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propafenone

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Description

Propafenone is a class IC antiarrhythmic drug used to treat atrial fibrillation, ventricular tachycardia, and other heart rhythm disorders. It is synthesized through a multi-step process involving a series of chemical reactions, starting with the compound 3,4-dimethoxyphenethylamine. Propafenone works by blocking sodium channels in the heart, which slows the conduction of electrical impulses and helps to restore a normal heart rhythm. Its effects include slowing the heart rate, reducing the frequency and duration of abnormal heartbeats, and improving the function of the heart. Propafenone is studied extensively for its potential to treat various cardiac arrhythmias, as well as for its possible benefits in other conditions such as migraines and epilepsy. The drug is also studied for its safety and efficacy in different populations, including pregnant women and children.'

Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias. [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 CID4932
CHEMBL ID631
CHEBI ID63619
SCHEMBL ID27865
SCHEMBL ID16730120
MeSH IDM0017736

Synonyms (129)

Synonym
STL284627
AB00053687-14
BRD-A26334849-001-02-1
BRD-A26334849-003-05-0
1-[2-(2-hydroxy-3-propylaminopropoxy)phenyl]-3-phenylpropan-1-one
gtpl2561
KBIO1_000906
DIVK1C_000906
SPECTRUM_001612
propafenone [inn:ban]
propafenonum [inn-latin]
1-propanone, 1-(2-(2-hydroxy-3-(propylamino)propoxy)phenyl)-3-phenyl-
propafenona [inn-spanish]
einecs 258-955-6
LOPAC0_000919
PRESTWICK3_000499
PRESTWICK2_000499
BSPBIO_003470
IDI1_000906
SPECTRUM5_001271
BSPBIO_000397
BSPBIO_001465
AB00053687
propafenone
54063-53-5
C07381 ,
1-(2-(2-hydroxy-3-(propylamino)propoxy)phenyl)-3-phenyl-1-propanone
DB01182
2-(2'-hydroxy-3'-propylaminopropoxy)-omega-phenylpropiophenone
NCGC00089784-04
NCGC00089784-03
KBIO2_002092
KBIOSS_002092
KBIO2_004660
KBIOGR_000817
KBIO3_002974
KBIO2_007228
SPECTRUM3_001905
NINDS_000906
SPBIO_001605
SPECTRUM2_001603
SPBIO_002318
SPECTRUM4_000209
PRESTWICK0_000499
PRESTWICK1_000499
BPBIO1_000437
BCBCMAP01_000079
NCGC00089784-02
NCGC00089784-05
propafenon hexal
HMS2089E09
HMS1989J07
NCGC00015819-10
gnf-pf-4594 ,
CHEMBL631 ,
chebi:63619 ,
AKOS000276940
propafenone (inn)
propafenon hexal (tn)
D08435
HMS1791J07
1-[2-(2-hydroxy-3-propylamino-propoxy)-phenyl]-3-phenyl-propan-1-one
1-(2-(2-hydroxy-3-(propylamino)propoxy)phenyl)-3-phenylpropan-1-one
1-[2-(2-hydroxy-3-propylamino-propoxy)-phenyl]-3-phenyl-propan-1-one (propafenone)
bdbm50067133
1-[2-[2-hydroxy-3-(propylamino)propoxy]phenyl]-3-phenylpropan-1-one
NCGC00015819-06
HMS3259O16
1-[2-[2-oxo-3-(propylamino)propoxy]phenyl]-3-phenyl-propan-1-one
A829936
dtxcid7025184
dtxsid9045184 ,
tox21_110228
cas-54063-53-5
CCG-205001
NCGC00015819-08
NCGC00015819-04
NCGC00015819-11
NCGC00015819-07
NCGC00015819-05
1-[2-[2-hydroxy-3-(propylamino)propoxy]phenyl]-3-phenyl-propan-1-one
FT-0674052
FT-0674053
unii-68iqx3t69u
propafenona
propafenonum
hsdb 7929
68iqx3t69u ,
1-(2-(2-hydroxy-3-propylaminopropoxy)phenyl)-3-phenylpropan-1-one
FT-0630665
1-{2-[2-hydroxy-3-(propylamino)propoxy]phenyl}-3-phenylpropan-1-one
S2500
S5789
AKOS022106720
propafenone [vandf]
propafenone [mi]
propafenone [inci]
propafenone [who-dd]
propafenone [inn]
NC00582
SCHEMBL27865
tox21_110228_1
NCGC00015819-15
1-[2-(2-hydroxy-3-propylamino-propoxy)phenyl]-3-phenyl-propan-1-one
SCHEMBL16730120
1-(2-[2-hydroxy-3-(propylamino)propoxy]phenyl)-3-phenyl-1-propanone #
2'-[2-hydroxy-3-(propylamino)propoxy]-3-phenylpropiophenone
1-propanone, 1-[2-[2-hydroxy-3-(propylamino)propoxy]phenyl]-3-phenyl-
rhytmol
HMS3402J07
AB00053687_16
AB00053687_15
HMS3656O08
SBI-0050894.P003
SW196964-3
1-(2-(2-hydroxy-3-(propylamino)propoxy)
phenyl)-3-phenylpropan-1-one
FT-0645120
Q662511
BRD-A26334849-003-16-7
SDCCGSBI-0050894.P004
NCGC00015819-24
CS-0009325
HY-B0432
EN300-58332
c01bc03
propafenona (inn-spanish)
propafenonum (inn-latin)
(+/-)-2'-(2-hydroxy-3-propylaminopropoxy)-3-phenylpropiophenone

Research Excerpts

Overview

Propafenone is an antiarrhythmic drug metabolized primarily by cytochrome P450 2D6 (CYP2D6) It is commonly used as the first-line therapy for patients with paroxysmal atrial fibrillation (AF) in Taiwan.

ExcerptReferenceRelevance
"Propafenone (PPF) is a class I"( Metabolic Activation and Cytotoxicity of Propafenone Mediated by CYP2D6.
Jia, C; Li, J; Li, W; Peng, Y; Shi, J; Zheng, J, 2022
)
2.43
"Propafenone is a well-known Class 1C antiarrhythmic agent that has sodium channel blocking properties as well as the ability to block 13 other channels and a modest calcium antagonistic effect. "( Effect of Rythmol (propafenone HCl) administration during pregnancy in Wistar rats.
Abd-Allah, ER; Amin, S; Badawy, MA; El Ghareeb, AEW, 2022
)
2.49
"Propafenone is an antiarrhythmic drug metabolized primarily by cytochrome P450 2D6 (CYP2D6). "( Influence of CYP2D6 genetic variation on adverse events with propafenone in the pediatric and young adult population.
Fish, FA; Gaedigk, A; Kannankeril, PJ; Radbill, AE; Sunthankar, SD; Van Driest, SL, 2022
)
2.41
"Propafenone is a class IC antiarrhythmic agent that is commonly used as the first-line therapy for patients with paroxysmal atrial fibrillation (AF) in Taiwan. "( An open-label randomized noninferior study of generic name and brand name of propafenone for rhythm control in patients with paroxysmal atrial fibrillation.
Chang, SL; Chin, CG; Chiou, CW; Hsieh, MH; Hsieh, YC; Huang, CL; Hung, Y; Lai, WT; Lee, HC; Lin, TH; Lin, WS; Lin, YJ; Lin, YK; Yeh, TC, 2023
)
2.58
"Propafenone is a safe and effective antiarrhythmic medication in children."( Electrophysiological effects and clinical utility of propafenone in children.
Ferns, SJ; Gehi, AK; Hudak, ML; McKenzie, K; Singh, M, 2022
)
2.41
"Propafenone is a Vaughan Williams class 1c antiarrhythmic medication widely used for treatment of arrhythmias. "( Revisiting propafenone toxicity.
Alsaad, AA; Austin, CO; Kusumoto, F; Ortiz Gonzalez, Y, 2017
)
2.29
"Propafenone is a class 1C antiarrhythmic drug used in the second-line management of supraventricular and ventricular arrhythmias and, when unintentionally ingested, can lead to severe and life-threatening poisoning."( Ventricular Tachycardia Induced by Propafenone Intoxication in a Pediatric Patient.
Di Mita, O; DʼAnna, C; Marzuillo, P; Pappacoda, S; Ponticiello, E; Rosa, M; Tipo, V, 2019
)
1.51
"Propafenone is a sodium-channel blocker, class IC antiarrhythmic drug, frequently used to manage supraventricular dysrhythmias, especially atrial fibrillation. "( Failure of Intracardiac Pacing After Fatal Propafenone Overdose: A Case Report.
Brkljačić, DD; Bulj, N; Čabrilo, V; Kolačević, M; Manola, Š; Zeljković, I, 2018
)
2.19
"Propafenone is a class Ic antiarrhythmic drug. "( Propafenone hepatotoxicity: report of a new case and review of the literature.
Barada, KA; El-Majzoub, NM; Eloubeidi, MA; Faraj, WG; Jabbour, MN; Khoury, MY; Tawil, AN; Younan, LB,
)
3.02
"Propafenone is an established class IC antiarrhythmic drug commonly used in the treatment of atrial fibrillation."( Propafenone associated severe central nervous system and cardiovascular toxicity due to mirtazapine: a case of severe drug interaction.
Aryal, SR; Khan, MA; Rajpurohit, N; Stys, AT; Stys, TP, 2014
)
2.57
"Propafenone is a well-known Class Ic antiarrhythmic agent. "( Propafenone shows class Ic and class II antiarrhythmic effects.
Brussee, H; Lamprecht, G; Lercher, P; Lindner, W; Stoschitzky, G; Stoschitzky, K, 2016
)
3.32
"Propafenone (PPF) is an antiarrhythmic drug, metabolized mainly by CYP2D6 to 5-hydroxypropafenone (5OH-PPF) and by CYP3A4 to norpropafenone (NOR-PPF). "( Effect of CYP2D6 polymorphisms on the pharmacokinetics of propafenone and its two main metabolites.
Afshar, M; Rouini, MR, 2017
)
2.14
"Propafenone is an antiarrhythmic that has been used for the treatment of tachiarrytmias in both adults and children. "( Clinical evidence of the antiarrhythmic effect of a magistral suspension of propafenone: a case report.
Barranco-Garduño, L; Bobadilla-Chávez, J; Flores-Pérez, C; Flores-Pérez, J; Juárez-Olguín, H; Osnaya, H,
)
1.8
"Propafenone is an anti-arrhythmic drug used in the management of supraventricular and ventricular arrhythmias. "( Propafenone poisoning--a case report with plasma propafenone concentrations.
Dargan, PI; Jones, AL; Ludman, A; Ovaska, H; Spencer, EP; Wood, DM, 2010
)
3.25
"Propafenone is an uncommonly encountered class IC antidysrhythmic that is a look-alike for the opioid, oxycodone/acetaminophen 5/325."( Overdose of propafenone surreptitiously sold as "Percocet".
Curtis, JA; D'Orazio, JL, 2011
)
1.47
"Propafenone HCl 225-mg is an uncommonly encountered pharmaceutical, but is a look-alike for oxycodone/acetaminophen 5/325."( Overdose of propafenone surreptitiously sold as "Percocet".
Curtis, JA; D'Orazio, JL, 2011
)
1.47
"Propafenone was found to be a safe and effective anti-arrhythmic drug and can be justifiably administered for AVNRT and AVRT termination."( Electrophysiological effects, efficacy and safety of intravenous propafenone in termination of atrioventricular nodal reentrant tachycardia and atrioventricular reentrant tachycardia: a prospective non-randomized interventional study.
Delić-Brkljacić, D; Manola, S; Nossan, JS; Pavlović, N; Pintarić, H; Radeljić, V, 2010
)
1.32
"Propafenone is a class I antiarrhythmic drug used to suppress cardiac arrhythmia both of atrial and ventricular origin. "( Beta-adrenergic stimulation modulates the sodium current block by propafenone in rat ventricular myocardium.
Kirstein, M; Maier, SK, 2002
)
1.99
"Propafenone is a class Ic antiarrhythmic drug used to maintain sinus rhythm in patients with atrial fibrillation. "( Effects of propafenone and its main metabolite, 5-hydroxypropafenone, on HERG channels.
Arias, C; Caballero, R; Delpón, E; González, T; Moreno, I; Tamargo, J; Valenzuela, C, 2003
)
2.15
"Propafenone is an antiarrhythmic agent with recognized cardiac myocyte repolarizing K+ current inhibitory effects. "( Propafenone and its metabolites preferentially inhibit IKr in rabbit ventricular myocytes.
Cahill, SA; Gross, GJ, 2004
)
3.21
"Propafenone is an effective antiarrhythmic agent used in children, while in Mexico no specific formulation for children is available, which causes errors in adequate dosage. "( Bioavailability of an extemporaneous suspension of propafenone made from tablets.
Chávez, JB; Mendiola, BR; Olguín, HJ; Pérez, CF; Pérez, JF; Portugal, MC, 2006
)
2.03
"Propafenone is a specific antagonist of the human beta adrenoceptor and this action can be demonstrated during in vivo study in human subjects."( Demonstration of beta adrenoceptor blockade by propafenone hydrochloride: clinical pharmacologic, radioligand binding and adenylate cyclase activation studies.
McLeod, AA; Shand, DG; Stiles, GL, 1984
)
1.25
"Propafenone is a considerably active drug against ventricular arrhythmias."( Antiarrhythmic effectiveness of propafenone compared to lorajmine in ventricular arrhythmias. Controlled clinical trial.
Bianchini, C; Meoli, P; Rovelli, F; Sanna, G, 1983
)
1.27
"Propafenone is a promising new antiarrhythmic agent marketed in Europe for the past 7 years. "( Clinical pharmacology of propafenone: pharmacokinetics, metabolism and concentration-response relations.
Roden, DM; Siddoway, LA; Woosley, RL, 1984
)
2.01
"Propafenone is a class 1C antiarrhythmic agent that blocks fast sodium channels in heart muscle and Purkinje fibers similar to the action of encainide and flecainide. "( Probable propafenone-induced transient global amnesia.
Brace, SR; Jones, RJ; Vander Tuin, EL, 1995
)
2.15
"Propafenone is an orally active sodium channel blocking agent with beta-adrenoceptor antagonist and weak calcium antagonist activity. "( Propafenone. A reappraisal of its pharmacology, pharmacokinetics and therapeutic use in cardiac arrhythmias.
Bryson, HM; Fitton, A; Langtry, HD; Palmer, KJ, 1993
)
3.17
"Propafenone is a potent antiarrhythmic agent effective in either supraventricular or ventricular tachyarrhythmias. "( Propafenone in the treatment of cardiac arrhythmias. A risk-benefit appraisal.
Boriani, G; Capucci, A, 1995
)
3.18
"Propafenone is an infrequently used class IC antiarrhythmic drug. "( Propafenone overdose.
English, B; Ford, M; Kerns, W, 1994
)
3.17
"Propafenone is an effective drug for the acute conversion of spontaneous monomorphic sustained ventricular tachycardia, especially in patients without organic heart disease. "( [The efficacy and safety of intravenous propafenone in the acute treatment of spontaneous sustained ventricular tachycardia].
Madrid, AH; Marín-Huerta, E; Mestre, JL; Moro, C; Novo, L, 1994
)
2
"Propafenone is a class 1c antiarrhythmic agent that has an electrophysiologic profile suggesting that it might be potentially effective in recent-onset AF."( Clinical course of recent-onset atrial fibrillation treated with oral propafenone.
Ganam, R; Ganem, R; Rabner, M; Weiner, P; Zidan, F, 1994
)
1.24
"Propafenone is a class Ic anti-arrhythmic agent with mild beta-blocking properties which has recently become available in South Africa. "( Normal left ventricular function does not protect against propafenone-induced incessant ventricular tachycardia.
Lawrenson, JB; Millar, RN; Milne, DA, 1993
)
1.97
"Propafenone is a sodium channel blocking agent with a mild beta- and calcium channel-blocking activity. "( Guidelines for the use of propafenone in treating supraventricular arrhythmias.
Camm, AJ; Kishore, AG, 1995
)
2.03
"Propafenone is an effective drug for preventing supraventricular tachyarrhythmia, but the incidence of side effects during longterm therapy in patients with such arrhythmias has not been adequately reported."( Safety and tolerability of long-term propafenone therapy for supraventricular tachyarrhythmias. The Propafenone Multicenter Study Group.
Anderson, JL; Podrid, PJ, 1996
)
1.29
"Propafenone is a sodium channel blocking antiarrhythmic drug. "( Propafenone: an effective agent for the management of supraventricular arrhythmias.
Grant, AO, 1996
)
3.18
"Propafenone is an antiarrhythmic drug used in the treatment of life-threatening ventricular tachyarrhythmias. "( Propafenone-induced drug fever in the absence of agranulocytosis.
Gerling, BR; Greenberg, ML; Holzberger, PT; O'Rourke, DJ; Palac, RT, 1997
)
3.18
"Propafenone (PF) is a class 1C antiarrhythmic agent. "( Identification and determination of phase I metabolites of propafenone in rat liver perfusate.
Li, Q; McKay, G; Semple, HA; Tan, W, 1998
)
1.99
"Propafenone is a class IC antiarrhythmic agent metabolized into two major metabolites, 5-hydroxypropafenone and N-depropylpropafenone. "( ECG changes and plasma concentrations of propafenone and its metabolites in a case of severe poisoning.
Belpaire, F; Buylaert, W; Calle, P; Fonck, K; Haenebalcke, C; Hemeryck, A; Jordaens, L, 1998
)
2.01
"Propafenone is a class Ic antiarrhythmic agent which also exhibits beta-adrenergic and fast sodium channel blockade. "( Recurrent convulsions and cardiac conduction disturbances after propafenone overdose.
Buffet, M; Grossenbacher, F; Lamiable, D; Rambourg-Schepens, MO, 1999
)
1.98
"Propafenone is a class Ic agent for the treatment of atrial arrhythmias with a main hepatic metabolism. "( Propafenone in the conversion of atrial fibrillation in patients suffering from chronic renal failure.
Di Benedetto, A; Di Ieso, N; Liguori, A; Napoli, C; Sorice, P, 1997
)
3.18
"Propafenone is an effective and safe antiarrhythmic drug for converting paroxysmal and/or recent-onset atrial fibrillation of various origins with a more limited efficacy in chronic atrial fibrillation."( [Pharmacological cardioversion with intravenous propafenone in atrial fibrillation].
Arias Estrada, S; Cancino Rodríguez, C; Hernández Morales, E; Rangel Rojo, J; Uribe Muñoz, A; Velázquez Rodríguez, E,
)
1.11
"Propafenone is a potent CYP2D6 inhibitor that may cause an increase in plasma concentrations of coadministered CYP2D6 substrates."( Pharmacokinetic and pharmacodynamic interaction between mexiletine and propafenone in human beings.
Adedoyin, A; Champagne, J; Gilbert, M; Hamelin, B; Labbé, L; Lefebvre, M; Lessard, E; O'Hara, G; Turgeon, J, 2000
)
1.98
"Propafenone is an effective antiarrhythmic drug used widely for the treatment of supraventricular and ventricular arrhythmias. "( Propafenone-induced ataxia: report of three cases.
Odeh, M; Oliven, A; Seligmann, H, 2000
)
3.19
"Propafenone (PPF) is an antiarrhythmic, Class Ic agent. "( The influence of CYP2D6 polymorphism on the antiarrhythmic efficacy of propafenone in patients with paroxysmal atrial fibrillation during 3 months propafenone prophylactic treatment.
Dmochowska-Perz, M; Jazwinska-Tarnawska, E; Loboz-Grudzien, K; Niewinski, P; Orzechowska-Juzwenko, K; Rzemislawska, Z; Slawin, J, 2001
)
1.99
"Propafenone hydrochloride is a drug used for treating arrhythmia. "( [Liver function test impairment induced by propafenone in a 73 year old woman].
Arinzon, Z; Fridman, R, 2001
)
2.02
"Propafenone is a class IC antiarrhythmic agent that is suitable for oral loading as it reaches peak plasma concentrations within 2 to 4 hours of administration."( Oral loading with propafenone for conversion of recent-onset atrial fibrillation: a review on in-hospital treatment.
Biffi, M; Boriani, G; Branzi, A; Capucci, A; Martignani, C, 2002
)
1.37
"Propafenone is an antiarrhythmic agent with fast sodium channel, calcium channel, and beta-adrenergic receptor blocking properties. "( Effects of propafenone on pacing-induced ventricular fibrillation and intracellular calcium in rat hearts.
Parmley, WW; Stefenelli, T; Wikman-Coffelt, J; Wu, ST, 1992
)
2.12
"Propafenone is a new drug that has been shown to be efficacious in the therapy of supraventricular and ventricular arrhythmias, and is of potential use in patients with defibrillators."( Effects of acute and prolonged administration of propafenone on internal defibrillation in the pig.
Barilaro, C; Bombardieri, G; Jones, DL; Kim, YH; Klein, GJ; Montenero, AS; Natale, A, 1992
)
1.26
"Propafenone is a class 1C antiarrhythmic agent which is administered as a racemate of S(+)- and R(-)-enantiomers. "( Clinical pharmacokinetics of propafenone.
Burgess, ED; Duff, HJ; Hii, JT, 1991
)
2.02
"Propafenone is a class 1c antiarrhythmic agent with moderate beta-blocking activity as a result of a structural similarity to beta-adrenoceptor antagonists. "( Different stereoselective effects of (R)- and (S)-propafenone: clinical pharmacologic, electrophysiologic, and radioligand binding studies.
Graziadei, I; Klein, W; Lindner, W; Stark, G; Stark, U; Stoschitzky, K; Zernig, G, 1990
)
1.97
"Propafenone is a type 1C antiarrhythmic drug with efficacy for both ventricular and supraventricular arrhythmias. "( Effects of propafenone on sinus node function in the rabbit heart.
Kerr, CR, 1990
)
2.11
"Propafenone (Pf) is a class I antiarrhythmic drug that can be given both orally and intravenously. "( Comparative electrophysiological effects of propafenone, 5-hydroxy-propafenone, and N-depropylpropafenone on guinea pig ventricular muscle fibers.
Adamantidis, MM; Broly, F; Caron, JF; Dupuis, BA; Honore, E; Libersa, CC; Rouet, R; Wajman, A, 1989
)
1.98
"Propafenone is an investigational type Ic anti-arrhythmic agent that markedly slows conduction velocity in all cardiac tissues. "( Propafenone: a novel type Ic antiarrhythmic agent.
Bauman, JL; McCollam, PL; Parker, RB, 1989
)
3.16
"Propafenone is an antiarrhythmic drug that produces a variable degree of beta-blockade in humans and is administered as a racemate. "( Stereoselective disposition and pharmacologic activity of propafenone enantiomers.
Eichelbaum, M; Funck-Brentano, C; Kroemer, HK; Roden, DM; Silberstein, DJ; Wood, AJ; Woosley, RL, 1989
)
1.96
"Propafenone is a new class 1 antiarrhythmic agent. "( In vitro characterization of the human cytochrome P-450 involved in polymorphic oxidation of propafenone.
Eichelbaum, M; Kroemer, HK; Kronbach, T; Meyer, UA; Mikus, G, 1989
)
1.94
"Propafenone is a new class Ic antiarrhythmic compound with a broad pharmacologic profile. "( Effects of propafenone on ventricular arrhythmias: double-blind, parallel, randomized, placebo-controlled dose-ranging study.
Guerrero, J; Kaplinsky, E; Kirsten, E; Singh, BN, 1988
)
2.11
"Propafenone is a class IC antiarrhythmic agent that is structurally similar to the beta blockers but that has only weak beta-blocking and calcium-channel-blocking activity."( Propafenone: a new antiarrhythmic agent.
Chow, MS; Hilleman, D; Lebsack, C, 1988
)
2.44
"Propafenone is a very promising agent for emergency intravenous therapy as well as long-term oral therapy in patients with Wolff-Parkinson-White syndrome."( Efficacy of propafenone in Wolff-Parkinson-White syndrome: electrophysiologic findings and long-term follow-up.
Antman, EM; Friedman, PL; Ludmer, PL; McGowan, NE, 1987
)
1.37
"Propafenone is a Class I antiarrhythmic agent with weak beta-adrenoceptor antagonist activity which can be given both intravenously and orally. "( Propafenone. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in the treatment of arrhythmias.
Brogden, RN; Harron, DW, 1987
)
3.16
"Propafenone is a new membrane-stabilizing antiarrhythmic agent that structurally resembles the beta-adrenergic receptor antagonist, propranolol. "( Evaluation of the asthmogenicity of propafenone, a new antiarrhythmic drug. Comparison of spirometry with methacholine challenge.
Gotz, VP; Harman, E; Hendeles, L; Hill, MR; McLeod, I, 1986
)
1.99
"Propafenone is a type 1c antiarrhythmic drug that recently has become available for clinical trials within the United States. "( Propafenone ingestion.
McHugh, TP; Perina, DG, 1987
)
3.16
"Oral propafenone was found to be an effective drug for reducing the level of chronic ventricular ectopy, as reflected by a short-term trial."( Oral propafenone in the suppression of chronic stable ventricular arrhythmias.
Kawalsky, DL; Myburgh, DP; Pincus, DR; Schamroth, CL; Schamroth, L; Scholtz, ME, 1985
)
1.24
"Propafenone is an effective well tolerated antiarrhythmic drug without major side effects in pediatric patients."( [The treatment of arrhythmias in infants and children using propafenone].
Dressler, F; Grävinghoff, L; Grütte, E; Jüngst, BK; Liersch, R; Nomayo, H; Puls, I; Rautenburg, HW; Schmaltz, A; Schumacher, G, 1985
)
1.23
"Propafenone is a new class Ic antiarrhythmic agent currently being investigated in the United States. "( Aggravation of electrically provoked ventricular tachycardia during treatment with propafenone.
Garan, H; McGovern, B; Ruskin, JN; Stavens, CS, 1985
)
1.94
"Propafenone is an effective drug for the management of ventricular tachyarrhythmias, and may be used in patients with impaired left ventricular function."( Propafenone therapy for ventricular tachycardia in the setting of congestive heart failure.
Abate, D; Allen, BJ; Brodsky, MA; Henry, WL, 1985
)
2.43
"Propafenone (Rythmol) is a very active anti-arrhythmic at the ventricular level which acts by decreasing the rate of atrio-ventricular and intra-ventricular conduction and by prolonging the refractory period of the right atrium and the accessory pathways."( [Oral propafenone in resistant auricular arrhythmia].
Bounhoure, JP; Calazel, J; Cassagneau, B; Dechandol, AM; Sabot, G,
)
1.33

