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rilmenidine

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Description

Rilmenidine is an antihypertensive medication that acts as an alpha-2 adrenergic agonist. It is synthesized through a multi-step process involving the condensation of 2-amino-4-thiazolecarboxylic acid with 2,6-dichloroaniline, followed by various reactions to introduce the desired functional groups. Rilmenidine exerts its antihypertensive effects primarily by stimulating alpha-2 adrenergic receptors in the central nervous system, leading to a decrease in sympathetic nervous system activity. This results in reduced peripheral vasoconstriction and a lowering of blood pressure. It is also thought to have a vasodilatory effect by acting on postsynaptic alpha-2 receptors. Rilmenidine is studied because of its potential therapeutic benefits for the treatment of hypertension, particularly for patients with mild to moderate hypertension who are unresponsive or intolerant to other antihypertensive drugs. Research is ongoing to investigate its potential role in other medical conditions, including anxiety disorders, Parkinson's disease, and pain management. Rilmenidine's importance lies in its ability to provide an alternative treatment option for hypertension, with a unique mechanism of action compared to other classes of antihypertensives.'

Rilmenidine: Oxazole derivative that acts as an agonist for ALPHA-2 ADRENERGIC RECEPTORS and IMIDAZOLINE RECEPTORS. It is used in the treatment of HYPERTENSION. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68712
CHEMBL ID289480
CHEBI ID8862
SCHEMBL ID114420
MeSH IDM0100916

Synonyms (97)

Synonym
n-(dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine
n-(dicyclopropylmethyl)-n-(4,5-dihydro-1,3-oxazol-2-yl)amine
n-(dicyclopropylmethyl)-4,5-dihydrooxazol-2-amine
AB00513728-09
LOPAC0_001104
NCI60_022181
hyperium
PRESTWICK3_000982
nsc-664312
nsc664312
EU-0101104
einecs 259-021-0
oxazolidine, 2-((dicyclopropylmethyl)imino)-
s 3341
rilmenidine [inn]
2-oxazolamine, n-(dicyclopropylmethyl)-4,5-dihydro-
2-oxazolamine, 4,5-dihydro-n-(dicyclopropylmethyl)-
methylamine, 1,1-dicyclopropyl-n-(2-oxazolinyl)-
rilmenidinum [latin]
rilmenidia [spanish]
brn 1211287
tocris-0790
cas-54187-04-1
lopac-r-134
NCGC00015884-01
NCGC00021689-02
NCGC00015884-02
PRESTWICK2_000982
BSPBIO_001043
BPBIO1_001149
AB00514648
rilmenidine
oxaminozoline
54187-04-1
NCGC00021689-06
PRESTWICK1_000982
PRESTWICK0_000982
SPBIO_002944
NCGC00021689-05
NCGC00015884-03
NCGC00021689-04
NCGC00015884-07
R-134
HMS2089G15
n-(dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine;
NCGC00015884-10
CHEMBL289480
chebi:8862 ,
L001230
hyperium (tn)
D08482
rilmenidine (inn)
NCGC00015884-09
HMS3263M10
AKOS006273431
n-(dicyclopropylmethyl)-4,5-dihydrooxazol-3-ium-2-amine
A830020
dtxcid1025194
dtxsid3045194 ,
tox21_110254
CCG-205180
NCGC00015884-05
NCGC00015884-06
NCGC00015884-11
NCGC00015884-04
NCGC00015884-08
unii-p67im25id8
p67im25id8 ,
FT-0630668
LP01104
AB07513
rilmenidine [who-dd]
rilmenidine [mi]
SCHEMBL114420
tox21_110254_1
NCGC00015884-13
tox21_501104
NCGC00261789-01
CQXADFVORZEARL-UHFFFAOYSA-N
2-(dicyclopropylmethylamino) oxazoline
W-105661
arsenictrifluoride
bdbm50070328
SR-01000002992-3
sr-01000002992
CS-0019423
HY-100490
SR-01000002992-4
(n-dicyclopropylmethyl)-amino-2-oxazoline
DB11738
Q967973
SDCCGSBI-0051073.P002
NCGC00015884-19
nsc 664312; oxaminozoline; rilmenidene;s 3341
mfcd00865924
SY267932
EN300-8092697

Research Excerpts

Overview

Rilmenidine is an alpha 2 adrenoreceptor agonist used in the treatment of mild and moderate hypertension. It acts mainly through the activation of the imidazoline (I(1) receptor in the rostral ventrolateral medulla (RVLM)

