Page last updated: 2024-08-05 14:58:32

serotonergic antagonist

Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or serotonergic agonists.

ChEBI ID: 48279

Members (70)

MemberDefinitionClass
1-(2-(4-(4-fluoro-benzoyl)-piperidin-1-yl)-ethyl)-3,3-dimethyl-1,2-dihydro-indol-2-oneA hydrochloride resulting from the formal reation of equimolar amount of LY-310762 with hydrogen chloride. A potent and selective antagonist for the 5-hydroxytryptamine 1D (5-HT1D) receptor.LY-310762 hydrochloride
1-(2-methoxyphenyl)-4-(4-(2-phthalimido)butyl)piperazineA hydrobromide obtained by reaction of NAN 190 with one equivalent of hydrobromic acid.NAN 190 hydrobromide
1-methyl-d-lysergic acid butanolamideA synthetic ergot alkaloid, structurally related to the oxytocic agent methylergonovine and to the potent hallucinogen LSD and used prophylactically to reduce the frequency and intensity of severe vascular headaches.methysergide
3alpha-hydroxy-4alpha-methylergosta-8,24(28)-dien-7,11-dione-26-oic acidA 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
8-hydroxy-2-(di-n-propylamino)tetralinA tetralin substituted at positions 1 and 7 by hydroxy and dipropylamino groups respectively8-OH-DPAT
alosetronA pyrido[4,3-b]indole compound having a 5-methyl-1H-imidazol-4-ylmethyl group at the 2-position.alosetron
alosetron hydrochlorideThe hydrochloride salt of alosetron.alosetron hydrochloride
amperozideA member of the class of ureas that is urea in which three of the four hydrogens are replaced by ethyl and 4-[4,4-bis(4-fluorophenyl)butyl]piperazin-1-yl groups. An atypical antipsychotic which was in clinical development for the treatment of schizophrenia and substance-related disorders. It is a potent 5-HT2A antagonist and used in veterinary medicine because of its sedative effect on pigs.amperozide
amperozide hydrochlorideThe hydrochloride salt of amperozide.amperozide hydrochloride
brl 15572An N-alkylpiperazine that is 1-(3-chlorophenyl)piperazine carrying a 3,3-diphenyl-2-hydroxyprop-1-yl group at position 4. A selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.3-[4-(3-chlorophenyl)piperazin-1-yl]-1,1-diphenylpropan-2-ol
brl 15572A hydrochloride that is the monohydrochloride salt of 3-[4-(3-chlorophenyl)piperazin-1-yl]-1,1-diphenylpropan-2-ol. A selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.3-[4-(3-chlorophenyl)piperazin-1-yl]-1,1-diphenylpropan-2-ol hydrochloride
clomipramineA dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressants, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias.clomipramine
clomipramine hydrochlorideA hydrochloride resulting from the reaction of equimolar amounts of clomipramine and hydrogen chloride. One of the more sedating tricyclic antidepressants, it is used for the treatment of depression as well as obsessive-compulsive disorder and phobias.clomipramine hydrochloride
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
clozapineA benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.clozapine
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
dotarizineAn N-alkylpiperazine in which the two amino hydrogens of piperazine have been replaced by diphenylmethyl and 3-(2-phenyl-1,3-dioxolan-2-yl)propyl groups. A calcium channel blocker and serotonin (5-HT2) receptor antagonist used in the treatment of migraine.dotarizine
fk 1052An organic heterotricyclic compound that is 8,9-dihydropyrido[1,2-a]indol-6(7H)-one substituted by a (5-methyl-1H-imidazol-4-yl)methyl group at position 7R and a methyl group at position 10. It is a dual 5-HT3 and 5-HT4 receptors antagonist whose clinical development was terminated in phase II. It was being developed for the treatment of chemotherapy-induced emesis and irritable bowel syndrome.fabesetron
flibanserinAn N-alkylpiperazine that is 1-[2-(1,3-dihydro-2-oxobenzimidazol-1-yl)ethyl]piperazine in which the remaining amino proton is replaced by a 3-(trifluoromethyl)phenyl group. A multifunctional serotonin agonist and antagonist which is used for the treatment of pre-menopausal women with hypoactive sexual desire disorder.flibanserin
gr 113808An indolyl carboxylate ester obtained by formal condensation between the carboxy group of 1-methylindole-3-carboxylic acid with the hydroxy group of N-{2-[4-(hydroxymethyl)piperidin-1-yl]ethyl}methanesulfonamide.GR 113808
GR 127935 hydrochlorideA hydrochloride obtained by reaction of GR 127935 with one equivalent of hydrochloric acid. Potent and selective 5-HT1B/1D receptor antagonist (pKi values are 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptors). Displays > 100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types. Centrally active following oral administration.GR 127935 hydrochloride
gramineAn aminoalkylindole that is indole carrying a dimethylaminomethyl substituent at postion 3.gramine
haloperidolA compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.haloperidol
hp 873A member of the class of piperidines that is the 4-acetyl-2-methoxyphenyl ether of 3-(piperidin-1-yl)propan-1-ol which is substituted at position 4 of the piperidine ring by a 6-fluoro-1,2-benzoxazol-3-yl group. A member of the group of second generation antipsychotics (also known as an atypical antipsychotics), it is used for the treatment of schizophrenia.iloperidone
ketanserinA member of the class of quinazolines that is quinazoline-2,4(1H,3H)-dione which is substituted at position 3 by a 2-[4-(p-fluorobenzoyl)piperidin-1-yl]ethyl group.ketanserin
lurasidoneAn N-arylpiperazine that is (3aR,4S,7R,7aS)-2-{[(1R,2R)-2-(piperazin-1-ylmethyl)cyclohexyl]methyl}hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione in which position N4 of the piperazine ring is substituted by a 1,2-benzothiazol-3-yl group. Lurasidone is used (generally as the hydrochloride salt) as an atypical antipsychotic for the treatment of schizophrenia.lurasidone
lurasidone hydrochlorideA hydrochloride obtained by reaction of lurasidone with one equivalent of hydrochloric acid. An atypical antipsychotic agent used for the treatment of schizophrenia.lurasidone hydrochloride
ly 367265A fluoroindole that is 1H-indole in which the hydrogens at positions 3 and 6 are replaced by 1-[2-(2,2-dioxo-5,6-dihydro-4H-2lambda(6)-[1,2,5]thiadiazolo[4,3,2-ij]quinolin-1(2H)-yl)ethyl]-1,2,3,6-tetrahydropyridin-4-yl and fluoro groups, respectively. It is an inhibitor of the 5-hydroxytryptamine transporter (Ki = 2.3 nM) and an antagonist of 5-hydroxytryptamine(2A) receptor (Ki = 0.81 nM).LY-367,265
LY-310762A member of the class of oxindoles that is 1-ethyl-3,3-dimethyl-1,3-dihydro-2H-indol-2-one in which the ethyl group has been substituted at position 2 by a 4-(p-fluorobenzoyl)piperidin-1-yl group. It is a potent and selective antagonist for the 5-hydroxytryptamine 1D (5-HT1D) receptor.LY-310762
mesulergineA member of the class of ergot alkaloids that is known to act on serotonin and dopamine receptors.mesulergine
metergolineAn ergoline alkaloid that is the N-benzyloxycarbonyl derivative of lysergamine. A 5-HT2 antagonist. Also 5-HT1 antagonist and 5-HT1D ligand. Has moderate affinity for 5-HT6 and high affinity for 5-HT7.metergoline
methiothepinA dibenzothiepine that is 10,11-dihydrodibenzo[b,f]thiepine bearing additional methylthio and 4-methylpiperazin-1-yl substituents at positions 8 and 10 respectively. Potent 5-HT2 antagonist, also active as 5-HT1 antagonist. Differentiates 5-HT1D sub-types. Also displays affinity for rodent 5-HT5B, 5-HT5A, 5-HT7 and 5-HT6 receptors (pK1 values are 6.6, 7.0, 8.4 and 8.7 respectively).methiothepin
methotrimeprazineA 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
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
