Page last updated: 2024-08-05 15:11:09

H1-receptor antagonist

H1-receptor antagonists are the drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine.

ChEBI ID: 37955

Members (64)

MemberDefinitionClass
(S)-carbinoxamine maleateThe maleic acid salt of (S)-carbinoxamine.(S)-carbinoxamine maleate
acrivastineA member of the class of pyridines that is (pyridin-2-yl)acrylic acid substituted at position 6 by a [(1E)-1-(4-methylphenyl)-3-(pyrrolidin-1-yl)prop-1-en-1-yl group. It is a non-sedating antihistamine used for treatment of hayfever, urticaria, and rhinitis.acrivastine
alcaftadineAn imidazobenzazepine that is 6,11-dihydro-5H-imidazo[2,1-b][3]benzazepine substituted at position 3 by a formyl group and at position 11 by a 1-methylpiperidin-4-ylidene group. An antihistamine used for treatment of allergic conjunctivitis.alcaftadine
antazolineA 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
aripiprazoleAn N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders.aripiprazole
aripiprazole lauroxilA dodecanoate ester obtained by formal condensation of the carboxy group of dodecanoic acid with the hydroxy group of 7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-2-oxo-3,4-dihydroquinolin-1(2H)-yl]methanol. A prodrug for aripiprazole, it is used for treatment of schizophrenia.aripiprazole lauroxil
astemizoleA piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.astemizole
azatadineA benzo[5,6]cyclohepta[1,2-b]pyridine having a 1-methylpiperidin-4-ylidene group at the 11-position.azatadine
azelastineA phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position.azelastine
azelastine hydrochlorideThe hydrochloride salt of azelastine.azelastine hydrochloride
benzquinamidebenzquinamide
bromodiphenhydramineA tertiary amino compound that is the 4-bromobenzhydryl ether of 2-(dimethylamino)ethanol. An antihistamine with antimicrobial properties, it is used in the control of cutaneous allergies.bromazine
brompheniraminePheniramine in which the hydrogen at position 4 of the phenyl substituent is substituted by bromine. A histamine H1 receptor antagonist, brompheniramine is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.brompheniramine
carbinoxamineAn organochlorine compound that is 2-(4-chlorobenzyl)pyridine in which one of the benzylic hydrogens is substituted by 2-(dimethylamino)ethoxy group. It is an ethanolamine-type antihistamine, used as its maleate salt for treating hay fever, as well as mild cases of Parkinson's disease.carbinoxamine
carbinoxamine maleateThe maleic acid salt of carbinoxamine. An ethanolamine-type antihistamine, used for treating hay fever, as well as mild cases of Parkinson's disease.carbinoxamine maleate
cetirizineA member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively.cetirizine
chlorpheniramineA tertiary amino compound that is propylamine which is substituted at position 3 by a pyridin-2-yl group and a p-chlorophenyl group and in which the hydrogens attached to the nitrogen are replaced by methyl groups. A histamine H1 antagonist, it is used to relieve the symptoms of hay fever, rhinitis, urticaria, and asthma.chlorphenamine
cinnarizinecinnarizine
clemastine2-[(2R)-1-Methylpyrrolidin-2-yl]ethanol in which the hydrogen of the hydroxy group is substituted by a 1-(4-chlorophenyl)-1-phenylethyl group (R configuration). An antihistamine with antimuscarinic and moderate sedative properties, it is used as its fumarate salt for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions.clemastine
clemastine fumarateThe fumaric acid salt of clemastine. An antihistamine with antimuscarinic and moderate sedative properties, it is used for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions.clemastine fumarate
clemizolpenicillinbenzylpenicillin clemizole
clopenthixolA thioxanthene derivative having a chloro substituent at the 2-position and an alkylidene group at the 10-position with undefined double bond stereochemistry.clopenthixol
cyclizineAn 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 hydrochlorideA hydrochloride salt consisting of equimolar amounts of cyclizine and hydrogen chloride.cyclizine hydrochloride
cyproheptadineThe product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia.cyproheptadine
demethylmirtazapineA benzazepine metabolite resulting from demethylation of the antidpressant, mirtazapine.N-demethylmirtazapine
desipramineA dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group.desipramine
desloratadineLoratadine 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
dexbrompheniramineThe (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.dexbrompheniramine
dexbrompheniramine maleateThe maleic acid salt of the (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.dexbrompheniramine maleate
diphenhydramineAn ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.diphenhydramine
diphenhydramine hydrochlorideThe hydrochloride salt of diphenhydramine.diphenhydramine hydrochloride