ExcerptReferenceRelevance
"Rilmenidine is an alpha 2 adrenoreceptor agonist used in the treatment of mild and moderate hypertension. "( Development of a fast LC-MS/MS method for quantification of rilmenidine in human serum: elucidation of fragmentation pathways by HRMS.
Chytil, L; Cvačka, J; Marešová, V; Slanař, O; Štícha, M; Štrauch, B; Widimský, J, 2010
)
2.05
"Rilmenidine is a second-generation centrally acting antihypertensive drug that acts mainly through the activation of the imidazoline (I(1)) receptor in the rostral ventrolateral medulla (RVLM). "( The hypotensive action of rilmenidine is dependent on functional N-methyl-D-aspartate receptor in the rostral ventrolateral medulla of conscious spontaneously hypertensive rats.
Abdel-Rahman, AA; Zhang, J, 2002
)
2.06
"Rilmenidine is a centraly acting drug of IInd generation (imidazoline I1 receptors agonist) with potent antihypertensive and mild negative chronotropic effect. "( [Efficacy and tolerance of rilmenidine in patients with mild to moderate hypertension. Results of a Czech and Slovak 6-month multicenter study].
Widimský, J, 2002
)
2.05
"Rilmenidine is an antihypertensive agent that selectively binds to imidazoline I1 receptor located in the brainstem and kidney. "( Efficacy and safety of rilmenidine, a selective imidazoline I1 receptor binding ligand, in mild-to-moderate Thai hypertensive patients.
Buranakitjaroen, P; Kittipawong, P; Koanantakul, B; Piamsomboon, C; Prasassarakich, N; Silaraks, S; Sukonthasarn, A; Tiyapant, A, 2003
)
2.07
"Rilmenidine is a centrally acting antihypertensive which differs from the other representatives of this class by its very high specificity for the imidazoline I1 receptors and its good tolerability. "( Efficacy and tolerability of long-term rilmenidine treatment in hypertensive diabetic patients. A retrospective analysis of a general practice study.
Meredith, PA; Reid, JL, 2004
)
2.04
"Rilmenidine is a potential antiglaucoma agent, though further studies are necessary."( [Effect of rilmenidine on intraocular pressure in rabbits, interaction with efaroxan and rauwolscine].
Merwid-Lad, A; Misiuk-Hojło, M; Pieśniewska, M; Szaliński, M; Trocha, M, 2004
)
2.16
"Rilmenidine is an antihypertensive drug whose antihypertensive effect occurs via a sympatholytic action on the central nervous system. "( [The effects of rilmenidine on cardiac autonomic function in healthy volunteers].
Celik, A; Kaya, D; Kerpeten, K; Kilit, C; Onrat, E, 2004
)
2.11
"Rilmenidine is an I(1)-imidazoline receptor agonist that reduces blood pressure by modulation of central sympathetic activity, but the effects of low-dose rilmenidine on the hemodynamic responses to physiological maneuvers that increase adrenergic drive is not known."( Reduced hemodynamic responses to physical and mental stress under low-dose rilmenidine in healthy subjects.
Catelli, MF; de Oliveira, MA; Moreira, PB; Nóbrega, AC; Rocha, NN; Teixeira de Castro, RR; Tibiriçá, E, 2006
)
1.29
"Rilmenidine is a novel oxazoline derivative that is effective in the treatment of hypertension. "( Effects of rilmenidine and clonidine on the electroencephalogram, saccadic eye movements, and psychomotor function.
Harron, DW; Hasson, B; King, DJ; McClelland, RJ; Regan, M, 1995
)
2.12
"Rilmenidine is an antihypertensive agent acting at the imidazoline receptor that may have both central effects in the ventral lateral medulla and direct effects on the kidney to alter Na+ excretion. "( Effect of rilmenidine on arterial pressure and urinary output in the spontaneously hypertensive rat.
Cechetto, DF; Kline, RL, 1997
)
2.14
"Rilmenidine is a central hypotensive drug which acts more specifically than clonidine on imidazoline receptors and which has no sedative side effects."( [Rilmenidine in rosacea: a double-blind study versus placebo].
Arcade, B; Cribier, B; Grosshans, E; Michel, C, 1997
)
1.93
"Rilmenidine is an imidazoline I1-receptor agonist that centrally acts by reducing the sympathetic tone. "( Effects of rilmenidine on stress-induced peak blood pressure and renal function.
Ducher, M; Fauvel, JP; Laville, M; Najem, R; Ryon, B, 1999
)
2.14
"Rilmenidine is an innovative antihypertensive agent that binds specifically to I1 imidazoline receptors. "( Rilmenidine in the hypertensive type-2 diabetic: a controlled pilot study versus captopril.
Bauduceau, B; Dupuy, O; Mayaudon, H, 2000
)
3.19
"Rilmenidine is an antihypertensive agent with selectivity for I1 imidazoline receptors that acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. "( Rilmenidine: a clinical overview.
Reid, JL, 2000
)
3.19
"Rilmenidine is an imidazoline derivative that appears to lower blood pressure (BP) by an interaction with imidazoline (I1) receptors in the brainstem (and kidneys). "( Update on rilmenidine: clinical benefits.
Reid, JL, 2001
)
2.16
"Rilmenidine is an oxazoline derivative with antihypertensive activity which was developed to enhance the dissociation between the hypotensive and adverse effect profile of centrally acting agents. "( Distinctive features of rilmenidine possibly related to its selectivity for imidazoline receptors.
Harron, DW, 1992
)
2.03
"Rilmenidine (RIL) is a novel antihypertensive drug selectively acting at the sites of imidazoline receptors. "( Rilmenidine: a novel approach to first-line treatment of hypertension.
Laurent, S; Safar, M, 1992
)
3.17
"Rilmenidine is an oxazoline analogue that has antihypertensive properties that resemble those of clonidine. "( Regional hemodynamic effects of rilmenidine and clonidine in the conscious spontaneously hypertensive rat.
Smits, JF; Struyker-Boudier, HA, 1991
)
2.01
"Rilmenidine is an oxazoline with antihypertensive properties characterised by a dissociation of its antihypertensive and central side effects and the absence of tolerance. "( [Effects of rilmenidine on the central nervous system and kidney].
Fillastre, JP, 1989
)
2.1
"Rilmenidine (RIL) is a new antihypertensive agent which lowers sympathetic tone, so reducing systemic peripheral resistance. "( [Effects of rilmenidine on arterial parameters in essential arterial hypertension].
Pannier, B; Safar, M, 1989
)
2.1
"Rilmenidine is a novel antihypertensive agent related to alpha 2-agonists. "( Rilmenidine: a novel antihypertensive agent.
Safar, ME, 1989
)
3.16
"Rilmenidine is a novel antihypertensive agent related to alpha 2-adrenoceptor agonist, used in the treatment of mild or moderate hypertension at the oral dose of 1 mg once a day or 1 mg twice a day. "( Pharmacokinetics of rilmenidine.
Bromet, N; Genissel, P, 1989
)
2.04
"Rilmenidine (S 3341) is a new alpha 2 agonist, with antihypertensive properties. "( Cardiovascular and central nervous system effects of rilmenidine (S 3341) in rats.
Beau, B; Delbarre, G; Koenig-Berard, E; Labrid, C; Lhoste, F; Tierney, C, 1988
)
1.97
"Rilmenidine (S 3341) is a new agonist of alpha 2 adrenoceptors."( Effects of two alpha 2 agonists, rilmenidine and clonidine, on the morphine withdrawal syndrome and their potential addictive properties in rats.
Koenig-Berard, E; Nadaud, D; Stinus, L; Tierney, C, 1988
)
1.28
"Rilmenidine is a novel alpha 2-adrenoceptor agonist, used in the treatment of mild or moderate hypertension at the oral dose of 1 mg once or twice daily. "( Pharmacokinetics of rilmenidine in healthy subjects.
Albin, H; Bromet, N; Fourtillan, JB; Genissel, P; Mignot, A, 1988
)
2.04

