Page last updated: 2024-11-04

psilocin

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Description

psilocin: psilocybine minus the phosphate ester; RN given refers to parent cpd; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

psilocin : A tryptamine alkaloid that is N,N-dimethyltryptamine carrying an additional hydroxy substituent at position 4. A hallucinogenic alkaloid isolated in trace amounts from Psilocybe mushrooms (also known as Teonanacatl or "magic mushrooms"). [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID4980
CHEMBL ID65547
CHEBI ID8613
SCHEMBL ID194899
MeSH IDM0053512

Synonyms (53)

Synonym
cms88kuw0g ,
5-22-12-00014 (beilstein handbook reference)
unii-cms88kuw0g
1h-indol-4-ol, 3-[2-(dimethylamino)ethyl]-
dea no. 7438
cx-59
psilocyn
indol-4-ol, 3-(2-(dimethylamino)ethyl)-
brn 0160503
3-(2-(dimethylamino)ethyl)-1h-indol-4-ol
einecs 208-296-5
C08312
psilocin
520-53-6
psilocine
psilotsin
CHEBI:8613 ,
n,n-dimethyl-4-hydroxytryptamine
3-[2-(dimethylamino)ethyl]-1h-indol-4-ol
4-oh-dmt
3-(2-(dimethylamino)ethyl)indol-4-ol
4-hydroxy-n,n-dimethyltryptamine
P-7800
spciygntamctro-uhfffaoysa-
inchi=1/c12h16n2o/c1-14(2)7-6-9-8-13-10-4-3-5-11(15)12(9)10/h3-5,8,13,15h,6-7h2,1-2h3
bdbm50081701
4-ho-dmt
CHEMBL65547 ,
L000675
NCGC00247728-01
dtxcid5028825
tox21_112894
dtxsid5048899 ,
cas-520-53-6
AKOS022505992
SCHEMBL194899
psilocin [mi]
psilocin [mart.]
psilocin [who-dd]
SPCIYGNTAMCTRO-UHFFFAOYSA-N
psilocin/psilocybin (salt/mix)
indol-4-ol, 3-[2-(dimethylamino)ethyl]-
cx 59
magic mushrooms (salt/mix)
3-[2-(dimethylamino)ethyl]-1h-indol-4-ol #
psilocin, vial of 5 mg, certified reference material
3-[2-(dimethylamino)ethyl]-indol-4-ol
Q409150
EN-0002
gtpl11291
91q ,
3-[2-(dimethylamino)ethyl]-1~{h}-indol-4-ol
psilocin, 1mg/ml in acetonitrile

Research Excerpts

Overview

Psilocin is an active metabolite form of psilocybin and exerts psychoactive effects.

ExcerptReferenceRelevance
"Psilocin is an active metabolite form of psilocybin and exerts psychoactive effects. "( Psilocin suppresses methamphetamine-induced hyperlocomotion and acquisition of conditioned place preference via D2R-mediated ERK signaling.
An, R; Li, T; Liang, M; Liu, H; Liu, X; Qian, H; Shang, Q; Shao, G; Wang, J, 2023
)
3.8

Effects

ExcerptReferenceRelevance
"Psilocin has regulatory effects on METH-induced alterations of behavior in mice via D2R-mediated signal regulation of ERK phosphorylation."( Psilocin suppresses methamphetamine-induced hyperlocomotion and acquisition of conditioned place preference via D2R-mediated ERK signaling.
An, R; Li, T; Liang, M; Liu, H; Liu, X; Qian, H; Shang, Q; Shao, G; Wang, J, 2023
)
3.8

Toxicity

ExcerptReferenceRelevance
" When the pure psilocin or fungal extracts were used, slight differences in determined LD50 values were observed."( Research on acute toxicity and the behavioral effects of methanolic extract from psilocybin mushrooms and psilocin in mice.
Godovan, VV; Halama, M; Jasicka-Misiak, I; Kazakova, A; Poliwoda, A; Wieczorek, PP; Zhuk, O, 2015
)
0.98

Pharmacokinetics

The pharmacokinetics of psilocin were linear within the twofold range of doses. The elimination half-life of pSilocin was 3 h (standard deviation 1.5h)

