Page last updated: 2024-10-24

signaling receptor ligand precursor processing

Definition

Target type: biologicalprocess

The cleavage of a peptide bond in a precursor form of a signaling receptor ligand, resulting in the mature (active) form of the ligand. [PMID:29247995]

Signaling receptor ligand precursor processing is a complex biological process that involves the synthesis, modification, and activation of signaling molecules, known as ligands, which bind to specific receptors on target cells. The process can be divided into several key steps:

1. Gene Transcription and Translation: The process begins with the transcription of the gene encoding the ligand precursor protein. This DNA sequence is copied into messenger RNA (mRNA), which is then translated into a polypeptide chain. The polypeptide chain is the primary structure of the protein and is often called a pre-proprotein.

2. Signal Peptide Cleavage: The pre-proprotein typically contains a signal peptide, a short amino acid sequence that directs the protein to the endoplasmic reticulum (ER). The signal peptide is cleaved off by a signal peptidase enzyme during or shortly after translocation into the ER lumen. This cleavage generates the proprotein, which now lacks the signal peptide and is ready for further processing.

3. Protein Folding and Glycosylation: Within the ER lumen, the proprotein undergoes folding into its correct three-dimensional structure, guided by chaperone proteins. This folding process is crucial for the protein's activity and stability. Additionally, many ligand precursors are glycosylated, meaning that sugar molecules are added to specific amino acid residues. Glycosylation can influence protein folding, stability, and biological activity.

4. Transport to Golgi Apparatus: Following folding and glycosylation, the proprotein is transported from the ER to the Golgi apparatus, a series of membrane-bound compartments that further process and sort proteins.

5. Post-translational Modifications: Within the Golgi, the proprotein undergoes further post-translational modifications, which may include additional glycosylation, phosphorylation, sulfation, or proteolytic cleavage. These modifications contribute to the final maturation and activation of the ligand.

6. Packaging and Sorting: As the ligand precursor progresses through the Golgi, it is packaged into vesicles for transport to its final destination. Depending on the specific ligand and its target cell, this destination may be the cell surface, secretory granules, or lysosomes.

7. Ligand Activation: The final activation step for the ligand often occurs after its release from the cell. This activation can involve proteolytic cleavage, phosphorylation, or other modifications that expose the binding site for the receptor.

8. Receptor Binding and Signal Transduction: Once activated, the ligand binds to its specific receptor on the target cell, initiating a cascade of events that ultimately alter cellular function. This signaling pathway can lead to a variety of responses, including changes in gene expression, cell growth, differentiation, or even cell death.

The processing of signaling receptor ligand precursors is a highly regulated and complex process, ensuring that the correct ligand is produced, activated, and delivered to its target cell at the appropriate time. Dysregulation of this process can contribute to a variety of diseases.'
"

Proteins (2)

ProteinDefinitionTaxonomy
Beta-secretase 1A beta-secretase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P56817]Homo sapiens (human)
Caspase-1A caspase-1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P29466]Homo sapiens (human)

Compounds (158)

CompoundDefinitionClassesRoles
coumarin2H-chromen-2-one: coumarin derivativecoumarinsfluorescent dye;
human metabolite;
plant metabolite
phloroglucinolphloroglucinol : A benzenetriol with hydroxy groups at position 1, 3 and 5.

Phloroglucinol: A trinitrobenzene derivative with antispasmodic properties that is used primarily as a laboratory reagent.
benzenetriol;
phenolic donor
algal metabolite
p-chloromercuribenzoic acidp-Chloromercuribenzoic Acid: An organic mercurial used as a sulfhydryl reagent.chlorine molecular entity;
mercuribenzoic acid
5,8,11,14-eicosatetraynoic acid5,8,11,14-Eicosatetraynoic Acid: A 20-carbon unsaturated fatty acid containing 4 alkyne bonds. It inhibits the enzymatic conversion of arachidonic acid to prostaglandins E(2) and F(2a).long-chain fatty acid
5-methoxypsoralen5-methoxypsoralen : A 5-methoxyfurocoumarin that is psoralen substituted by a methoxy group at position 5.

5-Methoxypsoralen: A linear furanocoumarin that has phototoxic and anti-inflammatory properties, with effects similar to METHOXSALEN. It is used in PUVA THERAPY for the treatment of PSORIASIS.
5-methoxyfurocoumarin;
organic heterotricyclic compound;
psoralens
hepatoprotective agent;
plant metabolite
chloroquinechloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.

Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.
aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound
anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
disulfiramorganic disulfide;
organosulfur acaricide
angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor;
EC 3.1.1.1 (carboxylesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
ferroptosis inducer;
fungicide;
NF-kappaB inhibitor
donepezil2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group.

donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.

Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.
aromatic ether;
indanones;
piperidines;
racemate
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
nootropic agent
ebselenebselen : A benzoselenazole that is 1,2-benzoselenazol-3-one carrying an additional phenyl substituent at position 2. Acts as a mimic of glutathione peroxidase.benzoselenazoleanti-inflammatory drug;
antibacterial agent;
anticoronaviral agent;
antifungal agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
EC 1.3.1.8 [acyl-CoA dehydrogenase (NADP(+))] inhibitor;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
EC 3.1.3.25 (inositol-phosphate phosphatase) inhibitor;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
EC 3.5.4.1 (cytosine deaminase) inhibitor;
EC 5.1.3.2 (UDP-glucose 4-epimerase) inhibitor;
enzyme mimic;
ferroptosis inhibitor;
genotoxin;
hepatoprotective agent;
neuroprotective agent;
radical scavenger
4-biphenylylacetic acidbiphenyl-4-ylacetic acid : A monocarboxylic acid in which one of the alpha-hydrogens is substituted by a biphenyl-4-yl group. An active metabolite of fenbufen, it is used as a topical medicine to treat muscle inflammation and arthritis.biphenyls;
monocarboxylic acid
non-steroidal anti-inflammatory drug
fenbufenfenbufen: structure; RN given refers to parent cpd4-oxo monocarboxylic acid;
biphenyls
non-steroidal anti-inflammatory drug
gossypolGossypol: A dimeric sesquiterpene found in cottonseed (GOSSYPIUM). The (-) isomer is active as a male contraceptive (CONTRACEPTIVE AGENTS, MALE) whereas toxic symptoms are associated with the (+) isomer.
p-hydroxyamphetaminep-Hydroxyamphetamine: Amphetamine metabolite with sympathomimetic effects. It is sometimes called alpha-methyltyramine, which may also refer to the meta isomer, gepefrine.amphetamines
ibuprofenMidol: combination of cinnamedrine, phenacetin, aspirin & caffeinemonocarboxylic acidantipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
radical scavenger;
xenobiotic
indomethacinindometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.

Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.
aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole
analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic;
xenobiotic metabolite
indoprofenindoprofen : A monocarboxylic acid that is propionic acid in which one of the hydrogens at position 2 is substituted by a 4-(1-oxo-1,3-dihydroisoindol-2-yl)phenyl group. Initially used as an anti-inflammatory and analgesic, it was withdrawn from the market due to causing severe gastrointestinal bleeding. It has been subsequently found to increase production of the survival motor neuron protein.

Indoprofen: A drug that has analgesic and anti-inflammatory properties. Following reports of adverse reactions including reports of carcinogenicity in animal studies it was withdrawn from the market worldwide. (From Martindale, The Extra Pharmacopoeia, 30th ed, p21)
gamma-lactam;
isoindoles;
monocarboxylic acid
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
ketoprofenketoprofen : An oxo monocarboxylic acid that consists of propionic acid substituted by a 3-benzoylphenyl group at position 2.

Ketoprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis.
benzophenones;
oxo monocarboxylic acid
antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
ketorolac5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid : A member of the class of pyrrolizines that is 2,3-dihydro-1H-pyrrolizine which is substituted at positions 1 and 5 by carboxy and benzoyl groups, respectively.

ketorolac : A racemate comprising equimolar amounts of (R)-(+)- and (S)-(-)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid. While only the (S)-(-) enantiomer is a COX1 and COX2 inhibitor, the (R)-(+) enantiomer exhibits potent analgesic activity. A non-steroidal anti-inflammatory drug, ketorolac is mainly used (generally as the tromethamine salt) for its potent analgesic properties in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis. It was withdrawn from the market in many countries in 1993 following association with haemorrhage and renal failure.

Ketorolac: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed)
amino acid;
aromatic ketone;
monocarboxylic acid;
pyrrolizines;
racemate
analgesic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
beta-lapachonebeta-lapachone : A benzochromenone that is 3,4-dihydro-2H-benzo[h]chromene-5,6-dione substituted by geminal methyl groups at position 2. Isolated from Tabebuia avellanedae, it exhibits antineoplastic and anti-inflammatory activities.

beta-lapachone: antineoplastic inhibitor of reverse transcriptase, DNA topoisomerase, and DNA polymerase
benzochromenone;
orthoquinones
anti-inflammatory agent;
antineoplastic agent;
plant metabolite
methoxsalenmethoxsalen : A member of the class of psoralens that is 7H-furo[3,2-g]chromen-7-one in which the 9 position is substituted by a methoxy group. It is a constituent of the fruits of Ammi majus. Like other psoralens, trioxsalen causes photosensitization of the skin. It is administered topically or orally in conjunction with UV-A for phototherapy treatment of vitiligo and severe psoriasis.

Methoxsalen: A naturally occurring furocoumarin compound found in several species of plants, including Psoralea corylifolia. It is a photoactive substance that forms DNA ADDUCTS in the presence of ultraviolet A irradiation.
aromatic ether;
psoralens
antineoplastic agent;
cross-linking reagent;
dermatologic drug;
photosensitizing agent;
plant metabolite
masoprocolnordihydroguaretic acid: antioxidant compound found in the creosote bush (Larrea tridentata)catechols;
lignan;
tetrol
antioxidant;
ferroptosis inhibitor;
geroprotector;
plant metabolite
quinone1,4-benzoquinone : The simplest member of the class of 1,4-benzoquinones, obtained by the formal oxidation of hydroquinone to the corresponding diketone. It is a metabolite of benzene.

benzoquinone : The simplest members of the class of benzoquinones, consisting of cyclohexadiene which is substituted by two oxo groups.

quinone : Compounds having a fully conjugated cyclic dione structure, such as that of benzoquinones, derived from aromatic compounds by conversion of an even number of -CH= groups into -C(=O)- groups with any necessary rearrangement of double bonds (polycyclic and heterocyclic analogues are included).
1,4-benzoquinonescofactor;
human xenobiotic metabolite;
mouse metabolite
sulfasalazinesulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position.

Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907)
tiaprofenic acidtiaprofenic acid : An aromatic ketone that is thiophene substituted at C-2 by benzoyl and at C-4 by a 1-carboxyethyl group.

tiaprofenic acid: RN given refers to parent cpd; structure
aromatic ketone;
monocarboxylic acid;
thiophenes
drug allergen;
non-steroidal anti-inflammatory drug
triamterenetriamterene : Pteridine substituted at positions 2, 4 and 7 with amino groups and at position 6 with a phenyl group. A sodium channel blocker, it is used as a diuretic in the treatment of hypertension and oedema.

Triamterene: A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.
pteridinesdiuretic;
sodium channel blocker
tyraminemonoamine molecular messenger;
primary amino compound;
tyramines
EC 3.1.1.8 (cholinesterase) inhibitor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
neurotransmitter
ficusinFicusin: A naturally occurring furocoumarin, found in PSORALEA. After photoactivation with UV radiation, it binds DNA via single and double-stranded cross-linking.

psoralen : The simplest member of the class of psoralens that is 7H-furo[3,2-g]chromene having a keto group at position 7. It has been found in plants like Psoralea corylifolia and Ficus salicifolia.
psoralensplant metabolite
scoparonescoparone : A member of the class of coumarins that is esculetin in which the two hydroxy groups at positions 6 and 7 are replaced by methoxy groups. It is a major constituent of the Chinese herbal medicine Yin Chen Hao, and exhibits a variety of pharmacological activities such as anti-inflammatory, anti-allergic, and anti-tumor activities.

scoparone: structure
aromatic ether;
coumarins
anti-allergic agent;
anti-inflammatory agent;
antihypertensive agent;
antilipemic drug;
immunosuppressive agent;
plant metabolite
catechin(+)-catechin : The (+)-enantiomer of catechin and a polyphenolic antioxidant plant metabolite.

catechin : Members of the class of hydroxyflavan that have a flavan-3-ol skeleton and its substituted derivatives.

Catechin: An antioxidant flavonoid, occurring especially in woody plants as both (+)-catechin and (-)-epicatechin (cis) forms.

rac-catechin : A racemate comprising equimolar amounts of (+)- and (-)-catechin
catechinantioxidant;
plant metabolite
rheindihydroxyanthraquinone
9-(2,3-dihydroxy-3-methylbutoxy)-4-methoxy-7h-furo(3,2-g)(1)benzopyran-7-one9-(2,3-dihydroxy-3-methylbutoxy)-4-methoxy-7H-furo(3,2-g)(1)benzopyran-7-one: isolated from Angelica dahurica (Umbelliferae); structure in first sourcepsoralens
imperatorinimperatorin : A member of the class of psoralens that is psoralen substituted by a prenyloxy group at position 8. Isolated from Angelica dahurica and Angelica koreana, it acts as a acetylcholinesterase inhibitor.

imperatorin: tumor necrosis factor antagonist; furanocoumarin from West African medicinal plant Clausena anisata; structure in Negwer, 5th ed, #3005
psoralensEC 3.1.1.7 (acetylcholinesterase) inhibitor;
metabolite
ostholosthol: from Cnidium monnieri and Angelica pubescens (both Apiaceae); structure given in first sourcebotanical anti-fungal agent;
coumarins
metabolite
ninhydrinninhydrin : A member of the class of indanones that is indane-1,3-dione bearing two additional hydroxy substituents at position 2.

Ninhydrin: 2,2-Dihydroxy-1H-indene-1,3-(2H)-dione. Reagent toxic to skin and mucus membranes. It is used in chemical assay for peptide bonds, i.e., protein determinations and has radiosensitizing properties.
aromatic ketone;
beta-diketone;
indanones;
ketone hydrate
colour indicator;
human metabolite
thymoquinonethymoquinone : A member of the class of 1,4-benzoquinones that is 1,4-bezoquinone in which the hydrogens at positions 2 and 5 are replaced by methyl and isopropyl groups, respectively. It is a natural compound isolated from Nigella sativa which has demonstrated promising chemotherapeutic activity.

thymoquinone: constituent of cedarwood; can cause dermatitis; structure
1,4-benzoquinonesadjuvant;
anti-inflammatory agent;
antidepressant;
antineoplastic agent;
antioxidant;
cardioprotective agent;
plant metabolite
angelicinangelicin: used as tranquillizer; sedative; or anticonvulsant; structurefuranocoumarin
herniarinherniarin : A member of the class of coumarins that is coumarin substituted by a methoxy group at position 7.

herniarin: methoxy analog of umbelliferone; structure
coumarinsfluorochrome
1,2-Dihydroquinolin-2-imineaminoquinoline
n-methylisatinN-methylisatin: structure given in first source
aviprinaviprin: isolated from Angelica dahurica; structure in first sourcefuranocoumarinmetabolite
oxypeucadanin, (s)-(-)-isomerepoxide;
furanocoumarin;
lactone
plant metabolite
epigallocatechin gallate(-)-epigallocatechin 3-gallate : A gallate ester obtained by the formal condensation of gallic acid with the (3R)-hydroxy group of (-)-epigallocatechin.

