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bepridil

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Description

Bepridil: A long-acting calcium-blocking agent with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

bepridil : A tertiary amine in which the substituents on nitrogen are benzyl, phenyl and 3-(2-methylpropoxy)-2-(pyrrolidin-1-yl)propyl. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID2351
CHEMBL ID1008
CHEBI ID3061
SCHEMBL ID34412
MeSH IDM0024153

Synonyms (125)

Synonym
AC-16059
org 5730
beta-((2-methylpropoxy)methyl)-n-phenyl-n-(phenylmethyl)-1-pyrrolidineethanamine
1-pyrrolidineethanamine, beta-((2-methylpropoxy)methyl)-n-phenyl-n-(phenylmethyl)-
c24h34n2o
BRD-A91008255-001-02-8
n-[3-(2-methylpropoxy)-2-pyrrolidin-1-ylpropyl]-n-(phenylmethyl)aniline
gtpl2337
DIVK1C_000110
KBIO1_000110
bepadin
n-{3-[(2-methylpropyl)oxy]-2-pyrrolidin-1-ylpropyl}-n-(phenylmethyl)aniline
n-benzyl-n-[3-(2-methylpropoxy)-2-pyrrolidin-1-yl-propyl]aniline hydrochloride
SPECTRUM_001745
BSPBIO_002334
BIO2_000021
BIO1_001366
BIO1_000388
BIO2_000501
BIO1_000877
D07520
bepridil (inn)
bepadin (tn)
PRESTWICK2_000368
IDI1_000110
BSPBIO_000495
BPBIO1_000545
SPECTRUM5_000978
HSCI1_000377
PRESTWICK3_000368
LOPAC0_000222
AB00053643
bepridil
C06847
64706-54-3
DB01244
NCGC00162097-02
NCGC00162097-03
KBIO2_000021
KBIOGR_000021
KBIO2_007361
KBIOSS_000021
KBIO3_000042
KBIO2_002589
KBIO3_000041
KBIO2_005157
KBIO3_001554
KBIOSS_002225
KBIO2_002225
KBIO2_004793
KBIOGR_001274
PRESTWICK1_000368
SPECTRUM2_000901
SPBIO_000742
NINDS_000110
SPBIO_002416
PRESTWICK0_000368
SPECTRUM4_000797
SPECTRUM3_000747
BCBCMAP01_000130
BSPBIO_001301
IDI1_033771
NCGC00162097-04
NCGC00162097-01
HMS2089C05
HMS1989B03
NCGC00015155-07
CHEMBL1008
CHEBI:3061 ,
n-benzyl-n-[3-(2-methylpropoxy)-2-(pyrrolidin-1-yl)propyl]aniline
HMS1791B03
HMS1361B03
n-benzyl-n-[3-(2-methylpropoxy)-2-pyrrolidin-1-ylpropyl]aniline
NCGC00015155-03
dtxcid402663
tox21_110089
dtxsid3022663 ,
cas-64706-54-3
CCG-204317
AKOS015962267
NCGC00015155-02
NCGC00015155-08
NCGC00015155-05
NCGC00015155-04
NCGC00015155-06
n-benzyl-n-(3-isobutoxy-2-pyrrolidin-1-yl-propyl)aniline
1-pyrrolidineethanamine, .beta.-[(2-methylpropoxy)methyl]-n-phenyl-n-(phenylmethyl)-, monohydrochloride
755bo701ma ,
unii-755bo701ma
bepridil [inn:ban]
FT-0630749
NCGC00015155-13
SCHEMBL34412
NCGC00015155-11
tox21_110089_1
bepridil [vandf]
1-pyrrolideneethanamine, .beta.-((2-methylpropoxy)methyl)-n-phenyl-n-(phenylmethyl)-
1-(2-(n-benzylanilino)-1-(isobutoxymethyl)ethyl)-pyrrolidine
bepridil [mi]
bepridil [inn]
bepridil [who-dd]
AB00053643-14
bdbm78577
n-[3-(2-methylpropoxy)-2-pyrrolidin-1-yl-propyl]-n-(phenylmethyl)aniline;hydrochloride
benzyl-(3-isobutoxy-2-pyrrolidino-propyl)-phenyl-amine;hydrochloride
n-[3-(2-methylpropoxy)-2-(1-pyrrolidinyl)propyl]-n-(phenylmethyl)aniline;hydrochloride
cid_50088
UIEATEWHFDRYRU-UHFFFAOYSA-N
tox21 110089
bepridil hydrochloride monohydrate/bepridil
n-benzyl-n-(3-isobutoxy-2-(pyrrolidin-1-yl)propyl)aniline
AB00053643_15
Q4890934
BRD-A91008255-003-16-4
mfcd00868313
SDCCGSBI-0050210.P003
NCGC00015155-19
(+/-)-bepridil;org 5730; dl-bepridil
64706-54-3 (free base)
bepridil free base
()-bepridil;org 5730; dl-bepridil
864868-68-8
EN300-22786142
CS-0013008
HY-16952

Research Excerpts

Overview

Bepridil is an anti-arrhythmic agent with anti-electrical remodelling effects that target many cardiac ion channels, including the voltage-gated Na+ channel. It is a calcium antagonist with direct negative chronotropic, dromotropic, inotropic and vasodilatory actions.

