Compounds > tiagabine hydrochloride
Page last updated: 2024-12-07

tiagabine hydrochloride

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Description

Tiagabine hydrochloride is an anticonvulsant medication used to treat partial seizures. It is a selective inhibitor of the GABA transporter protein (GAT-1), which is responsible for the reuptake of the neurotransmitter GABA from the synaptic cleft. By blocking GAT-1, tiagabine increases the concentration of GABA in the synapse, which has an inhibitory effect on neuronal activity and helps to prevent seizures. Tiagabine is synthesized through a multi-step process that involves the reaction of 2-amino-4-phenylbutanoic acid with thionyl chloride followed by reaction with an amine. The mechanism of action of tiagabine has been extensively studied, and its effects on GABAergic neurotransmission have been well-characterized. Tiagabine is an important medication for the treatment of partial seizures, and it is studied to improve its efficacy and safety. Tiagabine is also being investigated for its potential use in other neurological disorders, such as anxiety, depression, and neuropathic pain.'

tiagabine hydrochloride : A hydrochloride resulting from the reaction of equimolar amounts of tiagabine and hydrogen chloride. A GABA reuptake inhibitor, it is used for the treatment of epilepsy. [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 CID91274
CHEMBL ID1695
CHEBI ID85388
SCHEMBL ID41860
MeSH IDM0164768

Synonyms (92)

Synonym
nn-301
a-70569
cep-6671
abbott 70569.hcl
3-piperidinecarboxylic acid, 1-(4,4-bis(3-methyl-2-thienyl)-3-butenyl)-, hydrochloride, (r)-
no-328
abt 569
tiagabine hydrochloride [usan]
tiagabine hydrochloride
c20h25no2s2.hcl
abt-569
nnc-05-0328
tiabex
no-05-0328
(-)-(r)-1-(4,4-bis(3-methyl-2-thienyl)-3-butenyl)nipecotic acid, hydrochloride
3-piperidinecarboxylic acid, 1-(4,4-bis(3-methyl-2-thienyl)-3-buten-yl)-, hydrochloride, (r)-
(r)-(4,4-bis(3-methyl-2-thienyl)-3-butenyl)-3-piperidinecarboxylic acid, hydrochloride
MLS001401367
smr000469176
tiagabine hcl
145821-59-6
D02097
tiagabine hydrochloride (usp)
chebi:85388 ,
abbott-70569 hydrochloride
nnc-050328
CHEMBL1695
abbott-70569.1
abbott-705691
no-050328
abbott-70569.hcl
(3r)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid hydrochloride
dtxsid2044218 ,
cas-145821-59-6
tox21_112245
dtxcid0024218
unii-dqh6t6d8oy
dqh6t6d8oy ,
tiagabine hydrochloride [usan:usp]
S4661 ,
CCG-100885
(-)-(r)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]nipecotic acid hydrochloride
tiagabine hydrochloride [usp-rs]
tiagabine hydrochloride [who-dd]
tiagabine hydrochloride [mart.]
tiagabine hydrochloride [orange book]
tiagabine hydrochloride [vandf]
tiagabine hydrochloride [usp monograph]
tiagabine hydrochloride [mi]
YUKARLAABCGMCN-PKLMIRHRSA-N
tiagabine (hydrochloride)
HY-B0696A
NC00135
SCHEMBL41860
tox21_112245_1
NCGC00164626-02
KS-1217
T3165
AKOS024258856
(r)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-en-1-yl)piperidine-3-carboxylic acid hydrochloride
(-)-(r)-1-(4,4-bis(3-methyl-2-thienyl)-3-butenyl)nipecotic acid hydrochloride
tiagabine monohydrochloride
(3r)-1-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]piperidine-3-carboxylic acid monohydrochloride
(3r)-1-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]-3-carboxypiperidinium chloride
(3r)-1-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]piperidine-3-carboxylic acid hydrochloride
ethanone, 1-imidazo[1,2-b]pyridazin-3-yl-
HB0978
mfcd07369025
(3r)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-en-1-yl]piperidine-3-carboxylic acid hydrochloride
tiagabine hydrochloride, >=98% (hplc)
tiagabine hydrochloride 1.0 mg/ml in methanol (as free base)
J-008159
A884577
Q27158534
145821-59-6 (hcl)
Z2196311163
tgb hydrochloride
no328 hydrochloride
gabitril hydrochloride
no050328 hydrochloride
3-piperidinecarboxylic acid, 1-[4,4-bis(3-methyl-2-thienyl)-3-buten-1-yl]-, hydrochloride (1:1), (3r)-
C72768
(r)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-en-1-yl)piperidine-3-carboxylicacidhydrochloride
EN300-221591
tiagabine hydrochloride (usp monograph)
tiagabine hydrochloride (usan:usp)
tiagabine hydrochloride (usp-rs)
(3r)-1-(4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl)piperidine-3-carboxylic acid hydrochloride
3-piperidinecarboxylic acid, 1-(4,4-bis(3-methyl-2-thienyl)-3-buten-yl)-, hydrochloride,(r)-
(3r)-1-(4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl)-3-carboxypiperidinium chloride
tiagabine hydrochloride (mart.)
(3r)-1-(4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl)piperidine-3-carboxylic acid monohydrochloride