Effects

Rilmenidine has a remarkable role in NO-defective hypertension, possibly by inhibiting central sympathetic outflow. It has a chemical structure similar to that of the imidazolines and has a higher relative selectivity for theImidazoline binding sites than the reference molecule (clonidine) Rilmenpine has a prolonged antihypertensive activity with a chronic vasodilator effect.

Rilmenidine has a remarkable role in NO-defective hypertension, possibly by inhibiting central sympathetic outflow and by affecting receptors in vascular smooth muscle also. It has a prolonged antihypertensive activity with a chronic vasodilator effect and no negative inotropic effect. Rilmanidine has very good clinical tolerability without negative influence on metabolic parameters.

ExcerptReferenceRelevance
"As rilmenidine has a long safety record and is designed for chronic use, our data suggests that it should be considered for the treatment of HD and related conditions."( Rilmenidine attenuates toxicity of polyglutamine expansions in a mouse model of Huntington's disease.
Acevedo-Arozena, A; Brown, SD; Corrochano, S; Menzies, FM; Renna, M; Rose, C; Rubinsztein, DC; Sadiq, O, 2010
)
2.32
"Rilmenidine has a remarkable role in NO-defective hypertension, possibly by inhibiting central sympathetic outflow and by affecting receptors in vascular smooth muscle also. "( Rilmenidine prevents blood pressure increase in rats with compromised nitric oxide production.
Gerová, M; Matusková, J; Pecháòová, O; Török, J, 2004
)
3.21
"Rilmenidine, which has a chemical structure similar to that of the imidazolines, has a higher relative selectivity for the imidazoline binding sites than the reference molecule (clonidine)."( [From alpha 2-adrenergic to endazoline receptors].
Belcourt, A; Bousquet, P; Bricca, G; Dontenwill, M; Feldman, J; Molines, A; Tibirica, E, 1989
)
1
"Rilmenidine has a prolonged antihypertensive activity with a chronic vasodilator effect and no negative inotropic effect."( Noninvasive study of cardiac structure and function after rilmenidine for essential hypertension.
Levy, B; N'guyen van Cao, A; Slama, R, 1988
)
1.24
"As rilmenidine has a long safety record and is designed for chronic use, our data suggests that it should be considered for the treatment of HD and related conditions."( Rilmenidine attenuates toxicity of polyglutamine expansions in a mouse model of Huntington's disease.
Acevedo-Arozena, A; Brown, SD; Corrochano, S; Menzies, FM; Renna, M; Rose, C; Rubinsztein, DC; Sadiq, O, 2010
)
2.32
"Rilmenidine has very good clinical tolerability without negative influence on metabolic parameters."( [Efficacy and tolerance of rilmenidine in patients with mild to moderate hypertension. Results of a Czech and Slovak 6-month multicenter study].
Widimský, J, 2002
)
1.33
"Rilmenidine has a remarkable role in NO-defective hypertension, possibly by inhibiting central sympathetic outflow and by affecting receptors in vascular smooth muscle also. "( Rilmenidine prevents blood pressure increase in rats with compromised nitric oxide production.
Gerová, M; Matusková, J; Pecháòová, O; Török, J, 2004
)
3.21
"Rilmenidine has similar effects on ambulatory BP patterns in hypertensive women with metabolic syndrome as lisinopril. "( Comparison of rilmenidine and lisinopril on ambulatory blood pressure and plasma lipid and glucose levels in hypertensive women with metabolic syndrome.
Anichkov, DA; Schastnaya, OV; Shostak, NA, 2005
)
2.13
"1. Rilmenidine has recently been introduced as a new centrally-acting antihypertensive agent. "( Evidence for the involvement of imidazoline receptors in the central hypotensive effect of rilmenidine in the rabbit.
Belcourt, A; Bousquet, P; Bricca, G; Dontenwill, M; Feldman, J; Tibiriça, E, 1990
)
1.12
"Rilmenidine, which has a chemical structure similar to that of the imidazolines, has a higher relative selectivity for the imidazoline binding sites than the reference molecule (clonidine)."( [From alpha 2-adrenergic to endazoline receptors].
Belcourt, A; Bousquet, P; Bricca, G; Dontenwill, M; Feldman, J; Molines, A; Tibirica, E, 1989
)
1
"Rilmenidine has a prolonged antihypertensive activity with a chronic vasodilator effect and no negative inotropic effect."( Noninvasive study of cardiac structure and function after rilmenidine for essential hypertension.
Levy, B; N'guyen van Cao, A; Slama, R, 1988
)
1.24

Actions

Rilmenidine produced an increase in urine flow rate at doses that failed to significantly alter blood pressure, creatinine clearance, or heart rate. The drug reduced the increase in RSNA seen during the first minute of air jet stress by 35% and reduced the average increase over the next 9 min by 68%.