Effects

Propafenone hydrochloride has been widely used for the treatment of supraventricular and ventricular arrhythmias. It has a profound electrophysiologic effect on auxiliary atrioventricular circuits and can obstruct conduction in the fast conducting pathway.

ExcerptReferenceRelevance
"Propafenone has a profound electrophysiologic effect on auxiliary atrioventricular circuits and in patients with atrioventricular nodal reentry tachycardia can obstruct conduction in the fast conducting pathway."( Effect of Rythmol (propafenone HCl) administration during pregnancy in Wistar rats.
Abd-Allah, ER; Amin, S; Badawy, MA; El Ghareeb, AEW, 2022
)
1.77
"Propafenone has a profound electrophysiologic effect on auxiliary atrioventricular circuits and in patients with atrioventricular nodal reentry tachycardia can obstruct conduction in the fast conducting pathway."( Effect of Rythmol (propafenone HCl) administration during pregnancy in Wistar rats.
Abd-Allah, ER; Amin, S; Badawy, MA; El Ghareeb, AEW, 2022
)
1.77
"Propafenone hydrochloride has been widely used for the treatment of supraventricular and ventricular arrhythmias. "( Propafenone-associated Gross Hematuria: A Case Report and Review of the Literature.
Chen, S; Cui, Y; Ding, W; Wang, Z; Ye, J; Zhao, X, 2019
)
3.4
"Propafenone overdose has been reported to be associated with features of severe cardiovascular and CNS toxicity."( Propafenone poisoning--a case report with plasma propafenone concentrations.
Dargan, PI; Jones, AL; Ludman, A; Ovaska, H; Spencer, EP; Wood, DM, 2010
)
2.52
"Propafenone has also demonstrated efficacy in the treatment of malignant ventricular arrhythmias (ventricular fibrillation and sustained ventricular tachycardia); preliminary mortality data obtained with propafenone have been encouraging in this patient group."( Propafenone. A reappraisal of its pharmacology, pharmacokinetics and therapeutic use in cardiac arrhythmias.
Bryson, HM; Fitton, A; Langtry, HD; Palmer, KJ, 1993
)
2.45
"Propafenone has been efficient in preventing supraventricular tachycardias in all patients."( [Propafenone efficacy in preventing supraventricular tachycardia in childhood].
Barrenetxea, JI; Bodegas, A; Cabrera, A; Galdeano, JM; Idígoras, G; Pastor, E; Pérez García, P; Rumoroso, JR; Sarrionaindía, MJ; Sota, J, 1994
)
1.92
"Propafenone has comparatively few noncardiac side effects."( Propafenone: an effective agent for the management of supraventricular arrhythmias.
Grant, AO, 1996
)
2.46
"Propafenone has little effects on sinus node."( [The study of acute clinical electrophysiological effects of propafenone on paroxysmal supraventricular tachycardia using transesophageal atrial pacing technique].
Li, Q; Peng, D; Wang, Z, 1997
)
1.26
"Propafenone has been shown to affect the delayed-rectifier potassium currents in cardiomyocytes of different animal models. "( Blocking effects of the antiarrhythmic drug propafenone on the HERG potassium channel.
Borggrefe, M; Breithardt, G; Haverkamp, W; Hüttenhofer, A; Madeja, M; Mergenthaler, J; Musshoff, U; Skryabin, BV; Speckmann, EJ, 2001
)
2.01
"Thus propafenone has potent inhibitory effects on accessory pathways and has additional significant effects on atrial, AV nodal and ventricular refractoriness."( Electrophysiologic effects of oral propafenone in Wolff-Parkinson-White syndrome studied by programmed electrical stimulation.
Arora, R; Khalilullah, M; Mohan, JC; Prasad, GS; Sethi, KK,
)
0.86
"Propafenone has significantly improved our ability to control postoperative JET."( Newer antiarrhythmic drugs in children.
Garson, A; Moak, JP; Smith, RT, 1987
)
0.99
"Propafenone has sustained antiarrhythmic efficacy after 2 years without serious toxicity."( Sustained therapeutic efficacy and safety of oral propafenone for treatment of chronic ventricular arrhythmias: a 2-year experience.
Baker, BJ; de Soyza, N; Dinh, H; Murphy, ML, 1988
)
1.25
"Propafenone has been used to treat Torsade de pointes, but we show that it may also cause Torsade de pointes."( Torsade de pointes ventricular tachycardia in a hypothyroid patient treated with propafenone.
Brooks, R; Rosengarten, M,
)
1.08

Actions

Propafenone promotes slow monomorphic VT, probably by use-dependent conduction slowing and wavelength shortening. It may increase the proportion of asymptomatic atrial arrhythmia episodes.

ExcerptReferenceRelevance
"Propafenone toxicity can cause significant QRS widening and markedly abnormal ventricular activation pattern. "( Cardiac memory induced by QRS widening due to propafenone toxicity.
Josephson, ME; Shvilkin, A; Wylie, JV; Zimetbaum, P, 2007
)
2.04
"Propafenone promotes slow monomorphic VT, probably by use-dependent conduction slowing and wavelength shortening."( Postrepolarization refractoriness versus conduction slowing caused by class I antiarrhythmic drugs: antiarrhythmic and proarrhythmic effects.
Fabritz, CL; Franz, MR; Kirchhof, PF, 1998
)
1.02
"Propafenone may increase the proportion of asymptomatic atrial arrhythmia episodes."( Is there a synergic effect of propafenone associated with atrial overdrive pacing for atrial arrhythmia prevention? A randomised crossover study.
Barold, SS; Cazeau, S; Clementy, J; Garrigue, S; Haissaguerre, M; Hocini, M; Jais, P, 2000
)
1.32
"Thus propafenone can produce rate-dependent failure of ventricular capture which is associated with marked prolongation of refractoriness and QRS duration suggesting a marked use-dependent drug effect in selected patients."( Rate-dependent failure of ventricular capture in patients treated with oral propafenone.
Almendral, J; Arenal, A; Delcan, JL; Josephson, ME; San Román, D; Soriano, J, 1992
)
0.97
"Propafenone also showed a lower incidence of side effects."( Comparison of propafenone and disopyramide for treatment of chronic ventricular arrhythmias: placebo-controlled, double-blind, randomized crossover study.
Ambrosioni, E; Bertaccini, P; Bracchetti, D; Cantelli, I; Naccarella, F; Palmieri, M, 1985
)
1.35

Treatment

Propafenone treatment offered protection against ischemic stroke with HR 0.649 (95% CI 0.55-0.77, P<.001). Propafen one treatment was found to reduce significantly ectopic ventricular beats, especially with the higher dosage (44.9% reduction under 450 mg)

ExcerptReferenceRelevance
"Propafenone treatment offered protection against ischemic stroke with HR 0.649 (95% CI 0.55-0.77, P<.001)."( Factors predisposing to ventricular proarrhythmia during antiarrhythmic drug therapy for atrial fibrillation in patients with structurally normal heart.
Chang, SL; Chang, Y; Chao, TF; Chen, SA; Chen, YY; Chien, KL; Chiou, CW; Chong, E; Chung, FP; Hu, YF; Liao, JN; Lin, CY; Lin, YJ; Lo, LW; Tuan, TC, 2015
)
1.14
"If propafenone treatment failed, quinidine sulfate was administered."( Use of propafenone for conversion of chronic atrial fibrillation in horses.
De Clercq, D; Deprez, P; Tavernier, R; van Loon, G; Verbesselt, R, 2009
)
1.32
"Propafenone treatment was found to reduce significantly ectopic ventricular beats, especially with the higher dosage (44.9% reduction under 450 mg; 88.8% reduction under 900 mg)."( [Evaluation of the anti-arrhythmic action of propafenone treatment and its influence on left ventricular function].
Bonaiuto, M; Cinquegrani, M; Fodale, P; Giordano, G; Mileto, A; Oriti, S; Saitta, A; Saitta, M; Squadrito, F, 1993
)
1.27
"Propafenone was used in treatment in 31 patients, metoprolol in 30, amiodarone in 25."( [The effect of treatment with propafenone, metoprolol and amiodarone on lymphocyte sodium efflux and level of cAMP in serum].
Kosmala, W, 1995
)
1.3
"Propafenone treatment does not affect repolarization time indexes, affecting only depolarization time as expressed by an increase in QRS (p = 0.046)."( [Sotalol, propafenone, and flecainide: compared multiparametric analysis of ventricular repolarization in subjects without organic cardiopathy].
Briglia, N; Ducceschi, V; Esposito, R; Iacono, A; Mayer, MS; Santangelo, L; Sarubbi, B; Scialdone, A, 1996
)
1.42
"Propafenone treatment was administered at 2 mg/kg over 15 minutes under continuous electrocardiographic monitoring."( [Pharmacological cardioversion with intravenous propafenone in atrial fibrillation].
Arias Estrada, S; Cancino Rodríguez, C; Hernández Morales, E; Rangel Rojo, J; Uribe Muñoz, A; Velázquez Rodríguez, E,
)
1.11
"By treatment with propafenone, both patients showed dramatic and rapid improvement of symptoms and the left ventricular dysfunction."( Reversible left ventricular diastolic dysfunction resulting from frequent supraventricular tachycardia.
Hasatani, K; Nakao, T; Okamoto, S; Shimizu, M; Takeda, R; Zenda, T, 1993
)
0.61
"In untreated atria propafenone produced a dose-dependent decrease in the rate and maximum following frequency, prolonged the sinus node recovery time and reduced the maximum chronotropic responses to isoprenaline."( Electrophysiological effects of propafenone in untreated and propafenone-pretreated guinea-pig atrial and ventricular muscle fibres.
Delgado, C; Tamargo, J; Tejerina, T, 1985
)
0.87

Toxicity

Propafenone in a single oral loading dose is safe and promptly effective in patients with recent ons. In adults, propafen one adverse events (AEs) are associated with CYP2D6 poor metabolizer status.

