Assay Detail
Functional
CHEMBL888239
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 24 | 7.34 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL250516 | — | — | 1 | 9.00 |
| CHEMBL249489 | — | — | 1 | 8.10 |
| CHEMBL250540 | — | — | 1 | 7.60 |
| CHEMBL399721 | — | — | 1 | 7.46 |
| CHEMBL248694 | — | — | 1 | 7.38 |
| CHEMBL400298 | — | — | 1 | 7.23 |
| CHEMBL251701 | — | — | 1 | 7.08 |
| CHEMBL251290 | — | — | 1 | 7.07 |
| CHEMBL399367 | — | — | 1 | 7.05 |
| CHEMBL399244 | — | — | 1 | 7.01 |
| CHEMBL248673 | — | — | 1 | 6.93 |
| CHEMBL248863 | — | — | 1 | 6.90 |
| CHEMBL250927 | — | — | 1 | 6.63 |
| CHEMBL250541 | — | — | 1 | - |
| CHEMBL250544 | — | — | 1 | - |
| CHEMBL250746 | — | — | 1 | - |
| CHEMBL400321 | — | — | 1 | - |
| CHEMBL399312 | — | — | 1 | - |
| CHEMBL250311 | — | — | 1 | - |
| CHEMBL248881 | — | — | 1 | - |
| CHEMBL399712 | — | — | 1 | - |
| CHEMBL399734 | — | — | 1 | - |
| CHEMBL251702 | — | — | 1 | - |
| CHEMBL398748 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL250516 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL249489 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL250540 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL399721 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL248694 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL400298 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL251701 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL251290 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL399367 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL399244 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL248673 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL248863 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL250927 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL250541 | — | IC50 | - | — | - | |
| CHEMBL250544 | — | IC50 | - | — | - | |
| CHEMBL250746 | — | IC50 | - | — | - | |
| CHEMBL400321 | — | IC50 | - | — | - | |
| CHEMBL399312 | — | IC50 | - | — | - | |
| CHEMBL250311 | — | IC50 | - | — | - | |
| CHEMBL248881 | — | IC50 | - | — | - | |
| CHEMBL399712 | — | IC50 | - | — | - | |
| CHEMBL399734 | — | IC50 | - | — | - | |
| CHEMBL251702 | — | IC50 | - | — | - | |
| CHEMBL398748 | — | IC50 | - | — | - |