ExcerptReferenceRelevance
"Bepridil is an effective antiarrhythmic drug on supraventricular and ventricular arrhythmias, and inhibitor of calmodulin. "( Short- and long-term inhibition of cardiac inward-rectifier potassium channel current by an antiarrhythmic drug bepridil.
Ma, F; Masuda, K; Morishima, M; Ono, K; Takanari, H, 2016
)
2.09
"Bepridil is an anti-arrhythmic agent with anti-electrical remodelling effects that target many cardiac ion channels, including the voltage-gated Na+ channel. "( Bepridil up-regulates cardiac Na+ channels as a long-term effect by blunting proteasome signals through inhibition of calmodulin activity.
Kaku, T; Kang, L; Morishima, M; Ono, K; Wang, Y; Zheng, MQ, 2009
)
3.24
"Bepridil is a drug that binds to troponin and increases calcium sensitivity of muscle contraction."( A computational and experimental approach to investigate bepridil binding with cardiac troponin.
Baxley, T; Chalovich, JM; Li, Y; Varughese, JF, 2011
)
1.34
"Bepridil is an investigational calcium antagonist that also has fast sodium channel blocking and antidysrhythmic properties. "( Cardiac electrophysiologic interactions of bepridil, a new calcium antagonist, with enflurane, halothane, and isoflurane.
Buben, JA; Hantler, CB; Knight, PR; Landau, SN; Larson, LO; Lucchesi, BR; Lynch, JJ, 1988
)
1.98
"Bepridil is a novel substance with antianginal and specific antiarrhythmic activities. "( The effect of Bepridil on respiratory and cardiovascular function: a placebo-controlled study.
Forche, G; Kopera, H; Marsoner, HJ, 1983
)
2.07
"Bepridil (Cordium) is a calcium channel blocker which has been demonstrated to be effective in the preventive treatment of angina. "( [Comparison of anti-ischemic effect of bepridil and diltiazem evaluated by exercise test in patients with coronary disease. A multicenter study. Groupe d'Investigateurs].
Quilliet, L; Sellier, P, 1997
)
2.01
"1. Bepridil (BPD) is a pharmacological compound able to bind to the Ca2+ sensor protein troponin C (TnC), which triggers skeletal muscle contraction upon Ca2+-binding. "( Differential effects of bepridil on functional properties of troponin C in slow and fast skeletal muscles.
Kischel, P; Mounier, Y; Stevens, L, 1999
)
1.23
"Bepridil is a calcium antagonist with direct negative chronotropic, dromotropic, inotropic and vasodilatory actions which reduces myocardial oxygen consumption and increases coronary blood flow, leading to a significant anti-ischaemic and antianginal effect in the absence of reflex tachycardia. "( Bepridil. A review of its pharmacological properties and therapeutic use in stable angina pectoris.
Faulds, D; Fitton, A; Hollingshead, LM, 1992
)
3.17
"Bepridil is an antianginal agent with multiple therapeutic actions. "( Pharmacology of bepridil.
Brannan, MD; Damiano, BP; Flaim, SF; Gill, A; Sit, SP, 1992
)
2.07
"Bepridil is a unique calcium antagonist with a broad pharmacologic profile and demonstrated efficacy as an antianginal agent. "( Safety profile of bepridil determined from clinical trials in chronic stable angina in the United States.
Singh, BN, 1992
)
2.06
"Bepridil is a calcium antagonist with a unique chemical structure and properties that differ from other calcium antagonists (e.g., a long half-life, sodium channel inhibition). "( Hemodynamic effects of bepridil in patients with coronary artery disease.
Narahara, KA, 1992
)
2.04
"Bepridil is a calcium antagonist with a unique chemical composition and a long elimination half-life (42 hours). "( Bepridil hydrochloride compared with placebo in patients with stable angina pectoris.
Corday, SR; Hossack, KF; Karliner, JS; Narahara, KA; Singh, BN, 1992
)
3.17
"Bepridil is a calcium antagonist with a unique electrophysiologic profile, a long elimination half-life, and demonstrated efficacy as an antianginal agent in the setting of chronic stable angina. "( Bepridil therapy: guidelines for patient selection and monitoring of therapy.
Singh, BN, 1992
)
3.17
"Bepridil is a calcium antagonist that prolongs the duration of ventricular repolarization, whereas CERM 4205, another calcium antagonist, seems to be devoid of any effect on QT interval. "( Effects of bepridil and CERM 4205 (ORG 30701) on the relation between cardiac cycle length and QT duration in healthy volunteers.
Boisson, P; Fleurot, O; Jaillon, P; Lecocq, B; Lecocq, V; Prost, PL, 1990
)
2.11
"Bepridil is an anti-anginal agent with a novel chemical structure. "( Bepridil: a review of its pharmacology and clinical efficacy as an anti-anginal agent with anti-arrhythmic properties.
Alpert, JS; Coumel, P; Greeff, K; Krikler, DM; Remme, WJ; Schönbaum, E; Verduyn, CW, 1985
)
3.15
"Bepridil is an antianginal-antiarrhythmic agent with vasodilator and direct cardiac inotropic effects."( Bepridil and valproate retard Na+ reactivation in Myxicola.
Schauf, CL, 1987
)
2.44
"Bepridil is an effective antianginal drug, but, because of its proarrhythmic potential, it should probably not be used as a first-line agent."( Nicardipine, nitrendipine, and bepridil: new calcium antagonists for cardiovascular disorders.
Hasegawa, GR, 1988
)
1.28
"Bepridil hydrochloride is a unique calcium channel-blocking drug with anti-ischemic and type 1 antiarrhythmic properties. "( Comparison of bepridil with nadolol for angina pectoris.
Humen, DP; Jablonsky, G; Kostuk, WJ; O'Brien, PA; Pflugfelder, PW; Purves, PD, 1987
)
2.08
"Bepridil is an investigational calcium channel blocking agent with antianginal activity that has a distinct and complex pharmacologic profile. "( Bepridil: a new long-acting calcium channel blocking agent.
Spinler, SA; Zeller, FP, 1987
)
3.16
"Bepridil hydrochloride is a relatively new calcium antagonist which appears to have a complex pharmacologic profile, but its concentration-response characteristics with respect to its electrophysiologic properties of varying concentrations (0.1 to 10.0 micrograms/ml) of the drug were therefore determined in rabbit and canine myocardial fiber preparations in vitro by standard microelectrode techniques. "( Effects of bepridil on the electrophysiologic properties of isolated canine and rabbit myocardial fibers.
Kato, R; Singh, BN, 1986
)
2.1
"Bepridil is a molecule which, apart from its anti-anginal properties, also has antiarrhythmic effects due to its calcium antagonist action which depresses antero and retrograde AV conduction in the physiological pathways. "( [Treatment of supraventricular and paroxysmal ventricular tachycardia with bepridil].
Bonnet, P; Cosnay, P; Fauchier, JP; Néel, C; Quilliet, L; Rouesnel, P, 1985
)
1.94

Effects

Bepridil has complex pharmacokinetic (PK) properties with large interindividual differences in plasma concentrations. It has been used as an antiarrhythmic drug with multiple pharmacological effects. Whether it is effective for mechanically induced arrhythmia has not been well investigated.

ExcerptReferenceRelevance
"Bepridil has a broader spectrum of activity and also acts at the atrial and ventricular levels."( Electrophysiological effects of bepridil and its quaternary derivative CERM 11888 in closed chest anaesthetized dogs: a comparison with verapamil and diltiazem.
Lamar, JC; Leboeuf, J; Massingham, R; Ponsonnaille, J, 1989
)
1.28
"Bepridil has complex pharmacokinetic (PK) properties with large interindividual differences in plasma concentrations."( Contributing factors to the apparent clearance of bepridil in patients with paroxysmal or persistent atrial fibrillation: analysis using population pharmacokinetics.
Hagiwara, N; Hashiguchi, M; Naganuma, M; Shiga, T; Suzuki, A, 2013
)
1.36
"Bepridil has been used as an antiarrhythmic drug with multiple pharmacological effects; however, whether it is effective for mechanically induced arrhythmia has not been well investigated."( Effects of bepridil on stretch-activated BKca channels and stretch-induced extrasystoles in isolated chick hearts.
Iribe, G; Jin, H; Naruse, K, 2017
)
1.57
"Bepridil has multiple ion-channel blocking effects similar to amiodarone and is expected to have anti-arrhythmic effects that are useful for the management of atrial fibrillation (AF). "( Conversion and maintenance of sinus rhythm by bepridil in patients with persistent atrial fibrillation.
Daida, H; Iida, Y; Kawano, Y; Mineda, Y; Nakata, Y; Nakazato, K; Nakazato, Y; Sasaki, A; Sumiyoshi, M; Tokano, T; Yasuda, M, 2005
)
2.03
"Bepridil has multiple ion-channel blocking effects and is expected to be useful for managing atrial fibrillation (AF). "( Efficacy and safety of the additional bepridil treatment in patients with atrial fibrillation refractory to class I antiarrhythmic drugs.
Fukushima Kusano, K; Hashimoto, T; Hiramatsu, S; Kaseno, K; Miyaji, K; Naito, S; Nakamura, K; Ohe, T; Oshima, S; Tada, H; Tadokoro, K; Taniguchi, K, 2007
)
2.05
"Bepridil has Ca2+-antagonistic (or Ca2+ entry blocking or slow channel blocking) properties much like verapamil, but it is somewhat less potent than verapamil in this action (i.e., complete blockade occurred at 10(-5) M bepridil vs."( Bepridil blockade of Ca2+-dependent action potentials in vascular smooth muscle of dog coronary artery.
Harder, DR; Sperelakis, N,
)
2.3
"Bepridil has been used only rarely in unstable angina since its long half-life could imply a delayed action. "( [Comparative study of the efficacy and tolerability of bepridil and diltiazem in unstable angina. 277 patients].
Bory, M; Quilliet, L, 1994
)
1.98
"Bepridil has been observed to prolong the QT interval in the majority of patients in whom it is used for treatment of angina."( Effects of bepridil on cardiac electrophysiologic properties.
Prystowsky, EN, 1992
)
1.39
"Bepridil has a broader spectrum of activity and also acts at the atrial and ventricular levels."( Electrophysiological effects of bepridil and its quaternary derivative CERM 11888 in closed chest anaesthetized dogs: a comparison with verapamil and diltiazem.
Lamar, JC; Leboeuf, J; Massingham, R; Ponsonnaille, J, 1989
)
1.28
"Bepridil has vascular, sinoatrial and atrioventricular nodal, and myocardial effects qualitatively similar to those of the calcium antagonist verapamil; it also interferes with the fast sodium channel and prolongs refractoriness in atrial and ventricular tissue."( Nicardipine, nitrendipine, and bepridil: new calcium antagonists for cardiovascular disorders.
Hasegawa, GR, 1988
)
1.28
"Bepridil has both slow channel blocking properties and fast channel blocking effects and thus possesses an antiarrhythmic effect beyond the prolongation of repolarization."( Calcium channel blockers that prolong the QT interval.
Somberg, JC, 1985
)
0.99
"Bepridil has been shown to block both slow- and fast-channel activity in the heart. "( Electrophysiologic and antiarrhythmic properties of bepridil.
Prystowsky, EN, 1985
)
1.96

