Compounds > 4-(((r)-1-(benzo(b)thiophene-3-carbonyl)-2-methyl-azetidine-2-carbonyl)-(3-chloro-benzyl)-amino)-butyric acid
Page last updated: 2024-11-13

4-(((r)-1-(benzo(b)thiophene-3-carbonyl)-2-methyl-azetidine-2-carbonyl)-(3-chloro-benzyl)-amino)-butyric acid

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

Description

4-(((R)-1-(benzo(b)thiophene-3-carbonyl)-2-methyl-azetidine-2-carbonyl)-(3-chloro-benzyl)-amino)-butyric acid: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID57520598
CHEMBL ID3353541
SCHEMBL ID11298599
MeSH IDM000602714

Synonyms (29)

Synonym
chembl3353541 ,
bdbm50032334
SCHEMBL11298599
4-[[(r)-1-(benzo[b]thiophene-3-carbonyl)-2-methyl-azetidine-2-carbonyl]-(3-chloro-benzyl)-amino]-butyric acid
MPMKMQHJHDHPBE-RUZDIDTESA-N ,
glpg0974
gtpl8417
compound 99 [pmid 25380412]
4-[[(2r)-1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]-[(3-chlorophenyl)methyl]amino]butanoic acid
glpg-0974
4-[[[(2r)-1-(benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]butanoic acid
glpg 0974
1391076-61-1
AKOS027470232
1391075-84-5
4-(((r)-1-(benzo(b)thiophene-3-carbonyl)-2-methyl-azetidine-2-carbonyl)-(3-chloro-benzyl)-amino)-butyric acid
X7REK61AIS ,
4-((((2r)-1-(benzo(b)thien-3-ylcarbonyl)-2-methyl-2-azetidinyl)carbonyl)((3-chlorophenyl)methyl)amino)butanoic acid
butanoic acid, 4-((((2r)-1-(benzo(b)thien-3-ylcarbonyl)-2-methyl-2-azetidinyl)carbonyl)((3-chlorophenyl)methyl)amino)-
HY-12940
CS-0012804
DB15406
EX-A2832
SB16999
unii-x7rek61ais
4-[[[(2r)-1-(benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]butanoicacid
MS-29019
(R)-4-(1-(BENZO[B]THIOPHENE-3-CARBONYL)-N-(3-CHLOROBENZYL)-2-METHYLAZETIDINE-2-CARBOXAMIDO)BUTANOIC ACID
AC-36690

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"The investigation of safety/tolerability and pharmacokinetics in the early development phase showed that GLPG0974 was safe and well tolerated up to a daily dose of 400 mg."( Safety, pharmacokinetics and pharmacodynamics of GLPG0974, a potent and selective FFA2 antagonist, in healthy male subjects.
Beetens, J; Galien, R; Namour, F; Van der Aa, A; Van Kaem, T; Van't Klooster, G; Vanhoutte, F, 2016)		0.43

Pharmacokinetics

ExcerptReferenceRelevance
" The compound has high solubility, high chemical, microsomal, and hepatocyte stability, and favorable pharmacokinetic properties and was confirmed to induce human neutrophil mobilization and to inhibit lipolysis in murine adipocytes."( Discovery of a Potent Thiazolidine Free Fatty Acid Receptor 2 Agonist with Favorable Pharmacokinetic Properties.
Bolognini, D; Ejsing, CS; Ekberg, JH; Hansen, AH; McKenzie, CJ; Milligan, G; Rexen Ulven, E; Sergeev, E; Sprenger, RR; Ulven, T, 2018)		0.48
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency32.99930.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency32.99930.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Free fatty acid receptor 2Homo sapiens (human)IC50 (µMol)0.00900.00900.40450.8000AID1170751
[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)
Free fatty acid receptor 2Homo sapiens (human)EC50 (µMol)0.01200.01200.01200.0120AID1363029
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (48)