ExcerptReferenceRelevance
"Rilmenidine caused an increase in mean RR values after administration when compared to pre-drug administration recordings with the patient in supine decubitus (929 ms vs 860 ms, P<.05), but this effect was not found in the placebo group. "( [The effects of rilmenidine on cardiac autonomic function in healthy volunteers].
Celik, A; Kaya, D; Kerpeten, K; Kilit, C; Onrat, E, 2004
)
2.11
"Rilmenidine produced an increase in urine flow rate at doses that failed to significantly alter blood pressure, creatinine clearance, or heart rate."( Renal I1-imidazoline receptor-selective compounds mediate natriuresis in the rat.
Penner, SB; Smyth, DD, 1995
)
1.01
"Rilmenidine reduced the increase in RSNA seen during the first minute of air jet stress by 35% and reduced the average increase over the next 9 min by 68%."( Effect of rilmenidine on the cadiovascular responses to stress in the conscious rabbit.
Burke, SL; Head, GA; Malpas, SC, 1998
)
1.42

Treatment

Rilmenidine pretreatment (10 min), either administered intravenously (0.01, 0.1, 1 mg/kg) or intracisternally (3, 10, 30 microg/kg), dose-dependently prevented the occurrence of bicuculline-induced arrhythmias. Rilmanidine treatment resulted in normalisation of blood pressure (BP) or significant (decrease of SBP/DBP = 20/10 mm Hg) blood pressure decrease in 69%, 22% of subjects.

ExcerptReferenceRelevance
"The rilmenidine co-treatment with doxorubicin reverses G2/M arrest and triggers apoptotic response to DNA damage."( Rilmenidine suppresses proliferation and promotes apoptosis via the mitochondrial pathway in human leukemic K562 cells.
Cavic, M; Djokic, I; Gemovic, B; Nikolic, K; Perovic, V; Srdic-Rajic, T; Veljkovic, N, 2016
)
2.36
"Rilmenidine treatment resulted in normalisation of blood pressure (BP) or significant (decrease of SBP/DBP = 20/10 mm Hg) blood pressure decrease in 69%, 22% of subjects, respectively. "( [Efficacy and tolerance of rilmenidine in patients with mild to moderate hypertension. Results of a Czech and Slovak 6-month multicenter study].
Widimský, J, 2002
)
2.05
"Rilmenidine pretreatment also greatly reduced Fos expression in the lower brainstem, with a very similar pattern to that observed after clonidine pretreatment."( Clonidine and rilmenidine suppress hypotension-induced Fos expression in the lower brainstem of the conscious rabbit.
Dampney, RA; Li, YW, 1995
)
1.37
"Rilmenidine pretreatment (10 min), either administered intravenously (0.01, 0.1, 1 mg/kg) or intracisternally (3, 10, 30 microg/kg), dose-dependently prevented the occurrence of bicuculline-induced arrhythmias and, because of a lower baseline, the blood pressure values reached were less when compared with controls."( Preventive effect of rilmenidine on the occurrence of neurogenic ventricular arrhythmias in rabbits.
Bousquet, P; De Jong, W; Feldman, J; Roegel, JC; Yannoulis, N, 1998
)
1.34

Toxicity

ExcerptReferenceRelevance
" Two hundred sixty-nine were followed for 1 year and 48 withdrew from the trial without any symptom suggesting a withdrawal syndrome: 4 because of adverse effects; 6, lack of efficacy despite triple therapy; 9, intercurrent diseases; 10, noncompliance independent of adverse effects; 18, personal reasons not associated with treatment; and 1, lost to follow-up."( Efficacy and safety of rilmenidine for arterial hypertension.
Beau, B; Brisgand, B; Laurin, S; Mahieux, F; Paraire, M; Vitou, P, 1988
)
0.59
"Monotherapy with rilmenidine is safe and effective in BP treatment and significantly improves QoL in perimenopausal women with essential hypertension."( Rilmenidine--its antihypertensive efficacy, safety and impact on quality of life in perimenopausal women with mild to moderate essential hypertension.
Czarnecka, D; Jaworski, R; Kawecka-Jaszcz, K; Klocek, M; Kucharska, M; Pachocki, R; Zabojszcz, M, 2006
)
2.12
" Mutant huntingtin causes disease via a toxic gain-of-function mechanism and has the propensity to aggregate and form intraneuronal inclusions."( Rilmenidine attenuates toxicity of polyglutamine expansions in a mouse model of Huntington's disease.
Acevedo-Arozena, A; Brown, SD; Corrochano, S; Menzies, FM; Renna, M; Rose, C; Rubinsztein, DC; Sadiq, O, 2010
)
1.8

Pharmacokinetics

Rilmenidine, an alpha 2-adrenoceptor agonist, was studied (1 mg single dose) in order to determine the effects of pathology on its basic pharmacokinetic parameters. In patients with chronic renal failure, total plasma clearance and renal clearance of rilmanidine decreased. terminal half-life was 30-42 hours, which is clearly longer than previous values achieved in healthy volunteers.