n-(1-methyl-5-indolyl)-n'-(3-methyl-5-isothiazolyl)ureaA member of ther class of ureas that is urea in which a hydrogen attached to one of the nitrogens has been replaced by an N-methylindol-5-yl group, while a hydrogen attached to the other nitrogen has been replaced by a 3-methyl-1,2-thiazol-5-yl group. It is a potent and selective antagonist for the 5-hydroxytryptamine 2B (5-HT2B) receptor.1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea
nan 190An N-alkylpiperazine that consists of (2-methoxyphenyl)piperazine in which the amine hydrogen is substituted by a 4-(2-phthalimido)butyl group.NAN 190
nefazodonenefazodone
norclozapineA dibenzodoazepine substituted with chloro and piperazino groups which is a major metabolite of clozapine; a potent and selective 5-HT2C serotonin receptor antagonist.N-desmethylclozapine
olanzapineA benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.olanzapine
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
palonosetronAn organic heterotricyclic compound that is an antiemetic used (as its hydrochloride salt) in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy.palonosetron
picrotoxininA picrotoxane sesquiterpenoid that is 3a,4,5,6,7,7a-hexahydro-1H-indene-3,7-dicarboxylic acid which is substituted at positions 3a, 6, and 7a by methyl, isopropenyl, and hydroxy groups, respectively; in which the double bond at position 2-3 has been epoxidised; and in which the carboxy groups at positions 3 and 7 have undergone gamma-lactone formation by O-alkylation to positions 4 and 5, respectively. A component of picrotoxin.picrotoxinin
pimavanserinA member of the class of ureas in which three of the four hydrogens are replaced by 4-fluorobenzyl, 1-methylpiperidin-4-yl, and 4-(isopropyloxy)benzyl groups. An atypical antipsychotic that is used (in the form of its tartrate salt) for treatment of hallucinations and delusions associated with Parkinson's disease.pimavanserin
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
pindololA member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol.pindolol
pipamperoneA member of the class of bipiperidines that is 1,4'-bipiperidine which is substituted at the 1' and 4' positions by 4-(p-fluorophenyl)-4-oxobutyl and carboxamide groups, respectively. A first generation antipsychotic, its properties are generally similar to those of haloperidol.pipamperone
pipamperone dihydrochlorideA hydrochloride resulting from the reaction of pipamperone with 2 mol eq. of hydrogen chloride. It is used as an antipsychotic.pipamperone dihydrochloride
pizotylineA benzocycloheptathiophene that is 9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophene 4-ylidene)-1-methylpiperidine which is joined from the 4 position to the 4 position of an N-methylpiperidine moiety by a double bond. It is a sedating antihistamine, with strong serotonin antagonist and weak antimuscarinic activity. It is generally used as the malate salt for the treatment of migraine and the prevention of headache attacks during cluster periods.pizotifen
promazineA phenothiazine deriative in which the phenothiazine tricycle has a 3-(dimethylaminopropyl) group at the N-10 position.promazine
propiomazineA member of the class of phenothiazines that is 10H-phenothiazine substituted by a 2-(dimethylamino)propyl group at nitrogen atom and a propanoyl group at position 2.propiomazine
quetiapinequetiapine
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
ritanserinA thiazolopyrimidine that is 5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one which is substituted at position 7 by a methyl group and at position 6 by a 2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl group. A potent and long-acting seratonin (5-hydroxytryptamine, 5-HT) antagonist of the subtype 5-HT2 (Ki = 0.39 nM), it is used in the treatment of a variety of disorders including anxiety, depression and schizophrenia. It has little sedative action.ritanserin
rs 25259-197A hydrochloride obtained by combining palonosetron with one molar equivalent of hydrogen chloride; an antiemetic used in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy.palonosetron hydrochloride
rs 39604A hydrochloride salt obtained by mixing equimolar amounts of RS 39604 with hydrochloric acid. A potent and selective 5-HT4 antagonist, with a pKi of 9.1 at 5-HT4 receptors in guinea pig striatal membranes and greater than 1000-fold selectivity over 5-HT1A, 2C, 3 and D1, D2, M1, M2, AT1, B1 and alpha1C receptors. The ketone group gives RS 39604 a relatively long half life; it is also orally active and so suitable for in vivo studies.RS 39604 hydrochloride
sb-224289A member of the class of benzamides obtained by formal condensation of the carboxy group of 2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-carboxylic acid with the secondary amino group of 1'-methyl-6,7-dihydro-5H-spiro[furo[2,3-f]indole-3,4'-piperidine]. Selective 5-HT1B receptor antagonist (pKi = 8.2). Displays >60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C receptors in radioligand binding and functional assays. Centrally active following oral administration in vivo.SB 224289
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
setiptilineA tetracyclic antidepressant that is 2,3,4,9-tetrahydro-1H-dibenzo[3,4:6,7]cyclohepta[1,2-c]pyridine carrying a methyl group at position 2. Its maleate salt is used for the treatment of depression in Japan.setiptiline
spiperoneAn azaspiro compound that is 1,3,8-triazaspiro[4.5]decane which is substituted at positions 1, 4, and 8 by phenyl, oxo, and 4-(p-fluorophenyl)-4-oxobutyl groups, respectively.spiperone
spiramideAn azaspiro compound that consists of 1,3,8-triazaspiro[4.5]decan-4-one having a phenyl group attached to N-1 and a 3-(4-fluorophenoxy)propyl attached to N-8. Selective 5-HT antagonist, which binds to 5-HT2 sites as potently as spiperone but has lower affinity for 5-HT2C receptors. Also a high affinity D2 receptor antagonist (Ki = 3 nM). Lacks the disruptive effect of spiperone on animal behaviour.spiramide
thiethylperazineA member of the class of phenothiazines that is perazine substituted by a ethylsulfanyl group at position 2.thiethylperazine
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
tramadolA 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol in which both stereocentres have R-configuration; the (R,R)-enantiomer of the racemic opioid analgesic tramadol, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer.(R,R)-tramadol
tramadol hydrochlorideA hydrochloride resulting from the reaction of (R,R)-tramadol with 1 molar equivalent of hydrogen chloride; the (R,R)-enantiomer of the racemic opioid analgesic tramadol hydrochloride, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer.(R,R)-tramadol hydrochloride
vortioxetineAn N-arylpiperazine in which the aryl group is specified as 2-[(2,4-dimethylphenyl)sulfanyl]phenyl. Used (as its hydrobromide salt) for treatment of major depressive disorder.vortioxetine
yohimbineAn indole alkaloid with alpha2-adrenoceptor antagonist activity. It is produced by Corynanthe johimbe and Rauwolfia serpentina.yohimbine
ziprasidoneA piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms.ziprasidone
zuclopenthixolThe (Z)-isomer of clopenthixol.zuclopenthixol

Research

Studies (70,930)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199022,602 (31.87)18.7374
1990's15,485 (21.83)18.2507
2000's15,243 (21.49)29.6817
2010's13,356 (18.83)24.3611
2020's4,244 (5.98)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials11,248 (12.44%)5.53%
Reviews6,284 (6.95%)6.00%
Case Studies9,639 (10.66%)4.05%
Observational294 (0.33%)0.25%
Other62,941 (69.62%)84.16%

Protein Targets (497)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency22.925814
15-lipoxygenase, partialHomo sapiens (human)Potency24.016516