Actions

Bepridil was shown to increase the sensitivity of cTnC for Ca(2+) under all reconstitution conditions, sensitization by the other drugs was context dependent. At a lower concentration of 1 μM had no effect on the proteasome activity in vitro.

ExcerptReferenceRelevance
"Bepridil was shown to increase the sensitivity of cTnC for Ca(2+) under all reconstitution conditions, sensitization by the other drugs was context dependent."( Fluorescence Based Characterization of Calcium Sensitizer Action on the Troponin Complex.
Dong, W; Hu, D; Li, KL; Schlecht, W, 2016
)
1.16
"Bepridil at a lower concentration of 1 μM had no effect on the proteasome activity in vitro."( Stabilization of Kv1.5 channel protein by bepridil through its action as a chemical chaperone.
Hasegawa, A; Higaki, K; Hisatome, I; Ikeda, N; Kato, M; Kurata, Y; Li, P; Miake, J; Ninomiya, H; Notsu, T; Sakata, S; Shiota, G; Shirayoshi, Y; Suzuki, S; Yamamoto, K; Yoshida, A, 2012
)
1.36
"Bepridil inhibit IKr, IKs and IK1 in hypertrophied guinea pig ventricular myocytes, which may be important in understanding the antiarrhythmic effects of this drug."( [Bepridil inhibition on the delayed rectifier K+ currents in thyroxine induced hypertrophied guinea pig ventricular myocytes].
Dai, DZ; Hao, XM; Ma, YP; Wu, CH; Zhang, GQ; Zhou, PA, 2001
)
2.66
"Bepridil did not inhibit intracellular hemoglobin S polymerization even at 200 microM, as shown by oxygen scan ektacytometry."( Bepridil as an antisickling agent: membrane internalization and cell rigidity.
Acquaye, C; Féo, C; Johnson, RM; Sarnaik, S, 1994
)
2.45

Treatment

Bepridil treatment did not significantly affect heme oxygenase-1- or NAD(P)H quinone oxidoreductase- 1-mediated oxidative stress or inflammatory responses in the ipsilateral thalamus of MCAO rats. Treatment with bepridil (10-20 microM) for 30 min increased the production of reactive oxygen intermediates by 50%.

ExcerptReferenceRelevance
"Bepridil treatment did not significantly affect heme oxygenase-1- or NAD(P)H quinone oxidoreductase-1-mediated oxidative stress or inflammatory responses in the ipsilateral thalamus of MCAO rats."( Bepridil decreases Aβ and calcium levels in the thalamus after middle cerebral artery occlusion in rats.
Haapasalo, A; Hiltunen, M; Jolkkonen, J; Lipsanen, A; Mäkinen, P; Peräniemi, S; Sarajärvi, T; Soininen, H, 2012
)
2.54
"Treatment with bepridil prevented recurrence of VF along with improvement of ST elevation and LAS40 in patients with Brugada syndrome with the SCN5A mutation."( Efficacy of low-dose bepridil for prevention of ventricular fibrillation in patients with Brugada syndrome with and without SCN5A mutation.
Hata, Y; Ito, H; Kohno, K; Kusano, KF; Miura, D; Morita, H; Murakami, M; Nagase, S; Nakagawa, K; Nakamura, K; Nishii, N; Ohe, T; Tada, T; Tanaka, M; Toh, N, 2010
)
1.02
"Pretreatment with bepridil for 5 min before ischemia improved the recovery of developed tension measured after 60 min of reperfusion."( Bepridil, an antiarrhythmic drug, opens mitochondrial KATP channels, blocks sarcolemmal KATP channels, and confers cardioprotection.
Costa, AD; Garlid, KD; Ishida, H; Nakaya, H; Ogura, T; Saito, T; Sato, T, 2006
)
2.1
"Treatment with bepridil (10-20 microM) for 30 min increased the production of reactive oxygen intermediates (ROI) by more than 50%."( Effect of the antianginal drug bepridil on intracellular Ca2+ release and extracellular Ca2+ influx in human neutrophils.
Chen, LW; Jan, CR, 2001
)
0.94
"Treatment with bepridil before and during ischemia did not improve recovery of cardiac function, tissue energy reserves, or mitochondrial function upon reperfusion with control buffer."( Comparison of the effects of bepridil and diltiazem upon globally ischemic rat hearts.
Harwell, T; Maiorano, P; Watts, J, 1987
)
0.9

Toxicity

The addition of bepridil to class I AADs is effective and safe for AF, but careful observation using periodic ECG recordings is essential for avoiding torsades de pointes caused by QT prolongation. Bepridil is effective for terminating long-lasting persistent AF.