ExcerptReferenceRelevance
" The pharmacokinetic parameters were investigated after single or repeated administration in healthy subjects, using labeled and unlabeled compounds."( Pharmacokinetics of rilmenidine.
Bromet, N; Genissel, P, 1989
)
0.6
" The pharmacokinetic parameters were investigated after single or repeated administration in healthy subjects, using labeled and unlabeled compounds."( Pharmacokinetics of rilmenidine in healthy subjects.
Albin, H; Bromet, N; Fourtillan, JB; Genissel, P; Mignot, A, 1988
)
0.6
"Rilmenidine, an alpha 2-adrenoceptor agonist, was studied (1 mg single dose) in order to determine the effects of pathology on its basic pharmacokinetic parameters."( Pharmacokinetics of rilmenidine.
Ehrhardt, JD; Genissel, P; Pozet, N; Singlas, E; Zech, P, 1988
)
2.04
" In patients with chronic renal failure, total plasma clearance and renal clearance of rilmenidine decreased; terminal half-life was 30-42 hours, which is clearly longer than previous values achieved in healthy volunteers."( Pharmacokinetics of rilmenidine in patients with chronic renal insufficiency and in hemodialysis patients.
Aparicio, M; Dratwa, M; el Esper, N; Fillastre, JP; Levaltier, B; Lins, R; Meyrier, A; Mignon, F; Ryckelynck, JP; Sennesael, J, 1994
)
0.83
" Measurements for pharmacokinetic and pharmacodynamic evaluations were performed on the first day of the treatment period and repeated after 1 week and 4 weeks of treatment."( Pharmacokinetic/pharmacodynamic assessment of tolerance to central nervous system effects of a 3 mg sustained release tablet of rilmenidine in hypertensive patients.
Cohen, AF; de Visser, SJ; Schoemaker, RC; van der Post, JP; van Gerven, JM, 2004
)
0.53

Compound-Compound Interactions

ExcerptReferenceRelevance
"The primary objective was to assess the effects of rilmenidine monotherapy and in combination with perindopril on blood pressure (BP) in patients assessed with grade 1 or 2 essential hypertension."( Value of rilmenidine therapy and its combination with perindopril on blood pressure and left ventricular hypertrophy in patients with essential hypertension (VERITAS).
Borbás, S; Dienes, BS; Farsang, C; Lengyel, M; Zorándi, A, 2003
)
0.99

Bioavailability

The bioavailability of two rilmenidine tablet formulations was compared in healthy male (17) and female (8) subjects, aged 18 to 36 years. The tablets had an absolute bioavailability factor close to 1 and a maximal plasma concentration achieved within 2 hours.

ExcerptReferenceRelevance
" Rilmenidine was rapidly and extensively absorbed, with an absolute bioavailability close to one and a time to peak plasma concentration of two hours."( Pharmacokinetics of rilmenidine.
Bromet, N; Genissel, P, 1989
)
1.51
" Rilmenidine was rapidly and extensively absorbed, with an absolute bioavailability factor close to 1 and a maximal plasma concentration achieved within 2 hours."( Pharmacokinetics of rilmenidine in healthy subjects.
Albin, H; Bromet, N; Fourtillan, JB; Genissel, P; Mignot, A, 1988
)
1.51
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
"The bioavailability of two rilmenidine tablet formulations was compared in healthy male (17) and female (8) subjects, aged 18 to 36 years, during a laboratory-blind, randomized, two-treatment, two-period, cross-over study under fasting conditions."( Bioequivalence evaluation of rilmenidine in healthy volunteers.
Groenewoud, G; Meyer, B; Potgieter, L, 2009
)
0.94
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The daily dosage of rilmenidine was 1 mg, and could be increased to 2 mg/day. Dose-response curves were determined for the effects of. rilmanidine as well as of the alpha-2 selective agonist UK 14304 [5-bromo-6-(2-imidazolin-2-ylamino)-quinoxaline] on blood pressure.

