Substance which produces loss of feeling or sensation.
| Member | Definition | Class |
|---|
| 1,2-difluorobenzene | A difluorobenzene carrying fluoro groups at positions 1 and 2. | 1,2-difluorobenzene |
| benzonatate | The ester obtained by formal condensation of 4-butylaminobenzoic acid with nonaethylene glycol monomethyl ether. Structurally related to procaine and benzocaine, it has an anaesthetic effect on the stretch sensors in the lungs, and is used as a non-narcotic cough suppressant. | benzonatate |
| dizocilpine | An organic heterotetracyclic compound that is 1-methyl-8-azabicyclo[3.2.1]octane ortho-fused to two benzene rings at positions 2-3 and 6-7 (the 5S,10R-stereoisomer). It is a non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor and affects cognitive function, learning, and memory. | dizocilpine |
| dizocilpine maleate | A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid. | dizocilpine maleate |
| enflurane | An ether in which the oxygen atom is connected to 2-chloro-1,1,2-trifluoroethyl and difluoromethyl groups. | enflurane |
| fentanyl | A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid. | fentanyl |
| magnesium sulfate | A magnesium salt having sulfate as the counterion. | magnesium sulfate |
| morphine | A morphinane alkaloid that is a highly potent opiate analgesic psychoactive drug. Morphine acts directly on the central nervous system (CNS) to relieve pain but has a high potential for addiction, with tolerance and both physical and psychological dependence developing rapidly. Morphine is the most abundant opiate found in Papaver somniferum (the opium poppy). | morphine |
| phencyclidine | A member of the class of piperidines that is piperidine in which the nitrogen is substituted with a 1-phenylcyclohexyl group. Formerly used as an anaesthetic agent, it exhibits both hallucinogenic and neurotoxic effects. | phencyclidine |
| spathulenol | A tricyclic sesquiterpenoid that is 4-methylidenedecahydro-1H-cyclopropa[e]azulene carrying three methyl substituents at positions 1, 1 and 7 as well as a hydroxy substituent at position 7. | spathulenol |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| AR protein | Homo sapiens (human) | Potency | 20.6503 | 7 | 7 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 16.3535 | 1 | 1 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 9.5283 | 1 | 1 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 8.9125 | 2 | 2 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 7.9433 | 1 | 1 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 0.0050 | 1 | 1 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 0.0050 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 56.1048 | 2 | 2 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 6.9178 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 15.7591 | 2 | 6 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 8.0376 | 2 | 2 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 0.0398 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 12.6071 | 6 | 6 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 5.3218 | 4 | 4 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 5.2193 | 1 | 3 |
| G | Vesicular stomatitis virus | Potency | 6.9178 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 15.7591 | 1 | 3 |
| geminin | Homo sapiens (human) | Potency | 20.7939 | 2 | 4 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 8.4685 | 2 | 2 |
| GLS protein | Homo sapiens (human) | Potency | 0.6310 | 1 | 1 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 8.4127 | 1 | 1 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 0.7943 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 6.9178 | 1 | 1 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 2.1314 | 1 | 1 |
