Page last updated: 2024-11-12

omecamtiv mecarbil

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Cross-References

ID SourceID
PubMed CID11689883
CHEMBL ID1800955
CHEBI ID188664
SCHEMBL ID400544
MeSH IDM0543834

Synonyms (62)

Synonym
HY-14233
methyl 4-[[2-fluoro-3-[(6-methylpyridin-3-yl)carbamoylamino]phenyl]methyl]piperazine-1-carboxylate
amg-423
omecamtiv mecarbil ,
ck-452
ck-1827452
methyl 4-[[2-luoro-3-[(6-methylpyridin-3-yl)carbamoylamino]phenyl]methyl]piperazine-1-carboxylate
873697-71-3
CHEBI:188664
CHEMBL1800955 ,
D09648
omecamtiv mecarbil (usan/inn)
omecamtiv mecarbil [usan:inn]
methyl 4-((2-fluoro-3-(((6-methylpyridin-3-yl)carbamoyl)amino)phenyl)methyl) piperazine-1-carboxylate
unii-2m19539erk
2m19539erk ,
1-piperazinecarboxylic acid, 4-((2-fluoro-3-((((6-methyl-3-pyridinyl)amino)carbonyl)amino)phenyl)methyl)-, methyl ester
ck 1827452
bdbm50348423
methyl 4-(2-fluoro-3-(3-(6-methylpyridin-3-yl)ureido)benzyl)piperazine-1-carboxylate
BCP9001023
methyl 4-[(2-fluoro-3-{[(6-methylpyridin-3-yl)carbamoyl]amino}phenyl)methyl]piperazine-1-carboxylate
BCPP000140
BCP0726000250
omecamtiv mecarbil (ck-1827452)
NCGC00346618-01
CS-0460
omecamtiv mecarbil [usan]
omecamtiv mecarbil [who-dd]
omecamtiv mecarbil [inn]
S2623
amg 423
gtpl8740
smr004703017
MLS006011266
SCHEMBL400544
methyl 4-[[2-fluoro-3-[n'-(6-methylpyridin-3-yl)ureido]phenyl]methyl]piperazine-1-carboxylate
ck1827452
methyl 4-(2-fluoro-3-{[(6-methylpyridin-3-yl)carbamoyl]amino}benzyl)piperazine-1-carboxylate
AC-32748
AKOS026674125
J-690376
EX-A714
ck-1827452;omecamtiv mecarbil
HMS3656F05
mfcd18633260
AS-60560
NCGC00346618-07
RFUBTTPMWSKEIW-UHFFFAOYSA-N
SW219490-1
DB11816
omecamtiv mercarbil
FT-0700389
F15273
omecamtiv mecarbil;ck-1827452;ck 1827452
BCP03048
Q7089956
SB16684
omecamtiv-mecarbil
CCG-268662
NCGC00346618-02
DTXSID901025949

Research Excerpts

Overview

Omecamtiv mecarbil is a small molecule that has been shown to improve cardiac function in patients with heart failure (HF) with reduced ejection fraction. It is being developed as an oral modified release tablet for subjects with chronic HF.

