null
ChEBI ID: 64054
| Member | Definition | Class |
|---|---|---|
| enkephalin, d-penicillamine (2,5)- | A heterodetic cyclic peptide that is a cyclic enkephalin analogue, having D-penicillaminyl residues located at positions 2 and 5, which form the heterocycle via a disulfide bond. | DPDPE |
| enkephalin, leucine | A pentapeptide comprising L-tyrosine, glycine, glycine, L-phenylalanine and L-leucine residues joined in sequence by peptide linkages. It is an endogenous opioid peptide produced in vertebrate species, including rodents, primates and humans that results from decomposition of proenkephalin or dynorphin and exhibits antinociceptive properties. | Leu-enkephalin zwitterion; Leu-enkephalin |
| enkephalin, methionine | A pentapeptide comprising L-tyrosine, glycine, glycine, L-phenylalanine and L-methionine residues joined in sequence by peptide linkages. It is an endogenous opioid peptide with antitumor, analgesic, and immune-boosting properties. | Met-enkephalin zwitterion; Met-enkephalin |
| norclozapine | A dibenzodoazepine substituted with chloro and piperazino groups which is a major metabolite of clozapine; a potent and selective 5-HT2C serotonin receptor antagonist. | N-desmethylclozapine |
| proglumide | A racemate composed of equal amounts of (R)- and (S)-proglumide. A non-selective CCK antagonist that was used primarily for treatment of stomach ulcers, but has been replaced by newer drugs. | N(2)-benzoyl-N,N-dipropyl-alpha-glutamine; proglumide |
| tramadol | A 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol in which both stereocentres have R-configuration; the (R,R)-enantiomer of the racemic opioid analgesic tramadol, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer. | (R,R)-tramadol |
| tramadol hydrochloride | A hydrochloride resulting from the reaction of (R,R)-tramadol with 1 molar equivalent of hydrogen chloride; the (R,R)-enantiomer of the racemic opioid analgesic tramadol hydrochloride, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer. | (R,R)-tramadol hydrochloride |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 5,381 (34.45) | 18.7374 |
| 1990's | 4,479 (28.67) | 18.2507 |
| 2000's | 2,683 (17.18) | 29.6817 |
| 2010's | 2,318 (14.84) | 24.3611 |
| 2020's | 759 (4.86) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1,365 (7.71%) | 5.53% |
| Reviews | 1,041 (5.88%) | 6.00% |
| Case Studies | 411 (2.32%) | 4.05% |
| Observational | 58 (0.33%) | 0.25% |
| Other | 14,822 (83.75%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 67.9K protein | Vaccinia virus | Potency | 28.1838 | 1 | 1 |
| Ataxin-2 | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 4.7755 | 1 | 1 |
| atrial natriuretic peptide receptor 2 precursor | Homo sapiens (human) | Potency | 14.6892 | 1 | 1 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 7.9433 | 1 | 1 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 63.0957 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 2.2107 | 1 | 2 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 15.0916 | 1 | 1 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 6.3096 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 5.0119 | 2 | 3 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 7.5637 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 7.3438 | 2 | 2 |
| D(1A) dopamine receptor | Sus scrofa (pig) | Potency | 18.4927 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 1.2589 | 1 | 1 |
| endonuclease IV | Escherichia coli | Potency | 14.1254 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 15.0890 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 30.0474 | 2 | 2 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 14.1254 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 2.2107 | 1 | 2 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| geminin | Homo sapiens (human) | Potency | 6.5131 | 1 | 2 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 6.3096 | 1 | 1 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 8.9125 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 10.6822 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 12.5893 | 1 | 2 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 2.2107 | 1 | 2 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 2.2107 | 1 | 4 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 5.8334 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 2.2107 | 1 | 2 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 33.4889 | 1 | 1 |
| polyprotein | Zika virus | Potency | 14.1254 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 10.8717 | 1 | 3 |
| serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 15.7922 | 2 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 12.5559 | 2 | 5 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 89.1251 | 1 | 1 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 31.1184 | 2 | 2 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 63.0957 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 13.3332 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 42.2395 | 1 | 2 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 64.4679 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cannabinoid receptor 1 | Mus musculus (house mouse) | Ki | 0.0017 | 1 | 1 |
| Cholecystokinin receptor type A | Cavia porcellus (domestic guinea pig) | IC50 | 800.0000 | 1 | 1 |
| Cholecystokinin receptor type A | Rattus norvegicus (Norway rat) | IC50 | 250.0000 | 1 | 1 |
| Cytosol aminopeptidase | Sus scrofa (pig) | Ki | 0.0017 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 0.0800 | 1 | 1 |
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 0.4890 | 1 | 1 |
| Delta-type opioid receptor | Homo sapiens (human) | IC50 | 0.0024 | 4 | 4 |
| Delta-type opioid receptor | Mus musculus (house mouse) | IC50 | 0.0139 | 6 | 10 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 0.1290 | 2 | 2 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 0.5371 | 16 | 20 |
| Delta-type opioid receptor | Mus musculus (house mouse) | Ki | 0.0046 | 3 | 3 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0037 | 6 | 6 |
| Histamine H2 receptor | Rattus norvegicus (Norway rat) | IC50 | 2,500.0000 | 1 | 1 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | IC50 | 0.0417 | 2 | 2 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 0.1290 | 2 | 2 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 5.1526 | 2 | 4 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 7.7500 | 3 | 4 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 2 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.2460 | 1 | 1 |
| Mu-type opioid receptor | Homo sapiens (human) | IC50 | 3.1715 | 3 | 3 |
| Mu-type opioid receptor | Mus musculus (house mouse) | IC50 | 0.0308 | 3 | 4 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 0.1290 | 2 | 2 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.1295 | 3 | 3 |
| Mu-type opioid receptor | Danio rerio (zebrafish) | Ki | 1.0005 | 1 | 2 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 2.4683 | 5 | 7 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.1001 | 6 | 7 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | Ki | 0.0603 | 1 | 1 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Ki | 0.0200 | 1 | 1 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 0.2500 | 1 | 1 |
| Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | Ki | 0.0200 | 1 | 1 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Ki | 0.0900 | 1 | 1 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | Ki | 0.0200 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Ki | 0.2900 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | Ki | 0.0200 | 1 | 1 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | Ki | 0.0510 | 1 | 1 |
| Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | Ki | 0.0200 | 1 | 1 |
| Nociceptin receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0069 | 1 | 1 |
| Opioid receptor homologue | Danio rerio (zebrafish) | Ki | 0.0730 | 1 | 1 |
| Opioid receptor, delta 1b | Danio rerio (zebrafish) | Ki | 0.1100 | 1 | 2 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 9.9073 | 4 | 5 |
| Solute carrier family 22 member 1 | Homo sapiens (human) | IC50 | 88.7600 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Delta-type opioid receptor | Homo sapiens (human) | EC50 | 0.0167 | 18 | 21 |
| Delta-type opioid receptor | Mus musculus (house mouse) | EC50 | 0.0420 | 2 | 2 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | EC50 | 0.1847 | 2 | 2 |
| Delta-type opioid receptor | Homo sapiens (human) | Kd | 0.0005 | 3 | 3 |
| Gastrin/cholecystokinin type B receptor | Homo sapiens (human) | Kd | 0.0005 | 1 | 1 |
| Kappa-type opioid receptor | Homo sapiens (human) | EC50 | 0.0800 | 3 | 3 |
| Mu-type opioid receptor | Homo sapiens (human) | EC50 | 0.6446 | 7 | 8 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Kd | 0.0005 | 3 | 3 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | EC50 | 0.0687 | 3 | 3 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | EC50 | 0.6700 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | EC50 | 5.2000 | 2 | 2 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | EC50 | 0.1700 | 1 | 1 |
| Proenkephalin-B | Homo sapiens (human) | Kd | 0.0071 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | INH | 0.0040 | 1 | 1 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | INH | 0.0088 | 1 | 1 |
| Delta-type opioid receptor | Mus musculus (house mouse) | Ke | 0.0059 | 1 | 1 |
| Histamine H1 receptor | Homo sapiens (human) | INH | 0.0031 | 1 | 1 |
| UDP-glucuronosyltransferase 1A4 | Homo sapiens (human) | Km | 56.0000 | 1 | 1 |