Processvia Protein(s)Taxonomy
leukocyte chemotaxis involved in inflammatory responseFree fatty acid receptor 2Homo sapiens (human)
mucosal immune responseFree fatty acid receptor 2Homo sapiens (human)
regulation of acute inflammatory responseFree fatty acid receptor 2Homo sapiens (human)
positive regulation of cytokine production involved in immune responseFree fatty acid receptor 2Homo sapiens (human)
cell surface pattern recognition receptor signaling pathwayFree fatty acid receptor 2Homo sapiens (human)
positive regulation of acute inflammatory response to non-antigenic stimulusFree fatty acid receptor 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayFree fatty acid receptor 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayFree fatty acid receptor 2Homo sapiens (human)
lipid storageFree fatty acid receptor 2Homo sapiens (human)
positive regulation of insulin secretionFree fatty acid receptor 2Homo sapiens (human)
positive regulation of chemokine productionFree fatty acid receptor 2Homo sapiens (human)
positive regulation of interleukin-8 productionFree fatty acid receptor 2Homo sapiens (human)
glucose homeostasisFree fatty acid receptor 2Homo sapiens (human)
fat cell differentiationFree fatty acid receptor 2Homo sapiens (human)
negative regulation of insulin secretionFree fatty acid receptor 2Homo sapiens (human)
cellular response to fatty acidFree fatty acid receptor 2Homo sapiens (human)
regulation of peptide hormone secretionFree fatty acid receptor 2Homo sapiens (human)
ligand-gated ion channel signaling pathwayFree fatty acid receptor 2Homo sapiens (human)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityFree fatty acid receptor 2Homo sapiens (human)
protein bindingFree fatty acid receptor 2Homo sapiens (human)
lipid bindingFree fatty acid receptor 2Homo sapiens (human)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membraneFree fatty acid receptor 2Homo sapiens (human)
cell projectionFree fatty acid receptor 2Homo sapiens (human)
plasma membraneFree fatty acid receptor 2Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (38)

Assay IDTitleYearJournalArticle
AID1170779AUC (0 to 24 hrs) in Sprague-Dawley rat at 30 mg/kg, po by mass spectrometry2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170773Half life in Sprague-Dawley rat at 5 mg/kg, po2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170757Inhibition of FFA3 (unknown origin) up to 30 uM2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170780Cmax in Sprague-Dawley rat at 30 mg/kg, po by mass spectrometry2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1363029Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Discovery of a Potent Thiazolidine Free Fatty Acid Receptor 2 Agonist with Favorable Pharmacokinetic Properties.
AID1170768Initial plasma concentration in Sprague-Dawley rat at 1 mg/kg, iv2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170783Inhibition of fMLP-induced cell migration of human neutrophils after 1 hr by ATP luminescence based assay2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170774Oral bioavailability in Sprague-Dawley rat at 5 mg/kg2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170764Inhibition of human ERG at 10 uM2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170751Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170762Stability in human Hepatocytes assessed as parent compound remaining at 1 uM incubated for 90 mins by LC-MS/MS method2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170781Tmax in Sprague-Dawley rat at 30 mg/kg, po by mass spectrometry2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170753Stability in rat liver microsomes assessed as parent compound remaining at 3 uM incubated for 30 mins by LC-MS/MS method2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170760Stability in human liver microsomes assessed as parent compound remaining at 3 uM incubated for 30 mins by LC-MS/MS method2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170777Half life in Sprague-Dawley rat at 30 mg/kg, po2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170778Oral bioavailability in Sprague-Dawley rat at 30 mg/kg2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170754AUC (0 to 24 hrs) in Sprague-Dawley rat at 5 mg/kg, po by mass spectrometry2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170763Protein binding in human plasma2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170771Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170765Time dependent inhibition of CYP3A4 (unknown origin)2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170761Stability in rat liver microsomes assessed as parent compound remaining at 3 uM incubated for 90 mins by LC-MS/MS method2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170767Genotoxicity in Salmonella typhimurium by Ames-2 test2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170786Antagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometry2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170758Thermodynamic solubility of the compound at pH 3.02014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170776Tmax in Sprague-Dawley rat at 5 mg/kg, po by mass spectrometry2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170782Inhibition of sodium acetate-induced cell migration of human neutrophils after 1 hr by ATP luminescence based assay2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170759Thermodynamic solubility of the compound at pH 7.42014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170772AUC (0 to 24 hrs) in Sprague-Dawley rat at 1 mg/kg, iv2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170766Activation of PXR (unknown origin)2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170755Inhibition of CYP450 (unknown origin)2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170769Half life in Sprague-Dawley rat at 1 mg/kg, iv2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170784Inhibition of IL8-induced cell migration of human neutrophils after 1 hr by ATP luminescence based assay2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170770Clearance in Sprague-Dawley rat at 1 mg/kg, iv2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170785Inhibition of sodium acetate-induced cell migration of human neutrophils after 1 hr in presence of 90% plasma by ATP luminescence based assay2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1170775Cmax in Sprague-Dawley rat at 5 mg/kg, po by mass spectrometry2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1345904Human FFA2 receptor (Free fatty acid receptors)2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
AID1345904Human FFA2 receptor (Free fatty acid receptors)2016British journal of clinical pharmacology, 07, Volume: 82, Issue:1
Safety, pharmacokinetics and pharmacodynamics of GLPG0974, a potent and selective FFA2 antagonist, in healthy male subjects.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (62.50)24.3611
2020's3 (37.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.25