ExcerptReferenceRelevance
"Omecamtiv mecarbil is a small molecule that has been shown to improve cardiac function in patients with heart failure (HF) with reduced ejection fraction and is currently being developed as an oral modified release tablet for subjects with chronic HF. "( Population Pharmacokinetic Properties of Omecamtiv Mecarbil in Healthy Subjects and Patients With Heart Failure With Reduced Ejection Fraction.
Ahamadi, M; Chen, PW; Dutta, S; Lee, E; Trivedi, A, 2022
)
2.43
"Omecamtiv mecarbil (OM) is a selective small molecule activator of cardiac myosin that prolongs myocardial systole and increases stroke volume without apparent effects on myocardial oxygen demand."( Omecamtiv mecarbil treatment improves post-resuscitation cardiac function and neurological outcome in a rat model.
Chen, WJ; Huang, CH; Tsai, MS; Wu, SN, 2022
)
2.89
"Omecamtiv mecarbil is a well-tolerated drug in heart failure patients. "( Safety and efficacy of omecamtiv mecarbil for heart failure: A systematic review and meta-analysis.
Alqatati, F; Bugazia, S; Elbahnasawy, M; Elsayed, SM; Elsnhory, AB; Fathy, MA; Nourelden, AZ; Ragab, KM; Shehata, M,
)
1.88
"Omecamtiv mecarbil (OM) is a positive inotrope that is thought to bind directly to an allosteric site of the β-cardiac myosin. "( Insights into the Mechanism of the Cardiac Drug Omecamtiv Mecarbil─A Computational Study.
Chakraborti, A; Schwartz, SD; Tardiff, JC, 2022
)
2.42
"Omecamtiv mecarbil (OM) is a direct myosin activator that augments left ventricular systolic function. "( KCCQ total symptom score, clinical outcome measures, and adverse events associated with omecamtiv mecarbil for heart failure with reduced ejection fraction: a systematic review and meta-analysis of randomized controlled trials.
Ibrahim, R; Khludenev, G; Olagunju, A; Takamatsu, C; Terrani, K; William, P, 2023
)
2.58
"Omecamtiv mecarbil is a novel, selective cardiac myosin activator that has been shown to improve cardiac function and to decrease ventricular volumes, heart rate, and N-terminal pro-B-type natriuretic peptide in patients with chronic HF."( Omecamtiv Mecarbil in Chronic Heart Failure With Reduced Ejection Fraction: Rationale and Design of GALACTIC-HF.
Büchele, G; Diaz, R; Felker, GM; Honarpour, N; Kurtz, CE; Legg, JC; Malik, FI; McMurray, JJV; Metra, M; Solomon, SD; Teerlink, JR; Varin, C, 2020
)
2.72
"Omecamtiv mecarbil (OM) is a putative positive inotropic tool for treatment of systolic heart dysfunction, based on the finding that in vivo it increases the ejection fraction and in vitro it prolongs the actin-bond life time of the cardiac and slow-skeletal muscle isoforms of myosin. "( Orthophosphate increases the efficiency of slow muscle-myosin isoform in the presence of omecamtiv mecarbil.
Caremani, M; Gallart, C; Governali, S; Linari, M; Lombardi, V; Ottenheijm, C; Pertici, I; Piazzesi, G; Stienen, G, 2020
)
2.22
"Omecamtiv mecarbil (OM) is a selective cardiac myosin activator (myotrope), currently in Phase 3 clinical investigation as a novel treatment for heart failure with reduced ejection fraction. "( Effects of omecamtiv mecarbil on calcium-transients and contractility in a translational canine myocyte model.
Gao, B; Qu, Y; Sutherland, W; Vargas, HM, 2020
)
2.39
"Omecamtiv mecarbil (OM) is a novel medicine for systolic heart failure, targeting myosin to enhance cardiomyocyte performance. "( Effects of omecamtiv mecarbil on failing human ventricular trabeculae and interaction with (-)-noradrenaline.
Beard, N; Chan, W; Cheesman, E; Dashwood, A; Haqqani, H; Hay, K; Molenaar, P; Spratt, M; Wong, YW, 2021
)
2.45
"Omecamtiv mecarbil (OM) is a myosin activator (myotrope), developed as a potential therapeutic agent for heart failure with reduced ejection fraction. "( Comprehensive in vitro pro-arrhythmic assays demonstrate that omecamtiv mecarbil has low pro-arrhythmic risk.
Arimura, Z; Fang, M; Gao, B; Qu, Y; Vargas, HM, 2021
)
2.3
"Omecamtiv mecarbil (OM) is a novel cardiac myosin activator that is currently in clinical development for the treatment of heart failure. "( Pharmacokinetics, Disposition, and Biotransformation of [
Dutta, S; Lee, E; Mackowski, M; Trivedi, A; Wahlstrom, J, 2021
)
2.06
"Omecamtiv mecarbil (OM) is a cardiac myosin activator in clinical development for the treatment of heart failure. "( Switchability and minimal effect of food on pharmacokinetics of modified release tablet strengths of omecamtiv mecarbil, a cardiac myosin activator.
Abbasi, S; Dutta, S; Flach, S; Jafarinasabian, P; Lee, E; Mackowski, M; Oberoi, RK; Simiens, MA; Terminello, B; Trivedi, A; Zhang, H, 2021
)
2.28
"Omecamtiv mecarbil (OM) is a novel cardiac myosin activator in development for the treatment of heart failure with reduced ejection fraction. "( Effect of Omecamtiv Mecarbil on the Pharmacokinetics of Metformin, a Probe Substrate for MATE1/MATE2-K, in Healthy Subjects.
Abbasi, S; Dutta, S; Flach, S; Jafarinasabian, P; Lee, E; Oberoi, RK; Spring, M; Trivedi, A; Zhang, H, 2021
)
2.47
"Omecamtiv mecarbil (OM) is a novel selective cardiac myosin activator under investigation for the treatment of heart failure with reduced ejection fraction. "( Effect of Varying Degrees of Hepatic Impairment on the Pharmacokinetics of Omecamtiv Mecarbil.
Abbasi, S; Dutta, S; Flach, S; Hutton, S; Jafarinasabian, P; Lee, E; Mackowski, M; Oberoi, RK; Trivedi, A; Zhang, H, 2021
)
2.29
"Omecamtiv mecarbil (OM) is a cardiac myosin activator under clinical development for the treatment of heart failure. "( Relative Bioavailability of Omecamtiv Mecarbil Pediatric Minitablet Formulations in Healthy Adult Subjects.
Bhatia, A; Dutta, S; Flach, S; Jafarinasabian, P; Lee, E; Mackowski, M; Terminello, B; Trivedi, A; Zhang, H, 2021
)
2.36
"Omecamtiv mecarbil (OM) is a novel selective cardiac myosin activator under investigation for the treatment of heart failure. "( Omecamtiv mecarbil does not prolong QTc intervals at therapeutic concentrations.
Abbasi, S; Brooks, A; Darpo, B; Dutta, S; Flach, S; Hsu, CP; Israel, S; Jafarinasabian, P; Lee, E; Terminello, B; Trivedi, A; Xue, H; Zhang, H, 2022
)
3.61
