Page last updated: 2024-11-12

4-(4-(3-adamantan-1-ylureido)cyclohexyloxy)benzoic acid

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

Cross-References

ID SourceID
PubMed CID16038368
CHEMBL ID242459
CHEMBL ID244405
SCHEMBL ID653866
SCHEMBL ID653867
SCHEMBL ID14150188
SCHEMBL ID18465002
SCHEMBL ID18464995
SCHEMBL ID24617188
MeSH IDM0515379

Synonyms (35)

Synonym
urea-based compound, 20
urea-based compound, 21
bdbm25739
4-({4-[(adamantan-1-ylcarbamoyl)amino]cyclohexyl}oxy)benzoic acid
CHEMBL242459 ,
CHEMBL244405 ,
MLS002415558
smr001339073
trans-4-[4-(3-adamantan-1-ylureido)cyclohexyloxy]benzoic acid
bdbm50217448
bdbm50217439
cis-4-[4-(3-adamantan-1-ylureido)cyclohexyloxy]benzoic acid
HMS2202J19
t-aucb
HMS3350A02
4-[(trans-4-{[(3s,5s,7s)-tricyclo[3.3.1.1~3,7~]dec-1-ylcarbamoyl]amino}cyclohexyl)oxy]benzoic acid
AUB ,
SCHEMBL653866
SCHEMBL653867
SCHEMBL14150188
3WKE
SCHEMBL18465002
SCHEMBL18464995
trans-4-[4-(3-adamantan-1-yl-ureido)-cyclohexyloxy]-benzoic acid
885012-33-9
CS-0064805
HY-113974
Q27458076
trans-aucb
MS-27128
t-aucbt-aucb
4-[4-(1-adamantylcarbamoylamino)cyclohexyl]oxybenzoic acid
SCHEMBL24617188
AKOS040742774
EX-A7729

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"05 nM) had excellent oral bioavailability (98%, n = 2) and blood area under the curve in dogs and was effective in vivo to treat hypotension in lipopolysaccharide challenged murine models."( Orally bioavailable potent soluble epoxide hydrolase inhibitors.
Hammock, BD; Hwang, SH; Liu, JY; Morisseau, C; Tsai, HJ, 2007
)
0.34
" However, active compounds to date have high cLogP's and are poorly soluble, leading to low bioavailability and thus limiting any therapeutic application."( Screening a library of 1600 adamantyl ureas for anti-Mycobacterium tuberculosis activity in vitro and for better physical chemical properties for bioavailability.
Grzegorzewicz, AE; Hess, TN; Jackson, M; Jones, V; Kasagami, T; Kim, IH; Lee, RE; Lenaerts, AJ; McNeil, MR; Merzlikin, O; Morisseau, C; North, EJ; Scherman, MS, 2012
)
0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
importin subunit beta-1 isoform 1Homo sapiens (human)Potency5.80485.804836.130665.1308AID540253
snurportin-1Homo sapiens (human)Potency5.80485.804836.130665.1308AID540253
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency5.80485.804816.996225.9290AID540253
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency7.30780.004611.374133.4983AID624296
Guanine nucleotide-binding protein GHomo sapiens (human)Potency22.38721.995325.532750.1187AID624288
[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)
Fatty-acid amide hydrolase 1Homo sapiens (human)IC50 (µMol)10.00000.00020.59827.0000AID1373459
RAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)IC50 (µMol)10.00000.00100.33498.9000AID756116
Bifunctional epoxide hydrolase 2Homo sapiens (human)IC50 (µMol)0.00140.00000.54509.1000AID1373458; AID1551776; AID1601280; AID1706963; AID1722863; AID1814168; AID1833694; AID1857694; AID1873510; AID296655; AID296663; AID592803; AID661405; AID756127
Bifunctional epoxide hydrolase 2Homo sapiens (human)Ki0.00150.00150.04540.1560AID755345
Bifunctional epoxide hydrolase 2Mus musculus (house mouse)IC50 (µMol)0.00490.00170.05670.4220AID1814172; AID296658
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)100.00000.00010.995010.0000AID592802
Bifunctional epoxide hydrolase 2Rattus norvegicus (Norway rat)IC50 (µMol)0.00800.00600.09800.3700AID1814173; AID296659
Epoxide hydrolase BMycobacterium tuberculosis CDC1551IC50 (µMol)51.70000.01900.66403.4000AID1798579
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (108)

