An antagonist that binds to and deactivates type 1 cannabinoid receptors.
ChEBI ID: 73416
| Member | Definition | Class |
|---|---|---|
| am 251 | A carbohydrazide obtained by formal condensation of the carboxy group of 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid with the amino group of 1-aminopiperidine. An antagonist at the CB1 cannabinoid receptor. | AM-251 |
| fingolimod | An aminodiol that consists of propane-1,3-diol having amino and 2-(4-octylphenyl)ethyl substituents at the 2-position. It is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. A prodrug, fingolimod is phosphorylated by sphingosine kinase to active metabolite fingolimod-phosphate, a structural analogue of sphingosine 1-phosphate. | fingolimod |
| sr141716 | A carbohydrazide obtained by formal condensation of the carboxy group of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid with the amino group of 1-aminopiperidine. It is a potent and selective cannabinoid receptor 1 (CB1R) antagonist. Besides its antagonistic properties, numerous studies have shown that, at micromolar concentrations rimonabant behaves as an inverse agonist at CB1 receptors. The drug was the first selective CB1 antagonist/inverse agonist introduced into clinical practice to treat obesity and metabolic-related disorders. It was later withdrawn from market due to CNS-related adverse effects including depression and suicidal ideation. | rimonabant |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 205 (6.67) | 18.2507 |
| 2000's | 1,514 (49.27) | 29.6817 |
| 2010's | 1,226 (39.90) | 24.3611 |
| 2020's | 128 (4.17) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 61 (1.88%) | 5.53% |
| Reviews | 246 (7.59%) | 6.00% |
| Case Studies | 10 (0.31%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 2,925 (90.22%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| AR protein | Homo sapiens (human) | Potency | 26.9230 | 7 | 7 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 79.4328 | 1 | 1 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 23.1234 | 2 | 2 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 22.3872 | 1 | 1 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 7.9433 | 1 | 1 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 1.9953 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 24.5454 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 12.3018 | 1 | 1 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 3.9811 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 10.0000 | 2 | 2 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 13.8029 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 22.3701 | 4 | 4 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 9.4392 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 16.2971 | 6 | 6 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 14.9872 | 1 | 2 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 24.6762 | 4 | 8 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 33.4889 | 1 | 1 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 21.1619 | 1 | 3 |
| G | Vesicular stomatitis virus | Potency | 24.5454 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 13.3359 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 23.5183 | 2 | 2 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 26.6011 | 2 | 2 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 1.9953 | 1 | 3 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 55.1965 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 24.5454 | 1 | 1 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 26.8325 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 24.5454 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 20.6067 | 2 | 7 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 1.9910 | 1 | 2 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 10.0000 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 2.6601 | 1 | 1 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 18.5216 | 2 | 2 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 18.1056 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 8.3088 | 3 | 3 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 33.4889 | 1 | 1 |
| polyprotein | Zika virus | Potency | 21.1619 | 1 | 3 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 2.8184 | 1 | 1 |
| PPM1D protein | Homo sapiens (human) | Potency | 19.9502 | 1 | 4 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 33.4915 | 1 | 1 |
| progesterone receptor | Homo sapiens (human) | Potency | 11.8832 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 29.8493 | 2 | 2 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 29.9349 | 1 | 1 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 31.0634 | 3 | 3 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 16.1998 | 2 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 26.4766 | 2 | 4 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 12.2352 | 2 | 2 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 25.2704 | 2 | 2 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Androgen receptor | Rattus norvegicus (Norway rat) | Ki | 2.2900 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 17.5000 | 2 | 2 |