"Omecamtiv mecarbil (OM) is a cardiac myosin activator under development for the treatment of heart failure. "( Pharmacokinetic Evaluation of the CYP3A4 and CYP2D6 Drug-Drug Interaction and CYP3A4 Induction Potential of Omecamtiv Mecarbil: Two Open-Label Studies in Healthy Subjects.
Abbasi, S; Dutta, S; Flach, S; Jafarinasabian, P; Lee, E; Malik, FI; Trivedi, A; Zhang, H, 2022
)
2.38
"Omecamtiv mecarbil (OM) is a novel cardiac myosin activator in development for the treatment of heart failure (HF) with reduced ejection fraction. "( Pharmacokinetic Drug-Drug Interaction Study of Omecamtiv Mecarbil With Omeprazole, a Proton Pump Inhibitor, in Healthy Subjects.
Abbasi, S; Dutta, S; Flach, S; Jafarinasabian, P; Lee, E; Sohn, W; Terminello, B; Trivedi, A; Zhang, H, 2022
)
2.42
"Omecamtiv mecarbil (OM) is a cardiac myosin activator under development for the treatment of heart failure. "( Pharmacokinetics, Tolerability, and Safety of Single and Multiple Omecamtiv Mecarbil Doses in Healthy Japanese and Caucasian Subjects.
Abbasi, S; Aoki, M; Dutta, S; Hutton, S; Lee, E; Mackowski, M; Malik, FI; Trivedi, A, 2021
)
2.3
"Omecamtiv mecarbil (OM) is a novel cardiac myosin activator in development for the treatment of heart failure. "( Evaluation of drug-drug interaction potential between omecamtiv mecarbil and rosuvastatin, a BCRP substrate, with a clinical study in healthy subjects and using a physiologically-based pharmacokinetic model.
Abbasi, S; Dutta, S; Flach, S; Jafarinasabian, P; Kulkarni, P; Lee, E; Sohn, W; Spring, M; Trivedi, A; Wahlstrom, J; Zhang, H, 2021
)
2.31
"Omecamtiv mecarbil is a selective, small-molecule activator of cardiac myosin that is being developed as a potential treatment for heart failure with reduced ejection fraction. "( Mechanistic and structural basis for activation of cardiac myosin force production by omecamtiv mecarbil.
Hartman, JJ; Houdusse, A; Malik, FI; Planelles-Herrero, VJ; Robert-Paganin, J, 2017
)
2.12
"Omecamtiv mecarbil (OM) is a pharmacological agent that augments cardiac contractile function by enhancing myofilament Ca"( Omecamtiv Mecarbil Abolishes Length-Mediated Increase in Guinea Pig Cardiac Myofiber Ca
Chandra, M; Gollapudi, SK; Reda, SM, 2017
)
3.34
"Omecamtiv mecarbil (OM) is a myosin activator agent developed for the treatment of heart failure. "( Frequency-dependent effects of omecamtiv mecarbil on cell shortening of isolated canine ventricular cardiomyocytes.
Almássy, J; Bányász, T; Horváth, B; Magyar, J; Nánási, PP; Papp, Z; Szentandrássy, N; Tóth, A; Veress, R, 2017
)
2.18
"Omecamtiv mecarbil (OM) is a positive cardiac inotrope in phase-3 clinical trials for treatment of heart failure. "( Positive cardiac inotrope omecamtiv mecarbil activates muscle despite suppressing the myosin working stroke.
Barua, B; Goldman, YE; Greenberg, MJ; Ostap, EM; Winkelmann, DA; Woody, MS, 2018
)
2.22
"Omecamtiv mecarbil (OM) is a compound that has been developed to treat systolic heart failure via targeting the cardiac myosin heavy chain to increase myocardial contractility."( Omecamtiv Mecarbil Slows Myosin Kinetics in Skinned Rat Myocardium at Physiological Temperature.
Awinda, PO; Kieu, TT; Tanner, BCW, 2019
)
2.68
"Omecamtiv mecarbil is a selective cardiac myosin activator that augments cardiac contractility in patients with systolic heart failure through a dose-dependent increase in systolic ejection time."( Safety and tolerability of omecamtiv mecarbil during exercise in patients with ischemic cardiomyopathy and angina.
Chen, MM; Chou, W; Eisenberg, P; Escandón, R; Greenberg, BH; Lee, JH; Malik, FI; Megreladze, I; Saikali, KG; Shaburishvili, T; Treshkur, T; Wasserman, SM; Wolff, AA, 2015
)
2.16
"Omecamtiv mecarbil (OM) is a novel inotropic agent that prolongs systolic ejection time and increases ejection fraction through myosin ATPase activation. "( Myosin Activator Omecamtiv Mecarbil Increases Myocardial Oxygen Consumption and Impairs Cardiac Efficiency Mediated by Resting Myosin ATPase Activity.
Aasum, E; Bakkehaug, JP; Boardman, N; Engstad, ET; How, OJ; Kildal, AB; Larsen, TS; Myrmel, T; Næsheim, T; Rønning, L, 2015
)
2.2
"Omecamtiv mecarbil is a promising new inotropic agent developed for heart failure that may circumvent such limitations."( Omecamtiv Mecarbil, a Cardiac Myosin Activator, Increases Ca2+ Sensitivity in Myofilaments With a Dilated Cardiomyopathy Mutant Tropomyosin E54K.
Li, BH; Ryba, DM; Solaro, RJ; Utter, MS; Wolska, BM, 2015
)
2.58
"Omecamtiv Mecarbil (OM) is a small molecule allosteric effector of cardiac myosin that is in clinical trials for treatment of systolic heart failure. "( Structural basis for drug-induced allosteric changes to human β-cardiac myosin motor activity.
Forgacs, E; Miller, MT; Stock, AM; Winkelmann, DA, 2015
)
1.86
"Omecamtiv mecarbil is a novel small molecule that directly activates cardiac myosin and increases cardiac contractility without increasing cardiac myocyte intracellular calcium. "( Relative bioavailability, food effect, and safety of the single-dose pharmacokinetics of omecamtiv mecarbil following administration of different modified-release formulations in healthy subjects.
Alvarez, P; Banfield, C; Johnson, J; Malik, F; Monsalvo, ML; Palaparthy, R; Smith, B; Yan, L, 2016
)
2.1
"Omecamtiv mecarbil (OM) is a selective cardiac myosin activator that increases myocardial function in healthy volunteers and in patients with chronic heart failure."( Acute Treatment With Omecamtiv Mecarbil to Increase Contractility in Acute Heart Failure: The ATOMIC-AHF Study.
Cleland, JGF; Dickstein, K; Ezekowitz, JA; Felker, GM; Filippatos, GS; Kim, JB; Knusel, B; Lei, L; Malik, FI; McMurray, JJV; Metra, M; Ponikowski, P; Teerlink, JR; Wasserman, SM; Wolff, AA, 2016
)
2.2
"Omecamtiv mecarbil (OM) is a myosin activator agent recently developed for treatment of heart failure. "( Dose-dependent electrophysiological effects of the myosin activator omecamtiv mecarbil in canine ventricular cardiomyocytes.
Banyasz, T; Horvath, B; Kistamas, K; Magyar, J; Masuda, L; Nanasi, PP; Papp, Z; Szentandrassy, N; Vaczi, K, 2016
)
2.11

