Compounds > bay-68-4986
Page last updated: 2024-11-12

bay-68-4986

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

Cross-References

ID SourceID
PubMed CID9936489
CHEMBL ID3235279
SCHEMBL ID174016
MeSH IDM0578456

Synonyms (41)

Synonym
o519nvw73r ,
bay-68-4986
544417-40-5
capadenoson
capadenoson [inn]
unii-o519nvw73r
HY-14917
CS-1228
capadenoson [who-dd]
bay 68-4986
2-amino-6-(((2-(4-chlorophenyl)-1,3-thiazol-4-yl)methyl)sulfanyl)-4-(4-(2-hydroxyethoxy)phenyl)pyridine-3,5-dicarbonitrile
2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}sulphanyl)-4-[4-(2-hydroxyethoxy)phenyl]-3,5-pyridinedicarbonitrile
CITWCLNVRIKQAF-UHFFFAOYSA-N
2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxy-ethoxy)phenyl]pyridine-3,5-dicarbonitrile
2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}sulphanyl)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile
2-amino-6-({(2-(4-chlorophenyl)-1,3-thiazol-4-yl)methyl}sulfanyl)-4-(4-(2-hydroxyethoxy)phenyl)pyridine-3,5-dicarbonitrile
2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile
CHEMBL3235279 ,
bay-684986
SCHEMBL174016
bdbm50003646
AC-35269
2-amino-6-(((2-(4-chlorophenyl)thiazol-4-yl)methyl)thio)-4-(4-(2-hydroxyethoxy)phenyl)pyridine-3,5-dicarbonitrile
J-690318
capadenoson;bay 68-4986
EX-A848
2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}sulfanyl)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile
gtpl11221
bay684986
AKOS030632784
FT-0700327
BCP16060
2-amino-6-[[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methylsulfanyl]-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile
mfcd09954113
AS-35054
DTXSID50969597
Q27285331
2-amino-6-[[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methylsulfanyl]-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitril
bay 68-4986bay 68-4986
BC176871
A913734

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" antiarrhythmic agents that act as ventricular rate control agents, a selective response can be accomplished by careful dosing paradigms."( A1 adenosine receptor agonists and their potential therapeutic applications.
Elzein, E; Zablocki, J, 2008)		0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Adenosine receptor A1Homo sapiens (human)Ki0.00140.00020.931610.0000AID1244369
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Adenosine receptor A1Homo sapiens (human)EC50 (µMol)0.00060.00010.99169.8000AID1126019; AID1244377
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (51)