2,3-bisphosphoglycerate-independent phosphoglycerate mutaseLeishmania major strain FriedlinPotency0.047811
67.9K proteinVaccinia virusPotency31.216227
acetylcholinesteraseHomo sapiens (human)Potency27.4377429
activating transcription factor 6Homo sapiens (human)Potency25.339728
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency27.6115114
alpha-galactosidaseHomo sapiens (human)Potency19.936923
Alpha-synucleinHomo sapiens (human)Potency13.427012
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency32.587414
AR proteinHomo sapiens (human)Potency22.517610132
aryl hydrocarbon receptorHomo sapiens (human)Potency22.9983214
arylsulfatase AHomo sapiens (human)Potency12.0521113
ATAD5 protein, partialHomo sapiens (human)Potency18.4755431
Ataxin-2Homo sapiens (human)Potency19.8170224
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency21.1449214
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency24.5827211
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency16.128015
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency15.586518
Bloom syndrome protein isoform 1Homo sapiens (human)Potency19.5528219
BRCA1Homo sapiens (human)Potency10.000011
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency47.0063112
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency41.1184110
caspase-3Cricetulus griseus (Chinese hamster)Potency31.056014
caspase-3Homo sapiens (human)Potency41.1184110
Caspase-7Cricetulus griseus (Chinese hamster)Potency31.056014
Cellular tumor antigen p53Homo sapiens (human)Potency29.3139324
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency16.8825221
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency32.110317
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency3.295712
Chain A, Beta-lactamaseEscherichia coli K-12Potency21.3399213
Chain A, CruzipainTrypanosoma cruziPotency32.464812
Chain A, Ferritin light chainEquus caballus (horse)Potency33.658628
Chain A, HADH2 proteinHomo sapiens (human)Potency34.258028
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency52.618619
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency17.344628
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency7.924511
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency22.2320116
Chain B, HADH2 proteinHomo sapiens (human)Potency34.258028
chaperonin GroELMethanococcus maripaludis S2Potency100.000011
chromobox protein homolog 1Homo sapiens (human)Potency53.4364223
ClpPBacillus subtilisPotency14.125411
cytochrome P450 2C19 precursorHomo sapiens (human)Potency9.9730114
cytochrome P450 2C9 precursorHomo sapiens (human)Potency14.1533111
cytochrome P450 2C9, partialHomo sapiens (human)Potency20.5259114
cytochrome P450 2D6Homo sapiens (human)Potency5.3004131
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency7.9322135
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency13.9411258
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency16.6030232
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency31.8670112
D(1A) dopamine receptorHomo sapiens (human)Potency4.7594344
D(1A) dopamine receptorSus scrofa (pig)Potency19.593116
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency12.771113
DNA polymerase betaHomo sapiens (human)Potency79.432811
DNA polymerase eta isoform 1Homo sapiens (human)Potency39.810711
DNA polymerase III, partialBacillus subtilisPotency22.485212
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency70.504518
DNA polymerase kappa isoform 1Homo sapiens (human)Potency26.419415
dopamine D1 receptorHomo sapiens (human)Potency0.032612
endonuclease IVEscherichia coliPotency14.0463110
estrogen nuclear receptor alphaHomo sapiens (human)Potency25.451710125
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency21.9725217
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency23.397910127
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency23.4168242
EWS/FLI fusion proteinHomo sapiens (human)Potency20.7118440
farnesoid X nuclear receptorHomo sapiens (human)Potency29.1439318
flap endonuclease 1Homo sapiens (human)Potency33.635027
Fumarate hydrataseHomo sapiens (human)Potency27.8229123
GVesicular stomatitis virusPotency20.5259114
GABA theta subunitRattus norvegicus (Norway rat)Potency13.6126130
GALC proteinHomo sapiens (human)Potency13.742213
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency13.6126130
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency13.6126130
gemininHomo sapiens (human)Potency15.0120458
GLI family zinc finger 3Homo sapiens (human)Potency12.5564245
glp-1 receptor, partialHomo sapiens (human)Potency15.0345212
GLS proteinHomo sapiens (human)Potency12.6801213
glucocerebrosidaseHomo sapiens (human)Potency13.230318
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency25.7577342
glucokinase regulatory proteinHomo sapiens (human)Potency35.481311
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency29.0729113
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency3.622012
Guanine nucleotide-binding protein GHomo sapiens (human)Potency24.068212
guanine nucleotide-binding protein G(i) subunit alpha-1 isoform 1Homo sapiens (human)Potency25.118911
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency21.274129
heat shock protein beta-1Homo sapiens (human)Potency37.439428
hexokinase-4 isoform 1Homo sapiens (human)Potency35.481311
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency12.6887287
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency36.361517
Histone H2A.xCricetulus griseus (Chinese hamster)Potency63.5428213
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency58.654412
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency20.5259114
huntingtin isoform 2Homo sapiens (human)Potency29.621116
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency20.260224
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency14.1078232
IDH1Homo sapiens (human)Potency19.7410112
importin subunit beta-1 isoform 1Homo sapiens (human)Potency62.216125
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency20.5259128
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency5.7891214
Integrin alpha-IIbHomo sapiens (human)Potency17.412817
Integrin beta-3Homo sapiens (human)Potency17.412817
Interferon betaHomo sapiens (human)Potency19.5998334
lamin isoform A-delta10Homo sapiens (human)Potency14.7431232
lethal factor (plasmid)Bacillus anthracis str. A2012Potency17.8509121
LuciferasePhotinus pyralis (common eastern firefly)Potency33.742035
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency39.363933
M-phase phosphoprotein 8Homo sapiens (human)Potency37.7277116
Microtubule-associated protein tauHomo sapiens (human)Potency17.6654227
mitogen-activated protein kinase 1Homo sapiens (human)Potency19.7927218
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency10.1484235
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency23.595334
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency56.234111
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency56.234111
neuropeptide S receptor isoform AHomo sapiens (human)Potency9.1201110
NFKB1 protein, partialHomo sapiens (human)Potency7.0744214
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency10.6168110
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency63.388117
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency21.9096427
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency24.795616
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency35.481311
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency30.5943211
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency28.4715217
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency20.811412
