Compounds > ck-2017357
Page last updated: 2024-11-13

ck-2017357

Description

CK-2017357: a fast-skeletal-troponin activator; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23729157
CHEMBL ID3039529
SCHEMBL ID976988
MeSH IDM0574411

Synonyms (46)

Synonym
tirasemtiv
ck-2017357
bdbm50316148
D10327
tirasemtiv (usan/inn)
CHEMBL3039529
2h-imidazo(4,5-b)pyrazin-2-one, 1-(1-ethylpropyl)-6-ethynyl-1,3-dihydro-
6-ethynyl-1-(pentan-3-yl)-2h-imidazo(4,5-b)pyrazin-2-one
1005491-05-3
1-(1-ethylpropyl)-6-ethynyl-1,3-dihydro-2h-imidazo(4,5-b)pyrazin-2-one
unii-g8wsm7r635
tirasemtiv [usan:inn]
ck2017357
g8wsm7r635 ,
ck 2017357
tirasemtiv [who-dd]
tirasemtiv [inn]
tirasemtiv [usan]
RSQGZEAXODVTOL-UHFFFAOYSA-N
6-ethynyl-1-(pentan-3-yl)-1h-imidazo[4,5-b]pyrazin-2-ol
HY-15964
SCHEMBL976988
tirasemtiv(ck-2017357)
5-ethynyl-3-pentan-3-yl-1h-imidazo[4,5-b]pyrazin-2-one
tirasemtiv (ck-2017357)
gtpl8280
DTXSID90143379
EX-A367
AKOS027250724
mfcd28023588
NCGC00378555-02
2h-imidazo[4,5-b]pyrazin-2-one, 1-(1-ethylpropyl)-6-ethynyl-1,3-dihydro-;2h-imidazo[4,5-b]pyrazin-2-one, 1-(1-ethylpropyl)-6-ethynyl-1,3-dihydro-
DB12209
FT-0746303
6-ethynyl-1-(pentan-3-yl)-1,3-dihydro-2h-imidazo[4,5-b]pyrazin-2-one
Q27088998
BCP27991
ck2017357; ck-2017357; ck 2017357
S0196
SB16955
1-(1-ethylpropyl)-6-ethynyl-1,3-dihydro-2h-imidazo[4,5-b]pyrazin-2-one
W97 ,
A898831
6-ethynyl-1-(pentan-3-yl)-1h-imidazo[4,5-b]pyrazin-2(3h)-one
AC-35962
BS-22417

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" CK-2017357 was well tolerated, with dizziness and general fatigue being the most frequent adverse events."( Safety, tolerability and pharmacodynamics of a skeletal muscle activator in amyotrophic lateral sclerosis.
Cedarbaum, JM; Chen, M; Cudkowicz, ME; Hansen, RL; Jones, D; Lee, J; Mahoney, K; Malik, F; Mao, J; Maragakis, N; Russell, AJ; Saikali, K; Shefner, J; Watson, ML; Wolff, AA, 2012)		1.29
" Results showed that tirasemtiv was well tolerated, with dizziness the most common adverse event."( A study to evaluate safety and tolerability of repeated doses of tirasemtiv in patients with amyotrophic lateral sclerosis.
Meng, L; Shefner, JM; Watson, ML; Wolff, AA, 2013)		0.39
" Both doses of tirasemtiv were well tolerated; there were no premature terminations or serious adverse events."( A Double-Blinded, Randomized, Placebo-Controlled Trial to Evaluate Efficacy, Safety, and Tolerability of Single Doses of Tirasemtiv in Patients with Acetylcholine Receptor-Binding Antibody-Positive Myasthenia Gravis.
Dimachkie, MM; Malik, FI; Meng, L; Rosenfeld, J; Sanders, DB, 2015)		0.42
" Dropouts and serious adverse events occurred more frequently in the tirasemtiv group."( A randomized, placebo-controlled, double-blind phase IIb trial evaluating the safety and efficacy of tirasemtiv in patients with amyotrophic lateral sclerosis.
Andrews, JA; Barragan, D; Bian, A; Lee, J; Meng, L; Shefner, JM; Wolff, AA, )		0.13