ExcerptReferenceRelevance
" The most frequent adverse reactions were of gastrointestinal or neurologic origin."( Safety profile of bepridil determined from clinical trials in chronic stable angina in the United States.
Singh, BN, 1992
)
0.62
" The 9-year French experience suggests that bepridil is a safe and effective agent for treatment of angina pectoris in properly selected patients."( Safety of bepridil: from review of the European data.
Coumel, P, 1992
)
0.95
" The most frequent adverse effects in both groups were nausea, asthenia, dizziness, headache and diarrhea."( Comparative efficacy and safety of bepridil and diltiazem in chronic stable angina pectoris refractory to diltiazem. The Bepridil Collaborative Study Group.
Singh, BN, 1991
)
0.56
" The presence of substituents in different positions on the N-phenyl moiety increased liver toxicity; ortho-substituted analogs were more toxic than para- or meta-substituted ones."( Comparative study of the biotransformation of bepridil analogs in isolated liver cells from one rat. Relationships between structure and in vitro liver toxicity.
Busch, N; Chabard, JL; Damatte, E; Galmier, MJ; Lartigue-Mattei, C; Pognat, JF,
)
0.39
" The results suggested that the 50% ethanolic extract was safe in genotoxicity."( Antioxidative activity and safety of the 50 ethanolic extract from red bean fermented by Bacillus subtilis IMR-NK1.
Chang, CT; Chao, WW; Chou, ST; Chung, YC; Lin, CF, 2002
)
0.31
" Bepridil is effective and safe for terminating long-lasting persistent AF."( Usefulness and safety of bepridil in converting persistent atrial fibrillation to sinus rhythm.
Fujiki, A; Inoue, H; Mizumaki, K; Sugao, M; Tsuneda, T, 2003
)
1.53
" The most toxic compounds, the second one, characterized by the smallest variations of TEER, included verapamil and diltiazem."( Influence of different calcic antagonists on the Caco-2 cell monolayer integrity or "TEER, a measurement of toxicity?".
Galmier, MJ; Lartigue, C; Mathieu, F; Pognat, JF,
)
0.13
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" However, serious adverse effects, including torsade de pointes (Tdp), have been reported."( Clinical evaluation of adverse effects during bepridil administration for atrial fibrillation and flutter.
Daida, H; Kawano, Y; Nakazato, K; Nakazato, Y; Sasaki, A; Tokano, T; Yasuda, M, 2006
)
0.59
" Adverse effects were observed in 19 patients (4%) during an average follow-up of 20 months."( Clinical evaluation of adverse effects during bepridil administration for atrial fibrillation and flutter.
Daida, H; Kawano, Y; Nakazato, K; Nakazato, Y; Sasaki, A; Tokano, T; Yasuda, M, 2006
)
0.59
"The addition of bepridil to class I AADs is effective and safe for AF, but careful observation using periodic ECG recordings is essential for avoiding torsades de pointes caused by QT prolongation."( Efficacy and safety of the additional bepridil treatment in patients with atrial fibrillation refractory to class I antiarrhythmic drugs.
Fukushima Kusano, K; Hashimoto, T; Hiramatsu, S; Kaseno, K; Miyaji, K; Naito, S; Nakamura, K; Ohe, T; Oshima, S; Tada, H; Tadokoro, K; Taniguchi, K, 2007
)
0.96

Pharmacokinetics

The influence of bepridil on steady-state serum digoxin concentrations (SDCs) and the pharmacodynamic actions of both drugs were tested in 48 healthy subjects. Bepridil has complex pharmacokinetic (PK) properties with large interindividual differences in plasma concentrations.

ExcerptReferenceRelevance
"The influence of bepridil on steady-state serum digoxin concentrations (SDCs) and the pharmacodynamic actions of both drugs were tested in 48 healthy subjects in a randomized, double-blind study."( Digoxin and bepridil: pharmacokinetic and pharmacodynamic interactions.
Belz, GG; Matthews, JH; Wistuba, S, 1986
)
0.99
" The harmonic mean elimination half-life from model-independent analysis was 14."( Pharmacokinetics of intravenous bepridil in patients with coronary disease.
Alpert, JS; Benotti, JR; Brady, PM; Lesko, LJ; McCue, JE; Ockene, IS; Weiner, BH, 1986
)
0.55
"Bepridil hydrochloride differs from the other calcium antagonists in structure as well as in several clinical pharmacokinetic characteristics."( Pharmacokinetics and metabolism of bepridil.
Benet, LZ, 1985
)
1.99
" Bepridil has complex pharmacokinetic (PK) properties with large interindividual differences in plasma concentrations."( Contributing factors to the apparent clearance of bepridil in patients with paroxysmal or persistent atrial fibrillation: analysis using population pharmacokinetics.
Hagiwara, N; Hashiguchi, M; Naganuma, M; Shiga, T; Suzuki, A, 2013
)
1.55

Compound-Compound Interactions

Bepridil alone or in combination with aprindine converted long lasting persistent AF in association with an increase in both FCL and FOI. 14 patients with progressive advanced cancer, resistant to doxorubsicin or epirubicin, were treated with the same anthracycline in conjunction with bepridil.

ExcerptReferenceRelevance
" 14 patients with progressive advanced cancer, resistant to doxorubicin or epirubicin, were treated with the same anthracycline in combination with bepridil."( Bepridil in combination with anthracyclines to reverse anthracycline resistance in cancer patients.
Blokhuis, WM; de Jong, J; Giaccone, G; Maessen, PA; Pinedo, HM; Schuurhuis, GJ; van der Hoeven, JJ; van der Vijgh, WJ; van Kalken, CK, 1991
)
1.92
"The effects of bepridil (Bep) in combination with anisodamine (Ani) on myocardial ischemia and reperfusion injury induced by ligating the left coronary artery were studied in rats."( [Protective effects of bepridil in combination with anisodamine on myocardial ischemia and reperfusion injury in rats].
Chen, JM; Cui, JY; Dong, HY; Gu, SL; Peng, ZY; Zhou, J, 1995
)
0.95
" Bepridil alone or in combination with aprindine is effective for termination of persistent AF."( Maintenance of sinus rhythm and recovery of atrial mechanical function after cardioversion with bepridil or in combination with aprindine in long-lasting persistent atrial fibrillation.
Fujiki, A; Hirai, T; Inoue, H; Mizumaki, K; Nakagawa, K; Sakabe, M; Tsuneda, T, 2004
)
1.45
" In Group I, sinus rhythm was pharmacologically restored in 22 patients after an average 30 days (7-49 days) of bepridil administration, either alone (11) or in combination with oral aprindine (11); they were followed up while using the same drugs."( Maintenance of sinus rhythm and recovery of atrial mechanical function after cardioversion with bepridil or in combination with aprindine in long-lasting persistent atrial fibrillation.
Fujiki, A; Hirai, T; Inoue, H; Mizumaki, K; Nakagawa, K; Sakabe, M; Tsuneda, T, 2004
)
0.75
"In patients with long-lasting AF, pharmacological conversion with bepridil alone or in combination with aprindine recovered atrial mechanical function better and maintained sinus rhythm longer than electrical conversion."( Maintenance of sinus rhythm and recovery of atrial mechanical function after cardioversion with bepridil or in combination with aprindine in long-lasting persistent atrial fibrillation.
Fujiki, A; Hirai, T; Inoue, H; Mizumaki, K; Nakagawa, K; Sakabe, M; Tsuneda, T, 2004
)
0.78
"Bepridil alone or in combination with aprindine converted long lasting persistent AF in association with an increase in both FCL and FOI."( Drug-induced changes in fibrillation cycle length and organization index can predict chemical cardioversion of long-lasting atrial fibrillation with bepridil alone or in combination with aprindine.
Fujiki, A; Inoue, H; Iwamoto, J; Mizumaki, K; Nishida, K; Sakabe, M; Sugao, M; Tsuneda, T, 2004
)
1.97

Bioavailability

ExcerptReferenceRelevance
" Nicardipine and nitrendipine undergo extensive first-pass hepatic extraction after oral administration; oral bioavailability of bepridil is about 60%."( Nicardipine, nitrendipine, and bepridil: new calcium antagonists for cardiovascular disorders.
Hasegawa, GR, 1988
)
0.77
" The drug is completely absorbed from the gastrointestinal tract, but first-pass extraction reduces oral bioavailability to approximately 60%."( Pharmacokinetics and metabolism of bepridil.
Benet, LZ, 1985
)
0.55
" These products are well absorbed from the gastrointestinal tract but undergo variable degrees of transformation during the first passage through the liver."( [Clinical pharmacology of calcium inhibitors].
Martre, H; Singlas, E; Taburet, AM, 1985
)
0.27
"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 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

At the highest recommended oral dosage (400 mg/day), bepridil decreases resting heart rate and blood pressure. maximal exercise double product is not significantly reduced. Dose-response studies showed that thyroid hormone stimulation of Ca2+-ATPase activity in vitro was significantly inhibited by as little as 2 x 10(-5) M bePridil and cetiedil.