Processvia Protein(s)Taxonomy
fatty acid catabolic processFatty-acid amide hydrolase 1Homo sapiens (human)
arachidonic acid metabolic processFatty-acid amide hydrolase 1Homo sapiens (human)
positive regulation of vasoconstrictionFatty-acid amide hydrolase 1Homo sapiens (human)
monoacylglycerol catabolic processFatty-acid amide hydrolase 1Homo sapiens (human)
apoptotic processRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
protein phosphorylationRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
signal transductionRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
activation of adenylate cyclase activityRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of cell population proliferationRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
insulin receptor signaling pathwayRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
Schwann cell developmentRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
thyroid gland developmentRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of protein-containing complex assemblyRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
somatic stem cell population maintenanceRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
regulation of Rho protein signal transductionRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
insulin secretion involved in cellular response to glucose stimulusRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
response to muscle stretchRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
ERBB2-ERBB3 signaling pathwayRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
wound healingRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
myelinationRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
regulation of apoptotic processRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of apoptotic processRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of MAPK cascadeRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
type B pancreatic cell proliferationRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
intermediate filament cytoskeleton organizationRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
regulation of cell differentiationRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
insulin-like growth factor receptor signaling pathwayRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
neurotrophin TRK receptor signaling pathwayRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
thymus developmentRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
face developmentRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
type II interferon-mediated signaling pathwayRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
death-inducing signaling complex assemblyRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway via death domain receptorsRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
regulation of cell motilityRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
MAPK cascadeRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
response to toxic substanceBifunctional epoxide hydrolase 2Homo sapiens (human)
positive regulation of gene expressionBifunctional epoxide hydrolase 2Homo sapiens (human)
dephosphorylationBifunctional epoxide hydrolase 2Homo sapiens (human)
cholesterol homeostasisBifunctional epoxide hydrolase 2Homo sapiens (human)
stilbene catabolic processBifunctional epoxide hydrolase 2Homo sapiens (human)
phospholipid dephosphorylationBifunctional epoxide hydrolase 2Homo sapiens (human)
regulation of cholesterol metabolic processBifunctional epoxide hydrolase 2Homo sapiens (human)
epoxide metabolic processBifunctional epoxide hydrolase 2Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 2Homo sapiens (human)
embryo implantationProstaglandin G/H synthase 2Homo sapiens (human)
learningProstaglandin G/H synthase 2Homo sapiens (human)
memoryProstaglandin G/H synthase 2Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell population proliferationProstaglandin G/H synthase 2Homo sapiens (human)
response to xenobiotic stimulusProstaglandin G/H synthase 2Homo sapiens (human)
response to nematodeProstaglandin G/H synthase 2Homo sapiens (human)
response to fructoseProstaglandin G/H synthase 2Homo sapiens (human)
response to manganese ionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 2Homo sapiens (human)
bone mineralizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fever generationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic plasticityProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergicProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin secretionProstaglandin G/H synthase 2Homo sapiens (human)
response to estradiolProstaglandin G/H synthase 2Homo sapiens (human)
response to lipopolysaccharideProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationProstaglandin G/H synthase 2Homo sapiens (human)
response to vitamin DProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to heatProstaglandin G/H synthase 2Homo sapiens (human)
response to tumor necrosis factorProstaglandin G/H synthase 2Homo sapiens (human)
maintenance of blood-brain barrierProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of protein import into nucleusProstaglandin G/H synthase 2Homo sapiens (human)
hair cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of apoptotic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vasoconstrictionProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
decidualizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle cell proliferationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of inflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
response to glucocorticoidProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of calcium ion transportProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicProstaglandin G/H synthase 2Homo sapiens (human)
response to fatty acidProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to mechanical stimulusProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to lead ionProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to ATPProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to hypoxiaProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to non-ionic osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to fluid shear stressProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of transforming growth factor beta productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fibroblast growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of platelet-derived growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of neuroinflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to homocysteineProstaglandin G/H synthase 2Homo sapiens (human)
response to angiotensinProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (28)