ExcerptReferenceRelevance
" Adverse effects were encountered in 7 patients: in 1 case worsened arrhythmia and in 6 patients, with long-lasting arrhythmias, congestive heart failure."( [The emergency treatment of supraventricular tachyarrhythmias: the efficacy and safety of intravenous propafenone].
Annoni, P; Baroffio, R; Bossi, M; Cazzaniga, L; Ciaramella, C; Guzzini, F; Maestroni, A; Tisi, G, 1992
)
0.5
" Patients were assessed for safety and drug tolerance at designated intervals over the 12-month study unless discontinued for adverse experience or inadequate response."( Safety of long-term flecainide and propafenone in the management of patients with symptomatic paroxysmal atrial fibrillation: report from the Flecainide and Propafenone Italian Study Investigators.
Casadei, G; Chimienti, M; Cullen, MT, 1996
)
0.57
" At each visit, medical events, vital sign measurements (blood pressure, pulse rate), concomitant medications, adverse experiences, and study drug dosage changes were evaluated."( Comparison of the safety and efficacy of flecainide versus propafenone in hospital out-patients with symptomatic paroxysmal atrial fibrillation/flutter. The Flecainide AF French Study Group.
Aliot, E; Denjoy, I, 1996
)
0.54
"Follow-up duration was 12 months, or when patients stopped the treatment as a result of inadequate efficacy or adverse experiences."( Safety of flecainide versus propafenone for the long-term management of symptomatic paroxysmal supraventricular tachyarrhythmias. Report from the Flecainide and Propafenone Italian Study (FAPIS) Group.
Casadei, G; Chimienti, M; Cullen, MT, 1995
)
0.59
"4 months), 290 patients (60%) discontinued propafenone therapy, but in only 70 patients (15%) was the reason for discontinuation an adverse drug reaction."( Safety and tolerability of long-term propafenone therapy for supraventricular tachyarrhythmias. The Propafenone Multicenter Study Group.
Anderson, JL; Podrid, PJ, 1996
)
0.83
"This study was designed to assess adverse effects of oral propafenone in a large number of pediatric patients."( Safety of oral propafenone in the treatment of arrhythmias in infants and children (European retrospective multicenter study). Working Group on Pediatric Arrhythmias and Electrophysiology of the Association of European Pediatric Cardiologists.
Janousek, J; Paul, T, 1998
)
0.9
" Safety was assessed by evaluating the appearance of adverse events classified as mild, moderate and severe."( Safety of oral propafenone in the conversion of recent onset atrial fibrillation to sinus rhythm: a prospective parallel placebo-controlled multicentre study.
Aschieri, D; Capucci, A; Piepoli, M; Villani, GQ, 1999
)
0.66
"Propafenone in a single oral loading dose is safe and promptly effective in patients with recent onset atrial fibrillation."( Safety of oral propafenone in the conversion of recent onset atrial fibrillation to sinus rhythm: a prospective parallel placebo-controlled multicentre study.
Aschieri, D; Capucci, A; Piepoli, M; Villani, GQ, 1999
)
2.1
"Existing drug therapies for paroxysmal supraventricular tachycardia (PSVT) have potentially serious adverse effects."( Efficacy and safety of dofetilide in the prevention of symptomatic episodes of paroxysmal supraventricular tachycardia: a 6-month double-blind comparison with propafenone and placebo.
Droszcz, W; Graff, O; Kawecka-Jaszcz, K; Kozlowski, JW; Krzeminska-Pakula, M; Kulakowski, P; Malolepszy, J; Ruzyllo, W; Swiatecka, G; Szechinski, J; Tendera, M; Wnuk-Wojnar, AM, 2001
)
0.51
" Three patients taking propafenone had serious treatment-related adverse effects that required drug discontinuation."( Efficacy and safety of dofetilide in the prevention of symptomatic episodes of paroxysmal supraventricular tachycardia: a 6-month double-blind comparison with propafenone and placebo.
Droszcz, W; Graff, O; Kawecka-Jaszcz, K; Kozlowski, JW; Krzeminska-Pakula, M; Kulakowski, P; Malolepszy, J; Ruzyllo, W; Swiatecka, G; Szechinski, J; Tendera, M; Wnuk-Wojnar, AM, 2001
)
0.82
" Nine patients (9%) in the propafenone group, 11 (10%) in the sotalol group, and 3 (3%) in the placebo group discontinued therapy due to adverse effects."( Long-term efficacy and safety of propafenone and sotalol for the maintenance of sinus rhythm after conversion of recurrent symptomatic atrial fibrillation.
Bellandi, F; Dabizzi, RP; Frascarelli, F; Giovannini, T; Leoncini, M; Maioli, M; Simonetti, I, 2001
)
0.89
" We conclude that oral and intravenous propafenone is safe in the termination of propafenone."( [Comparison of efficacy, safety and cost-effectiveness of intravenous versus oral propafenone in paroxysmal atrial fibrillation].
Grossmann, G; Klecha, T; Klepacka, H; Modrzewska, A; Rumiński, W; Zadura, M, 2001
)
0.81
" Adverse effects leading to withdrawal were higher in the propafenone SR 425-mg twice daily group than in any other group."( Efficacy and safety of sustained-release propafenone (propafenone SR) for patients with atrial fibrillation.
Carlson, M; Fava, G; Page, RL; Pritchett, EL; Undesser, K, 2003
)
0.83
"The use of IB in patients receiving amiodarone or propafenone for AFL or AF is equally effective and safe as the use of IB alone."( Efficacy and safety of ibutilide for cardioversion of atrial flutter and fibrillation in patients receiving amiodarone or propafenone.
Fragakis, N; Katsaris, G; Kozirakis, M; Maligkos, G; Papadopoulos, N; Papanastasiou, S; Tsaritsaniotis, E, 2005
)
0.79
"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
" Despite careful precautions, serious proarrhythmias, the major limiting side effect of dofetilide, still occurred during long-term follow-up."( Observations on the safety and effectiveness of dofetilide in patients with paroxysmal atrial fibrillation and normal left ventricular function.
Bauman, JL; Kehoe, RF; Leal, S; Mykytsey, A; Razminia, M; Saleem, M; Wang, T; Zheutlin, T, 2007
)
0.34
"The goal of this article was to describe a potential drug-drug interaction between propafenone and citalopram, which caused symptoms of propafenone adverse effects."( Adverse effects of propafenone after long-term therapy with the addition of citalopram.
Garcia, A, 2008
)
0.9
"An 80-year-old white female, followed up at the Memory Clinic for mild cognitive impairment, had been taking propafenone 900 mg/d for >10 years for paroxysmal atrial fibrillation without adverse effects."( Adverse effects of propafenone after long-term therapy with the addition of citalopram.
Garcia, A, 2008
)
0.89
"This is the first report of a possible interaction between propafenone and citalopram, which caused propafenone adverse effects (eg, dizziness, falls) and mimicked coronary artery disease."( Adverse effects of propafenone after long-term therapy with the addition of citalopram.
Garcia, A, 2008
)
0.92
" Therefore, oral loading with propafenone (as "pill-in-the-pocket" treatment of recent-onset atrial fibrillation) in a patient on concurrent carvedilol treatment may lead to a pharmacokinetic interaction, with high plasma levels of propafenone and potential drug-related adverse effects."( Atrial fibrillation: adverse effects of "pill-in-the-pocket" treatment and propafenone-carvedilol interaction.
Biffi, M; Boriani, G; Diemberger, I; Domenichini, G; Martignani, C; Marziali, A, 2010
)
0.88
"Pill-in-the-pocket treatment should be prescribed only if the administration of a loading oral dose of flecainide or propafenone has been proved safe in hospital, since major adverse effects have been reported in 5% of patients during in-hospital treatment."( Intravenous administration of flecainide or propafenone in patients with recent-onset atrial fibrillation does not predict adverse effects during 'pill-in-the-pocket' treatment.
Alboni, P; Boriani, G; Botto, GL; Capucci, A; Iori, M; Mancini, M; Mariconti, B; Pacchioni, F; Pasanisi, G; Russo, G, 2010
)
0.83
"One hundred and twenty-two patients with AF of recent onset who were successfully treated (conversion of AF within 2 h without major adverse effects) in hospital with intravenous flecainide or propafenone were discharged on pill-in-the-pocket treatment."( Intravenous administration of flecainide or propafenone in patients with recent-onset atrial fibrillation does not predict adverse effects during 'pill-in-the-pocket' treatment.
Alboni, P; Boriani, G; Botto, GL; Capucci, A; Iori, M; Mancini, M; Mariconti, B; Pacchioni, F; Pasanisi, G; Russo, G, 2010
)
0.81
" Major adverse events occurred in five patients (6%) and in four (5%) of these during the first oral treatment (one syncope, two presyncope, one sinus arrest)."( Intravenous administration of flecainide or propafenone in patients with recent-onset atrial fibrillation does not predict adverse effects during 'pill-in-the-pocket' treatment.
Alboni, P; Boriani, G; Botto, GL; Capucci, A; Iori, M; Mancini, M; Mariconti, B; Pacchioni, F; Pasanisi, G; Russo, G, 2010
)
0.62
"The patient's tolerance of intravenous administration of flecainide or propafenone does not seem to predict adverse effects during out-of-hospital self-administration of these drugs."( Intravenous administration of flecainide or propafenone in patients with recent-onset atrial fibrillation does not predict adverse effects during 'pill-in-the-pocket' treatment.
Alboni, P; Boriani, G; Botto, GL; Capucci, A; Iori, M; Mancini, M; Mariconti, B; Pacchioni, F; Pasanisi, G; Russo, G, 2010
)
0.85
" Sodium bicarbonate therapy is advocated to directly counteract the toxic effects of propafenone."( Acute propafenone toxicity after two exposures at standard dosing.
Gin, K; Parwana, H; Shanks, D; Yeung, A,
)
0.84
" No propafenone-related adverse effects were recorded during the study period."( Electrophysiological effects, efficacy and safety of intravenous propafenone in termination of atrioventricular nodal reentrant tachycardia and atrioventricular reentrant tachycardia: a prospective non-randomized interventional study.
Delić-Brkljacić, D; Manola, S; Nossan, JS; Pavlović, N; Pintarić, H; Radeljić, V, 2010
)
1.16
" The most serious adverse effect of ibutilide was non-sustained monomorphic ventricular tachycardia (3/49,6."( [Efficacy and safety of ibutilide for conversion of atrial fibrillation/flutter].
Ma, C; Xiang, M; Yang, Y; Yu, Z; Zhang, S, 2013
)
0.39
"Intravenous ibutilide is a safe and effective agent for cardioversion of recent-onset AF/AFL."( [Efficacy and safety of ibutilide for conversion of atrial fibrillation/flutter].
Ma, C; Xiang, M; Yang, Y; Yu, Z; Zhang, S, 2013
)
0.39
" Mirtazapine is a commonly prescribed antidepressant drug, which is also metabolized through and may modulate the CYP4502D6 pathway leading to altered metabolism of propafenone and possible adverse effects."( Propafenone associated severe central nervous system and cardiovascular toxicity due to mirtazapine: a case of severe drug interaction.
Aryal, SR; Khan, MA; Rajpurohit, N; Stys, AT; Stys, TP, 2014
)
2.04
" The primary safety endpoint was hospitalization due to the adverse effects of the treatment."( Comparative effectiveness and safety of antazoline‑based and propafenone‑based strategies for pharmacological cardioversion of short‑duration atrial fibrillation in the emergency department.
Farkowski, MM; Kowalik, I; Maciąg, A; Pytkowski, M; Sterliński, M; Szwed, H; Woźniak, J; Żurawska, M, 2016
)
0.68
" We analysed the differences between amiodarone and class IC group in terms of efficacy and safety that is conversion to sinus rhythm rates within 12 and 48 h after starting treatment, time to conversion, and adverse drug effects."( Efficacy and safety in pharmacological cardioversion of recent-onset atrial fibrillation: a propensity score matching to compare amiodarone vs class IC antiarrhythmic drugs.
Bonora, A; Dilda, A; Franchi, E; Maccagnani, A; Olivieri, O; Pistorelli, C; Taioli, G; Turcato, G; Zerman, G, 2017
)
0.46
"This retrospective study included 1777 non-permanent AF patients taking rivaroxaban for ≥ 1 month between 2011 and 2016 from a multicenter cohort in Taiwan, and compared concomitant AAD use against clinical outcome endpoints for safety, effectiveness, and major adverse cardiac events (MACE)."( Safety and Effectiveness of Rivaroxaban in Combination with Various Antiarrhythmic Drugs in Patients with Non-Permanent Atrial Fibrillation.
Chen, CY; Chiou, WR; Chuang, JY; Huang, CC; Kuo, JY; Lee, YH; Liao, FC; Lin, PL; Liu, LY; Su, MI; Tsai, CT; Wu, YJ, 2021
)
0.62
" In adults, propafenone adverse events (AEs) are associated with CYP2D6 poor metabolizer status; however, pediatric data are lacking."( Influence of CYP2D6 genetic variation on adverse events with propafenone in the pediatric and young adult population.
Fish, FA; Gaedigk, A; Kannankeril, PJ; Radbill, AE; Sunthankar, SD; Van Driest, SL, 2022
)
1.34
"Guidelines recommend that initial trial of a "pill-in-the-pocket" (PIP) Class 1C antiarrhythmic drug (AAD) for cardioversion of atrial fibrillation (AF) be performed in a monitored setting because of the potential for adverse reactions."( Safety of Pill-in-the-Pocket Class 1C Antiarrhythmic Drugs for Atrial Fibrillation.
Arkles, JS; Callans, DJ; Deo, R; Dixit, S; Epstein, AE; Frankel, DS; Guandalini, GS; Hyman, MC; Jarrah, AA; Lin, D; Marchlinski, FE; Markman, TM; Mustin, E; Nazarian, S; Riley, M; Santangeli, P; Schaller, RD; Supple, GE; Tian, Y, 2022
)
0.72
"This study sought to characterize real-world, contemporary use of the PIP approach, including the setting of initiation and incidence of adverse events."( Safety of Pill-in-the-Pocket Class 1C Antiarrhythmic Drugs for Atrial Fibrillation.
Arkles, JS; Callans, DJ; Deo, R; Dixit, S; Epstein, AE; Frankel, DS; Guandalini, GS; Hyman, MC; Jarrah, AA; Lin, D; Marchlinski, FE; Markman, TM; Mustin, E; Nazarian, S; Riley, M; Santangeli, P; Schaller, RD; Supple, GE; Tian, Y, 2022
)
0.72
"Our data support the current recommendation to initiate PIP AAD in a monitored setting because of rare significant adverse reactions that can require urgent intervention."( Safety of Pill-in-the-Pocket Class 1C Antiarrhythmic Drugs for Atrial Fibrillation.
Arkles, JS; Callans, DJ; Deo, R; Dixit, S; Epstein, AE; Frankel, DS; Guandalini, GS; Hyman, MC; Jarrah, AA; Lin, D; Marchlinski, FE; Markman, TM; Mustin, E; Nazarian, S; Riley, M; Santangeli, P; Schaller, RD; Supple, GE; Tian, Y, 2022
)
0.72

Pharmacokinetics

Propafenone enantiomers may be relevant to diminished capacity of CYP2D6 enzyme in Chinese subjects. In 450 mg/d group, patients with homozygous mutant of CY P2 D6*10 had a Cmax of propafen one two times as high as those of wild-type genotype.

ExcerptReferenceRelevance
" In this paper, we present an allometric study of propafenone carried out in eight animal species, all treated and handled under the same conditions, and taking into account their weight to calculate different pharmacokinetic parameters."( Prediction of the disposition of propafenone in humans and dogs from pharmacokinetic parameters in other animal species.
Arboix, M; de Mora, F; Guitart, R; Puigdemont, A, 1991
)
0.82
" This polymorphic metabolism accounts for the marked interindividual variability in the relationships between dose and concentration, and between concentration and pharmacodynamic effects."( Clinical pharmacokinetics of propafenone.
Burgess, ED; Duff, HJ; Hii, JT, 1991
)
0.57
" The renal clearance and half-life of digoxin were not significantly altered by propafenone."( Effects of coadministration of propafenone on the pharmacokinetics of digoxin in healthy volunteer subjects.
Erstad, BL; Furman, C; Hoyer, GL; Kirsten, EB; Marcus, FI; Nolan, PE, 1989
)
0.79
" After the first administration of P, major interindividual variability in pharmacokinetic parameters was observed."( [Pharmacokinetics of oral propafenone in patients with supraventricular arrhythmia].
Buoncuore, A; Cheymol, G; Colombel, B; Ferry, A; Jaillon, P; Pochmalicki, G; Poirier, JM; Valty, J; Vrancea, F,
)
0.43
"The pharmacodynamic and pharmacokinetic behavior of (R)- and (S)-propafenone was investigated in a group of seven healthy volunteers, one of whom belonged to the phenotype of poor debrisoquine hydroxylators."( Comparative pharmacokinetics and clinical pharmacology of propafenone enantiomers after oral administration to man.
Brode, E; Hollmann, M; Müller-Peltzer, H, 1988
)
0.76
" After 1 month of treatment the plasma elimination half-life of propafenone (6."( Pharmacokinetics and pharmacodynamics of propafenone during acute and chronic administration.
Bianchini, C; Ferrario, G; Giani, P; Giudici, V; Landolina, M; Latini, R; Marchi, S; Riva, E, 1988
)
0.78
" Pharmacokinetic parameters were determined by fitting the coronary sinus effluent propafenone concentration-time data to a one-compartment pharmacokinetic model."( Myocardial uptake kinetics and pharmacodynamics of propafenone in the isolated perfused rabbit heart.
Gillis, AM; Kates, RE, 1986
)
0.75
"005), in area under the serum-digoxin concentration curve (4 h: 520."( [Effect of propafenone on the pharmacokinetics of digoxin administered orally: a study in healthy volunteers].
Cardaioli, P; Compostella, L; Cucchini, F; De Domenico, R; Libardoni, M; Papalia, D; Pulido, E; Zeppellini, R, 1986
)
0.66
" EMs were characterized by a shorter propafenone elimination half-life (5."( Polymorphism of propafenone metabolism and disposition in man: clinical and pharmacokinetic consequences.
McAllister, CB; Roden, DM; Siddoway, LA; Thompson, KA; Wang, T; Wilkinson, GR; Woosley, RL, 1987
)
0.89
"This article reviews clinical pharmacokinetic data on 8 new antiarrhythmic agents."( Clinical pharmacokinetics of the newer antiarrhythmic agents.
Gillis, AM; Kates, RE,
)
0.13
" The drug is remarkable for great interindividual variability in its pharmacokinetic and pharmacodynamic properties."( Clinical pharmacology of propafenone: pharmacokinetics, metabolism and concentration-response relations.
Roden, DM; Siddoway, LA; Woosley, RL, 1984
)
0.57
" The pharmacokinetic profile of propafenone is complex, characterised as typically nonlinear, saturable, stereoselective and dependent on both dose and debrisoquin metaboliser phenotype; individualised dosage titration is required."( Propafenone. A reappraisal of its pharmacology, pharmacokinetics and therapeutic use in cardiac arrhythmias.
Bryson, HM; Fitton, A; Langtry, HD; Palmer, KJ, 1993
)
2.01
" Blood and urine samples were collected for pharmacokinetic analyses."( Effect of diprafenone on the pharmacokinetics of digoxin.
Alken, RG; Koytchev, R; Mayer, O, 1996
)
0.29
"The most important pharmacokinetic parameters (Cmax, t1/2, AUC) and the relative oral availability of a solid oral preparation of racemic diprafenone were investigated when administered to fasting subjects and 10 min after a standard meal, in an open, randomised, crossover trial."( Influence of food on the bioavailability and some pharmacokinetic parameters of diprafenone--a novel antiarrhythmic agent.
Alken, RG; Greenwood, M; Koytchev, R; Mayer, O; Smith, I, 1996
)
0.29
"CYP2D6 phenotype determines the pharmacokinetic variability of propafenone enantiomers and existence of IM may be relevant to diminished capacity of CYP2D6 enzyme in Chinese subjects."( CYP2D6 phenotype determines pharmacokinetic variability of propafenone enantiomers in 16 HAN Chinese subjects.
Cai, MH; Cai, WM; Chen, B; Zhang, YD, 1999
)
0.79
" Our objective was to study the potential pharmacokinetic and electrophysiological interactions between mexiletine and propafenone."( Pharmacokinetic and pharmacodynamic interaction between mexiletine and propafenone in human beings.
Adedoyin, A; Champagne, J; Gilbert, M; Hamelin, B; Labbé, L; Lefebvre, M; Lessard, E; O'Hara, G; Turgeon, J, 2000
)
0.75
" Pharmacokinetic parameters of propafenone were not changed during concomitant administration of mexiletine in subjects of either phenotype."( Pharmacokinetic and pharmacodynamic interaction between mexiletine and propafenone in human beings.
Adedoyin, A; Champagne, J; Gilbert, M; Hamelin, B; Labbé, L; Lefebvre, M; Lessard, E; O'Hara, G; Turgeon, J, 2000
)
0.83
"CYP2D6 phenotype of human may influence not only pharmacokinetic of Pro but also its pharmacological effects."( Simultaneous modeling of pharmacokinetics and pharmacodynamics of propafenone in healthy subjects.
Cai, MH; Cai, WM; Chen, B; Ling, SS; Luo, JP; Zhang, YD, 2001
)
0.55
" In 450 mg/d group, patients with homozygous mutant of CYP2D6*10 not only had a Cmax of propafenone two times as high as those of wild-type genotype, but also showed a two fold higher inhibitory rate of VPC compared with those with homozygous CYP2D6*1 (P<0."( Effect of CYP2D6*10 genotype on propafenone pharmacodynamics in Chinese patients with ventricular arrhythmia.
Cai, WM; Chen, B; Huang, YZ; Xu, J; Zhang, FM; Zhang, YD, 2002
)
0.82
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
"Linear pharmacokinetic profiles of propafenone in female Wistar rats were found after oral administration of up to 20 mg/kg."( Nonlinear pharmacokinetics of propafenone in rats and humans: application of a substrate depletion assay using hepatocytes for assessment of nonlinearity.
Iwaki, M; Komura, H, 2005
)
0.89
" Recent studies with a 103-compound dataset suggested that scaling from monkey pharmacokinetic data tended to be the most accurate method for predicting human clearance."( Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
Evans, CA; Jolivette, LJ; Nagilla, R; Ward, KW, 2006
)
0.33
" Serial blood samples were collected and pharmacokinetic parameters were estimated using a population pharmacokinetic approach."( Inhibitory effects of propafenone on the pharmacokinetics of caffeine in humans.
Bélanger, PM; Ferron, LA; Gilbert, M; Grech-Bélanger, O; Labbé, L; Michaud, V; Mouksassi, MS; Turgeon, J, 2006
)
0.65
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" The method was successfully applied to a pharmacokinetic study of PPF and 5-OHP in healthy Chinese volunteers."( A Sensitive and Rapid LC-MS-MS Method for Simultaneous Determination of Propafenone and Its Active Metabolite 5-Hydroxypropafenone in Human Plasma and Its Application in a Pharmacokinetic Study.
Chi, Z; Ding, L; Li, Y; Liu, R; Shu, C; Wang, K, 2017
)
0.69

Compound-Compound Interactions

We describe a rare case of severe drug-drug interaction between propafenone and mirtazapine. No changes in the steady-state levels were observed between both treatment periods. Racemic propafENone was successfully enantioseparated by CCC.