ExcerptRelevanceReference
" At the highest recommended oral dosage (400 mg/day), bepridil decreases resting heart rate and blood pressure; maximal exercise double product is not significantly reduced."( Hemodynamic effects of bepridil in patients with coronary artery disease.
Narahara, KA, 1992
)
0.84
" It was concluded that bepridil, at a mean maintenance dosage of 324 mg/day, was at least as effective as propranolol in improving exercise tolerance--specifically time to angina and total work--and that tolerability of the 2 drugs was comparable."( Comparative efficacy and concomitant use of bepridil and beta blockers in the management of angina pectoris.
Frishman, WH, 1992
)
0.86
") infusion of either BP at three dosage levels (3."( Effects of bepridil hydrochloride on cardiocirculatory dynamics, coronary vascular resistance, and cardiac output distribution in normal, conscious rats.
Flaim, SF; Mathiasen, JR; Stranieri, MT, 1988
)
0.66
"9 hours) were randomly assigned to two treatment groups: The first one was treated with bepridil (BEP, n = 100), and the second one was considered as a control group, using isosorbide dinitrate at a low dosage (ISDN, n = 100)."( Myocardial infarction: is bepridil, a new calcium antagonist, able to improve the course of the acute phase?
Chassing, A; Cosson, G; Flammang, D; Paillet, R; Pruvot, C; Waynberger, M, 1989
)
0.8
" Serious adverse reactions necessitate a change in antiarrhythmic therapy, as opposed to lowering drug dosage to an ineffective level."( Antiarrhythmic drug therapy. Recent advances and current status.
Somberg, J, 1985
)
0.27
" Dose-response studies showed that thyroid hormone stimulation of Ca2+-ATPase activity in vitro was significantly inhibited by as little as 2 x 10(-5) M bepridil and cetiedil."( Bepridil and cetiedil reversibly inhibit thyroid hormone stimulation in vitro of human red cell Ca2+-ATPase activity.
Blas, SD; Davis, FB; Davis, PJ; Dube, MP, 1987
)
1.91
" Since nicardipine, nitrendipine, and nifedipine are similar in efficacy and safety, the eventual availability of sustained-release dosage forms may determine how these drugs are ultimately used."( Nicardipine, nitrendipine, and bepridil: new calcium antagonists for cardiovascular disorders.
Hasegawa, GR, 1988
)
0.56
" After 2 weeks of single-blind placebo therapy and a 12-week parallel placebo-controlled, dose-response study, each patient received open-label bepridil."( Long-term bepridil monotherapy for angina pectoris.
Prasad, R; Sharma, MK; Teague, SM; Thadani, U; Voyles, W, 1988
)
0.88
" It is unclear whether bepridil will be used as a first-line agent in the treatment of chronic stable angina pectoris; however, its long half-life, which makes once daily dosing possible, is certainly a significant advantage."( Bepridil: a new long-acting calcium channel blocking agent.
Spinler, SA; Zeller, FP, 1987
)
2.03
" After two runs with comparable regional contractile dysfunction bepridil was infused intravenously at a dosage of 2 mg/kg per 5 min."( Bepridil abolishes exercise-induced regional contractile dysfunction in dogs.
Krumpl, G; Mayer, N; Raberger, G; Schneider, W, 1986
)
1.95
" Patients entering the study were receiving an average propranolol dosage of 131 mg/day (range 20 to 240)."( Combination propranolol and bepridil therapy in stable angina pectoris.
Charlap, S; Crawford, MH; DiBianco, R; Farnham, DJ; Frishman, WH; Kostis, JB; Michelson, EL; Michie, DD; Sawin, HS; Zellner, SR, 1985
)
0.56
" Dosage for the bepridil group was constantly maintained for each patient at a level observed to be clinically effective."( Long-term efficacy of bepridil in patients with chronic stable angina pectoris: results of a multicenter, placebo-controlled study of extended bepridil use.
Alpert, JS; Chesler, E; DiBianco, R; Katz, RJ; Spann, JF, 1985
)
0.93
" The patients were divided into 3 groups according to the arrhythmias observed and the dosage used."( [Efficacy of oral bepridil in ventricular arrhythmias in stable coronary insufficiency].
Brechenmacher, C; Deroubaix, G; Dupont, T; Moulinie, E; Pasco, A; Pellet, J; Rio, A; Rossignol, B, 1985
)
0.6
" The influence of bepridil on the dose-response curves of mesenteric arterial strips for CaCl2, norepinephrine and serotonin differed from the influence seen with nifedipine, another Ca++ blocker."( Effects on calmodulin of bepridil, an antianginal agent.
Hidaka, H; Ishikawa, T; Itoh, H, 1984
)
0.9
" If side effects intervene that may cause continued therapy to be intolerable, changing the antiarrhythmic agent, as opposed to decreasing the dosage to an ineffective range, may be appropriate."( New directions in antiarrhythmic drug therapy.
Somberg, JC, 1984
)
0.27
" Dose-response curves for the physiological effects of the drugs are observed over the same range of concentrations as their inhibition of [3H]nitrendipine binding to its receptor."( Activation of the voltage-dependent Ca2+ channel in rat heart cells by dihydropyridine derivatives.
Lazdunski, M; Méaux, JP; Renaud, JF; Romey, G; Schmid, A, 1984
)
0.27
"Bepridil, a new anti-anginal drug, was given in a daily dosage of 400 to 600 mg to twenty patients with unstable angina pectoris."( [A clinical trial of the effectiveness and tolerance of bepridil in unstable angina pectoris].
Amat, G; Boch, C; Colonna, D; Curnier, JM, 1982
)
1.95
" It is therefore concluded that continuous control of water intake and analysis of the stability of the drug is essential for the establishment of proper dose-response relationships."( Drinking water and drug dosage in rat studies.
Jakobsen, P; Jespersen, LT; Mikkelsen, EO; Pedersen, OL, 1983
)
0.27
"The relaxant effects of five organic calcium antagonists (nicardipine, diltiazem, PY 108068, verapamil and bepridil) on guinea-pig isolated trachea were tested against contractions induced by acetylcholine, histamine, 5-hydroxytryptamine, potassium chloride (KCl) and tetraethylammonium (TEA) in a medium containing the normal amount of calcium and against calcium dose-response curves in a calcium-free, potassium-enriched medium."( Effects of five different organic calcium antagonists on guinea-pig isolated trachea.
Advenier, C; Cerrina, J; Duroux, P; Floch, A; Renier, A, 1984
)
0.48
" Thus, no dosage adjustment will be required for ESRD patients and those receiving hemodialysis with cuprophane filters."( Pharmacokinetics of bepridil and two of its metabolites in patients with end-stage renal disease.
Awni, WM; Desiraju, RK; Halstenson, CE; Matzke, GR; Minn, FL; Nayak, RK; Opsahl, JA, 1995
)
0.61
"A multicenter, randomized, placebo-controlled, double-blind trial was conducted with patients with persistent atrial fibrillation (AF) to determine the dose-response effects and safety of bepridil, using every-day transtelephonic monitorings."( Dose-response effects of bepridil in patients with persistent atrial fibrillation monitored with transtelephonic electrocardiograms: a multicenter, randomized, placebo-controlled,double-blind study (J-BAF Study).
Aizawa, Y; Atarashi, H; Fujiki, A; Inoue, H; Ito, M; Katoh, T; Kobayashi, Y; Koretsune, Y; Kumagai, K; Niwano, S; Ogawa, S; Okazaki, O; Okumura, K; Origasa, H; Saku, K; Sato, T; Tanabe, T; Yamashita, T, 2009
)
0.85
"0% in those who received 200 mg/day, thus demonstrating a linear dose-response relationship for AF conversion."( Dose-response effects of bepridil in patients with persistent atrial fibrillation monitored with transtelephonic electrocardiograms: a multicenter, randomized, placebo-controlled,double-blind study (J-BAF Study).
Aizawa, Y; Atarashi, H; Fujiki, A; Inoue, H; Ito, M; Katoh, T; Kobayashi, Y; Koretsune, Y; Kumagai, K; Niwano, S; Ogawa, S; Okazaki, O; Okumura, K; Origasa, H; Saku, K; Sato, T; Tanabe, T; Yamashita, T, 2009
)
0.66
" These samples were collected just before each dosage of bepridil."( An LC method for quantifying bepridil in human plasma using 1-naphthol as the internal standard.
Goto, Y; Itoh, K; Iwai, S; Katoh, N; Kobayashi, M; Kuronuma, H; Narayama, Y; Noda, K; Tadano, K, 2011
)
0.91
" When comparing these responders and nonresponders, clinical background characteristics other than the dosage of bepridil did not show any difference and neither did temporal changes in QT parameters and heart rate."( Repetitive evaluation of fibrillation cycle length predicts the efficacy of bepridil for interruption of long-lasting persistent atrial fibrillation.
Aoyama, Y; Fukumoto, K; Ishikawa, S; Izumi, T; Kishihara, J; Murakami, M; Niwano, H; Niwano, S; Satoh, A; Ueno, K, 2011
)
0.81
" We investigated the relationship between plasma concentrations of bepridil just before dosing (Cbep) and its clinical efficacy in Japanese patients (n=36) with AF."( The relationship between the plasma concentration of bepridil and its efficacy in the treatment of atrial fibrillation in Japanese patients.
Gotoh, Y; Iwai, S; Katoh, N; Kobayashi, M; Narayama, Y; Noda, K; Tadano, K; Tanioka, S, 2012
)
0.86
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
vasodilator agentA drug used to cause dilation of the blood vessels.
anti-arrhythmia drugA drug used for the treatment or prevention of cardiac arrhythmias. Anti-arrhythmia drugs may affect the polarisation-repolarisation phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibres.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
calcium channel blockerOne of a class of drugs that acts by selective inhibition of calcium influx through cell membranes or on the release and binding of calcium in intracellular pools.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
tertiary amineA compound formally derived from ammonia by replacing three hydrogen atoms by hydrocarbyl groups.
pyrrolidinesAny of a class of heterocyclic amines having a saturated five-membered ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (74)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency34.67130.002541.796015,848.9004AID1347398
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency26.08203.189029.884159.4836AID1224846; AID1224894
RAR-related orphan receptor gammaMus musculus (house mouse)Potency24.65590.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency5.12980.173734.304761.8120AID1346859; AID1346924
ATAD5 protein, partialHomo sapiens (human)Potency29.08100.004110.890331.5287AID493107
Fumarate hydrataseHomo sapiens (human)Potency22.38720.00308.794948.0869AID1347053
GLS proteinHomo sapiens (human)Potency8.18200.35487.935539.8107AID624146; AID624170
PPM1D proteinHomo sapiens (human)Potency29.41070.00529.466132.9993AID1347411
SMAD family member 3Homo sapiens (human)Potency5.12980.173734.304761.8120AID1346859; AID1346924
TDP1 proteinHomo sapiens (human)Potency8.10630.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency18.39770.000714.592883.7951AID1259369; AID1259392
Microtubule-associated protein tauHomo sapiens (human)Potency39.81070.180013.557439.8107AID1460
AR proteinHomo sapiens (human)Potency26.35950.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743042; AID743063
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency33.49150.013326.981070.7614AID1346978
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency32.09060.000657.913322,387.1992AID1259377; AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency24.48560.001022.650876.6163AID1224838; AID1224839; AID1224893
progesterone receptorHomo sapiens (human)Potency31.67040.000417.946075.1148AID1346784; AID1346795
regulator of G-protein signaling 4Homo sapiens (human)Potency8.43680.531815.435837.6858AID504845
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency9.77170.01237.983543.2770AID1645841
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency17.47520.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency26.83250.000817.505159.3239AID1159527
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency23.87420.001530.607315,848.9004AID1224841; AID1224848; AID1224849; AID1259401; AID1259403
pregnane X nuclear receptorHomo sapiens (human)Potency5.30800.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency27.68470.000229.305416,493.5996AID1259244; AID1259248; AID743069; AID743078
GVesicular stomatitis virusPotency27.54040.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency0.03470.00108.379861.1304AID1645840
polyproteinZika virusPotency22.38720.00308.794948.0869AID1347053
67.9K proteinVaccinia virusPotency17.78280.00018.4406100.0000AID720580
glucocerebrosidaseHomo sapiens (human)Potency39.81070.01268.156944.6684AID2101
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency26.83250.023723.228263.5986AID743223
arylsulfatase AHomo sapiens (human)Potency37.93301.069113.955137.9330AID720538
caspase-3Homo sapiens (human)Potency33.49150.013326.981070.7614AID1346978
IDH1Homo sapiens (human)Potency12.58930.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency20.81140.035520.977089.1251AID504332; AID588346
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency13.33320.001723.839378.1014AID743083
activating transcription factor 6Homo sapiens (human)Potency26.83250.143427.612159.8106AID1159516
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency12.49100.057821.109761.2679AID1159526; AID1159528
Histone H2A.xCricetulus griseus (Chinese hamster)Potency49.19400.039147.5451146.8240AID1224845; AID1224896
Caspase-7Cricetulus griseus (Chinese hamster)Potency33.49150.006723.496068.5896AID1346980
chromobox protein homolog 1Homo sapiens (human)Potency6.70160.006026.168889.1251AID488953
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency0.39810.01789.637444.6684AID588834
caspase-3Cricetulus griseus (Chinese hamster)Potency33.49150.006723.496068.5896AID1346980
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency10.01500.000323.4451159.6830AID743065; AID743067
heat shock protein beta-1Homo sapiens (human)Potency29.84700.042027.378961.6448AID743210
huntingtin isoform 2Homo sapiens (human)Potency28.18380.000618.41981,122.0200AID1688
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency27.66190.000627.21521,122.0200AID743202; AID743219
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency10.18150.005612.367736.1254AID624032
survival motor neuron protein isoform dHomo sapiens (human)Potency12.58930.125912.234435.4813AID1458
lamin isoform A-delta10Homo sapiens (human)Potency31.62280.891312.067628.1838AID1487
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency29.84930.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency28.94310.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency27.54040.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency13.33320.002319.595674.0614AID651631; AID720552
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency29.84930.001551.739315,848.9004AID1259244
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency12.58930.009610.525035.4813AID1479145
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency1.58491.000010.475628.1838AID1457
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency27.54040.01238.964839.8107AID1645842
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency10.59090.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency10.59090.011912.222168.7989AID651632
cytochrome P450 2C9, partialHomo sapiens (human)Potency27.54040.01238.964839.8107AID1645842
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency8.49210.060110.745337.9330AID485368
[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)
Voltage-dependent L-type calcium channel subunit alpha-1CCavia porcellus (domestic guinea pig)IC50 (µMol)1.40000.02201.64228.9000AID1207619
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50 (µMol)1.00000.00032.63119.0000AID1207728
Bile salt export pumpHomo sapiens (human)IC50 (µMol)16.46000.11007.190310.0000AID1449628
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)11.50000.00002.800510.0000AID1210069
Lethal factorBacillus anthracisIC50 (µMol)4.80000.09702.85976.0000AID406412
Cytochrome P450 2J2Homo sapiens (human)IC50 (µMol)11.50000.01202.53129.4700AID1210069
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50 (µMol)1.00000.00032.59559.0000AID1207728
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)0.51840.00091.901410.0000AID1207208; AID161281; AID1649553; AID240820; AID243151; AID243188; AID408340; AID420668; AID46687; AID576612
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki0.30630.00211.840710.0000AID274128; AID290939; AID290940
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50 (µMol)1.00000.00032.63119.0000AID1207728
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50 (µMol)1.20000.00032.25459.6000AID1207619; AID1207728
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC50 (µMol)3.70000.00033.64849.2000AID1207149
[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)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (309)