Effects

ExcerptReferenceRelevance
"Omecamtiv mecarbil has a clearance of 11.7 L/h (0.701% relative standard error) and a central volume distribution of 275 L (2.12% relative standard error)."( Population Pharmacokinetic Properties of Omecamtiv Mecarbil in Healthy Subjects and Patients With Heart Failure With Reduced Ejection Fraction.
Ahamadi, M; Chen, PW; Dutta, S; Lee, E; Trivedi, A, 2022
)
1.71

Toxicity

ExcerptReferenceRelevance
" An ideal inotropic drug should restore effective tissue perfusion by enhancing myocardial contractility without causing adverse effects."( Acute heart failure with low cardiac output: can we develop a short-term inotropic agent that does not increase adverse events?
Campia, U; Gheorghiade, M; Nodari, S, 2010
)
0.36
" No dose-dependent differences emerged in the proportion of patients stopping ETT3 for any reason or in the pattern of adverse events."( Safety and tolerability of omecamtiv mecarbil during exercise in patients with ischemic cardiomyopathy and angina.
Chen, MM; Chou, W; Eisenberg, P; Escandón, R; Greenberg, BH; Lee, JH; Malik, FI; Megreladze, I; Saikali, KG; Shaburishvili, T; Treshkur, T; Wasserman, SM; Wolff, AA, 2015
)
0.71
" Pooled analysis showed that omecamtiv mecarbil is not associated with increased incidence of death, any adverse events, hypotension, heart failure, ventricular tachyarrhythmia, dyspnea, dizziness, and serious adverse events."( Safety and efficacy of omecamtiv mecarbil for heart failure: A systematic review and meta-analysis.
Alqatati, F; Bugazia, S; Elbahnasawy, M; Elsayed, SM; Elsnhory, AB; Fathy, MA; Nourelden, AZ; Ragab, KM; Shehata, M,
)
0.73
" This review compares OM to placebo by evaluating its effect on clinical outcomes and adverse events in patients with heart failure with reduced left ventricular ejection fraction."( KCCQ total symptom score, clinical outcome measures, and adverse events associated with omecamtiv mecarbil for heart failure with reduced ejection fraction: a systematic review and meta-analysis of randomized controlled trials.
Ibrahim, R; Khludenev, G; Olagunju, A; Takamatsu, C; Terrani, K; William, P, 2023
)
1.13

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic and safety data were analyzed from 62 and 63 subjects in the fasting and fed states, respectively."( Relative bioavailability, food effect, and safety of the single-dose pharmacokinetics of omecamtiv mecarbil following administration of different modified-release formulations in healthy subjects.
Alvarez, P; Banfield, C; Johnson, J; Malik, F; Monsalvo, ML; Palaparthy, R; Smith, B; Yan, L, 2016
)
0.66
" Coadministration of OM with omeprazole was not associated with any clinically significant pharmacokinetic drug interactions."( Pharmacokinetic Drug-Drug Interaction Study of Omecamtiv Mecarbil With Omeprazole, a Proton Pump Inhibitor, in Healthy Subjects.
Abbasi, S; Dutta, S; Flach, S; Jafarinasabian, P; Lee, E; Sohn, W; Terminello, B; Trivedi, A; Zhang, H, 2022
)
0.98
" The potential for a pharmacokinetic (PK) drug-drug interaction (DDI) was investigated, specifically to determine whether a single 50 mg dose of OM would impact the PKs of a single 10 mg dose of rosuvastatin in an open-label study in 14 healthy subjects."( Evaluation of drug-drug interaction potential between omecamtiv mecarbil and rosuvastatin, a BCRP substrate, with a clinical study in healthy subjects and using a physiologically-based pharmacokinetic model.
Abbasi, S; Dutta, S; Flach, S; Jafarinasabian, P; Kulkarni, P; Lee, E; Sohn, W; Spring, M; Trivedi, A; Wahlstrom, J; Zhang, H, 2021
)
0.87
" In conclusion, OM coadministered with digoxin or amiodarone did not result in any clinically relevant pharmacokinetic drug-drug interactions."( Pharmacokinetic Drug-Drug Interaction Study of Omecamtiv Mecarbil With Amiodarone and Digoxin in Healthy Subjects.
Abbasi, S; Dutta, S; Flach, S; Hsu, CP; Hutton, S; Jafarinasabian, P; Lee, E; Sohn, W; Trivedi, A; Zhang, H, 2022
)
0.98
" The objectives of this study were to analyze the pharmacokinetic (PK) properties of omecamtiv mecarbil and to investigate the effects of potential covariates on pertinent PK parameters using population PK modeling of data from 3 clinical trials in healthy subjects (n = 85) and 3 clinical trials in patients with HF (n = 4261)."( Population Pharmacokinetic Properties of Omecamtiv Mecarbil in Healthy Subjects and Patients With Heart Failure With Reduced Ejection Fraction.
Ahamadi, M; Chen, PW; Dutta, S; Lee, E; Trivedi, A, 2022
)
1.21