diphenylpyralineA 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 hydrochlorideThe 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
doxylaminedoxylamine
emedastine1-Methyl-1,4-diazepane in which the hydrogen attached to the nitrogen at position 4 is substituted by a 1-(2-ethoxyethyl)-1H-benzimidazol-2-yl group. A relatively selective histamine H1 antagonist, it is used as the difumatate salt for allergic rhinitis, urticaria, and pruritic skin disorders, and in eyedrops for the symptomatic relief of allergic conjuntivitis.emedastine
epinastineA benzazepine that is 6,11-dihydro-5H-dibenzo[b,e]azepine in which the azepine ring is fused to the e side of 4,5-dihydro-1H-imidazol-2-amine.epinastine
fexofenadineA piperidine-based anti-histamine compound.fexofenadine
hydroxyzineA N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively.hydroxyzine
ketotifenAn organic heterotricyclic compound that is 4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one which is substituted at position 4 by a 1-methylpiperidin-4-ylidene group. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is used (usually as its hydrogen fumarate salt) for the treatment of asthma, where it may take several weeks to exert its full effect.ketotifen
ketotifen fumarateAn organoammonium salt consisting of equimolar amounts of ketotifen(1+) and fumarate(1-) ions. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is a non-bronchodilator anti-asthmatic drug.ketotifen fumarate
loratadineA 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
methapyrileneA member of the class of ethylenediamine derivatives that is ethylenediamine in which one of the nitrogens is substituted by two methyl groups, and the other nitrogen is substituted by a 2-pyridyl group and a (2-thienyl)methyl group.methapyrilene
methapyrilene hydrochlorideA hydrochloride that is the monohydrochloride salt of methapyrilene.methapyrilene hydrochloride
mianserinA dibenzoazepine (specifically 1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine) methyl-substituted on N-2. Closely related to (and now mostly superseded by) the tetracyclic antidepressant mirtazapinean, it is an atypical antidepressant used in the treatment of depression throughout Europe and elsewhere.mianserin
mirtazapinemirtazapine
orphenadrineA tertiary amino compound which is the phenyl-o-tolylmethyl ether of 2-(dimethylamino)ethanol.orphenadrine
orphenadrine citrateA citrate salt which comprises equimolar amounts of orphenadrine and citric acid.orphenadrine citrate
orphenadrine hydrochlorideA hydrochloride comprising equimolar amounts of ophenadrine and hydrogen chloride.orphenadrine hydrochloride
oxatomideA member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one substituted by a 3-[4-(diphenylmethyl)piperazin-1-yl]propyl group at position 1. It is an anti-allergic drug.oxatomide
pimozideA member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group.pimozide
promazineA phenothiazine deriative in which the phenothiazine tricycle has a 3-(dimethylaminopropyl) group at the N-10 position.promazine
promethazineA tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety.promethazine
promethazine hydrochlorideThe hydrochloride salt of promethazine.promethazine hydrochloride
pyrilamineAn ethylenediamine derivative that is ethylenediamine in which one of the amino nitrogens is substituted by two methyl groups and the remaining amino nitrogen is substituted by a 4-methoxybenzyl and a pyridin-2-yl group.mepyramine
risperidoneA member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.risperidone
sertindoleA phenylindole that is 1H-indole which is substituted on the nitrogen by a p-chlorophenyl group, at position 5 by chlorine, and at position 3 by a piperidin-4-yl group, which is itself substituted on the nitrogen by a 2-(2-oxoimidazolidin-1-yl)ethyl group.sertindole
tau 284An organosulfonate salt obtained by combining equimolar amounts of bepotastine and benzenesulfonic acid. A topical, selective and non-sedating histamine (H1) receptor antagonist used for treatment of itching associated with allergic conjunctivitis.bepotastine besylate
thioridazineA phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position.thioridazine
trazodoneAn N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group.trazodone
trazodone hydrochlorideA hydrochloride salt prepared from equimolar amounts of trazodone and hydrogen chloride.trazodone hydrochloride
triprolidineAn N-alkylpyrrolidine that is acrivastine in which the pyridine ring is lacking the propenoic acid substituent. It is a sedating antihistamine that is used (generally as the monohydrochloride monohydrate) for the relief of the symptoms of uticaria, rhinitis, and various pruritic skin disorders.triprolidine
triprolidine hydrochloride anhydrousA hydrochloride resulting from the formal reaction of equimolar amounts of triprolidine and hydrogen chloride. Its monohydrate is used for the symptomatic relief of uticaria, rhinitis, and various pruritic skin disorders.triprolidine hydrochloride (anh.)