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency26.4414346
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency3.971614
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency45.675216
ParkinHomo sapiens (human)Potency24.264425
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency39.114327
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency20.5730115
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency57.5812114
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency18.6737522
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency23.9828525
phosphopantetheinyl transferaseBacillus subtilisPotency61.6927322
PINK1Homo sapiens (human)Potency50.118711
plasminogen precursorMus musculus (house mouse)Potency13.101313
polyproteinZika virusPotency27.8229123
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency11.965113
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency11.7937127
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency7.1960135
PPM1D proteinHomo sapiens (human)Potency14.811418
pregnane X nuclear receptorHomo sapiens (human)Potency17.2855321
pregnane X receptorRattus norvegicus (Norway rat)Potency50.118712
progesterone receptorHomo sapiens (human)Potency34.4173320
pyruvate kinaseLeishmania mexicana mexicanaPotency14.219124
pyruvate kinase PKM isoform bHomo sapiens (human)Potency4.538127
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency119.047012
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency39.810711
RAR-related orphan receptor gammaMus musculus (house mouse)Potency17.3631232
ras-related protein Rab-9AHomo sapiens (human)Potency67.2588111
regulator of G-protein signaling 4Homo sapiens (human)Potency12.5590117
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency28.3391343
retinoid X nuclear receptor alphaHomo sapiens (human)Potency12.6452429
RGS12Homo sapiens (human)Potency25.118911
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency19.2051425
SMAD family member 2Homo sapiens (human)Potency22.620929
SMAD family member 3Homo sapiens (human)Potency22.620929
Smad3Homo sapiens (human)Potency19.905118
snurportin-1Homo sapiens (human)Potency62.216125
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency24.2302228
survival motor neuron protein isoform dHomo sapiens (human)Potency19.6466118
TAR DNA-binding protein 43Homo sapiens (human)Potency1.359813
TDP1 proteinHomo sapiens (human)Potency18.21712123
thioredoxin glutathione reductaseSchistosoma mansoniPotency60.374012
thioredoxin reductaseRattus norvegicus (Norway rat)Potency24.8349424
ThrombopoietinHomo sapiens (human)Potency9.5180218
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency19.2398364
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency25.087123
thyroid stimulating hormone receptorHomo sapiens (human)Potency24.8944544
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency18.236226
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency6.048614
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency16.663114
tumor susceptibility gene 101 proteinHomo sapiens (human)Potency31.622811
tyrosine-protein kinase YesHomo sapiens (human)Potency34.499311
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency12.078424
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency13.101313
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency13.101313
USP1 protein, partialHomo sapiens (human)Potency40.5263422
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency14.5446230
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency20.3862425
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency57.2140110
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency29.0729113

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)Ki0.190011
3-hydroxy-3-methylglutaryl-coenzyme A reductase Rattus norvegicus (Norway rat)Ki0.015215
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC500.13741618
5-hydroxytryptamine receptor 1AMus musculus (house mouse)IC500.880023
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC501.37761329
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.429790122
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.39855989
5-hydroxytryptamine receptor 1BHomo sapiens (human)IC508.250022
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC500.9858516
5-hydroxytryptamine receptor 1BHomo sapiens (human)Ki1.981367
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki4.0537928
5-hydroxytryptamine receptor 1DHomo sapiens (human)IC502.048466
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC501.322035
5-hydroxytryptamine receptor 1DHomo sapiens (human)Ki2.695044
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.892948
5-hydroxytryptamine receptor 1EHomo sapiens (human)IC5050.000011
5-hydroxytryptamine receptor 1EHomo sapiens (human)Ki55.000022
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC501.322035
5-hydroxytryptamine receptor 1FHomo sapiens (human)Ki10.000011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.892948
5-hydroxytryptamine receptor 2ABos taurus (cattle)IC500.009011
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.03133050
5-hydroxytryptamine receptor 2AMus musculus (house mouse)IC500.014812
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.36222753
5-hydroxytryptamine receptor 2ABos taurus (cattle)Ki1.000011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.110387167
5-hydroxytryptamine receptor 2AMus musculus (house mouse)Ki0.013712
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki2.214372118
5-hydroxytryptamine receptor 2ASus scrofa (pig)Ki0.030011
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.1726423
5-hydroxytryptamine receptor 2BMus musculus (house mouse)IC500.014812
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.20082038
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.1162824
5-hydroxytryptamine receptor 2BMus musculus (house mouse)Ki0.013712
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki5.31032649
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.59741029
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.21602140
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki1.237943113
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki3.77774672
5-hydroxytryptamine receptor 2C Mus musculus (house mouse)IC500.014812
5-hydroxytryptamine receptor 2C Mus musculus (house mouse)Ki0.388034
5-hydroxytryptamine receptor 3ACavia porcellus (domestic guinea pig)IC50110.000011
5-hydroxytryptamine receptor 3AHomo sapiens (human)IC500.23791212
5-hydroxytryptamine receptor 3AMus musculus (house mouse)IC501.412511
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC501.501834
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki1.20891012
5-hydroxytryptamine receptor 3AMus musculus (house mouse)Ki3.428023
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki2.531044
5-hydroxytryptamine receptor 3BHomo sapiens (human)IC500.942033
5-hydroxytryptamine receptor 3BMus musculus (house mouse)IC501.412511
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC501.501834
5-hydroxytryptamine receptor 3BHomo sapiens (human)Ki0.353924
5-hydroxytryptamine receptor 3BMus musculus (house mouse)Ki0.252011
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki2.531144
5-hydroxytryptamine receptor 3CHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3CHomo sapiens (human)Ki0.353924
5-hydroxytryptamine receptor 3DHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3DHomo sapiens (human)Ki0.353924
5-hydroxytryptamine receptor 3EHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3EHomo sapiens (human)Ki0.353924
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.5077214
5-hydroxytryptamine receptor 4Homo sapiens (human)IC500.000211
