1248.0 | nM | 5.90 |