Page last updated: 2024-11-06

stiripentol

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

stiripentol: structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5311454
CHEMBL ID1983350
CHEBI ID94435
SCHEMBL ID216436
SCHEMBL ID2533815
MeSH IDM0075555

Synonyms (71)

Synonym
me-2080
bcx-2600
diacomit
stiripentol [usan:inn]
1-penten-3-ol, 4,4-dimethyl-1-(3,4-methylenedioxyphenyl)-
1-(1,3-benzodioxol-5-yl)-4,4-dimethyl-1-penten-3-ol
stiripentolum [inn-latin]
brn 1313047
einecs 256-480-9
estiripentol [inn-spanish]
bcx 2600
4,4-dimethyl-1-((3,4-methylenedioxy)phenyl)-1-penten-3-ol
diacomit (tn)
D05928
stiripentol (jan/usan/inn)
MLS001424144
stiripentol
MLS000758313
smr000449279
cpd000449279
49763-96-4
HMS2052K07
NCGC00185769-01
cas-49763-96-4
dtxsid6049068 ,
tox21_113622
dtxcid1028994
HMS2232P06
CHEMBL1983350
CCG-101092
estiripentol
stiripentolum
5-19-02-00640 (beilstein handbook reference)
S5266
(1e)-1-(2h-1,3-benzodioxol-5-yl)-4,4-dimethylpent-1-en-3-ol
gtpl5469
131206-47-8
stiripentol [orange book]
SCHEMBL216436
NC00342
(e)-1-(benzo[d][1,3]dioxol-5-yl)-4,4-dimethylpent-1-en-3-ol
SCHEMBL2533815
AKOS025149123
mfcd00869310
DB09118
AKOS027255159
CHEBI:94435
137767-55-6
bdbm50504273
stiripentol, >=98% (hplc)
CS-7801
HY-103392
Q412182
1-(benzo[d][1,3]dioxol-5-yl)-4,4-dimethylpent-1-en-3-ol
BS-16863
bcx2600; bcx-2600; bcx 2600
BCP10434
HMS3886M17
CCG-266819
NCGC00185769-02
bcx2600
W10731
DTXSID80860609
(1e)-1-(1,3-benzodioxol-5-yl)-4,4-dimethyl-1-penten-3-ol
(1e)-1-(1,3-dioxaindan-5-yl)-4,4-dimethylpent-1-en-3-ol
EN300-7393003
n03ax17
stiripentolum (inn-latin)
estiripentol (inn-spanish)
(1e,3rs)-1-(benzo(d)(1,3)dioxol-5-yl)-4,4-dimethylpent-1-en-3-ol
stiripentol (mart.)

Research Excerpts

Toxicity

Stiripentol is safe and effective during long-term use in patients with DS in routine clinical practice. In infants with Dravet syndrome, stiripents significantly reduce long-lasting seizures including status epilepticus.