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki1.0136416
5-hydroxytryptamine receptor 4Homo sapiens (human)Ki0.01521415
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)IC5013.335023
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Ki0.003911
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)IC502.502512
5-hydroxytryptamine receptor 5AHomo sapiens (human)Ki10.0121411
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)IC502.502512
5-hydroxytryptamine receptor 6Homo sapiens (human)IC500.1708917
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)IC502.502512
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.51514484
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)Ki0.067933
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5059.466716
5-hydroxytryptamine receptor 7Homo sapiens (human)IC500.064399
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)Ki0.002623
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.30535796
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)IC502.502512
5-hydroxytryptamine receptor 7 Mus musculus (house mouse)Ki0.063011
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.0389623
AcetylcholinesteraseHomo sapiens (human)IC501.190522
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki0.252013
Adenylate cyclase type 1 Rattus norvegicus (Norway rat)IC501.220012
Adenylate cyclase type 2Rattus norvegicus (Norway rat)IC501.220012
Adenylate cyclase type 3Rattus norvegicus (Norway rat)IC501.220012
Adenylate cyclase type 4Rattus norvegicus (Norway rat)IC501.220012
Adenylate cyclase type 5Rattus norvegicus (Norway rat)IC500.996723
Adenylate cyclase type 6Rattus norvegicus (Norway rat)IC501.220012
Adenylate cyclase type 8Rattus norvegicus (Norway rat)IC501.220012
Adenylyl cyclase 7 Rattus norvegicus (Norway rat)IC501.220012
AlbuminHomo sapiens (human)IC503.500012
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC500.754218
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki0.747818
Alpha-1A adrenergic receptorHomo sapiens (human)IC500.449099
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC501.66171832
Alpha-1A adrenergic receptorBos taurus (cattle)Ki0.003655
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.25442441
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.29033670
Alpha-1B adrenergic receptorHomo sapiens (human)IC500.011011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC501.96581427
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.52222439
Alpha-1B adrenergic receptorMesocricetus auratus (golden hamster)Ki0.000333
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.28523364
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.1436213
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC501.96581427
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.21712349
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.24843770
Alpha-2A adrenergic receptorHomo sapiens (human)IC500.5091921
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC500.6927815
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.29382754
Alpha-2A adrenergic receptorMus musculus (house mouse)Ki0.028134
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.36992434
Alpha-2A adrenergic receptorSus scrofa (pig)Ki0.004411
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.1562719
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC500.7422714
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.25432246
Alpha-2B adrenergic receptorMus musculus (house mouse)Ki0.222545
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.38862332
Alpha-2C adrenergic receptorHomo sapiens (human)IC500.3244921
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC500.7422714
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.23052350
Alpha-2C adrenergic receptorMus musculus (house mouse)Ki0.028134
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.40112231
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC5020.342627
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki3.429128
Angiotensin-converting enzymeRattus norvegicus (Norway rat)Ki0.1650210
AP-2 complex subunit sigmaRattus norvegicus (Norway rat)Ki0.024211
Aspartate aminotransferase, cytoplasmicHomo sapiens (human)IC505.390011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.0000111
ATP-dependent translocase ABCB1Homo sapiens (human)IC503.850066
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC5027.450044
ATP-dependent translocase ABCB1Homo sapiens (human)Ki0.200011
Beta-1 adrenergic receptorHomo sapiens (human)IC500.000911
Beta-1 adrenergic receptorHomo sapiens (human)Ki0.333733
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki17.000034
Beta-1 adrenergic receptor Cavia porcellus (domestic guinea pig)Ki0.150011
Beta-2 adrenergic receptorHomo sapiens (human)IC500.000511
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)IC501.220012
Beta-2 adrenergic receptorHomo sapiens (human)Ki0.333633
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)Ki10.000022
Beta-3 adrenergic receptorHomo sapiens (human)IC500.088011
Beta-3 adrenergic receptorHomo sapiens (human)Ki0.066011
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)Ki10.000022
Beta-caseinRattus norvegicus (Norway rat)Ki0.001511
Bile salt export pumpHomo sapiens (human)IC5079.4986636
Bile salt export pumpRattus norvegicus (Norway rat)IC50106.950012
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC506.600011
C-8 sterol isomeraseSaccharomyces cerevisiae S288CKi0.000511
Calcitonin gene-related peptide type 1 receptorHomo sapiens (human)Ki0.000411
Calmodulin-1Homo sapiens (human)IC5080.000022
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.0000111
Cathepsin D Bos taurus (cattle)IC500.060011
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)Ki0.055012
Cocaine esteraseHomo sapiens (human)Ki0.006311
Cytochrome P450 1A2Homo sapiens (human)IC5017.984334
Cytochrome P450 2B6Homo sapiens (human)IC5010.000011
Cytochrome P450 2C19Homo sapiens (human)IC5022.059333
Cytochrome P450 2C9 Homo sapiens (human)IC5032.197534
Cytochrome P450 2C9 Homo sapiens (human)Ki0.003711
Cytochrome P450 2D6Homo sapiens (human)IC5013.725849
Cytochrome P450 2D6Homo sapiens (human)Ki0.350022
Cytochrome P450 2J2Homo sapiens (human)IC509.395012
Cytochrome P450 3A4Homo sapiens (human)IC5018.592566
Cytochrome P450 3A4Homo sapiens (human)Ki0.3751415
DBos taurus (cattle)IC501.762435
DMus musculus (house mouse)IC5017.875022
DRattus norvegicus (Norway rat)IC503.45711534
DBos taurus (cattle)Ki0.4200813
DMus musculus (house mouse)Ki1.765022
DRattus norvegicus (Norway rat)Ki0.68422664
D(1A) dopamine receptorHomo sapiens (human)IC500.4790212
D(1A) dopamine receptorHomo sapiens (human)Ki0.47361950
D(1A) dopamine receptorSus scrofa (pig)Ki0.009511
D(1B) dopamine receptorHomo sapiens (human)IC500.005011
D(1B) dopamine receptorMus musculus (house mouse)IC5035.000011
D(1B) dopamine receptorRattus norvegicus (Norway rat)IC500.4402720
D(1B) dopamine receptorHomo sapiens (human)Ki0.230356
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki0.552148
D(2) dopamine receptorBos taurus (cattle)IC500.9403812
D(2) dopamine receptorHomo sapiens (human)IC500.60102138
D(2) dopamine receptorMus musculus (house mouse)IC507.125225
D(2) dopamine receptorRattus norvegicus (Norway rat)IC500.50724397
D(2) dopamine receptorBos taurus (cattle)Ki0.177844
D(2) dopamine receptorChlorocebus aethiops (grivet)Ki0.129424
D(2) dopamine receptorHomo sapiens (human)Ki0.2367176272
D(2) dopamine receptorMus musculus (house mouse)Ki0.112011
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.175769169
D(3) dopamine receptorHomo sapiens (human)IC500.49491121
D(3) dopamine receptorMus musculus (house mouse)IC5035.000011
D(3) dopamine receptorRattus norvegicus (Norway rat)IC500.4402720