ExcerptReferenceRelevance
"In order to investigate the pharmacokinetic properties of psilocybin (PY), the main psychoactive compound of Psilocybe mushrooms, high performance liquid chromatographic procedures with column-switching coupled with electrochemical detection (HPLC-ECD) for reliable quantitative determination of the PY metabolites psilocin (PI) and 4-hydroxyindole-3-acetic acid (4HIAA) in human plasma were established."( Determination of psilocin and 4-hydroxyindole-3-acetic acid in plasma by HPLC-ECD and pharmacokinetic profiles of oral and intravenous psilocybin in man.
Bär, T; Bourquin, D; Brenneisen, R; Hasler, F; Vollenweider, FX, 1997
)
0.81

Bioavailability

ExcerptReferenceRelevance
" Estimates for the absolute bioavailability of PI after oral administration of PY were 52."( Determination of psilocin and 4-hydroxyindole-3-acetic acid in plasma by HPLC-ECD and pharmacokinetic profiles of oral and intravenous psilocybin in man.
Bär, T; Bourquin, D; Brenneisen, R; Hasler, F; Vollenweider, FX, 1997
)
0.64
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Dose-response and time-response curves were obtained."( Psilocybin as a discriminative stimulus: lack of specificity in an animal behavior model for 'hallucinogens'.
Appel, JB; Koerner, J, 1982
)
0.26
" In reviewing these topics, we identify three knowledge gaps as areas of future inquiry: sex differences, oral dosing rather than injection, and chronic dosing regimens."( Addressing the Current Knowledge and Gaps in Research Surrounding Lysergic Acid Diethylamide (LSD), Psilocybin, and Psilocin in Rodent Models.
Ezeaka, UC; Kim, HJJ; Laprairie, RB, 2023
)
1.12
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
hallucinogenDrugs capable of inducing illusions, hallucinations, delusions, paranoid ideations and other alterations of mood and thinking.
serotonergic agonistAn agent that has an affinity for serotonin receptors and is able to mimic the effects of serotonin by stimulating the physiologic activity at the cell receptors. Serotonin agonists are used as antidepressants, anxiolytics, and in the treatment of migraine disorders.
fungal metaboliteAny eukaryotic metabolite produced during a metabolic reaction in fungi, the kingdom that includes microorganisms such as the yeasts and moulds.
human xenobiotic metaboliteAny human metabolite produced by metabolism of a xenobiotic compound in humans.
drug metabolitenull
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
tryptamine alkaloid
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
hydroxyindolesAny member of the class of indoles carrying at least one hydroxy group.
phenolsOrganic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (24)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency15.47430.002541.796015,848.9004AID1347395; AID1347398
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency61.01933.189029.884159.4836AID1224846
TDP1 proteinHomo sapiens (human)Potency24.24910.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency38.11930.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency0.85470.000221.22318,912.5098AID743042
progesterone receptorHomo sapiens (human)Potency67.89270.000417.946075.1148AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.11400.01237.983543.2770AID1645841
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency75.06240.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency41.97630.000817.505159.3239AID1159527; AID1159531
estrogen nuclear receptor alphaHomo sapiens (human)Potency42.46550.000229.305416,493.5996AID1259248; AID743075; AID743079; AID743080; AID743091
cytochrome P450 2D6Homo sapiens (human)Potency12.49870.00108.379861.1304AID1645840
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency5.39290.001723.839378.1014AID743083
thyroid stimulating hormone receptorHomo sapiens (human)Potency43.76900.001628.015177.1139AID1259385; AID1259395
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency61.019319.739145.978464.9432AID1159509
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency48.46940.057821.109761.2679AID1159526; AID1159528
Histone H2A.xCricetulus griseus (Chinese hamster)Potency56.05000.039147.5451146.8240AID1224845
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency57.21920.000323.4451159.6830AID743065; AID743067
heat shock protein beta-1Homo sapiens (human)Potency60.49060.042027.378961.6448AID743210; AID743228
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency24.08170.000627.21521,122.0200AID743202
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.28200.00010.601710.0000AID385348; AID5496; AID5577
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)0.00830.00010.88018.8500AID1834408
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)0.00780.00011.03029.0000AID1834410
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)0.00110.00011.18738.9125AID1834409
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)EC50 (µMol)2.30000.00010.49294.0000AID5466
5-hydroxytryptamine receptor 2AHomo sapiens (human)EC50 (µMol)0.26510.00000.22763.4750AID1648179; AID1769402; AID1782619; AID1815952; AID1880246; AID1893756; AID255670
5-hydroxytryptamine receptor 2CHomo sapiens (human)EC50 (µMol)0.03000.00010.10082.4500AID255671
5-hydroxytryptamine receptor 2AMus musculus (house mouse)EC50 (µMol)0.00980.00980.00980.0099AID1648181
5-hydroxytryptamine receptor 2BHomo sapiens (human)EC50 (µMol)0.05800.00040.20611.0000AID255672
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)K0.50.00600.00600.01350.0210AID5495
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (72)

