Page last updated: 2024-08-05 15:44:51
CB2 receptor antagonist
An antagonist that binds to and deactivates type 2 cannabinoid receptors.
ChEBI ID: 73417
Members (1)
| Member | Definition | Class |
|---|---|---|
| sr 144528 | A secondary carboxamide resulting from the formal condensation of the carboxy group of 5-(4-chloro-3-methylphenyl)-1-(4-methylbenzyl)-1H-pyrazole-3-carboxylic acid with the amino group of (1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]heptan-2-amine. A potent and selective cannabinoid receptor type 2 (CB2 receptor) inverse agonist (Ki = 0.6 nM). | SR 144528 |
Research
Studies (257)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 14 (5.45) | 18.2507 |
| 2000's | 150 (58.37) | 29.6817 |
| 2010's | 81 (31.52) | 24.3611 |
| 2020's | 12 (4.67) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 3 (1.15%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 258 (98.85%) | 84.16% |
Protein Targets (9)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 2.6837 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 1.8999 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 2.6837 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 2.6837 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 2.6837 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 2.6837 | 1 | 1 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cannabinoid receptor 1 | Homo sapiens (human) | IC50 | 271.3472 | 2 | 2 |
| Cannabinoid receptor 1 | Homo sapiens (human) | Ki | 9.8712 | 12 | 13 |
| Cannabinoid receptor 2 | Homo sapiens (human) | IC50 | 2.0090 | 4 | 4 |
| Cannabinoid receptor 2 | Homo sapiens (human) | Ki | 0.1296 | 15 | 16 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cannabinoid receptor 2 | Rattus norvegicus (Norway rat) | EC50 | 0.0233 | 1 | 1 |
| Cannabinoid receptor 2 | Homo sapiens (human) | EC50 | 5.8578 | 5 | 5 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cannabinoid receptor 1 | Homo sapiens (human) | Kieq | 2.8200 | 1 | 1 |
| Cannabinoid receptor 2 | Homo sapiens (human) | Kieq | 0.0054 | 1 | 1 |