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cholinergic antagonist
Any drug that binds to but does not activate cholinergic receptors, thereby blocking the actions of acetylcholine or cholinergic agonists.
ChEBI ID: 48873
Members (22)
| Member | Definition | Class |
|---|---|---|
| 3alpha-hydroxy-4alpha-methylergosta-8,24(28)-dien-7,11-dione-26-oic acid | A steroid acid that is ergosta-8,24(28)-dien-26-oic acid substituted by a hydroxy group at position 3, a methyl group at position 4 and oxo groups at positions 7 and 11 (the 3alpha,4alpha,5alpha stereoisomer). Isolated from Antrodia cinnamomea and Antrodia camphorata, it exhibits cytotoxic, anticholinergic and antiserotonergic activities. | zhankuic acid B |
| 4-diphenylacetoxy-1,1-dimethylpiperidinium | A quaternary ammonium salt obtained by formal methylation of the tertiary amino function of 4-diphenylacetoxy-N-methylpiperidine. | 4-DAMP(1+) |
| 4-diphenylacetoxy-n-methylpiperidine methiodide | A quaternary ammonium salt obtained by combining equimolar amounts of 4-diphenylacetoxy-N-methylpiperidine and iodomethane. | 4-DAMP methiodide |
| alverine citrate | The citrate salt of alverine, resulting from the reaction of equimolar amounts of alvarine and citric acid. An antispasmodic that acts directly on intestinal and uterine smooth muscle, it is used in the treatment of irritable bowel syndrome. | alverine citrate |
| antazoline | A member of the class of imidazolines that is 2-aminomethyl-2-imidazoline in which the exocyclic amino hydrogens are replaced by benzyl and phenyl groups. Antazoline is only found in individuals that have taken the drug. | antazoline |
| buclizine | An N-alkylpiperazine carrying (4-chlorophenyl)(phenyl)methyl and 4-tert-butylbenzyl groups. | buclizine |
| cyclizine | An N-alkylpiperazine in which one nitrogen of the piperazine ring is substituted by a methyl group, while the other is substituted by a diphenylmethyl group. | cyclizine |
| cyclizine hydrochloride | A hydrochloride salt consisting of equimolar amounts of cyclizine and hydrogen chloride. | cyclizine hydrochloride |
| desipramine | A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group. | desipramine |
| desloratadine | Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness. | desloratadine |
| diphenylpyraline | A member of the class of piperidines that is the benzhydryl ether derivative of 1-methyl-4-hydroxypiperidine. A sedating antihistamine, it is used as the hydrochloride for the symptomatic relief of allergic conditions including rhinitis and hay fever, and in pruritic skin disorders. It is also used as the teoclate salt (piprinhydrinate) as an ingredient in compound preparations for the symptomatic relief of coughs and the common cold. | diphenylpyraline |
| diphenylpyraline hydrochloride | The hydrochloride salt of diphenylpyraline. A sedating antihistamine, it is used as the hydrochloride for the symptomatic relief of allergic conditions including rhinitis and hay fever, and in pruritic skin disorders. | diphenylpyraline hydrochloride |
| doxylamine | doxylamine | |
| loratadine | A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders. | loratadine |
| methdilazine | A phenothiazine substituted on nitrogen by a (1-methylpyrrolidin-3-yl)methyl group; a first-generation antihistamine with anticholinergic properties. | methdilazine |
| methotrimeprazine | A member of the class of phenothiazines that is 10H-phenothiazine substituted by a (2R)-3-(dimethylamino)-2-methylpropyl group and a methoxy group at positions 10 and 2 respectively. | methotrimeprazine |
| pancuronium | A steroid ester in which a 5alpha-androstane skeleton is C-3alpha- and C-17beta-disubstituted with acetoxy groups and 2beta- and 16beta-disubstituted with 1-methylpiperidinium-1-yl groups. It is a non-depolarizing curare-mimetic muscle relaxant. | pancuronium |
| pancuronium bromide | A bromide salt consisting of two bromide ions and one pancuronium dication. | pancuronium bromide |
| prochlorperazine | A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position. | prochlorperazine |
| 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 |
| strychnine | A monoterpenoid indole alkaloid that is strychnidine bearing a keto substituent at the 10-position. | strychnine |
| toluene | The simplest member of the class toluenes consisting of a benzene core which bears a single methyl substituent. | toluene |
Research
Studies (25,121)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 11,461 (45.62) | 18.7374 |
| 1990's | 4,476 (17.82) | 18.2507 |
| 2000's | 4,570 (18.19) | 29.6817 |
