Assay Detail
Binding
CHEMBL888238
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Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
49
Total Activities
49
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 | Intermediate |
Target
Melanin-concentrating hormone receptor 1 (CHEMBL344) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 7.03 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL250516 | — | — | 1 | 10.00 |
| CHEMBL400883 | — | — | 1 | 8.52 |
| CHEMBL399721 | — | — | 1 | 8.30 |
| CHEMBL400298 | — | — | 1 | 8.15 |
| CHEMBL251290 | — | — | 1 | 8.05 |
| CHEMBL249489 | — | — | 1 | 8.05 |
| CHEMBL250327 | — | — | 1 | 8.00 |
| CHEMBL250123 | — | — | 1 | 7.89 |
| CHEMBL400679 | — | — | 1 | 7.82 |
| CHEMBL250124 | — | — | 1 | 7.82 |
| CHEMBL249716 | — | — | 1 | 7.80 |
| CHEMBL248863 | — | — | 1 | 7.70 |
| CHEMBL250530 | — | — | 1 | 7.66 |
| CHEMBL399367 | — | — | 1 | 7.58 |
| CHEMBL250326 | — | — | 1 | 7.55 |
| CHEMBL399244 | — | — | 1 | 7.54 |
| CHEMBL251701 | — | — | 1 | 7.54 |
| CHEMBL248673 | — | — | 1 | 7.48 |
| CHEMBL398864 | — | — | 1 | 7.46 |
| CHEMBL398748 | — | — | 1 | 7.41 |
| CHEMBL398964 | — | — | 1 | 7.30 |
| CHEMBL248694 | — | — | 1 | 7.27 |
| CHEMBL250540 | — | — | 1 | 7.24 |
| CHEMBL249714 | — | — | 1 | 7.24 |
| CHEMBL250526 | — | — | 1 | 7.21 |
| CHEMBL400799 | — | — | 1 | 7.21 |
| CHEMBL250927 | — | — | 1 | 7.17 |
| CHEMBL251702 | — | — | 1 | 7.15 |
| CHEMBL399734 | — | — | 1 | 7.10 |
| CHEMBL250122 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL250516 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL400883 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL399721 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL400298 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL251290 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL249489 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL250327 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL250123 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL400679 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL250124 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL249716 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL248863 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL250530 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL399367 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL250326 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL399244 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL251701 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL248673 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL398864 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL398748 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL398964 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL248694 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL250540 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL249714 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL250526 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL400799 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL250927 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL251702 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL399734 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL250122 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL250728 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL250729 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL429301 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL250311 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL250528 | — | IC50 | = | 369.0 | nM | 6.43 |
| CHEMBL250321 | — | IC50 | = | 411.0 | nM | 6.39 |
| CHEMBL250541 | — | IC50 | = | 571.0 | nM | 6.24 |
| CHEMBL250544 | — | IC50 | = | 847.0 | nM | 6.07 |
| CHEMBL248881 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL250926 | — | IC50 | = | 2130.0 | nM | 5.67 |
| CHEMBL250730 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL250746 | — | IC50 | = | 2520.0 | nM | 5.60 |
| CHEMBL400297 | — | IC50 | = | 2990.0 | nM | 5.52 |
| CHEMBL250118 | — | IC50 | = | 3590.0 | nM | 5.45 |
| CHEMBL400321 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL250527 | — | IC50 | = | 5010.0 | nM | 5.30 |
| CHEMBL399712 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL399312 | — | IC50 | = | 9920.0 | nM | 5.00 |
| CHEMBL250319 | — | IC50 | > | 33000.0 | nM | - |