Assay Detail
Binding
CHEMBL863666
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Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells
44
Total Activities
44
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
Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 44 | 6.66 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL206364 | — | — | 1 | 8.80 |
| CHEMBL365597 | — | — | 1 | 8.74 |
| CHEMBL195071 | — | — | 1 | 8.62 |
| CHEMBL364560 | — | — | 1 | 8.38 |
| CHEMBL378046 | — | — | 1 | 8.17 |
| CHEMBL208860 | — | — | 1 | 8.06 |
| CHEMBL211742 | — | — | 1 | 8.00 |
| CHEMBL378866 | — | — | 1 | 7.92 |
| CHEMBL439168 | — | — | 1 | 7.82 |
| CHEMBL380222 | — | — | 1 | 7.68 |
| CHEMBL188432 | — | — | 1 | 7.44 |
| CHEMBL379417 | — | — | 1 | 7.06 |
| CHEMBL379400 | — | — | 1 | 6.89 |
| CHEMBL212358 | — | — | 1 | 6.77 |
| CHEMBL212308 | — | — | 1 | 6.75 |
| CHEMBL377258 | — | — | 1 | 6.70 |
| CHEMBL185934 | — | — | 1 | 6.60 |
| CHEMBL448475 | — | — | 1 | 6.51 |
| CHEMBL211279 | — | — | 1 | 6.44 |
| CHEMBL210600 | — | — | 1 | 6.38 |
| CHEMBL211680 | — | — | 1 | 6.36 |
| CHEMBL377762 | — | — | 1 | 6.35 |
| CHEMBL377186 | — | — | 1 | 6.32 |
| CHEMBL208553 | — | — | 1 | 6.28 |
| CHEMBL376973 | — | — | 1 | 6.26 |
| CHEMBL377269 | — | — | 1 | 6.25 |
| CHEMBL208552 | — | — | 1 | 6.15 |
| CHEMBL212325 | — | — | 1 | 6.15 |
| CHEMBL208694 | — | — | 1 | 6.12 |
| CHEMBL211280 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL206364 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL365597 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL195071 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL364560 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL378046 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL208860 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL211742 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL378866 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL439168 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL380222 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL188432 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL379417 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL379400 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL212358 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL212308 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL377258 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL185934 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL448475 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL211279 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL210600 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL211680 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL377762 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL377186 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL208553 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL376973 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL377269 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL208552 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL212325 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL208694 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL211280 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL211366 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL211364 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL378105 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL211540 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL207166 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL376974 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL382353 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL377761 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL378412 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL379091 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL441532 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL210450 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL208679 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL211187 | — | Ki | = | 2800.0 | nM | 5.55 |