zuclopenthixolThe (Z)-isomer of clopenthixol.zuclopenthixol

Research

Studies (79,668)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199023,181 (29.10)18.7374
1990's9,564 (12.00)18.2507
2000's16,214 (20.35)29.6817
2010's21,639 (27.16)24.3611
2020's9,070 (11.38)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials9,588 (10.38%)5.53%
Reviews5,089 (5.51%)6.00%
Case Studies6,702 (7.25%)4.05%
Observational152 (0.16%)0.25%
Other70,866 (76.70%)84.16%

Protein Targets (438)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency26.109614
15-lipoxygenase, partialHomo sapiens (human)Potency20.483912
67.9K proteinVaccinia virusPotency15.7421210
acetylcholinesteraseHomo sapiens (human)Potency29.9099333
acid sphingomyelinaseHomo sapiens (human)Potency19.952611
activating transcription factor 6Homo sapiens (human)Potency42.336925
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency29.998019
alpha-galactosidaseHomo sapiens (human)Potency50.118711
Alpha-synucleinHomo sapiens (human)Potency10.134013
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency31.622811
AR proteinHomo sapiens (human)Potency27.93699126
aryl hydrocarbon receptorHomo sapiens (human)Potency21.140123
arylsulfatase AHomo sapiens (human)Potency15.0581113
ATAD5 protein, partialHomo sapiens (human)Potency20.7538311
Ataxin-2Homo sapiens (human)Potency26.3596222
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency20.6901111
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency35.2096216
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency7.563514
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency16.759618
Bloom syndrome protein isoform 1Homo sapiens (human)Potency38.2295214
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency54.576319
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency36.5137110
caspase-3Cricetulus griseus (Chinese hamster)Potency28.137416
caspase-3Homo sapiens (human)Potency36.5137110
Caspase-7Cricetulus griseus (Chinese hamster)Potency28.137416
Cellular tumor antigen p53Homo sapiens (human)Potency30.3347341
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency16.9550211
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency24.945918
Chain A, Beta-lactamaseEscherichia coli K-12Potency86.8325210
Chain A, CruzipainTrypanosoma cruziPotency34.201515
Chain A, Ferritin light chainEquus caballus (horse)Potency22.697313
Chain A, HADH2 proteinHomo sapiens (human)Potency24.833225
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency58.557315
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency31.840528
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency24.235118
Chain B, HADH2 proteinHomo sapiens (human)Potency24.833225
chaperonin GroELMethanococcus maripaludis S2Potency100.000011
chaperonin-containing TCP-1 beta subunit homologHomo sapiens (human)Potency52.487012
chromobox protein homolog 1Homo sapiens (human)Potency51.7538217
cytochrome P450 2C19 precursorHomo sapiens (human)Potency8.7224119
cytochrome P450 2C9 precursorHomo sapiens (human)Potency15.885916
cytochrome P450 2C9, partialHomo sapiens (human)Potency20.288418
cytochrome P450 2D6Homo sapiens (human)Potency3.8390130
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency6.7176133
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency7.5041229
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency15.8288221
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency33.2112112
D(1A) dopamine receptorHomo sapiens (human)Potency4.7098323
D(1A) dopamine receptorSus scrofa (pig)Potency15.137314
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency8.175614
DNA polymerase III, partialBacillus subtilisPotency23.778111
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency64.727416
DNA polymerase kappa isoform 1Homo sapiens (human)Potency15.323513
dopamine D1 receptorHomo sapiens (human)Potency0.075012
endonuclease IVEscherichia coliPotency20.632313
estrogen nuclear receptor alphaHomo sapiens (human)Potency30.313211133
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency30.9363327
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency30.85539125
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency26.6077253
EWS/FLI fusion proteinHomo sapiens (human)Potency17.8347429
eyes absent homolog 2 isoform aHomo sapiens (human)Potency22.387211
farnesoid X nuclear receptorHomo sapiens (human)Potency28.8175420
flap endonuclease 1Homo sapiens (human)Potency6.145414
Fumarate hydrataseHomo sapiens (human)Potency29.2232114
GVesicular stomatitis virusPotency20.288418
GABA theta subunitRattus norvegicus (Norway rat)Potency7.5873115
GALC proteinHomo sapiens (human)Potency13.742213
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency7.5873115
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency7.5873115
gemininHomo sapiens (human)Potency16.6810444
GLI family zinc finger 3Homo sapiens (human)Potency17.0757366
glp-1 receptor, partialHomo sapiens (human)Potency12.476819
GLS proteinHomo sapiens (human)Potency13.7670215
glucocerebrosidaseHomo sapiens (human)Potency20.085012
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency30.4966442
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency32.6130112
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency3.662611
Guanine nucleotide-binding protein GHomo sapiens (human)Potency39.810711
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency47.186814
heat shock protein beta-1Homo sapiens (human)Potency36.8727215
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency15.0435260
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency31.767215
Histone H2A.xCricetulus griseus (Chinese hamster)Potency62.5084217
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency55.302612
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency20.288418
huntingtin isoform 2Homo sapiens (human)Potency31.2354210
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency28.6898212
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency11.6045222