Processvia Protein(s)Taxonomy
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (74)

Assay IDTitleYearJournalArticle
AID5495Compound was tested for binding affinity at 5-hydroxytryptamine 2A receptor sites in rat cortical homogenate using [125I]-2,5-Dimethoxy -4-iodoamphetamine (DOI).1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Further studies on oxygenated tryptamines with LSD-like activity incorporating a chiral pyrrolidine moiety into the side chain.
AID21908Partition coefficient of octanol and water was determined1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Comparison of solution conformational preferences for the hallucinogens bufotenin and psilocin using 360-MHz proton NMR spectroscopy.
AID1834411Modulation of human 5HT2A expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Improved 5-HT2 Selective Receptor Modulators for the Treatment of Psychological Disorders.
AID1769403Metabolic stability in human liver microsomes assessed as intrinsic clearance measured after 60 mins by LC-MS/MS analysis2021ACS medicinal chemistry letters, Oct-14, Volume: 12, Issue:10
Psilocin Derivatives as Serotonergic Psychedelic Agents for the Treatment of CNS Disorders.
AID5577In vitro binding to 5-hydroxytryptamine 2A receptor using [125 I]-DOI2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands.
AID5466Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands.
AID1893756Agonist activity at human 5-HT2A receptor assessed as activation of calcium mobilization incubated for 2 mins by Calcium-6 dye based FLIPR assay2022ACS medicinal chemistry letters, Sep-08, Volume: 13, Issue:9
Restoration of Motor Function Post-Neurological Injury Using Serotonergic Agonist.
AID1815952Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay2022ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
Improved Metabolically Stable 5-HT Receptor Modulators and the Development of New Antidepressants.
AID1648180Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay relative to serotonin2020Journal of natural products, 02-28, Volume: 83, Issue:2
Synthesis and Biological Evaluation of Tryptamines Found in Hallucinogenic Mushrooms: Norbaeocystin, Baeocystin, Norpsilocin, and Aeruginascin.
AID1815948Stability in human liver mitochondria assessed as intrinsic clearance in presence of MAO-A and MAO-B2022ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
Improved Metabolically Stable 5-HT Receptor Modulators and the Development of New Antidepressants.
AID25806Ionization constant of compound was determined1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Comparison of solution conformational preferences for the hallucinogens bufotenin and psilocin using 360-MHz proton NMR spectroscopy.
AID185557Maximum 5-HT stimulation was determined in cloned rats2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands.
AID385348Displacement of [3H]MDL100907 from 5HT2A receptor in Sprague-Dawley rat brain by liquid scintillation spectroscopy2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands.
AID1880246Agonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
3-Pyrrolidine-indole Derivatives as 5-HT2-Selective Receptor Modulators for the Potential Treatment of Mental Disorders.
AID385349Lipophilicity of compound by immobilized artificial membrane column containing phosphatidylcholine head groups HPLC2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands.
AID1834409Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Improved 5-HT2 Selective Receptor Modulators for the Treatment of Psychological Disorders.
AID1769402Displacement of [3H]-ketanserin from human 5-HT2A receptor incubated for 90 mins by scintillation counting analysis2021ACS medicinal chemistry letters, Oct-14, Volume: 12, Issue:10
Psilocin Derivatives as Serotonergic Psychedelic Agents for the Treatment of CNS Disorders.
AID24170Partition coefficient (logP)1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Comparison of solution conformational preferences for the hallucinogens bufotenin and psilocin using 360-MHz proton NMR spectroscopy.
AID3864Tested in vitro for its ability to bind to 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand; ND means Not determined2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands.
AID1815951Stability in rat brain homogenate assessed as half life2022ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
Improved Metabolically Stable 5-HT Receptor Modulators and the Development of New Antidepressants.
AID1815949Stability in human liver mitochondria assessed as compound remaining in presence of MAO-A and MAO-B measured after 60 mins2022ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
Improved Metabolically Stable 5-HT Receptor Modulators and the Development of New Antidepressants.
AID26061True partition coefficient corrected for ionization was determined1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Comparison of solution conformational preferences for the hallucinogens bufotenin and psilocin using 360-MHz proton NMR spectroscopy.
AID1782619Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
The Psychedelic Renaissance: Addressing Potential Adverse Effects in a Therapeutic Setting.
AID1834413Modulation of human 5HT2C expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Improved 5-HT2 Selective Receptor Modulators for the Treatment of Psychological Disorders.
AID385350Agonist activity at Sprague-Dawley rat 5HT2A receptor by drug discrimination assay2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands.
AID1131957Hallucinogenic activity in human relative to mescaline1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Structure-activity studies on hallucinogenic amphetamines using molecular connectivity.
AID1769404Metabolic stability in human liver microsomes assessed as half life measured after 60 mins by LC-MS/MS analysis2021ACS medicinal chemistry letters, Oct-14, Volume: 12, Issue:10
Psilocin Derivatives as Serotonergic Psychedelic Agents for the Treatment of CNS Disorders.
AID1782621Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as maximal effect by FLIPR calcium flux assay relative to control2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
The Psychedelic Renaissance: Addressing Potential Adverse Effects in a Therapeutic Setting.
AID1648182Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay relative to serotonin2020Journal of natural products, 02-28, Volume: 83, Issue:2
Synthesis and Biological Evaluation of Tryptamines Found in Hallucinogenic Mushrooms: Norbaeocystin, Baeocystin, Norpsilocin, and Aeruginascin.
AID5496Compound was tested for binding affinity using [3H]MDL-100,907 at 5-hydroxytryptamine 2A receptor sites in rat cortical homogenate.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Further studies on oxygenated tryptamines with LSD-like activity incorporating a chiral pyrrolidine moiety into the side chain.
AID1648181Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay2020Journal of natural products, 02-28, Volume: 83, Issue:2
Synthesis and Biological Evaluation of Tryptamines Found in Hallucinogenic Mushrooms: Norbaeocystin, Baeocystin, Norpsilocin, and Aeruginascin.
AID1834410Modulation of human 5HT2C expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Improved 5-HT2 Selective Receptor Modulators for the Treatment of Psychological Disorders.
AID1815947Stability in human liver mitochondria assessed as half life in presence of MAO-A and MAO-B2022ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
Improved Metabolically Stable 5-HT Receptor Modulators and the Development of New Antidepressants.
AID1648179Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay2020Journal of natural products, 02-28, Volume: 83, Issue:2
Synthesis and Biological Evaluation of Tryptamines Found in Hallucinogenic Mushrooms: Norbaeocystin, Baeocystin, Norpsilocin, and Aeruginascin.
AID1815950Stability in rat brain homogenate assessed as compound remaining measured after 120 mins2022ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
Improved Metabolically Stable 5-HT Receptor Modulators and the Development of New Antidepressants.
AID1834408Modulation of human 5HT2A expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Improved 5-HT2 Selective Receptor Modulators for the Treatment of Psychological Disorders.
AID1834412Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Improved 5-HT2 Selective Receptor Modulators for the Treatment of Psychological Disorders.
AID255671Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2C receptor determined by phosphoinositide hydrolysis assay2005Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
AID255672Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay2005Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
AID255670Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assay2005Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
AID5747Tested in vitro for its ability to bind to 5-hydroxytryptamine 2C receptor using [125 I]-DOI as radioligand; Not determined2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (126)

