Assay Detail
Binding
CHEMBL829432
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells
45
Total Activities
45
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
Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 45 | 7.06 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL364560 | — | — | 1 | 8.38 |
| CHEMBL363019 | — | — | 1 | 8.12 |
| CHEMBL188651 | — | — | 1 | 8.08 |
| CHEMBL185862 | — | — | 1 | 8.06 |
| CHEMBL365237 | — | — | 1 | 7.96 |
| CHEMBL187659 | — | — | 1 | 7.92 |
| CHEMBL365465 | — | — | 1 | 7.92 |
| CHEMBL187390 | — | — | 1 | 7.75 |
| CHEMBL361693 | — | — | 1 | 7.75 |
| CHEMBL361882 | — | — | 1 | 7.68 |
| CHEMBL187224 | — | — | 1 | 7.66 |
| CHEMBL189004 | — | — | 1 | 7.64 |
| CHEMBL189172 | — | — | 1 | 7.44 |
| CHEMBL188432 | — | — | 1 | 7.44 |
| CHEMBL362158 | — | — | 1 | 7.35 |
| CHEMBL2113035 | — | — | 1 | 7.31 |
| CHEMBL188341 | — | — | 1 | 7.22 |
| CHEMBL361719 | — | — | 1 | 7.21 |
| CHEMBL433555 | — | — | 1 | 7.21 |
| CHEMBL186227 | — | — | 1 | 7.04 |
| CHEMBL366334 | — | — | 1 | 6.96 |
| CHEMBL186370 | — | — | 1 | 6.92 |
| CHEMBL2113033 | — | — | 1 | 6.82 |
| CHEMBL366313 | — | — | 1 | 6.75 |
| CHEMBL189601 | — | — | 1 | 6.72 |
| CHEMBL189032 | — | — | 1 | 6.68 |
| CHEMBL363445 | — | — | 1 | 6.68 |
| CHEMBL187521 | — | — | 1 | 6.66 |
| CHEMBL363239 | — | — | 1 | 6.66 |
| CHEMBL425353 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL364560 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL363019 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL188651 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL185862 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL365237 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL187659 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL365465 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL187390 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL361693 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL361882 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL187224 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL189004 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL189172 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL188432 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL362158 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL2113035 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL188341 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL361719 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL433555 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL186227 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL366334 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL186370 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL2113033 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL366313 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL189601 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL189032 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL363445 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL187521 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL363239 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL425353 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL189341 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL365223 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL185934 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL188980 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL191159 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL186188 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL365491 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL433598 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL187657 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL365893 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL185625 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL187439 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL364772 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL363877 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL413064 | — | Ki | = | 540.0 | nM | 6.27 |