Assay Detail
Binding
CHEMBL1105741
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Inhibition of cannabinoid CB1 receptor
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.74 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL220360 | TARANABANT | 3.0 | 1 | 9.52 |
| CHEMBL1092169 | — | — | 1 | 8.37 |
| CHEMBL1094521 | — | — | 1 | 8.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL220360 | TARANABANT | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1092169 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1094521 | — | IC50 | = | 4.8 | nM | 8.32 |