Page last updated: 2024-08-05 15:18:59

first generation antipsychotic

Antipsychotic drugs which can have different modes of action but which tend to be more likely than second generation antipsychotics to cause extrapyramidal motor control disabilities such as body rigidity or Parkinson's disease-type movements; such body movements can become permanent even after treatment has ceased.

ChEBI ID: 65190

Members (15)

MemberDefinitionClass
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
droperidolAn organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon.droperidol
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
mesoridazineA phenothiazine substituted at position 2 (para to the S atom) by a methylsulfinyl group, and on the nitrogen by a 2-(1-methylpiperidin-2-yl)ethyl group.mesoridazine
periciazineA member of the class of phenothiazines that is 10H-phenothiazine substituted by a 3-(4-hydroxypiperidin-1-yl)propyl group at the nitrogen atom and a carbonitrile group at position 2. Periciazine is a first generation antipsychotic.periciazine
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
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
prochlorperazineA member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position.prochlorperazine
reserpineAn alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.reserpine
serentilThe benzenesulfonate salt of mesoridazine prepared using equimolar amounts of mesoridazine and benzenesulfonic acid.mesoridazine 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
thioridazine hydrochloridethioridazine hydrochloride
triflupromazineA member of the class of phenothiazines that is 10H-phenothiazine having a trifluoromethyl subsitituent at the 2-position and a 3-(dimethylamino)propyl group at the N-10 position.triflupromazine
zuclopenthixolThe (Z)-isomer of clopenthixol.zuclopenthixol

Research

Studies (39,447)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199023,829 (60.41)18.7374
1990's6,071 (15.39)18.2507
2000's4,796 (12.16)29.6817
2010's3,646 (9.24)24.3611
2020's1,105 (2.80)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials3,216 (7.22%)5.53%
Reviews1,705 (3.83%)6.00%
Case Studies2,671 (6.00%)4.05%
Observational47 (0.11%)0.25%
Other36,879 (82.84%)84.16%

Protein Targets (377)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-lipoxygenase, partialHomo sapiens (human)Potency20.306813
67.9K proteinVaccinia virusPotency20.237527
acetylcholinesteraseHomo sapiens (human)Potency45.795039
activating transcription factor 6Homo sapiens (human)Potency57.483625
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency23.814314
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency26.364813
AR proteinHomo sapiens (human)Potency29.97041153
aryl hydrocarbon receptorHomo sapiens (human)Potency41.280026
arylsulfatase AHomo sapiens (human)Potency13.203614
ATAD5 protein, partialHomo sapiens (human)Potency19.4544310
Ataxin-2Homo sapiens (human)Potency25.849228
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency15.488915
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency34.516828
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency9.930412
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency22.631713
Bloom syndrome protein isoform 1Homo sapiens (human)Potency17.782824
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency25.536614
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency46.926616
caspase-1 isoform alpha precursorHomo sapiens (human)Potency7.943311
caspase-3Cricetulus griseus (Chinese hamster)Potency29.218414
caspase-3Homo sapiens (human)Potency46.926616
Caspase-7Cricetulus griseus (Chinese hamster)Potency29.218414
Caspase-7Homo sapiens (human)Potency7.943311
Cellular tumor antigen p53Homo sapiens (human)Potency44.3599313
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency17.182829
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency30.688116
Chain A, Beta-lactamaseEscherichia coli K-12Potency52.773925
Chain A, Ferritin light chainEquus caballus (horse)Potency3.162311
Chain A, HADH2 proteinHomo sapiens (human)Potency25.118911
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency47.708014
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency10.176624
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency15.811411
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency21.7088112
Chain B, HADH2 proteinHomo sapiens (human)Potency25.118911
chromobox protein homolog 1Homo sapiens (human)Potency43.6752210
cytochrome P450 2C19 precursorHomo sapiens (human)Potency10.923314
cytochrome P450 2C9 precursorHomo sapiens (human)Potency20.811412
cytochrome P450 2C9, partialHomo sapiens (human)Potency27.723112
cytochrome P450 2D6Homo sapiens (human)Potency3.791917
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency4.5880110
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency9.4972220
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency12.4293210