Compound-Compound Interactions

ExcerptReferenceRelevance
" The potential for a pharmacokinetic (PK) drug-drug interaction (DDI) was investigated, specifically to determine whether a single 50 mg dose of OM would impact the PKs of a single 10 mg dose of rosuvastatin in an open-label study in 14 healthy subjects."( Evaluation of drug-drug interaction potential between omecamtiv mecarbil and rosuvastatin, a BCRP substrate, with a clinical study in healthy subjects and using a physiologically-based pharmacokinetic model.
Abbasi, S; Dutta, S; Flach, S; Jafarinasabian, P; Kulkarni, P; Lee, E; Sohn, W; Spring, M; Trivedi, A; Wahlstrom, J; Zhang, H, 2021
)
0.87
" In vitro studies demonstrate OM as a substrate and inhibitor of P-glycoprotein (P-gp), which can result in drug-drug interactions."( Pharmacokinetic Drug-Drug Interaction Study of Omecamtiv Mecarbil With Amiodarone and Digoxin in Healthy Subjects.
Abbasi, S; Dutta, S; Flach, S; Hsu, CP; Hutton, S; Jafarinasabian, P; Lee, E; Sohn, W; Trivedi, A; Zhang, H, 2022
)
0.98

Bioavailability

ExcerptReferenceRelevance
"62 hours, and absolute bioavailability was estimated as 90%; elimination half-life was approximately 18."( Population pharmacokinetic-pharmacodynamic modeling of omecamtiv mecarbil, a cardiac myosin activator, in healthy volunteers and patients with stable heart failure.
Chow, AT; Ma, P; Malik, FI; Vu, T; Wang, YM; Xiao, JJ, 2015
)
0.66
" The relative bioavailability was high (> 75%) for three MR formulations but lower (< 65%) for the other two."( Relative bioavailability, food effect, and safety of the single-dose pharmacokinetics of omecamtiv mecarbil following administration of different modified-release formulations in healthy subjects.
Alvarez, P; Banfield, C; Johnson, J; Malik, F; Monsalvo, ML; Palaparthy, R; Smith, B; Yan, L, 2016
)
0.66
"The relative bioavailability of omecamtiv mecarbil was high (> 75%) for 3 of the five MR formulations."( Relative bioavailability, food effect, and safety of the single-dose pharmacokinetics of omecamtiv mecarbil following administration of different modified-release formulations in healthy subjects.
Alvarez, P; Banfield, C; Johnson, J; Malik, F; Monsalvo, ML; Palaparthy, R; Smith, B; Yan, L, 2016
)
0.94
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"5 mg OM MR tablets and to assess its relative bioavailability to the 25 mg MR tablet, a 25 mg oral solution under fed or fasted states in Study 2 (n = 34)."( Switchability and minimal effect of food on pharmacokinetics of modified release tablet strengths of omecamtiv mecarbil, a cardiac myosin activator.
Abbasi, S; Dutta, S; Flach, S; Jafarinasabian, P; Lee, E; Mackowski, M; Oberoi, RK; Simiens, MA; Terminello, B; Trivedi, A; Zhang, H, 2021
)
0.84
" The primary objective of this study was to determine the bioavailability of the minitablets relative to the adult matrix MR formulation tablets."( Relative Bioavailability of Omecamtiv Mecarbil Pediatric Minitablet Formulations in Healthy Adult Subjects.
Bhatia, A; Dutta, S; Flach, S; Jafarinasabian, P; Lee, E; Mackowski, M; Terminello, B; Trivedi, A; Zhang, H, 2021
)
0.92
"Relative bioavailability of slow-release minitablets was demonstrated to be similar to the adult matrix MR formulation."( Relative Bioavailability of Omecamtiv Mecarbil Pediatric Minitablet Formulations in Healthy Adult Subjects.
Bhatia, A; Dutta, S; Flach, S; Jafarinasabian, P; Lee, E; Mackowski, M; Terminello, B; Trivedi, A; Zhang, H, 2021
)
0.92
"Study 1 (n = 36) evaluated the bioavailability and pharmacokinetics after intravenous infusion (15 mg/h for 4 h) and an oral modified release (MR) tablet in healthy Japanese and Caucasian subjects using 25 mg single and multiple doses and 50 mg single dose."( Pharmacokinetics, Tolerability, and Safety of Single and Multiple Omecamtiv Mecarbil Doses in Healthy Japanese and Caucasian Subjects.
Abbasi, S; Aoki, M; Dutta, S; Hutton, S; Lee, E; Mackowski, M; Malik, FI; Trivedi, A, 2021
)
0.86

Dosage Studied

Omecamtiv mecarbil dosing guided by pharmacokinetics achieved plasma concentrations associated with improved cardiac function and decreased ventricular diameter. This study will provide essential dosing information for the requisite phase III trials.