Processvia Protein(s)Taxonomy
protein bindingFatty-acid amide hydrolase 1Homo sapiens (human)
phospholipid bindingFatty-acid amide hydrolase 1Homo sapiens (human)
fatty acid amide hydrolase activityFatty-acid amide hydrolase 1Homo sapiens (human)
identical protein bindingFatty-acid amide hydrolase 1Homo sapiens (human)
acylglycerol lipase activityFatty-acid amide hydrolase 1Homo sapiens (human)
amidase activityFatty-acid amide hydrolase 1Homo sapiens (human)
small GTPase bindingRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
protein kinase activityRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
protein serine/threonine kinase activityRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
protein bindingRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
ATP bindingRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
enzyme bindingRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
identical protein bindingRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
metal ion bindingRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
protein serine kinase activityRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
MAP kinase kinase kinase activityRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
magnesium ion bindingBifunctional epoxide hydrolase 2Homo sapiens (human)
epoxide hydrolase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
toxic substance bindingBifunctional epoxide hydrolase 2Homo sapiens (human)
phosphatase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
10-hydroxy-9-(phosphonooxy)octadecanoate phosphatase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
lipid phosphatase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
protein homodimerization activityBifunctional epoxide hydrolase 2Homo sapiens (human)
lysophosphatidic acid phosphatase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 2Homo sapiens (human)
protein bindingProstaglandin G/H synthase 2Homo sapiens (human)
enzyme bindingProstaglandin G/H synthase 2Homo sapiens (human)
heme bindingProstaglandin G/H synthase 2Homo sapiens (human)
protein homodimerization activityProstaglandin G/H synthase 2Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 2Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 2Homo sapiens (human)
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneFatty-acid amide hydrolase 1Homo sapiens (human)
cytoskeletonFatty-acid amide hydrolase 1Homo sapiens (human)
organelle membraneFatty-acid amide hydrolase 1Homo sapiens (human)
plasma membraneRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
nucleusRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
cytoplasmRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
mitochondrial outer membraneRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
Golgi apparatusRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
cytosolRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
plasma membraneRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
pseudopodiumRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
cytosolRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
mitochondrionRAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)
peroxisomeBifunctional epoxide hydrolase 2Homo sapiens (human)
peroxisomal matrixBifunctional epoxide hydrolase 2Homo sapiens (human)
cytosolBifunctional epoxide hydrolase 2Homo sapiens (human)
extracellular exosomeBifunctional epoxide hydrolase 2Homo sapiens (human)
peroxisomeBifunctional epoxide hydrolase 2Homo sapiens (human)
nuclear inner membraneProstaglandin G/H synthase 2Homo sapiens (human)
nuclear outer membraneProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulumProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum lumenProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 2Homo sapiens (human)
caveolaProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
protein-containing complexProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (109)