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency31.897616
D(1A) dopamine receptorHomo sapiens (human)Potency4.4998310
D(1A) dopamine receptorSus scrofa (pig)Potency19.744014
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency2.511911
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency31.622811
DNA polymerase betaHomo sapiens (human)Potency35.716812
DNA polymerase eta isoform 1Homo sapiens (human)Potency7.943311
DNA polymerase III, partialBacillus subtilisPotency23.778111
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency36.584814
DNA polymerase kappa isoform 1Homo sapiens (human)Potency19.959413
endonuclease IVEscherichia coliPotency17.263613
estrogen nuclear receptor alphaHomo sapiens (human)Potency36.03671269
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency25.171527
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency28.97331063
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency15.2613218
EWS/FLI fusion proteinHomo sapiens (human)Potency23.159244
farnesoid X nuclear receptorHomo sapiens (human)Potency35.2856514
flap endonuclease 1Homo sapiens (human)Potency35.379915
Fumarate hydrataseHomo sapiens (human)Potency29.094414
GVesicular stomatitis virusPotency27.723112
GABA theta subunitRattus norvegicus (Norway rat)Potency9.4972110
GALC proteinHomo sapiens (human)Potency20.259312
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency9.4972110
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency9.4972110
gemininHomo sapiens (human)Potency17.4503419
GLI family zinc finger 3Homo sapiens (human)Potency12.5621218
glp-1 receptor, partialHomo sapiens (human)Potency18.423916
GLS proteinHomo sapiens (human)Potency15.062424
glucocerebrosidaseHomo sapiens (human)Potency16.208612
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency29.4693419
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency44.925218
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency11.582111
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency58.478911
heat shock protein beta-1Homo sapiens (human)Potency44.067727
hemoglobin subunit betaHomo sapiens (human)Potency31.622811
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency14.4045222
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency19.351212
Histone H2A.xCricetulus griseus (Chinese hamster)Potency54.271423
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency58.654412
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency27.723112
huntingtin isoform 2Homo sapiens (human)Potency23.760913
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency40.375524
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency7.5765210
IDH1Homo sapiens (human)Potency20.863517
importin subunit beta-1 isoform 1Homo sapiens (human)Potency28.125222
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency27.723114
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency11.294724
Integrin alpha-IIbHomo sapiens (human)Potency24.196913
Integrin beta-3Homo sapiens (human)Potency24.196913
Interferon betaHomo sapiens (human)Potency27.891424
interleukin 8Homo sapiens (human)Potency66.824211
lamin isoform A-delta10Homo sapiens (human)Potency17.4548212
lethal factor (plasmid)Bacillus anthracis str. A2012Potency18.980518
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency28.183811
LuciferasePhotinus pyralis (common eastern firefly)Potency40.533412
M-phase phosphoprotein 8Homo sapiens (human)Potency22.801117
Microtubule-associated protein tauHomo sapiens (human)Potency24.5806212
mitogen-activated protein kinase 1Homo sapiens (human)Potency20.2430212
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency7.2138210
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency39.810711
neuropeptide S receptor isoform AHomo sapiens (human)Potency13.199416
NFKB1 protein, partialHomo sapiens (human)Potency17.861526
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency6.352214
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency58.047912
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency32.5000415
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency22.142712
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency39.986813
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency45.501526
Nuclear receptor ROR-gammaHomo sapiens (human)Potency37.578011
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency26.4538210
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency41.5875322
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency44.668411
ParkinHomo sapiens (human)Potency23.109311
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency37.026422
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency23.194617
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency40.395914
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency23.5330519
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency29.9758520
phosphopantetheinyl transferaseBacillus subtilisPotency58.7622310
