Page last updated: 2024-12-05

acecainide

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

Description

Acecainide is a class I antiarrhythmic drug. It was synthesized in the 1970s. Acecainide is a potent sodium channel blocker, which is why it is used to treat supraventricular and ventricular arrhythmias. It was withdrawn from the market due to hepatotoxicity. However, its sodium channel blocking properties have been explored as a potential treatment for other conditions, such as neuropathic pain and epilepsy. Research is ongoing to further explore the potential therapeutic applications of acecainide.'

Acecainide: A major metabolite of PROCAINAMIDE. Its anti-arrhythmic action may cause cardiac toxicity in kidney failure. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

N-acetylprocainamide : A benzamide obtained via formal condensation of 4-acetamidobenzoic acid and 2-(diethylamino)ethylamine. [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 CID4342
CHEMBL ID1097
CHEBI ID60728
SCHEMBL ID156943
MeSH IDM0000193

Synonyms (83)

Synonym
CHEMBL1097 ,
n-acetylnovocainamide
n-acetylprocaine amide
n-acetyl procainamide
n-acetyl-procainamide
acetylprocainamide, n-
MLS001146871
bdbm50151860
n-acetyl procainamide(<30%)
4-acetylamino-n-(2-diethylamino-ethyl)-benzamide
BRD-K07753030-003-01-0
n-acetylprocainamide
acecainidum [inn-latin]
acetylprocainamide
acekainid [polish]
acecainida [inn-spanish]
n-acetyloprokainamid [polish]
4'-((2-(diethylamino)ethyl)carbamoyl)acetanilide
acecainide
brn 2868559
acetanilide, 4'-((2-(diethylamino)ethyl)carbamoyl)-
benzamide, 4-(acetylamino)-n-(2-(diethylamino)ethyl)-
acecainide [inn]
lopac-a-5909
NCGC00015072-01
LOPAC0_000009
BSPBIO_003226
napa
n-acetylprocainamide, >=99%
MLS000069490 ,
smr000059070
KBIO3_002726
SPECTRUM3_001843
NCGC00015072-02
NCGC00023226-04
NCGC00023226-03
NCGC00015072-07
32795-44-1
4-acetamido-n-[2-(diethylamino)ethyl]benzamide
acekainid
n-acetyloprokainamid
acecainidum
CHEBI:60728 ,
acecainida
CCG-204105
HMS2232G18
NCGC00015072-04
NCGC00015072-06
NCGC00015072-03
NCGC00015072-05
910q707v6f ,
unii-910q707v6f
FT-0639052
EPITOPE ID:140121
acecainide [mi]
acecainide [who-dd]
AKOS016614968
HMS3372E09
SCHEMBL156943
CS-4707
DTXSID6048414
procainamide-n-acetyl
4-(acetylamino)-n-[2-(diethylamino)ethyl]benzamide #
HY-B1109
OPERA_ID_1541
AB00384286_20
n-(4-{[2-(diethylamino)ethyl]carbamoyl}phenyl)ethanimidic acid
n-acetylprocainamide 1.0 mg/ml in methanol
J-018880
SBI-0049998.P002
Z26393212
BCP26213
Q4726688
4-acetamido-n-(2-(diethylamino)ethyl)benzamide
BRD-K07753030-003-11-9
SDCCGSBI-0049998.P003
NCGC00015072-13
acecainide;napa
F85241
AS-57414
n-[2-(diethylamino)ethyl]-4-acetamidobenzamide
A905428
EN300-6492978

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"To assess the efficacy, plasma drug concentrations and adverse effects of a new sustained release preparation of procainamide, 33 patients with heart disease were studied in an acute dose-ranging protocol and a chronic treatment protocol."( Efficacy, plasma concentrations and adverse effects of a new sustained release procainamide preparation.
Bigger, JT; Fenster, PE; Giardina, EG; Marcus, FI; Mayersohn, M; Perrier, D, 1980
)
0.26

Pharmacokinetics

Acecainide renal clearance, nonrenal clearance, steady-state volume of distribution, and other pharmacokinetic parameters were estimated using standard approaches. The mean half-life of elimination after a single 500 mg dose of aceCainide was 7.