Processvia Protein(s)Taxonomy
visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
detection of light stimulus involved in visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
fatty acid metabolic processCytochrome P450 2J2Homo sapiens (human)
icosanoid metabolic processCytochrome P450 2J2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2J2Homo sapiens (human)
regulation of heart contractionCytochrome P450 2J2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2J2Homo sapiens (human)
linoleic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
organic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
sensory perception of soundVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion importVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transporter activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
skeletal system developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
extraocular skeletal muscle developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
striated muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
endoplasmic reticulum organizationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
myoblast fusionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
neuromuscular junction developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle adaptationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle fiber developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
release of sequestered calcium ion into cytosolVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cellular response to caffeineVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
immune system developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
heart developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
embryonic forelimb morphogenesisVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
camera-type eye developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transport into cytosolVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of ventricular cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rateSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac conduction system developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac ventricle developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
brainstem developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
response to denervation involved in regulation of muscle adaptationSodium channel protein type 5 subunit alphaHomo sapiens (human)
telencephalon developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cerebellum developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
odontogenesis of dentin-containing toothSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of epithelial cell proliferationSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cellular response to calcium ionSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of cardiac muscle cell contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
ventricular cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during Purkinje myocyte cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell to bundle of His cell communicationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of heart rate by cardiac conductionSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (108)