plasminogen precursorMus musculus (house mouse)Potency11.599714
polyproteinZika virusPotency29.094414
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency12.001918
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency3.0421113
pregnane X nuclear receptorHomo sapiens (human)Potency17.3049318
pregnane X receptorRattus norvegicus (Norway rat)Potency50.118712
progesterone receptorHomo sapiens (human)Potency41.896027
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency12.589311
RAR-related orphan receptor gammaMus musculus (house mouse)Potency26.5529217
ras-related protein Rab-9AHomo sapiens (human)Potency77.305613
regulator of G-protein signaling 4Homo sapiens (human)Potency8.664716
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency37.2216316
retinoid X nuclear receptor alphaHomo sapiens (human)Potency16.6441417
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency19.8129415
signal transducer and activator of transcription 6, interleukin-4 inducedHomo sapiens (human)Potency30.016233
SMAD family member 2Homo sapiens (human)Potency23.4260212
SMAD family member 3Homo sapiens (human)Potency23.4260212
Smad3Homo sapiens (human)Potency33.552012
snurportin-1Homo sapiens (human)Potency28.125222
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency24.865128
survival motor neuron protein isoform dHomo sapiens (human)Potency14.501018
TAR DNA-binding protein 43Homo sapiens (human)Potency1.862312
TDP1 proteinHomo sapiens (human)Potency20.5879239
thioredoxin glutathione reductaseSchistosoma mansoniPotency89.125111
thioredoxin reductaseRattus norvegicus (Norway rat)Potency18.468825
ThrombopoietinHomo sapiens (human)Potency17.7800210
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency21.6059330
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency50.845413
thyroid stimulating hormone receptorHomo sapiens (human)Potency39.2662620
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency28.765222
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency11.220211
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency2.511911
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency11.599714
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency11.599714
USP1 protein, partialHomo sapiens (human)Potency38.8337312
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency18.1692210
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency22.9259520
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency45.239613
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency44.925218

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)Ki0.190011
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC501.500011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC502.274469
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki2.341055
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki1.3139810
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC500.454035
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.238313
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC500.509022
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC500.509022
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.075425
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.12881212
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.14801821
5-hydroxytryptamine receptor 2AMus musculus (house mouse)Ki0.026511
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.04832021
5-hydroxytryptamine receptor 2ASus scrofa (pig)Ki0.030011
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.905814
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.145199
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.465225
5-hydroxytryptamine receptor 2BMus musculus (house mouse)Ki0.026511
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.026199
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC502.784625
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.23061010
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki3.74331114
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.49351010
5-hydroxytryptamine receptor 2C Mus musculus (house mouse)Ki0.026511
5-hydroxytryptamine receptor 3AMus musculus (house mouse)Ki10.000011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.785825
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.913425
5-hydroxytryptamine receptor 4Homo sapiens (human)Ki0.000611
5-hydroxytryptamine receptor 6Homo sapiens (human)IC500.169012
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki1.568968
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5095.750014
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.532956
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.088523
Acetylcholinesterase Bos taurus (cattle)IC507.000011
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki0.318011
Adenylate cyclase type 1 Rattus norvegicus (Norway rat)IC502.300011
Adenylate cyclase type 2Rattus norvegicus (Norway rat)IC502.300011