ExcerptReferenceRelevance
" Pharmacokinetic parameters were calculated with the aid of pharmacokinetics independent of the model principles."( [Pharmacokinetics of procainamide and its metabolite depending on acetylator phenotype].
Gawrońska-Szklarz, B; Górnik, W; Kutrzeba, J; Wójcicki, J; Zakrzewski, J,
)
0.13
" Disposition kinetics of NAPA in rats was predicted with combination of gamma variate and physiological pharmacokinetic model."( Prediction of N-acetylprocainamide disposition kinetics in rat by combination of gamma variate and physiological pharmacokinetic model.
Deng, N; Huang, SK; Liu, XD, 1992
)
0.28
"The pharmacokinetic and pharmacodynamic profiles of N-acetyl procainamide were analyzed by integrated PK-PD model following intravenous infusion to rabbits."( [Combined pharmacokinetic--pharmacodynamic model analysis of N-acetyl procainamids following intravenous infusion in rabbits].
Gong, L; Huang, SK; Liu, XQ; Yang, JY, 1990
)
0.28
"The pharmacokinetic and pharmacodynamic profiles of procainamide (PA) and its major metabolite, acetylprocainamide (NAPA), were analyzed by extended combined pharmacokinetic and pharmacodynamic model in rabbits."( [Combined pharmacokinetic and pharmacodynamic model analysis for procainamide and its metabolite].
Huang, SK; Liu, XQ, 1991
)
0.28
" Acecainide renal clearance, nonrenal clearance, steady-state volume of distribution, and other pharmacokinetic parameters were estimated using standard approaches."( Acecainide pharmacokinetics in normal subjects of known acetylator phenotype.
Boudoulas, H; Coyle, JD; Lima, JJ, 1991
)
2.63
" We analyzed the pharmacokinetic properties of PA and NAPA and elucidated their effect kinetics with a pharmacokinetic-pharmacodynamic (PK/PD) model in view of different transfer qualities."( [Combined pharmacokinetic-pharmacodynamic model of procainamide in rabbits with induced ventricular fibrillation threshold (VFT) changes].
Huang, SK; Lu, DY; Lu, H; Lu, JF; Yang, JY, 1991
)
0.28
"Disposition kinetics of procainamide (PA) and its metabolite N-acetylprocainamide (NAPA) in rats was simulataneously predicted by a physiological pharmacokinetic model."( [Simultaneous predictions of disposition kinetics of procainamide and its metabolite N-acetylprocainamide in rat by a physiological pharmacokinetic model].
Deng, N; Huang, SK; Liu, XD, 1991
)
0.28
" The reported concentrations and pharmacokinetic parameters are from the HPLC data unless otherwise indicated."( Concentration-dependent clearance of procainamide in normal subjects.
Boudoulas, H; Coyle, JD; Lima, JJ; Mackichan, JJ,
)
0.13
"The pharmacokinetic profile and the cardiovascular actions of desethyl-N-acetylprocainamide (NAPADE) were studied in chloralose-urethane anesthetized dogs."( Cardiovascular actions and pharmacokinetics of desethyl-N-acetylprocainamide in the dog.
King, LW; Lertora, JJ, 1986
)
0.27
" In group 1, the elimination of procainamide was described by a 1-compartment, open pharmacokinetic model."( Pharmacokinetics of procainamide hydrochloride in dogs.
Brown, SA; Davis, CA; Davis, LE; McKiernan, BC; Papich, MG, 1986
)
0.27
" In these studies, we showed that NAPA has an elimination-phase half-life that is more than twice as long as procainamide and suggested that patient compliance and arrhythmia suppression might be improved if NAPA were used to circumvent the inconvenience of the frequent dosing schedule that has been recommended for procainamide."( Pharmacokinetics of N-acetylprocainamide.
Atkinson, AJ; Ruo, TI, 1986
)
0.27
" There were no significant differences in the mean pharmacokinetic parameters of procainamide and NAPA after ranitidine coadministration compared to base line."( Ranitidine-induced changes in the renal and hepatic clearances of procainamide are correlated.
Ferguson, RK; Kosoglou, T; Rocci, ML; Vlasses, PH, 1989
)
0.28
" Trimethoprim may increase procainamide and N-acetylprocainamide plasma concentrations, resulting in increased pharmacodynamic response apparently caused by the competition for renal tubular cationic secretion."( Trimethoprim inhibition of the renal clearance of procainamide and N-acetylprocainamide.
Andress, E; Chase, SL; Ferguson, RK; Greenspon, AJ; Kosoglou, T; Lottes, S; Rocci, ML; Vlasses, PH, 1989
)
0.28
" The mean area under the plasma concentration-time curve, elimination half-life or oral clearance of the morning and evening dosages did not differ."( Chronopharmacokinetic studies of pranoprofen and procainamide.
Ebihara, A; Fujimura, A; Kajiyama, H; Kumagai, Y; Nakashima, H; Sugimoto, K, 1989
)
0.28
" Substantial differences in pharmacokinetic parameters of PA depending on acetylation phenotype were found."( Pharmacokinetic studies of procainamide (PA) and N-acetylprocainamide (NAPA) in healthy subjects.
Grześkowiak, A; Lowicki, Z; Michałowska, D; Ochotny, R; Tomaszkiewicz, T; Wierzchowiecki, M, 1980
)
0.26
" The plasma concentrations of PA and N-acetylprocainamide (NAPA) as well as the pharmacodynamic effect (prolongation of the QT interval) were monitored."( The pharmacokinetics and pharmacodynamics of procainamide in horses after intravenous administration.
Duran, SH; Ellis, EJ; Malloy, M; Ravis, WR; Smyth, BG, 1994
)
0.29
" However, the following main changes in N-acetylprocainamide (metabolite) pharmacokinetic parameters were found: 1) increase of the penetration rate constants between the compartments and mean residence time during propofol anesthesia 2) prolongation of the mean residence time during thiopental anesthesia 3) increase of mean residence time of N-acetylprocainamide during anesthesia with ketamine, pentobarbital or propofol."( The influence of selected general anesthetics on pharmacokinetic parameters of some antiarrhythmic drugs in rabbits. Part I. Procainamide and its active metabolite-N-acetylprocainamide.
Orszulak-Michalak, D,
)
0.13
"The influence of general anesthesia with thiopental (10 mg/kg), ketamine (4 mg/kg), propofol (10 mg/kg) or pentobarbital (20 mg/kg) on the N-acetylprocainamide (15 mg/kg) pharmacokinetic parameters was studied in rabbits."( The influence of selected general anesthetics on pharmacokinetic parameters of some antiarrhythmic drugs in rabbits. Part II. N-acetylprocainamide.
Orszulak-Michalak, D,
)
0.13
" Procainamide and NAPA pharmacokinetic parameters observed after administration of Procanbid tablets were similar in blacks and whites, and in men and women."( Effect of age, gender, and race on steady state procainamide pharmacokinetics after administration of procanbid sustained-release tablets.
Abel, RB; de Vries, TM; Eldon, MA; Koup, JR; Smithers, JA, 1998
)
0.3
" Noncompartmental analysis was performed to estimate the pharmacokinetic parameters."( The influence of moderate and chronic exercise training on the pharmacokinetics of procainamide and N-acetylprocainamide.
Adekoya, F; Eddington, ND; Kharidia, J, 1998
)
0.3
" In an accompanying paper, we have presented a unique, generic, physiologically based pharmacokinetic model and described its application to the prediction of rat plasma pharmacokinetics from in vitro data alone."( Application of a generic physiologically based pharmacokinetic model to the estimation of xenobiotic levels in human plasma.
Brightman, FA; Leahy, DE; Searle, GE; Thomas, S, 2006
)
0.33
" 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
" Pharmacokinetic analysis of procainamide and its metabolite, N-acetylprocainamide (NAPA), was performed using serum and urine specimens."( Procainamide pharmacokinetics during extracorporeal membrane oxygenation.
Rosenbaum, AN; Vollmer, NJ; Wieruszewski, PM; Wittwer, ED, 2023
)
0.91