ExcerptReferenceRelevance
" 3 In four patients being treated with the drug combination first and thereafter with propafenone alone no changes in the steady-state levels of propafenone were observed between both treatment periods."( Drug interaction between propafenone and metoprolol.
Jähnchen, E; Kalusche, D; Roskamm, H; Trenk, D; Wagner, F, 1987
)
0.8
"The purpose of this study was to propose a new method to predict in vivo drug-drug interactions (DDIs) for a high clearance drug from in vitro data."( Prediction of drug-drug interactions for AUCoral of high clearance drug from in vitro data: utilization of a microtiter plate assay and a dispersion model.
Kohno, Y; Nagata, K; Suzuki, A; Yamamoto, T; Yamazoe, Y, 2006
)
0.33
" Drug-drug binding interaction studies showed that verapamil, diazepam, nifedipine, furosemide, nitrendipine, and nimodipine did not affect the binding of PPF enantiomers except quinidine and aprindine at the therapeutic concentration."( Enantioselective plasma protein binding of propafenone: mechanism, drug interaction, and species difference.
Hong, Y; Tang, Y; Zeng, S, 2009
)
0.62
" Racemic propafenone was successfully enantioseparated by CCC with di-n-butyl l-tartrate combined with boric acid as the chiral selector."( Preparative enantioseparation of propafenone by counter-current chromatography using di-n-butyl L-tartrate combined with boric acid as the chiral selector.
Chu, C; Li, XN; Shen, M; Tong, S; Yan, J; Zheng, Y, 2013
)
1.09
"We describe a rare case of severe drug-drug interaction between propafenone and mirtazapine leading to propafenone toxicity."( Propafenone associated severe central nervous system and cardiovascular toxicity due to mirtazapine: a case of severe drug interaction.
Aryal, SR; Khan, MA; Rajpurohit, N; Stys, AT; Stys, TP, 2014
)
2.08
"Concomitant use of rivaroxaban with AADs appears to be well tolerated, warranting further investigation into the apparent benefits of a reduced dose of rivaroxaban combined with dronedarone."( Safety and Effectiveness of Rivaroxaban in Combination with Various Antiarrhythmic Drugs in Patients with Non-Permanent Atrial Fibrillation.
Chen, CY; Chiou, WR; Chuang, JY; Huang, CC; Kuo, JY; Lee, YH; Liao, FC; Lin, PL; Liu, LY; Su, MI; Tsai, CT; Wu, YJ, 2021
)
0.62

Bioavailability

The effect of food intake on the bioavailability of propafenone, a new antiarrhythmic agent, was evaluated by comparing its kinetics in 24 healthy volunteers in a fasted state and after a standard breakfast. The total body clearance of propafienone was 963 ml/min, the terminal half-life 198 min and its absolute bi is 8%.

ExcerptReferenceRelevance
" In man the oral bioavailability of propafenone is only about 5-40%."( LG 6-101 and LG 6-102, two new propafenone-related antiarrhythmic agents with good oral activity in rats.
Dittrich, P; Kukovetz, WR; Wascher, TC, 1992
)
0.84
" It is well absorbed and is predominantly bound to alpha 1-acid glycoprotein in the plasma."( Clinical pharmacokinetics of propafenone.
Burgess, ED; Duff, HJ; Hii, JT, 1991
)
0.57
" The total body clearance of propafenone was 963 ml/min, the terminal half-life 198 min and its absolute bioavailability was 15."( Nonlinear kinetics of propafenone metabolites in healthy man.
Follath, F; Ha, HR; Haefeli, W; Vlcek, J; Vozeh, S, 1990
)
0.88
" Following oral administration, a dose-dependent increase in bioavailability from 10."( Pharmacokinetic characterization of the antiarrhythmic drug diprafenone in man.
Jähnchen, E; Sachs, W; Trenk, D; Wagner, F, 1989
)
0.28
" The bioavailability of propafenone is dose-dependent."( Propafenone: a novel type Ic antiarrhythmic agent.
Bauman, JL; McCollam, PL; Parker, RB, 1989
)
2.03
" Bioavailability was 48%."( Hemodialysis removal of propafenone.
Burgess, ED; Duff, HJ, 1989
)
0.58
" It is well absorbed after oral administration, but systemic bioavailability is only 12% after a 300-mg dose."( Propafenone: a new antiarrhythmic agent.
Chow, MS; Hilleman, D; Lebsack, C, 1988
)
1.72
"The effect of food intake on the bioavailability of propafenone, a new antiarrhythmic agent, was evaluated by comparing its kinetics in 24 healthy volunteers in a fasted state and after a standard breakfast."( Food increases the bioavailability of propafenone.
Axelson, JE; Chan, GL; Kerr, CR; Kirsten, EB; Lanman, RC; Mason, WD, 1987
)
0.79
" Our results demonstrate that both systemic clearance and bioavailability of propafenone are sensitive to variability in liver function."( Influence of hepatic dysfunction on the pharmacokinetics of propafenone.
Dorian, P; Kates, RE; Lee, JT; Yee, YG,
)
0.6
" Lorcainide is also a class Ic antiarrhythmic drug, the bioavailability of which is nonlinear."( Clinical pharmacokinetics of the newer antiarrhythmic agents.
Gillis, AM; Kates, RE,
)
0.13
" Propafenone undergoes extensive presystemic clearance that appears to be saturable, with bioavailability increasing as dosage increases."( Clinical pharmacology of propafenone: pharmacokinetics, metabolism and concentration-response relations.
Roden, DM; Siddoway, LA; Woosley, RL, 1984
)
1.48
" The results show a dose dependence of bioavailability and maximum plasma concentrations after oral application with over-proportionate increase at higher dose levels yielding bioavailabilities up to 40-50% with single applications of 450 mg."( Investigations on the pharmacokinetics of propafenone in man.
Brode, E; Hollmann, M; Hotz, D; Kaumeier, S; Kehrhahn, OH, 1983
)
0.53
" Bioavailability is on the average 50%."( [Clinical pharmacology of propafenone].
Ambrosioni, E; Marchesini, B, 1984
)
0.57
" The longer t1/2s and the estimates of steady-state bioavailability above 100% suggests that clearance decreases during chronic oral dosing."( Propafenone disposition kinetics in cardiac arrhythmia.
Connolly, S; Harrison, DC; Kates, RE; Lebsack, C; Winkle, RA, 1984
)
1.71
"The present study was done to investigate the effect of food on the bioavailability of diprafenone."( Influence of food on the bioavailability and some pharmacokinetic parameters of diprafenone--a novel antiarrhythmic agent.
Alken, RG; Greenwood, M; Koytchev, R; Mayer, O; Smith, I, 1996
)
0.29
"Food increased the oral bioavailability of diprafenone by approximately 50%."( Influence of food on the bioavailability and some pharmacokinetic parameters of diprafenone--a novel antiarrhythmic agent.
Alken, RG; Greenwood, M; Koytchev, R; Mayer, O; Smith, I, 1996
)
0.29
" However, bioavailability of propafenone dropped from 30% +/- 24% to 4% +/- 3% (P < ."( Enzyme induction in the elderly: effect of rifampin on the pharmacokinetics and pharmacodynamics of propafenone.
Dilger, K; Hofmann, U; Klotz, U, 2000
)
0.81
"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
" Age-related delays in hepatic drug metabolism should explain the hazardous increase in the bioavailability of this drug."( Propafenone-related cholestatic hepatitis in an elderly patient.
Forgione, A; Gasbarrini, G; Giorgi, A; Grieco, A; Miele, L, 2002
)
1.76
"Estimation of bioavailability and toxicity at the very beginning of the drug development process is one of the big challenges in drug discovery."( Similarity based SAR (SIBAR) as tool for early ADME profiling.
Chiba, P; Ecker, GF; Kaiser, D; Klein, C; Kopp, S, 2002
)
0.31
" The aim of this study was to determine the bioavailability of a suspension prepared extemporaneously using commercial tablets of propafenone."( Bioavailability of an extemporaneous suspension of propafenone made from tablets.
Chávez, JB; Mendiola, BR; Olguín, HJ; Pérez, CF; Pérez, JF; Portugal, MC, 2006
)
0.79
" The proposed method is simple, with low instrumentation requirements, suitable for quality control application, bioavailability and bioequivalency studies."( Spectrofluorimetric determination of drugs containing active methylene group using N1-methyl nicotinamide chloride as a fluorigenic agent.
El Barbary, RA; El Dawya, MA; Mabrouk, MM, 2006
)
0.33
" The aim of this study is to compare the relative bioavailability of a magistral (MAG) preparation of propafenone versus its commercial (COM) presentation in a group of 16 Mexican healthy volunteers."( Comparative bioavailability of propafenone after administration of a magistral suspension vs. commercial tablets in healthy volunteers.
Barranco Garduño, L; Flores Pérez, C; Flores Pérez, J; Juárez Olguín, H; Ramírez Mendiola, B; Sandoval Ramírez, E, 2009
)
0.85
" The orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 milligrams/kilogram) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity."( Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
Barnes, SW; Bonamy, GM; Bopp, SE; Borboa, R; Bright, AT; Chatterjee, A; Che, J; Cohen, S; Dharia, NV; Diagana, TT; Fidock, DA; Froissard, P; Gagaring, K; Gettayacamin, M; Glynne, RJ; Gordon, P; Groessl, T; Kato, N; Kuhen, KL; Lee, MC; Mazier, D; McNamara, CW; Meister, S; Nagle, A; Nam, TG; Plouffe, DM; Richmond, W; Roland, J; Rottmann, M; Sattabongkot, J; Schultz, PG; Tuntland, T; Walker, JR; Winzeler, EA; Wu, T; Zhou, B; Zhou, Y, 2011
)
0.37
" Careful examination of the bioavailability, pharmacokinetics, toxicology, and efficacy of this series of compounds using rodent models revealed orally bioavailable compounds that are nontoxic and suppress parasitemia in vivo."( Lead optimization of antimalarial propafenone analogues.
Clark, JA; Connelly, MC; Derisi, JL; Furimsky, A; Gow, J; Guiguemde, WA; Guy, RK; Iyer, LV; Kyle, DE; Lemoff, A; Lowes, D; Mirsalis, J; Parman, T; Pradhan, A; Sigal, M; Tang, L; Wilson, E; Zhu, F, 2012
)
0.66
" Its bioavailability and plasma concentration differ among patients under long-term therapy."( Propafenone hepatotoxicity: report of a new case and review of the literature.
Barada, KA; El-Majzoub, NM; Eloubeidi, MA; Faraj, WG; Jabbour, MN; Khoury, MY; Tawil, AN; Younan, LB,
)
1.57
"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

Oral propafenone at a low dosage 150 mg 3 times daily is well tolerated and effective in maintaining sinus rhythm for 6 months. ECG, blood pressure (MAP) and heart rate were monitored.