TimeframeStudies, This Drug (%)All Drugs %
pre-199024 (19.05)18.7374
1990's8 (6.35)18.2507
2000's27 (21.43)29.6817
2010's31 (24.60)24.3611
2020's36 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 76.85

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index76.85 (24.57)
Research Supply Index4.93 (2.92)
Research Growth Index4.90 (4.65)
Search Engine Demand Index133.77 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (76.85)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (3.79%)5.53%
Reviews7 (5.30%)6.00%
Case Studies6 (4.55%)4.05%
Observational0 (0.00%)0.25%
Other114 (86.36%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase 1, Open-Label, One-Treatment, Single-Dose, One-Period, Pharmacokinetic Study of Psilocin 4 mg as Its Mucic Acid Salt (L-130) Form, in Healthy Subjects Under Fasted Conditions [NCT06035900]Phase 110 participants (Actual)Interventional2023-06-21Completed
Precision Functional Brain Mapping to Understand the Mechanisms of Psilocybin [NCT04501653]Early Phase 125 participants (Anticipated)Interventional2021-06-01Active, not recruiting
Comparison of the Effects of PEX20 (Oral Psilocin), PEX30 (Sublingual Psilocin), and PEX10 (Oral Psilocybin) in Healthy Adults [NCT05317689]Phase 120 participants (Anticipated)Interventional2022-05-26Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]