Compound-Compound Interactions

ExcerptReferenceRelevance
" By using programmed electrical stimulation in combination with MAP recordings at different pacing rates in the intact dog heart, it was possible to classify and to a certain extent to elucidate the mode of action of various cardioactive drugs in vivo."( Classification of cardioactive drugs in vivo by using programmed electrical stimulation in combination with monophasic action potential recordings at different pacing rates.
Amlie, JP; Landmark, K; Refsum, H, 1981
)
0.26

Bioavailability

ExcerptReferenceRelevance
" Cimetidine significantly increased the procainamide area under the serum concentration-time curve by 43%, decreased renal clearance by 36%, and decreased the ratio of systemic clearance of procainamide to bioavailability by 28%."( Interaction of steady-state procainamide with H2-receptor antagonists cimetidine and ranitidine.
Gallastegui, J; Jung, D; Paloucek, FP; Rodvold, KA, 1987
)
0.27
" In the first (pranoprofen) study, the mean time to maximum concentration was significantly shorter, and the mean maximum plasma concentration as well as absorption rate constant had a tendency to be greater after the morning than after the evening trial."( Chronopharmacokinetic studies of pranoprofen and procainamide.
Ebihara, A; Fujimura, A; Kajiyama, H; Kumagai, Y; Nakashima, H; Sugimoto, K, 1989
)
0.28
" PA's clinical pharmacology has been studied extensively and its bioavailability (75-95%); volume of distribution (1."( Procainamide: clinical pharmacology and efficacy against ventricular arrhythmias.
Giardina, EG, 1984
)
0.27
"The purpose of this study was to determine the bioavailability of N-Acetylprocainamide (NAPA) from mixed diet in rats."( Bioavailability of N-acetylprocainamide from mixed diet in rats.
Durrani, M; Gupta, SD; Kamath, BL; Lai, CM; Stampfli, H; Yacobi, A, 1981
)
0.26
" A substantial degree of interpatient and intrapatient variability in the absorption rate for NAPA was observed."( N-Acetylprocainamide kinetics and clinical response during repeated dosing.
Cohen, J; Gaarder, T; Hurst, A; Jelliffe, RW; Rodman, JH, 1982
)
0.26
" The elimination rate constant, clearance, and absolute bioavailability of the drug (determined by AUC measurements and the amounts excreted unchanged in the urine) decreased significantly with age."( Age-related pharmacokinetics of N-acetylprocainamide in rats.
Kamath, BL; Lai, CM; Look, ZM; Stampfli, HF; Yacobi, A, 1983
)
0.27
"Thin-layer chromatographic methods were applied for bioavailability studies of procainamide in serum and urine."( Thin-layer chromatographic determination of procainamide and N-acetylprocainamide in human serum and urine at single-dose levels.
Kark, B; Keller, A; Sistovaris, N, 1983
)
0.27
" In a separate experiment when mice were fed purified hypericin, the active component of St John's wort, a significant increase in bioavailability (53%) of procainamide was observed compared with the control group."( Drug-herb interaction: effect of St John's wort on bioavailability and metabolism of procainamide in mice.
Actor, JK; Dasgupta, A; Hovanetz, M; Olsen, M; Wells, A, 2007
)
0.34
"St John's wort has an acute effect to increase bioavailability of procainamide but has no effect on its metabolism."( Drug-herb interaction: effect of St John's wort on bioavailability and metabolism of procainamide in mice.
Actor, JK; Dasgupta, A; Hovanetz, M; Olsen, M; Wells, A, 2007
)
0.34