| 2010's | 3,673 (14.62) | 24.3611 |
| 2020's | 941 (3.75) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 2,001 (7.22%) | 5.53% |
| Reviews | 942 (3.40%) | 6.00% |
| Case Studies | 1,290 (4.66%) | 4.05% |
| Observational | 17 (0.06%) | 0.25% |
| Other | 23,456 (84.66%) | 84.16% |
Protein Targets (280)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| 67.9K protein | Vaccinia virus | Potency | 16.8747 | 2 | 3 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 40.4796 | 2 | 3 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 0.4364 | 1 | 1 |
| alpha-galactosidase | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 15.8489 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 30.8717 | 8 | 16 |
| arylsulfatase A | Homo sapiens (human) | Potency | 12.9358 | 1 | 4 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 16.9408 | 2 | 4 |
| Ataxin-2 | Homo sapiens (human) | Potency | 22.8871 | 2 | 5 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 0.7569 | 1 | 1 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 28.1538 | 1 | 3 |
| atrial natriuretic peptide receptor 2 precursor | Homo sapiens (human) | Potency | 17.4872 | 1 | 2 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 14.1044 | 2 | 4 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 51.4346 | 1 | 4 |
| caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 33.4915 | 1 | 1 |
| caspase-3 | Homo sapiens (human) | Potency | 33.4915 | 1 | 1 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 36.5681 | 2 | 6 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 20.2058 | 2 | 5 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 16.6268 | 1 | 3 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 36.7188 | 2 | 8 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 32.7992 | 1 | 4 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 7.9433 | 1 | 1 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 30.7248 | 1 | 3 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 26.7904 | 1 | 2 |
| Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 15.8114 | 1 | 1 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 63.0957 | 1 | 1 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 7.9433 | 1 | 1 |
| chaperonin-containing TCP-1 beta subunit homolog | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 48.3135 | 2 | 4 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 7.7079 | 1 | 4 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 18.5665 | 1 | 3 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 5.5368 | 1 | 2 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 5.9760 | 1 | 5 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 12.6767 | 1 | 11 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 11.9425 | 2 | 10 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 14.2087 | 2 | 5 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 51.0406 | 1 | 2 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 2.9447 | 2 | 5 |
| D(1A) dopamine receptor | Sus scrofa (pig) | Potency | 13.8905 | 1 | 2 |
| Disintegrin and metalloproteinase domain-containing protein 17 | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 6.2396 | 1 | 2 |
| endonuclease IV | Escherichia coli | Potency | 14.1254 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 33.7132 | 8 | 20 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 26.9278 | 2 | 4 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 23.2148 | 8 | 18 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 29.0324 | 1 | 15 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 25.6342 | 4 | 4 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 23.1226 | 2 | 4 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 25.1538 | 1 | 2 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 37.2212 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 5.5368 | 1 | 2 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| GALC protein | Homo sapiens (human) | Potency | 0.7079 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 11.9425 | 1 | 5 |
| geminin | Homo sapiens (human) | Potency | 15.7176 | 4 | 14 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 18.8011 | 3 | 9 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 9.9493 | 1 | 4 |
| GLS protein | Homo sapiens (human) | Potency | 20.7244 | 2 | 6 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 40.9796 | 3 | 5 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 43.8669 | 1 | 2 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 39.2774 | 2 | 4 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 14.6606 | 2 | 27 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 29.9033 | 1 | 2 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 78.9557 | 1 | 3 |
