Compounds > FR900359
Page last updated: 2024-11-12

FR900359

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Description

FR900359: G-protein inhibitor from Ardisia crenata sims that shows inhibition of platelet aggregation and decrease of blood pressure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID14101198
CHEMBL ID4171381
CHEBI ID178012
SCHEMBL ID22133450

Synonyms (16)

Synonym
CHEBI:178012
fr900359
[(1r)-1-[(3s,6s,9s,12s,18r,21s,22r)-21-acetamido-18-benzyl-3-[(1r)-1-methoxyethyl]-4,9,10,12,16-pentamethyl-15-methylidene-2,5,8,11,14,17,20-heptaoxo-22-propan-2-yl-1,19-dioxa-4,7,10,13,16-pentazacyclodocos-6-yl]-2-methylpropyl] (2s,3r)-3-hydroxy-4-methyl
gtpl9336
fr-900359
SCHEMBL22133450
ubo-qic
107530-18-7
CHEMBL4171381 ,
bdbm50514449
n7m4365u6y ,
fr 900359
(r)-1-((3s,6s,9s,12s,18r,21s,22r)-21-acetamido-18-benzyl-22-isopropyl-3-((r)-1-methoxyethyl)-4,9,10,12,16-pentamethyl-15-methylene-2,5,8,11,14,17,20-heptaoxo-1,19-dioxa-4,7,10,13,16-pentaazacyclodocosan-6-yl)-2-methylpropyl (2s,3r)-3-hydroxy-4-methyl-2-pr
l-threonine, (3r)-n-acetyl-3-hydroxy-l-leucyl-(alphar)-alpha-hydroxybenzenepropanoyl-2,3-didehydro-n-methylalanyl-l-alanyl-n-methyl-l-alanyl-(3r)-3-[[(2s,3r)-3-hydroxy-4-methyl-1-oxo-2-[(1-oxopropyl)amino]pentyl]oxy]-l-leucyl-n,o-dimethyl-, (7-->1)-lacton
CS-0063541
HY-117037
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
cyclodepsipeptideA depsipeptide in which the amino and hydroxy carboxylic acid residues are connected in a ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Guanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)IC50 (µMol)0.03200.03200.10610.1549AID1749890
Guanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)IC50 (µMol)0.03200.03200.08300.1000AID1749890
Guanine nucleotide binding protein q polypeptideCricetulus griseus (Chinese hamster)IC50 (µMol)0.03300.03300.06400.0950AID1559771
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (27)

Processvia Protein(s)Taxonomy
skeletal system developmentGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
signal transductionGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
heart developmentGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
phototransduction, visible lightGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
regulation of blood pressureGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
entrainment of circadian clockGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
positive regulation of insulin secretionGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
regulation of melanocyte differentiationGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
developmental pigmentationGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
cellular response to pHGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
endothelin receptor signaling pathwayGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
cranial skeletal system developmentGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
ligand-gated ion channel signaling pathwayGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
action potentialGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
negative regulation of protein kinase activityGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
activation of phospholipase C activityGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
blood coagulationGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
phototransduction, visible lightGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
entrainment of circadian clockGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
regulation of platelet activationGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
protein stabilizationGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
regulation of canonical Wnt signaling pathwayGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
glutamate receptor signaling pathwayGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
action potentialGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
GTPase activityGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
G protein activityGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
protein bindingGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
GTP bindingGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
enzyme regulator activityGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
metal ion bindingGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
G-protein beta/gamma-subunit complex bindingGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
G protein-coupled receptor bindingGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
GTPase activityGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
GTPase activator activityGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
protein bindingGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
GTP bindingGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
metal ion bindingGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
G-protein beta/gamma-subunit complex bindingGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
G protein-coupled receptor bindingGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
photoreceptor outer segmentGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
cytoplasmGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
lysosomal membraneGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
plasma membraneGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
synapseGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
extracellular exosomeGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
heterotrimeric G-protein complexGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
cytoplasmGuanine nucleotide-binding protein subunit alpha-11Homo sapiens (human)
photoreceptor outer segmentGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
lysosomal membraneGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
Golgi apparatusGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
plasma membraneGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
nuclear membraneGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
synapseGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
extracellular exosomeGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
cytoplasmGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
heterotrimeric G-protein complexGuanine nucleotide-binding protein G(q) subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID1749890Inhibition of Galphaq/11 (unknown origin)
AID1779417Displacement of [3H]-PSB15900 from human platelet membrane Gq incubated for 90 mins by scintillation counter method2021Journal of natural products, 07-23, Volume: 84, Issue:7
Feature-Based Molecular Networking for the Targeted Identification of G
AID1355748Displacement of [3H]PSB-15900 from Gq (unknown origin) expressed in platelet cell membranes2018Journal of natural products, 07-27, Volume: 81, Issue:7
Applying Molecular Networking for the Detection of Natural Sources and Analogues of the Selective Gq Protein Inhibitor FR900359.
AID1559771Inhibition of Gq-mediated signalling in CHOK1 cells stably expressing M1 muscarinic receptor assessed as inhibition of carbachol-induced IP1 production by HTRF assay2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Heterotrimeric G Proteins as Therapeutic Targets in Drug Discovery.
AID1355747Inhibition of Gq (unknown origin) coupled with muscarinic M1 receptor expressed in CHO cells assessed as reduction in carbachol-induced IP1 accumulation pretreated for 1 hr followed by carbachol addition measured after 35 mins by HTRF assay2018Journal of natural products, 07-27, Volume: 81, Issue:7
Applying Molecular Networking for the Detection of Natural Sources and Analogues of the Selective Gq Protein Inhibitor FR900359.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (32)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's21 (65.63)24.3611
2020's11 (34.38)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.40