Pharmacokinetics

ExcerptReferenceRelevance
"This study was designed to evaluate the safety and tolerability of single doses of CK-2017357, an orally bioavailable fast skeletal muscle troponin activator, in patients with amyotrophic lateral sclerosis (ALS), and to explore pharmacodynamic markers related to strength, endurance, and function."( Safety, tolerability and pharmacodynamics of a skeletal muscle activator in amyotrophic lateral sclerosis.
Cedarbaum, JM; Chen, M; Cudkowicz, ME; Hansen, RL; Jones, D; Lee, J; Mahoney, K; Malik, F; Mao, J; Maragakis, N; Russell, AJ; Saikali, K; Shefner, J; Watson, ML; Wolff, AA, 2012)		0.6

Bioavailability

ExcerptReferenceRelevance
"This study was designed to evaluate the safety and tolerability of single doses of CK-2017357, an orally bioavailable fast skeletal muscle troponin activator, in patients with amyotrophic lateral sclerosis (ALS), and to explore pharmacodynamic markers related to strength, endurance, and function."( Safety, tolerability and pharmacodynamics of a skeletal muscle activator in amyotrophic lateral sclerosis.
Cedarbaum, JM; Chen, M; Cudkowicz, ME; Hansen, RL; Jones, D; Lee, J; Mahoney, K; Malik, F; Mao, J; Maragakis, N; Russell, AJ; Saikali, K; Shefner, J; Watson, ML; Wolff, AA, 2012)		0.6
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51

Dosage Studied

ExcerptRelevanceReference
" Sixty-three patients completed all three dosing periods."( Safety, tolerability and pharmacodynamics of a skeletal muscle activator in amyotrophic lateral sclerosis.
Cedarbaum, JM; Chen, M; Cudkowicz, ME; Hansen, RL; Jones, D; Lee, J; Mahoney, K; Malik, F; Mao, J; Maragakis, N; Russell, AJ; Saikali, K; Shefner, J; Watson, ML; Wolff, AA, 2012)		0.38
" Participants tolerating 2 weeks of open-label tirasemtiv (125 mg twice daily) were randomized 3:2:2:2 to placebo or one of three target tirasemtiv dose levels, using an escalating dosage protocol lasting 28 days."( A phase III trial of
Andrews, JA; Cockcroft, BM; Cudkowicz, ME; Hardiman, O; Lee, JH; Malik, FI; Meng, L; Rudnicki, SA; Shefner, JM; Wolff, AA, 2019)		0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency5.35470.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency8.48660.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency26.83700.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency8.48660.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency8.48660.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency8.48660.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency8.48660.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

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)
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 (18)

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)
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 (22)