Dosage Studied

ExcerptRelevanceReference
" The presence of PG generally enhanced the absorption of each drug, and the degree of enhancement appeared to be related to the percentage of PG in the dosing solution."( Propylene glycol as a vehicle for percutaneous absorption of therapeutic agents.
Bailey, DN,
)
0.13
"2 ml/min, was less than half that observed in healthy adults suggesting markedly reduced dosage requirements."( Procainamide pharmacokinetics in patients on continuous ambulatory peritoneal dialysis.
Beirne, GJ; Moorthy, AV; Raehl, CL, 1986
)
0.27
" In these studies, we showed that NAPA has an elimination-phase half-life that is more than twice as long as procainamide and suggested that patient compliance and arrhythmia suppression might be improved if NAPA were used to circumvent the inconvenience of the frequent dosing schedule that has been recommended for procainamide."( Pharmacokinetics of N-acetylprocainamide.
Atkinson, AJ; Ruo, TI, 1986
)
0.27
" Such a test was needed to evaluate the pharmacokinetic characteristics of controlled-release dosage forms characterized by long half-lives at low plasma concentration."( More-sensitive enzyme-multiplied immunoassay technique for procainamide and N-acetylprocainamide in plasma, serum, and urine.
Dhruv, RA; Henry, PR, 1988
)
0.27
" Although the greater bioequivalence, lesser variability, and the greater number of tablet dosage sizes would favor product A, patients stabilized on a particular brand of sustained-release procainamide should not be switched to another product without careful monitoring."( Comparative bioequivalence and efficacy of two sustained-release procainamide formulations in patients with cardiac arrhythmias.
Destache, CJ; Hilleman, DE; Mohiuddin, SM; Ortmeier, BG; Patterson, AJ,
)
0.13
" The mean area under plasma concentration--time curve 0 to 12 hours after dosing increased 39% for procainamide (19."( Trimethoprim inhibition of the renal clearance of procainamide and N-acetylprocainamide.
Andress, E; Chase, SL; Ferguson, RK; Greenspon, AJ; Kosoglou, T; Lottes, S; Rocci, ML; Vlasses, PH, 1989
)
0.28
"5 and 3 g every 8 hours resulted in systematic underprediction of observed concentrations at the two highest oral dosing rates."( N-acetylprocainamide kinetics during intravenous infusions and subsequent oral doses in patients with coronary artery disease and ventricular arrhythmias.
Crawford, MH; Kennedy, GT; Ludden, TM,
)
0.13
" An extensive trial design incorporated the approaches of (1) generation of dose-response relations, (2) randomized crossover, and (3) prolonged electrocardiographic monitoring."( Antiarrhythmic efficacy, pharmacokinetics and safety of N-acetylprocainamide in human subjects: comparison with procainamide.
Higgins, SB; Oates, JA; Reele, SB; Roden, DM; Smith, RF; Wilkinson, GR; Woosley, RL, 1980
)
0.26
" Thus, the dosage of procainamide must be individualized for both overall renal function (GFR) and the age-related variations in renal tubular secretion that are of most note in children and the elderly."( Aging and renal clearance of procainamide and acetylprocainamide.
Camacho, M; Drayer, DE; Kluger, J; Reidenberg, MM, 1980
)
0.26
" The initial dosage of NAPA was 500 mg every 8 hours, which was increased by 500 mg increments every few days until 90 percent suppression of arrhythmia or intolerable adverse effects occurred."( Clinical pharmacology and antiarrhythmic efficacy of N-acetylprocainamide.
Jaillon, P; Kates, RE; Peters, F; Winkle, RA, 1981
)
0.26
" Drug fever developed in one patient, and another had a mild recurrence of lupus symptoms during high-dose acetylprocainamide therapy that regressed with dosage reduction."( Acetylprocainamide therapy in patients with previous procainamide-induced lupus syndrome.
Drayer, DE; Kluger, J; Lahita, R; Reidenberg, MM, 1981
)
0.26