D(3) dopamine receptorChlorocebus aethiops (grivet)Ki0.234512
D(3) dopamine receptorHomo sapiens (human)Ki0.441280138
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.41241626
D(4) dopamine receptorHomo sapiens (human)IC500.42631723
D(4) dopamine receptorMus musculus (house mouse)IC5035.000011
D(4) dopamine receptorRattus norvegicus (Norway rat)IC500.4402720
D(4) dopamine receptorHomo sapiens (human)Ki0.148775123
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.4106711
Delta-type opioid receptorHomo sapiens (human)IC503.760011
Delta-type opioid receptorHomo sapiens (human)Ki10.000011
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki7.070023
Diacylglycerol kinase alphaHomo sapiens (human)IC5012.850022
Dihydrofolate reductase Bacillus anthracisIC50102.000011
DNA damage-inducible transcript 3 proteinMus musculus (house mouse)IC506.340011
DNA topoisomerase 1Homo sapiens (human)IC5030.000011
Endothelin receptor type BHomo sapiens (human)Ki0.0236216
Endothelin receptor type BRattus norvegicus (Norway rat)Ki0.023618
Endothelin-1 receptorHomo sapiens (human)IC500.114811
Epidermal growth factor receptorHomo sapiens (human)IC502.947011
Estrogen receptorMus musculus (house mouse)Ki0.084012
Estrogen receptor betaMus musculus (house mouse)Ki0.084012
Fatty-acid amide hydrolase 1Homo sapiens (human)IC500.897522
G-protein coupled receptor Apis mellifera (honey bee)IC5073.000011
GABA theta subunitRattus norvegicus (Norway rat)IC501.000023
GABA theta subunitRattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC501.000027
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki2.750634
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC501.000023
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki2.750634
Gastrin/cholecystokinin type B receptorMus musculus (house mouse)Ki0.013614
Genome polyprotein Human rhinovirus sp.IC50140.000011
Genome polyprotein Human rhinovirus sp.Ki0.100011
Glucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)Ki497.200011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki5.000622
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki10.000011
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)IC502.400011
Glycogen phosphorylase, brain formHomo sapiens (human)Ki24.802012
Glycogen phosphorylase, muscle formHomo sapiens (human)Ki24.802012
high affinity choline transporter 1 isoform aHomo sapiens (human)IC501.762522
Histamine H1 receptorCavia porcellus (domestic guinea pig)IC500.097011
Histamine H1 receptorHomo sapiens (human)IC500.6836818
Histamine H1 receptorRattus norvegicus (Norway rat)IC500.238439
Histamine H1 receptorCavia porcellus (domestic guinea pig)Ki0.4369612
Histamine H1 receptorHomo sapiens (human)Ki0.09221648
Histamine H1 receptorRattus norvegicus (Norway rat)Ki0.703323
Histamine H2 receptorCavia porcellus (domestic guinea pig)IC500.800012
Histamine H2 receptorHomo sapiens (human)IC501.588619
Histamine H2 receptorCavia porcellus (domestic guinea pig)Ki1.000012
Histamine H2 receptorHomo sapiens (human)Ki1.562219
Histamine H3 receptorHomo sapiens (human)Ki0.912233
Histamine H4 receptorHomo sapiens (human)Ki0.644344
Histone-lysine N-methyltransferase SETD7Homo sapiens (human)IC508.133333
Histone-lysine N-methyltransferase SETD7Homo sapiens (human)Ki15.000011
Integrin alpha-4Homo sapiens (human)Ki0.003911
Integrin beta-1Homo sapiens (human)Ki0.003911
Kappa-type opioid receptorHomo sapiens (human)IC501.740022
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.002611
Kappa-type opioid receptorHomo sapiens (human)Ki5.498022
Kappa-type opioid receptorRattus norvegicus (Norway rat)Ki7.070023
Lysosomal alpha-glucosidaseBos taurus (cattle)IC500.002111
Lysosomal alpha-glucosidaseBos taurus (cattle)Ki0.008711
Lysosomal alpha-glucosidaseRattus norvegicus (Norway rat)Ki0.008711
M-phase inducer phosphatase 1Homo sapiens (human)IC5022.300011
Mu-type opioid receptorHomo sapiens (human)IC501.407522
Mu-type opioid receptorHomo sapiens (human)Ki3.965544
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki7.070023
Mucosa-associated lymphoid tissue lymphoma translocation protein 1Homo sapiens (human)IC503.765022
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50250.800012
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC50395.500012
Multidrug resistance-associated protein 4Homo sapiens (human)IC50127.3636111
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC501.4243311
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC500.1028511
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki2.83481135
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki8.087169
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC500.910017
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC500.132457
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki4.1038518
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki8.438579
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC5012.510839
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC500.325269
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki4.1762417
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki13.408435
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.541318
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC500.132457
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki3.4000521
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki13.408435
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.821519
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC500.353468
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki3.9851419
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki13.408435
Muscarinic receptor M1 Bos taurus (cattle)IC501.000011
N-acetyltransferase EisMycobacterium tuberculosis H37RvIC500.390011
N-acetyltransferase EisMycobacterium tuberculosis H37RvKi0.390011
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.831811
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.831811
Nitric oxide synthase, inducibleMus musculus (house mouse)IC509.600011
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC5026.679615
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki6.840614
P2X purinoceptor 7Homo sapiens (human)IC500.830011
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CIC506.125014
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC502.768011
Potassium channel subfamily K member 2Homo sapiens (human)IC503.650012
Potassium voltage-gated channel subfamily A member 5Homo sapiens (human)IC502.000011
Potassium voltage-gated channel subfamily E member 1Homo sapiens (human)IC5050.118711
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC502.067143123
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki9.5310615
Potassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)IC5050.118711
Prostaglandin G/H synthase 1Ovis aries (sheep)Ki0.001611
Protease Human immunodeficiency virus 1IC50125.000011
Protease Human immunodeficiency virus 1Ki50.050022
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC506.690011
sentrin-specific protease 8Homo sapiens (human)IC5012.650022
Sigma intracellular receptor 2Homo sapiens (human)Ki0.061666
Sigma intracellular receptor 2Rattus norvegicus (Norway rat)Ki0.07211111
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.4474715
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)IC500.250957
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki0.00493737
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.27583847
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)Ki0.014877
Sodium channel protein type 1 subunit alphaHomo sapiens (human)IC503.118033
Sodium channel protein type 10 subunit alphaHomo sapiens (human)IC503.118033