ExcerptRelevanceReference
" During dosing (10 mg kg-1 twice a day for 10 days) no effects on the electrocardiogram, monitored in conscious animals, were observed despite modest reductions (15-18%) in the maximum rate of depolarization of papillary muscle excised 1 or 6 h after completion of the dosing regime."( Antiarrhythmic, electrophysiological and haemodynamic effects of prolonged oral dosing with Org 7797 in the anaesthetized rat.
Delbressine, L; Harris, N; Kane, KA; Muir, AW; Winslow, E, 1992
)
0.28
" Threshold was tested at baseline and at each dosage after 7 days of therapy."( Effects of oral propafenone therapy on chronic myocardial pacing threshold.
Altamura, G; Bianconi, L; Boccadamo, R; Carpino, A; Iesi, AP; Serdoz, R; Toscano, S, 1992
)
0.63
" The threshold rise and loss of atrial capture occurred after 7 days of treatment with propafenone at the dosage of 450 mg daily; drug withdrawal resulted in resumption of atrial capture and a return to prior pacing thresholds."( Propafenone induced acute variation of chronic atrial pacing threshold: a case report.
Boccadamo, R; Montefoschi, N, 1990
)
1.94
" Because this metabolic pathway is saturable, at the usual highest clinical dosage (900 mg/24 h) plasma propafenone concentration rises disproportionately in patients with normal 5-hydroxylation, and more comparable degrees of beta-blockade are noted in both metabolizer types."( Clinical pharmacology and beta-blocking efficacy of propafenone.
Barbey, JT, 1991
)
0.75
" These ventricular arrhythmias, although generally at a low rate, sometimes had the potential to degenerate into ventricular fibrillation and disappeared after both discontinuation of propafenone or increase of its dosage (1 patient)."( The use of associated propafenone in patients with amiodarone-resistant ventricular tachycardia.
Camerini, F; Chersevani, D; Dreas, L; Humar, F; Maras, P; Morgera, T, 1991
)
0.79
" The median dosage of propafenone at discharge was 300 mg/m2/day (range 250-400 mg/m2/day) every eight hours."( Experience with propafenone for the treatment of cardiac arrhythmias in children.
Celiker, A; Kahramanyol, O; Ozer, S; Ozkutlu, S; Ozme, S,
)
0.79
" Three patients reported minor side effects including nausea, dizziness and constipation that were tolerable and dosage dependent."( Propafenone in the prevention of non-ventricular arrhythmias associated with the Wolff-Parkinson-White syndrome.
Kallikazaros, I; Papoutsakis, P; Stefanadis, C; Vassiliadis, I, 1990
)
1.72
" After oral administration peak 5-hydroxy-propafenone levels were 194 +/- 65 ng/ml, whereas after intravenous dosing no metabolite was detected, except in one subject."( Comparison of the pharmacodynamic effects of intravenous and oral propafenone.
Follath, F; Ha, HR; Haefeli, EW; Vozeh, S, 1990
)
0.78
" More than 50% of all patients had these results with a daily dosage of 2 X 150 mg."( [Significance of cardiac arrhythmias in the aged and their treatment with propafenone controlled by plasma level].
Lachnit, KS; Rieder, L,
)
0.36
" Increase of the dosage to 900 mg does not improve significantly the anti-arrhythmic efficacy while the side effects seem more frequent."( [Propafenone in ventricular extrasystole in elderly patients. Tolerance and efficacy].
Baudouy, M; Benoit, P; Camous, JP; Gibelin, P; Morand, P; Schenowitz, A; Varenne, A; Vrancea, F, 1987
)
1.18
" Conduction disorders were present with a propafenone dosage or on preexisting conduction anomalies."( [Long-term study of propafenone in severe ventricular extrasystole in elderly subjects].
Diadema, B; Escande, M; Maarek-Charbit, M, 1989
)
0.86
" According to the result of the first and second control, the P dosage was increased to 600 and 900 mg for those patients who failed to show any improvement."( [Medium term study of the efficacy of propafenone in the treatment of hyperkinetic ventricular arrhythmia].
Cairo, GF; Mascelli, G; Zangara, A; Zanni, PP, 1989
)
0.55
" This dosage of propafenone did not provoke serious adverse effects in our patient."( Lidocaine, mexiletine and propafenone in the treatment of arrhythmias complicating myocardial infarction. A case report.
Aguglia, F; De Marzio, P; Gnecchi, M, 1985
)
0.92
" dosing highest levels of radioactivity were found in the lung; after oral application in the gastrointestinal tract."( Pharmacokinetics and metabolism of the antiarrhythmic agent [3H]-diprafenone in the rat.
Brunner, F; Kolmayr, U; Kukovetz, WR, 1989
)
0.28
" In 11/12 patients responsive to oral propafenone the minimum effective dosage in preventing the induction of the arrhythmia was 600 mg/day."( Paroxysmal supraventricular tachycardia: experience with propafenone.
Chiariello, M; De Paola, M; Santinelli, V; Smimmo, D; Turco, P, 1989
)
0.79
"Twenty-one patients presenting ventricular rhythm disorders and admitted to the Intensive Care Unit were treated with oral propafenone at the dosage of 450 to 900 mg/hours."( [Propafenone per os in ventricular arrhythmia].
Colas, A; Maarek-Charbit, M,
)
1.25
"Propafenone kinetics were studied after intravenous and oral dosing in a patient with end-stage renal disease."( Hemodialysis removal of propafenone.
Burgess, ED; Duff, HJ, 1989
)
2.03
" Within 20-30 min, both optical enantiomers caused a Vmax depression which occurred predominantly as a phasic blockade at a low dosage (10 mumol/l)."( Inhibitory effects of diprafenone stereoenantiomers on cardiac Na+ channels.
Fichtner, H; Kohlhardt, M, 1988
)
0.27
" 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
" Propafenone controlled dysrhythmia very well in 4 out of the ten patients, and satisfactorily in another one at a dosage ranging from 450 to 900 mg/day in 3 or 4 divided doses; this result was documented using continuous 24 hr."( [Anti-arrhythmia efficacy of propafenone per os in the prevention of paroxysmal supraventricular arrhythmia resistant to class Ia agents].
Amiel, A; Boutaud, P; Ciber, M; Demange, J; Guillem, JP; Herpin, D; Maarek-Charbit, M, 1989
)
1.48
" In this study, its dose-response relationship was examined in a double-blind, randomized, placebo-controlled five treatment parallel design protocol."( Effects of propafenone on ventricular arrhythmias: double-blind, parallel, randomized, placebo-controlled dose-ranging study.
Guerrero, J; Kaplinsky, E; Kirsten, E; Singh, BN, 1988
)
0.66
"The chemical and pharmacologic properties, pharmacokinetics, drug interactions, clinical efficacy, adverse effects, and dosage of propafenone are reviewed."( Propafenone: a new antiarrhythmic agent.
Chow, MS; Hilleman, D; Lebsack, C, 1988
)
1.92
" The same holds true for general tolerance: in 2 cases drug administration is discontinued and 11 patients present neurologic and digestive troubles improving after lowering the dosage or increasing the fractionation."( [Injectable and oral propafenone in nodal reentry and pathways of ventricular preexcitation].
Cosnay, P; Fauchier, JP; Kapusta, P; Moquet, B; Rouesnel, P; Vrancea, F, 1986
)
0.59
" Long-term oral therapy at the same dosage level prevented recurrences of VT in 7 out of 14 patients; the drug was discontinued in 2 patients owing to its arrhythmogenic effect on induced VT."( [Treatment of ventricular tachycardia with propafenone. Parallel study of ventricular provocation tests].
Balleh, H; Cosnay, P; Faućhier, JP; Huguet, R; Moquet, B; Rouesnel, P; Van Viet, H, 1987
)
0.54
" Dosage must be individualised because of dose-dependent pharmacokinetics, a wide range of clinically effective plasma concentrations (64 to 3271 micrograms/L) after comparable doses, the presence of an active metabolite (5-hydroxy-propafenone) and genetically determined metabolic oxidation."( Propafenone. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in the treatment of arrhythmias.
Brogden, RN; Harron, DW, 1987
)
1.9
" dosing in selected patients."( Pharmacokinetics and pharmacodynamics of propafenone during acute and chronic administration.
Bianchini, C; Ferrario, G; Giani, P; Giudici, V; Landolina, M; Latini, R; Marchi, S; Riva, E, 1988
)
0.54
" To determine the potential asthmogenicity of this new drug, pulmonary function, airway reactivity to methacholine, blood pressure, the electrocardiogram, and plasma concentrations were measured in 12 patients with mild intermittent asthma after 48 to 72 hours of treatment with placebo and with oral propafenone in low dosage (150 mg every eight hours) and high dosage (300 mg every eight hours) in a double-blind crossover manner."( Evaluation of the asthmogenicity of propafenone, a new antiarrhythmic drug. Comparison of spirometry with methacholine challenge.
Gotz, VP; Harman, E; Hendeles, L; Hill, MR; McLeod, I, 1986
)
0.72
" Patients with abnormal liver function probably will require treatment with propafenone for cardiac arrhythmias; an understanding of the relationship between liver function and the pharmacokinetics of propafenone will provide a rational basis for optimal dosage adjustments in these individuals."( Influence of hepatic dysfunction on the pharmacokinetics of propafenone.
Dorian, P; Kates, RE; Lee, JT; Yee, YG,
)
0.6
" 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
" The average daily dosage was 600 mg for propafenon and 180 mg for lidoflazine."( [Combined use of propafenon and lidoflazine in chronic atrial fibrillation and flutter (author's transl)].
Beck, OA; Hochrein, H, 1980
)
0.26
"Propafenone, three times 150 mg/d over 33 days and two years later at the same dosage over six days, was administered to an 84-year-old man with ventricular extrasystoles (Lown IVa)."( [Cholestasis after antiarrhythmic therapy with propafenone].
Berg, PA; Konz, KH; Seipel, L, 1984
)
1.97
"The effects of orally administered propafenone on ejection fraction (EF) determined by radionuclide angiography were studied in 2 groups of patients receiving different dosing regimens."( Effect of propafenone on left ventricular ejection fraction.
Baker, BJ; de Soyza, ND; Dinh, H; Franciosa, JA; Kroskey, D; Murphy, ML, 1984
)
0.95
" The remaining side effects, if present, were tolerated, and dosage dependent."( Effect of propafenone in the Wolff-Parkinson-White syndrome: electrophysiologic findings and long-term follow-up.
Borggrefe, M; Breithardt, G; Seipel, L; Wiebringhaus, E, 1984
)
0.67
" Propafenone undergoes extensive presystemic clearance that appears to be saturable, with bioavailability increasing as dosage increases."( Clinical pharmacology of propafenone: pharmacokinetics, metabolism and concentration-response relations.
Roden, DM; Siddoway, LA; Woosley, RL, 1984
)
1.48
" The latter, however, was taking antiarrhythmic drugs at a dosage less than that proved to be effective during electropharmacological testing."( [Value of a serial electropharmacologic study in survivors of a cardiac arrest secondary to ventricular tachycardia or ventricular fibrillation].
Delise, P; Di Pede, F; Piccolo, E; Raviele, A, 1984
)
0.27
" After 12 days of oral dosing (2 tablets of 150 mg propafenone daily) no statistically significant changes of kinetic parameters could be demonstrated although with some volunteers the total clearance decreased."( Investigations on the pharmacokinetics of propafenone in man.
Brode, E; Hollmann, M; Hotz, D; Kaumeier, S; Kehrhahn, OH, 1983
)
0.78
" Dosage and serum levels of propafenone did not differ whether the patients were treated successfully or not."( Clinical experience with propafenone for cardiac arrhythmias in the young.
Bourgeous, M; Heusch, A; Kramer, HH; Krogmann, ON; Rammos, S, 1994
)
0.89
" The pharmacokinetic profile of propafenone is complex, characterised as typically nonlinear, saturable, stereoselective and dependent on both dose and debrisoquin metaboliser phenotype; individualised dosage titration is required."( Propafenone. A reappraisal of its pharmacology, pharmacokinetics and therapeutic use in cardiac arrhythmias.
Bryson, HM; Fitton, A; Langtry, HD; Palmer, KJ, 1993
)
2.01
"Six dogs were anaesthetized with 1% of halothane-Group I, and six dogs with an equianaesthetic dosage of isoflurane (1."( [Hemodynamic effects of propafenone in dogs anesthesized with halothane or isoflurane].
Castro, G; Figueiredo, F; Fonseca, P; Freitas, M; Godinho, AM; Morais, J; Providência, LA; Viana, Jda S, 1994
)
0.6
" The drug was administered, at a dosage of 2 mg/kg, to 46 consecutive patients (with age variable from 35 to 86 years), 36 with atrial fibrillation, 10 with atrial flutter."( [Efficacy of intravenous propafenone in the management of arterial flutter and fibrillation of recent onset].
Minutiello, L, 1994
)
0.59
" After establishing an HPLC assay, urinary excretion of PPFG was quantified during one dosage interval and related to individual CYP2D6 activity as determined by phenotyping."( Rapid determination of CYP2D6 phenotype during propafenone therapy by analysing urinary excretion of propafenone glucuronides.
Botsch, S; Eichelbaum, M; Heinkele, G; Kroemer, HK; Meese, CO, 1994
)
0.55
" During A treatment (average daily dosage 216 mg) 32% of patients had reported more than two episodes of AF, 52% one or two episodes, and 16 none during the last 6 months."( [Prevention of paroxysmal atrial fibrillation with propafenone after withdrawal of amiodarone because of side effects].
Foscoli, M; Giofrè, R; Labriola, E; Lolli, C; Tarquinii, M; Toschi, GP, 1993
)
0.54
"0 years) with hyperkinetic ventricular arrhythmias were treated for 30 days with 150 mg propafenone three times daily; the daily dosage was raised to 900 mg in non responders (< 85% reduction of ectopic ventricular beats/h)."( [Evaluation of the anti-arrhythmic action of propafenone treatment and its influence on left ventricular function].
Bonaiuto, M; Cinquegrani, M; Fodale, P; Giordano, G; Mileto, A; Oriti, S; Saitta, A; Saitta, M; Squadrito, F, 1993
)
0.77
" Despite a decrease in theophylline dosage, theophylline concentrations continued to rise as the dosage of propafenone was increased to 300 mg every 8 hours."( Propafenone-theophylline interaction.
Charland, SL; Gammaitoni, A; Hurwitz, J; Spinler, SA,
)
1.79
" At each visit, medical events, vital sign measurements (blood pressure, pulse rate), concomitant medications, adverse experiences, and study drug dosage changes were evaluated."( Comparison of the safety and efficacy of flecainide versus propafenone in hospital out-patients with symptomatic paroxysmal atrial fibrillation/flutter. The Flecainide AF French Study Group.
Aliot, E; Denjoy, I, 1996
)
0.54
" The results of the eight drugs revealed that ciliary movement is frequently affected by many drugs and, therefore, care must be taken in developing any nasal dosage form to ensure its least ciliotoxicity."( [Toxicity of drugs on nasal mucocilia and the method of its evaluation].
Cui, JB; Fang, XL; Jiang, XG; Wei, Y; Xi, NZ, 1995
)
0.29
" Oral propafenone at a low dosage 150 mg 3 times daily is well tolerated and effective in maintaining sinus rhythm for 6 months after pharmacologic or electrical restoration of sinus rhythm."( Propafenone for conversion and prophylaxis of atrial fibrillation. Propafenone Atrial Fibrillation Trial Investigators.
Hoebrechts, R; Stiels, B; Stroobandt, R, 1997
)
2.22
" Best results were obtained by using a combined simultaneous analysis of dose-response curve families."( Estimation of the chemosensitizing activity of modulators of multi-drug resistance via combined simultaneous analysis of sigmoidal dose-response curves.
Chiba, P; Ecker, G; Schaper, KJ, 1997
)
0.3
" Little justification for the use of agents or dosing in children is available."( Pharmacologic management of supraventricular tachycardias in children. Part 1: Wolff-Parkinson-White and atrioventricular nodal reentry.
Kuhn, RJ; Luedtke, SA; McCaffrey, FM, 1997
)
0.3
" Additional well-designed, controlled trials are needed to further evaluate the comparative efficacy of antiarrhythmics in the management of WPW and AVNRT in children, as well as to evaluate dosing and toxicity in various age groups."( Pharmacologic management of supraventricular tachycardias in children. Part 1: Wolff-Parkinson-White and atrioventricular nodal reentry.
Kuhn, RJ; Luedtke, SA; McCaffrey, FM, 1997
)
0.3
" The dosage from 50 to 100 mg/day made no difference."( Preliminary study of the effects of metoprolol and propafenone on ventricular arrhythmia with positive ventricular late potential.
Duan, Y; Gao, E; Li, H; Yang, C; Zhou, Y, 1997
)
0.55
" During the last dosing interval the plasma concentrations of both enantiomers of propafenone were measured and ECG, blood pressure (MAP) and heart rate were monitored."( Stereoselective steady state disposition and action of propafenone in Chinese subjects.
Gong, PL; Klotz, U; Li, G; Qiu, J; Zeng, FD, 1998
)
0.77
" During dosing with racemic propafenone CLO of (S)- and (R)-propafenone averaged (+/-s."( Stereoselective steady state disposition and action of propafenone in Chinese subjects.
Gong, PL; Klotz, U; Li, G; Qiu, J; Zeng, FD, 1998
)
0.84
" The results indicate that dosage adjustments are probably not required in Chinese patients receiving propafenone."( Stereoselective steady state disposition and action of propafenone in Chinese subjects.
Gong, PL; Klotz, U; Li, G; Qiu, J; Zeng, FD, 1998
)
0.76
" There appeared to be a dose-response relationship between Ic dose and its effects on QTc prolongation."( The actions of ibutilide and class Ic drugs on the slow sodium channel: new insights regarding individual pharmacologic effects elucidated through combination therapies.
Blitzer, M; Reiffel, JA, 2000
)
0.31
" The close temporal relationship between the administration of the drug and the acute onset of signs of liver injury, the marked rise in liver function tests following the increase of the drug dosage and their gradual normalization after its withdrawal strongly suggest that propafenone is involved in the pathogenesis of this syndrome."( [Hepatic toxicity of propafenone: a case description].
La Brocca, A,
)
0.63
" Two different propafenone dosage regimens were used according to the duration of the presenting arrhythmia: patients with paroxysmal arrhythmia (n = 48) received 600 mg loading dose, and patients with chronic arrhythmia (n = 56) were receiving 150 mg three times a day as stable-dose pre-treatment."( Ibutilide added to propafenone for the conversion of atrial fibrillation and atrial flutter.
Chiladakis, JA; Kalogeropoulos, A; Manolis, AS; Patsouras, N, 2004
)
1
" These results are consistent with previous reports for solid dosage forms."( Bioavailability of an extemporaneous suspension of propafenone made from tablets.
Chávez, JB; Mendiola, BR; Olguín, HJ; Pérez, CF; Pérez, JF; Portugal, MC, 2006
)
0.59
"With the dosage used in the present study, the efficacy on terminating PSVT was comparable between AHH and PRO."( [Efficacy of intravenous Acehytisine Hydrochloride versus propafenone on terminating paroxysmal supraventricular tachycardia: a double-blinded, randomized multi-center study].
Gao, X; Li, JD; Liu, JH; Yang, YM; Yang, ZM; Zhu, J, 2007
)
0.58
" Four weeks later, because of the persistence of psychiatric disturbance, the venlafaxine dosage was increased to 150 mg/day."( Venlafaxine-propafenone interaction resulting in hallucinations and psychomotor agitation.
Cotroneo, A; Davoli, A; De Fazio, P; De Fazio, S; De Sarro, G; Gallelli, L; Gareri, P; Seminara, G, 2008
)
0.72
" A rare phenomenon in which toxicity occurred at therapeutic dosing is reported."( Acute propafenone toxicity after two exposures at standard dosing.
Gin, K; Parwana, H; Shanks, D; Yeung, A,
)
0.61
" These acute findings may have been consequent to an increased dosage of propafenone combined with heavy alcohol consumption that led to decreased metabolism of propafenone."( Syncope, widened QRS interval, and left ventricular systolic depression: coincident with propafenone therapy for atrial fibrillation.
Grodman, R; Isber, N; Samaan, RA; Sobamowo, HO; Tamburrino, F, 2010
)
0.81
" For each drug, 6 healthy male volunteers were dosed with 100 μg (14)C-labelled compound."( Comparative pharmacokinetics between a microdose and therapeutic dose for clarithromycin, sumatriptan, propafenone, paracetamol (acetaminophen), and phenobarbital in human volunteers.
Alder, J; Bjerrum, OJ; Brian Houston, J; Garner, C; Gesson, C; Grynkiewicz, G; Jochemsen, R; Lappin, G; Oosterhuis, B; Rowland, M; Shishikura, Y; Weaver, RJ, 2011
)
0.58
"The development of a sustained-release formulation of propafenone allowed to reduce the wide fluctuations in plasma levels observed with the immediate release preparation, improving compliance and adherence to therapy, by simplifying the dosing regimen from 3 to 2 daily doses."( Atrial fibrillation and the pharmacological treatment: the role of propafenone.
Molina, E; Sestito, A, 2012
)
0.86
"0078 mg/kg/min for 120 min and orally in dosage of 300 mg three times every 8 hours if arrhythmia persisted."( Effect of selective beta-blockade with bisoprolol in the treatment of recent-onset atrial fibrillation.
Negreva, MN; Penev, AP,
)
0.13
" Except for the dosage of noradrenaline (0."( Propafenone for supraventricular arrhythmias in septic shock-Comparison to amiodarone and metoprolol.
Balik, M; Kolnikova, I; Kristof, J; Maly, M; Tavazzi, G; Waldauf, P, 2017
)
1.9
" This finding enables us to improve the accuracy of dosage administration and reduce the risk of medication errors affecting the paediatric population."( Formulation and stability of an extemporaneously compounded propafenone hydrochloride oral suspension for children with arrhythmia.
Hsieh, YT; Huang, CF; Lin, CH; Lin, SC; Lin, YS; Liu, LY; Shen, LJ, 2022
)
0.96
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
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.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
secondary alcoholA secondary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has two other carbon atoms attached to it.
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic 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 (61)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.67830.100020.879379.4328AID588453; AID588456
RAR-related orphan receptor gammaMus musculus (house mouse)Potency29.84930.006038.004119,952.5996AID1159521; AID1159523
Fumarate hydrataseHomo sapiens (human)Potency33.17340.00308.794948.0869AID1347053
TDP1 proteinHomo sapiens (human)Potency10.15530.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency5.34330.000714.592883.7951AID1259369; AID1259392
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency26.60320.000657.913322,387.1992AID1259378
regulator of G-protein signaling 4Homo sapiens (human)Potency0.60610.531815.435837.6858AID504845
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.45450.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency23.10190.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency29.84930.003041.611522,387.1992AID1159552
retinoid X nuclear receptor alphaHomo sapiens (human)Potency26.08200.000817.505159.3239AID1159527; AID1159531
estrogen nuclear receptor alphaHomo sapiens (human)Potency29.84930.000229.305416,493.5996AID743079
cytochrome P450 2D6Homo sapiens (human)Potency0.09770.00108.379861.1304AID1645840
polyproteinZika virusPotency33.17340.00308.794948.0869AID1347053
thyroid stimulating hormone receptorHomo sapiens (human)Potency29.84930.001628.015177.1139AID1259385
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency25.37350.057821.109761.2679AID1159526; AID1159528
D(1A) dopamine receptorHomo sapiens (human)Potency10.00000.02245.944922.3872AID488983
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency1.41250.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency24.41260.000323.4451159.6830AID743065; AID743067
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency21.30160.00378.618923.2809AID2667; AID2668
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency10.59010.000627.21521,122.0200AID743202
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency17.78360.005612.367736.1254AID624032; AID624044
survival motor neuron protein isoform dHomo sapiens (human)Potency2.23870.125912.234435.4813AID1458
lamin isoform A-delta10Homo sapiens (human)Potency17.78280.891312.067628.1838AID1487
Cellular tumor antigen p53Homo sapiens (human)Potency16.78550.002319.595674.0614AID651631
D(1A) dopamine receptorSus scrofa (pig)Potency16.48160.00378.108123.2809AID2667
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
Ataxin-2Homo sapiens (human)Potency17.78280.011912.222168.7989AID588378
[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)
Potassium channel subfamily K member 3Homo sapiens (human)IC50 (µMol)5.10000.00700.89855.1000AID1307734
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)13.32000.21005.553710.0000AID1442001; AID386625
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
ATP-binding cassette sub-family C member 9Homo sapiens (human)IC50 (µMol)2.20000.22001.56004.3000AID630546
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC50 (µMol)0.38400.00011.00768.7800AID625218
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.20100.00000.887110.0000AID625218
Potassium channel subfamily K member 2Homo sapiens (human)IC50 (µMol)7.60000.40003.92279.0000AID1307730
Bile salt export pumpHomo sapiens (human)IC50 (µMol)93.35000.11007.190310.0000AID1449628; AID1473738
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)3.29200.00011.774010.0000AID625245
Beta-2 adrenergic receptorHomo sapiens (human)IC50 (µMol)0.05200.00020.93267.2000AID625205
Beta-2 adrenergic receptorHomo sapiens (human)Ki0.03600.00000.66359.5499AID625205
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC50 (µMol)3.01600.00041.877310.0000AID625207
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki2.99100.00322.28879.3160AID625207
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)0.33110.00022.318510.0000AID672543
ATP-dependent translocase ABCB1Homo sapiens (human)Ki4.20000.02002.35948.5900AID150616
Beta-1 adrenergic receptorHomo sapiens (human)IC50 (µMol)0.35400.00021.46819.0000AID625204
Beta-1 adrenergic receptorHomo sapiens (human)Ki0.20500.00011.33919.9840AID625204
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)4.60340.00002.015110.0000AID625249
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)50.00000.00002.800510.0000AID1210069
Beta-3 adrenergic receptorHomo sapiens (human)IC50 (µMol)0.42400.00233.24158.0600AID625206
Beta-3 adrenergic receptorHomo sapiens (human)Ki0.31800.00302.30986.0450AID625206
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)1.63700.00031.38338.4000AID625190
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.93500.00010.739610.0000AID625190
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC50 (µMol)3.01600.00081.541620.0000AID625207
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki2.99100.00031.465610.0000AID625207
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)0.65400.00010.88018.8500AID625192
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.18700.00000.385510.0000AID625192
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)0.38400.00011.03029.0000AID625218
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.20100.00010.954910.0000AID625218
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)1.63700.00051.48357.8000AID625190
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.93500.00031.29679.2440AID625190
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)0.09200.00011.18738.9125AID625217
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.05800.00030.769310.0000AID625217
5-hydroxytryptamine receptor 6Homo sapiens (human)IC50 (µMol)1.86300.00170.83815.4200AID625221
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.86500.00020.522910.0000AID625221
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC50 (µMol)11.10002.03005.53139.9000AID386625
Cytochrome P450 2J2Homo sapiens (human)IC50 (µMol)50.00000.01202.53129.4700AID1210069
Sodium-dependent dopamine transporter Homo sapiens (human)IC50 (µMol)1.86800.00071.841946.0000AID625256
Sodium-dependent dopamine transporter Homo sapiens (human)Ki1.48400.00021.11158.0280AID625256
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)1.37330.00091.901410.0000AID1207226; AID240820; AID630543
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC50 (µMol)3.16330.00033.64849.2000AID1207167; AID630544; AID630545
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)IC50 (µMol)2.20000.00431.36868.2000AID630546
Lanosterol 14-alpha demethylaseHomo sapiens (human)IC50 (µMol)200.00000.05001.43904.0000AID322753
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)2.61000.00030.70285.3660AID625223
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki1.09700.00000.490110.0000AID625223
[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)
ATP-dependent translocase ABCB1Homo sapiens (human)EC50 (µMol)0.32670.01600.67863.1000AID210307; AID281137; AID781331
Nuclear receptor subfamily 2 group E member 1Homo sapiens (human)EC50 (µMol)47.00005.00005.00005.0000AID1810681
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (500)