ExcerptReferenceRelevance
" Twenty-two patients experienced stiripentol-related adverse events, with two having severe ones."( Long-term safety and efficacy of stiripentol for the treatment of Dravet syndrome: A multicenter, open-label study in Japan.
Inoue, Y; Ohtsuka, Y, 2015
)
0.42
"During adjunctive stiripentol use with clobazam and valproate, careful monitoring for adverse events such as somnolence and loss of appetite is recommended, and dose reduction may become needed for any of the antiepileptics."( Long-term safety and efficacy of stiripentol for the treatment of Dravet syndrome: A multicenter, open-label study in Japan.
Inoue, Y; Ohtsuka, Y, 2015
)
0.42
" Frequency of generalized tonic-clonic seizures, focal seizures, status epilepticus, and adverse events were recorded."( Stiripentol efficacy and safety in Dravet syndrome: a 12-year observational study.
Cross, JH; Lightfoot, P; Myers, KA; Patil, SG; Scheffer, IE, 2018
)
0.48
" The most common adverse events were anorexia, weight loss, sedation, and behavioural changes."( Stiripentol efficacy and safety in Dravet syndrome: a 12-year observational study.
Cross, JH; Lightfoot, P; Myers, KA; Patil, SG; Scheffer, IE, 2018
)
0.48
" Adverse drug reactions occurred in 70 % of new patients; the most common were somnolence (39 %) and loss of appetite (25 %)."( Long-term safety and effectiveness of stiripentol in patients with Dravet syndrome: Interim report of a post-marketing surveillance study in Japan.
Inoue, Y; Matsui, D; Ohtsuka, Y; Suzuki, K; Yamada, M, 2021
)
0.62
"Stiripentol is safe and effective during long-term use in patients with DS in routine clinical practice."( Long-term safety and effectiveness of stiripentol in patients with Dravet syndrome: Interim report of a post-marketing surveillance study in Japan.
Inoue, Y; Matsui, D; Ohtsuka, Y; Suzuki, K; Yamada, M, 2021
)
0.62
" Three patients discontinued stiripentol for adverse events; 55% reported at least one adverse event, mostly loss of appetite/weight (21%) and somnolence (11%)."( Initiating stiripentol before 2 years of age in patients with Dravet syndrome is safe and beneficial against status epilepticus.
Chancharme, L; Chemaly, N; Chiron, C; Nabbout, R, 2023
)
0.91
"Initiating stiripentol in infants with Dravet syndrome is safe and beneficial, significantly reducing long-lasting seizures including status epilepticus, hospitalizations, and mortality in the critical first years of life."( Initiating stiripentol before 2 years of age in patients with Dravet syndrome is safe and beneficial against status epilepticus.
Chancharme, L; Chemaly, N; Chiron, C; Nabbout, R, 2023
)
0.91

Pharmacokinetics

Stiripentol showed a significant degree of tolerance to the anticonvulsant and neurotoxic effects following subacute treatment with the racemic compound. Study undertook to define the overall pharmacokinetic profile of stiripentl in rhesus monkey prior to its efficacy evaluation.

ExcerptReferenceRelevance
"557 l/h/kg) and a shorter half-life (2."( Comparative anticonvulsant potency and pharmacokinetics of (+)-and (-)-enantiomers of stiripentol.
Boddy, AV; Lepage, F; Levy, RH; Savitch, JL; Shen, DD; Tombret, F, 1992
)
0.28
" This study undertook to define the overall pharmacokinetic profile of stiripentol in rhesus monkey prior to its efficacy evaluation."( Pharmacokinetic profile of a new anticonvulsant, stiripentol, in the rhesus monkey.
Levy, RH; Lin, HS, 1983
)
0.27
"An earlier pharmacodynamic study of the chiral antiepileptic drug stiripentol in an intravenous pentylenetetrazol-induced seizure model in the rat showed the development of a significant degree of tolerance to the anticonvulsant and neurotoxic effects following subacute treatment with the racemic compound."( Stereoselective pharmacokinetics of stiripentol: an explanation for the development of tolerance to anticonvulsant effect.
Arends, RH; Baillie, TA; Levy, RH; Shen, DD; Zhang, K, 1994
)
0.29
" Three of the new drugs, gabapentin, topiramate and vigabatrin, are more promising on the basis of their pharmacokinetic features."( Comparative pharmacokinetics of the newer antiepileptic drugs.
Bialer, M, 1993
)
0.29
" Brain AED concentrations were also measured so as to ascertain any pharmacokinetic contribution to the pharmacodynamic interactions."( Characterization of the anticonvulsant, behavioral and pharmacokinetic interaction profiles of stiripentol in combination with clonazepam, ethosuximide, phenobarbital, and valproate using isobolographic analysis.
Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2006
)
0.33
" However, these interactions were complicated by changes in brain AED concentrations consequent to pharmacokinetic interactions."( Characterization of the anticonvulsant, behavioral and pharmacokinetic interaction profiles of stiripentol in combination with clonazepam, ethosuximide, phenobarbital, and valproate using isobolographic analysis.
Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2006
)
0.33
" However, these conclusions are confounded by the fact that STP is associated with significant pharmacokinetic interactions."( Characterization of the anticonvulsant, behavioral and pharmacokinetic interaction profiles of stiripentol in combination with clonazepam, ethosuximide, phenobarbital, and valproate using isobolographic analysis.
Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2006
)
0.33
" Median area under the curve (AUC), terminal elimination half-life (t1/2,z) and maximal concentration (Cmax) were calculated for between-dose comparison."( Reassessment of stiripentol pharmacokinetics in healthy adult volunteers.
Chiron, C; Dulac, O; Jullien, V; Le Guern, ME; Peigné, S; Pons, G; Rey, E, 2014
)
0.4
"To develop a physiologically based pharmacokinetic model in adults and children for clobazam, its active metabolite norclobazam and stiripentol and to account for significant clinical interaction that has been reported when clobazam and stiripentol are co-administered."( A physiologically based pharmacokinetic model for clobazam and stiripentol in adults and children.
Aarons, L; Ogungbenro, K, 2015
)
0.42
"Thirty-five children with epilepsy were included in a prospective population pharmacokinetic study (using NONMEM(®) software)."( Pharmacokinetics of clobazam and N-desmethylclobazam in children with dravet syndrome receiving concomitant stiripentol and valproic Acid.
Chhun, S; Chiron, C; Dulac, O; Jullien, V; Pons, G; Rey, E; Tod, M, 2015
)
0.42
"This is the first simultaneous pharmacokinetic model for clobazam and N-CLB in epileptic children."( Pharmacokinetics of clobazam and N-desmethylclobazam in children with dravet syndrome receiving concomitant stiripentol and valproic Acid.
Chhun, S; Chiron, C; Dulac, O; Jullien, V; Pons, G; Rey, E; Tod, M, 2015
)
0.42
" Both the safety and the pharmacokinetic populations of the stiripentol arm comprised 14 patients (2 placebo; 12 cannabidiol)."( A Phase II Randomized Trial to Explore the Potential for Pharmacokinetic Drug-Drug Interactions with Stiripentol or Valproate when Combined with Cannabidiol in Patients with Epilepsy.
Arenas Cabrera, CM; Ben-Menachem, E; Critchley, D; Crockett, J; Gunning, B; Morrison, G; Tayo, B; Toledo, M; VanLandingham, K; Wray, L, 2020
)
0.56
" The aim was to use long-term TDM to investigate pharmacokinetic variability of ASMs in these patients."( Pharmacokinetic Variability During Long-Term Therapeutic Drug Monitoring of Valproate, Clobazam, and Levetiracetam in Patients With Dravet Syndrome.
Bjørnvold, M; Burns, ML; Heger, K; Johannessen Landmark, C; Johannessen, SI; Lund, C; Sætre, E, 2020
)
0.56
" Pharmacokinetic variability of the total number of measurements of valproate (n = 417), clobazam and N-desmethylclobazam (n = 328), and levetiracetam (n = 238) was determined."( Pharmacokinetic Variability During Long-Term Therapeutic Drug Monitoring of Valproate, Clobazam, and Levetiracetam in Patients With Dravet Syndrome.
Bjørnvold, M; Burns, ML; Heger, K; Johannessen Landmark, C; Johannessen, SI; Lund, C; Sætre, E, 2020
)
0.56
" Pharmacokinetic variability and interactions can thus be identified and adjusted to facilitate decision making to achieve the optimal treatment outcome."( Pharmacokinetic Variability During Long-Term Therapeutic Drug Monitoring of Valproate, Clobazam, and Levetiracetam in Patients With Dravet Syndrome.
Bjørnvold, M; Burns, ML; Heger, K; Johannessen Landmark, C; Johannessen, SI; Lund, C; Sætre, E, 2020
)
0.56

Compound-Compound Interactions

Cannabidiol was investigated in an experimental model of stroke. Study looked at impact of cannabidio on steady-state pharmacokinetics of clobazam, stiripentol, and valproate.

ExcerptReferenceRelevance
"The anticonvulsant and acute adverse (neurotoxic) effects of STP in combination with the various conventional antiepileptic drugs (AEDs), at fixed ratios of 1:3, 1:1, and 3:1, were evaluated in the PTZ and chimney tests in mice using the isobolographic analysis."( Characterization of the anticonvulsant, behavioral and pharmacokinetic interaction profiles of stiripentol in combination with clonazepam, ethosuximide, phenobarbital, and valproate using isobolographic analysis.
Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2006
)
0.33
"Phase I, open-label, randomized, single-dose, 3-period crossover study assessing pharmacokinetics (PK) and safety of ZX008, a liquid oral formulation of fenfluramine (FFA) under development for adjunctive treatment of Dravet syndrome and Lennox-Gastaut syndrome, administered with and without a combined antiepileptic drug (AED) regimen of stiripentol (STP), valproate (VPA), and clobazam (CLB) (STP regimen)."( A phase I, randomized, open-label, single-dose, 3-period crossover study to evaluate the drug-drug interaction between ZX008 (fenfluramine HCl oral solution) and a regimen of stiripentol, clobazam, and valproate in healthy subjects
.
Boyd, B; Farfel, GM; Galer, BS; Gammaitoni, A; Smith, S, 2019
)
0.51
" This open-label, fixed-sequence, drug-drug interaction, healthy volunteer trial investigated the impact of cannabidiol on steady-state pharmacokinetics of clobazam (and N-desmethylclobazam), stiripentol, and valproate; the reciprocal effect of clobazam, stiripentol, and valproate on cannabidiol and its major metabolites (7-hydroxy-cannabidiol [7-OH-CBD] and 7-carboxy-cannabidiol [7-COOH-CBD]); and cannabidiol safety and tolerability when coadministered with each antiepileptic drug."( A Phase 1, Open-Label, Pharmacokinetic Trial to Investigate Possible Drug-Drug Interactions Between Clobazam, Stiripentol, or Valproate and Cannabidiol in Healthy Subjects.
Blakey, G; Crockett, J; Morrison, G; Sommerville, K, 2019
)
0.51
" It is important to consider the possibility of drug-drug interactions (DDIs)."( Clinical implications of trials investigating drug-drug interactions between cannabidiol and enzyme inducers or inhibitors or common antiseizure drugs.
Critchley, D; Gidal, B; Morrison, G; Patsalos, PN; Szaflarski, JP; VanLandingham, K, 2020
)
0.56
" Hence, their metabolic stability and potential involvement in relevant drug-drug interactions (DDI) are of great clinical interest, being HepaRG cells herein used as an in vitro human model."( Study of the metabolic stability profiles of perampanel, rufinamide and stiripentol and prediction of drug interactions using HepaRG cells as an in vitro human model.
Alves, G; Falcão, A; Fortuna, A; Meirinho, S; Rodrigues, M, 2022
)
0.72
" In the current study, we have investigated the neuroprotective effect of stiripentol (STP) and trans integrated stress response inhibitor (ISRIB) alone and in combination with rat bone marrow derived mesenchymal stem cells (BM-MSCs) secretome in an experimental model of stroke."( Rat BM-MSCs secretome alone and in combination with stiripentol and ISRIB, ameliorated microglial activation and apoptosis in experimental stroke.
Attri, SV; Bhattacharyya, S; Das Radotra, B; Dhir, N; Jain, A; Mahendru, D; Malik, D; Medhi, B; Patial, A; Prakash, A; Sharma, AR; Sharma, S, 2023
)
0.91
"STP and trans ISRIB, alone and in combination with rat BM-MSCs secretome, significantly improved neurological, motor function and memory deficits along with significant reduction in pyknotic neurons in the brain of post MCAO rats."( Rat BM-MSCs secretome alone and in combination with stiripentol and ISRIB, ameliorated microglial activation and apoptosis in experimental stroke.
Attri, SV; Bhattacharyya, S; Das Radotra, B; Dhir, N; Jain, A; Mahendru, D; Malik, D; Medhi, B; Patial, A; Prakash, A; Sharma, AR; Sharma, S, 2023
)
0.91
"STP and trans ISRIB, alone and in combination with rat BM-MSCs secretome, might be considered as potential neuroprotective agents in the acute ischemic stroke (AIS) management."( Rat BM-MSCs secretome alone and in combination with stiripentol and ISRIB, ameliorated microglial activation and apoptosis in experimental stroke.
Attri, SV; Bhattacharyya, S; Das Radotra, B; Dhir, N; Jain, A; Mahendru, D; Malik, D; Medhi, B; Patial, A; Prakash, A; Sharma, AR; Sharma, S, 2023
)
0.91

Bioavailability

ExcerptReferenceRelevance
" This paper aimed to explore the performance of polymeric mixed micelles on solubilization, stabilization and bioavailability enhancement with stiripentol as model drug."( Exploring the potential of self-assembled mixed micelles in enhancing the stability and oral bioavailability of an acid-labile drug.
Wang, H; Wu, B; Zhang, T; Zhang, X; Zhou, X, 2014
)
0.4
" A bioavailability study was performed in rats after oral administration of either STP-NEs, or commercial formulation (Diacomit)."( Nanoemulsions as novel oral carriers of stiripentol: insights into the protective effect and absorption enhancement.
Li, X; Liu, S; Lu, R; Wang, Q, 2015
)
0.42
"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
" Moreover, compared with STP suspensions, the bioavailability of STP-SD-ETs was as high as 138."( Stiripentol Enteric Solid Dispersion-Loaded Effervescent Tablets: Enhanced Dissolution, Stability, and Absorption.
He, W; Jiang, Q; Jiang, Y; Li, J; Wang, Y; Xiao, Z; Xu, S, 2022
)
0.72

Dosage Studied

Stiripentol was very highly bound to plasma proteins in plasma from dosed subjects as well as spiked human plasma (free fraction of 1 per cent) This suggests in vivo activation to a metabolic intermediate forming a complex with cerebral cytochrome P-450.

ExcerptRelevanceReference
"The inhibitory effect of stiripentol (STP) on disposition of carbamazepine (CBZ) and carbamazepine-10,11-epoxide (CBZE) was quantitated to establish CBZ dosage reduction guidelines for future clinical add-on efficacy trials of STP."( Carbamazepine dose requirements during stiripentol therapy: influence of cytochrome P-450 inhibition by stiripentol.
Eddy, AC; Kerr, BM; Levy, RH; Martinez-Lage, JM; Tor, J; Viteri, C,
)
0.13
" Blood and urine samples in the studies were collected during a dosing interval at steady state."( Effects of polytherapy with phenytoin, carbamazepine, and stiripentol on formation of 4-ene-valproate, a hepatotoxic metabolite of valproic acid.
Acheampong, A; Anderson, GD; Baillie, TA; Friel, PN; Guyot, M; Levy, RH; Loiseau, P; Rettenmeier, AW; Tor, J; Wilensky, AJ, 1990
)
0.28
" Dose-response studies were performed after acute intraperitoneal injection and subacute oral drug treatment."( Efficacy of stiripentol in the intravenous pentylenetetrazol infusion seizure model in the rat.
Levy, RH; Moor, MJ; Savitch, JL; Shen, DD,
)
0.13
" From a quantitative standpoint, the most important pathway of biotransformation of I following both acute and chronic dosing involved opening of the methylenedioxy ring to generate catechol derivatives."( The metabolic fate of stiripentol in man.
Astoin, J; Baillie, TA; Lepage, F; Levy, RH; Moreland, TA; Tombret, F,
)
0.13
" This suggests in vivo activation to a metabolic intermediate forming a complex with cerebral cytochrome P-450, which 2 hr after dosing is fully insensitive to stiripentol added to incubates."( Ex vivo inhibition of rat brain cytochrome P-450 activity by stiripentol.
Jenner, P; Mesnil, M; Testa, B, 1988
)
0.27
" Stiripentol was very highly bound to plasma proteins in plasma from dosed subjects as well as spiked human plasma (free fraction of 1 per cent)."( Pharmacokinetics of stiripentol in normal man: evidence of nonlinearity.
Blehaut, HM; Levy, RH; Lin, HS; Tor, JA,
)
0.13
" Stiripentol was administered orally three times a day in dosage increments of 600, 1,200, and 1,800 mg/day for consecutive periods of 3, 4, and 7 days, respectively."( Michaelis-Menten kinetics of stiripentol in normal humans.
Blehaut, HM; Guyot, M; Levy, RH; Loiseau, P; Moreland, TA; Tor, J, 1984
)
0.27
" The frequency of congenital defects in PHT-treated animals was dosage dependent, ranging from 7 to 55%."( Protection from phenytoin-induced congenital malformations by coadministration of the antiepileptic drug stiripentol in a mouse model.
Finnell, RH; Kerr, BM; Levy, RH; Steward, RL; van Waes, M,
)
0.13
"05), compared with mice dosed with CBZ alone (1,000 mg/kg/day)."( Effect of treatment with phenobarbital and stiripentol on carbamazepine-induced teratogenicity and reactive metabolite formation.
Amore, BM; Bajpai, M; Bennett, GD; Finnell, RH; Levy, RH; Slattery, JT, 1995
)
0.29
"l-1 and the dosage of CBZ should simultaneously be decreased in steps by more than 50% to minimize the change in CBZ plasma concentration."( Effect of stiripentol on carbamazepine plasma concentration and metabolism in epileptic children.
Chiron, C; d'Athis, P; Dulac, O; Olive, G; Pous, G; Renard, F; Rey, E; Tran, A; Vauzelle-Kervroedan, F, 1996
)
0.29
" This study sought to determine the lowest dosage of stiripentol (STP) protective against phenytoin-induced teratogenesis in a mouse model, and to determine mechanistically if inhibition of oxidative metabolism by STP in vitro decreased production of reactive phenytoin (PHT) metabolites."( Effect of stiripentol dose on phenytoin-induced teratogenesis in a mouse model.
Bajpai, M; Bennett, GD; Finnell, RH; Levy, RH; Mather, GG; Wlodarczyk, B,
)
0.13
" They could be so severe in patients over 12 years of age that the stiripentol dosage could not be increased to 50 mg kg-1 j-1."( [Long-term efficacy and tolerance of stiripentaol in severe myoclonic epilepsy of infancy (Dravet's syndrome)].
Chiron, C; Dellatolas, G; Dulac, O; Pons, G; Rey, E; Thanh, TN; Vincent, J, 2002
)
0.31
"The aim of this study was to characterize the anticonvulsant effects of stiripentol (STP) in combination with clobazam [CLB], and valproate [VPA]) in the mouse maximal electroshock (MES)-induced seizure model using the type I isobolographic analysis for parallel and non-parallel dose-response relationship curves (DRRCs)."( Interactions of stiripentol with clobazam and valproate in the mouse maximal electroshock-induced seizure model.
Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N; Trojnar, MK, 2010
)
0.36
" They were also offered an increased dosage of stiripentol if treatment with carnitine improved the encephalopathy."( Starting stiripentol in adults with Dravet syndrome? Watch for ammonia and carnitine.
Andrade, DM; Marques, P; Sadoway, T; Selvarajah, A; Tabarestani, S; Zulfiqar Ali, Q, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LuciferasePhotinus pyralis (common eastern firefly)Potency22.43010.007215.758889.3584AID1224835; AID624030
glp-1 receptor, partialHomo sapiens (human)Potency35.48130.01846.806014.1254AID624172
RAR-related orphan receptor gammaMus musculus (house mouse)Potency22.68740.006038.004119,952.5996AID1159521; AID1159523
AR proteinHomo sapiens (human)Potency32.25430.000221.22318,912.5098AID1259243; AID1259247
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency29.11420.001022.650876.6163AID1224838; AID1224839; AID1224893
progesterone receptorHomo sapiens (human)Potency23.71010.000417.946075.1148AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency6.91780.01237.983543.2770AID1645841
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency29.84930.003041.611522,387.1992AID1159552; AID1159553; AID1159555
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency25.67700.001530.607315,848.9004AID1224841; AID1259401
pregnane X nuclear receptorHomo sapiens (human)Potency29.84930.005428.02631,258.9301AID1346982
GVesicular stomatitis virusPotency3.09010.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency10.96400.00108.379861.1304AID1645840
aryl hydrocarbon receptorHomo sapiens (human)Potency12.60820.000723.06741,258.9301AID743085; AID743122
Interferon betaHomo sapiens (human)Potency3.09010.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency3.09010.01238.964839.8107AID1645842
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency3.09010.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency3.09010.01238.964839.8107AID1645842
[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)
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)EC50 (µMol)46.00000.00112.000910.0000AID1517295
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)EC50 (µMol)46.00000.00141.957810.0000AID1517295
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)EC50 (µMol)46.00000.00141.776810.0000AID1517295
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (58)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
post-embryonic developmentGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
adult behaviorGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inner ear receptor cell developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
innervationGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cochlea developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (25)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
GABA receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
axonGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
extracellular exosomeGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (63)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
AID696708Neurotoxicity in Swiss albino mouse assessed as effect on hindlimb grip strength at 747 umol/kg, sc administered measured every 15 mins for 2 hrs2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design and synthesis of novel stiripentol analogues as potential anticonvulsants.
AID696703Anticonvulsant activity in ip dosed Swiss albino mouse assessed as maximal electroshock-induced seizures administered 30 mins before electroshock challenge2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design and synthesis of novel stiripentol analogues as potential anticonvulsants.
AID696696Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 640 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design and synthesis of novel stiripentol analogues as potential anticonvulsants.
AID696698Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 747 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design and synthesis of novel stiripentol analogues as potential anticonvulsants.
AID1517295Agonist activity at GABA alpha1beta2gamma2 receptor in human HEK293T at -50 mV holding potential by whole cell voltage clamp assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID1868303Cytotoxicity against hyperoxaluric-primary hepatocyte isolated from Hoga1-knockdown PH3 C57BL/6 mouse assessed as cell death at 10 uM by MTS assay2022European journal of medicinal chemistry, Jul-05, Volume: 237New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production.
AID696709Neurotoxicity in Swiss albino mouse assessed as climbing response to inverted mesh at at 747 umol/kg, sc administered measured every 15 mins for 2 hrs by wire mesh grasping test2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design and synthesis of novel stiripentol analogues as potential anticonvulsants.
AID1517332Inhibition of human LDH5 at 2 mM using sodium pyruvate as substrate by UV-VIS spectrophotometry method relative to control2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID696692Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 427 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design and synthesis of novel stiripentol analogues as potential anticonvulsants.
AID1323834Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Identification of small molecules that bind to the mitochondrial protein mitoNEET.
AID1517254Anticonvulsant activity in Kunming mouse assessed as MES-induced hind limb extension at 100 mg/kg, ip administered 0. 5 to 2 hrs before MES stimulation2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID1868301Inhibition of GO/LDHA in hyperoxaluric-primary hepatocyte isolated from Hoga1-knockdown PH3 C57BL/6 mouse assessed as relative oxalate output at 10 uM measured at 24 hrs in the presence of hydroxyproline relative to control2022European journal of medicinal chemistry, Jul-05, Volume: 237New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production.
AID696691Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 384 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design and synthesis of novel stiripentol analogues as potential anticonvulsants.
AID1868305Cytotoxicity against hyperoxaluric-primary hepatocyte isolated from Agxt1-knockdown PH1 C57BL/6 mouse assessed as cell death at 10 uM by MTS assay2022European journal of medicinal chemistry, Jul-05, Volume: 237New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production.
AID1517288Inhibition of human LDH1 at 2 mM using sodium pyruvate as substrate by UV-VIS spectrophotometry method relative to control2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID696702Anticonvulsant activity in ip dosed Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures administered 30 mins before pentylenetetrazole challenge measured after 30 mins2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design and synthesis of novel stiripentol analogues as potential anticonvulsants.
AID1517286Inhibition of human LDH1 at 0.5 mM using sodium pyruvate as substrate by UV-VIS spectrophotometry method relative to control2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID1868302Inhibition of GO/LDHA in hyperoxaluric-primary hepatocyte isolated from Hoga1-knockdown PH3 C57BL/6 mouse assessed as relative oxalate output at 10 uM measured at 48 hrs in the presence of hydroxyproline relative to control2022European journal of medicinal chemistry, Jul-05, Volume: 237New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production.
AID1517287Inhibition of human LDH5 at 0.5 mM using sodium pyruvate as substrate by UV-VIS spectrophotometry method relative to control2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID1868300Inhibition of GO/LDHA in hyperoxaluric-primary hepatocyte isolated from Grhpr-knockdown PH2 C57BL/6 mouse assessed as relative oxalate output at 10 uM measured at 48 hrs in the presence of glycolate relative to control2022European journal of medicinal chemistry, Jul-05, Volume: 237New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production.
AID1323835Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Identification of small molecules that bind to the mitochondrial protein mitoNEET.
AID696693Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 491 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design and synthesis of novel stiripentol analogues as potential anticonvulsants.
AID696694Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 534 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design and synthesis of novel stiripentol analogues as potential anticonvulsants.
AID1868304Cytotoxicity against hyperoxaluric-primary hepatocyte isolated from Grhpr-knockdown PH2 C57BL/6 mouse assessed as cell death at 10 uM by MTS assay2022European journal of medicinal chemistry, Jul-05, Volume: 237New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production.
AID696695Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 576 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design and synthesis of novel stiripentol analogues as potential anticonvulsants.
AID1517296Agonist activity at GABA alpha1beta2gamma2 receptor in human HEK293T at 3.3 to 300 uM at -50 mV holding potential by whole cell voltage clamp assay relative to control2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID1868299Inhibition of GO/LDHA in hyperoxaluric-primary hepatocyte isolated from Grhpr-knockdown PH2 C57BL/6 mouse assessed as relative oxalate output at 10 uM measured at 24 hrs in the presence of glycolate relative to control2022European journal of medicinal chemistry, Jul-05, Volume: 237New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production.
AID696697Anticonvulsant activity in Swiss albino mouse assessed as maximal electroshock-induced seizures at 640 umol/kg, ip administered 30 mins before electroshock challenge2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Design and synthesis of novel stiripentol analogues as potential anticonvulsants.
AID1517256Neurotoxicity against Kunming mouse assessed as time remained in rod at 100 mg/kg, ip administered 0.5 to 2 hrs by rotarod test2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (171)

TimeframeStudies, This Drug (%)All Drugs %
pre-199011 (6.43)18.7374
1990's17 (9.94)18.2507
2000's22 (12.87)29.6817
2010's78 (45.61)24.3611
2020's43 (25.15)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials18 (9.63%)5.53%
Reviews45 (24.06%)6.00%
Case Studies10 (5.35%)4.05%
Observational3 (1.60%)0.25%
Other111 (59.36%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (10)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Pharmacokinetic Study of Stiripentol and Its Metabolites After Multiple Dose Oral Administration in Healthy Male Volunteers [NCT03866928]Phase 114 participants (Actual)Interventional2019-02-12Completed
Expanded Access Use of Stiripentol in Participants With Dravet Syndrome or Epileptic Encephalopathies Associated With Sodium Channel Mutations [NCT02239276]0 participants Expanded AccessNo longer available
Evaluation of the Efficacy of Stiripentol (Diacomit) as Monotherapy for the Treatment of Primary Hyperoxaluria [NCT03819647]Phase 215 participants (Actual)Interventional2019-05-21Completed
A Randomised Controlled Trial of the Ketogenic Diet in the Treatment of Epilepsy in Children Under the Age of Two Years [NCT02205931]Phase 4160 participants (Anticipated)Interventional2015-01-31Recruiting
Study of the Interest of the Combination of Stiripentol (Diacomit®) and Carbamazepine in the Treatment of Patients With Pharmacoresistant Focal Epilepsies [NCT05419180]Phase 4100 participants (Anticipated)Interventional2022-10-13Recruiting
Treatment Plan to Provide Expanded Access to Stiripentol for Patients With Dravet Syndrome [NCT01983722]0 participants Expanded AccessApproved for marketing
Compassionate Use of Stiripentol in Intractable Epilepsy Due to Dravet Syndrome [NCT01533506]0 participants Expanded Access2012-02-29No longer available
Open Label, Phase I Study to Assess and Compare the Pharmacokinetic Parameters After Multiple Oral Administration of Stiripentol 1000 mg in Renal Impaired Patients and Matching Controls With Normal Renal Function [NCT05735951]Phase 148 participants (Anticipated)Interventional2023-03-25Not yet recruiting
Population Pharmacokinetics of Antiepileptic in Pediatrics [NCT03196466]1,000 participants (Anticipated)Observational2017-06-19Recruiting
Compassionate Use of Stiripentol in Dravet Syndrome [NCT01835314]0 participants Expanded AccessNo longer available
[information is prepared from clinicaltrials.gov, extracted Sep-2024]