| IDH1 | Homo sapiens (human) | Potency | 29.0929 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 6.9178 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 6.9178 | 1 | 1 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 40.5334 | 1 | 1 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 0.0020 | 1 | 1 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 0.1995 | 1 | 1 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 10.0000 | 2 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 30.0450 | 2 | 2 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 26.6032 | 1 | 1 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 20.3148 | 1 | 1 |
| polyunsaturated fatty acid lipoxygenase ALOX12 | Homo sapiens (human) | Potency | 8.9125 | 1 | 1 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 4.6591 | 1 | 2 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 10.0000 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 52.5925 | 2 | 4 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 19.4007 | 2 | 5 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 5.9728 | 2 | 2 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 34.4989 | 2 | 4 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 39.8107 | 2 | 2 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 8.4127 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| 5-hydroxytryptamine receptor 7 | Cavia porcellus (domestic guinea pig) | IC50 | 28.0000 | 1 | 2 |
| Acetylcholinesterase | Electrophorus electricus (electric eel) | Ki | 109.0000 | 1 | 1 |
| Acyl-CoA desaturase 1 | Rattus norvegicus (Norway rat) | Ki | 0.2990 | 1 | 1 |
| Amine oxidase [flavin-containing] A | Homo sapiens (human) | Ki | 5.4620 | 1 | 1 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | Ki | 5.4620 | 1 | 1 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 | 39.1250 | 4 | 4 |
| ATP-dependent translocase ABCB1 | Mus musculus (house mouse) | IC50 | 50.0000 | 4 | 4 |
| Beta-2 adrenergic receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.2500 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 72.5000 | 2 | 2 |
| Cholinesterase | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| Cholinesterase | Mus musculus (house mouse) | Ki | 0.5224 | 2 | 2 |
| Cytochrome P450 2B6 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 21.0000 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 26.2000 | 1 | 1 |
| D(4) dopamine receptor | Homo sapiens (human) | Ki | 0.5540 | 1 | 1 |
| Delta-type opioid receptor | Homo sapiens (human) | IC50 | 0.1740 | 7 | 7 |
| Delta-type opioid receptor | Mus musculus (house mouse) | IC50 | 0.4094 | 8 | 12 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 0.1765 | 12 | 21 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 0.2987 | 30 | 37 |
| Delta-type opioid receptor | Mus musculus (house mouse) | Ki | 0.5690 | 2 | 2 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.2430 | 13 | 18 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Ki | 70.4335 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 1 | Homo sapiens (human) | IC50 | 0.4195 | 4 | 4 |
| Glutamate receptor ionotropic, NMDA 1 | Homo sapiens (human) | Ki | 0.0211 | 3 | 5 |
| Glutamate receptor ionotropic, NMDA 1 | Rattus norvegicus (Norway rat) | IC50 | 0.0532 | 7 | 9 |
| Glutamate receptor ionotropic, NMDA 1 | Rattus norvegicus (Norway rat) | Ki | 0.0328 | 6 | 12 |
| Glutamate receptor ionotropic, NMDA 2A | Homo sapiens (human) | IC50 | 0.1463 | 3 | 3 |
| Glutamate receptor ionotropic, NMDA 2A | Homo sapiens (human) | Ki | 0.0211 | 3 | 5 |
| Glutamate receptor ionotropic, NMDA 2A | Rattus norvegicus (Norway rat) | IC50 | 0.0532 | 7 | 9 |
| Glutamate receptor ionotropic, NMDA 2A | Rattus norvegicus (Norway rat) | Ki | 0.0328 | 6 | 12 |
| Glutamate receptor ionotropic, NMDA 2B | Homo sapiens (human) | IC50 | 0.6340 | 2 | 2 |
| Glutamate receptor ionotropic, NMDA 2B | Rattus norvegicus (Norway rat) | IC50 | 0.0532 | 7 | 9 |
| Glutamate receptor ionotropic, NMDA 2B | Homo sapiens (human) | Ki | 0.0211 | 3 | 5 |
| Glutamate receptor ionotropic, NMDA 2B | Rattus norvegicus (Norway rat) | Ki | 0.0328 | 6 | 12 |
| Glutamate receptor ionotropic, NMDA 2C | Rattus norvegicus (Norway rat) | IC50 | 0.0532 | 7 | 9 |
| Glutamate receptor ionotropic, NMDA 2C | Homo sapiens (human) | Ki | 0.0211 | 3 | 5 |
| Glutamate receptor ionotropic, NMDA 2C | Rattus norvegicus (Norway rat) | Ki | 0.0725 | 8 | 14 |
| Glutamate receptor ionotropic, NMDA 2D | Rattus norvegicus (Norway rat) | IC50 | 0.0532 | 7 | 9 |
| Glutamate receptor ionotropic, NMDA 2D | Homo sapiens (human) | Ki | 0.0211 | 3 | 5 |
| Glutamate receptor ionotropic, NMDA 2D | Rattus norvegicus (Norway rat) | Ki | 0.0328 | 6 | 12 |
| Glutamate receptor ionotropic, NMDA 3A | Rattus norvegicus (Norway rat) | IC50 | 0.0532 | 7 | 9 |
| Glutamate receptor ionotropic, NMDA 3A | Homo sapiens (human) | Ki | 0.0211 | 3 | 5 |
| Glutamate receptor ionotropic, NMDA 3A | Rattus norvegicus (Norway rat) | Ki | 0.0328 | 6 | 12 |
| Glutamate receptor ionotropic, NMDA 3B | Rattus norvegicus (Norway rat) | IC50 | 0.0532 | 7 | 9 |
| Glutamate receptor ionotropic, NMDA 3B | Homo sapiens (human) | Ki | 0.0211 | 3 | 5 |
| Glutamate receptor ionotropic, NMDA 3B | Rattus norvegicus (Norway rat) | Ki | 0.0328 | 6 | 12 |
| Histamine H1 receptor | Homo sapiens (human) | IC50 | 147.9110 | 1 | 1 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 | 1.6397 | 6 | 7 |
| Kappa-type opioid receptor | Homo sapiens (human) | IC50 | 0.8863 | 4 | 4 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | IC50 | 0.0828 | 2 | 4 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0394 | 9 | 14 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 4.4918 | 20 | 27 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 0.1130 | 27 | 27 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | Ki | 0.9252 | 2 | 2 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.1130 | 2 | 2 |
| Lysosomal Pro-X carboxypeptidase | Homo sapiens (human) | IC50 | 0.0482 | 1 | 2 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.1357 | 5 | 6 |
| Mu-type opioid receptor | Homo sapiens (human) | IC50 | 0.0930 | 12 | 12 |
| Mu-type opioid receptor | Mus musculus (house mouse) | IC50 | 0.3305 | 7 | 9 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0911 | 14 | 20 |
| Mu-type opioid receptor | Bos taurus (cattle) | Ki | 0.0013 | 3 | 3 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0398 | 16 | 25 |
| Mu-type opioid receptor | Danio rerio (zebrafish) | Ki | 0.1872 | 2 | 2 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.0039 | 38 | 38 |
| Mu-type opioid receptor | Mus musculus (house mouse) | Ki | 0.0695 | 5 | 7 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 2.8822 | 19 | 35 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Ki | 14.3131 | 3 | 7 |
| Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | Ki | 14.3131 | 3 | 7 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | Ki | 14.3131 | 3 | 7 |
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | Ki | 14.3131 | 3 | 7 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
| Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | Ki | 14.3131 | 3 | 7 |
| Nociceptin receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0025 | 1 | 1 |
| Opioid receptor homologue | Danio rerio (zebrafish) | Ki | 0.2230 | 1 | 1 |
| Opioid receptor, delta 1b | Danio rerio (zebrafish) | Ki | 1.4270 | 1 | 1 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 500.9098 | 1 | 2 |
| Proteinase-activated receptor 1 | Homo sapiens (human) | Ki | 0.0022 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Cavia porcellus (domestic guinea pig) | IC50 | 4.9730 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | IC50 | 0.3540 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Rattus norvegicus (Norway rat) | IC50 | 1.1150 | 1 | 2 |
| Sigma non-opioid intracellular receptor 1 | Cavia porcellus (domestic guinea pig) | Ki | 2.4743 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 43.8849 | 4 | 5 |
| Sigma non-opioid intracellular receptor 1 | Rattus norvegicus (Norway rat) | Ki | 20.4190 | 3 | 3 |
| Sodium-dependent serotonin transporter | Rattus norvegicus (Norway rat) | Ki | 0.8724 | 2 | 5 |
| Solute carrier family 22 member 1 | Homo sapiens (human) | IC50 | 48.6533 | 2 | 3 |