ExcerptRelevanceReference
" Although these results were much better than those obtained in previous studies of this drug, our study shows that blood pressure was rapidly normalized in the majority of hypertensive patients by a daily 1 mg dose of rilmenidine and that doubling this dosage after two weeks of treatment is not necessarily justified, since the percentage of normalized patients increases up to 98 percent after eight weeks of treatment."( [Treatment with rilmenidine 1 mg per day: time-lag to maximum response. A multicenter ambulatory study. Le Groupe Français d'étude Multicentrique d'Hyperium].
Guillet, C; Passeron, J, 1992
)
0.81
" Both depressor and bradycardia responses to intracisternal clonidine were attenuated after 1 day's dosing but only depressor responses were influenced after 6 days."( Do centrally-acting antihypertensive drugs act at non-adrenergic as well as alpha-2 adrenoceptor sites?
Hamilton, CA; Howie, CA; Reid, JL; Yakubu, MA, 1992
)
0.28
" Pretreatment with the same dose of yohimbine or idazoxan shifted the rilmenidine dose-response curves for its hypotensive and bradycardic effects to the right."( Evidence for the involvement of imidazoline receptors in the central hypotensive effect of rilmenidine in the rabbit.
Belcourt, A; Bousquet, P; Bricca, G; Dontenwill, M; Feldman, J; Tibiriça, E, 1990
)
0.73
" In conclusion, these results lead to a decreased dosage regimen in patients with severe renal failure."( Pharmacokinetics of rilmenidine.
Ehrhardt, JD; Genissel, P; Pozet, N; Singlas, E; Zech, P, 1988
)
0.6
" The three dose-response curves were compared by analysis of variance."( Comparative effects of rilmenidine and clonidine on bronchial responses to histamine in asthmatic subjects.
Advenier, C; Dinh Xuan, AT; Lockhart, A; Matran, R; Regnard, J; Vitou, P, 1988
)
0.59
" Dose-response curves for the effects on the plasma noradrenaline concentration (stimulated pithed rabbits) were compared with previously obtained dose-response curves for depression of renal sympathetic nerve activity (conscious rabbits)."( Involvement of peripheral presynaptic inhibition in the reduction of sympathetic tone by moxonidine, rilmenidine and UK 14304.
Starke, K; Szabo, B; Urban, R, 1995
)
0.51
" Dose-response curves were determined for the effects of rilmenidine as well as of the alpha-2 selective agonist UK 14304 [5-bromo-6-(2-imidazolin-2-ylamino)-quinoxaline] on blood pressure, heart rate, renal postganglionic sympathetic nerve activity and the plasma norepinephrine concentration."( Is the sympathoinhibitory effect of rilmenidine mediated by alpha-2 adrenoceptors or imidazoline receptors?
Starke, K; Szabo, B; Urban, R, 1994
)
0.81
" Thus, the following dosage schedule can be proposed."( Pharmacokinetics of rilmenidine in patients with chronic renal insufficiency and in hemodialysis patients.
Aparicio, M; Dratwa, M; el Esper, N; Fillastre, JP; Levaltier, B; Lins, R; Meyrier, A; Mignon, F; Ryckelynck, JP; Sennesael, J, 1994
)
0.61
"5 months), if SDBP was > 90 mm Hg, dosage of rilmenidine was 1 mg twice daily during the following 6 weeks."( Long-term control of blood pressure by rilmenidine in high-risk populations.
Codis, P; Fevrier, B; Pillion, G; Schutz, D, 1994
)
0.82
" This frequency domain analysis demonstrates a modified BP and HR variability profile with an acute dosing of rilmenidine."( Cardiovascular variability after rilmenidine challenge: assessment of acute dosing effects by means of spectral analysis.
Elghozi, JL; Février, B; Girard, A, 1995
)
0.78
"We determined the relative potency of these drugs with respect to their effects on mean arterial pressure and heart rate by performing cumulative intravenous dose-response relationship studies in six conscious rabbits."( Relative importance of central imidazoline receptors for the antihypertensive effects of moxonidine and rilmenidine.
Chan, CK; Head, GA, 1996
)
0.51
" The daily dosage of rilmenidine was 1 mg, and could be increased to 2 mg/day."( Regression of left ventricular hypertrophy in hypertensive patients after 1 year of treatment with rilmenidine: a double-blind, randomized, controlled (versus nifedipine) study.
Balazovjech, I; Dubai, G; Dvorak, I; Januszewicz, W; Krupa-Wojciechowska, B; Kubasik, A; Kuch-Wocial, A; Polak, G; Sadowski, Z; Simon, K; Stejfa, M; Szwed, H, 1998
)
0.84
"One-year treatment with a daily dosage of 1 or 2 mg rilmenidine achieves a significant reduction of left ventricular mass, which is not statistically different than that occurring with a daily dosage of 40 mg of slow-release nifedipine."( Regression of left ventricular hypertrophy in hypertensive patients after 1 year of treatment with rilmenidine: a double-blind, randomized, controlled (versus nifedipine) study.
Balazovjech, I; Dubai, G; Dvorak, I; Januszewicz, W; Krupa-Wojciechowska, B; Kubasik, A; Kuch-Wocial, A; Polak, G; Sadowski, Z; Simon, K; Stejfa, M; Szwed, H, 1998
)
0.77
" Dose-response data show dexmedetomidine to be the most potent inhibitor."( Inhibition of water permeability in the rat collecting duct: effect of imidazoline and alpha-2 compounds.
Hébert, CA; Kudo, LH; Rouch, AJ, 1999
)
0.3
" Both drugs, when applied in a once-daily dosage schedule, appear to control hypertension in most patients."( Central I1-imidazoline receptors as targets of centrally acting antihypertensive drugs. Clinical pharmacology of moxonidine and rilmenidine.
Peters, SL; Van Zwieten, PA, 1999
)
0.51
" In 15 hypertensive patients, noradrenaline and adrenaline plasma kinetics and intra-arterial blood pressure measurements were performed at rest, after mental stress (difficult mental arithmetic) and during head-up tilting, at the end of the 2-week dosing periods."( Rilmenidine sympatholytic activity preserves mental stress, orthostatic sympathetic responses and adrenaline secretion.
Esler, M; Hastings, J; Jennings, G; Lambert, G; Lux, A; Socratous, F, 2004
)
1.77
" In 15 hypertensive patients, noradrenaline and adrenaline plasma kinetics and intra-arterial blood pressure measurements were performed at rest, after mental stress (difficult mental arithmetic) and during head-up tilting, at the end of the 2-week dosing periods."( [Rilmenidine sympatholytic activity preserves mental and orthostatic sympathetic response and epinephrine secretion].
Esler, M; Hastings, J; Jennings, G; Lambert, G; Lux, A; Socratous, F,
)
1.04
" Dose-response curves were determined for phenylephrine and for several imidazoline ligands, using endothelium denuded, isolated ring segments, of tail arteries from adult male Sprague-Dawley rats."( Centrally acting imidazolines stimulate vascular alpha 1A-adrenergic receptors in Rat-Tail Artery.
Crane, L; Edwards, LP; George, OK; Gonzalez, RR; Kennedy, WB,
)
0.13
"Initial dose-response curves to rilmenidine were determined in urethane anaesthetized rabbits."( Contribution of imidazoline receptors and alpha2-adrenoceptors in the rostral ventrolateral medulla to sympathetic baroreflex inhibition by systemic rilmenidine.
Burke, SL; Chan, CK; Head, GA, 2007
)
0.82
" This reduction of energy intake was abolished by efaroxan at the same dosing for blockade of I1R."( Improvement of obesity by activation of I1-imidazoline receptors in high fat diet-fed mice.
Cheng, J; Chung, HH, 2013
)
0.39
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
isoureaA carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (51)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency31.67680.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency18.83360.000714.592883.7951AID1259392
AR proteinHomo sapiens (human)Potency30.10650.000221.22318,912.5098AID743035
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency25.11890.00137.762544.6684AID914; AID915
thyroid stimulating hormone receptorHomo sapiens (human)Potency39.81070.001318.074339.8107AID926
regulator of G-protein signaling 4Homo sapiens (human)Potency37.68580.531815.435837.6858AID504845
EWS/FLI fusion proteinHomo sapiens (human)Potency1.86550.001310.157742.8575AID1259252
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency18.99590.000214.376460.0339AID720692
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency33.49150.001530.607315,848.9004AID1224820
estrogen nuclear receptor alphaHomo sapiens (human)Potency0.00070.000229.305416,493.5996AID743079
cytochrome P450 2D6Homo sapiens (human)Potency27.54040.00108.379861.1304AID1645840
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency13.33220.023723.228263.5986AID743222
arylsulfatase AHomo sapiens (human)Potency5.35821.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency10.00000.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency17.59940.00207.533739.8107AID891
cytochrome P450 2C9 precursorHomo sapiens (human)Potency10.00000.00636.904339.8107AID883
D(1A) dopamine receptorHomo sapiens (human)Potency0.18360.02245.944922.3872AID488982
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency35.48130.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency0.18890.006026.168889.1251AID488953
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency29.84930.000323.4451159.6830AID743065; AID743067
gemininHomo sapiens (human)Potency23.81180.004611.374133.4983AID463097; AID624296
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency25.57480.005612.367736.1254AID624032
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency11.89610.031610.279239.8107AID884; AID885
lethal factor (plasmid)Bacillus anthracis str. A2012Potency31.62280.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Cellular tumor antigen p53Homo sapiens (human)Potency29.84930.002319.595674.0614AID651631
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency10.00000.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency11.89611.000012.224831.6228AID885
[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)
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.17210.00010.807410.0000AID1195979; AID1306485; AID671634
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.11130.00020.725710.0000AID1195979; AID671635
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.09630.00030.483410.0000AID1195979; AID671636
Amine oxidase [flavin-containing] AHomo sapiens (human)Ki10.00000.00192.379710.0000AID91713
Amine oxidase [flavin-containing] BHomo sapiens (human)Ki10.00000.00061.777110.0000AID91713
Delta-type opioid receptorMus musculus (house mouse)Ki0.08310.00000.53939.4000AID1195978
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.08310.00000.27869.0000AID1195978
NischarinRattus norvegicus (Norway rat)Ki0.03560.00080.13881.2589AID1195978; AID1306516; AID671632
NischarinHomo sapiens (human)Ki0.06420.00420.21923.8019AID342861; AID91714
[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)
Alpha-2A adrenergic receptorHomo sapiens (human)EC50 (µMol)0.17780.00080.37336.7100AID1306486
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (192)