| histone-lysine N-methyltransferase 2A isoform 2 precursor | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 5.5368 | 1 | 2 |
| huntingtin isoform 2 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 35.0775 | 2 | 4 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 20.4839 | 2 | 4 |
| IDH1 | Homo sapiens (human) | Potency | 24.2556 | 1 | 3 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 5.5368 | 1 | 4 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 1.3397 | 2 | 5 |
| Integrin alpha-IIb | Homo sapiens (human) | Potency | 23.7358 | 1 | 2 |
| Integrin beta-3 | Homo sapiens (human) | Potency | 23.7358 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 14.7892 | 2 | 3 |
| isocitrate dehydrogenase 1, partial | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 14.8431 | 2 | 12 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 16.5841 | 1 | 5 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 28.6552 | 1 | 3 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 21.8876 | 1 | 6 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 21.9164 | 2 | 5 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 4.4525 | 2 | 8 |
| muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 79.4328 | 1 | 1 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 12.4082 | 1 | 4 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 17.5594 | 2 | 4 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 14.1209 | 1 | 4 |
| NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 58.0479 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 27.0238 | 2 | 5 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 26.9951 | 1 | 3 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 18.1267 | 2 | 3 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 25.5330 | 3 | 8 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 94.5626 | 1 | 2 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 17.5782 | 1 | 4 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 27.2785 | 1 | 2 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 26.4208 | 2 | 4 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 51.4392 | 3 | 4 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 42.2395 | 1 | 2 |
| plasminogen precursor | Mus musculus (house mouse) | Potency | 12.5893 | 1 | 1 |
| polyprotein | Zika virus | Potency | 37.2212 | 1 | 1 |
| polyunsaturated fatty acid lipoxygenase ALOX12 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 12.7077 | 1 | 9 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 14.4132 | 1 | 6 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 26.5709 | 3 | 7 |
| progesterone receptor | Homo sapiens (human) | Potency | 24.4802 | 2 | 5 |
| Rap guanine nucleotide exchange factor 4 | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 10.1366 | 2 | 5 |
| ras-related protein Rab-9A | Homo sapiens (human) | Potency | 100.0000 | 1 | 2 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 13.4238 | 1 | 2 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 37.1490 | 3 | 7 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 11.8855 | 2 | 3 |
| serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 16.1500 | 4 | 9 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 23.7338 | 1 | 3 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 23.7338 | 1 | 3 |
| Smad3 | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 34.8462 | 1 | 4 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 14.9461 | 1 | 3 |
| TDP1 protein | Homo sapiens (human) | Potency | 16.4363 | 2 | 22 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 24.3247 | 1 | 2 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 2.9629 | 2 | 3 |
| Thrombopoietin | Homo sapiens (human) | Potency | 19.2203 | 2 | 6 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 11.5033 | 2 | 10 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 98.6547 | 2 | 3 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 24.6185 | 5 | 15 |
| ubiquitin carboxyl-terminal hydrolase 2 isoform a | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 12.5893 | 1 | 1 |
| urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 12.5893 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 47.3008 | 1 | 6 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 18.7047 | 2 | 4 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 42.5238 | 1 | 2 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 46.4852 | 1 | 3 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 43.8669 | 1 | 2 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 1-acylglycerol-3-phosphate O-acyltransferase ABHD5 isoform a | Homo sapiens (human) | IC50 | 2.6350 | 2 | 2 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | IC50 | 0.6500 | 2 | 2 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Ki | 0.5430 | 1 | 1 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | IC50 | 0.6500 | 2 | 2 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | Ki | 0.5430 | 1 | 1 |
| 5-hydroxytryptamine receptor 1D | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| 5-hydroxytryptamine receptor 1F | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | IC50 | 0.0884 | 1 | 3 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 0.0472 | 3 | 5 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | IC50 | 0.1908 | 1 | 4 |
| 5-hydroxytryptamine receptor 2B | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | Ki | 0.1218 | 1 | 4 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | IC50 | 0.3763 | 1 | 3 |
| 5-hydroxytryptamine receptor 2C | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 0.1973 | 1 | 3 |
| 5-hydroxytryptamine receptor 3A | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| 5-hydroxytryptamine receptor 3B | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | IC50 | 0.3763 | 1 | 3 |
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | Ki | 0.1973 | 1 | 3 |
| 5-hydroxytryptamine receptor 4 | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| 5-hydroxytryptamine receptor 5A | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| 5-hydroxytryptamine receptor 5B | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | IC50 | 1.2190 | 1 | 2 |
| 5-hydroxytryptamine receptor 6 | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | Ki | 0.5660 | 1 | 2 |
| 5-hydroxytryptamine receptor 7 | Cavia porcellus (domestic guinea pig) | IC50 | 53.2000 | 1 | 4 |
| 5-hydroxytryptamine receptor 7 | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| Acetylcholinesterase | Homo sapiens (human) | IC50 | 2.4526 | 2 | 2 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | IC50 | 0.7580 | 1 | 2 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | Ki | 0.7515 | 1 | 2 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0002 | 1 | 1 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0034 | 1 | 1 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | IC50 | 0.6245 | 1 | 2 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | Ki | 0.3065 | 1 | 2 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | IC50 | 0.5734 | 2 | 3 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 0.3225 | 1 | 2 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | IC50 | 0.7188 | 2 | 3 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 0.4924 | 1 | 2 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | IC50 | 0.0411 | 2 | 2 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
| Angiotensin-converting enzyme | Oryctolagus cuniculus (rabbit) | IC50 | 22.9281 | 1 | 3 |
| Angiotensin-converting enzyme | Oryctolagus cuniculus (rabbit) | Ki | 18.7845 | 1 | 3 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 5 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 | 27.2000 | 1 | 2 |
| Bile acid receptor | Homo sapiens (human) | IC50 | 3.0700 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 277.7077 | 3 | 13 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 5 |
| 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 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 | 0.0160 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 3.2588 | 1 | 2 |
| Cytochrome P450 2J2 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | IC50 | 0.1550 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 0.0780 | 1 | 1 |
| D(2) dopamine receptor | Homo sapiens (human) | IC50 | 0.0110 | 1 | 1 |
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 0.0036 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | IC50 | 1.6370 | 1 | 3 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 0.5558 | 1 | 3 |
| D(4) dopamine receptor | Homo sapiens (human) | IC50 | 2.3110 | 1 | 1 |
| D(4) dopamine receptor | Homo sapiens (human) | Ki | 0.8100 | 1 | 1 |
| fMet-Leu-Phe receptor | Homo sapiens (human) | IC50 | 66.7000 | 1 | 1 |
| Glycine receptor subunit alpha-1 | Homo sapiens (human) | IC50 | 0.1843 | 14 | 20 |
| Glycine receptor subunit alpha-1 | Homo sapiens (human) | Ki | 0.0503 | 3 | 3 |
| Glycine receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Ki | 0.0120 | 1 | 1 |