"With ordinary procainamide tablets a dosing interval of 3-4 hours must be chosen to achieve therapeutically useful plasma concentrations during the entire interval."( [Steady-state plasma and saliva concentrations of procainamide and N-acetyl-procainamide after a sustained release preparation].
Galeazzi, RL; Karlaganis, G; Pirovino, M, 1980
)
0.26
" Symptomatic effects were common, with seven patients requiring a reduction in dosage or discontinuation of therapy."( Long-term antiarrhythmic therapy with acetylprocainamide.
Drayer, DE; Kluger, J; Leech, S; Lloyd, V; Reidenberg, MM, 1981
)
0.26
"In six normal subjects and 6 patients with primary cardiomyopathy, left ventricular performance was evaluated at rest and during isometric handgrip exercise after 4 days of oral N-acetylprocainamide (NAPA) at each of the three dosage levels (3, 4, 5, and 6 gm/day)."( Hemodynamic effects of N-acetylprocainamide in heart disease.
Amon, KW; Crawford, MH; Kennedy, GT; Ludden, TM; O'Rourke, RA; Sodums, MT, 1982
)
0.26
"Despite widespread marketing of a sustained release preparation of procainamide hydrochloride (PROCAN-SR, Parke-Davis), published literature demonstrating its efficacy in maintaining uniform serum drug levels over a 6-hour dosing interval is derived from only normal healthy volunteers."( Serum drug concentrations in patients with ischemic heart disease after administration of a sustained release procainamide preparation.
Mirando, T; Zema, MJ, 1983
)
0.27
" The clinical implications from this study necessitate dosage adjustments of procainamide in patients being concomitantly treated with cimetidine."( Cimetidine-procainamide pharmacokinetic interaction in man: evidence of competition for tubular secretion of basic drugs.
Heinzow, B; McLean, A; Somogyi, A, 1983
)
0.27
" The trend of nonlinearity may be more evident on chronic dosing of the drug when accumulation sets in."( Kinetics of procainamide N-acetylation in the rat in vivo and in the perfused rat liver preparation.
Cherry, WF; Fayz, S; Finkle, C; Huang, JC; Kong, P; Pang, KS,
)
0.13
" PD measurements (PQ, QS, QR, QT, RR, and HR) were collected prior to dosing and over a 24 h period."( Application of computer-assisted radiotelemetry in the pharmacokinetic and pharmacodynamic modeling of procainamide and N-acetylprocainamide.
Eddington, ND; Kharidia, J, 1996
)
0.29
" A new sustained-release formulation, Procanbid, which allows for twice-daily dosing was recently approved for marketing in the United States."( Effect of age, gender, and race on steady state procainamide pharmacokinetics after administration of procanbid sustained-release tablets.
Abel, RB; de Vries, TM; Eldon, MA; Koup, JR; Smithers, JA, 1998
)
0.3
"The dosage regimen of a drug eliminated predominantly through the kidney need to be adjusted for the patients with renal disease."( Quantitative estimation of renal clearance of N-acetylprocainamide in rats with various experimental acute renal failure.
He, YL; Hori, R; Kitada, N; Yasuhara, M, 2001
)
0.31
"To evaluate dosing and pharmacokinetic parameters of intravenous continuous-infusion procainamide in neonates, and to identify dosage regimens and factors leading to therapeutic procainamide levels and minimal adverse events."( Therapeutic levels of intravenous procainamide in neonates: a retrospective assessment.
Cannon, BC; Friedman, RA; Kertesz, NJ; Moffett, BS, 2006
)
0.33
" The dosage regimen for intravenous procainamide required to achieve therapeutic levels in neonates is similar to that of older infants and children."( Therapeutic levels of intravenous procainamide in neonates: a retrospective assessment.
Cannon, BC; Friedman, RA; Kertesz, NJ; Moffett, BS, 2006
)
0.33
"Procainamide is a useful agent for management of ventricular arrhythmia, however its disposition and appropriate dosing during extracorporeal membrane oxygenation (ECMO) is unknown."( Procainamide pharmacokinetics during extracorporeal membrane oxygenation.
Rosenbaum, AN; Vollmer, NJ; Wieruszewski, PM; Wittwer, ED, 2023
)
0.91
[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 (2)