Processvia Protein(s)Taxonomy
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
biogenic amine metabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
positive regulation of signal transductionAmine oxidase [flavin-containing] AHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
response to xenobiotic stimulusAmine oxidase [flavin-containing] BHomo sapiens (human)
response to toxic substanceAmine oxidase [flavin-containing] BHomo sapiens (human)
response to aluminum ionAmine oxidase [flavin-containing] BHomo sapiens (human)
response to selenium ionAmine oxidase [flavin-containing] BHomo sapiens (human)
negative regulation of serotonin secretionAmine oxidase [flavin-containing] BHomo sapiens (human)
phenylethylamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
substantia nigra developmentAmine oxidase [flavin-containing] BHomo sapiens (human)
response to lipopolysaccharideAmine oxidase [flavin-containing] BHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to ethanolAmine oxidase [flavin-containing] BHomo sapiens (human)
positive regulation of dopamine metabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
hydrogen peroxide biosynthetic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to corticosteroneAmine oxidase [flavin-containing] BHomo sapiens (human)
apoptotic processNischarinHomo sapiens (human)
Rac protein signal transductionNischarinHomo sapiens (human)
actin cytoskeleton organizationNischarinHomo sapiens (human)
negative regulation of cell migrationNischarinHomo sapiens (human)
outer dynein arm assemblyNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (54)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
electron transfer activityAmine oxidase [flavin-containing] BHomo sapiens (human)
identical protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
integrin bindingNischarinHomo sapiens (human)
protein bindingNischarinHomo sapiens (human)
phosphatidylinositol bindingNischarinHomo sapiens (human)
identical protein bindingNischarinHomo sapiens (human)
dynein heavy chain bindingNischarinHomo sapiens (human)
alpha-tubulin bindingNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (40)

Processvia Protein(s)Taxonomy
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] AHomo sapiens (human)
cytosolAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial envelopeAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] BHomo sapiens (human)
dendriteAmine oxidase [flavin-containing] BHomo sapiens (human)
neuronal cell bodyAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
nucleoplasmNischarinHomo sapiens (human)
early endosomeNischarinHomo sapiens (human)
cytosolNischarinHomo sapiens (human)
plasma membraneNischarinHomo sapiens (human)
microtubule cytoskeletonNischarinHomo sapiens (human)
membraneNischarinHomo sapiens (human)
intracellular membrane-bounded organelleNischarinHomo sapiens (human)
intercellular bridgeNischarinHomo sapiens (human)
recycling endosomeNischarinHomo sapiens (human)
cytoplasmNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (87)