ExcerptRelevanceReference
" New insight has been gained regarding volume management, including dosing strategies for intravenous loop diuretics and the role of ultrafiltration in patients with heart failure and renal dysfunction."( Acute decompensated heart failure: update on new and emerging evidence and directions for future research.
Albert, NM; Butler, J; Carson, PE; Collins, SP; Colvin-Adams, M; Dimarco, JP; Ezekowitz, JA; Fang, JC; Givertz, MM; Hernandez, AF; Hershberger, RE; Katz, SD; Krishnamani, R; Rogers, JG; Spertus, JA; Starling, RC; Stevenson, WG; Stough, WG; Sweitzer, NK; Tang, WH; Teerlink, JR; Walsh, MN; Westlake Canary, CA, 2013
)
0.39
"5 mg dosed every 8, 12, and 24 hours) showed that a pharmacodynamic effect (delta SET ≥20 milliseconds) could be maintained in the absence of excessive omecamtiv mecarbil plasma concentrations."( Population pharmacokinetic-pharmacodynamic modeling of omecamtiv mecarbil, a cardiac myosin activator, in healthy volunteers and patients with stable heart failure.
Chow, AT; Ma, P; Malik, FI; Vu, T; Wang, YM; Xiao, JJ, 2015
)
0.86
" This study will provide essential dosing information for the requisite phase III trials which will investigate whether the beneficial effects of omecamtiv mecarbil translate into improved clinical outcomes."( Omecamtiv mecarbil: a new cardiac myosin activator for the treatment of heart failure.
Dorhout, B; Liu, LC; Teerlink, JR; van der Meer, P; Voors, AA, 2016
)
2.08
"Omecamtiv mecarbil dosing guided by pharmacokinetics achieved plasma concentrations associated with improved cardiac function and decreased ventricular diameter."( Chronic Oral Study of Myosin Activation to Increase Contractility in Heart Failure (COSMIC-HF): a phase 2, pharmacokinetic, randomised, placebo-controlled trial.
Adams, KF; Cleland, JG; Ezekowitz, JA; Felker, GM; Goudev, A; Honarpour, N; Johnston, J; Macdonald, P; Malik, FI; McMurray, JJ; Metra, M; Mitrovic, V; Monsalvo, ML; Ponikowski, P; Serpytis, P; Solomon, SD; Spinar, J; Teerlink, JR; Tomcsányi, J; Vandekerckhove, HJ; Voors, AA, 2016
)
1.88
" Blood samples were collected up to 144 hours after dosing following administration of OM on days 1 and 9 to characterize plasma concentrations of OM."( Pharmacokinetic Drug-Drug Interaction Study of Omecamtiv Mecarbil With Omeprazole, a Proton Pump Inhibitor, in Healthy Subjects.
Abbasi, S; Dutta, S; Flach, S; Jafarinasabian, P; Lee, E; Sohn, W; Terminello, B; Trivedi, A; Zhang, H, 2022
)
0.98
"OM showed consistent and predictable pharmacokinetics after multiple dosing in Japanese subjects."( Pharmacokinetics, Tolerability, and Safety of Single and Multiple Omecamtiv Mecarbil Doses in Healthy Japanese and Caucasian Subjects.
Abbasi, S; Aoki, M; Dutta, S; Hutton, S; Lee, E; Mackowski, M; Malik, FI; Trivedi, A, 2021
)
0.86
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
ureas
[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 (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
EWS/FLI fusion proteinHomo sapiens (human)Potency6.66100.001310.157742.8575AID1259252; AID1259253; AID1259256
GVesicular stomatitis virusPotency15.09160.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency15.09160.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)10.00000.00011.774010.0000AID605254
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (69)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (31)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (24)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (112)