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
anticonvulsantA drug used to prevent seizures or reduce their severity.
GABA reuptake inhibitorA compound that inhibits the re-uptake of the neurotransmitter GABA from the synapse into the pre-synaptic neuron, so increasing the extracellular concentrations of the neurotransmitter and hence increasing neurotransmission.
[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 (1)

ClassDescription
hydrochlorideA salt formally resulting from the reaction of hydrochloric acid with an organic base.
[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 (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.33490.006038.004119,952.5996AID1159521
TDP1 proteinHomo sapiens (human)Potency31.67680.000811.382244.6684AID686978; AID686979
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency38.90180.01237.983543.2770AID1645841
estrogen nuclear receptor alphaHomo sapiens (human)Potency21.13170.000229.305416,493.5996AID743079
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency8.41200.023723.228263.5986AID743222
gemininHomo sapiens (human)Potency1.25890.004611.374133.4983AID624297
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency3.98110.009610.525035.4813AID1479145
[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)
Sodium- and chloride-dependent GABA transporter 1Homo sapiens (human)IC50 (µMol)0.04900.01013.090310.0000AID764978
Sodium- and chloride-dependent GABA transporter 1Mus musculus (house mouse)IC50 (µMol)0.08000.03712.19228.5114AID308127
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
memorySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
associative learningSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
synapse organizationSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
chemical synaptic transmissionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to toxic substanceSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to sucroseSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to inorganic substanceSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to lead ionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
positive regulation of gamma-aminobutyric acid secretionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to purine-containing compoundSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to estradiolSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to cocaineSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to calcium ionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
gamma-aminobutyric acid reuptakeSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
gamma-aminobutyric acid importSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
inorganic anion import across plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
sodium ion import across plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
transport across blood-brain barrierSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
chloride transmembrane transportSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
sodium ion transmembrane transportSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
amino acid transportSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
gamma-aminobutyric acid:sodium:chloride symporter activitySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
protein bindingSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
gamma-aminobutyric acid transmembrane transporter activitySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
sodium:chloride symporter activitySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
identical protein bindingSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
metal ion bindingSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
axonSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
presynaptic membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
neuronal cell bodySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
postsynaptic membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
GABA-ergic synapseSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
axonSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
cell surfaceSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (62)