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)
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 (34)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
AID1785408Drug distribution in Sprague-Dawley rat Soleus muscle to blood ratio at 100 mg/kg, po by HPLC analysis2021Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function.
AID1354435Ratio of IC50 for CYP1A2 in human liver microsomes to IC50 for CYP1A2 in human liver microsomes preincubated for 20 mins with compound2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1785411Efflux ratio of apparent permeability in human Caco-2 cells2021Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function.
AID1354431Oral bioavailability in mouse at 1 mg/kg by HPLC method2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354417Extraction ratio in human liver microsomes measured up to 90 mins by HPLC/MS/MS analysis2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354418Clearance in Sprague-Dawley rat at 1 mg/kg, po or 1 mg/kg iv via bolus by HPLC method2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354419Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, po or 1 mg/kg iv via bolus by HPLC method2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1785406Plasma protein binding in male rat assessed as unbound fraction2021Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function.
AID1354433Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate in presence of NADP2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354427Clearance in mouse at 1 mg/kg, po or 1 mg/kg iv via bolus by HPLC method2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354412Activation of troponin in rabbit fast skeletal muscle fibers assessed as increase in calcium stimulated activity by measuring compound concentration that produces 40% increase in myofibril ATPase activity at 25% of calcium concentration needed for maximal2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354432Apparent permeability of the compound in human Caco2 cells2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354429Volume of distribution at steady state in mouse at 1 mg/kg, po or 1 mg/kg iv via bolus by HPLC method2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354434Time dependent inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate preincubated for 20 mins followed by NADP addition2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354421Fraction unbound in rat plasma at 5 uM after 6 hrs by equilibrium dialysis based HPLC method2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354420Oral bioavailability in Sprague-Dawley rat at 1 mg/kg by HPLC method2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1785407Drug distribution in Sprague-Dawley rat brain to blood ratio at 100 mg/kg, po by HPLC analysis2021Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function.
AID1354416Extraction ratio in rat liver microsomes measured up to 90 mins by HPLC/MS/MS analysis2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354425Extraction ratio in mouse liver microsomes measured up to 90 mins by HPLC/MS/MS analysis2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354422Fraction unbound in human plasma at 5 uM after 6 hrs by equilibrium dialysis based HPLC method2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354428Volume of distribution at steady state in Beagle dog at 1 mg/kg, po or 1 mg/kg iv via bolus by HPLC method2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354415Activation of troponin in rabbit fast skeletal muscle fibers assessed as increase in calcium stimulated activity by measuring compound concentration that produces 30% increase in tension at 25% of calcium concentration needed for maximal response by pyruv2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354423Increase in muscle force in rat extensor digitorum longus muscle dosed systemically measured every two mins by in situ live fiber activity assay2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354430Oral bioavailability in Beagle dog at 1 mg/kg by HPLC method2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1785405Increase in muscle tension in rat extensor digitorum longus muscle rat model assessed as free plasma concentration to increase muscle tension at subtetanic nerve stimulation rate of 30 Hz2021Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function.
AID1354424Extraction ratio in dog liver microsomes measured up to 90 mins by HPLC/MS/MS analysis2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1354426Clearance in Beagle dog at 1 mg/kg, po or 1 mg/kg iv via bolus by HPLC method2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of
AID1785410Drug distribution in Sprague-Dawley rat plasma to blood ratio at 100 mg/kg, po by HPLC analysis2021Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function.
AID1785409Drug distribution in Sprague-Dawley rat extensor digitorum longus to blood ratio at 100 mg/kg, po by HPLC analysis2021Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (22)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's16 (72.73)24.3611
2020's6 (27.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.30