Sodium channel protein type 11 subunit alphaHomo sapiens (human)IC503.118033
Sodium channel protein type 2 subunit alphaHomo sapiens (human)IC503.118033
Sodium channel protein type 2 subunit alphaRattus norvegicus (Norway rat)IC500.340011
Sodium channel protein type 3 subunit alphaHomo sapiens (human)IC503.118033
Sodium channel protein type 4 subunit alphaHomo sapiens (human)IC503.118033
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC5021.433877
Sodium channel protein type 7 subunit alphaHomo sapiens (human)IC503.118033
Sodium channel protein type 8 subunit alphaHomo sapiens (human)IC503.118033
Sodium channel protein type 9 subunit alphaHomo sapiens (human)IC503.118033
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC501.4902212
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki0.50151020
Sodium-dependent dopamine transporter Homo sapiens (human)IC501.990524
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.693936
Sodium-dependent noradrenaline transporterMus musculus (house mouse)Ki0.290011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC500.677629
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki1.8147512
Sodium-dependent serotonin transporterHomo sapiens (human)IC501.3230310
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC500.875748
Sodium-dependent serotonin transporterHomo sapiens (human)Ki2.64881023
Sodium-dependent serotonin transporterMus musculus (house mouse)Ki4.100011
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki2.759144
Solute carrier family 22 member 1 Homo sapiens (human)IC5066.790024
Solute carrier family 22 member 2Homo sapiens (human)IC5022.600012
sphingosine 1-phosphate receptor 3Homo sapiens (human)IC5050.000011
Substance-K receptorHomo sapiens (human)IC504.071011
Substance-K receptorHomo sapiens (human)Ki1.357011
Synaptic vesicular amine transporterHomo sapiens (human)IC500.180011
Synaptic vesicular amine transporterHomo sapiens (human)Ki0.540033
TPA: protein transporter TIM10Saccharomyces cerevisiae S288CIC5037.800011
Transient receptor potential cation channel subfamily V member 1Rattus norvegicus (Norway rat)Ki0.005011
Transient receptor potential cation channel subfamily V member 2Rattus norvegicus (Norway rat)Ki0.005011
Transient receptor potential cation channel subfamily V member 4Rattus norvegicus (Norway rat)Ki0.005011
Translocator proteinRattus norvegicus (Norway rat)Ki0.004311
TransporterRattus norvegicus (Norway rat)IC500.427326
TransporterRattus norvegicus (Norway rat)Ki3.8132312
Trypanothione reductaseTrypanosoma brucei bruceiIC503.400011
Trypanothione reductaseTrypanosoma cruziIC5045.166733
Trypanothione reductaseTrypanosoma cruziKi17.120055
Tryptophan 5-hydroxylase 1Rattus norvegicus (Norway rat)IC500.060011
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)IC505.050011
Ubiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)IC502.000022
ubiquitin-conjugating enzyme E2 NHomo sapiens (human)IC5020.000012
UDP-glucuronosyltransferase 1A9Homo sapiens (human)Ki344.000011
UDP-glucuronosyltransferase 2B7Homo sapiens (human)Ki590.000011
Vesicular acetylcholine transporterRattus norvegicus (Norway rat)Ki3.808023
Vitamin D-binding proteinRattus norvegicus (Norway rat)Ki0.003711
Voltage-dependent L-type calcium channel subunit alpha-1CCavia porcellus (domestic guinea pig)IC502.912035
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC5048.69411212
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC506.655899
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC506.655899
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC506.655899
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC509.000011
WD repeat-containing protein 48Homo sapiens (human)IC502.000011
XBP1Homo sapiens (human)IC5010.000011
Zinc finger protein 664Cavia porcellus (domestic guinea pig)Ki0.006611

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)EC500.46142324
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd0.7757211
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Kd0.002511
5-hydroxytryptamine receptor 1BHomo sapiens (human)EC500.260011
5-hydroxytryptamine receptor 2AHomo sapiens (human)EC500.001011
5-hydroxytryptamine receptor 2AMus musculus (house mouse)EC5076.083011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Kd0.001244
5-hydroxytryptamine receptor 2BHomo sapiens (human)EC500.020011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Kd0.051345
5-hydroxytryptamine receptor 2CHomo sapiens (human)EC500.125222
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Kd0.001533
5-hydroxytryptamine receptor 3AHomo sapiens (human)Kd0.00041111
5-hydroxytryptamine receptor 3BHomo sapiens (human)Kd0.000366
5-hydroxytryptamine receptor 7Homo sapiens (human)EC500.000611
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Kd0.000111
AlbuminRattus norvegicus (Norway rat)Kd56.547514
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd0.5994615
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kd0.5994615
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd0.5994615
Alpha-2A adrenergic receptorHomo sapiens (human)EC500.008511
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)EC500.027012
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Kd3.799946
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)EC500.027012
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Kd3.799946
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)EC500.027012
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Kd3.799946
alternatively spliced Trp4Mus musculus (house mouse)EC506.682711
Angiotensin-converting enzyme 2 Homo sapiens (human)EC508.230014
Beta-1 adrenergic receptorHomo sapiens (human)Kd3.335033
Beta-2 adrenergic receptorHomo sapiens (human)Kd0.000622
Beta-3 adrenergic receptorHomo sapiens (human)Kd0.583022
Calmodulin Bos taurus (cattle)Kd61.000011
D(2) dopamine receptorHomo sapiens (human)Kd0.007444
D(3) dopamine receptorHomo sapiens (human)Kd0.316211
D(4) dopamine receptorHomo sapiens (human)EC505.008522
Envelope glycoproteinEbola virus - Mayinga, Zaire, 1976Kd118.000011
G protein-coupled receptorHuman betaherpesvirus 5EC500.330612
G-protein coupled receptor homolog US28Human herpesvirus 5 strain AD169EC500.352412
Glycine receptor subunit alpha-1Homo sapiens (human)EC501.010012
HeparanaseHomo sapiens (human)Kd1,000.000011
Histamine H1 receptorHomo sapiens (human)EC500.000411
Histamine H1 receptorHomo sapiens (human)Kd1.801123
Histamine H4 receptorHomo sapiens (human)Kd0.029444
HLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)Kd6.250012
Major prion proteinHomo sapiens (human)EC507.500012
Mu-type opioid receptorHomo sapiens (human)EC505.500022
mu-type opioid receptor isoform MOR-1Homo sapiens (human)EC5092.470011
Muscarinic acetylcholine receptor M1Homo sapiens (human)EC5020.034336
Muscarinic acetylcholine receptor M2Homo sapiens (human)EC5010.000012
Muscarinic acetylcholine receptor M3Homo sapiens (human)EC505.335012
Muscarinic acetylcholine receptor M4Homo sapiens (human)EC506.800023
Muscarinic acetylcholine receptor M5Homo sapiens (human)EC500.170011
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC5010.100045
Nuclear receptor subfamily 1 group I member 2Rattus norvegicus (Norway rat)EC5025.100011
POsterior SegregationCaenorhabditis elegansEC50300.000011
Potassium channel subfamily K member 2Homo sapiens (human)EC500.354011
Procathepsin LHomo sapiens (human)EC508.230014
Proteasome subunit alpha type-6Homo sapiens (human)EC5012.200012
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC508.230014
Replicase polyprotein 1abBetacoronavirus England 1EC508.230014
Replicase polyprotein 1abHuman coronavirus 229EEC508.230014
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC508.230014
