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)

MemberDefinitionClass
sr 144528A 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)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19900 (0.00)18.7374
1990's14 (5.45)18.2507
2000's150 (58.37)29.6817
2010's81 (31.52)24.3611
2020's12 (4.67)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (1.15%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other258 (98.85%)84.16%

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
cytochrome P450 2C9, partialHomo sapiens (human)Potency2.683711
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.899911
GVesicular stomatitis virusPotency2.683711
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency2.683711
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency2.683712
Interferon betaHomo sapiens (human)Potency2.683711

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Cannabinoid receptor 1Homo sapiens (human)IC50271.347222
Cannabinoid receptor 1Homo sapiens (human)Ki9.87121213
Cannabinoid receptor 2 Homo sapiens (human)IC502.009044
Cannabinoid receptor 2 Homo sapiens (human)Ki0.12961516

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Cannabinoid receptor 2Rattus norvegicus (Norway rat)EC500.023311
Cannabinoid receptor 2 Homo sapiens (human)EC505.857855

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Cannabinoid receptor 1Homo sapiens (human)Kieq2.820011
Cannabinoid receptor 2 Homo sapiens (human)Kieq0.005411