| C-X-C chemokine receptor type 3 | Homo sapiens (human) | Ki | 0.0016 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Cannabinoid receptor 1 | Homo sapiens (human) | IC50 | 0.0343 | 38 | 38 |
| Cannabinoid receptor 1 | Mus musculus (house mouse) | IC50 | 0.0250 | 1 | 1 |
| Cannabinoid receptor 1 | Rattus norvegicus (Norway rat) | IC50 | 0.0081 | 3 | 3 |
| Cannabinoid receptor 1 | Homo sapiens (human) | Ki | 0.0422 | 81 | 91 |
| Cannabinoid receptor 1 | Mus musculus (house mouse) | Ki | 0.0062 | 2 | 2 |
| Cannabinoid receptor 1 | Rattus norvegicus (Norway rat) | Ki | 0.0042 | 8 | 14 |
| Cannabinoid receptor 2 | Homo sapiens (human) | IC50 | 2.3894 | 19 | 19 |
| Cannabinoid receptor 2 | Homo sapiens (human) | Ki | 1.5569 | 47 | 57 |
| Cathepsin B | Mus musculus (house mouse) | Ki | 1.5800 | 1 | 1 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 | 0.0069 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 0.0069 | 1 | 1 |
| Fatty acid-binding protein, liver | Mus musculus (house mouse) | Ki | 2.0000 | 1 | 1 |
| G-protein coupled bile acid receptor 1 | Homo sapiens (human) | Ki | 0.9000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 1 | Rattus norvegicus (Norway rat) | Ki | 0.0250 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2A | Rattus norvegicus (Norway rat) | Ki | 0.0250 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2B | Rattus norvegicus (Norway rat) | Ki | 0.0250 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2C | Rattus norvegicus (Norway rat) | Ki | 0.0250 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2D | Rattus norvegicus (Norway rat) | Ki | 0.0250 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 3A | Rattus norvegicus (Norway rat) | Ki | 0.0250 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 3B | Rattus norvegicus (Norway rat) | Ki | 0.0250 | 1 | 1 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.1080 | 1 | 1 |
| Multidrug resistance-associated protein 1 | Homo sapiens (human) | Ki | 1.4000 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | Ki | 4.0000 | 1 | 1 |
| N-arachidonyl glycine receptor | Homo sapiens (human) | IC50 | 10.1000 | 1 | 1 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 3.7950 | 2 | 2 |
| Sphingosine 1-phosphate receptor 1 | Homo sapiens (human) | IC50 | 0.7219 | 2 | 2 |
| Sphingosine 1-phosphate receptor 2 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Sphingosine 1-phosphate receptor 3 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Sphingosine 1-phosphate receptor 4 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Sphingosine 1-phosphate receptor 5 | Homo sapiens (human) | IC50 | 2.1000 | 1 | 1 |
| Sphingosine-1-phosphate lyase 1 | Homo sapiens (human) | IC50 | 34.5000 | 2 | 2 |
| Sphingosine-1-phosphate lyase 1 | Mus musculus (house mouse) | IC50 | 52.4000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cannabinoid receptor 1 | Homo sapiens (human) | EC50 | 0.0654 | 16 | 19 |
| Cannabinoid receptor 1 | Rattus norvegicus (Norway rat) | EC50 | 28.1526 | 2 | 2 |
| Cannabinoid receptor 1 | Homo sapiens (human) | Kd | 0.0027 | 8 | 16 |
| Cannabinoid receptor 1 | Mus musculus (house mouse) | Kd | 0.0025 | 1 | 1 |
| Cannabinoid receptor 1 | Rattus norvegicus (Norway rat) | Kd | 0.0018 | 1 | 1 |
| Cannabinoid receptor 2 | Mus musculus (house mouse) | EC50 | 0.0150 | 1 | 1 |
| Cannabinoid receptor 2 | Homo sapiens (human) | EC50 | 20.6050 | 2 | 2 |
| Cytochrome P450 2D6 | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| G-protein coupled receptor 55 | Homo sapiens (human) | EC50 | 2.0100 | 1 | 1 |
| Sphingosine 1-phosphate receptor 1 | Homo sapiens (human) | EC50 | 4.0019 | 5 | 5 |
| Sphingosine 1-phosphate receptor 2 | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| Sphingosine 1-phosphate receptor 3 | Homo sapiens (human) | EC50 | 5.6287 | 4 | 4 |
| Sphingosine 1-phosphate receptor 4 | Homo sapiens (human) | EC50 | 5.0002 | 2 | 2 |
| Sphingosine 1-phosphate receptor 5 | Homo sapiens (human) | EC50 | 4.3875 | 3 | 3 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cannabinoid receptor 1 | Homo sapiens (human) | Kb | 0.0007 | 1 | 1 |
| Cannabinoid receptor 1 | Homo sapiens (human) | Ke | 1.4294 | 7 | 7 |
| Cannabinoid receptor 1 | Homo sapiens (human) | Kieq | 0.0120 | 1 | 1 |
| Cannabinoid receptor 1 | Homo sapiens (human) | Log Ki | 0.0011 | 1 | 1 |
| Cannabinoid receptor 2 | Homo sapiens (human) | Kb | 1.9770 | 1 | 1 |
| Cannabinoid receptor 2 | Homo sapiens (human) | Kieq | 0.7900 | 1 | 1 |
| Cannabinoid receptor 2 | Homo sapiens (human) | Log Ki | 0.0028 | 1 | 1 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Kb | 0.0007 | 1 | 2 |
| Orexin receptor type 1 | Homo sapiens (human) | Ke | 6.6670 | 3 | 3 |