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 Index16.30 (24.57)
Research Supply Index3.47 (2.92)
Research Growth Index4.58 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.30)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (34.78%)5.53%
Reviews2 (8.70%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (56.52%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
antipyrine
Antipyrine: An analgesic and antipyretic that has been given by mouth and as ear drops. Antipyrine is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29). antipyrine : A pyrazolone derivative that is 1,2-dihydropyrazol-3-one substituted with methyl groups at N-1 and C-5 and with a phenyl group at N-2.		2.1510pyrazoloneantipyretic;
cyclooxygenase 3 inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
caffeine
[no description available]		2.3110purine alkaloid;
trimethylxanthine		adenosine A2A receptor antagonist;
adenosine receptor antagonist;
adjuvant;
central nervous system stimulant;
diuretic;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
environmental contaminant;
food additive;
fungal metabolite;
geroprotector;
human blood serum metabolite;
mouse metabolite;
mutagen;
plant metabolite;
psychotropic drug;
ryanodine receptor agonist;
xenobiotic
edaravone
[no description available]		2.1510pyrazoloneantioxidant;
radical scavenger
riluzole
Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.		4.8121benzothiazoles
tecnazene
tetrachloronitrobenzene: sprout suppressant for potatoes; can be either the 1,2,4,5- and/or the 1,2,3,5-tetrachloro isomer; RN given refers to cpd with unspecified isomeric designation. tecnazene : A C-nitro compound that is nitrobenzene in which the four hydrogens located ortho- and para- to the nitro group have been replaced by chlorines. A fungicide used to control dry rot, it is no longer approved for use within the European Union.		2.2110aromatic fungicide;
C-nitro compound;
tetrachlorobenzene		antifungal agrochemical
thiazoles
[no description available]		2.15101,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
pyrazines
Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.		11.34188diazine;
pyrazines		Daphnia magna metabolite
olesoxime
olesoxime: drug candidate for amyotrophic lateral sclerosis; structure in first source		3.2710
masitinib
[no description available]		2.15101,3-thiazoles;
benzamides;
N-alkylpiperazine;
pyridines		antineoplastic agent;
antirheumatic drug;
tyrosine kinase inhibitor
oligonucleotides
[no description available]		3.2710
piperidines
Piperidines: A family of hexahydropyridines.		2.1510
nusinersen
nusinersen: an antisense oligonucleotide that induces SMN protein expression		3.2710
ConditionIndicatedRelationship StrengthStudiesTrials
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.0540
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		02.8530
Adult Onset Nemaline Myopathy
[description not available]		02.6620
Myopathies, Nemaline
A group of inherited congenital myopathic conditions characterized clinically by weakness, hypotonia, and prominent hypoplasia of proximal muscles including the face. Muscle biopsy reveals large numbers of rod-shaped structures beneath the muscle fiber plasma membrane. This disorder is genetically heterogeneous and may occasionally present in adults. (Adams et al., Principles of Neurology, 6th ed, p1453)		02.6620
Disease Exacerbation
[description not available]		04.8821
ALS - Amyotrophic Lateral Sclerosis
[description not available]		010.47118
Amyotrophic Lateral Sclerosis
A degenerative disorder affecting upper MOTOR NEURONS in the brain and lower motor neurons in the brain stem and SPINAL CORD. Disease onset is usually after the age of 50 and the process is usually fatal within 3 to 6 years. Clinical manifestations include progressive weakness, atrophy, FASCICULATION, hyperreflexia, DYSARTHRIA, dysphagia, and eventual paralysis of respiratory function. Pathologic features include the replacement of motor neurons with fibrous ASTROCYTES and atrophy of anterior SPINAL NERVE ROOTS and corticospinal tracts. (From Adams et al., Principles of Neurology, 6th ed, pp1089-94)		112.47118
HMN (Hereditary Motor Neuropathy) Proximal Type I
[description not available]		03.0910
Spinal Muscular Atrophies of Childhood
A group of recessive inherited diseases that feature progressive muscular atrophy and hypotonia. They are classified as type I (Werdnig-Hoffman disease), type II (intermediate form), and type III (Kugelberg-Welander disease). Type I is fatal in infancy, type II has a late infantile onset and is associated with survival into the second or third decade. Type III has its onset in childhood, and is slowly progressive. (J Med Genet 1996 Apr:33(4):281-3)		03.0910
Muscular Dystrophy
[description not available]		02.0810
Muscular Dystrophies
A heterogeneous group of inherited MYOPATHIES, characterized by wasting and weakness of the SKELETAL MUSCLE. They are categorized by the sites of MUSCLE WEAKNESS; AGE OF ONSET; and INHERITANCE PATTERNS.		02.0810
Anti-MuSK Myasthenia Gravis
[description not available]		03.8821
Myasthenia Gravis
A disorder of neuromuscular transmission characterized by fatigable weakness of cranial and skeletal muscles with elevated titers of ACETYLCHOLINE RECEPTORS or muscle-specific receptor tyrosine kinase (MuSK) autoantibodies. Clinical manifestations may include ocular muscle weakness (fluctuating, asymmetric, external ophthalmoplegia; diplopia; ptosis; and weakness of eye closure) and extraocular fatigable weakness of facial, bulbar, respiratory, and proximal limb muscles. The disease may remain limited to the ocular muscles (ocular myasthenia). THYMOMA is commonly associated with this condition.		15.8821
Amyotonia Congenita
[description not available]		02.0710
Neuromuscular Diseases
A general term encompassing lower MOTOR NEURON DISEASE; PERIPHERAL NERVOUS SYSTEM DISEASES; and certain MUSCULAR DISEASES. Manifestations include MUSCLE WEAKNESS; FASCICULATION; muscle ATROPHY; SPASM; MYOKYMIA; MUSCLE HYPERTONIA, myalgias, and MUSCLE HYPOTONIA.		02.0710
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