IDH1Homo sapiens (human)Potency20.835716
importin subunit beta-1 isoform 1Homo sapiens (human)Potency3.662611
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency20.2884116
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency4.9934222
Integrin alpha-IIbHomo sapiens (human)Potency23.110313
Integrin beta-3Homo sapiens (human)Potency23.110313
Interferon betaHomo sapiens (human)Potency21.5651320
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency50.118711
lamin isoform A-delta10Homo sapiens (human)Potency13.8354235
lethal factor (plasmid)Bacillus anthracis str. A2012Potency13.6103111
LuciferasePhotinus pyralis (common eastern firefly)Potency30.747224
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency21.039126
M-phase phosphoprotein 8Homo sapiens (human)Potency27.763019
Microtubule-associated protein tauHomo sapiens (human)Potency19.8353115
mitogen-activated protein kinase 1Homo sapiens (human)Potency20.7911216
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency6.9761227
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency21.039113
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency21.039113
neuropeptide S receptor isoform AHomo sapiens (human)Potency12.8481313
NFKB1 protein, partialHomo sapiens (human)Potency13.320726
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency17.681414
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency58.047912
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency27.5667435
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency22.780814
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency30.300112
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency30.1837215
Nuclear receptor ROR-gammaHomo sapiens (human)Potency0.595611
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency25.0795213
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency32.5187340
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency0.025111
P53Homo sapiens (human)Potency70.794611
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency44.668412
ParkinHomo sapiens (human)Potency31.460022
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency52.387722
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency20.4701218
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency65.8443110
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency25.1013532
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency33.3738539
phosphopantetheinyl transferaseBacillus subtilisPotency61.8452317
PINK1Homo sapiens (human)Potency39.810711
plasminogen precursorMus musculus (house mouse)Potency7.809915
polyproteinZika virusPotency29.2232114
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency14.6825121
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency9.0836137
PPM1D proteinHomo sapiens (human)Potency16.648614
pregnane X nuclear receptorHomo sapiens (human)Potency21.0735334
pregnane X receptorRattus norvegicus (Norway rat)Potency50.118712
progesterone receptorHomo sapiens (human)Potency30.8472223
pyruvate kinase PKM isoform bHomo sapiens (human)Potency0.025122
RAR-related orphan receptor gammaMus musculus (house mouse)Potency21.5571235
ras-related protein Rab-9AHomo sapiens (human)Potency74.828715
regulator of G-protein signaling 4Homo sapiens (human)Potency23.6592110
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency29.6881359
retinoid X nuclear receptor alphaHomo sapiens (human)Potency18.6247435
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency18.5203415
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency26.679511
SMAD family member 2Homo sapiens (human)Potency24.4831215
SMAD family member 3Homo sapiens (human)Potency24.4831215
Smad3Homo sapiens (human)Potency17.147513
snurportin-1Homo sapiens (human)Potency3.662611
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency24.1974229
survival motor neuron protein isoform dHomo sapiens (human)Potency17.4774114
TAR DNA-binding protein 43Homo sapiens (human)Potency4.999214
TDP1 proteinHomo sapiens (human)Potency17.0138282
thioredoxin glutathione reductaseSchistosoma mansoniPotency38.750614
thioredoxin reductaseRattus norvegicus (Norway rat)Potency23.3241325
ThrombopoietinHomo sapiens (human)Potency10.8657212
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency22.7820384
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency25.309223
thyroid stimulating hormone receptorHomo sapiens (human)Potency25.4347649
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency14.823022
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency16.976515
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency23.735812
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency8.175614
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency7.809915
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency7.809915
USP1 protein, partialHomo sapiens (human)Potency38.5538318
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency17.8045254
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency27.8624421
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency64.813818
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency32.6130112

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
1-acylglycerol-3-phosphate O-acyltransferase ABHD5 isoform aHomo sapiens (human)IC5027.427855
3-hydroxy-3-methylglutaryl-coenzyme A reductase Rattus norvegicus (Norway rat)Ki0.018713
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC500.398122
5-hydroxytryptamine receptor 1AMus musculus (house mouse)IC500.430011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC501.6391212
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.11662329
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.6244919
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC501.6391212
5-hydroxytryptamine receptor 1BHomo sapiens (human)Ki0.056011
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki1.1202413
5-hydroxytryptamine receptor 1DHomo sapiens (human)IC500.380222
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC502.675012