ClassDescription
benzamides
acetamidesCompounds with the general formula RNHC(=O)CH3.
[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 (17)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency3.16230.100020.879379.4328AID588453
NFKB1 protein, partialHomo sapiens (human)Potency5.01190.02827.055915.8489AID895; AID928
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
regulator of G-protein signaling 4Homo sapiens (human)Potency0.21170.531815.435837.6858AID504845
arylsulfatase AHomo sapiens (human)Potency3.01311.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency1.88880.035520.977089.1251AID504332
gemininHomo sapiens (human)Potency0.73080.004611.374133.4983AID624296
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency35.48130.251215.843239.8107AID504327
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency6.30960.00106.000935.4813AID944
Ataxin-2Homo sapiens (human)Potency25.11890.011912.222168.7989AID588378
[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)
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
Bile salt export pumpHomo sapiens (human)IC50 (µMol)422.66670.11007.190310.0000AID1443980; AID1449628; AID1473738
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)100.00000.00091.901410.0000AID240820
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)IC50 (µMol)8.80000.18003.68578.8000AID681348
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)IC50 (µMol)5.00001.00004.446710.0000AID681345
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (69)

Processvia Protein(s)Taxonomy
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)
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)
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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (38)

Processvia Protein(s)Taxonomy
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)
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 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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
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)
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)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (78)