Assay IDTitleYearJournalArticle
AID205445In vitro inhibition of [3H]GABA uptake at the Sodium- and chloride-dependent GABA transporter 1 (GAT-1) uptake site in rat brain synaptosomes1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Synthesis of novel GABA uptake inhibitors. 3. Diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents.
AID113027In vivo anticonvulsant effect of DMCM-induced clonic seizures in mice at 15 mg/kg intraperitoneal dose expressed as effective dose1993Journal of medicinal chemistry, Jun-11, Volume: 36, Issue:12
The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidate.
AID114502Evaluation for Ataxia (neurological toxicity) in mice using a rotarod apparatus.1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Synthesis of novel GABA uptake inhibitors. 3. Diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents.
AID113025In vivo anticonvulsant effect measured as inhibition of DMCM -induced seizures in mice after ip administration.2001Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
Synthesis of novel gamma-aminobutyric acid (GABA) uptake inhibitors. 5.(1) Preparation and structure-activity studies of tricyclic analogues of known GABA uptake inhibitors.
AID1859399Inhibition of GAT-mediated [3H]-GABA uptake in rat forebrain synaptosomes preincubated for 8 mins followed by [3H]-GABA addition measured after 8 mins by scintillation counting method2022European journal of medicinal chemistry, Apr-15, Volume: 234Nipecotic acid as potential lead molecule for the development of GABA uptake inhibitors; structural insights and design strategies.
AID764967Anticonvulsant activity in icv dosed PTZ-induced ICR mouse seizure model assessed as delay in latency of clonic convulsions administered 30 mins prior to PTZ-challenge measured for 15 mins2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports.
AID226944Ratio for ED50 for inhibition of rotarod and inhibition of DMCM induced convulsions in mice1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Synthesis of novel GABA uptake inhibitors. 4. Bioisosteric transformation and successive optimization of known GABA uptake inhibitors leading to a series of potent anticonvulsant drug candidates.
AID764971Anticonvulsant activity in PTZ-induced ICR mouse seizure model assessed as increase in duration of tremor at 30 to 1000 nmol, icv administered 30 mins prior to PTZ-challenge measured for 15 mins2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports.
AID764963Anticonvulsant activity in PTZ-induced ICR mouse seizure model assessed as inhibition of tonic convulsions at 100 nmol, icv administered 30 mins prior to PTZ-challenge measured for 15 mins relative to vehicle-treated control2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports.
AID764965Anticonvulsant activity in icv dosed PTZ-induced ICR mouse seizure model assessed as inhibition of tonic convulsions administered 30 mins prior to PTZ-challenge measured for 15 mins2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports.
AID180487In vitro inhibition of [3H]GABA uptake in rat synaptosomes1993Journal of medicinal chemistry, Jun-11, Volume: 36, Issue:12
The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidate.
AID113322Dose that protected 50% of the mice against seizures induced by intraperitoneally administered DMCM (15 mg/Kg) 30 min after intraperitoneal administration1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Synthesis of novel GABA uptake inhibitors. 3. Diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents.
AID308127Inhibition of [3H]GABA uptake at mouse GAT1 expressed in D8 cells2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and biological evaluation of (R)-N-(diarylmethylthio/sulfinyl)ethyl/propyl-piperidine-3-carboxylic acid hydrochlorides as novel GABA uptake inhibitors.
AID205300In vitro inhibition of [3H]GABA uptake in rat synaptosomes1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Synthesis of novel GABA uptake inhibitors. 4. Bioisosteric transformation and successive optimization of known GABA uptake inhibitors leading to a series of potent anticonvulsant drug candidates.
AID112192The anticonvulsant activity was measured by performing rotarod test in mice.1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Synthesis of novel GABA uptake inhibitors. 4. Bioisosteric transformation and successive optimization of known GABA uptake inhibitors leading to a series of potent anticonvulsant drug candidates.
AID112193Anticonvulsant activity measured by the inhibition of DMCM-induced seizures in mice.1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Synthesis of novel GABA uptake inhibitors. 4. Bioisosteric transformation and successive optimization of known GABA uptake inhibitors leading to a series of potent anticonvulsant drug candidates.
AID1859400Anticonvulsant activity in mouse assessed as inhibition of DMCM-induced seizures administered intraperitoneally2022European journal of medicinal chemistry, Apr-15, Volume: 234Nipecotic acid as potential lead molecule for the development of GABA uptake inhibitors; structural insights and design strategies.
AID113026In vivo anticonvulsant effect measured as rotarod in mice after ip administration2001Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
Synthesis of novel gamma-aminobutyric acid (GABA) uptake inhibitors. 5.(1) Preparation and structure-activity studies of tricyclic analogues of known GABA uptake inhibitors.
AID26799Lipophilicity measured as partition between octanol and pH 7.4 buffer1993Journal of medicinal chemistry, Jun-11, Volume: 36, Issue:12
The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidate.
AID764978Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (15.79)18.2507
2000's3 (15.79)29.6817
2010's6 (31.58)24.3611
2020's7 (36.84)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.08

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index31.08 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.81 (4.65)
Search Engine Demand Index38.54 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (31.08)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.26%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other18 (94.74%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
beta-alanine
[no description available]		2.0810amino acid zwitterion;
beta-amino acid		agonist;
fundamental metabolite;
human metabolite;
inhibitor;
neurotransmitter
baclofen
[no description available]		2.0810amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid;
monochlorobenzenes;
primary amino compound		central nervous system depressant;
GABA agonist;
muscle relaxant
diazepam
Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.		1.98101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
muscimol
Muscimol: A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies.. muscimol : A member of the class of isoxazoles that is 1,2-oxazol-3(2H)-one substituted by an aminomethyl group at position 5. It has been isolated from mushrooms of the genus Amanita.		2.0810alkaloid;
isoxazoles;
primary amino compound		fungal metabolite;
GABA agonist;
oneirogen;
psychotropic drug
tiagabine
Tiagabine: A nipecotic acid derivative that acts as a GABA uptake inhibitor and anticonvulsant agent. It is used in the treatment of EPILEPSY, for refractory PARTIAL SEIZURES.. tiagabine : A piperidinemonocarboxylic acid that is (R)-nipecotic acid in which the hydrogen attached to the nitrogen has been replaced by a 1,1-bis(3-methyl-2-thienyl)but-1-en-4-yl group. A GABA reuptake inhibitor, it is used (generally as the hydrochloride salt) for the treatment of epilepsy.		3.5110beta-amino acid;
piperidinemonocarboxylic acid;
tertiary amino compound;
thiophenes		anticonvulsant;
GABA reuptake inhibitor
nnc 711
NNC 711: structure in first source		210
nipecotic acid
(R)-nipecotic acid : The (R)-enantiopmer of nipecotic acid.		2.4620amino acid zwitterion;
nipecotic acid
nipecotic acid, (s)-isomer
(S)-nipecotic acid : The (S)-enantiomer of nipecotic acid.		2.0810nipecotic acid
sk&f 89976-a
[no description available]		2.9140
nnc 05-2090
NNC 05-2090: structure given in first source		2.0810carbazoles
snap 5114
[no description available]		2.0810
ConditionIndicatedRelationship StrengthStudiesTrials
Absence Seizure
[description not available]		02.7130
Seizures
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.		14.7130
Innate Inflammatory Response
[description not available]		02.0510
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.0510
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510