| Glycine receptor subunit beta | Homo sapiens (human) | IC50 | 0.2871 | 6 | 9 |
| hepatocyte nuclear factor 4-alpha isoform 2 | Homo sapiens (human) | IC50 | 39.8410 | 1 | 1 |
| Histamine H1 receptor | Homo sapiens (human) | IC50 | 0.0890 | 3 | 6 |
| Histamine H1 receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0008 | 1 | 2 |
| Histamine H1 receptor | Homo sapiens (human) | Ki | 0.0881 | 5 | 9 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | IC50 | 3.8000 | 1 | 1 |
| Histamine H2 receptor | Homo sapiens (human) | IC50 | 1.0990 | 1 | 1 |
| Histamine H2 receptor | Rattus norvegicus (Norway rat) | IC50 | 2,500.0000 | 1 | 1 |
| Histamine H2 receptor | Homo sapiens (human) | Ki | 1.0800 | 1 | 1 |
| Histamine H3 receptor | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| Histamine H3 receptor | Rattus norvegicus (Norway rat) | Ki | 5.0000 | 1 | 1 |
| Histamine H4 receptor | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| Mcl-1 | Homo sapiens (human) | IC50 | 3.7733 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 5 |
| Muscarinic acetylcholine receptor DM1 | Drosophila melanogaster (fruit fly) | Ki | 0.0165 | 2 | 2 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | IC50 | 0.4899 | 2 | 4 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | Ki | 0.1180 | 2 | 4 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | IC50 | 1.1080 | 2 | 4 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 0.3950 | 2 | 4 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | IC50 | 0.2267 | 10 | 12 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Ki | 0.0580 | 8 | 10 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | IC50 | 0.2844 | 7 | 9 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Ki | 0.0597 | 4 | 6 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | IC50 | 0.1435 | 6 | 8 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | Ki | 0.1374 | 4 | 6 |
| neutrophil cytosol factor 1 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Nitric oxide synthase, inducible | Mus musculus (house mouse) | IC50 | 9.6000 | 1 | 1 |
| Nuclear receptor subfamily 3 group C member 3 | Bos taurus (cattle) | IC50 | 22.9281 | 1 | 3 |
| Nuclear receptor subfamily 3 group C member 3 | Bos taurus (cattle) | Ki | 18.7845 | 1 | 3 |
| perilipin-1 | Homo sapiens (human) | IC50 | 2.2610 | 1 | 1 |
| perilipin-5 | Homo sapiens (human) | IC50 | 2.6350 | 2 | 2 |
| Platelet-activating factor receptor | Homo sapiens (human) | IC50 | 135.0000 | 1 | 1 |
| Pleiotropic ABC efflux transporter of multiple drugs | Saccharomyces cerevisiae S288C | IC50 | 5.6500 | 1 | 2 |
| Potassium channel subfamily K member 9 | Homo sapiens (human) | IC50 | 63.4000 | 1 | 1 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 4.9774 | 9 | 16 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | Ki | 18.7845 | 1 | 3 |
| Prostaglandin G/H synthase 1 | Ovis aries (sheep) | Ki | 0.1600 | 1 | 1 |
| Protein farnesyltransferase subunit beta | Homo sapiens (human) | IC50 | 65.0000 | 1 | 1 |
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Homo sapiens (human) | IC50 | 65.0000 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | IC50 | 0.0540 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 0.0230 | 1 | 1 |
| Small conductance calcium-activated potassium channel protein 1 | Rattus norvegicus (Norway rat) | IC50 | 6.8000 | 1 | 1 |
| Small conductance calcium-activated potassium channel protein 2 | Rattus norvegicus (Norway rat) | IC50 | 6.8000 | 1 | 1 |
| Small conductance calcium-activated potassium channel protein 3 | Rattus norvegicus (Norway rat) | IC50 | 6.8000 | 1 | 1 |
| Sodium channel protein type 5 subunit alpha | Homo sapiens (human) | IC50 | 1.5200 | 1 | 1 |
| Sodium-dependent dopamine transporter | Rattus norvegicus (Norway rat) | IC50 | 7.8000 | 1 | 1 |
| Sodium-dependent dopamine transporter | Rattus norvegicus (Norway rat) | Ki | 7.0000 | 2 | 2 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | IC50 | 26.7971 | 6 | 8 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | Ki | 1.1526 | 3 | 7 |
| Sodium-dependent neutral amino acid transporter B(0)AT2 | Homo sapiens (human) | IC50 | 88.0000 | 1 | 2 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | IC50 | 0.0870 | 17 | 18 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | Ki | 0.1242 | 15 | 17 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | IC50 | 0.3639 | 5 | 6 |
| Sodium-dependent serotonin transporter | Rattus norvegicus (Norway rat) | IC50 | 20.0000 | 1 | 1 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | Ki | 0.2543 | 2 | 3 |