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.840022
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC502.675012
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.840022
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.3218926
5-hydroxytryptamine receptor 2AMus musculus (house mouse)IC500.001511
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.31911519
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.02525279
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.00341822
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.5732118
5-hydroxytryptamine receptor 2BMus musculus (house mouse)IC500.001511
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.41871113
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.2769624
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.003244
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.3723725
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.41871113
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.08632753
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.01581012
5-hydroxytryptamine receptor 2C Mus musculus (house mouse)IC500.001511
5-hydroxytryptamine receptor 2C Mus musculus (house mouse)Ki0.011011
5-hydroxytryptamine receptor 3ACavia porcellus (domestic guinea pig)IC50630.000011
5-hydroxytryptamine receptor 3AHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3AMus musculus (house mouse)IC501.412511
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC502.675012
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki1.700622
5-hydroxytryptamine receptor 3AMus musculus (house mouse)Ki0.252011
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.070011
5-hydroxytryptamine receptor 3BHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3BMus musculus (house mouse)IC501.412511
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC502.675012
5-hydroxytryptamine receptor 3BHomo sapiens (human)Ki0.501211
5-hydroxytryptamine receptor 3BMus musculus (house mouse)Ki0.252011
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.070011
5-hydroxytryptamine receptor 3CHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3CHomo sapiens (human)Ki0.501211
5-hydroxytryptamine receptor 3DHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3DHomo sapiens (human)Ki0.501211
5-hydroxytryptamine receptor 3EHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3EHomo sapiens (human)Ki0.501211
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.3213116
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.1638217
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)IC502.675012
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)IC502.675012
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)IC502.675012
5-hydroxytryptamine receptor 6Homo sapiens (human)IC501.2734111
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)IC502.675012
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.60541530
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5025.3200110
5-hydroxytryptamine receptor 7Homo sapiens (human)IC500.114811
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.47451319
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)IC502.675012
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.049337
6-phosphogluconate dehydrogenase, decarboxylatingHomo sapiens (human)Ki8.300011
Adenosine receptor A3Homo sapiens (human)IC5029.120011
Adenosine receptor A3Homo sapiens (human)Ki16.461011
AlbuminHomo sapiens (human)IC503.500012
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC501.8781112
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki1.8624112
Alpha-1A adrenergic receptorHomo sapiens (human)IC500.4127811
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC503.0142910
Alpha-1A adrenergic receptorBos taurus (cattle)Ki0.000433
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.0207912
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.82761623
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC503.767788
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.0236810
Alpha-1B adrenergic receptorMesocricetus auratus (golden hamster)Ki0.000333
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.94791420
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.6314112
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC500.169766
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.2004619
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.11361622
Alpha-2A adrenergic receptorHomo sapiens (human)IC500.9479419
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC500.122722
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.3756623
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.030233
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.9201317
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC500.122722
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.5115418
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.032822
Alpha-2C adrenergic receptorHomo sapiens (human)IC500.6168515
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC500.122722
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.1822618
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.032822
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC5016.829518
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki11.0370210
Angiotensin-converting enzymeRattus norvegicus (Norway rat)Ki0.259016
Angiotensin-converting enzyme 2 Homo sapiens (human)IC5013.645012
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.0000115
ATP-dependent translocase ABCB1Homo sapiens (human)IC509.7650712
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC5014.475048
Beta-1 adrenergic receptorHomo sapiens (human)IC5017.382011
Beta-1 adrenergic receptorHomo sapiens (human)Ki10.037011
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki22.000011
Beta-3 adrenergic receptorHomo sapiens (human)IC508.060011
Beta-3 adrenergic receptorHomo sapiens (human)Ki6.045011
Bile acid receptorHomo sapiens (human)IC503.070011