epigallocatechin gallate: a steroid 5alpha-reductase inhibitor and antimutagen in green tea (Camellia sinensis)
flavans;
gallate ester;
polyphenol
antineoplastic agent;
antioxidant;
apoptosis inducer;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent;
plant metabolite
gallocatechol(+)-gallocatechin : A gallocatechin that has (2R,3S)-configuration. It is found in green tea and bananas.

gallocatechin : A catechin that is a flavan substituted by hydroxy groups at positions 3, 3', 4', 5, 5' and 7 (the trans isomer). It is isolated from Acacia mearnsii.

gallocatechol: structure give in first source; RN given for (trans-(+-))-omer; inhibits DNA-dependent DNA & RNA polymerases
gallocatechinantioxidant;
metabolite;
radical scavenger
xanthotoxol8-hydroxyfurocoumarin : A furanocoumarin which bears a hydroxy group at position 8.8-hydroxyfurocoumarin
xanthyletinexanthyletine: structurecoumarins
1,2,3,4,6-pentakis-O-galloyl-beta-D-glucose1,2,3,4,6-pentakis-O-galloyl-beta-D-glucose : A galloyl-beta-D-glucose compound having five galloyl groups in the 1-, 2-, 3-, 4- and 6-positions.

pentagalloylglucose: pentahydroxy gallic acid ester of glucose; a phytogenic antineoplastic agent and antibacterial agent
gallate ester;
galloyl beta-D-glucose
anti-inflammatory agent;
antineoplastic agent;
geroprotector;
hepatoprotective agent;
plant metabolite;
radiation protective agent;
radical scavenger
toxoflavintoxoflavin : A pyrimidotriazine that is 1,6-dimethyl-1,5,6,7-tetrahydropyrimido[5,4-e][1,2,4]triazine with oxo groups at positions 5 and 7.

toxoflavin: azapteridine antibiotic; structure
carbonyl compound;
pyrimidotriazine
antibacterial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
toxin;
virulence factor;
Wnt signalling inhibitor
isopimpinellinisopimpinellin: from Ruta graveolens & Heracleum lanatum; structurepsoralens
isoimperatorinisoimperatorin : A member of the class of psoralens that is psoralen substituted by a prenyloxy group at position 5. Isolated from Angelica dahurica and Angelica koreana, it acts as a acetylcholinesterase inhibitor.

isoimperatorin: tumor necrosis factor antagonist isolated from Glehniae root
psoralensEC 3.1.1.7 (acetylcholinesterase) inhibitor;
metabolite
seselinseselin: structure in first sourcecoumarinsmetabolite
suberosinsuberosin : A member of the class of coumarins in which the coumarin ring is substituted at positions 6 and 7 by a 3-methylbut-2-en-1-yl group and a methoxy group, respectively. A natural product found in Citropsis articulata.

suberosin: has anti-inflammatory activity
aromatic ether;
coumarins
anticoagulant;
plant metabolite
vexibinolsophoraflavanone G : A tetrahydroxyflavanone having a structure of naringenin bearing an additional hydroxyl substituent at position 2' as well as a (2R)-5-methyl-2-(prop-1-en-2-yl)hex-4-en-1-yl (lavandulyl) substituent at position 8'.

vexibinol: flavanol from Sophora; structure in first source; RN given refers to (S-(R*,S*))-isomer
(2S)-flavan-4-one;
4'-hydroxyflavanones;
tetrahydroxyflavanone
antimalarial;
antimicrobial agent;
antioxidant;
plant metabolite
(-)-catechin(-)-catechin : The (-)-enantiomer of catechin.catechinmetabolite
heraclenolheraclenol: isolated from the herb Huanghuaren
1-aminoisoquinoline
rivastigminecarbamate ester;
tertiary amino compound
cholinergic drug;
EC 3.1.1.8 (cholinesterase) inhibitor;
neuroprotective agent
columbianetin, (s)-isomer(S)-columbianetin : The (S)-(+)-enantiomer of columbianetin.columbianetin
phellopterinphellopterin: a naturally occurring furanocoumarin found in roots of Angelica dahurica; structure in first sourcepsoralens
parthenolidegermacranolide
gefitinibaromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound
antineoplastic agent;
epidermal growth factor receptor antagonist
n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine3-iodobenzyl-5'-N-methylcarboxamidoadenosine : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by N-ethylcarboxamido and one of the hydrogens of the exocyclic amino function is substituted by a 3-iodobenzyl group.

N(6)-(3-iodobenzyl)-5'-N-methylcarboxamidoadenosine: structure given in first source; a selective A(3) adenosine receptor agonist
adenosines;
monocarboxylic acid amide;
organoiodine compound
adenosine A3 receptor agonist
phlorofucofuroeckol aphlorofucofuroeckol A: phlorotannin from Ecklonia kurome; structure given in first source
isoteolinisoteolin: mixture of isomers isoboldine (RN 3019-51-0) & bracteoline (RN 25651-04-1)aporphine alkaloid
eckoleckol : A phlorotannin that is oxanthrene-1,3,6,8-tetrol substituted by a 3,5-dihydroxyphenoxy moiety at position 4. Isolated from the marine brown alga, Ecklonia cava, it exhibits antioxidant activity.

eckol: structure given in first source; isolated from brown alga Ecklonia kurome Okamura; inhibitor of alpha 2-antiplasmin
phlorotanninantioxidant;
metabolite
pralnacasanpralnacasan: NSAID, ICE inhibitor & metastasis inhibitor; RN & structure in first source
naproxennaproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes.

Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.
methoxynaphthalene;
monocarboxylic acid
antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
gout suppressant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
(+)-epicatechin(+)-epicatechin : A catechin that is flavan carrying five hydroxy substituents at positions 3, 3', 4', 5 and 7 (the 2S,3S-stereoisomer).catechin;
polyphenol
cyclooxygenase 1 inhibitor;
plant metabolite
a-130a
marmesinmarmesin: RN given refers to (S)-isomer; nodakenetin is the (R)-isomermarmesin
latifolinlatifolin: structure in first source
nsc 663284NSC 663284: structure in first sourcequinolone
decursindecursin: activates protein kinase C; isolated from the root of Angelica gigas; RN given for (S)-isomer; structure in first sourcecoumarins
decursinoldecursinol : An organic heterotricyclic compound that is 7,8-dihydro-2H,6H-pyrano[3,2-g]chromen-2-one substituted by a beta-hydroxy group at position 7 and two methyl groups at position 8. It is isolated from the roots of Angelica gigas and has been found to possess significant inhibitory activity against acetylcholinesterase enzyme (EC 3.1.1.7).cyclic ether;
delta-lactone;
organic heterotricyclic compound;
secondary alcohol
analgesic;
antineoplastic agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
metabolite
eugeniineugeniin : An ellagitannin isolated from the dried flower buds of Eugenia caryophyllata. It exhibits alpha-glucosidase inhibitory activity and antiviral activity against acyclovir and phosphonoacetic acid (PAA)-resistant herpes simplex virus type 1 (HSV-1) as well as the wild-type HSV-1.

eugeniin: structure in first source
beta-D-glucoside;
ellagitannin;
gallate ester;
lactone
anti-HSV-1 agent;
antifungal agent;
antineoplastic agent;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
metabolite
docosahexaenoateall-cis-docosa-4,7,10,13,16,19-hexaenoic acid : A docosahexaenoic acid having six cis-double bonds at positions 4, 7, 10, 13, 16 and 19.

docosahexaenoate : A polyunsaturated fatty acid anion that is the conjugate base of docosahexaenoic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.

docosahexaenoic acid : Any C22 polyunsaturated fatty acid containing six double bonds.

efalex: a mixture of fish oil and primrose oil; used as a high-docosahexaenoic acid fatty acid supplement
docosahexaenoic acid;
omega-3 fatty acid
algal metabolite;
antineoplastic agent;
Daphnia tenebrosa metabolite;
human metabolite;
mouse metabolite;
nutraceutical
om99-2OM99-2: eight-residue memapsin 2 inhibitor; structure in first source
om00-3OM00-3: second-generation 8-residue memapsin 2 inhibitor; structure in first source
heracleninheraclenin: from Chlamydomonas reinhardii; structure given in first source; RN given refers to (R)-isomer
isoxanthohumolisoxanthohumol: structure in first sourceflavanones
lomatinlomatin: isolated from Lomatium nutalli and various Umbelliferae; structure in first sourcecoumarins
2,2'-dihydroxychalcone2,2'-dihydroxychalcone: an antineoplastic agent; structure in first source
isoliquiritigeninchalconesantineoplastic agent;
biological pigment;
EC 1.14.18.1 (tyrosinase) inhibitor;
GABA modulator;
geroprotector;
metabolite;
NMDA receptor antagonist
cannabidiolcannabidiol : An cannabinoid that is cyclohexene which is substituted by a methyl group at position 1, a 2,6-dihydroxy-4-pentylphenyl group at position 3, and a prop-1-en-2-yl group at position 4.

Cannabidiol: Compound isolated from Cannabis sativa extract.
olefinic compound;
phytocannabinoid;
resorcinols
antimicrobial agent;
plant metabolite
acetyl-aspartyl-glutamyl-valyl-aspartalAc-Asp-Glu-Val-Asp-H : A tetrapeptide consisting of two L-aspartic acid residues, an L-glutamyl residue and an L-valine residue with an acetyl group at the N-terminal and with the C-terminal carboxy group reduced to an aldehyde. It is an inhibitor of caspase-3/7.

acetyl-aspartyl-glutamyl-valyl-aspartal: a capase inhibitor
tetrapeptideprotease inhibitor
cnidilincnidilin: from roots of Angelica pubescens Maxim. f. biserrata Shan et Yuan; structure in first sourcepsoralens
curcumincurcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.

Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.
aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol
anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger
auraptenaurapten: RN refers to (E)-isomer; structure given in first source

auraptene : A member of the class of coumarins that is umbelliferone in which the phenolic hydrogen has been replaced by a geranyl group. Ii is isolated from several edible fruits and vegetables and exhibits a variety of therapeutic properties.
coumarins;
monoterpenoid
antihypertensive agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
dopaminergic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
gamma-secretase modulator;
gastrointestinal drug;
hepatoprotective agent;
matrix metalloproteinase inhibitor;
neuroprotective agent;
plant metabolite;
PPARalpha agonist;
vulnerary
dieckoldieckol : A phlorotannin isolated from a brown alga Ecklonia cava which exhibits antioxidant, hepatoprotective and anticoagulant activities.

dieckol: found in brown Eisenia and Ecklonia algae, have several pharmacologically beneficial effects such as anti-inflammation; structure in first source
aromatic ether;
oxacycle;
phlorotannin
anticoagulant;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
hepatoprotective agent;
metabolite;
radical scavenger
2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide2-chloro-N(6)-(3-iodobenzyl)adenosine-5'-N-methyluronamide: structure given in first source
byakangelicolbyakangelicol: RN given for (R)-isomer; structure in first sourcepsoralens
n-(6-chloropyridin-3-yl)-4-fluorobenzamideN-(6-chloropyridin-3-yl)-4-fluorobenzamide: structure in first source
5-Nitroisatinindolesanticoronaviral agent
ginkgetinginkgetin : A biflavonoid that is the 7,4'-dimethyl ether derivative of amentoflavone. Isolated from Ginkgo biloba and Dioon, it exhibits anti-HSV-1, antineoplastic and inhibitory activities towards arachidonate 5-lipoxygenase and cyclooxygenase 2.

ginkgetin: from Cephalotaxus drupacea; biflavone; active against HSV-1; structure given in first source
biflavonoid;
hydroxyflavone;
methoxyflavone;
ring assembly
anti-HSV-1 agent;
antineoplastic agent;
cyclooxygenase 2 inhibitor;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
metabolite
gallocatechin-3-gallate(+)-gallocatechin gallate : A gallate ester obtained by formal condensation of the carboxy group of gallic acid with the (3S)-hydroxy group of (+)-gallocatechin.

gallocatechin gallate: structure in first source
catechin;
gallate ester;
polyphenol
plant metabolite
quercetin7-hydroxyflavonol;
pentahydroxyflavone
antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
bergaptol5-hydroxyfurocoumarin : A furanocoumarin which bears a hydroxy group at position 5.5-hydroxyfurocoumarin;
psoralens
apigeninChamomile: Common name for several daisy-like plants (MATRICARIA; TRIPLEUROSPERMUM; ANTHEMIS; CHAMAEMELUM) native to Europe and Western Asia, now naturalized in the United States and Australia.trihydroxyflavoneantineoplastic agent;
metabolite
buteinchalcones;
polyphenol
antineoplastic agent;
antioxidant;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
geroprotector;
hypoglycemic agent;
plant metabolite;
radiosensitizing agent;
tyrosine kinase inhibitor
esculetinesculetin : A hydroxycoumarin that is umbelliferone in which the hydrogen at position 6 is substituted by a hydroxy group. It is used in filters for absorption of ultraviolet light.

esculetin: used in filters for absorption of ultraviolet light; structure
hydroxycoumarinantioxidant;
plant metabolite;
ultraviolet filter
7-hydroxycoumarin7-oxycoumarin: derivatives have anti-oxidant properties

umbelliferone : A hydroxycoumarin that is coumarin substituted by a hydroxy group ay position 7.
hydroxycoumarinfluorescent probe;
food component;
plant metabolite
amentoflavonebiflavonoid;
hydroxyflavone;
ring assembly
angiogenesis inhibitor;
antiviral agent;
cathepsin B inhibitor;
P450 inhibitor;
plant metabolite
cupressuflavonecupressuflavone : A biflavonoid that is obtained by oxidative coupling of two molecules of apigenin resulting in a bond between positions C-8 of the two chromene rings respectively. Isolated from Cupressus sempervirens and Juniperus occidentalis, it exhibits free radical scavenging and antielastase activities.

cupressuflavone: from Cupressus macrocarpa; structure in first source
biflavonoid;
hydroxyflavone;
ring assembly
EC 3.4.21.37 (leukocyte elastase) inhibitor;
metabolite;
radical scavenger
hinokiflavonehinokiflavone : A biflavonoid that is apigenin substituted by a 4-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)phenoxy group at position 6. A diflavonyl ether, it is isolated from Rhus succedanea and has been found to possess significant cytotoxic potential.

hinokiflavone: from Rhus succedanea; structure given in first source
aromatic ether;
biflavonoid;
hydroxyflavone
antineoplastic agent;
metabolite;
neuroprotective agent
morinmorin : A pentahydroxyflavone that is 7-hydroxyflavonol bearing three additional hydroxy substituents at positions 2' 4' and 5.

morin: a light yellowish pigment found in the wood of old fustic (Chlorophora tinctoria)
7-hydroxyflavonol;
pentahydroxyflavone
angiogenesis modulating agent;
anti-inflammatory agent;
antibacterial agent;
antihypertensive agent;
antineoplastic agent;
antioxidant;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
hepatoprotective agent;
metabolite;
neuroprotective agent
morusinmorusin : An extended flavonoid that is flavone substituted by hydroxy groups at positions 5, 2' and 4', a prenyl group at position 3 and a 2,2-dimethyl pyran group across positions 7 and 8.