Processvia Protein(s)Taxonomy
potassium ion transportPotassium channel subfamily K member 3Homo sapiens (human)
chemical synaptic transmissionPotassium channel subfamily K member 3Homo sapiens (human)
response to xenobiotic stimulusPotassium channel subfamily K member 3Homo sapiens (human)
monoatomic ion transmembrane transportPotassium channel subfamily K member 3Homo sapiens (human)
negative regulation of cytosolic calcium ion concentrationPotassium channel subfamily K member 3Homo sapiens (human)
regulation of resting membrane potentialPotassium channel subfamily K member 3Homo sapiens (human)
cellular response to zinc ionPotassium channel subfamily K member 3Homo sapiens (human)
cellular response to hypoxiaPotassium channel subfamily K member 3Homo sapiens (human)
cochlea developmentPotassium channel subfamily K member 3Homo sapiens (human)
potassium ion transmembrane transportPotassium channel subfamily K member 3Homo sapiens (human)
stabilization of membrane potentialPotassium channel subfamily K member 3Homo sapiens (human)
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
defense response to virusATP-binding cassette sub-family C member 9Homo sapiens (human)
action potentialATP-binding cassette sub-family C member 9Homo sapiens (human)
heart morphogenesisATP-binding cassette sub-family C member 9Homo sapiens (human)
response to xenobiotic stimulusATP-binding cassette sub-family C member 9Homo sapiens (human)
response to ATPATP-binding cassette sub-family C member 9Homo sapiens (human)
negative regulation of blood pressureATP-binding cassette sub-family C member 9Homo sapiens (human)
fibroblast proliferationATP-binding cassette sub-family C member 9Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
coronary vasculature developmentATP-binding cassette sub-family C member 9Homo sapiens (human)
cardiac conductionATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium ion transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
cardiac muscle cell contractionATP-binding cassette sub-family C member 9Homo sapiens (human)
monoatomic cation transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
inorganic cation transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium ion import across plasma membraneATP-binding cassette sub-family C member 9Homo sapiens (human)
cardiac ventricle developmentPotassium channel subfamily K member 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayPotassium channel subfamily K member 2Homo sapiens (human)
memoryPotassium channel subfamily K member 2Homo sapiens (human)
response to mechanical stimulusPotassium channel subfamily K member 2Homo sapiens (human)
response to axon injuryPotassium channel subfamily K member 2Homo sapiens (human)
negative regulation of cardiac muscle cell proliferationPotassium channel subfamily K member 2Homo sapiens (human)
cellular response to hypoxiaPotassium channel subfamily K member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium channel subfamily K member 2Homo sapiens (human)
cochlea developmentPotassium channel subfamily K member 2Homo sapiens (human)
positive regulation of cellular response to hypoxiaPotassium channel subfamily K member 2Homo sapiens (human)
negative regulation of DNA biosynthetic processPotassium channel subfamily K member 2Homo sapiens (human)
stabilization of membrane potentialPotassium channel subfamily K member 2Homo 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)
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)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
diet induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
regulation of sodium ion transportBeta-2 adrenergic receptorHomo sapiens (human)
transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-2 adrenergic receptorHomo sapiens (human)
smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
cell surface receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
endosome to lysosome transportBeta-2 adrenergic receptorHomo sapiens (human)
response to coldBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase A signalingBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of bone mineralizationBeta-2 adrenergic receptorHomo sapiens (human)
heat generationBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-2 adrenergic receptorHomo sapiens (human)
bone resorptionBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of mini excitatory postsynaptic potentialBeta-2 adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of autophagosome maturationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of lipophagyBeta-2 adrenergic receptorHomo sapiens (human)
cellular response to amyloid-betaBeta-2 adrenergic receptorHomo sapiens (human)
response to psychosocial stressBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cAMP-dependent protein kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of AMPA receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-2 adrenergic receptorHomo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
response to coldBeta-1 adrenergic receptorHomo sapiens (human)
heat generationBeta-1 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-1 adrenergic receptorHomo sapiens (human)
fear responseBeta-1 adrenergic receptorHomo sapiens (human)
regulation of circadian sleep/wake cycle, sleepBeta-1 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-1 adrenergic receptorHomo sapiens (human)
regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-1 adrenergic receptorHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo 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)
receptor-mediated endocytosisBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
carbohydrate metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
generation of precursor metabolites and energyBeta-3 adrenergic receptorHomo sapiens (human)
energy reserve metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
response to coldBeta-3 adrenergic receptorHomo sapiens (human)
heat generationBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-3 adrenergic receptorHomo sapiens (human)
eating behaviorBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-3 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-3 adrenergic receptorHomo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
cerebral cortex cell migration5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of TOR signaling5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 6Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 6Homo 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)
monoamine transportSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent dopamine transporter Homo sapiens (human)
lactationSodium-dependent dopamine transporter Homo sapiens (human)
sensory perception of smellSodium-dependent dopamine transporter Homo sapiens (human)
locomotory behaviorSodium-dependent dopamine transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent dopamine transporter Homo sapiens (human)
response to iron ionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine transportSodium-dependent dopamine transporter Homo sapiens (human)
adenohypophysis developmentSodium-dependent dopamine transporter Homo sapiens (human)
response to nicotineSodium-dependent dopamine transporter Homo sapiens (human)
positive regulation of multicellular organism growthSodium-dependent dopamine transporter Homo sapiens (human)
regulation of dopamine metabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to cocaineSodium-dependent dopamine transporter Homo sapiens (human)
dopamine biosynthetic processSodium-dependent dopamine transporter Homo sapiens (human)
dopamine catabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to ethanolSodium-dependent dopamine transporter Homo sapiens (human)
cognitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent dopamine transporter Homo sapiens (human)
response to cAMPSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
prepulse inhibitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
hyaloid vascular plexus regressionSodium-dependent dopamine transporter Homo sapiens (human)
amino acid transportSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine transportSodium-dependent dopamine transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent dopamine transporter 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)
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)
action potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to hypoxiaATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to ischemiaATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ventricular cardiac muscle tissue developmentATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
glucose metabolic processATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
apoptotic processATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
determination of adult lifespanATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to xenobiotic stimulusATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to estradiolATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to ATPATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to testosteroneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of membrane potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
negative regulation of insulin secretionATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of insulin secretionATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
nervous system processATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
CAMKK-AMPK signaling cascadeATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cellular response to nicotineATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cellular response to glucose stimulusATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cellular response to tumor necrosis factorATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
potassium ion transmembrane transportATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
inorganic cation transmembrane transportATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of presynaptic membrane potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
positive regulation of protein localization to plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to resveratrolATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
potassium ion import across plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of monoatomic ion transmembrane transportATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
steroid biosynthetic processLanosterol 14-alpha demethylaseHomo sapiens (human)
cholesterol biosynthetic processLanosterol 14-alpha demethylaseHomo sapiens (human)
sterol metabolic processLanosterol 14-alpha demethylaseHomo sapiens (human)
negative regulation of protein catabolic processLanosterol 14-alpha demethylaseHomo sapiens (human)
negative regulation of protein secretionLanosterol 14-alpha demethylaseHomo sapiens (human)
negative regulation of amyloid-beta clearanceLanosterol 14-alpha demethylaseHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo 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)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
angiogenesisNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
behavioral fear responseNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
positive regulation of neuroblast proliferationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
aggressive behaviorNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
apoptotic processNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
nervous system developmentNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
neuroblast proliferationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
visual perceptionNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
dentate gyrus developmentNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
amygdala developmentNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
olfactory bulb developmentNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
layer formation in cerebral cortexNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
forebrain generation of neuronsNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
cerebral cortex neuron differentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
anterior commissure morphogenesisNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
extracellular matrix organizationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
somatic stem cell population maintenanceNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
social behaviorNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
negative regulation of apoptotic processNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
steroid hormone mediated signaling pathwayNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
astrocyte cell migrationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
cell fate commitmentNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
negative regulation of neuron differentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
positive regulation of angiogenesisNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
positive regulation of cell cycleNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor subfamily 2 group E member 1Homo sapiens (human)
astrocyte differentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
negative regulation of astrocyte differentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
regulation of dendrite morphogenesisNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
retina development in camera-type eyeNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
regulation of timing of neuron differentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
long-term synaptic potentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
regulation of cell migration involved in sprouting angiogenesisNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
negative regulation of neural precursor cell proliferationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
positive regulation of stem cell proliferationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
anatomical structure developmentNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 2 group E member 1Homo sapiens (human)
cell differentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (178)

Processvia Protein(s)Taxonomy
monoatomic ion channel activityPotassium channel subfamily K member 3Homo sapiens (human)
open rectifier potassium channel activityPotassium channel subfamily K member 3Homo sapiens (human)
potassium channel activityPotassium channel subfamily K member 3Homo sapiens (human)
potassium ion leak channel activityPotassium channel subfamily K member 3Homo sapiens (human)
S100 protein bindingPotassium channel subfamily K member 3Homo sapiens (human)
outward rectifier potassium channel activityPotassium channel subfamily K member 3Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic cation channel activityATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium channel activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-binding cassette sub-family C member 9Homo sapiens (human)
transmembrane transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 9Homo sapiens (human)
sulfonylurea receptor activityATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium channel regulator activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
transmembrane transporter bindingATP-binding cassette sub-family C member 9Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
outward rectifier potassium channel activityPotassium channel subfamily K member 2Homo sapiens (human)
potassium ion leak channel activityPotassium channel subfamily K member 2Homo 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)
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 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo 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 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
amyloid-beta bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta2-adrenergic receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase bindingBeta-2 adrenergic receptorHomo sapiens (human)
potassium channel regulator activityBeta-2 adrenergic receptorHomo sapiens (human)
identical protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-2 adrenergic receptorHomo sapiens (human)
protein-containing complex bindingBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-2 adrenergic receptorHomo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
beta-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
beta1-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
protein bindingBeta-1 adrenergic receptorHomo sapiens (human)
PDZ domain bindingBeta-1 adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingBeta-1 adrenergic receptorHomo sapiens (human)
protein heterodimerization activityBeta-1 adrenergic receptorHomo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo 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 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo 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)
norepinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
protein bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta3-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
beta-3 adrenergic receptor bindingBeta-3 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-3 adrenergic receptorHomo sapiens (human)
epinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
histamine receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 6Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 6Homo 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)
protease bindingSodium-dependent dopamine transporter Homo sapiens (human)
signaling receptor bindingSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
protein bindingSodium-dependent dopamine transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine bindingSodium-dependent dopamine transporter Homo sapiens (human)
amine bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein-containing complex bindingSodium-dependent dopamine transporter Homo sapiens (human)
metal ion bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein phosphatase 2A bindingSodium-dependent dopamine transporter Homo sapiens (human)
heterocyclic compound bindingSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent dopamine transporter 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 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)
voltage-gated potassium channel activityATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
protein bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ATP bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activityATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ankyrin bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
potassium ion bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
heat shock protein bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
transmembrane transporter bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
iron ion bindingLanosterol 14-alpha demethylaseHomo sapiens (human)
sterol 14-demethylase activityLanosterol 14-alpha demethylaseHomo sapiens (human)
heme bindingLanosterol 14-alpha demethylaseHomo sapiens (human)
oxidoreductase activityLanosterol 14-alpha demethylaseHomo 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 oxygenLanosterol 14-alpha demethylaseHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo 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)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
nuclear steroid receptor activityNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
protein bindingNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
zinc ion bindingNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
histone deacetylase bindingNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
nuclear receptor activityNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (93)