Assay IDTitleYearJournalArticle
AID1452489Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as end-systolic pressure at 16 ug/kg/min (Rvb = 87.48 to 97.85 mmHg)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1402191Positive inotropic activity in Sprague-Dawley rat ventricular myocytes assessed as change in ventricular cell contractility by measuring cell shortening at 1 uM2018European journal of medicinal chemistry, Jan-01, Volume: 143Design and synthesis of sulfonamidophenylethylureas as novel cardiac myosin activator.
AID1452486Positive inotropic activity in Sprague-Dawley rat heart assessed as fractional shortening at 8 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 38.60 to 55.81%)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID605332Volume of distribution in Beagle dog heart failure model2010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
AID1452483Positive inotropic activity in Sprague-Dawley rat heart assessed as ejection fraction at 4 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 67.16 to 85.81%)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1577036Activation of bovine cardiac actin thin filament complex-stimulated myosin S1 ATPase activity assessed as inorganic phosphate liberated at 10 uM incubated for 10 mins in presence of ATP by spectrophotometry relative to control2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design and synthesis of sulfonamidophenylethylamides as novel cardiac myosin activator.
AID605333Bioavailability in Beagle dog heart failure model2010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
AID1577035Activation of rabbit skeletal muscle actin thin filament complex-stimulated myosin S1 ATPase activity assessed as inorganic phosphate liberated at 100 uM incubated for 10 mins in presence of ATP by spectrophotometry relative to control2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design and synthesis of sulfonamidophenylethylamides as novel cardiac myosin activator.
AID1498822Activation of actin-stimulated bovine cardiac myosin S1 fragment ATPase activity in sarcomere at 10 uM after 10 mins by spectrophotometric analysis relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Exploration of diphenylalkyloxadiazoles as novel cardiac myosin activator.
AID605247Induction of contractility in Sprague-Dawley rat Cardiomyocytes assessed as change in fractional shortening at 0.2 uM2010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
AID605244Solubility of the compound at pH 5 by shake flask method2010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
AID1452469Positive inotropic activity in Sprague-Dawley rat heart assessed as heart rate at 8 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 281 to 347 bpm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452474Positive inotropic activity in Sprague-Dawley rat heart assessed as left ventricular internal diameter end diastole at 4 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 5.66 to 7.80 mm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452488Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as end-systolic pressure at 8 ug/kg/min (Rvb = 87.48 to 97.85 mmHg)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID605334Bioavailability in Sprague-Dawley rat2010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
AID605254Inhibition of CYP1A22010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
AID1452468Positive inotropic activity in Sprague-Dawley rat heart assessed as heart rate at 4 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 281 to 347 bpm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452498Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as dPdT max at 8 ug/kg/min (Rvb = 4162 to 5214 mmHg/s)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1402184Activation of actin-stimulated bovine cardiac myosin S1 fragment ATPase activity in sarcomere at 10 uM after 10 mins by spectrophotometric analysis relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Design and synthesis of sulfonamidophenylethylureas as novel cardiac myosin activator.
AID1452487Positive inotropic activity in Sprague-Dawley rat heart assessed as fractional shortening at 16 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 38.60 to 55.81%)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452494Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as end-diastolic pressure at 16 ug/kg/min (Rvb = 7.68 to 9.64 mmHg)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452504Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as dPdT min at 16 ug/kg/min (Rvb = -5462 to -4611 mmHg/s)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452477Positive inotropic activity in Sprague-Dawley rat heart assessed as left ventricular posterior wall thickness end systole at 4 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 2.07 to 2.46 mm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1498823Activation of actin-stimulated bovine cardiac myosin S1 fragment ATPase activity in sarcomere at 5 uM after 10 mins by spectrophotometric analysis relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Exploration of diphenylalkyloxadiazoles as novel cardiac myosin activator.
AID1452514Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as end-diastolic pressure at 2 ug/kg/min (Rvb = 7.68 mmHg)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID605255Ratio of extraction in human Liver microsomes2010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
AID1452519Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as dPdT min at 4 ug/kg/min (Rvb = -5462 to -4898 mmHg/s)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1242379Positive inotropic effect in Sprague-Dawley rat ventricular myocytes assessed as change in ventricular cell contractility at 400 nM by video edge detector relative to control2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Exploration of Pharmacophore in Chrysosplenol C as Activator in Ventricular Myocyte Contraction.
AID1452480Positive inotropic activity in Sprague-Dawley rat heart assessed as left ventricular posterior wall thickness end diastole at 4 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 0.88 to 1.54 mm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452503Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as dPdT min at 8 ug/kg/min (Rvb = -5462 to -4611 mmHg/s)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1402188Positive inotropic activity in Sprague-Dawley rat heart assessed as increase in ejection fraction at 2 to 16 ug/kg/min infused for 3 mins by echocardiographic analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Design and synthesis of sulfonamidophenylethylureas as novel cardiac myosin activator.
AID605331Volume of distribution in Sprague-Dawley rat2010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
AID1498825Activation of actin-stimulated bovine cardiac myosin S1 fragment ATPase activity in sarcomere after 10 mins by spectrophotometric analysis2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Exploration of diphenylalkyloxadiazoles as novel cardiac myosin activator.
AID1452485Positive inotropic activity in Sprague-Dawley rat heart assessed as ejection fraction at 16 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 67.16 to 85.81%)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452462Activation of actin-stimulated bovine cardiac myosin S1 fragment ATPase activity in sarcomere at 10 uM after 10 mins by spectrophotometric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1577033Positive ionotropic activity in Sprague-Dawley rat assessed as increase in ejection fraction at 16 ug/kg/min, iv for 3 mins by echocardiography relative to control2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design and synthesis of sulfonamidophenylethylamides as novel cardiac myosin activator.
AID1242380Positive inotropic effect in Sprague-Dawley rat ventricular myocytes assessed as change in ventricular cell contractility at 1 uM by video edge detector relative to control2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Exploration of Pharmacophore in Chrysosplenol C as Activator in Ventricular Myocyte Contraction.
AID1452464Positive inotropic activity in Sprague-Dawley rat heart assessed as left ventricle fractional shortening at 2 to 16 ug/kg/min for 3 mins by echocardiographic analysis2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452493Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as end-diastolic pressure at 8 ug/kg/min (Rvb = 7.68 to 9.83 mmHg)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1577034Positive ionotropic activity in Sprague-Dawley rat assessed as increase in fractional shortening at 16 ug/kg/min, iv for 3 mins by echocardiography relative to control2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design and synthesis of sulfonamidophenylethylamides as novel cardiac myosin activator.
AID1452476Positive inotropic activity in Sprague-Dawley rat heart assessed as left ventricular internal diameter end diastole at 16 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 5.66 to 7.80 mm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452521Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as heart rate at 4 ug/kg/min (Rvb = 260 to 322 bpm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID605329Clearance in Sprague-Dawley rat2010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