Assay IDTitleYearJournalArticle
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
AID350216Dissociation constant, pKa of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1306486Agonist activity at recombinant human alpha2A adrenoreceptor expressed in CHOK1 cell membrane incubated for 30 mins by [35S]GTPgammaS binding assay2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.
AID1306487Intrinsic activity at recombinant human alpha2A adrenoreceptor expressed in CHOK1 cell membrane incubated for 30 mins by [35S]GTPgammaS binding assay relative to adrenaline2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.
AID1306482Induction of apoptosis in human K562 cells assessed as early apoptotic cells at 50 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 5%)2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.
AID671636Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counter2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.
AID513634Induction of autophagy in rat stable inducible PC12 cells assessed as increase in LC3-2 level after 24 hrs by immunoblotting analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID35915Displacement of [3H]RX-821002 from alpha-2 adrenergic receptor of calf frontal cortex membranes2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of pyrrolinic isosteres of rilmenidine. Discovery of cis-/trans-dicyclopropylmethyl-(4,5-dimethyl-4,5-dihydro-3H-pyrrol-2-yl)-amine (LNP 509), an I1 imidazoline receptor selective ligand with hypotensive activity.
AID513639Induction of autophagy in human SK-N-MC cells expressing EGFP-HDQ74 and endogenously I1R/alpha2 AR assessed as decrease in EGFP-HDQ74 aggregation at 1 uM after 24 hrs by densitometric analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID671635Displacement of [3H]RX821001 from human alpha2B adrenoceptor expressed in CHO cells after 60 mins by gamma counter2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.
AID91713Displacement of [3H]idazoxan from I2 imidazoline binding sites (I2Bs) of rabbit renal cortex membranes2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of pyrrolinic isosteres of rilmenidine. Discovery of cis-/trans-dicyclopropylmethyl-(4,5-dimethyl-4,5-dihydro-3H-pyrrol-2-yl)-amine (LNP 509), an I1 imidazoline receptor selective ligand with hypotensive activity.
AID1195979Displacement of [3H]RX821002 from human alpha2 adrenoceptor expressed in CHO cell membranes after 60 mins2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.
AID35772Compound was evaluated for hypotensive activity mediated by Alpha-2 adrenergic receptor; no data2003Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
Synthesis and biological evaluation of new 2-(4,5-dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives.
AID1195980Selectivity ratio of Ki for I1 imidazoline receptor in rat PC12 cells to Ki for human alpha2 adrenoceptor expressed in CHO cell membranes2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1195978Displacement of [125I] PIC from I1 imidazoline receptor in rat PC12 cells after 45 mins by gamma counting2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.
AID350220Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 100% water as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1306503Potentiation of doxorubicin-induced apoptosis in human K562 cells assessed as early apoptotic cells at 50 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry relative to control2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.
AID350218Octanol-water partition coefficient, log PC of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1306516Displacement of [125I]PIC from Imidazoline-1 receptor in rat PC12 cell membrane incubated for 30 mins by gamma counting method2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.
AID1306485Displacement of [3H]RS-79948-197 from recombinant human alpha2A adrenoreceptor expressed in CHOK1 cell membrane by scintillation counting method2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.
AID671633Displacement of [3H]idazoxan from imidazoline I2 receptor in New Zealand rabbit renal cortex homogenate after 60 mins by gamma counter2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.
AID342860Displacement of [125I]PIC from human alpha2 adrenoceptors expressed in CHO cells2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID513637Induction of autophagy in rat stable inducible PC12 cells expressing EGFP-HDQ74 and endogenously I1R assessed as decrease in EGFP-HDQ74 aggregation at 1 uM after 24 hrs by densitometric analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID671632Displacement of [3H]paraiodoclonidine from imidazoline I1 receptor in rat PC12 cells after 30 mins by gamma counter2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.
AID513636Induction of autophagy in rat stable inducible PC12 cells expressing A53T alpha-synuclein and endogenously I1R assessed as increase in A53T alpha-synuclein clearance at 1 uM after 24 hrs by densitometric analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID342863Selectivity ratio of pKi for human imidazoline receptor 1 to pKi for human alpha2 adrenoceptors2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID342861Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID91714Displacement of [3H]clonidine from imidazoline receptor I-1 of bovine chromaffin cell membranes2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of pyrrolinic isosteres of rilmenidine. Discovery of cis-/trans-dicyclopropylmethyl-(4,5-dimethyl-4,5-dihydro-3H-pyrrol-2-yl)-amine (LNP 509), an I1 imidazoline receptor selective ligand with hypotensive activity.
AID513638Induction of autophagy in human SK-N-MC cells expressing A53T alpha-synuclein and endogenously I1R/alpha2 AR assessed as increase in A53T alpha-synuclein clearance at 1 uM after 24 hrs by densitometric analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID671634Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.
AID1306484Antiproliferative activity against human K562 cells assessed as inhibition of cell survival after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.
AID350219Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 95% acetonitrile as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
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.
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.
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.
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.
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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (375)

TimeframeStudies, This Drug (%)All Drugs %
pre-199061 (16.27)18.7374
1990's157 (41.87)18.2507
2000's105 (28.00)29.6817
2010's40 (10.67)24.3611
2020's12 (3.20)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 74.33

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 Index74.33 (24.57)
Research Supply Index6.12 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index129.96 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (74.33)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials61 (15.48%)5.53%
Reviews52 (13.20%)6.00%
Case Studies2 (0.51%)4.05%
Observational0 (0.00%)0.25%
Other279 (70.81%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Role of the Sympathetic Nerve System for the Pathogenesis and Progression of Chronic Kidney Failure [NCT00892892]Phase 40 participants (Actual)Interventional2009-11-30Withdrawn
[information is prepared from clinicaltrials.gov, extracted Sep-2024]