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 Index12.25 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.25)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (12.50%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
butyric acid
Butyric Acid: A four carbon acid, CH3CH2CH2COOH, with an unpleasant odor that occurs in butter and animal fat as the glycerol ester.. butyrate : A short-chain fatty acid anion that is the conjugate base of butyric acid, obtained by deprotonation of the carboxy group.. butyric acid : A straight-chain saturated fatty acid that is butane in which one of the terminal methyl groups has been oxidised to a carboxy group.		2.1310fatty acid 4:0;
straight-chain saturated fatty acid		human urinary metabolite;
Mycoplasma genitalium metabolite
propionic acid
propionic acid : A short-chain saturated fatty acid comprising ethane attached to the carbon of a carboxy group.		2.1710saturated fatty acid;
short-chain fatty acid		antifungal drug
xanthenes
Xanthenes: Compounds with three aromatic rings in linear arrangement with an OXYGEN in the center ring.		2.3110xanthene
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		4.861mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
enkephalin, d-penicillamine (2,5)-
Enkephalin, D-Penicillamine (2,5)-: A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.. DPDPE : A heterodetic cyclic peptide that is a cyclic enkephalin analogue, having D-penicillaminyl residues located at positions 2 and 5, which form the heterocycle via a disulfide bond.		2.3110heterodetic cyclic peptidedelta-opioid receptor agonist
naloxone
Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.		2.3110morphinane alkaloid;
organic heteropentacyclic compound;
tertiary alcohol		antidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist
enkephalin, ala(2)-mephe(4)-gly(5)-
Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.		2.3110
mocetinostat
mocetinostat: undergoing phase II clinical trials for treatment of cancer. mocetinostat : A benzamide obtained by formal condensation of the carboxy group of 4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzoic acid with one of the amino groups of benzene-1,2-diamine. It is an orally active and isotype-selective HDAC inhibitor which exhibits antitumour activity (IC50 = 0.15, 0.29, 1.66 and 0.59 muM for HDAC1, HDAC2, HDAC3 and HDAC11).		2.3110aminopyrimidine;
benzamides;
pyridines;
secondary amino compound;
secondary carboxamide;
substituted aniline		antineoplastic agent;
apoptosis inducer;
autophagy inducer;
cardioprotective agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
hepatotoxic agent
ConditionIndicatedRelationship StrengthStudiesTrials
Diseases of Immune System
[description not available]		02.110
Leukocyte Disorders
Disordered formation of various types of leukocytes or an abnormal accumulation or deficiency of these cells.		02.110
Immune System Diseases
Disorders caused by abnormal or absent immunologic mechanisms, whether humoral, cell-mediated, or both.		02.110
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.3110
Innate Inflammatory Response
[description not available]		02.6920
Colitis
Inflammation of the COLON section of the large intestine (INTESTINE, LARGE), usually with symptoms such as DIARRHEA (often with blood and mucus), ABDOMINAL PAIN, and FEVER.		02.3110
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.6920
Cancer of Cervix
[description not available]		02.2110
Uterine Cervical Neoplasms
Tumors or cancer of the UTERINE CERVIX.		02.2110