morusin: from Morus root bark; structure given in first source
extended flavonoid;
trihydroxyflavone
antineoplastic agent;
plant metabolite
myricetin7-hydroxyflavonol;
hexahydroxyflavone
antineoplastic agent;
antioxidant;
cyclooxygenase 1 inhibitor;
food component;
geroprotector;
hypoglycemic agent;
plant metabolite
robustaflavonerobustaflavone : A biflavonoid that is obtained by oxidative coupling of two molecules of apigenin resulting in a bond between positions C-3 of the hydroxyphenyl ring and C-6 of the chromene ring. Isolated from Thuja orientalis and Rhus succedanea it exhibits antioxidant, cytotoxic and anti-hepatitis B activity.

robustaflavone: bis-apigenin coupled at 6 and 3' positions; a potential non-nucleoside anti-hepatitis B agent;
biflavonoid;
hydroxyflavone;
ring assembly
anti-HBV agent;
antineoplastic agent;
antioxidant;
metabolite
sciadopitysinsciadopitysin : A biflavonoid that is a 7, 4', 4'''-trimethyl ether derivative of amentoflavone.

sciadopitysin: biflavonoid from Taxus celebica & Ginkgo biloba
biflavonoid;
hydroxyflavone;
methoxyflavone;
ring assembly
bone density conservation agent;
platelet aggregation inhibitor
ellagic acidcatechols;
cyclic ketone;
lactone;
organic heterotetracyclic compound;
polyphenol
antioxidant;
EC 1.14.18.1 (tyrosinase) inhibitor;
EC 2.3.1.5 (arylamine N-acetyltransferase) inhibitor;
EC 2.4.1.1 (glycogen phosphorylase) inhibitor;
EC 2.5.1.18 (glutathione transferase) inhibitor;
EC 2.7.1.127 (inositol-trisphosphate 3-kinase) inhibitor;
EC 2.7.1.151 (inositol-polyphosphate multikinase) inhibitor;
EC 2.7.4.6 (nucleoside-diphosphate kinase) inhibitor;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
food additive;
fungal metabolite;
geroprotector;
plant metabolite;
skin lightening agent
n-acetyltyrosyl-valyl-alanyl-aspartyl aldehyde
irl 2500IRL 2500: Endothelin-B receptor antagonist; structure in first source
bilobetinbilobetin: a phospholipase A2 antagonistflavonoid oligomer
7-demethylsuberosin7-demethylsuberosin : A hydroxycoumarin that is 7-hydroxycoumarin which is substituted at position 6 by a 3-methylbut-2-en-1-yl group. A natural product found in Citropsis articulata.

7-demethylsuberosin: fucocoumarin derivative of Angelicae dahuricae
hydroxycoumarinplant metabolite
8-geranyloxypsoralenterpene lactone
isoginkgetinisoginkgetin : A biflavonoid resulting from the formal oxidative dimerisation between position 8 of one molecule of 5,7-dihydroxy-4'-methoxyflavone and the 3' position of another. Found in the leaves of Ginkgo biloba, it is a potent inhibitor of matrix metalloproteinase 9 (MMP-9).

isoginkgetin: Isolated from Ginkgo biloba; structure in first source
aromatic ether;
biflavonoid
antineoplastic agent;
EC 3.4.24.35 (gelatinase B) inhibitor;
plant metabolite
osthenolosthenol : A hydroxycoumarin that is umbelliferone in which the hydrogen at position 8 has been replaced by a prenyl group.

osthenol: structure in first source
hydroxycoumarinantifungal agent;
plant metabolite
podocarpusflavone apodocarpusflavone A: isolated from Podocarpus imbricatusflavonoid oligomer
grifolingrifolin: antibiotic isolated from Grifola confluenssesquiterpenoid
bergamottinbergamottin: constituent of bergamot oil; structure given in first sourcefuranocoumarinmetabolite
l 685458L 685458: a gamma-secretase inhibitor; structure in first source

L-685,458 : A peptide and carboxamide that is L-leucyl-L-phenylalaninamide, L-Leu-L-Phe-NH2, which has been acylated on the N-terminus by a Phe-Phe hydroxyethylene dipeptide isotere, 2R-benzyl-5S-tert-butoxycarbonylamino-4R-hydroxy-6-phenylhexanoic acid. Compounds based on the structure of L-685,458 are potent inhibitors of gamma-secretase, which mediates the final catalytic step that generates the amyloid beta-peptide (Abeta), which assembles into the neurotoxic aggregates in the brains of sufferers of Alzheimer's disease.
carbamate ester;
monocarboxylic acid amide;
peptide;
secondary alcohol
EC 3.4.23.46 (memapsin 2) inhibitor;
peptidomimetic
morusinolmorusinol: extracted from Morus alba inhibits arterial thrombosis and modulates platelet activation for the treatment of cardiovascular disease; structure in first sourceflavones
Norartocarpetinflavones
sequoiaflavonesequoiaflavone: Isolated from Ginkgo biloba; structure in first source
w-13
2,4,2'-trihydroxychalcone2,4,2'-trihydroxychalcone: structure in first source
4-hydroxylonchocarpin4-hydroxylonchocarpin: structure in first source
(-)-catechin-3-O-gallate(-)-catechin-3-O-gallate : A gallate ester obtained by formal condensation of the carboxy group of gallic acid with the (3R)-hydroxy group of (-)-catechin.flavans;
gallate ester;
polyphenol
metabolite
bvt.948
kmi-420KMI-420: a protease inhibitor; structure in first source
kmi-429KMI-429: a protease inhibitor; structure in first source
bis(7)-tacrinesecondary amino compoundapoptosis inhibitor;
EC 1.14.13.39 (nitric oxide synthase) inhibitor;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
neuroprotective agent
memoquinmemoquin: structure in first source
cnidicincnidicin: a coumarin from the root of Angelica koreana; structure in first source
2,4,2',4'-Tetrahydroxychalconechalcones
octyl caffeateoctyl caffeate: an antioxidant; structure in first source
sargahydroquinoic acidsargahydroquinoic acid: vasodilatator from the brown alga Sargassum macrocarpum; structure in first source
eckstolonoleckstolonol : A phlorotannin that is [1,4]benzodioxino[2,3-a]oxanthrene substituted by hydroxy groups at positions 1, 3, 6, 9 and 11. Isolated from the brown alga Ecklonia stolonifera, it exhibits radical scavenging activity.