Adenylate cyclase type 3Rattus norvegicus (Norway rat)IC502.300011
Adenylate cyclase type 4Rattus norvegicus (Norway rat)IC502.300011
Adenylate cyclase type 5Rattus norvegicus (Norway rat)IC501.425022
Adenylate cyclase type 6Rattus norvegicus (Norway rat)IC502.300011
Adenylate cyclase type 8Rattus norvegicus (Norway rat)IC502.300011
Adenylyl cyclase 7 Rattus norvegicus (Norway rat)IC502.300011
AlbuminHomo sapiens (human)IC503.500012
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC501.262313
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki1.251313
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.079457
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.012422
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.01421012
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC500.079457
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.012422
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.01421012
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.051714
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC500.079457
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.020936
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.01421012
Alpha-2A adrenergic receptorHomo sapiens (human)IC502.060014
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC500.035511
Alpha-2A adrenergic receptorHomo sapiens (human)Ki1.618025
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki9.600011
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.491014
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC500.035511
Alpha-2B adrenergic receptorHomo sapiens (human)Ki1.179525
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki9.600011
Alpha-2C adrenergic receptorHomo sapiens (human)IC500.965214
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC500.035511
Alpha-2C adrenergic receptorHomo sapiens (human)Ki1.112225
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki9.600011
Androgen receptorRattus norvegicus (Norway rat)Ki3.000011
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC502.840824
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki1.191613
AP-2 complex subunit sigmaRattus norvegicus (Norway rat)Ki0.024211
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000013
ATP-dependent translocase ABCB1Homo sapiens (human)IC503.14231414
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC5027.450044
ATP-dependent translocase ABCB1Homo sapiens (human)Ki6.140067
ATP-dependent translocase ABCB1Mus musculus (house mouse)Ki10.965022
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki10.000011
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)IC502.300011
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)Ki10.000011
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)Ki10.000011
Bile salt export pumpHomo sapiens (human)IC5046.4967515
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC5014.325744
C-8 sterol isomeraseSaccharomyces cerevisiae S288CKi0.000511
Calcitonin gene-related peptide type 1 receptorHomo sapiens (human)Ki0.000411
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50111.466713
Canalicular multispecific organic anion transporter 1Homo sapiens (human)Ki295.000011
Cathepsin D Bos taurus (cattle)IC500.060011
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)Ki0.050011
CholinesteraseEquus caballus (horse)IC503.815012
Chromaffin granule amine transporterHomo sapiens (human)IC500.050022
Cocaine esteraseHomo sapiens (human)Ki0.006311
Cytochrome P450 1A2Homo sapiens (human)IC505.666212
Cytochrome P450 2C19Homo sapiens (human)IC506.377811
Cytochrome P450 2C9 Homo sapiens (human)IC504.690011
Cytochrome P450 2D6Homo sapiens (human)IC501.036312
Cytochrome P450 2J2Homo sapiens (human)IC504.690011
Cytochrome P450 3A4Homo sapiens (human)IC504.877522
DBos taurus (cattle)IC500.250922
DRattus norvegicus (Norway rat)IC500.13981118
DRattus norvegicus (Norway rat)Ki0.15501723
D(1A) dopamine receptorHomo sapiens (human)IC500.311225
D(1A) dopamine receptorHomo sapiens (human)Ki0.1296912
D(1A) dopamine receptorSus scrofa (pig)Ki0.009511
D(1B) dopamine receptorHomo sapiens (human)IC500.005011
D(1B) dopamine receptorRattus norvegicus (Norway rat)IC500.0187511
D(1B) dopamine receptorHomo sapiens (human)Ki0.101044
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki0.001722
D(2) dopamine receptorBos taurus (cattle)IC500.133244
D(2) dopamine receptorHomo sapiens (human)IC500.07391014
D(2) dopamine receptorRattus norvegicus (Norway rat)IC500.02052336
D(2) dopamine receptorBos taurus (cattle)Ki0.007033
D(2) dopamine receptorChlorocebus aethiops (grivet)Ki0.004922
D(2) dopamine receptorHomo sapiens (human)Ki0.065499106
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.00293660
D(3) dopamine receptorHomo sapiens (human)IC500.007269
D(3) dopamine receptorRattus norvegicus (Norway rat)IC500.0187511
D(3) dopamine receptorChlorocebus aethiops (grivet)Ki0.003011
D(3) dopamine receptorHomo sapiens (human)Ki0.00954853