Bile salt export pumpHomo sapiens (human)IC50284.2669542
Bile salt export pumpRattus norvegicus (Norway rat)IC501,000.000012
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC506.600011
Calcium release-activated calcium channel protein 1Homo sapiens (human)IC50500.000022
Calmodulin-1Homo sapiens (human)IC5060.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.0000113
Cathepsin D Bos taurus (cattle)IC500.060011
Chloroquine resistance transporterPlasmodium falciparum (malaria parasite P. falciparum)IC5069.500012
CruzipainTrypanosoma cruziIC50212.000022
Cytochrome P450 1A2Homo sapiens (human)IC509.332311
Cytochrome P450 2C19Homo sapiens (human)IC502.331313
Cytochrome P450 2C9 Homo sapiens (human)IC5050.000013
Cytochrome P450 2D6Homo sapiens (human)IC502.335529
Cytochrome P450 2D6Homo sapiens (human)Ki0.050111
Cytochrome P450 2J2Homo sapiens (human)IC5050.000013
Cytochrome P450 3A4Homo sapiens (human)IC506.500012
Cytochrome P450 3A4Homo sapiens (human)Ki0.232327
DBos taurus (cattle)IC500.130011
DRattus norvegicus (Norway rat)IC500.3277611
DRattus norvegicus (Norway rat)Ki0.6573612
D(1A) dopamine receptorHomo sapiens (human)IC501.444319
D(1A) dopamine receptorHomo sapiens (human)Ki0.58061020
D(1B) dopamine receptorRattus norvegicus (Norway rat)IC500.281538
D(1B) dopamine receptorHomo sapiens (human)Ki1.600022
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki0.063011
D(2) dopamine receptorBos taurus (cattle)IC500.130011
D(2) dopamine receptorHomo sapiens (human)IC501.35731119
D(2) dopamine receptorMus musculus (house mouse)IC500.023012
D(2) dopamine receptorRattus norvegicus (Norway rat)IC500.37801626
D(2) dopamine receptorHomo sapiens (human)Ki0.15435269
D(2) dopamine receptorMus musculus (house mouse)Ki0.112011
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.22001627
D(3) dopamine receptorHomo sapiens (human)IC501.4233314
D(3) dopamine receptorRattus norvegicus (Norway rat)IC500.281538
D(3) dopamine receptorHomo sapiens (human)Ki0.27142948
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.539633
D(4) dopamine receptorHomo sapiens (human)IC503.544434
D(4) dopamine receptorRattus norvegicus (Norway rat)IC500.281538
D(4) dopamine receptorHomo sapiens (human)Ki0.20271923
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.286522
Delta-type opioid receptorHomo sapiens (human)IC508.369522
Delta-type opioid receptorHomo sapiens (human)Ki4.575011
DNA damage-inducible transcript 3 proteinMus musculus (house mouse)IC506.340011
DNA gyrase subunit AStaphylococcus aureusIC50500.000011
DNA gyrase subunit BStaphylococcus aureusIC50500.000011
Endothelin receptor type BHomo sapiens (human)Ki0.056624
Endothelin receptor type BRattus norvegicus (Norway rat)Ki0.056612
Endothelin-1 receptorHomo sapiens (human)IC500.114811
Epidermal growth factor receptorHomo sapiens (human)IC504.502012
Estrogen receptor 1Homo sapiens (human)IC5050.000011
estrogen receptor beta isoform 1Homo sapiens (human)IC5050.000011
G-protein coupled receptor Apis mellifera (honey bee)IC5073.000011
GABA theta subunitRattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC501.000014
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC501.000011
Glucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)Ki5.200011
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)Ki6.000011
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)Ki6.000011
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)Ki6.000011
Glutamate receptor ionotropic, NMDA 2CHomo sapiens (human)Ki6.000011
Glutamate receptor ionotropic, NMDA 2DHomo sapiens (human)Ki6.000011
Glutamate receptor ionotropic, NMDA 3AHomo sapiens (human)Ki6.000011
Glutamate receptor ionotropic, NMDA 3BHomo sapiens (human)Ki6.000011
Glutathione reductase, mitochondrialHomo sapiens (human)Ki0.800011
Glycogen phosphorylase, brain formHomo sapiens (human)Ki0.004011
Glycogen phosphorylase, muscle formHomo sapiens (human)Ki0.004011
hepatocyte nuclear factor 4-alpha isoform 2Homo sapiens (human)IC5039.841022
Histamine H1 receptorCavia porcellus (domestic guinea pig)IC500.001511
Histamine H1 receptorHomo sapiens (human)IC501.98542954
Histamine H1 receptorRattus norvegicus (Norway rat)IC500.017338
Histamine H1 receptorCavia porcellus (domestic guinea pig)Ki0.041423
Histamine H1 receptorHomo sapiens (human)Ki6,960,930,555,555.58904572
Histamine H1 receptorRattus norvegicus (Norway rat)Ki501,187,000,000,000.000011
Histamine H2 receptorCavia porcellus (domestic guinea pig)IC502.340012
Histamine H2 receptorHomo sapiens (human)IC501.9912111
Histamine H2 receptorHomo sapiens (human)Ki1.9580111
Histamine H3 receptorHomo sapiens (human)Ki1.486856
Histamine H3 receptorRattus norvegicus (Norway rat)Ki5.000011
Histamine H4 receptorHomo sapiens (human)Ki11.2648310
Histone-lysine N-methyltransferase SETD7Homo sapiens (human)IC508.133333
Histone-lysine N-methyltransferase SETD7Homo sapiens (human)Ki15.000011
Kappa-type opioid receptorHomo sapiens (human)IC503.365323
Kappa-type opioid receptorHomo sapiens (human)Ki1.821012
Lethal(3)malignant brain tumor-like protein 1Homo sapiens (human)IC5041.000011
Lethal(3)malignant brain tumor-like protein 3Homo sapiens (human)IC5042.000011
Lethal(3)malignant brain tumor-like protein 4Homo sapiens (human)IC50100.000011
MBT domain-containing protein 1Homo sapiens (human)IC5034.000011
Melanocortin receptor 3Homo sapiens (human)IC5015.525011
Melanocortin receptor 3Homo sapiens (human)Ki13.549011
Melanocortin receptor 4Homo sapiens (human)IC5014.041011
Melanocortin receptor 4Homo sapiens (human)Ki13.501011
Melanocortin receptor 5Homo sapiens (human)IC502.263011
Melanocortin receptor 5Homo sapiens (human)Ki2.123011
Mu-type opioid receptorHomo sapiens (human)IC501.378723
Mu-type opioid receptorHomo sapiens (human)Ki0.764012
Mucosa-associated lymphoid tissue lymphoma translocation protein 1Homo sapiens (human)IC503.765022
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50174.871427
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC50284.160025