Assay IDTitleYearJournalArticle
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
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.
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.
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
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.
AID22810The maximum Percent change from control in the rate of rise of phase 0 of the action potential at 1 uM concentration on Canine Purkinje fibers.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID60486Efficacy in blocking sustained ventricular tachycardia (rate>250 bpm) elicited by programmed electrical stimulation in anesthetized dogs after iv administration of dose 9 mg/kg; no. of successful exp / total no. of exp = 4/41987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Rational design of 4-[(methylsulfonyl)amino]benzamides as class III antiarrhythmic agents.
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.
AID681348TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT1-expressing MDCK cells2001Pharmaceutical research, Nov, Volume: 18, Issue:11
Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules.
AID56859Maximum percent change in repolarization at 100 uM concentration on Canine Purkinje fibers.; value ranges from 14-201989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
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.
AID55751Concentration required for 20% increase in action potential duration of canine Purkinje fiber (intracellular electrophysiology) in vitro measured at 95% repolarization was reported. NR means 10% increase in APD95 (C10APD95) was observed at 30 um(221987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Rational design of 4-[(methylsulfonyl)amino]benzamides as class III antiarrhythmic agents.
AID681981TP_TRANSPORTER: inhibition of TEA uptake (TEA: 5 uM, N-acetyl procainamide: 1000 uM) in OCT2-expressing HEK293 cells2002Journal of the American Society of Nephrology : JASN, Jul, Volume: 13, Issue:7
cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID56083Maximum percent change in conduction time (CT) at 100 uM concentration tested on Canine ventricular muscle fibre1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
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.
AID22813The maximum percent change in action potential (Vmax ) at concentration observed (0.1 uM ) was tested on Canine Purkinje fibers.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
AID56082Maximum percent change in conduction time (CT) at 0.1 uM concentration tested on Canine ventricular muscle fibre1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
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.
AID681980TP_TRANSPORTER: inhibition of TEA uptake (TEA: 5 uM, N-acetyl procainamide: 1000 uM) in OCT2A-expressing HEK293 cells2002Journal of the American Society of Nephrology : JASN, Jul, Volume: 13, Issue:7
cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney.
AID55769Concentration required for 20% increase in the functional refractory period of canine ventricular muscle (extracellular electrophysiology) in vitro was reported. Range is between 5.6-8001987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Rational design of 4-[(methylsulfonyl)amino]benzamides as class III antiarrhythmic agents.
AID60823Maximum percent change in functional refractory period (FRP) at 100 uM on Canine ventricular muscle fibre.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
AID22809The maximum Percent change from control in the rate of rise of phase 0 of the action potential at 100 uM concentration on Canine Purkinje fibers.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
AID22800Percent change from control in the rate of rise of phase 0 of the action potential at 10 uM concentration on Canine Purkinje fibers.; value ranges from 0-21989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
AID60086Efficacy in blocking sustained ventricular tachycardia (rate>250 bpm) elicited by programmed electrical stimulation in conscious dogs after iv administration; NT means not tested1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Rational design of 4-[(methylsulfonyl)amino]benzamides as class III antiarrhythmic agents.
AID56087Maximum percent change in conduction time (CT) at 1 uM concentration tested on Canine ventricular muscle fibre1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
AID60836Percent change from control in the functional refractory period (FRP) at 10 uM conc. on Canine ventricular muscle fibre.; value ranges from 11-231989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
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.
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.
AID60827Maximum percent change in functional refractory period (FRP) at 10 uM on Canine ventricular muscle fibre.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID227700Anticonvulsant activity2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity.
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.
AID75809Concentration of compound which gives a 20% decrease in contractile force was tested on papillary muscle of guinea pig, activity was expressed as EC-20.; NR is not reached.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
AID681345TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT2-expressing MDCK cells2001Pharmaceutical research, Nov, Volume: 18, Issue:11
Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules.
AID56997Percent change in repolarization at 10 Purkinje fibers; value ranges from -3.0-7.0.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
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.
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.
AID56090Percent change from control in conduction time (CT) at 10 uM concentration tested on Canine ventricular muscle fibre.; value ranges from -11.0-01989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Heterocyclic analogues of benzamide antiarrhythmic agents.
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.
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.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (256)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990174 (67.97)18.7374
1990's44 (17.19)18.2507
2000's18 (7.03)29.6817
2010's13 (5.08)24.3611
2020's7 (2.73)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.10

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

MetricThis Compound (vs All)
Research Demand Index19.10 (24.57)
Research Supply Index5.71 (2.92)
Research Growth Index4.23 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.10)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials16 (5.59%)5.53%
Reviews14 (4.90%)6.00%
Case Studies28 (9.79%)4.05%
Observational0 (0.00%)0.25%
Other228 (79.72%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]