Processvia Protein(s)Taxonomy
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
monooxygenase activityCytochrome P450 2J2Homo sapiens (human)
iron ion bindingCytochrome P450 2J2Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
isomerase activityCytochrome P450 2J2Homo sapiens (human)
linoleic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
heme bindingCytochrome P450 2J2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2J2Homo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
ankyrin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
small molecule bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
molecular function activator activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 5 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
fibroblast growth factor bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
enzyme bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein kinase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein domain specific bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ankyrin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ubiquitin protein ligase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
nitric-oxide synthase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in Purkinje myocyte action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
scaffold protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (68)

Processvia Protein(s)Taxonomy
photoreceptor outer segmentVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneCytochrome P450 2J2Homo sapiens (human)
extracellular exosomeCytochrome P450 2J2Homo sapiens (human)
cytoplasmCytochrome P450 2J2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2J2Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
sarcoplasmic reticulumVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
T-tubuleVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
I bandVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic densityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
dendriteVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic density membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleolusSodium channel protein type 5 subunit alphaHomo sapiens (human)
endoplasmic reticulumSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
cell surfaceSodium channel protein type 5 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 5 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
lateral plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 5 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 5 subunit alphaHomo sapiens (human)
sarcolemmaSodium channel protein type 5 subunit alphaHomo sapiens (human)
perinuclear region of cytoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 5 subunit alphaHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (189)