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.01511010
D(4) dopamine receptorHomo sapiens (human)IC500.545768
D(4) dopamine receptorRattus norvegicus (Norway rat)IC500.0187511
D(4) dopamine receptorHomo sapiens (human)Ki0.04304144
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.006022
Delta-type opioid receptorHomo sapiens (human)IC503.760011
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki7.070023
DNA damage-inducible transcript 3 proteinMus musculus (house mouse)IC506.340011
DNA topoisomerase 1Homo sapiens (human)IC50160.000011
Epidermal growth factor receptorHomo sapiens (human)IC502.947011
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
Gastrin/cholecystokinin type B receptorMus musculus (house mouse)Ki0.023412
Genome polyprotein Human rhinovirus sp.IC50140.000011
Genome polyprotein Human rhinovirus sp.Ki0.100011
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
Histamine H1 receptorHomo sapiens (human)IC501.849014
Histamine H1 receptorRattus norvegicus (Norway rat)IC500.699723
Histamine H1 receptorHomo sapiens (human)Ki0.363758
Histamine H1 receptorRattus norvegicus (Norway rat)Ki2.100011
Histamine H2 receptorHomo sapiens (human)IC501.058012
Histamine H2 receptorHomo sapiens (human)Ki1.040512
Histamine H4 receptorHomo sapiens (human)Ki2.000011
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)Ki0.996011
Kappa-type opioid receptorRattus norvegicus (Norway rat)Ki7.070023
Mcl-1Homo sapiens (human)IC503.773311
Mu-type opioid receptorHomo sapiens (human)IC502.322323
Mu-type opioid receptorHomo sapiens (human)Ki3.787034
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)IC50500.000011
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC50500.000011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000013
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC503.005034
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC501.316336
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki1.623145
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki4.630645
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC501.609012
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC501.947534
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki1.938323
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki5.254255
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.802012
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC501.947534
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki1.670023
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki8.706622
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC501.764013
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC501.947534
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki1.352024
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki8.706622
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC501.604314
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC501.947534
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki1.856125
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki8.706622
N-acetyltransferase EisMycobacterium tuberculosis H37RvIC506.295012
N-acetyltransferase EisMycobacterium tuberculosis H37RvKi0.390011
neutrophil cytosol factor 1Homo sapiens (human)IC5050.000011
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC501.454413
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki1.191613
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CIC502.633313
Potassium channel subfamily K member 2Homo sapiens (human)IC503.650012
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC500.25052158
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki0.731137
Protease Human immunodeficiency virus 1IC50125.000011
Protease Human immunodeficiency virus 1Ki50.050022
Quinolone resistance protein NorAStaphylococcus aureusIC508.542977
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC506.690011
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)IC500.100769
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)IC500.126156
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki0.00483636
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.00953743
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)Ki0.014877
Sodium channel protein type 1 subunit alphaHomo sapiens (human)IC503.527022
Sodium channel protein type 10 subunit alphaHomo sapiens (human)IC503.527022
Sodium channel protein type 11 subunit alphaHomo sapiens (human)IC503.527022
Sodium channel protein type 2 subunit alphaHomo sapiens (human)IC503.527022
Sodium channel protein type 2 subunit alphaRattus norvegicus (Norway rat)IC500.340011
Sodium channel protein type 3 subunit alphaHomo sapiens (human)IC503.527022
Sodium channel protein type 4 subunit alphaHomo sapiens (human)IC503.527022
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC502.961333
Sodium channel protein type 7 subunit alphaHomo sapiens (human)IC503.527022
Sodium channel protein type 8 subunit alphaHomo sapiens (human)IC503.527022
