Assay Detail
Binding
CHEMBL869276
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Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 57 | 6.30 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL215659 | — | — | 1 | 7.89 |
| CHEMBL212192 | — | — | 1 | 7.75 |
| CHEMBL211564 | — | — | 1 | 7.72 |
| CHEMBL215601 | — | — | 1 | 7.60 |
| CHEMBL384636 | — | — | 1 | 7.52 |
| CHEMBL212897 | — | — | 1 | 7.25 |
| CHEMBL379625 | — | — | 1 | 7.24 |
| CHEMBL214217 | — | — | 1 | 7.19 |
| CHEMBL213738 | — | — | 1 | 7.13 |
| CHEMBL213691 | — | — | 1 | 7.12 |
| CHEMBL215886 | — | — | 1 | 7.07 |
| CHEMBL209954 | — | — | 1 | 7.05 |
| CHEMBL214000 | — | — | 1 | 7.04 |
| CHEMBL213381 | — | — | 1 | 7.03 |
| CHEMBL213380 | — | — | 1 | 6.96 |
| CHEMBL213264 | — | — | 1 | 6.96 |
| CHEMBL215851 | — | — | 1 | 6.85 |
| CHEMBL213739 | — | — | 1 | 6.80 |
| CHEMBL377480 | — | — | 1 | 6.77 |
| CHEMBL215974 | — | — | 1 | 6.72 |
| CHEMBL213953 | — | — | 1 | 6.68 |
| CHEMBL214204 | — | — | 1 | 6.52 |
| CHEMBL213041 | — | — | 1 | 6.46 |
| CHEMBL212303 | — | — | 1 | 6.44 |
| CHEMBL214988 | — | — | 1 | 6.40 |
| CHEMBL384138 | — | — | 1 | 6.31 |
| CHEMBL378397 | — | — | 1 | 6.21 |
| CHEMBL384389 | — | — | 1 | 6.19 |
| CHEMBL212889 | — | — | 1 | 6.16 |
| CHEMBL215741 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL215659 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL212192 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL211564 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL215601 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL384636 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL212897 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL379625 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL214217 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL213738 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL213691 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL215886 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL209954 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL214000 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL213381 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL213264 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL213380 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL215851 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL213739 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL377480 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL215974 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL213953 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL214204 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL213041 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL212303 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL214988 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL384138 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL378397 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL384389 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL212889 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL215741 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL212653 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL379792 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL215697 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL378016 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL438793 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL212553 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL215712 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL384040 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL213776 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL209869 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL213935 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL214537 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL209682 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL385437 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL215646 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL211462 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL213389 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL384390 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL384965 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL386868 | — | Ki | = | 4000.0 | nM | 5.40 |