Assay IDTitleYearJournalArticle
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID127919Concentration causing local anesthetic activity in mice; Not tested1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1472912Antiviral activity against Ebolavirus infected in human HepG2 cells assessed as reduction in virus entry after 48 hrs by Celltiter-Glo luminescent assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Target Identification and Mode of Action of Four Chemically Divergent Drugs against Ebolavirus Infection.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID60874Percent inhibition of calcium-dependent potassium-polarized smooth muscle contraction in canine trachea1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity.
AID243151Inhibitory concentration against potassium channel HERG2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1209974Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID62112Evaluated for the heart rate at dose 0.5 mg/kg in 4 animals by poldine tachycardia test1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1210016Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID58751Relative activity (fraction of the most active compound 24) was determined1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID1533458Antiviral activity against Ebolavirus infected in mouse assessed as protection against viral infection at 24 mg/kg/day relative to control2019European journal of medicinal chemistry, Jan-15, Volume: 162Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action.
AID243188Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
A two-state homology model of the hERG K+ channel: application to ligand binding.
AID62237Evaluated for the heart rate at dose 2.5 mg/kg in 4 animals by glucagon-induced tachycardia test1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID62113Evaluated for the heart rate at dose 1.0 mg/kg in 3 animals by aminophylline-induced sinus tachycardia test1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID290939Displacement of [3H]dofetilide from hERG expressed in HEK293 cells by SPA2007Journal of medicinal chemistry, Jun-28, Volume: 50, Issue:13
Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID59380Evaluated for the myocardial depression rating which is barely observable for the given compound in Conscious Dog1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1210073Inhibition of CYP2C19 in human liver microsomes using omeprazole substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID324434Increase in light chain 3-GFP+ autophagosome vesicle number per cell in human H4 cells at 6.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID420669Lipophilicity, log D at pH 7.02009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID62238Evaluated for the heart rate at dose 2.5 mg/kg in 4 animals by poldine tachycardia test1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID1207617Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1210072Inhibition of CYP2C9 in human liver microsomes using tolbutamide substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1209972Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID62119Evaluated for the heart rate at dose 2.5 mg/kg in 3 animals by aminophylline-induced sinus tachycardia test1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID420668Inhibition of human ERG in MCF7 cells2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID62115Evaluated for the heart rate at dose 1.0 mg/kg in 4 animals by glucagon-induced tachycardia test1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID62241Evaluated for the heart rate at dose 5.0 mg/kg in 3 animals by aminophylline-induced sinus tachycardia test1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID1210015Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1209973Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID324580Decrease in FYVE-RFP+ vesicle intensity per cell in human H4 cells after 4 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1207180Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID58437Change in heart rate at the above D50 dose in conscious dogs1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID45634Inhibition of [3H]nitrendipine binding to calcium channels in Rabbit cardiac muscle.1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity.
AID521209Antiproliferative activity against mouse astrocyte cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID62116Evaluated for the heart rate at dose 1.0 mg/kg in 4 animals by poldine tachycardia test1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID1207149Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1472913Binding affinity to Ebola virus Zaire Mayinga-76 recombinant GP protein assessed as change in melting temperature at 500 uM by SYPRO orange dye-based fluorescence assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Target Identification and Mode of Action of Four Chemically Divergent Drugs against Ebolavirus Infection.
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID406412Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability after 24 hrs by WST1 dye reduction assay2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1207616Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1061889Displacement of [3H]BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes after 60 mins by scintillation counting2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
A highly predictive 3D-QSAR model for binding to the voltage-gated sodium channel: design of potent new ligands.
AID324382Induction of light chain 3-GFP level in human H4 cells at 6.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID240820Inhibitory concentration against IKr potassium channel2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents.
AID1472910Binding affinity to Ebola virus Zaire Mayinga-76 recombinant GP protein by SYPRO orange dye-based fluorescence assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Target Identification and Mode of Action of Four Chemically Divergent Drugs against Ebolavirus Infection.
AID521210Ratio of EC50 for mouse astrocytes to EC50 for mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID406411Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability at 0.125 to 12.5 uM relative to toxin-treated control2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID1207728Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits2013Scientific reports, , Volume: 3MICE models: superior to the HERG model in predicting Torsade de Pointes.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID406416Inhibition of Bacillus anthracis edema toxin-mediated intoxication in CHOK1 cells assessed as cAMP levels after 4 hrs by HTRF assay2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID1210017Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1649553Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
AID411793Metabolic stability in human liver microsomes assessed as intrinsic clearance per mg of protein2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Metabolic soft spot identification and compound optimization in early discovery phases using MetaSite and LC-MS/MS validation.
AID29813Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID62243Evaluated for the heart rate at dose 5.0 mg/kg in 4 animals by glucagon-induced tachycardia test1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID1207239Effective free therapeutic plasma concentration (EFTPC): the concentration of unbound compund in the blood plasma at therapeutic dose (mean of range)2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID324583Increase in long-lived protein degradation in human H4 cells after 2 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID324486Increase in light chain 3-GFP+ autophagosome vesicle area per cell in human H4 cells at 6.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID60470Dose required to achieve 50 % of maximal cardiac slowing in triazine tachycardia test in conscious dog1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID250135Inhibition of compound against MES-SA/DX5 cell line was determined using P-glycoprotein assay2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
A pharmacophore hypothesis for P-glycoprotein substrate recognition using GRIND-based 3D-QSAR.
AID1847246Antiviral activity against Ebola virus infected in African green monkey assessed as reduction in viral infection incubated for 48 hrs by CellTiter-Glo Luminescent Cell Viability Assay2021European journal of medicinal chemistry, Nov-05, Volume: 223Potential pharmacological strategies targeting the Niemann-Pick C1 receptor and Ebola virus glycoprotein interaction.
AID324582Increase in long-lived protein degradation in human H4 cells after 1 hr relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID324579Decrease in FYVE-RFP+ vesicle intensity per cell in human H4 cells after 2 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1472911Antiviral activity against Ebolavirus infected in african green monkey Vero E6 cells assessed as reduction in virus entry after 48 hrs by by Celltiter-Glo luminescent assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Target Identification and Mode of Action of Four Chemically Divergent Drugs against Ebolavirus Infection.
AID1207208Inhibition of hERG K channel2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1210069Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID406417Inhibition of cholera toxin-mediated intoxication in CHOK1 cells assessed as cAMP levels after 4 hrs by HTRF assay2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID1207619Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID406424Drug level in human serum2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID58438Percent decrease from initial heart rate (percent delta HR50/HR0 x 100) in dogs1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID46687K+ channel blocking activity in COS-7 African green monkey kidney derived cells expressing HERG Kv11.12002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.
AID406413Protection against Bacillus anthracis protective antigen and lethal toxin-diphtheria toxin chimeric protein mediated cytotoxicity in mouse RAW264.7 cells assessed as cell viability after 24 hrs by WST1 dye reduction assay2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID406410Protection against Bacillus anthracis protective antigen and lethal toxin-diphtheria toxin chimeric protein mediated cytotoxicity in mouse RAW264.7 cells assessed as cell viability2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID406418Inhibition of Bacillus anthracis lethal toxin entry in mouse RAW264.7 cells assessed as MEK cleavage at 12.5 uM after 4 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID55922Cardiac slowing index was measured for potency and efficacy1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.
AID406414Protection against diphtheria toxin-mediated cytotoxicity in CHOK1 cells assessed as cell viability after 48 hrs by WST1 dye reduction assay2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID290941Ratio of Ki for hERG by SPA to Ki for hERG by fluorescence polarization assay in HEK293 cells2007Journal of medicinal chemistry, Jun-28, Volume: 50, Issue:13
Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel.
AID324538Increase in light chain 3-GFP+ autophagosome vesicle intensity per cell in human H4 cells at 6.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1210071Inhibition of CYP3A4 in human liver microsomes using testosterone substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID521208Antiproliferative activity against mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID290940Binding affinity at hERG expressed in HEK293 cells by fluorescence polarization assay2007Journal of medicinal chemistry, Jun-28, Volume: 50, Issue:13
Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel.
AID406425Antimalarial activity against Plasmodium falciparum2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID1210070Inhibition of CYP2D6 in human liver microsomes using bufuralol substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID324581Decrease in FYVE-RFP+ vesicle intensity per cell in human H4 cells after 8 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1210074Inhibition of CYP1A2 in human liver microsomes using phenacetin substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID324584Increase in long-lived protein degradation in human H4 cells after 4 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1207618Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID406420Inhibition of Bacillus anthracis protective antigen pore formation in mouse RAW264.7 cells at 12.5 uM after 2 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID406415Protection against Bacillus anthracis protective antigen and lethal toxin-diphtheria toxin chimeric protein-mediated cytotoxicity in CHOK1 cells assessed as cell viability after 48 hrs by WST1 dye reduction assay2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID406419Inhibition of Bacillus anthracis protective antigen binding to cell surface of mouse RAW264.7 cells at 12.5 uM after 2 hrs by flow cytometry2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID311932Inhibition of ASM in human H4 cells assessed as residual activity at 10 uM2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID274128Displacement of [3H]Astemizole from hERG expressed in HEK293 cells at 10 uM2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides.
AID1863562Antiviral activity against pseudotyped Ebola virus assessed as inhibition of viral entry2022European journal of medicinal chemistry, Oct-05, Volume: 240Discovery of potent ebola entry inhibitors with (3S,4aS,8aS)-2-(3-amino-2-hydroxypropyl) decahydroisoquinoline-3-carboxamide scaffold.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID324585Increase in long-lived protein degradation in human H4 cells after 24 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID680720TP_TRANSPORTER: increase in Rhodamine 123 intracellular accumulation (R123: 150 uM, Bepridil: 5 ug/mL) in MDR1-expressing NIH3T3 cells2000The Journal of pharmacology and experimental therapeutics, Dec, Volume: 295, Issue:3
Influence of antipsychotic, antiemetic, and Ca(2+) channel blocker drugs on the cellular accumulation of the anticancer drug daunorubicin: P-glycoprotein modulation.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
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.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1346465Rat KNa1.1 (Calcium- and sodium-activated potassium channels)2006Neuropharmacology, Sep, Volume: 51, Issue:4
Pharmacological activation and inhibition of Slack (Slo2.2) channels.
AID1346699Human Kv7.4 (Voltage-gated potassium channels)2001American journal of physiology. Cell physiology, Apr, Volume: 280, Issue:4
KCNQ4 channels expressed in mammalian cells: functional characteristics and pharmacology.
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.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (746)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990224 (30.03)18.7374
1990's225 (30.16)18.2507
2000's190 (25.47)29.6817
2010's87 (11.66)24.3611
2020's20 (2.68)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 42.93

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

MetricThis Compound (vs All)
Research Demand Index42.93 (24.57)
Research Supply Index6.77 (2.92)
Research Growth Index4.39 (4.65)
Search Engine Demand Index67.24 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (42.93)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials70 (8.77%)5.53%
Reviews27 (3.38%)6.00%
Case Studies18 (2.26%)4.05%
Observational1 (0.13%)0.25%
Other682 (85.46%)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
Integrated Silicon Photonics for Cardiovascular Disease Monitoring InSiDe-CC Clinical Validation of the Diagnostic Device (LDV) for the Measurement of Heart-carotid Pulse Wave Velocity (PWV) by Magnetic Resonance Imaging (MRI) [NCT05711693]100 participants (Anticipated)Interventional2023-02-01Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]