eckstolonol: structure in first source
organic heteropentacyclic compound;
oxacycle;
phlorotannin
metabolite;
radical scavenger
sargachromenolsargachromenol: nerve growth factor-potentiating substance from Sargassum macrocarpum; structure in first source
7-phloroeckol7-phloroeckol : A phlorotannin that is eckol in which the hydroxy group at position 7 is replaced by a 2,4,6-trihydroxyphenoxy group. Isolated from the marine brown alga, Ecklonia cava, it exhibits antioxidant activity.

7-phloroeckol: isolated from Ecklonia cava; structure in first source
aromatic ether;
phlorotannin
antioxidant;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor;
metabolite
tasiamide btasiamide B: 4-amino-3-hydroxy-5-phenylpentanoic acid containing peptide from the marine cyanobacterium Symploca sp.; structure in first source
boeravinone eboeravinone E: from Boerhaavia diffusa L; structure in first source
sesone7-deazaxanthine: structure in first source
2'-methoxykurarinone(2S)-2'-methoxykurarinone : A dimethoxyflavanone that is (2S)-(-)-kurarinone in which the hydroxy group at position 2' is replaced by a methoxy group. Isolated from the roots of Sophora flavescens, it exhibits cytotoxicity against human myeloid leukemia HL-60 cells.

2'-methoxykurarinone: cytotoxic lavandulyl flavanone from Sophora flavescens; structure in first source
4'-hydroxyflavanones;
dihydroxyflavanone;
dimethoxyflavanone
antineoplastic agent;
metabolite
gsk188909GSK188909: a potent and selective non-peptidic BACE-1 inhibitor; structure in first source
6-(3,5-difluoroanilino)-9-ethyl-2-purinecarbonitrile6-aminopurines
6-(3,5-difluoroanilino)-9-(2,2-difluoroethyl)-2-purinecarbonitrile6-aminopurines
9-(3,5-difluorophenyl)-6-(ethylamino)-2-purinecarbonitrileimidazoles
ly2811376
grassystatin agrassystatin A: isolated from a cyanobacterium, identified as Lyngbya cf.; structure in first source
Kushenol Akushenol A: a tyrosinase inhibitor derived from Sophora flavescensflavanones
kurarinolkurarinol : A trihydroxyflavanone that is (2S)-flavanone substituted by hydroxy groups at positions 7, 2' and 4' , a methoxy group at position 5 and a (2S)-5-hydroxy-5-methyl-2-(prop-1-en-2-yl)hexyl group at position 8 respectively.

kurarinol: from Sophora flavescens; has inhibitory effect on tyrosinase and melanin synthesis; structure in first source
4'-hydroxyflavanones;
monomethoxyflavanone;
trihydroxyflavanone
anti-inflammatory agent;
antioxidant;
plant metabolite
leachianone aleachianone A : A trihydroxyflavanone that is (2S)-flavanone substituted by a lavandulyl group at position 8, hydroxy groups at positions 5, 7 and 4' and a methoxy group at position 2'. Isolated from the roots of Sophora flavescens and Sophora leachiana, it exhibits antineoplastic and antimalarial activity.

leachianone A: isolated from the Chinese herbal medicine Radix Sophorae; structure in first source
4'-hydroxyflavanones;
monomethoxyflavanone;
trihydroxyflavanone
antimalarial;
antineoplastic agent;
metabolite
azd3839AZD3839: a BACE1 inhibitor; structure in first source
ly2886721
ass234
6-o-palmitoylascorbic acidfatty acid ester
MK-8353MK-8353 : A member of the class of indazoles that is 1H-indazole substituted by a 6-(propan-2-yloxy)pyridin-3-yl group at position 3 and by a {[(3S)-3-(methylsulfanyl)-1-(2-{4-[4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl]-3,6-dihydropyridin-1(2H)-yl}-2-oxoethyl)pyrrolidin-3-yl]carbonyl}amino group at position 5. It is a potent and selective inhibitor of ERK1 and ERK2 in vitro (IC50 values of 23.0 nM and 8.8 nM, respectively). The drug is being developed by Merck Sharp & Dohme and is currently in clinical development for the treatment of advanced/metastatic solid tumors.

MK-8353: ERK inhibitor used in oncology
aromatic ether;
dihydropyridine;
indazoles;
methyl sulfide;
N-alkylpyrrolidine;
pyridines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide;
triazoles
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
rifampinRifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion
angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor