Page last updated: 2024-11-04

epinastine

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

Description

Epinastine is a second-generation antihistamine that is a selective antagonist of the H1 receptor. It was initially developed for the treatment of allergic rhinitis, but it has also been studied for its potential use in other conditions such as allergic conjunctivitis, urticaria, and pruritus. The synthesis of epinastine involves a multi-step process that starts with the reaction of 4-chlorobenzaldehyde with ethyl acetoacetate. The resulting compound is then reacted with a series of reagents to yield epinastine. Epinastine has been shown to be effective in reducing nasal symptoms associated with allergic rhinitis, including sneezing, rhinorrhea, and nasal congestion. It has also been found to be effective in reducing conjunctival symptoms associated with allergic conjunctivitis, such as itching, redness, and tearing. Epinastine is generally well tolerated and has a low incidence of side effects. However, it may cause drowsiness in some individuals, so it is important to use caution when driving or operating machinery. Epinastine is a commonly studied compound due to its efficacy and safety in treating allergic rhinitis and other allergic conditions. Researchers continue to investigate its potential use in a variety of other medical conditions. '

epinastine: RN given refers parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

epinastine : A benzazepine that is 6,11-dihydro-5H-dibenzo[b,e]azepine in which the azepine ring is fused to the e side of 4,5-dihydro-1H-imidazol-2-amine. [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]

dexamethasone acetate: RN given refers to (11beta,16alpha)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3241
CHEMBL ID1106
CHEBI ID51032
SCHEMBL ID18794
MeSH IDM0150487
PubMed CID236702
CHEMBL ID1530428
CHEBI ID4463
SCHEMBL ID136861
MeSH IDM0150487

Synonyms (189)

Synonym
CHEMBL1106 ,
wal-801
purivist
epinastina
80012-43-7
epinastinum
CHEBI:51032 ,
9,13b-dihydro-1h-dibenzo[c,f]imidazo[1,5-a]azepin-3-amine
3-amino-9,13b-dihydro-1h-dibenz(c,f)imidazo(1,5-a)azepine
DB00751
(+/-)-epinastine
epinastine
NCGC00165791-01
3-amino-9,13b-dihydro-1h-benz(c,f)imidazo(1,5a)azepine
(+-)-epinastine
1h-dibenz(c,f)imidazo(1,5-a)azepin-3-amino, 9,13b-dihydro-
epinastinum [latin]
epinastina [spanish]
epinastine [inn]
wal 801
NCGC00165791-03
bdbm50131441
L000716
D07900
epinastine (inn)
purivist (tn)
epinastine [inn:ban]
9,13b-dihydro-1h-dibenz(c,f)imidazo(1,5a)azepin-3-amin
unii-q13wx941ef
ec 616-785-3
q13wx941ef ,
FT-0630877
AKOS015895203
gtpl7176
epinastine [who-dd]
1h-dibenz(c,f)imidazo(1,5-a)azepin-3-amine, 9,13b-dihydro-
epinastine [vandf]
134507-59-8
epinastine [mi]
9,13b-dihydro-1h-dibenz(c,f)imidazo(1,5-a)azepin-3-amine
HY-B0640
WHWZLSFABNNENI-UHFFFAOYSA-N
SCHEMBL18794
DTXSID2048371 ,
3-amino-9,13b-dihydro-1h-dibenz[c,f]imidazo[1,5-a]azepine
AC-24691
MRF-0000757
Q632405
mfcd00865648
AS-12835
BCP28446
SDCCGSBI-0633722.P001
NCGC00165791-11
AMY33372
2,4-diazatetracyclo[12.4.0.02,6.07,12]octadeca-1(18),3,7,9,11,14,16-heptaen-3-amine
A917968
9,13b-dihydro-1h-dibenz[c,f]imidazo[1,5-a]azepin-3-amine
EX-A4762
1h-dibenz[c,f]imidazo[1,5-a]azepin-3-amine, 9,13b-dihydro-
2,4-diazatetracyclo[12.4.0.0^{2,6}.0^{7,12}]octadeca-1(18),3,7,9,11,14,16-heptaen-3-amine
EN300-18166758
9,13b-dihydro-1h-dibenzo(c,f)imidazo(1,5-a)azepin-3-amine
dtxcid8028345
epinastin
epinastinum (latin)
s01gx10
r06ax24
unii-k7v8p532wp
k7v8p532wp ,
MLS001148106 ,
brd-5719
brd5719
BRD-K47635719-001-03-9
16.alpha.-methyl-9.alpha.-fluoroprednisolone 21-acetate
dexamethasone acetate
pregna-1,20-dione, 21-(acetyloxy)-9-fluoro-11,17-dihydroxy-16-methyl-, (11.beta.,16.alpha.)-
nsc39471
decadronal
pregna-1,20-dione, 9-fluoro-11.beta.,17,21-trihydroxy-16.alpha.-methyl-, acetate
nsc-39471
pregna-1,20-dione, 9-fluoro-11.beta.,17,21-trihydroxy-16.alpha.-methyl-, 21-acetate
dexamethasone 21-acetate
dex-cortidelt acetate
9.alpha.-fluoro-16.alpha.-methylprednisolone acetate
fortecortin (crystal suspension)
panasone
smr000058327
MLS000028544 ,
pregna-1,4-diene-3,20-dione, 21-(acetyloxy)-9-fluoro-11,17-dihydroxy-16-methyl-, (11.beta.,16.alpha.)-
dexamethasone-21-acetate
PRESTWICK_157
NCGC00016566-01
cas-1177-87-3
dexamethasone acetate, (6alpha,11beta)-isomer
BSPBIO_000180
BPBIO1_000198
9-fluoro-11-beta,17,21-trihydroxy-16-alpha-methylpregna-1,4-diene-3,20-dione acetate
dectan
fortecortin (van)
16alpha-methyl-9alpha-fluoroprednisolone 21-acetate
9alpha-fluoro-16alpha-methylprednisolone acetate
einecs 214-646-8
pregna-1,4-diene-3,20-dione, 9-fluoro-11beta,17,21-trihydroxy-16alpha-methyl-, 21-acetate
nsc 39471
pregna-1,4-diene-3,20-dione, 21-(acetyloxy)-9-fluoro-11,17-dihydroxy-16-methyl-, (11beta,16alpha)-
pregna-1,4-diene-3,20-dione, 9-fluoro-11-beta,17,21-trihydroxy-16-alpha-methyl-, acetate
1177-87-3
C08174
dexamethasone acetate anhydrous
dexamethasone 21-acetate, >=99%
decadron-la
PRESTWICK1_000130
SPBIO_002119
PRESTWICK0_000130
PRESTWICK3_000130
PRESTWICK2_000130
NCGC00022662-03
decaject-l.a. (tn)
D07796
[2-[(8s,9r,10s,11s,13s,14s,16r,17r)-9-fluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl]-2-oxoethyl] acetate
HMS1568I22
HMS2095I22
2-((2s,10s,11s,15s,17s,1r,13r,14r)-1-fluoro-14,17-dihydroxy-2,13,15-trimethyl- 5-oxotetracyclo[8.7.0.0<2,7>.0<11,15>]heptadeca-3,6-dien-14-yl)-2-oxoethyl ace tate
tox21_112928
CHEMBL1530428 ,
dexamethasoni acetas monohydrate
dexamethasoni acetas
chebi:4463 ,
dtxcid402901
tox21_110499
dtxsid8022901 ,
AKOS015951406
HMS2233A20
dexamethasone acetate [ep monograph]
dexamethasone acetate [who-ip]
betamethasone acetate impurity b [ep impurity]
9-fluoro-11.beta.,17,21-trihydroxy-16.alpha.-methylpregna-1,4-diene-3,20-dione 21-acetate
dexamethasone acetate [who-dd]
dexamethasone 21-acetate [mi]
dexamethasoni acetas [who-ip latin]
dexamethasone acetate [usp monograph]
dexamethasone acetate [usp-rs]
dexamethasone acetate, anhydrous
dexamethasone impurity g [ep impurity]
S3124
CCG-220130
HY-14648A
CS-1941
SCHEMBL136861
NCGC00022662-05
tox21_112928_1
dexamethason-21-acetate
dalalone la
pregna-1,4-diene-3,20-dione, 9-fluoro-11.beta.,17,21-trihydroxy-16.alpha.-methyl-, 21-acetate
AKUJBENLRBOFTD-RPRRAYFGSA-N
prednisolone, 9.alpha.-fluoro-16.alpha.-methyl-, acetate
dalalone dp
decadron-l.a.
9-fluoro-11.beta.,17-dihydroxy-16.alpha.-methyl-3,20-dioxopregna-1,4-dien-21-yl acetate #
pregna-1,4-diene-3,20-dione, 9-fluoro-11.beta.,17,21-trihydroxy-16.alpha.-methyl-, acetate
W-108559
9alpha-fluoro-16alpha-methylprednisolone-21-acetate
OPERA_ID_1620
mfcd00027407
dexamethasone (acetate)
dexamethason acetate
sr-01000000099
SR-01000000099-2
2-((8s,9r,10s,11s,13s,14s,16r,17r)-9-fluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3h-cyclopenta[a]phenanthren-17-yl)-2-oxoethyl acetate
dexamethasone acetate, united states pharmacopeia (usp) reference standard
dexamethasone 21-acetate, vetranal(tm), analytical standard
dexamethasone acetate, european pharmacopoeia (ep) reference standard
bdbm50103620
dexamethasone acetate, pharmaceutical secondary standard; certified reference material
betamethasone acetate imp. b (ep); dexamethasone imp. g (ep); betamethasone acetate impurity b; dexamethasone impurity g; dexamethasone isonicotinate impurity b
HMS3712I22
NCGC00022662-06
pregna-1,4-diene-3,20-dione, 21-(acetyloxy)-9-fluoro-11,17-dihydroxy-16-methyl-, (11b,16a)-
DB14649
21-o-acetyl dexamethasone
Q27106392
AS-13327
BCP28591
BRD-K47635719-001-21-1
dexamethasone-acetate
[2-[(8r,9s,10s,11s,13s,14s,16r,17r)-9-fluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl]-2-oxoethyl] acetate
2-[(1r,2r,3as,3bs,9as,9br,10s,11as)-9b-fluoro-1,10-dihydroxy-2,9a,11a-trimethyl-7-oxo-1h,2h,3h,3ah,3bh,4h,5h,7h,9ah,9bh,10h,11h,11ah-cyclopenta[a]phenanthren-1-yl]-2-oxoethyl acetate
EN300-19631802
Z2417819627

Research Excerpts

Overview

Epinastine hydrochloride is a selective histamine H1 receptor antagonist that also inhibits IgE receptor-mediated histamine release from mast cells. Epinastine is an antihistamine drug with binding affinities at 5-hydroxytryptamine (5-HT) receptors.

ExcerptReferenceRelevance
"Epinastine hydrochloride is a selective histamine H1 receptor antagonist that also inhibits IgE receptor-mediated histamine release from mast cells."( Efficacy of epinastine hydrochloride ophthalmic solution in allergic conjunctivitis by conjunctival cedar pollen allergen challenge.
Fujishima, H; Ohashi, Y; Takamura, E, 2014
)
2.22
"Epinastine is a topical ophthalmic antihistamine and a mast cell stabilizer indicated for treatment of symptoms associated with allergic conjunctivitis."( Epinastine: topical ophthalmic second generation antihistamine without significant systemic side effects.
Abhishek, K; Mah, F; Pradhan, S, 2009
)
3.24
"Epinastine hydrochloride is an antihistamine with mast cell-stabilizing and anti-inflammatory activity."( Efficacy and tolerability of ophthalmic epinastine: a randomized, double-masked, parallel-group, active- and vehicle-controlled environmental trial in patients with seasonal allergic conjunctivitis.
Abelson, MB; Bradford, R; Lue, J; Schiffman, RM; Whitcup, SM, 2004
)
2.03
"Epinastine hydrochloride is a nonsedating antihistamine with a high affinity for histamine H(1) receptors, together with mast cell-stabilizing and anti-inflammatory activities."( Efficacy and tolerability of ophthalmic epinastine assessed using the conjunctival antigen challenge model in patients with a history of allergic conjunctivitis.
Abelson, MB; Bradford, RR; Crampton, HJ; Gomes, P; Schiffman, RM; Whitcup, SM, 2004
)
2.03
"Epinastine (WAL 801CL) is an antihistaminic drug with binding affinity at certain other receptors, including alpha-adrenergic receptors and various serotonin (5-HT) receptor subtypes."( Epinastine (WAL 801CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor.
Demedts, MG; Dupont, LJ; Meade, CJ; Verleden, GM, 1996
)
2.46
"Epinastine is an antihistamine and antiallergic drug. "( The mechanism by which epinastine stops an adenosine analog from contracting BDE rat airways.
Meade, CJ, 1998
)
2.05
"Epinastine is a non-sedative second-generation antiallergic drug, like terfenadine. "( Metabolism of epinastine, a histamine H1 receptor antagonist, in human liver microsomes in comparison with that of terfenadine.
Funae, Y; Hiroi, T; Igarashi, T; Kishimoto, W; Sakai, K, 1997
)
2.1
"Epinastine is an antihistamine drug with binding affinities at 5-hydroxytryptamine (5-HT) receptors. "( Epinastine (WAL 801CL) inhibits the electrical field stimulation-induced cholinergic contraction in guinea pig and human airways in vitro.
DeLeyn, P; Demedts, MG; Deneffe, G; Dupont, LJ; Meade, CJ; Pype, JL; Verleden, GM, 1999
)
3.19

Effects

Equinastine has no inhibitory effect on histamine release induced by Ca2+ or IP3 from permeabilized mast cells. Epinastine, however, has not been reported to have the adverse effect.

ExcerptReferenceRelevance
"Epinastine has other modes of action apart from its antihistamine activity that may be relevant to its use in asthma."( The mechanism by which epinastine stops an adenosine analog from contracting BDE rat airways.
Meade, CJ, 1998
)
1.33
"Epinastine, however, has not been reported to have the adverse effect."( Epinastine, a nonsedating histamine H1 receptor antagonist, has a negligible effect on HERG channel.
Chachin, M; Horio, Y; Katayama, Y; Kitagawa, H; Kurachi, Y; Ohmura, T; Uchida, S; Yamada, M, 1999
)
2.47
"Epinastine has no inhibitory effect on histamine release induced by Ca2+ or IP3 from permeabilized mast cells."( Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition.
Akagi, M; Izushi, K; Kamei, C; Kitazumi, K; Masaki, S; Mio, M; Tasaka, K, 1992
)
1.32

Actions

Epinastine may inhibit the NADPH oxidase system through the obstruction of cytosol components. It did not inhibit isolated protein kinase C from rat brain.

ExcerptReferenceRelevance
"Epinastine may inhibit the NADPH oxidase system through the obstruction of NADPH oxidase-associated cytosol components."( Inhibitory effect of epinastine on superoxide generation by rat neutrophils.
Akagi, M; Akagi, R; Fukuishi, N; Hirose, K; Kan, T, 1995
)
1.33
"Epinastine did not inhibit isolated protein kinase C from rat brain."( In vitro investigations with the histamine H1 receptor antagonist, epinastine (WAL 801 CL), on isolated human allergic effector cells.
Amon, U; Buss, G; Gibbs, BF; Nitschke, M, 2000
)
1.26

Treatment

ExcerptReferenceRelevance
"Epinastine-treated patients reported significantly less ocular itching than those receiving vehicle (P=0.045); scores for hyperemia were similar between these 2 groups."( Efficacy and tolerability of ophthalmic epinastine: a randomized, double-masked, parallel-group, active- and vehicle-controlled environmental trial in patients with seasonal allergic conjunctivitis.
Abelson, MB; Bradford, R; Lue, J; Schiffman, RM; Whitcup, SM, 2004
)
1.31

Toxicity

ExcerptReferenceRelevance
"05% ophthalmic solution was found to be a safe and effective medication for the relief of symptoms of allergic conjunctivitis."( Epinastine: topical ophthalmic second generation antihistamine without significant systemic side effects.
Abhishek, K; Mah, F; Pradhan, S, 2009
)
1.8
" Thus, toxic effects can be caused by preservatives or inadequate osmolarity of the vehicles alone."( Experimental and clinical observations of the intraocular toxicity of commercial corticosteroid preparations.
Arena, JE; Chandler, D; Hida, T; Machemer, R, 1986
)
0.27
" The system under study was not toxic to the normal rabbit retina, and no significant increase in intraocular pressure was observed."( Safety and pharmacokinetics of an intravitreal biodegradable implant of dexamethasone acetate in rabbit eyes.
Fialho, SL; Haddad, A; Jorge, R; Maia-Filho, A; Rêgo, MB; Rodrigues, AL; Silva-Cunha, A; Siqueira, RC, 2006
)
0.33

Pharmacokinetics

The purpose of the study was to develop two new methods, HPLC-UV and UPLC-MS/MS, for quantifying epinastine in human plasma and to compare pharmacokinetic (PK) parameters obtained using them.

ExcerptReferenceRelevance
"The effects of epinastine hydrochloride and terfenadine on electrocardiographic (ECG) parameters in rats were investigated from a pharmacokinetic and pharmacodynamic perspective."( A comparative pharmacokinetic-pharmacodynamic study of the electrocardiographic effects of epinastine and terfenadine in rats.
Iga, T; Kotaki, H; Ohtani, H; Sawada, Y, 1997
)
0.87
"5 and 20 mg/kg), the drug was rapidly absorbed, and Cmax was reached 2 h after dosing."( Pharmacokinetics of epinastine and a possible mechanism for double peaks in oral plasma concentration profiles.
Iwaki, M; Kasutani, M; Ogiso, T; Tanaka, H; Tanino, T, 2001
)
0.63
"Our objective was to develop a population pharmacokinetic (PPK) model for epinastine, a histamine H(1) receptor antagonist, in adults and children and to obtain pharmacokinetic information to support dosing recommendations in children."( Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and children.
Igarashi, T; Sarashina, A; Tatami, S; Tsuda, Y; Yamamura, N, 2005
)
0.85
"The purpose of the study was to develop two new methods, HPLC-UV and UPLC-MS/MS, for quantifying epinastine in human plasma and to compare pharmacokinetic (PK) parameters obtained using them."( Pharmacokinetic Comparison of Epinastine Using Developed Human Plasma Assays.
Cho, HY; Jang, JH; Jeong, SH; Lee, YB, 2020
)
1.06
" The objective of the current study was to determine the pharmacokinetic profile of a biodegradable dexamethasone acetate implant inserted into the vitreous of rabbits and to evaluate its potential signs of toxicity to the rabbits' eyes."( Safety and pharmacokinetics of an intravitreal biodegradable implant of dexamethasone acetate in rabbit eyes.
Fialho, SL; Haddad, A; Jorge, R; Maia-Filho, A; Rêgo, MB; Rodrigues, AL; Silva-Cunha, A; Siqueira, RC, 2006
)
0.33

Compound-Compound Interactions

ExcerptReferenceRelevance
" Polymeric nanoparticles combined with ultrasound (US) are widely applied in cancer treatment due to their time applications, low cost, simplicity, and safety."( Prevention of Oxidized Low Density Lipoprotein-Induced Endothelial Cell Injury by DA-PLGA-PEG-cRGD Nanoparticles Combined with Ultrasound.
Du, L; Duan, Y; Huang, H; Huang, L; Li, Z; Sun, Y, 2017
)
0.46
" This method was successfully applied to establish the cell pharmacokinetics methodology and preliminary studied the metabolism of drug-drug interaction of ketoconazole and dexamethasone acetate."( Simultaneous determination the concentration change of ketoconazole and dexamethasone acetate: application to drug-drug interaction in human keratinocyte.
Li, H; Li, L; Ma, P; Qian, K; Wang, C, 2020
)
0.56

Bioavailability

ExcerptReferenceRelevance
" The bioavailability of EPN after oral dosing was 41 and 40%."( Pharmacokinetics of epinastine and a possible mechanism for double peaks in oral plasma concentration profiles.
Iwaki, M; Kasutani, M; Ogiso, T; Tanaka, H; Tanino, T, 2001
)
0.63
" On the other hand, other covariates (formulation on V(1)/F, volume of distribution of the peripheral compartment (V(2)/F), first-order absorption rate constant (Ka) and absorption lag time (ALAG); food status on V(2)/F and Ka; body weight on V(2)/F) were not statistically significant."( Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and children.
Igarashi, T; Sarashina, A; Tatami, S; Tsuda, Y; Yamamura, N, 2005
)
0.61
" Bioavailability of the acetate was greatest; that of the sodium phosphate was the lowest."( Effect of derivatization of the bioavailability of ophthalmic steroids. Development of an in vitro method of evaluation.
Flint, GR; Morton, DJ, 1984
)
0.27
"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
"A drug with poor water-solubility, like Dexamethasone acetate, can present lower bioavailability conventional for pharmaceutical formulations, and the presence of polymorphs in the raw material can lead to drug quality problems."( Dexamethasone Acetate Nanocrystals, Characterization and Dissolution Studies in Presence of Polymorphic Phases.
Chiavacci, LA; da Gama Bastos, FLA; da Silva, BL; Junior, JAO; Lemos Barbosa, TW, 2023
)
0.91

Dosage Studied

Epinastine slightly increased the heart rate, but did not affect any of the other ECG parameters even at a plasma concentration of 400 ng mL-1. The model shows that, if dosage is adjusted based on the body weight, the epinstine exposure in paediatric patients is similar to that in adults.

ExcerptRelevanceReference
" In conclusion, epinastine is one of the most effective peripherally acting H1 antagonist which lacks significant CNS side effects and is suitable as a once daily dosage regimen."( Antihistaminic activity and side effect profile of epinastine and terfenadine in healthy volunteers.
Adamus, WS; Kuthan, H; Schilling, JC, 1990
)
0.88
" Epinastine (100 microM) did not displace the dose-response curve to exogenously applied substance P (0."( Epinastine (WAL 801CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor.
Demedts, MG; Dupont, LJ; Meade, CJ; Verleden, GM, 1996
)
2.65
" Epinastine slightly increased the heart rate, but did not affect any of the other ECG parameters even at a plasma concentration of 400 ng mL-1, which is more than 10 times the maximum concentration attained after an ordinary dosage regimen in man."( A comparative pharmacokinetic-pharmacodynamic study of the electrocardiographic effects of epinastine and terfenadine in rats.
Iga, T; Kotaki, H; Ohtani, H; Sawada, Y, 1997
)
1.43
" The bioavailability of EPN after oral dosing was 41 and 40%."( Pharmacokinetics of epinastine and a possible mechanism for double peaks in oral plasma concentration profiles.
Iwaki, M; Kasutani, M; Ogiso, T; Tanaka, H; Tanino, T, 2001
)
0.63
"Our objective was to develop a population pharmacokinetic (PPK) model for epinastine, a histamine H(1) receptor antagonist, in adults and children and to obtain pharmacokinetic information to support dosing recommendations in children."( Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and children.
Igarashi, T; Sarashina, A; Tatami, S; Tsuda, Y; Yamamura, N, 2005
)
0.85
" The result of the application of the PPK model to the clinical trial in paediatric patients, in which dosage was determined based on the body weight (from 14 kg to less than 24 kg; 10 mg dose, 24 kg or more; 20 mg dose), showed that the C(max) and AUC (25."( Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and children.
Igarashi, T; Sarashina, A; Tatami, S; Tsuda, Y; Yamamura, N, 2005
)
0.61
" The model shows that, if dosage is adjusted based on the body weight, the epinastine exposure in paediatric patients is similar to that in adults."( Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and children.
Igarashi, T; Sarashina, A; Tatami, S; Tsuda, Y; Yamamura, N, 2005
)
0.84
" Bulk drug or dosage form is dissolved in an acetonitrile-buffer mixture and analyzed by an external standard method."( Reverse-phase liquid chromatographic determination of dexamethasone acetate and cortisone acetate in bulk drug substance and dosage forms: collaborative study.
Ng, LL,
)
0.13
" The method was then optimized for dexamethasone acetate and cortisone acetate bulk drug and dosage forms."( Reverse phase liquid chromatographic determination of dexamethasone acetate and cortisone acetate in bulk drug substances and dosage forms: method development.
NG, LL,
)
0.13
" Also there was achieved a parallel analysis of buthylhydroxyanisol, as a preservative, and hydroquinone, as a degradation product of calcium dobesilate, present in these dosage forms."( Validation of liquid chromatographic method for analysis of lidocaine hydrochloride, dexamethasone acetate, calcium dobesilate, buthylhydroxyanisol and degradation product hydroquinone in suppositories and ointment.
Ivanovic, I; Markovic, S; Petrovic, S; Zecevic, M; Zivanovic, Lj, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
anti-allergic agentA drug used to treat allergic reactions.
histamine antagonistHistamine antagonists are the drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists.
ophthalmology drugAny compound used for the treatment of eye conditions or eye diseases.
H1-receptor antagonistH1-receptor antagonists are the drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine.
[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 (3)

ClassDescription
guanidinesAny organonitrogen compound containing a carbamimidamido (guanidino) group. Guanidines have the general structure (R(1)R(2)N)(R(3)R(4)N)C=N-R(5) and are related structurally to amidines and ureas.
benzazepineA group of two-ring heterocyclic compounds consisting of a benzene ring fused to an azepine ring.
corticosteroid hormoneAny of a class of steroid hormones that are produced in the adrenal cortex.
[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]

Pathways (1)

PathwayProteinsCompounds
Epinastine H1-Antihistamine Action87

Protein Targets (34)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
dopamine D1 receptorHomo sapiens (human)Potency0.09200.00521.30228.1995AID624455
thioredoxin reductaseRattus norvegicus (Norway rat)Potency31.62280.100020.879379.4328AID588453
ATAD5 protein, partialHomo sapiens (human)Potency12.99000.004110.890331.5287AID493107
regulator of G-protein signaling 4Homo sapiens (human)Potency37.64990.531815.435837.6858AID504845
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency33.58750.035520.977089.1251AID504332
D(1A) dopamine receptorHomo sapiens (human)Potency8.65340.02245.944922.3872AID488982; AID488983
glp-1 receptor, partialHomo sapiens (human)Potency0.89130.01846.806014.1254AID624417
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency0.01513.189029.884159.4836AID1224846
AR proteinHomo sapiens (human)Potency1.30390.000221.22318,912.5098AID1259243; AID1259247; AID1259381; AID743035; AID743036; AID743040; AID743042; AID743053; AID743054; AID743063
Smad3Homo sapiens (human)Potency4.46680.00527.809829.0929AID588855
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency0.00790.00137.762544.6684AID914; AID915
progesterone receptorHomo sapiens (human)Potency12.36650.000417.946075.1148AID1346784; AID1346795; AID1347036
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency38.90180.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.08190.000214.376460.0339AID720691; AID720692; AID720719
estrogen nuclear receptor alphaHomo sapiens (human)Potency0.11910.000229.305416,493.5996AID1259244; AID743075; AID743078; AID743080; AID743091
GVesicular stomatitis virusPotency30.90080.01238.964839.8107AID1645842
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency0.02360.001723.839378.1014AID743083
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency9.520519.739145.978464.9432AID1159509
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency4.46680.10009.191631.6228AID1346983
gemininHomo sapiens (human)Potency1.25890.004611.374133.4983AID624297
survival motor neuron protein isoform dHomo sapiens (human)Potency2.51190.125912.234435.4813AID1458
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency0.09440.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency30.90080.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency30.90080.01238.964839.8107AID1645842
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency0.09440.001551.739315,848.9004AID1259244
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency30.90080.01238.964839.8107AID1645842
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency0.00510.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency0.00510.011912.222168.7989AID651632
cytochrome P450 2C9, partialHomo sapiens (human)Potency30.90080.01238.964839.8107AID1645842
[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)
Solute carrier family 22 member 2Homo sapiens (human)IC50 (µMol)4.30000.40003.10009.7000AID721751
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)97.06700.00091.901410.0000AID161281; AID243151; AID408340
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC50 (µMol)29.80000.16003.95718.6000AID721752
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50 (µMol)1.10000.01002.765610.0000AID721754
[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)
Nuclear receptor subfamily 1 group I member 2Rattus norvegicus (Norway rat)EC50 (µMol)4.50000.01004.139410.0000AID1215090
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (123)

Processvia Protein(s)Taxonomy
activation of cysteine-type endopeptidase activity involved in apoptotic processSolute carrier family 22 member 2Homo sapiens (human)
positive regulation of gene expressionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
monoatomic cation transportSolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin transportSolute carrier family 22 member 2Homo sapiens (human)
body fluid secretionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 2Homo sapiens (human)
amine transportSolute carrier family 22 member 2Homo sapiens (human)
putrescine transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transportSolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 2Homo sapiens (human)
choline transportSolute carrier family 22 member 2Homo sapiens (human)
dopamine transportSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 2Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
histamine transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 2Homo sapiens (human)
histamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
amino acid import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
L-arginine import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
export across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
L-alpha-amino acid transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
organic cation transportMultidrug and toxin extrusion protein 2Homo sapiens (human)
transmembrane transportMultidrug and toxin extrusion protein 2Homo sapiens (human)
proton transmembrane transportMultidrug and toxin extrusion protein 2Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
xenobiotic transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
amino acid import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-alpha-amino acid transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
proton transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
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)
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)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (56)

Processvia Protein(s)Taxonomy
amine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-amino acid transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
choline transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
efflux transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
organic cation transmembrane transporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
antiporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
transmembrane transporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
polyspecific organic cation:proton antiporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
protein bindingMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-amino acid transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
polyspecific organic cation:proton antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
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)
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)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (33)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
membraneSolute carrier family 22 member 2Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 2Homo sapiens (human)
presynapseSolute carrier family 22 member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
apical plasma membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
basolateral plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
apical plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
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 membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
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)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (157)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1053266Agonist activity at human recombinant dopamine D1 receptor expressed in CHOK1 cells assessed as stimulation of cAMP accumulation at 100 uM after 30 mins by HTRF assay relative to SKF812972013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1053262Agonist activity at human recombinant dopamine D2 long receptor expressed in CHOK1 cells coexpressing mitochondrial apoaequorin at 100 uM by luminometric analysis relative to quinpirol2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID243151Inhibitory concentration against potassium channel HERG2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID721754Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID679115TP_TRANSPORTER: transepithelial transport (basal to apical) of Epinastine at a concentration of 5uM in LLC-GA5-COL150 cells2004Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 32, Issue:5
Influx and efflux transport of H1-antagonist epinastine across the blood-brain barrier.
AID88624Potency against histamine H1 receptor on guinea pig ileum1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
The histamine H1-receptor antagonist binding site. A stereoselective pharmacophoric model based upon (semi-)rigid H1-antagonists and including a known interaction site on the receptor.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID86244Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
The histamine H1-receptor antagonist binding site. A stereoselective pharmacophoric model based upon (semi-)rigid H1-antagonists and including a known interaction site on the receptor.
AID1053260Antagonist activity at human recombinant dopamine D2 long receptor expressed in CHOK1 cells coexpressing mitochondrial apoaequorin assessed as inhibition of agonist-induced effect at 50 uM after 15 mins by luminometric analysis relative to haloperidol2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID237685Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).
AID1053264Antagonist activity at human recombinant dopamine D1 receptor expressed in CHOK1 cells assessed as inhibition of agonist-induced cAMP accumulation at 100 uM preincubated for 10 mins prior to agonist addition measured after 30 mins by HTRF assay relative t2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.
AID721751Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID721752Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID721753Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC 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.
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.
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.
AID1346037Human H1 receptor (Histamine receptors)2008Journal of pharmacological sciences, May, Volume: 107, Issue:1
Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, 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.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
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.
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.
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.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID213396Glucocorticoid induced Tyrosine Aminotransferase activity relative to Dexamethasone1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID74376Relative binding affinity to glucocorticoid receptor on cytosol from liver at 4 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID1348553Anti-asthmatic activity in ovalbumin-induced asthmatic Sprague-Dawley rat model assessed as improvement in lung function by measuring airway resistance at 0.5 g/kg, po co-administered with OVA from day 15 to 21 of experiment period (Rvb = 67.33 +/- 10.54 2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of a novel series of α-terpineol derivatives as promising anti-asthmatic agents: Their design, synthesis, and biological evaluation.
AID1215087Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID74378Relative binding affinity to glucocorticoid receptor on cytosol from thymus at 4 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1514419Anti-asthmatic activity in ovalbumin-induced asthmatic BALB/c mouse model assessed as IgE level in plasma at 0.6 mg/kg, po co-administered with ovalbumin from day 21 to 28 of experiment period by ELISA (Rvb = 2544.05 +/- 229.07 ng/ml)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis and biological evaluation of Ginsenoside Compound K analogues as a novel class of anti-asthmatic agents.
AID1514421Anti-asthmatic activity in ovalbumin-induced asthmatic BALB/c mouse model assessed as 6.25 mg/ml methacholine-induced airway resistance at 0.6 mg/kg, po co-administered with ovalbumin from day 21 to 28 of experiment period measured post last dose by pleth2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis and biological evaluation of Ginsenoside Compound K analogues as a novel class of anti-asthmatic agents.
AID1215090Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID1348561Anti-asthmatic activity in ovalbumin-induced asthmatic Sprague-Dawley rat model assessed as IL-17 levels in serum at 0.5 g/kg, po co-administered with OVA from day 15 to 21 of experiment period (Rvb = 16.85 +/- 1.13 pg/ml)2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of a novel series of α-terpineol derivatives as promising anti-asthmatic agents: Their design, synthesis, and biological evaluation.
AID1514422Anti-asthmatic activity in ovalbumin-induced asthmatic BALB/c mouse model assessed as 12.5 mg/ml methacholine-induced airway resistance at 0.6 mg/kg, po co-administered with ovalbumin from day 21 to 28 of experiment period measured post last dose by pleth2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis and biological evaluation of Ginsenoside Compound K analogues as a novel class of anti-asthmatic agents.
AID1514424Anti-asthmatic activity in ovalbumin-induced asthmatic BALB/c mouse model assessed as 50 mg/ml methacholine-induced airway resistance at 0.6 mg/kg, po co-administered with ovalbumin from day 21 to 28 of experiment period measured post last dose by plethys2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis and biological evaluation of Ginsenoside Compound K analogues as a novel class of anti-asthmatic agents.
AID74373Relative binding affinity to glucocorticoid receptor on cytosol from hepatoma tissue cells at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID74375Relative binding affinity to glucocorticoid receptor on cytosol from liver at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1514425Anti-asthmatic activity in ovalbumin-induced asthmatic BALB/c mouse model assessed as 100 mg/ml methacholine-induced airway resistance at 0.6 mg/kg, po co-administered with ovalbumin from day 21 to 28 of experiment period measured post last dose by plethy2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis and biological evaluation of Ginsenoside Compound K analogues as a novel class of anti-asthmatic agents.
AID384955Intrinsic aqueous solubility at pH 10 by shake-flask method2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Molecular characteristics for solid-state limited solubility.
AID39320Relative binding affinity for androgen receptor of prostate of rat at 2 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID126435Relative binding affinity for mineralocorticoid receptor of rat kidney at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID74374Relative binding affinity to glucocorticoid receptor on cytosol from hepatoma tissue cells at 4 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID1514423Anti-asthmatic activity in ovalbumin-induced asthmatic BALB/c mouse model assessed as 25 mg/ml methacholine-induced airway resistance at 0.6 mg/kg, po co-administered with ovalbumin from day 21 to 28 of experiment period measured post last dose by plethys2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis and biological evaluation of Ginsenoside Compound K analogues as a novel class of anti-asthmatic agents.
AID1348552Anti-asthmatic activity in ovalbumin-induced asthmatic Sprague-Dawley rat model assessed as improvement in lung function by measuring dynamic compliance of the airway at 0.5 g/kg, po co-administered with OVA from day 15 to 21 of experiment period (Rvb = 02018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of a novel series of α-terpineol derivatives as promising anti-asthmatic agents: Their design, synthesis, and biological evaluation.
AID74377Relative binding affinity to glucocorticoid receptor on cytosol from thymus at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID1348558Anti-asthmatic activity in ovalbumin-induced asthmatic Sprague-Dawley rat model assessed as IL-14 levels in serum at 0.5 g/kg, po co-administered with OVA from day 15 to 21 of experiment period (Rvb = 16.04 +/- 1.41 pg/ml)2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of a novel series of α-terpineol derivatives as promising anti-asthmatic agents: Their design, synthesis, and biological evaluation.
AID162613Relative binding affinity for progestin receptor of uterus of rabbit at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID90104Potency relative to fluocinolone 16,17-acetonide in the human vasoconstictor test1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
Structure-activity relationships in the antiinflammatory steroids: a pattern-recognition approach.
AID91224Antiinflammatory activity measured by using McKenzie-Stoughton human vasoconstrictor assay1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Computer-aided studies of the structure-activity relationships between the structure of some steroids and their antiinflammatory activity.
AID1215086Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID1347160Primary screen NINDS Rhodamine 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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
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.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (272)

TimeframeStudies, This Drug (%)All Drugs %
pre-199045 (16.54)18.7374
1990's51 (18.75)18.2507
2000's93 (34.19)29.6817
2010's70 (25.74)24.3611
2020's13 (4.78)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 54.03

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

MetricThis Compound (vs All)
Research Demand Index54.03 (24.57)
Research Supply Index5.24 (2.92)
Research Growth Index5.64 (4.65)
Search Engine Demand Index98.23 (26.88)
Search Engine Supply Index2.30 (0.95)

This Compound (54.03)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials31 (19.75%)5.53%
Trials8 (5.88%)5.53%
Reviews8 (5.10%)6.00%
Reviews2 (1.47%)6.00%
Case Studies4 (2.55%)4.05%
Case Studies8 (5.88%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other114 (72.61%)84.16%
Other118 (86.76%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (15)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Bioequivalence of 20 mg of the New Formulation of WAL 801 CL Dry Syrup Compared to 20 mg of the Conventional Formulation of WAL 801 CL Dry Syrup Following Oral Administration in Healthy Male Volunteers (an Open-label, Randomised, Single-dose, 2x2 Crossove [NCT02260050]Phase 134 participants (Actual)Interventional2004-06-30Completed
Phase III Double-blind Comparative Study of WAL801CL Dry Syrup in Paediatric Perennial Allergic Rhinitis [NCT02182544]Phase 3151 participants (Actual)Interventional2001-06-30Completed
Phase III Double-Blind Comparative Study of WAL 801 CL Dry Syrup in Paediatric Atopic Dermatitis Patients [NCT02182557]Phase 3162 participants (Actual)Interventional2001-06-30Completed
[NCT01382654]Phase 2131 participants (Actual)Interventional2006-09-30Completed
Double-blind, Randomized, Parallel Trial to Evaluate the Clinical Efficacy and Safety of Epinastine 10 mg + Pseudoephedrine 120 mg SR, Twice a Day, Versus Epinastine 10 mg Alone, Twice a Day, in the Treatment of Outpatients With Perennial Allergic Rhiniti [NCT02182518]Phase 3101 participants (Actual)Interventional2000-05-31Completed
Phase III Open-labeled Study of WAL 801 CL Dry Syrup in Pediatric Atopic Dermatitis Patients [NCT02182570]Phase 362 participants (Actual)Interventional2001-06-30Completed
A Phase 3 Randomized, Multi-Center, Double-Blind, Placebo-Controlled, Parallel-Group, Multiple Dose Safety and Efficacy Study of Epinastine Nasal Spray vs. Placebo in Subjects With Seasonal Allergic Rhinitis [NCT00564421]Phase 3798 participants (Actual)Interventional2007-12-18Completed
A Trial in Healthy Volunteers of the Relative Bioavailability of Epinastine Syrup, a New Galenic Form, Compared to the Reference Product Tablets [NCT02260063]Phase 124 participants (Actual)Interventional1998-11-30Completed
A Double-blind, Randomised, Placebo-controlled Single Increasing Dose Tolerance Study in Healthy Male Volunteers After Intranasal Application of Epinastine Nasal (Dosage: 0.035 mg (0.025 % Solution) - 0.42 mg (0.3 % Solution)) [NCT02260037]Phase 139 participants (Actual)Interventional2001-08-31Completed
A Randomized, Multi-Center, Double-Blind, Placebo-Controlled, Parallel-Group, Dose-Ranging Safety, Efficacy, and Tolerability Study of Two Doses of Epinastine Nasal Spray (0.05% and 0.1%) vs. Placebo in Subjects With Seasonal Allergic Rhinitis [NCT00407927]Phase 2571 participants (Actual)Interventional2006-12-31Completed
Study of the Pharmacokinetic Interactions and Relative Bioavailability of Epinastine and Pseudoephedrine in Healthy Volunteers, Comparing Tablets Containing the Fixed Combination of the Two Substances With Tablets Containing Each of the Two Substances Sep [NCT02182531]Phase 125 participants (Actual)Interventional1999-08-31Completed
Comparison of CL Wear Between Epinastine Hydrochloride and Olopatadine Hydrochloride [NCT00489398]Phase 425 participants (Anticipated)Interventional2007-07-31Withdrawn(stopped due to Protocol changes)
Effectiveness of Olopatadine HCl Ophthalmic Solution, 0.1% Compared to Epinastine HCl Ophthalmic Solution, 0.05% in the Treatment of Allergic Conjunctivitis to Japanese Cedar Pollen [NCT02251613]Phase 450 participants (Actual)Interventional2013-12-31Completed
Investigating the Efficacy of Artificial Tear Supplements and Cold Compresses for the Treatment of Seasonal Allergic Conjunctivitis [NCT01569191]Phase 418 participants (Actual)Interventional2012-03-31Completed
Double-masked, Comparison Study of DE-114 Ophthalmic Solution in Patients With Allergic Conjunctivitis - Phase 3, Confirmatory Study - [NCT01363700]Phase 387 participants (Actual)InterventionalCompleted
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01363700 (4) [back to overview]Mean Hyperemia Score Compared to Olopatadine Period2
NCT01363700 (4) [back to overview]Mean Hyperemia Score Compared to Placebo Period1
NCT01363700 (4) [back to overview]Mean Ocular Itching Score Compared to Olopatadine Period2
NCT01363700 (4) [back to overview]Mean Ocular Itching Score Compared to Placebo Period1
NCT01569191 (3) [back to overview]Ocular Redness
NCT01569191 (3) [back to overview]Ocular Temperature
NCT01569191 (3) [back to overview]Symptoms
NCT02251613 (2) [back to overview]Mean Conjunctival Hyperemia at 20 Minutes Post-CAC, Day 1
NCT02251613 (2) [back to overview]Mean Ocular Itching at 7 Minutes Post-CAC, Day 1

Mean Hyperemia Score Compared to Olopatadine Period2

"A conjunctivitis allergic challenge (CAC) was performed 4 hours after drop instillation. Mean palpebral and bulbar conjunctiva hyperemia was assessed by the investigator at 5, 10, and 20 min post challenge and graded on a 4 points scale of 0-3 (0=none and 3= extremely severe). Total hyperemia score is defined as the sum of the palpebral and bulbar conjunctiva scores.~The endpoint used the average score of three time points (5, 10, and 20 minutes) after allergen challenge ." (NCT01363700)
Timeframe: Visit 7 (5, 10, and 20 minutes post-CAC)

Interventionscore (Mean)
Epinastine (DE-114) Ophthalmic Solution2.4
Olopatadine Ophthalmic Solution2.7
Placebo Ophthalmic Solution3.7

[back to top]

Mean Hyperemia Score Compared to Placebo Period1

"A conjunctivitis allergic challenge (CAC) was performed 4 hours after drop instillation. Mean palpebral and bulbar conjunctiva hyperemia was assessed by the investigator at 5, 10, and 20 min post challenge and graded on a 4 points scale of 0-3 (0=none and 3= extremely severe). Total hyperemia score is defined as the sum of the palpebral and bulbar conjunctiva scores. Count unit was defined each eye.~The endpoint used the average score of three time points (5, 10, and 20 minutes) after allergen challenge ." (NCT01363700)
Timeframe: Visit 5 (5, 10, and 20 minutes post-CAC)

Interventionscore (Mean)
Epinastine (DE-114) Ophthalmic Solution2.7
Placebo Ophthalmic Solution4.1

[back to top]

Mean Ocular Itching Score Compared to Olopatadine Period2

"A conjunctivitis allergic challenge (CAC) was performed 4 hours after drop instillation. Mean ocular itching score was assessed by the subject at 3, 5, and 10 min post challenge on a 5 points scale of 0-4 where 0=no itching and 4=incapacitating itch.~The endpoint used the average score of three time points (3, 5, and 10 minutes) after allergen challenge ." (NCT01363700)
Timeframe: Visit 7 (3, 5, and 10 minutes post-CAC)

Interventionscore (Mean)
Epinastine (DE-114) Ophthalmic Solution0.2
Olopatadine Ophthalmic Solution0.2
Placebo Ophthalmic Solution1.5

[back to top]

Mean Ocular Itching Score Compared to Placebo Period1

"A conjunctivitis allergic challenge (CAC) was performed 4 hours after drop instillation. Mean ocular itching score was assessed by the subject at 3, 5, and 10 min post challenge and graded on a 5 points scale of 0-4 where 0=no itching and 4=incapacitating itch. Count unit was defined each eye.~The endpoint used the average score of three time points (3, 5, and 10 minutes) after allergen challenge ." (NCT01363700)
Timeframe: Visit 5 (3, 5, and 10 minutes post-CAC)

Interventionscore (Mean)
Epinastine (DE-114) Ophthalmic Solution0.4
Placebo Ophthalmic Solution1.7

[back to top]

Ocular Redness

"Bulbar and limbal redness will be observed with a slit lamp biomicroscope and graded using a validated scale~• The 'Efron' grading scale consists of 5 pictures of eyes of increasing severity of blood vessels over the white of the eye, with the clinician selecting the image closest to what they observe on the patient (0 indicating a white eye and 4 a very irritated eye). There are no subscales" (NCT01569191)
Timeframe: 1 hour

Interventionunits on a scale (Mean)
No Treatment2.15
Artificial Tear Supplement1.79
Cold Compress1.61
Anti-allergic Medication1.78

[back to top]

Ocular Temperature

Ocular surface temperature will be measured with an infra-red camera (NCT01569191)
Timeframe: 1 hour

Interventiondegrees centrigrade (Mean)
No Treatment35.88
Artificial Tear Supplement35.91
Cold Compress35.41
Anti-allergic Medication34.56

[back to top]

Symptoms

Short questionnaire Ocular allergy symptomology was also measured using the eye symptom section from the Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ) on a 0 to 6 scale, with the summed score for itching, watering, swelling and soreness resulting in a summed score between 0 and 24. A higher score indicates a worse outcome (more severe symptoms) (NCT01569191)
Timeframe: 1 hour

InterventionUnits on a scale (Mean)
No Treatment15.3
Artificial Tear Supplement11.3
Cold Compress13.3
Anti-allergic Medication9.8

[back to top]

Mean Conjunctival Hyperemia at 20 Minutes Post-CAC, Day 1

A CAC (one drop of allergen solution to each eye) was performed 5 minutes after study medication instillation. Conjunctival hyperemia (redness) was evaluated by the investigator based on biomicroscopy for each eye at 20 (±1) minutes post-CAC and rated on a 0-4 scale (0=none, 4=extremely severe). (NCT02251613)
Timeframe: Day 1, 20 minutes post-CAC

Interventionunits on a scale (Mean)
Olopatadine 0.1%0.89
Epinastine 0.05%1.12

[back to top]

Mean Ocular Itching at 7 Minutes Post-CAC, Day 1

A CAC (one drop of allergen solution to each eye) was performed 5 minutes after study medication instillation. Ocular itching was assessed by the patient for each eye at 7 (±1) minutes post-CAC and rated on a 0-4 scale (0=none, 4=incapacitating itch with irresistible urge to rub). (NCT02251613)
Timeframe: Day 1, 7 minutes post-CAC

Interventionunits on a scale (Mean)
Olopatadine 0.1%0.23
Epinastine 0.05%0.37

[back to top]