Sodium channel protein type 9 subunit alphaHomo sapiens (human)IC503.527022
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC500.035512
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki2.023723
Sodium-dependent dopamine transporter Homo sapiens (human)IC502.055512
Sodium-dependent dopamine transporter Homo sapiens (human)Ki1.633512
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC501.262313
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki2.313524
Sodium-dependent serotonin transporterHomo sapiens (human)IC501.768713
Sodium-dependent serotonin transporterHomo sapiens (human)Ki1.283835
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.034211
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Ki20.000011
Solute carrier family 22 member 1 Homo sapiens (human)IC5095.750012
Solute carrier family 22 member 2Homo sapiens (human)IC5034.200011
Synaptic vesicular amine transporterHomo sapiens (human)IC500.014733
Synaptic vesicular amine transporterRattus norvegicus (Norway rat)IC500.0177110
Synaptic vesicular amine transporterBos taurus (cattle)Ki0.001011
Synaptic vesicular amine transporterHomo sapiens (human)Ki0.348433
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
TransporterRattus norvegicus (Norway rat)Ki5.500011
Trypanothione reductaseTrypanosoma cruziIC50110.000011
Trypanothione reductaseTrypanosoma cruziKi30.200011
Tryptophan 5-hydroxylase 1Rattus norvegicus (Norway rat)IC500.060011
Tyrosine-protein kinase FynHomo sapiens (human)IC505.367012
Ubiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)IC502.000022
UDP-glucuronosyltransferase 1A9Homo sapiens (human)Ki344.000011
UDP-glucuronosyltransferase 2B7Homo sapiens (human)Ki590.000011
Vesicular acetylcholine transporterRattus norvegicus (Norway rat)Ki0.391011
Vitamin D-binding proteinRattus norvegicus (Norway rat)Ki0.003711
Voltage-dependent L-type calcium channel subunit alpha-1CCavia porcellus (domestic guinea pig)IC501.415024
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC502.260377
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC502.417066
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC502.417066
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC502.417066
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
AlbuminRattus norvegicus (Norway rat)Kd51.795012
Angiotensin-converting enzyme 2 Homo sapiens (human)EC506.070012
D(2) dopamine receptorHomo sapiens (human)Kd0.014722
D(3) dopamine receptorHomo sapiens (human)Kd0.316211
D(4) dopamine receptorHomo sapiens (human)EC505.008522
Glycine receptor subunit alpha-1Homo sapiens (human)EC501.700011
HLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)Kd10.000011
Major prion proteinHomo sapiens (human)EC5010.000011
Mu-type opioid receptorHomo sapiens (human)EC5010.000011
Potassium channel subfamily K member 2Homo sapiens (human)EC500.354011
Procathepsin LHomo sapiens (human)EC506.070012
Proteasome subunit alpha type-6Homo sapiens (human)EC509.900012
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC506.070012
Replicase polyprotein 1abBetacoronavirus England 1EC506.070012
Replicase polyprotein 1abHuman coronavirus 229EEC506.070012
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC506.070012
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC506.070012
Spike glycoproteinBetacoronavirus England 1EC506.070012
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC506.070012
Synaptic vesicular amine transporterHomo sapiens (human)Kd0.008011
Transmembrane protease serine 2Homo sapiens (human)EC506.070012
Voltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)Kd0.040011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Aldehyde oxidaseHomo sapiens (human)Kii1.300011
Aldehyde oxidaseHomo sapiens (human)Kis1.300011
ATP-dependent translocase ABCB1Homo sapiens (human)Km33.000011
Carbonyl reductase [NADPH] 1Homo sapiens (human)Km1,200.000011
Cytochrome P450 3A4Homo sapiens (human)INH26.200011
D(1A) dopamine receptorHomo sapiens (human)Kb0.001411
D(1B) dopamine receptorHomo sapiens (human)Kb0.001411
D(2) dopamine receptorHomo sapiens (human)Kb0.001411
D(2) dopamine receptorHomo sapiens (human)pKi0.009111
D(3) dopamine receptorHomo sapiens (human)Kb0.001411
D(3) dopamine receptorHomo sapiens (human)pKi0.008311
D(4) dopamine receptorHomo sapiens (human)Kb0.001411
D(4) dopamine receptorHomo sapiens (human)pKi0.008011
DNA repair protein RAD52 homolog isoform aHomo sapiens (human)AC5013.660011
Histamine H2 receptorCavia porcellus (domestic guinea pig)K0.50.215012
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CINH23.733313
protein AF-9 isoform aHomo sapiens (human)AC506.310011
Quinolone resistance protein NorAStaphylococcus aureusMMC6.570011
Snq2pSaccharomyces cerevisiae EC1118INH24.333313
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km64.000011
UDP-glucuronosyltransferase 1A9Homo sapiens (human)Km174.000011
UDP-glucuronosyltransferase 2B7Homo sapiens (human)Km45.000011