AID1452465Positive inotropic activity in Sprague-Dawley rat heart assessed as ejection fraction at 2 to 16 ug/kg/min for 3 mins by echocardiographic analysis2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID605328Inhibition of vasodilation in Sprague-Dawley rat aortic ring2010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
AID1452520Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as heart rate at 2 ug/kg/min (Rvb = 322 bpm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452461Positive inotropic activity in Sprague-Dawley rat heart assessed as fractional shortening at 4 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 38.60 to 55.81%)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452508Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as heart rate at 8 ug/kg/min (Rvb = 260 to 322 bpm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452513Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as end-systolic pressure at 4 ug/kg/min (Rvb = 94.65 to 97.85 mmHg)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452516Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as dPdT max at 2 ug/kg/min (Rvb = 5214 mmHg/s)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1577038Activation of chicken gizzard muscle actin and tropomyosin-stimulated myosin S1 ATPase activity assessed as inorganic phosphate liberated at 100 uM incubated for 10 mins in presence of ATP by spectrophotometry relative to control2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design and synthesis of sulfonamidophenylethylamides as novel cardiac myosin activator.
AID605327Activation of Sprague-Dawley rat myosin in cardiomyocytes assessed as compound concentration resulting in 40% increase in ATPase activity at calcium concentrations that produced 25-50% of maximum calcium dependent activation2010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
AID1452472Positive inotropic activity in Sprague-Dawley rat heart assessed as left ventricular internal diameter end systole at 8 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 2.50 to 4.78 mm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452466Activation of actin-stimulated rabbit psoas skeletal muscle myosin S1 fragment ATPase activity at 100 uM after 10 mins by spectrophotometric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID605245Plasma protein binding in Sprague-Dawley rat2010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
AID1452460Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as end-systolic pressure at 2 ug/kg/min (Rvb = 97.85 mmHg)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452484Positive inotropic activity in Sprague-Dawley rat heart assessed as ejection fraction at 8 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 67.16 to 85.81%)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452515Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as end-diastolic pressure at 4 ug/kg/min (Rvb = 7.68 to 9.83 mmHg)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1402187Positive inotropic activity in Sprague-Dawley rat heart assessed as increase in left ventricle fractional shortening at 2 to 16 ug/kg/min infused for 3 mins by echocardiographic analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Design and synthesis of sulfonamidophenylethylureas as novel cardiac myosin activator.
AID1452509Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as heart rate at 16 ug/kg/min (Rvb = 274 to 322 bpm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452517Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as dPdT max at 4 ug/kg/min (Rvb = 4985 to 5214 mmHg/s)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452479Positive inotropic activity in Sprague-Dawley rat heart assessed as left ventricular posterior wall thickness end systole at 16 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 2.07 to 2.46 mm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452471Positive inotropic activity in Sprague-Dawley rat heart assessed as left ventricular internal diameter end systole at 4 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 2.50 to 4.78 mm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1498827Activation of actin-stimulated chicken gizzard smooth muscle myosin S1 fragment ATPase activity at 100 uM after 10 mins by spectrophotometric analysis relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Exploration of diphenylalkyloxadiazoles as novel cardiac myosin activator.
AID1452470Positive inotropic activity in Sprague-Dawley rat heart assessed as heart rate at 16 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 281 to 347 bpm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1577037Activation of myosin ATPase activity in Sprague-Dawley rat ventricular myocytes assessed as increase in ventricular cell shortening by measuring change in ventricular cell contractility at 1 uM by electrophysiology relative to control2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design and synthesis of sulfonamidophenylethylamides as novel cardiac myosin activator.
AID1498826Activation of actin-stimulated rabbit psoas skeletal muscle myosin S1 fragment ATPase activity at 100 uM after 10 mins by spectrophotometric analysis relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Exploration of diphenylalkyloxadiazoles as novel cardiac myosin activator.
AID1452475Positive inotropic activity in Sprague-Dawley rat heart assessed as left ventricular internal diameter end diastole at 8 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 5.66 to 7.80 mm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452499Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as dPdT max at 16 ug/kg/min (Rvb = 4162 to 5214 mmHg/s)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452481Positive inotropic activity in Sprague-Dawley rat heart assessed as left ventricular posterior wall thickness end diastole at 8 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 0.88 to 1.54 mm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452473Positive inotropic activity in Sprague-Dawley rat heart assessed as left ventricular internal diameter end systole at 16 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 2.50 to 4.78 mm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1498824Activation of actin-stimulated bovine cardiac myosin S1 fragment ATPase activity in sarcomere at 1 uM after 10 mins by spectrophotometric analysis relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Exploration of diphenylalkyloxadiazoles as novel cardiac myosin activator.
AID1402185Activation of actin-stimulated rabbit skeletal muscle myosin S1 fragment ATPase activity at 100 uM after 10 mins by spectrophotometric analysis relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Design and synthesis of sulfonamidophenylethylureas as novel cardiac myosin activator.
AID605330Clearance in Beagle dog heart failure model2010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
AID1402186Activation of actin-stimulated chicken gizzard smooth muscle myosin S1 fragment ATPase activity at 100 uM after 10 mins by spectrophotometric analysis relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Design and synthesis of sulfonamidophenylethylureas as novel cardiac myosin activator.
AID1452482Positive inotropic activity in Sprague-Dawley rat heart assessed as left ventricular posterior wall thickness end diastole at 16 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 0.88 to 1.54 mm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1242381Activation of cardiac myosin S1 ATPase in bovine sarcomere at 10 uM by spectrophometric analysis in presence of actin thin filament complex relative to control2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Exploration of Pharmacophore in Chrysosplenol C as Activator in Ventricular Myocyte Contraction.
AID1452478Positive inotropic activity in Sprague-Dawley rat heart assessed as left ventricular posterior wall thickness end systole at 8 ug/kg/min for 3 mins by echocardiographic analysis (Rvb = 2.07 to 2.46 mm)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452467Activation of actin-stimulated chicken gizzard smooth muscle myosin S1 fragment ATPase activity at 100 uM after 10 mins by spectrophotometric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
AID1452518Effect on hemodynamic parameters in Sprague-Dawley rat heart assessed as dPdT min at 2 ug/kg/min (Rvb = -5462 mmHg/s)2017European journal of medicinal chemistry, Jul-07, Volume: 134Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (150)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (1.33)29.6817
2010's69 (46.00)24.3611
2020's79 (52.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.06

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 Index53.06 (24.57)
Research Supply Index5.18 (2.92)
Research Growth Index6.00 (4.65)
Search Engine Demand Index82.74 (26.88)
Search Engine Supply Index1.99 (0.95)

This Compound (53.06)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials24 (15.79%)5.53%
Reviews26 (17.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other102 (67.11%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]