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 Index29.40 (24.57)
Research Supply Index3.56 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index36.71 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.40)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (8.82%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other31 (91.18%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
aspirin
Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity.		2.1110benzoic acids;
phenyl acetates;
salicylates		anticoagulant;
antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
EC 1.1.1.188 (prostaglandin-F synthase) inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
plant activator;
platelet aggregation inhibitor;
prostaglandin antagonist;
teratogenic agent
rolipram
[no description available]		2.1710pyrrolidin-2-onesantidepressant;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
adenosine diphosphate
Adenosine Diphosphate: Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.		2.1110adenosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate		fundamental metabolite;
human metabolite
vasotocin
Vasotocin: A nonapeptide that contains the ring of OXYTOCIN and the side chain of ARG-VASOPRESSIN with the latter determining the specific recognition of hormone receptors. Vasotocin is the non-mammalian vasopressin-like hormone or antidiuretic hormone regulating water and salt metabolism.. vasotocin : A heterodetic cyclic peptide that is homologous to oxytocin and vasopressin. It is a pituitary hormone that acts as an endocrine regulator for water balance, osmotic homoeostasis and is involved in social and sexual behavior in non-mammalian vertebrates.		2.1310
aminoquinuride
[no description available]		3.3510
gallein
gallein: do not confuse with gallin; structure. gallein : A xanthene dye that is fluoran carrying four hydroxy substituents at positions 3', 4', 5' and 6'.		3.35102-benzofurans;
gamma-lactone;
organic heteropentacyclic compound;
oxaspiro compound;
polyphenol;
xanthene dye		fluorochrome;
G-protein-coupled receptor antagonist;
histological dye
scymnol
scymnol: structure given in first source		2.311012alpha-hydroxy steroid;
24-hydroxy steroid;
26-hydroxy steroid;
27-hydroxy steroid;
3alpha-hydroxy steroid;
7alpha-hydroxy steroid
oxytocin
Oxytocin: A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.. oxytocin : A cyclic nonapeptide hormone with amino acid sequence CYIQNCPLG that also acts as a neurotransmitter in the brain; the principal uterine-contracting and milk-ejecting hormone of the posterior pituitary. Together with the neuropeptide vasopressin, it is believed to influence social cognition and behaviour.		2.1310heterodetic cyclic peptide;
peptide hormone		oxytocic;
vasodilator agent
ovalbumin
Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.		2.1510
thromboxane a2
Thromboxane A2: An unstable intermediate between the prostaglandin endoperoxides and thromboxane B2. The compound has a bicyclic oxaneoxetane structure. It is a potent inducer of platelet aggregation and causes vasoconstriction. It is the principal component of rabbit aorta contracting substance (RCS).. thromboxane A2 : A thromboxane which is produced by activated platelets and has prothrombotic properties: it stimulates activation of new platelets as well as increases platelet aggregation.		2.1510epoxy monocarboxylic acid;
thromboxanes A		mouse metabolite
atosiban
[no description available]		2.1310oligopeptide
ym-254890
YM-254890: structure in first source		5.1970
guanosine 5'-o-(3-thiotriphosphate)
Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.		2.2110nucleoside triphosphate analogue
ConditionIndicatedRelationship StrengthStudiesTrials
Asthma, Bronchial
[description not available]		03.5120
Cardiac Failure
[description not available]		03.1710
Benign Neoplasms
[description not available]		03.1710
Blood Clot
[description not available]		03.1710
Asthma
A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).		03.5120
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.		03.1710
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		03.1710
Thrombosis
Formation and development of a thrombus or blood clot in the blood vessel.		03.1710
Uveal Neoplasms
Tumors or cancer of the UVEA.		04.0540
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.1510
Experimental Lung Inflammation
Inflammation of any part, segment or lobe, of the lung parenchyma.		02.1510
Muscle Relaxation
That phase of a muscle twitch during which a muscle returns to a resting position.		02.1510
Pneumonia
Infection of the lung often accompanied by inflammation.		02.1510
Malignant Melanoma
[description not available]		03.9940
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		03.9940
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		02.1310
Genetic Predisposition
[description not available]		03.0610
Metastase
[description not available]		03.0610
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		03.0610