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.0000115
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC501.3683214
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC500.106011
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki1.1010619
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.004011
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC500.7455112
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC500.106011
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.8313416
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki0.004011
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC5013.6152316
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC500.106011
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.6896417
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki0.004011
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.8236113
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC500.106011
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.6794417
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki0.004011
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.4733114
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC501.003022
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.8218418
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki0.004011
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC5016.829518
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki13.788018
P2X purinoceptor 7Homo sapiens (human)IC500.830011
perilipin-1Homo sapiens (human)IC5027.799022
perilipin-5Homo sapiens (human)IC5024.324544
Platelet-activating factor receptorHomo sapiens (human)IC50135.000011
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CIC5010.100013
Polycomb protein EEDHomo sapiens (human)IC5093.800011
Polycomb protein EEDHomo sapiens (human)Ki23.010011
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC50100.000011
Potassium channel subfamily K member 2Homo sapiens (human)IC501.800011
Potassium channel subfamily K member 9Homo sapiens (human)IC5063.400011
Potassium voltage-gated channel subfamily A member 5Homo sapiens (human)IC502.000011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC508.673953141
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki6.57051221
Procathepsin LHomo sapiens (human)IC5013.645012
Prostaglandin G/H synthase 1Ovis aries (sheep)Ki0.080812
Protein farnesyltransferase subunit betaHomo sapiens (human)IC5065.000011
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)IC5065.000011
Protein orai-2Homo sapiens (human)IC50500.000022
Protein orai-3Homo sapiens (human)IC50500.000022
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)IC5013.084011
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusIC5013.645012
Replicase polyprotein 1abBetacoronavirus England 1IC5013.645012
Replicase polyprotein 1abHuman coronavirus 229EIC5013.645012
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC5011.326723
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC5013.645012
Sigma intracellular receptor 2Homo sapiens (human)Ki0.071913
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.875218
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)IC500.750011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.4980211
Sodium channel protein type 1 subunit alphaHomo sapiens (human)IC501.177022
Sodium channel protein type 10 subunit alphaHomo sapiens (human)IC501.177022
Sodium channel protein type 11 subunit alphaHomo sapiens (human)IC501.177022
Sodium channel protein type 2 subunit alphaHomo sapiens (human)IC501.177022
Sodium channel protein type 2 subunit alphaRattus norvegicus (Norway rat)IC500.340011
Sodium channel protein type 3 subunit alphaHomo sapiens (human)IC501.177022
Sodium channel protein type 4 subunit alphaHomo sapiens (human)IC501.177022
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC5024.784066
Sodium channel protein type 7 subunit alphaHomo sapiens (human)IC501.177022
Sodium channel protein type 8 subunit alphaHomo sapiens (human)IC501.177022
Sodium channel protein type 9 subunit alphaHomo sapiens (human)IC501.177022
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC501.811836
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki2.826645
Sodium-dependent dopamine transporter Homo sapiens (human)IC5017.0747613
Sodium-dependent dopamine transporter Homo sapiens (human)Ki1.1751312
Sodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)IC5088.000012
Sodium-dependent noradrenaline transporterMus musculus (house mouse)Ki0.290011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC500.80671728
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.83021628
Sodium-dependent serotonin transporterHomo sapiens (human)IC501.1765616
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC505.000035
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.7600919
Sodium-dependent serotonin transporterMus musculus (house mouse)Ki4.100011
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.163011
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)IC5018.500023
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Ki2.800011
Solute carrier family 22 member 1 Homo sapiens (human)IC5033.682937
Solute carrier family 22 member 1 Homo sapiens (human)Ki5.360011
Solute carrier family 22 member 2Homo sapiens (human)IC5058.200025
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)IC5022.666723
Solute carrier family 22 member 2Homo sapiens (human)Ki16.000011
Solute carrier family 22 member 3Rattus norvegicus (Norway rat)IC5068.000011
Solute carrier family 22 member 3Homo sapiens (human)Ki14.000011
Solute carrier family 22 member 4Rattus norvegicus (Norway rat)IC5080.000011
Somatostatin receptor type 2Homo sapiens (human)Ki10.000011
Somatostatin receptor type 3Homo sapiens (human)Ki10.000011
Somatostatin receptor type 4Homo sapiens (human)Ki10.000011
Somatostatin receptor type 5Homo sapiens (human)Ki4.070022
Spike glycoproteinBetacoronavirus England 1IC5013.645012
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusIC5013.645012
Substance-K receptorHomo sapiens (human)IC502.986011
Substance-K receptorHomo sapiens (human)Ki0.995011
Substance-P receptorHomo sapiens (human)IC5015.793011
Substance-P receptorHomo sapiens (human)Ki8.615011
Transmembrane protease serine 2Homo sapiens (human)IC5013.645012
TransporterRattus norvegicus (Norway rat)IC503.266347
TransporterRattus norvegicus (Norway rat)Ki4.438458
Trypanothione reductaseTrypanosoma cruziIC50189.500012
Trypanothione reductaseTrypanosoma cruziKi137.550012
Tryptophan 5-hydroxylase 1Rattus norvegicus (Norway rat)IC500.060011
Tryptophan 5-hydroxylase 1Rattus norvegicus (Norway rat)Ki0.000511
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)IC500.210011
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)Ki0.259012
Tyrosine-protein kinase FynHomo sapiens (human)IC503.948512
Tyrosine-protein kinase LckHomo sapiens (human)IC5019.920011
Ubiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)IC502.000022
ubiquitin-conjugating enzyme E2 NHomo sapiens (human)IC5020.000011
Voltage-dependent L-type calcium channel subunit alpha-1CCavia porcellus (domestic guinea pig)IC503.215024
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC5019.21221010
Voltage-dependent L-type calcium channel subunit alpha-1CRattus norvegicus (Norway rat)Ki1.080011
Voltage-dependent L-type calcium channel subunit alpha-1DRattus norvegicus (Norway rat)Ki1.080011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC508.225388
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC508.225388
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC508.225388
Voltage-dependent L-type calcium channel subunit alpha-1SRattus norvegicus (Norway rat)Ki1.080011
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC5014.500012
WD repeat-containing protein 48Homo sapiens (human)IC502.000011
XBP1Homo sapiens (human)IC5010.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)EC502.773544
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd1.936013
5-hydroxytryptamine receptor 2AMus musculus (house mouse)EC508.393011
AlbuminHomo sapiens (human)Kd851.138011
AlbuminRattus norvegicus (Norway rat)Kd19.480013
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd1.974022
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kd1.974022
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd1.974022
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Kd1.095822
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Kd1.095822
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Kd1.095822
Angiopoietin-1 receptorHomo sapiens (human)Kd90.000011
Angiotensin-converting enzyme 2 Homo sapiens (human)EC508.842015
Calmodulin Bos taurus (cattle)Kd50.000011
D(2) dopamine receptorHomo sapiens (human)EC500.82222328
D(2) dopamine receptorHomo sapiens (human)Kd0.029011
D(3) dopamine receptorHomo sapiens (human)EC500.019824
Glycine receptor subunit alpha-1Homo sapiens (human)EC502.073313
HeparanaseHomo sapiens (human)Kd1,000.000011
Histamine H1 receptorHomo sapiens (human)EC500.002611
Histamine H1 receptorCavia porcellus (domestic guinea pig)Kd0.072422
Histamine H1 receptorHomo sapiens (human)Kd0.802167
HLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)Kd2.500012
Major prion proteinHomo sapiens (human)EC506.500012
mu-type opioid receptor isoform MOR-1Homo sapiens (human)EC5092.469011
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC506.812558
Nuclear receptor subfamily 1 group I member 2Rattus norvegicus (Norway rat)EC5025.100011
Potassium channel subfamily K member 2Homo sapiens (human)EC500.354011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)EC500.001911
Procathepsin LHomo sapiens (human)EC508.842015
Proteasome subunit alpha type-6Homo sapiens (human)EC5012.000011
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC508.842015
Replicase polyprotein 1abBetacoronavirus England 1EC508.842015
Replicase polyprotein 1abHuman coronavirus 229EEC508.842015
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC508.842015
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC508.842015
short transient receptor potential channel 6 isoform 1Mus musculus (house mouse)EC5015.850011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Kd0.000811
Spike glycoproteinBetacoronavirus England 1EC508.842015
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC508.842015
Transmembrane protease serine 2Homo sapiens (human)EC508.842015
Voltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)Kd0.040011
voltage-dependent T-type calcium channel subunit alpha-1H isoform aHomo sapiens (human)EC505.150011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 6Homo sapiens (human)Kb0.030011
Aldehyde oxidaseHomo sapiens (human)Kii1.300011
Aldehyde oxidaseHomo sapiens (human)Kis1.300011
Alpha-1A adrenergic receptorHomo sapiens (human)Activity0.001011
Alpha-1B adrenergic receptorHomo sapiens (human)Activity0.003211
Alpha-1D adrenergic receptorHomo sapiens (human)Activity0.009011
ATP-dependent translocase ABCB1Homo sapiens (human)Km12.400011
Cytochrome P450 2J2Homo sapiens (human)Km0.090011
FAD-linked sulfhydryl oxidase ALRHomo sapiens (human)AC500.367011
Histamine H1 receptorCavia porcellus (domestic guinea pig)K0.50.003312
Histamine H1 receptorHomo sapiens (human)Kb0.000311
Histamine H2 receptorCavia porcellus (domestic guinea pig)K0.50.0151223
Histamine H3 receptorCavia porcellus (domestic guinea pig)K0.50.003312
Histamine N-methyltransferaseHomo sapiens (human)Activity0.010011
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CINH132.666713
Snq2pSaccharomyces cerevisiae EC1118INH89.133313
Solute carrier organic anion transporter family member 1A1Rattus norvegicus (Norway rat)Km32.000011
Solute carrier organic anion transporter family member 1A2Homo sapiens (human)Km6.400011
Solute carrier organic anion transporter family member 1A4Rattus norvegicus (Norway rat)Km6.000011
UDP-glucuronosyltransferase 1A3Homo sapiens (human)Km196.000013
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km85.400025