Processvia Protein(s)Taxonomy
temperature homeostasisAdenosine receptor A1Homo sapiens (human)
response to hypoxiaAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
regulation of respiratory gaseous exchange by nervous system processAdenosine receptor A1Homo sapiens (human)
negative regulation of acute inflammatory responseAdenosine receptor A1Homo sapiens (human)
negative regulation of leukocyte migrationAdenosine receptor A1Homo sapiens (human)
positive regulation of peptide secretionAdenosine receptor A1Homo sapiens (human)
positive regulation of systemic arterial blood pressureAdenosine receptor A1Homo sapiens (human)
negative regulation of systemic arterial blood pressureAdenosine receptor A1Homo sapiens (human)
regulation of glomerular filtrationAdenosine receptor A1Homo sapiens (human)
protein targeting to membraneAdenosine receptor A1Homo sapiens (human)
phagocytosisAdenosine receptor A1Homo sapiens (human)
inflammatory responseAdenosine receptor A1Homo sapiens (human)
signal transductionAdenosine receptor A1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
cell-cell signalingAdenosine receptor A1Homo sapiens (human)
nervous system developmentAdenosine receptor A1Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A1Homo sapiens (human)
response to inorganic substanceAdenosine receptor A1Homo sapiens (human)
negative regulation of glutamate secretionAdenosine receptor A1Homo sapiens (human)
response to purine-containing compoundAdenosine receptor A1Homo sapiens (human)
lipid catabolic processAdenosine receptor A1Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicAdenosine receptor A1Homo sapiens (human)
positive regulation of nucleoside transportAdenosine receptor A1Homo sapiens (human)
negative regulation of neurotrophin productionAdenosine receptor A1Homo sapiens (human)
positive regulation of protein dephosphorylationAdenosine receptor A1Homo sapiens (human)
vasodilationAdenosine receptor A1Homo sapiens (human)
negative regulation of circadian sleep/wake cycle, non-REM sleepAdenosine receptor A1Homo sapiens (human)
negative regulation of apoptotic processAdenosine receptor A1Homo sapiens (human)
positive regulation of potassium ion transportAdenosine receptor A1Homo sapiens (human)
positive regulation of MAPK cascadeAdenosine receptor A1Homo sapiens (human)
negative regulation of hormone secretionAdenosine receptor A1Homo sapiens (human)
cognitionAdenosine receptor A1Homo sapiens (human)
leukocyte migrationAdenosine receptor A1Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painAdenosine receptor A1Homo sapiens (human)
negative regulation of lipid catabolic processAdenosine receptor A1Homo sapiens (human)
positive regulation of lipid catabolic processAdenosine receptor A1Homo sapiens (human)
regulation of sensory perception of painAdenosine receptor A1Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergicAdenosine receptor A1Homo sapiens (human)
fatty acid homeostasisAdenosine receptor A1Homo sapiens (human)
excitatory postsynaptic potentialAdenosine receptor A1Homo sapiens (human)
long-term synaptic depressionAdenosine receptor A1Homo sapiens (human)
mucus secretionAdenosine receptor A1Homo sapiens (human)
negative regulation of mucus secretionAdenosine receptor A1Homo sapiens (human)
triglyceride homeostasisAdenosine receptor A1Homo sapiens (human)
regulation of cardiac muscle cell contractionAdenosine receptor A1Homo sapiens (human)
apoptotic signaling pathwayAdenosine receptor A1Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationAdenosine receptor A1Homo sapiens (human)
negative regulation of long-term synaptic potentiationAdenosine receptor A1Homo sapiens (human)
negative regulation of long-term synaptic depressionAdenosine receptor A1Homo sapiens (human)
G protein-coupled receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
G protein-coupled receptor bindingAdenosine receptor A1Homo sapiens (human)
purine nucleoside bindingAdenosine receptor A1Homo sapiens (human)
protein bindingAdenosine receptor A1Homo sapiens (human)
heat shock protein bindingAdenosine receptor A1Homo sapiens (human)
G-protein beta/gamma-subunit complex bindingAdenosine receptor A1Homo sapiens (human)
heterotrimeric G-protein bindingAdenosine receptor A1Homo sapiens (human)
protein heterodimerization activityAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
plasma membraneAdenosine receptor A1Homo sapiens (human)
plasma membraneAdenosine receptor A1Homo sapiens (human)
basolateral plasma membraneAdenosine receptor A1Homo sapiens (human)
axolemmaAdenosine receptor A1Homo sapiens (human)
asymmetric synapseAdenosine receptor A1Homo sapiens (human)
presynaptic membraneAdenosine receptor A1Homo sapiens (human)
neuronal cell bodyAdenosine receptor A1Homo sapiens (human)
terminal boutonAdenosine receptor A1Homo sapiens (human)
dendritic spineAdenosine receptor A1Homo sapiens (human)
calyx of HeldAdenosine receptor A1Homo sapiens (human)
postsynaptic membraneAdenosine receptor A1Homo sapiens (human)
presynaptic active zoneAdenosine receptor A1Homo sapiens (human)
synapseAdenosine receptor A1Homo sapiens (human)
dendriteAdenosine receptor A1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID1244380Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes at 1 uM by competition association assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
AID1244374Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cell membranes at 1 uM by competition association assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
AID1244379Selectivity for human adenosine A1 receptor expressed in CHO cell membranes over human adenosine A3 receptor expressed in CHO cell membrane2015European journal of medicinal chemistry, Aug-28, Volume: 101Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
AID1126027Ratio for displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes at 10 times Ki after 15 mins by dual-point competition association assay to ratio for displacement of [3H]DPCPX from human adenosine A1 receptor expressed2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Agonists for the adenosine A1 receptor with tunable residence time. A Case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines.
AID1244376Displacement of [3H]PSB11 from human adenosine A3 receptor expressed in CHO cell membranes at 1 uM by competition association assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
AID1244378Agonist activity at human adenosine A1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay relative to 100 uM CPA2015European journal of medicinal chemistry, Aug-28, Volume: 101Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
AID1244373Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes assessed as residence time by competition association assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
AID1126019Agonist activity at adenosine A1 receptor (unknown origin) expressed in CHO cells assessed as increase in intracellular cAMP level by RIA2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Agonists for the adenosine A1 receptor with tunable residence time. A Case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines.
AID1244372Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes assessed as dissociation rate constant by competition association assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
AID1244369Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes by competition association assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
AID1244370Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes assessed as kinetic rate index by measuring ratio of binding at earlier and later time points by competition association assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
AID1244377Agonist activity at human adenosine A1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
AID1244371Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes assessed as association rate constant by competition association assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
AID1244375Displacement of [3H]PSB603 from human adenosine A2B receptor expressed in CHO cell membranes at 1 uM by competition association assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (14.29)29.6817
2010's5 (71.43)24.3611
2020's1 (14.29)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 13.13

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

MetricThis Compound (vs All)
Research Demand Index13.13 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index5.33 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (13.13)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (14.29%)5.53%
Reviews2 (28.57%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (57.14%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		2.2510mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
thiazoles
[no description available]		6.35611,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
alpha-aminopyridine
alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.		6.3561
adenosine
quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit		3.6920adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
2-chloro-n(6)cyclopentyladenosine
2-chloro-N(6)cyclopentyladenosine: highly selective agonist at A1 adenosine receptors		2.2510
tecadenoson
tecadenoson: an A1 adenosine receptor agonist		3.2510
ConditionIndicatedRelationship StrengthStudiesTrials
Cardiac Remodeling, Ventricular
[description not available]		02.0810
Cardiac Failure
[description not available]		03.4320
Heart Failure
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.		03.4320
Kidney Failure
A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.		03.0610
Angor Pectoris
[description not available]		03.8720
Arteriosclerosis, Coronary
[description not available]		03.0610
Insulin Sensitivity
[description not available]		03.0610
Angina Pectoris
The symptom of paroxysmal pain consequent to MYOCARDIAL ISCHEMIA usually of distinctive character, location and radiation. It is thought to be provoked by a transient stressful situation during which the oxygen requirements of the MYOCARDIUM exceed that supplied by the CORONARY CIRCULATION.		03.8720
Coronary Artery Disease
Pathological processes of CORONARY ARTERIES that may derive from a congenital abnormality, atherosclerotic, or non-atherosclerotic cause.		03.0610
Diabetes Mellitus
A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.		03.0610
Insulin Resistance
Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.		03.0610
Tachycardia, Supraventricular
A generic expression for any tachycardia that originates above the BUNDLE OF HIS.		03.0610
Renal Insufficiency
Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.		03.0610
Ache
[description not available]		02.9610
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		02.9610
Angina Pectoris, Stable
[description not available]		03.4611
Angina, Stable
Persistent and reproducible chest discomfort usually precipitated by a physical exertion that dissipates upon cessation of such an activity. The symptoms are manifestations of MYOCARDIAL ISCHEMIA.		15.4611