Processvia Protein(s)Taxonomy
plasma membranePotassium channel subfamily K member 3Homo sapiens (human)
synapsePotassium channel subfamily K member 3Homo sapiens (human)
plasma membranePotassium channel subfamily K member 3Homo sapiens (human)
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 9Homo sapiens (human)
sarcomereATP-binding cassette sub-family C member 9Homo sapiens (human)
inward rectifying potassium channelATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium ion-transporting ATPase complexATP-binding cassette sub-family C member 9Homo sapiens (human)
membraneATP-binding cassette sub-family C member 9Homo sapiens (human)
endoplasmic reticulum membranePotassium channel subfamily K member 2Homo sapiens (human)
plasma membranePotassium channel subfamily K member 2Homo sapiens (human)
cell surfacePotassium channel subfamily K member 2Homo sapiens (human)
apical plasma membranePotassium channel subfamily K member 2Homo sapiens (human)
neuronal cell bodyPotassium channel subfamily K member 2Homo sapiens (human)
calyx of HeldPotassium channel subfamily K member 2Homo sapiens (human)
astrocyte projectionPotassium channel subfamily K member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium channel subfamily K member 2Homo sapiens (human)
plasma membranePotassium channel subfamily K member 2Homo 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)
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 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
nucleusBeta-2 adrenergic receptorHomo sapiens (human)
lysosomeBeta-2 adrenergic receptorHomo sapiens (human)
endosomeBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-2 adrenergic receptorHomo sapiens (human)
Golgi apparatusBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
endosome membraneBeta-2 adrenergic receptorHomo sapiens (human)
membraneBeta-2 adrenergic receptorHomo sapiens (human)
apical plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneBeta-2 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-2 adrenergic receptorHomo sapiens (human)
receptor complexBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
early endosomeBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
Schaffer collateral - CA1 synapseBeta-1 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo 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 membraneBeta-3 adrenergic receptorHomo sapiens (human)
receptor complexBeta-3 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cilium5-hydroxytryptamine receptor 6Homo sapiens (human)
synapse5-hydroxytryptamine receptor 6Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
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
cytoplasmSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
cell surfaceSodium-dependent dopamine transporter Homo sapiens (human)
membraneSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
neuron projectionSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell bodySodium-dependent dopamine transporter Homo sapiens (human)
axon terminusSodium-dependent dopamine transporter Homo sapiens (human)
membrane raftSodium-dependent dopamine transporter Homo sapiens (human)
postsynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
dopaminergic synapseSodium-dependent dopamine transporter Homo sapiens (human)
flotillin complexSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
presynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent dopamine transporter 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)
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)
acrosomal vesicleATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
nuclear envelopeATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
endosomeATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
inward rectifying potassium channelATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
intercalated discATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
T-tubuleATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
axolemmaATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
presynaptic membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
neuronal cell bodyATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cell body fiberATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
glutamatergic synapseATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
endoplasmic reticulum membraneLanosterol 14-alpha demethylaseHomo sapiens (human)
membraneLanosterol 14-alpha demethylaseHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo 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)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
nucleoplasmNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
chromatinNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (364)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
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.
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.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508628Confirmatory 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.
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.
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.
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.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
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.
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.
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.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
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.
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.
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.
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.
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.
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.
AID1582078Metabolic stability in human liver microsomes assessed as intrinsic clearance at 10 uM incubated for 1 hr2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Discovery and Characterization of 1
AID1736740Metabolic stability in human liver microsomes assessed as intrinsic clearance incubated for 1 hr by LC/MS/MS method2020European journal of medicinal chemistry, Mar-15, Volume: 190Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.
AID696476Permeability of the compound at 10 uM at pH 7.4 by PAMPA2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Lead optimization of antimalarial propafenone analogues.
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.
AID1718808Metabolic stability in CD-1 mouse liver microsomes assessed as parent compound remaining at 100 uM measured after 60 mins in presence of NADPH by LC-MS/MS analysis
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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]
AID1582081Metabolic stability in CD1 mouse liver microsomes assessed as intrinsic clearance at 10 uM incubated for 1 hr2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Discovery and Characterization of 1
AID1355799Metabolic stability in human liver microsomes assessed as compound remaining after 60 mins in presence of NADPH by LC/MS/MS analysis2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID150616Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1524890Intrinsic clearance in human liver microsomes further incubated of 5 to 60 mins in presence of NADPH regenerating system by LC/MS analysis2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Discovery of novel pyrazole derivatives as potential anticancer agents in MCL.
AID1207689Inhibition 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.
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.
AID1211794Fraction unbound in blood (not specified)2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1571694Intrinsic clearance in human liver microsomes assessed per mg protein in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID1810681Agonist activity at in human TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP 16 assessed as increase in reporter activity measured after 14 hrs by luciferase reporter gene assay relative to control2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells.
AID630462Inhibition of KvLQT/minK at 10 uM after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID1355798Intrinsic clearance in human liver after 10 mins in presence of NADPH by LC/MS/MS analysis2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1718811Metabolic stability in CD-1 mouse liver microsomes assessed as half-life at 100 uM measured after 60 mins in presence of NADPH by LC-MS/MS analysis
AID1744366Half life in human liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID630553Solubility of the compound in phosphate buffered saline by UV spectrophotometry2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID324578Effect on 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.
AID1593391Stability in human liver microsomes assessed as parent compound remaining measured after 60 mins2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID1779259Metabolic stability in human liver microsome assessed as half life2021European journal of medicinal chemistry, Oct-05, Volume: 221Discovery of hydrazide-containing oseltamivir analogues as potent inhibitors of influenza A neuraminidase.
AID1887671Metabolic stability in human liver microsome assessed as parent compound remaining at 100 uM measured after 60 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.
AID19006Calculated membrane partition coefficient (Kmemb)2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
AID696479Intrinsic clearance in human liver microsomes at 2 mM2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Lead optimization of antimalarial propafenone analogues.
AID1736739Metabolic stability in human liver microsomes assessed as half life incubated for 1 hr by LC/MS/MS method2020European journal of medicinal chemistry, Mar-15, Volume: 190Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.
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.
AID112269ED 50 value against aconitine-induced arrhythmias in mice1986Journal of medicinal chemistry, Feb, Volume: 29, Issue:2
Antiarrhythmic activity of 17 beta-aminoestratrienes. Comparison of 3-ols and 3-acetates with the corresponding 3-(3-amino-2-hydroxypropyl) ethers.
AID1744368Intrinsic clearance in human liver at 1 uM in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID630547Therapeutic index, ratio of IC50 for human ERG expressed in CHO cells to EC50 for chloroquine-resistant Plasmodium falciparum K12011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID696474Inhibition of CYP2D6 in human liver microsomes at 1 uM after 20 mins by LC-MS/MS analysis relative to control2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Lead optimization of antimalarial propafenone analogues.
AID1876431Metabolic stability in human liver microsomes assessed as half life2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.
AID1307734Inhibition of of TASK1 (unknown origin) expressed in CHO cells assessed as reduction in channel currents2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target?
AID28233Fraction ionized (pH 7.4)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1355797Intrinsic clearance in human liver microsomes assessed per mg protein after 10 mins in presence of NADPH by LC/MS/MS analysis2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID75921Concentration required to reduce maximum following frequencu (MFF) of isolated guinea pig atria by 25%1986Journal of medicinal chemistry, Feb, Volume: 29, Issue:2
Antiarrhythmic activity of 17 beta-aminoestratrienes. Comparison of 3-ols and 3-acetates with the corresponding 3-(3-amino-2-hydroxypropyl) ethers.
AID1519611Metabolic stability in rat liver microsomes assessed as half life incubated for 60 mins by LC-MS/MS analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.
AID1614372Intrinsic clearance in human liver measured from intrinsic clearance in human liver microsomes in presence of NADPH regenerating system by LC/MS/MS analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus.
AID28236Unbound fraction (tissues)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID630445Antimalarial activity against erythrocytic stage of chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by spectrophotometry2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1824587Metabolic stability in Sprague-Dawley rat liver microsomes assessed as intrinsic clearance measured upto 45 mins by LC-MS/MS analysis2022European journal of medicinal chemistry, Feb-05, Volume: 229The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.
AID696497Toxicity in po dosed CD1 mouse after 48 hrs2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Lead optimization of antimalarial propafenone analogues.
AID1887670Metabolic stability in human liver microsome assessed as parent compound remaining at 100 uM measured after 60 mins in presence of NADPH by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.
AID630446Antimalarial activity against erythrocytic stage of chloroquine-resistant Plasmodium falciparum K1 after 72 hrs by spectrophotometry2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
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.
AID630461Inhibition of Kv4.3 at 10 uM after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID1413499Half life in human liver microsomes at 10 mM preincubated for 10 mins followed by NADPH addition by LC-MS analysis2018MedChemComm, Aug-01, Volume: 9, Issue:8
Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant.
AID1583033Clearance in human liver derived from intrinsic clearance in human liver microsomes2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID1524892Stability in human liver microsomes assessed as compound remaining incubated of 60 mins in presence of NADPH regenerating system by LC/MS analysis2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Discovery of novel pyrazole derivatives as potential anticancer agents in MCL.
AID672543Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein.
AID1582079Metabolic stability in human liver microsomes assessed as compound remaining at 10 uM incubated for 1 hr2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Discovery and Characterization of 1
AID1876432Metabolic stability in human liver microsomes assessed as intrinsic clearance2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.
AID19431Partition coefficient (logP)1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Structure-activity relationship studies on benzofuran analogs of propafenone-type modulators of tumor cell multidrug resistance.
AID1718809Intrinsic clearance in CD-1 mouse liver microsomes at 100 uM measured after 60 mins in presence of NADPH by LC-MS/MS analysis
AID395038Inhibition of P-gp ATPase activity in human DC-3F/ADX cells assessed as increase in basal activity measured by NADH level at 0.5 uM by spectrophotometric method2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Search for MDR modulators: design, syntheses and evaluations of N-substituted acridones for interactions with p-glycoprotein and Mg2+.
AID386625Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
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
AID1862631Metabolic stability in rat liver microsomes assessed as intrinsic clearance per mg protein measured upto 6 hrs in presence of NADPH generating system by HPLC-MS/MS analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1706961Half life in Sprague-Dawley rat liver microsomes at 10 uM measured up to 60 mins in presence of NADPH regenerating system by HPLC analysis2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID630545Inhibition of human cloned Nav1.5 channel expressed in chinese hamster CHO cells assessed as phasic inhibition after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
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.
AID193769Effect on heart rate after isoprenaline induced tachycardia in the anesthetized rat at 1 mg/kg dose1986Journal of medicinal chemistry, Feb, Volume: 29, Issue:2
Antiarrhythmic activity of 17 beta-aminoestratrienes. Comparison of 3-ols and 3-acetates with the corresponding 3-(3-amino-2-hydroxypropyl) ethers.
AID324436Increase in light chain 3-GFP+ autophagosome vesicle number per cell in human H4 cells at 6.6 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.
AID1887669Metabolic stability in human liver microsomes assessed as intrinsic clearance at 100 uM incubated for 180 mins in presence of NADPH by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.
AID449704NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID324576Effect on 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.
AID449705NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
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.
AID1423580Inhibition of GIRK-1/4 channel (unknown origin) expressed in HEK293 cells at 1 uM by automated patch clamp method relative to control
AID29119Calculated partition coefficient (clogP) (HINT)2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Three-dimensional quantitative structure-activity relationship analysis of propafenone-type multidrug resistance modulators: influence of variable selection on test set predictivity.
AID1571699Intrinsic clearance in liver by measuring in intrinsic clearance in rat liver microsomes in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID467613Volume of distribution at steady state in human2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1593390Intrinsic clearance in human liver measured from intrinsic clearance in human liver microsomes2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID1895927Metabolic stability in human liver microsome assessed as intrinsic clearance by LC-MS/MS analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID1571700Metabolic stability in rat liver microsomes assessed as compound remaining after 60 mins in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID630463Inhibition of Nav1.5 assessed as tonic inhibition at 10 uM after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
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.
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.
AID1824588Metabolic stability in CD-1 mouse liver microsomes assessed as half life measured upto 45 mins by LC-MS/MS analysis2022European journal of medicinal chemistry, Feb-05, Volume: 229The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.
AID1211791Fraction unbound in human hepatocytes2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID696478Intrinsic clearance in CD9 mouse liver microsomes at 2 mM2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Lead optimization of antimalarial propafenone analogues.
AID193682Mean change in heart rate recorded 14 min after the administration of compound.1986Journal of medicinal chemistry, Feb, Volume: 29, Issue:2
Antiarrhythmic activity of 17 beta-aminoestratrienes. Comparison of 3-ols and 3-acetates with the corresponding 3-(3-amino-2-hydroxypropyl) ethers.
AID630458Inhibition of Kir3.1/3.4 at 10 uM after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID361986Lipophilicity, log D of compound at pH 7.4 by shake flask method2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Determination of log D via automated microfluidic liquid-liquid extraction.
AID324540Increase in light chain 3-GFP+ autophagosome vesicle intensity per cell in human H4 cells at 6.6 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.
AID1706967Intrinsic liver clearance in Sprague-Dawley rat liver microsomes at 10 uM measured up to 60 mins in presence of NADPH regenerating system by HPLC analysis2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID29120Calculated partition coefficient (clogP) (Molgen)2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Three-dimensional quantitative structure-activity relationship analysis of propafenone-type multidrug resistance modulators: influence of variable selection on test set predictivity.
AID1824586Metabolic stability in Sprague-Dawley rat liver microsomes assessed as half life measured upto 45 mins by LC-MS/MS analysis2022European journal of medicinal chemistry, Feb-05, Volume: 229The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID29812Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID26362Ionization constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1355796Half life in human liver microsomes after 10 mins in presence of NADPH by LC/MS/MS analysis2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1222793Dissociation constant, pKa of the compound2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Which metabolites circulate?
AID696475Inhibition of CYP2D6 in human liver microsomes at 10 uM after 20 mins by LC-MS/MS analysis relative to control2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Lead optimization of antimalarial propafenone analogues.
AID1887668Metabolic stability in human liver microsomes assessed as half life at 100 uM incubated for 180 mins in presence of NADPH by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.
AID29337Ionisation constant (pKa)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1232215Intrinsic clearance in rat liver microsomes at 1 uM preincubated for 10 mins followed by addition of NADPH regenerating system by LC-MS analysis2015Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14
Novel 3-(1H-indol-3-yl)-2-[3-(4-methoxyphenyl)ureido]propanamides as selective agonists of human formyl-peptide receptor 2.
AID1758024Metabolic stability in mouse liver microsomes assessed as clearance2021European journal of medicinal chemistry, Apr-15, Volume: 216Lead optimization generates selenium-containing miconazole CYP51 inhibitors with improved pharmacological profile for the treatment of fungal infections.
AID1886475Metabolic stability in human liver assessed as parent compound remaining preincubated for 10 mins followed by NADPH addition for 2 hrs and measured at 60 mins by high performance liquid chromatography-tandem mass spectrometry
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1571697Half life in rat liver microsomes in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID1571696Metabolic stability in human liver microsomes assessed as compound remaining after 60 mins in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID1614348Stability in human liver microsomes assessed as compound remaining in absence of NADPH regenerating system after 60 mins by LC/MS/MS analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus.
AID1779257Metabolic stability in mouse liver microsome assessed as half life2021European journal of medicinal chemistry, Oct-05, Volume: 221Discovery of hydrazide-containing oseltamivir analogues as potent inhibitors of influenza A neuraminidase.
AID1422272Stability in human liver microsomes assessed as parent compound remaining at 1 uM after 20 mins in presence of NADPH by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
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.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1422273Stability in human liver microsomes assessed as parent compound remaining at 1 uM after 10 mins in presence of NADPH by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID540229Volume of distribution at steady state in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1355800Metabolic stability in human liver microsomes assessed as compound remaining after 60 mins in absence of NADPH by LC/MS/MS analysis2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID540227Volume of distribution at steady state in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1583034Stability in human liver microsomes assessed as parent compound remaining measured at 60 mins2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID1413500Intrinsic clearance in human liver microsomes at 10 mM preincubated for 10 mins followed by NADPH addition and measured after 5 to 60 mins by LC-MS analysis2018MedChemComm, Aug-01, Volume: 9, Issue:8
Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant.
AID1692513Half life in human liver microsomes measured up to 60 mins by LC/MS-MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID29925Volume of distribution in man (IV dose)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID630454Inhibition of HCN2 at 10 uM after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID1211798Intrinsic clearance in human using well stirred liver model by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1744367Intrinsic clearance in human liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.
AID1706970Stability in Sprague-Dawley rat liver microsomes assessed as parent compound remaining at 10 uM measured after 60 mins in absence of NADPH regenerating system by HPLC analysis2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID184112Maximum increase in heart rate evoked by isoprenaline.1986Journal of medicinal chemistry, Feb, Volume: 29, Issue:2
Antiarrhythmic activity of 17 beta-aminoestratrienes. Comparison of 3-ols and 3-acetates with the corresponding 3-(3-amino-2-hydroxypropyl) ethers.
AID1614345Half life in human liver microsomes in presence of NADPH regenerating system by LC/MS/MS analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus.
AID1706968Intrinsic microsomal clearance in Sprague-Dawley rat liver microsomes at 10 uM measured up to 60 mins in presence of NADPH regenerating system by HPLC analysis2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID630452Inhibition of Cav1.2 at 10 uM after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID1583031Half life in human liver microsomes2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID630457Inhibition of Kir2.1 at 10 uM after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
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.
AID1524891Hepatic clearance in human liver microsomes further incubated of 5 to 60 mins in presence of NADPH regenerating system by LC/MS analysis2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Discovery of novel pyrazole derivatives as potential anticancer agents in MCL.
AID281137Inhibition of P-glycoprotein expressed in MDR CCRF vcr1000 cells by daunorubicin efflux assay2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Self-organizing maps for identification of new inhibitors of P-glycoprotein.
AID1409435Intrinsic clearance in human liver microsomes at 2 uL after 20 mins by LC/MS/MS analysis2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID1519610Metabolic stability in human liver microsomes assessed as compound remaining incubated for 60 mins by LC-MS/MS analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.
AID630546Inhibition of human kir6.2/SUR2A ion channel coexpressed in human HEK293 cells after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID1422276Intrinsic clearance in human liver microsomes at 1 uM by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID1571693Half life in human liver microsomes in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID44361In vitro multi drug resistance (MDR) reversal inhibitory activity against CCRF-CEM/VCR-1000 cell line2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Three-dimensional quantitative structure-activity relationship analysis of propafenone-type multidrug resistance modulators: influence of variable selection on test set predictivity.
AID449703NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay 2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1519612Metabolic stability in rat liver microsomes assessed as compound remaining incubated for 60 mins by LC-MS/MS analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1773844Half life in human liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1895928Metabolic stability in human liver assessed as intrinsic clearance by LC-MS/MS analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID322753Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID1895926Metabolic stability in human liver microsome assessed as half life by LC-MS/MS analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
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]
AID540224Clearance in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1773845Intrinsic clearance in human liver microsomes at 1 uM measured after 60 mins in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1862633Metabolic stability in human liver microsomes assessed as intrinsic clearance per mg protein measured upto 6 hrs in presence of NADPH generating system by HPLC-MS/MS analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
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.
AID1571698Intrinsic clearance in rat liver microsomes assessed per mg protein in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID1779258Metabolic stability in rat liver microsome assessed as half life2021European journal of medicinal chemistry, Oct-05, Volume: 221Discovery of hydrazide-containing oseltamivir analogues as potent inhibitors of influenza A neuraminidase.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1692512Metabolic stability in human liver microsomes assessed as compound remaining measured after 60 mins by LC/MS-MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.
AID630548Intrinsic clearance in CD9 mouse liver microsomes by UPLC-MS analysis2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID29423HPLC capacity factor (k')2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID540226Clearance in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID540225Volume of distribution at steady state in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1422270Stability in human liver microsomes assessed as parent compound remaining at 1 uM after 60 mins in presence of NADPH by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID540223Volume of distribution at steady state in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1692509Half life in mouse liver microsomes measured up to 60 mins by LC/MS-MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.
AID1571695Intrinsic clearance in liver by measuring in intrinsic clearance in human liver microsomes in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID1449547Metabolic stability in human liver microsomes assessed as parent compound remaining at 1 uM at 60 mins by LC-MS/MS analysis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
2'-Chloro,2'-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture.
AID1692508Metabolic stability in mouse liver microsomes assessed as compound remaining measured after 60 mins by LC/MS-MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.
AID1211797Intrinsic clearance in cryopreserved human hepatocytes cells assessed per 10'6 cells by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1744369Stability in human liver microsomes assessed as parent compound remaining at 1 uM incubated for 60 mins in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.
AID1614346Intrinsic clearance in human liver microsomes in presence of NADPH regenerating system by LC/MS/MS analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus.
AID1810682Agonist activity at in human TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP 16 assessed as remaining activity measured after 14 hrs by luciferase reporter gene assay relative to control2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells.
AID193779Effect on heart rate on 1 min post isoprenaline induced tachycardia in the anesthetized rat at 1 mg/kg dose.1986Journal of medicinal chemistry, Feb, Volume: 29, Issue:2
Antiarrhythmic activity of 17 beta-aminoestratrienes. Comparison of 3-ols and 3-acetates with the corresponding 3-(3-amino-2-hydroxypropyl) ethers.
AID1583032Intrinsic clearance in human liver microsomes2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID1211792Hepatic clearance in human2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1876435Metabolic stability in human liver microsomes assessed as parent compound remaining measured after 60 mins in absence of NADPH2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.
AID1422271Stability in human liver microsomes assessed as parent compound remaining at 1 uM after 30 mins in presence of NADPH by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID29139Calculated dissociation constant (pKa, calculated with ACD/pKa)2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
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]
AID1307730Inhibition of of human TREK1 expressed in CHO cells assessed as reduction in channel currents2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target?
AID630444Antimalarial activity against erythrocytic stage of chloroquine-resistant Plasmodium falciparum K1 after 72 hrs by FACS method2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID99501Compound was tested for inhibition of rhodamine 123 efflux in mdr 1 transfectant L5178Y VMDRI C.06 mouse lymphoma cells; nd=Not determined1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Substituted 4-acylpyrazoles and 4-acylpyrazolones: synthesis and multidrug resistance-modulating activity.
AID1692510Metabolic stability in rat liver microsomes assessed as compound remaining measured after 60 mins by LC/MS-MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1449545Half life in human liver microsomes at 1 uM by LC-MS/MS analysis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
2'-Chloro,2'-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture.
AID1886472Metabolic stability in human liver microsomes assessed as half-life preincubated for 10 mins followed by NADPH addition for 2 hrs and measured upto 60 mins by high performance liquid chromatography-tandem mass spectrometry
AID1211795Dissociation constant, pKa of the compound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID191714Compound was tested for antagonism of Ventricular Fibrilloflutter (VF) evoked by coronary artery ligation in the rat measured at 0.02 mg/kg dose1986Journal of medicinal chemistry, Feb, Volume: 29, Issue:2
Antiarrhythmic activity of 17 beta-aminoestratrienes. Comparison of 3-ols and 3-acetates with the corresponding 3-(3-amino-2-hydroxypropyl) ethers.
AID1614347Stability in human liver microsomes assessed as compound remaining in presence of NADPH regenerating system measured after 60 mins by LC/MS/MS analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1211793Lipophilicity, log P of the compound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1862632Metabolic stability in human liver microsomes assessed as half-life measured upto 6 hrs in presence of NADPH generating system by HPLC-MS/MS analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1207196Inhibition 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.
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]
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1442001Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID43400Effective dose against CCRF-CEM vcr 100 cells by using MTT assay1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Structure-activity relationship studies on benzofuran analogs of propafenone-type modulators of tumor cell multidrug resistance.
AID1718810Intrinsic clearance in CD-1 mouse microsomes at 100 uM measured after 60 mins in presence of NADPH by LC-MS/MS analysis
AID210307Compound was tested for inhibition of daunomycin efflux in the resistant human T-lymphoblast cell line CEM vcr1000.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Substituted 4-acylpyrazoles and 4-acylpyrazolones: synthesis and multidrug resistance-modulating activity.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID361985Lipophilicity, log D of compound at pH 7.4 by microfluidic liquid-liquid extraction method2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Determination of log D via automated microfluidic liquid-liquid extraction.
AID1207257Effective 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.
AID1593388Half life in human liver microsomes2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID193774Effect on heart rate before isoprenaline induced tachycardia in the anesthetized rat at 1 mg/kg dose1986Journal of medicinal chemistry, Feb, Volume: 29, Issue:2
Antiarrhythmic activity of 17 beta-aminoestratrienes. Comparison of 3-ols and 3-acetates with the corresponding 3-(3-amino-2-hydroxypropyl) ethers.
AID1895930Metabolic stability in human liver microsomes assessed as parent compound remaining at 60 mins in absence of NADPH regenerating system by LC-MS/MS analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID630455Inhibition of HCN4 at 10 uM after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID1886473Metabolic stability in human liver microsomes assessed as intrinsic clearance preincubated for 10 mins followed by NADPH addition for 2 hrs and measured upto 60 mins by high performance liquid chromatography-tandem mass spectrometry
AID630453Inhibition of Cav3.2 at 10 uM after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID540228Clearance in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1519609Metabolic stability in human liver microsomes assessed as half life incubated for 60 mins by LC-MS/MS analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.
AID1706966Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1810686Agonist activity at TAE expressed in human HEK293T cells coexpressing human full-length TLX/Gal4-VP 16 assessed as renilla luciferase reporter activity incubated for 14 hrs by Dual-glo luciferase2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID43402Effective dose against CCRF-CEM vcr 100 cells by using rhodamine efflux studies.1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Structure-activity relationship studies on benzofuran analogs of propafenone-type modulators of tumor cell multidrug resistance.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID630549Intrinsic clearance in human liver microsomes by UPLC-MS analysis2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID1876433Metabolic stability in human liver assessed as intrinsic clearance2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.
AID1809978Metabolic stability in mouse liver microsomes assessed as half-life2021Bioorganic & medicinal chemistry letters, 12-01, Volume: 53Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors.
AID540222Clearance in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1736741Metabolic stability in human liver assessed as intrinsic clearance incubated for 1 hr by LC/MS/MS method2020European journal of medicinal chemistry, Mar-15, Volume: 190Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.
AID630544Inhibition of human cloned Nav1.5 channel expressed in chinese hamster CHO cells assessed as tonic inhibition after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID1582077Metabolic stability in human liver microsomes assessed as half life at 10 uM incubated for 1 hr2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Discovery and Characterization of 1
AID1409437Metabolic stability in human liver microsomes assessed as compound remaining at 2 uL after 60 mins in absence of NADPH by LC/MS/MS analysis2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID28235Unbound fraction (plasma)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
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.
AID1824589Metabolic stability in CD-1 mouse liver microsomes assessed as intrinsic clearance measured upto 45 mins by LC-MS/MS analysis2022European journal of medicinal chemistry, Feb-05, Volume: 229The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID467612Fraction unbound in human plasma2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID467611Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1809979Metabolic stability in mouse liver microsomes assessed as clearance2021Bioorganic & medicinal chemistry letters, 12-01, Volume: 53Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors.
AID1736742Metabolic stability in human liver microsomes assessed as parent compound remaining in presence of NADPH after 1 hr by LC/MS/MS method2020European journal of medicinal chemistry, Mar-15, Volume: 190Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' 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.
AID630459Inhibition of Kir6.2/SUR2A at 10 uM after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID781328pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 20052014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID395037Inhibition of P-gp ATPase activity in human DC-3F/ADX cells assessed as increase in basal activity measured by NADH level at 5 uM by spectrophotometric method2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Search for MDR modulators: design, syntheses and evaluations of N-substituted acridones for interactions with p-glycoprotein and Mg2+.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1886474Metabolic stability in human liver assessed as intrinsic clearance preincubated for 10 mins followed by NADPH addition for 2 hrs and measured upto 60 mins by high performance liquid chromatography-tandem mass spectrometry
AID449706NOVARTIS: Inhibition Frequency Index (IFI) - the number of HTS assays where a compound showed > 50% inhibition/induction, expressed as a percentage of the number of assays in which the compound was tested.2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID43525The chemosensitizing effect was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM daunomycin1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Synthesis, pharmacologic activity, and structure-activity relationships of a series of propafenone-related modulators of multidrug resistance.
AID1442006Ratio of Kii for human OCT1-ASP+-inhibitor complex to Kis for human OCT1-inhibitor complex by Lineweaver-Burk plot analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).
AID324577Effect on 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.
AID1422269Half life in human liver microsomes at 1 uM by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID1593389Intrinsic clearance in human liver microsomes2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID1232214Half life in rat liver microsomes at 1 uM preincubated for 10 mins followed by addition of NADPH regenerating system by LC-MS analysis2015Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14
Novel 3-(1H-indol-3-yl)-2-[3-(4-methoxyphenyl)ureido]propanamides as selective agonists of human formyl-peptide receptor 2.
AID1706969Stability in Sprague-Dawley rat liver microsomes assessed as parent compound remaining at 10 uM measured after 60 mins in presence of NADPH regenerating system by HPLC analysis2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID485979Inhibition of CETP in rabbit serum at 10 uM after 1 hr by fluorescent cholesteryl esters transfer assay2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Discovery of new cholesteryl ester transfer protein inhibitors via ligand-based pharmacophore modeling and QSAR analysis followed by synthetic exploration.
AID191716Compound was tested for antagonism of Ventricular Fibrilloflutter (VF) evoked by coronary artery ligation in the rat measured at 0.1 mg/kg dose1986Journal of medicinal chemistry, Feb, Volume: 29, Issue:2
Antiarrhythmic activity of 17 beta-aminoestratrienes. Comparison of 3-ols and 3-acetates with the corresponding 3-(3-amino-2-hydroxypropyl) ethers.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1449546Clearance in human liver microsomes at 1 uM by LC-MS/MS analysis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
2'-Chloro,2'-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture.
AID1736743Metabolic stability in human liver microsomes assessed as parent compound remaining in absence of NADPH after 1 hr by LC/MS/MS method2020European journal of medicinal chemistry, Mar-15, Volume: 190Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.
AID43874The percentage uptake of [3H]daunomycin in resistant CCRF-CEM vcr 100 cells to sensitive CCRF-CEM cells in presence of the compound.1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Synthesis, pharmacologic activity, and structure-activity relationships of a series of propafenone-related modulators of multidrug resistance.
AID43867The reversion potency of compound was measured against P-glycoprotein expressing CCRF-CEM cells and expressed as the ratio of ED50 in the absence and presence of daunomycin1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Synthesis, pharmacologic activity, and structure-activity relationships of a series of propafenone-related modulators of multidrug resistance.
AID1718807Metabolic stability in CD-1 mouse liver microsomes assessed as parent compound remaining at 100 uM measured after 60 mins by LC-MS/MS analysis
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID696477Solubility of the compound in PBS at 10 mM after 18 hrs by UV spectroscopic analysis2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Lead optimization of antimalarial propafenone analogues.
AID1692511Half life in rat liver microsomes measured up to 60 mins by LC/MS-MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.
AID630464Inhibition of Nav1.5 assessed as phasic inhibition at 10 uM after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1422275Stability in human liver microsomes assessed as parent compound remaining at 1 uM after 60 mins in absence of NADPH by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID630460Inhibition of Kv1.5 at 10 uM after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID324488Increase in light chain 3-GFP+ autophagosome vesicle area per cell in human H4 cells at 6.6 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.
AID781329pKa (acid-base dissociation constant) as determined by other workers2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID630543Inhibition of human cloned ERG channel expressed in chinese hamster CHO cells after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1409434Half life in human liver microsomes at 2 uL by LC/MS/MS analysis2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID630443Antimalarial activity against erythrocytic stage of chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by FACS method2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1862630Metabolic stability in rat liver microsomes assessed as half-life measured upto 6 hrs in presence of NADPH generating system by HPLC-MS/MS analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID176509Compound that antagonized arrhythmias evoked by coronary artery ligation in the rat was measured at 0.05 mg/kg dose1986Journal of medicinal chemistry, Feb, Volume: 29, Issue:2
Antiarrhythmic activity of 17 beta-aminoestratrienes. Comparison of 3-ols and 3-acetates with the corresponding 3-(3-amino-2-hydroxypropyl) ethers.
AID1895929Metabolic stability in human liver microsomes assessed as parent compound remaining at 60 mins in presence of NADPH regenerating system by LC-MS/MS analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID1422274Stability in human liver microsomes assessed as parent compound remaining at 1 uM after 5 mins in presence of NADPH by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID1887655Metabolic stability in human liver assessed as intrinsic clearance at 100 uM incubated for 180 mins in presence of NADPH by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.
AID1758023Metabolic stability in mouse liver microsomes assessed as half life2021European journal of medicinal chemistry, Apr-15, Volume: 216Lead optimization generates selenium-containing miconazole CYP51 inhibitors with improved pharmacological profile for the treatment of fungal infections.
AID1413501Stability in human liver microsomes assessed as parent compound remaining at 10 mM preincubated for 10 mins followed by NADPH addition and measured after 60 mins by LC-MS analysis2018MedChemComm, Aug-01, Volume: 9, Issue:8
Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant.
AID1207226Inhibition 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.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1207167Inhibition 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.
AID1582080Metabolic stability in CD1 mouse liver microsomes assessed as half life at 10 uM incubated for 1 hr2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Discovery and Characterization of 1
AID630456Inhibition of human ERG at 10 uM after 5 mins by patch clamp assay2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Optimization of propafenone analogues as antimalarial leads.
AID191715Compound was tested for antagonism of Ventricular Fibrilloflutter (VF) evoked by coronary artery ligation in the rat measured at 0.05 mg/kg dose1986Journal of medicinal chemistry, Feb, Volume: 29, Issue:2
Antiarrhythmic activity of 17 beta-aminoestratrienes. Comparison of 3-ols and 3-acetates with the corresponding 3-(3-amino-2-hydroxypropyl) ethers.
AID1876434Metabolic stability in human liver microsomes assessed as parent compound remaining measured after 60 mins2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID19424Partition coefficient (logD7.4)2001Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID1524889Half life in human liver microsomes further incubated of 5 to 60 mins in presence of NADPH regenerating system by LC/MS analysis2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Discovery of novel pyrazole derivatives as potential anticancer agents in MCL.
AID1409436Metabolic stability in human liver microsomes assessed as compound remaining at 2 uL after 60 mins by LC/MS/MS analysis2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID781330pKa (acid-base dissociation constant) as determined by potentiometric titration2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
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]
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.
AID324384Induction of light chain 3-GFP level in human H4 cells at 6.6 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.
AID1582082Metabolic stability in CD1 mouse liver microsomes assessed as compound remaining at 10 uM incubated for 1 hr2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Discovery and Characterization of 1
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
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.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
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.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
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.
AID1346684Human Kv1.5 (Voltage-gated potassium channels)1998British journal of pharmacology, Nov, Volume: 125, Issue:5
Effects of propafenone and 5-hydroxy-propafenone on hKv1.5 channels.
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.
AID602156Novartis GNF Liver Stage Dataset: Malariabox Annotation2011Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,382)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990380 (27.50)18.7374
1990's447 (32.34)18.2507
2000's284 (20.55)29.6817
2010's205 (14.83)24.3611
2020's66 (4.78)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 83.21