| Sodium-dependent serotonin transporter | Rattus norvegicus (Norway rat) | Ki | 0.1630 | 1 | 1 |
| Solute carrier family 22 member 1 | Rattus norvegicus (Norway rat) | IC50 | 17.5000 | 1 | 1 |
| Solute carrier family 22 member 1 | Rattus norvegicus (Norway rat) | Ki | 2.8000 | 1 | 1 |
| Solute carrier family 22 member 1 | Homo sapiens (human) | IC50 | 38.5267 | 2 | 3 |
| Solute carrier family 22 member 1 | Homo sapiens (human) | Ki | 5.3600 | 1 | 1 |
| Solute carrier family 22 member 2 | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 1 |
| Solute carrier family 22 member 2 | Homo sapiens (human) | Ki | 16.0000 | 1 | 1 |
| Solute carrier family 22 member 3 | Rattus norvegicus (Norway rat) | IC50 | 68.0000 | 1 | 1 |
| Solute carrier family 22 member 3 | Homo sapiens (human) | Ki | 14.0000 | 1 | 1 |
| Solute carrier family 22 member 4 | Rattus norvegicus (Norway rat) | IC50 | 80.0000 | 1 | 1 |
| Transporter | Rattus norvegicus (Norway rat) | IC50 | 10.6500 | 2 | 2 |
| Transporter | Rattus norvegicus (Norway rat) | Ki | 0.0074 | 2 | 3 |
| Tryptophan 5-hydroxylase 1 | Rattus norvegicus (Norway rat) | Ki | 0.0005 | 1 | 1 |
| Tyrosine-protein kinase Fyn | Homo sapiens (human) | IC50 | 5.6840 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1C | Homo sapiens (human) | IC50 | 11.4000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1D | Homo sapiens (human) | IC50 | 11.4000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1F | Homo sapiens (human) | IC50 | 11.4000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1S | Homo sapiens (human) | IC50 | 11.4000 | 1 | 1 |
| Voltage-dependent N-type calcium channel subunit alpha-1B | Homo sapiens (human) | IC50 | 11.0000 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Albumin | Homo sapiens (human) | Kd | 851.1380 | 1 | 1 |
| Angiotensin-converting enzyme 2 | Homo sapiens (human) | EC50 | 2.5000 | 1 | 1 |
| Endolysin | Tequatrovirus T4 | Kd | 248.6667 | 6 | 6 |
| Histamine H1 receptor | Cavia porcellus (domestic guinea pig) | Kd | 0.0724 | 2 | 2 |
| Histamine H1 receptor | Homo sapiens (human) | Kd | 0.1070 | 1 | 2 |
| Nuclear receptor subfamily 1 group I member 2 | Homo sapiens (human) | EC50 | 8.9000 | 4 | 4 |
| Procathepsin L | Homo sapiens (human) | EC50 | 2.5000 | 1 | 1 |
| Replicase polyprotein 1a | Severe acute respiratory syndrome-related coronavirus | EC50 | 2.5000 | 1 | 1 |
| Replicase polyprotein 1ab | Betacoronavirus England 1 | EC50 | 2.5000 | 1 | 1 |
| Replicase polyprotein 1ab | Human coronavirus 229E | EC50 | 2.5000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | EC50 | 2.5000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | EC50 | 2.5000 | 1 | 1 |
| short transient receptor potential channel 6 isoform 1 | Mus musculus (house mouse) | EC50 | 8.0650 | 1 | 2 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | Kd | 0.0008 | 1 | 1 |
| Spike glycoprotein | Betacoronavirus England 1 | EC50 | 2.5000 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | EC50 | 2.5000 | 1 | 1 |
| Taste receptor type 2 member 10 | Homo sapiens (human) | EC50 | 22.5000 | 2 | 2 |
| Taste receptor type 2 member 46 | Homo sapiens (human) | EC50 | 0.6900 | 1 | 1 |
| Transmembrane protease serine 2 | Homo sapiens (human) | EC50 | 2.5000 | 1 | 1 |
| voltage-dependent T-type calcium channel subunit alpha-1H isoform a | Homo sapiens (human) | EC50 | 0.0000 | 1 | 1 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Gamma-aminobutyric acid receptor subunit rho-1 | Homo sapiens (human) | Kb | 69.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit rho-2 | Homo sapiens (human) | Kb | 69.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit rho-3 | Homo sapiens (human) | Kb | 69.0000 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | K0.5 | 0.0454 | 1 | 7 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | KA | 0.0210 | 1 | 1 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Kb | 0.0085 | 1 | 2 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Kb | 0.0085 | 1 | 1 |
| Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | Kb | 0.0085 | 1 | 2 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | Kb | 0.0085 | 1 | 2 |
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | Kb | 0.0085 | 1 | 2 |
| Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | Kb | 0.0085 | 1 | 2 |
| Pleiotropic ABC efflux transporter of multiple drugs | Saccharomyces cerevisiae S288C | INH | 67.6000 | 1 | 2 |
| Snq2p | Saccharomyces cerevisiae EC1118 | INH | 53.3000 | 1 | 2 |
| Taste receptor type 2 member 10 | Homo sapiens (human) | Activity | 1.5500 | 2 | 2 |