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC508.230014
short transient receptor potential channel 6 isoform 1Mus musculus (house mouse)EC5015.850011
Sodium-dependent dopamine transporter Homo sapiens (human)Kd0.360011
Sodium-dependent noradrenaline transporter Homo sapiens (human)EC50103.486011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Kd0.360011
Sodium-dependent serotonin transporterHomo sapiens (human)Kd0.200011
Spike glycoproteinBetacoronavirus England 1EC508.230014
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC508.230014
Transmembrane protease serine 2Homo sapiens (human)EC508.230014
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
Zinc finger protein mex-5Caenorhabditis elegansEC50103.486011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)Activity0.010011
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kb0.000644
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)KiAH0.001211
5-hydroxytryptamine receptor 1AHomo sapiens (human)Log Ki0.008511
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Log Ki0.006011
5-hydroxytryptamine receptor 1BHomo sapiens (human)Activity0.028011
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Log Ki0.006011
5-hydroxytryptamine receptor 1DHomo sapiens (human)Activity0.000911
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Kb0.014011
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Log Ki0.006011
5-hydroxytryptamine receptor 1EHomo sapiens (human)Activity1.659011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Log Ki0.006011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Activity0.004323
5-hydroxytryptamine receptor 2AHomo sapiens (human)INH0.004712
5-hydroxytryptamine receptor 2AHomo sapiens (human)Kb0.001644
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ke0.032011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Log Ki0.006011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Activity0.002611
5-hydroxytryptamine receptor 2BHomo sapiens (human)Kb1.980011
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Activity0.009511
5-hydroxytryptamine receptor 2CHomo sapiens (human)Kb0.112011
5-hydroxytryptamine receptor 3AHomo sapiens (human)Activity10.000011
5-hydroxytryptamine receptor 4Homo sapiens (human)Activity1.274011
5-hydroxytryptamine receptor 4Homo sapiens (human)Kb0.000011
5-hydroxytryptamine receptor 5AHomo sapiens (human)Activity0.562011
5-hydroxytryptamine receptor 6Homo sapiens (human)Activity0.091011
5-hydroxytryptamine receptor 6Homo sapiens (human)INH0.007612
5-hydroxytryptamine receptor 6Homo sapiens (human)Kb0.016822
5-hydroxytryptamine receptor 7Homo sapiens (human)Activity0.018011
5-hydroxytryptamine receptor 7Homo sapiens (human)Kb0.003833
5-hydroxytryptamine receptor 7Homo sapiens (human)Kbapp0.016011
Aldehyde oxidaseHomo sapiens (human)Kii1.300011
Aldehyde oxidaseHomo sapiens (human)Kis1.300011
Alpha-1A adrenergic receptorHomo sapiens (human)Activity0.015522
Alpha-1A adrenergic receptorHomo sapiens (human)Kapp0.093011
Alpha-1A adrenergic receptorHomo sapiens (human)Log Ki0.006011
Alpha-1B adrenergic receptorHomo sapiens (human)Activity0.063122
Alpha-1B adrenergic receptorHomo sapiens (human)Kapp0.093011
Alpha-1B adrenergic receptorHomo sapiens (human)Log Ki0.006011
Alpha-1D adrenergic receptorHomo sapiens (human)Activity0.050022
Alpha-1D adrenergic receptorHomo sapiens (human)Kapp0.093011
Alpha-1D adrenergic receptorHomo sapiens (human)Log Ki0.006011
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Log Ki0.006012
Alpha-2A adrenergic receptorHomo sapiens (human)Activity0.031011
Alpha-2A adrenergic receptorHomo sapiens (human)Kapp0.093011
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Log Ki0.006023
Alpha-2B adrenergic receptorHomo sapiens (human)Activity0.041011
Alpha-2B adrenergic receptorHomo sapiens (human)Kapp0.093011
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Log Ki0.006023
Alpha-2C adrenergic receptorHomo sapiens (human)Activity0.030011
Alpha-2C adrenergic receptorHomo sapiens (human)Kapp0.093011
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Log Ki0.006023
ATP-dependent translocase ABCB1Homo sapiens (human)Km24.800015
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Kapp0.014011
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)Kapp0.093011
Carbonyl reductase [NADPH] 1Homo sapiens (human)Km1,200.000011
Caspase 6, apoptosis-related cysteine peptidaseHomo sapiens (human)AC5011.510011
cystic fibrosis transmembrane conductance regulator ATP-binding cassette sub-family C member 7Homo sapiens (human)AC5050.000011
Cytochrome P450 2C19Homo sapiens (human)Km25.300011
Cytochrome P450 2C9 Homo sapiens (human)Km25.300011
Cytochrome P450 2D6Homo sapiens (human)Km43.766733
Cytochrome P450 2J2Homo sapiens (human)Km25.300011
Cytochrome P450 3A4Homo sapiens (human)INH26.200011
Cytochrome P450 3A4Homo sapiens (human)Km45.240045
D(1A) dopamine receptorHomo sapiens (human)Activity0.009011
D(1A) dopamine receptorHomo sapiens (human)Kb5.000712
D(1B) dopamine receptorHomo sapiens (human)Kb5.000712
D(2) dopamine receptorHomo sapiens (human)Activity0.113223
D(2) dopamine receptorRattus norvegicus (Norway rat)K 0.50.000222
D(2) dopamine receptorHomo sapiens (human)Kb5.000712
D(2) dopamine receptorHomo sapiens (human)pKi0.008012
D(3) dopamine receptorRattus norvegicus (Norway rat)Activity0.014011
D(3) dopamine receptorRattus norvegicus (Norway rat)K 0.50.000411
D(3) dopamine receptorHomo sapiens (human)Kb5.000712
D(3) dopamine receptorHomo sapiens (human)pKi0.007512
D(4) dopamine receptorHomo sapiens (human)Activity0.004911
D(4) dopamine receptorHomo sapiens (human)Kb5.000712
D(4) dopamine receptorHomo sapiens (human)pKi0.007612
Delta-type opioid receptorHomo sapiens (human)Activity0.018911
DNA repair and recombination protein RAD54-like isoform 1Homo sapiens (human)AC5078.950011
DNA repair protein RAD52 homolog isoform aHomo sapiens (human)AC507.710011
FAD-linked sulfhydryl oxidase ALRHomo sapiens (human)AC500.369011
fibroblast growth factor 22 isoform 1 precursorHomo sapiens (human)AbsAC0.47_uM24.720011
fibroblast growth factor 22 isoform 1 precursorHomo sapiens (human)AbsAC1_uM3.420011
Histamine H1 receptorHomo sapiens (human)Activity0.047523
Histamine H1 receptorHomo sapiens (human)INH0.002212
Histamine H2 receptorHomo sapiens (human)Activity0.104011
Histamine H2 receptorCavia porcellus (domestic guinea pig)K0.50.0759213
Histamine H4 receptorHomo sapiens (human)Activity0.012711
Kappa-type opioid receptorRattus norvegicus (Norway rat)Activity0.063211
MSHDrosophila melanogaster (fruit fly)AC5027.640011
Muscarinic acetylcholine receptor M1Homo sapiens (human)Activity0.001211
Muscarinic acetylcholine receptor M2Homo sapiens (human)Activity0.017711
Muscarinic acetylcholine receptor M3Homo sapiens (human)Activity0.003811
Muscarinic acetylcholine receptor M4Homo sapiens (human)Activity0.036911
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CINH61.650014
Prostaglandin E2 receptor EP3 subtypeHomo sapiens (human)Activity0.021711
Prostaglandin E2 receptor EP4 subtypeHomo sapiens (human)Activity0.015211
protein AF-9 isoform aHomo sapiens (human)AC5013.100011
scavenger receptor class B member 1 isoform 1Mus musculus (house mouse)AC5087.830011
Snq2pSaccharomyces cerevisiae EC1118INH63.400014
Sodium-dependent noradrenaline transporter Homo sapiens (human)Activity1.132011
Sodium-dependent serotonin transporterHomo sapiens (human)Activity0.089711
Solute carrier family 22 member 1 Homo sapiens (human)Activity9.700011
UDP-glucuronosyltransferase 1A3Homo sapiens (human)Km240.000011
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km103.500036
UDP-glucuronosyltransferase 1A9Homo sapiens (human)Km174.000011
UDP-glucuronosyltransferase 2B7Homo sapiens (human)Km45.000011