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

MetricThis Compound (vs All)
Research Demand Index83.21 (24.57)
Research Supply Index7.46 (2.92)
Research Growth Index4.48 (4.65)
Search Engine Demand Index151.13 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (83.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials268 (18.22%)5.53%
Reviews106 (7.21%)6.00%
Case Studies212 (14.41%)4.05%
Observational2 (0.14%)0.25%
Other883 (60.03%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (29)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
An Open-Label Randomized Study of Propafenone in the Treatment of Atrial Fibrillation [NCT03674658]71 participants (Actual)Interventional2019-07-11Completed
Single Dose, Full Replicate, Crossover Comparative Bioavailability Study of Propafenone 300 mg Film-Coated Tablets in Healthy Adult Subjects / Fasting State [NCT03915340]Phase 132 participants (Actual)Interventional2019-03-23Completed
Population Pharmacokinetics of Propafenone and Propranolol in Children Patients [NCT05463614]500 participants (Anticipated)Observational2019-02-01Recruiting
Catheter Ablation Compared With Pharmacological Therapy for Atrial Fibrillation - a Randomized Multicentre Study Comparing Atrial Fibrillation Ablation Strategy With Optimized Conventional Pharmacological Strategy After 12 Months Follow-up. [NCT02294955]152 participants (Actual)Interventional2008-05-31Active, not recruiting
Antiarrhythmic Drugs Assessment in Preventing Atrial Fibrillation [NCT02145546]Phase 4600 participants (Anticipated)Interventional2014-05-31Not yet recruiting
Using Cryoballoon Ablation as Initial Treatment for Patients With Persistent Atrial Fibrillation Comparing to Anti-arrhythmic Drugs [NCT04942834]286 participants (Anticipated)Interventional2021-08-31Not yet recruiting
Multicenter Clinical Study of Therapeutic Effect of Sotalol on Children With Arrhythmia (Paroxysmal Supraventricular Tachycardia, Paroxysmal Atrial Tachycardia, Ventricular Tachycardia, Idiopathic Ventricular Tachycardia, Premature Ventricular Contraction [NCT03895411]Phase 4500 participants (Anticipated)Interventional2019-08-31Not yet recruiting
Clinical Efficacy and Safety of Antazoline in Comparison to Propafenone in Conversion of Paroxysmal Atrial Fibrillation to Sinus Rhythm - a Single Center, Randomized, Double-blinded Study (the AnProAF Study). [NCT05720572]Phase 4105 participants (Anticipated)Interventional2019-09-01Recruiting
Outcome of Medical Treatment for Idiopathic Premature Ventricular Complexes - Beta-blocker vs Ic Antiarrhythmic Agent; Randomized Controlled Trial [NCT03561935]350 participants (Anticipated)Interventional2015-06-30Recruiting
A Prospective Randomized Multicenter Global Study Comparing Pulsed Field Ablation (PFA) Versus Anti-Arrhythmic Drug (AAD) Therapy as a First Line Treatment for Persistent Atrial Fibrillation [NCT06096337]387 participants (Anticipated)Interventional2023-12-15Not yet recruiting
Efficacy and Safety of Electrical Versus Pharmacological Cardioversion in Early Atrial Fibrillation: a Randomized Controlled Trial [NCT00933634]247 participants (Anticipated)Interventional2006-01-31Completed
A Randomized, Controlled Clinical Trial of Catheter Cryoablation in the Treatment of Paroxysmal Atrial Fibrillation. [NCT00523978]Phase 3245 participants (Actual)Interventional2006-10-31Completed
[NCT00000556]Phase 30 participants Interventional1995-03-31Completed
A Phase 1, Open-Label, Crossover Study to Demonstrate the Bioequivalence of RYTHMOL SR® (Propafenone Hydrochloride) Manufactured at Two Different Sites [NCT01956487]Phase 138 participants (Actual)Interventional2012-04-11Completed
Efficacy of Propafenone Versus Dronedarone for the Maintenance of Sinus Rhythm in Patients With Atrial Fibrillation After DC Cardioversion [NCT01991119]98 participants (Actual)Interventional2011-05-31Completed
First-line Cryoablation for Early Treatment of Persistent Atrial Fibrillation - a Randomized Study Comparing Early Trigger Isolation Using the Cryoballoon Versus Antiarrhythmic Medication [NCT05939076]Phase 3220 participants (Anticipated)Interventional2023-08-21Not yet recruiting
Comparison of Brain Perfusion in Rhythm Control and Rate Control of Persistent Atrial Fibrillation: Prospective Randomized Trial [NCT02633774]200 participants (Anticipated)Interventional2015-11-30Recruiting
A Randomized Comparison of the Efficacy of Antiarrhythmic Drug Therapy and Radiofrequency Catheter Ablation for the Maintenance of Sinus Rhythm In Patients With Paroxysmal Atrial Fibrillation [NCT00540787]Phase 4112 participants (Actual)Interventional2003-08-31Completed
[NCT00000464]Phase 30 participants Interventional1987-04-30Completed
Study of Focused Circumferential UltraSound for the Treatment of Atrial Fibrillation [NCT00392106]Phase 3240 participants (Anticipated)Interventional2006-04-30Suspended(stopped due to voluntarily by Sponsor to investigate an anticipated SAE)
Early Aggressive Invasive Intervention for Atrial Fibrillation [NCT02825979]303 participants (Actual)Interventional2017-01-31Active, not recruiting
Progression of Atrial Fibrillation After a Failed Initial Ablation Procedure in Patients With Paroxysmal Atrial Fibrillation: A Randomized Comparison of the Drug Therapy Versus Re-Ablation [NCT01709682]Phase 2154 participants (Actual)Interventional2007-11-30Completed
Efficacy of Pilsicainide After Radiofrequency Ablation of Paroxysmal Atrial Fibrillation Compared With Other Class IC Anti-arrhythmic Drugs [NCT01775891]245 participants (Anticipated)Interventional2012-07-31Recruiting
[NCT01780311]Phase 40 participants Interventional2013-01-31Recruiting
Prospective Randomized Study of Efficacy and Safety of 1c Class Antiarrhythmic Agent (Propafenone) in Septic Shock [NCT03029169]Phase 4210 participants (Actual)Interventional2017-10-23Completed
A Prospective Study of Medical Therapy Against Cryoballoon Ablation in Symptomatic Recent Onset Persistent Atrial Fibrilation [NCT02389218]Phase 413 participants (Actual)Interventional2015-03-03Completed
Comparison of (R) and (S) Propafenone for Prevention of Atrial Fibrillation Induction [NCT02710669]Phase 1/Phase 2193 participants (Actual)Interventional2016-10-31Terminated(stopped due to Study halted/terminated prematurely due to COVID.)
A Randomized Trial to Assess the Utility of Empirical Anti-Arrhythmic Drug Therapy to Prevent Atrial Arrhythmia During the 6 Weeks Following Pulmonary Vein Isolation to Treat Paroxysmal Atrial Fibrillation [NCT00408200]110 participants (Actual)Interventional2006-11-30Completed
Ablation Verses Anti-arrhythmic Therapy for Reducing All Hospital Episodes From Recurrent Atrial Fibrillation [NCT02459574]300 participants (Anticipated)Interventional2015-05-01Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00408200 (2) [back to overview]Composite Endpoint: Atrial Arrhythmias Lasting >24 Hrs or Requiring Antiarrhythmic Drug Therapy; Need for Cardioversion/Repeat Ablation During the Study Period; Adverse Outcome/Intolerance of Antiarrhythmic Agent Requiring Cessation or Change of Drug
NCT00408200 (2) [back to overview]Freedom From Atrial Arrhythmia at 6 Months Post Procedure.
NCT00523978 (5) [back to overview]Acute Procedural Success (APS)
NCT00523978 (5) [back to overview]Cryoablation Procedure Events (CPEs)
NCT00523978 (5) [back to overview]Freedom From Chronic Treatment Failure (CTF)
NCT00523978 (5) [back to overview]Freedom From Major Atrial Fibrillation Events (MAFEs)
NCT00523978 (5) [back to overview]Treatment Success
NCT02710669 (3) [back to overview]Number of Participants With Successful Inducibility of Atrial Fibrillation/Atrial Flutter Expressed as an Ordinal Variable Based on Stage of the Induction Protocol
NCT02710669 (3) [back to overview]Number of Participants With Successful Induction of 30 Seconds of Atrial Fibrillation/Atrial Flutter
NCT02710669 (3) [back to overview]Number of Participants With Successful Induction of 30 Seconds of Atrial Flutter

Composite Endpoint: Atrial Arrhythmias Lasting >24 Hrs or Requiring Antiarrhythmic Drug Therapy; Need for Cardioversion/Repeat Ablation During the Study Period; Adverse Outcome/Intolerance of Antiarrhythmic Agent Requiring Cessation or Change of Drug

(NCT00408200)
Timeframe: 6 weeks

Interventionparticipants (Number)
AAD:NO24
AAD:YES10

[back to top]

Freedom From Atrial Arrhythmia at 6 Months Post Procedure.

(NCT00408200)
Timeframe: 6 weeks

Interventionparticipants (Number)
AAD:NO39
AAD:YES35

[back to top]

Acute Procedural Success (APS)

Acute Procedural Success was defined as a demonstration of electrical isolation in ≥ 3 Pulmonary Veins (PVs) at the conclusion of the first protocol-defined cryoablation procedure. APS was decided at the end of the procedure the mean time was calculated for the time frame. (NCT00523978)
Timeframe: 371.4 Minutes (Average)

Interventionparticipants (Number)
Cryoablation160

[back to top]

Cryoablation Procedure Events (CPEs)

Subjects that had CPEs. CPEs were device- or procedure-related serious adverse events (SAE) categorized as access site complications, cardiac damage, pulmonary vein (PV) stenosis, embolic complications, arrhythmias, unresolved phrenic nerve palsy and death. (NCT00523978)
Timeframe: To end of ablation procedure

Interventionparticipants (Number)
Cryoablation5

[back to top]

Freedom From Chronic Treatment Failure (CTF)

Subjects that did not have or were free of CTF. CTF was defined as the occurence of an Atrial Fibrillation (AF) intervention, use of non-study AF drug therapy, or the occurence of detectable AF which is is defined as an episode of AF, documented in a tracing, and lasting more than 30 seconds, occurring during a Non Blanked Follow-up Period. (NCT00523978)
Timeframe: 12 month follow up period

Interventionparticipants (Number)
Cryoablation117
Standard Treatment With Drugs Only6

[back to top]

Freedom From Major Atrial Fibrillation Events (MAFEs)

Subjects that did not have or were free of MAFEs. MAFEs were serious adverse events categorized as cardiovascular death, myocardial infarction, stroke, or hospitalization for AF recurrence/ablation, flutter ablation, embolic events, heart failure, hemorrhage or anti-arrhythmic drug treatment. (NCT00523978)
Timeframe: 12 Months

Interventionparticipants (Number)
Cryoablation158
Standard Treatment With Drugs Only75

[back to top]

Treatment Success

Treatment Success was defined as Acute Procedure Success (APS) and freedom from Chronic Treatment Failure (CTF) for Experimental Subjects, and freedom from CTF for Control Subjects. Under this pre-specified definition of Treatment Success, Experimental Subjects must have had APS and remained free of CTF during the 12-month follow-up duration, while Control Subjects must have remained free of CTF during the 12-month follow-up duration. (NCT00523978)
Timeframe: 12 months

Interventionparticipants (Number)
Cryoablation114
Standard Treatment With Drugs Only6

[back to top]

Number of Participants With Successful Inducibility of Atrial Fibrillation/Atrial Flutter Expressed as an Ordinal Variable Based on Stage of the Induction Protocol

"Inducibility of atrial fibrillation (AF) or atrial flutter (AFL) expressed as an ordinal variable based on stage of the induction protocol.~Stage 1 measured the AV block (Wenckebach) cycle length (AVBCL), AV node effective refractory period (AVN ERP) and atrial ERP (AERP). AVN ERP and AERP were measured at drive trains (S1) of 600 ms and 450 ms. Extrastimuli (S2) were introduced starting at a coupling interval of 500ms and decremented by 10ms with each pacing train.~Stage 2 consisted of 15-beat bursts from the CS proximal electrode. The starting cycle length was 250ms, which was decremented by 10ms with each burst. A 10-second rest period was used between bursts. Step 2 was complete when 1:1 atrial capture was lost or a minimum cycle length of 180ms was reached.~Stage 3 consisted of 15-second bursts. The cycle length used for the bursts was the fastest cycle length achieved during Step 2 that maintained 1:1 atrial conduction." (NCT02710669)
Timeframe: Twenty minutes post-dosage to end of induction protocol (approximately 10 minutes)

,,
InterventionParticipants (Count of Participants)
Stage 1Stage 2Stage 3Non-inducible AF/AFL
(R)-Propafenone5282711
(S)-Propafenone5312415
Placebo1387

[back to top]

Number of Participants With Successful Induction of 30 Seconds of Atrial Fibrillation/Atrial Flutter

A rapid atrial pacing protocol was used to attempt to induce atrial fibrillation/atrial flutter. Twenty minutes after start of the study drug, participants underwent placement of a decapolar coronary sinus catheter. Pacing was performed from the proximal electrode at 20 milliamps and a pulse width of 2 ms. Bursts from the CS proximal electrode were induced to attempt atrial fibrillation. (NCT02710669)
Timeframe: Twenty minutes post-dosage to end of induction protocol (approximately 10 minutes)

,,
InterventionParticipants (Count of Participants)
Sustained AF and/or AFL inducedNon-sustained AF and/or AFL induced
(R)-Propafenone6011
(S)-Propafenone6015
Placebo127

[back to top]

Number of Participants With Successful Induction of 30 Seconds of Atrial Flutter

A rapid atrial pacing protocol was used to attempt to induce atrial flutter. Twenty minutes after start of the study drug, participants underwent placement of a decapolar coronary sinus catheter. Pacing was performed from the proximal electrode at 20 milliamps and a pulse width of 2 ms. Bursts from the CS proximal electrode were induced to attempt atrial flutter. (NCT02710669)
Timeframe: Twenty minutes post-dosage to end of induction protocol (approximately 10 minutes)

,,
InterventionParticipants (Count of Participants)
Sustained AFLNon-Sustained AFL
(R)-Propafenone2348
(S)-Propafenone2649
Placebo118

[back to top]