Assay IDTitleYearJournalArticle
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID296660Inhibition of hamster soluble epoxide hydrolase by radioactive assay2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID1814170Metabolic stability in mouse liver recombinant microsomes assessed as parent compound remaining measured after 60 mins in presence of NADP by UPLC-MS/MS analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
From the Design to the
AID296666Bioavailability in dog at 0.3 mg/kg, po2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID296659Inhibition of rat recombinant soluble epoxide hydrolase by fluorescent assay2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID296671Half life in dog at 0.3 mg/kg, po or 0.3 mg/kg, iv2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID296655Inhibition of human recombinant soluble epoxide hydrolase2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID756119Inhibition of recombinant PDGFRalpha (unknown origin) at 10 uM2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID755349Inhibition of human recombinant soluble epoxide hydrolase using ((3-phenyl-oxiranyl)-acetic acid cyano-(6-methoxy-naphthalen-2-yl)-methyl ester) as substrate at 1 nM preincubated for 5 mins prior to substrate addition measured after 60 mins by fluorescenc2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides.
AID1706976Antiinflammatory activity in BALB/c mouse model of carrageenan-induced paw edema assessed as paw thickness at 100 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 3 hrs by caliper method (Rvb = 3.61 +/- 0.36 millimeter)2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1175621Inhibition of recombinant purified chicken soluble epoxide hydrolase using fluorescent PHOME as substrate2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of potent inhibitors of the chicken soluble epoxide hydrolase.
AID1706963Inhibition of recombinant human sEH using PHOME as substrate measured after 15 mins by fluorescence assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1873515Antinociceptive activity in carrageenan-induced inflammatory pain Sprague-Dawley rat model assessed as increase in mechanical withdrawal threshold at 50 mg/kg, ip by von-frey filament assay2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Synthesis and biological evaluation of new series of benzamide derivatives containing urea moiety as sEH inhibitors.
AID1175627Inhibition of recombinant purified chicken soluble epoxide hydrolase by FRET-based competitive displacement assay in presence of ACPU2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of potent inhibitors of the chicken soluble epoxide hydrolase.
AID756127Inhibition of human recombinant soluble epoxide hydrolase assessed as cyano(6-methoxy-naphthalen-2-yl)methyl trans-[(3-phenyloxyran-2-yl)methyl] carbonate conversion to 6-methoxy-2-naphthaldehyde preincubated for 5 mins prior to substrate addition by fluo2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID296664AUC in in dog at 0.3 mg/kg, po2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID1706974Antiinflammatory activity in BALB/c mouse model of carrageenan-induced paw edema assessed as paw thickness at 100 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 2 hrs by caliper method (Rvb = 3.56 +/- 0.29 millimeter)2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1175625Stability in chicken liver microsomes assessed as compound remaining at 1 uM after 30 mins by mass spectrometry2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of potent inhibitors of the chicken soluble epoxide hydrolase.
AID756121Inhibition of recombinant GSK3alpha (unknown origin) at 10 uM2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID296669Reduction of LPS-induced blood pressure mouse C57BL/6 at 0.5 mg/kg, po2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID1722863Inhibition of recombinant human soluble epoxide hydrolase using CMNPC as substrate preincubated for 5 mins followed by substrate addition and measured at 30 secs interval for 10 mins by fluorescence assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors:
AID756126Inhibition of recombinant ABL-2 (unknown origin) at 10 uM2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID1814166Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in human Caco2 cells at 10 uM incubated for 2 hrs treated with Lucifer Yellow by UPLC-MS/MS analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
From the Design to the
AID755345Competitive inhibition of human recombinant soluble epoxide hydrolase using [3H]-tDPPO as substrate2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides.
AID296663Inhibition of human sEH by fluorescent assay2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID1833694Inhibition of human sEH using cyano(6-methoxynaphthalen-2-yl)methyl((3-phenyloxiran-2-yl)methyl)carbonate as a substrate assessed as reduction in 6-methoxynaphthaldehyde formation by fluorescence microplate reader assay2021Bioorganic & medicinal chemistry, 12-01, Volume: 51Further exploration of the structure-activity relationship of dual soluble epoxide hydrolase/fatty acid amide hydrolase inhibitors.
AID592802Inhibition of human recombinant COX-2 after 2 mins by fluorescence assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.
AID296657Solubility in sodium phosphate buffer at pH 7.42007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID1814168Inhibition of human recombinant sEH using CMNPC as substrate incubated for 5 mins by fluorescent based assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
From the Design to the
AID592801Inhibition of ovine COX-1 at 100 uM after 2 mins by fluorescence assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.
AID1722866Apparent permeability across basolateral to apical side in human Caco-2 cells at 10 uM measured after 2 hrs by LC-MS/MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors:
AID296667Reduction of LPS-induced blood pressure mouse C57BL/6 at 1 mg/kg, po2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID1706971Toxicity in BALB/c mouse assessed as effect on paw thickness at 100 mg/kg, ip measured after 1 hr by caliber method (Rvb = 2.64 +/- 0.09 millimeter)2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1373459Inhibition of human FAAH expressed in baculovirus-infected High Five cells S9 fraction using OMP substrate by fluorescence based assay2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Identification and optimization of soluble epoxide hydrolase inhibitors with dual potency towards fatty acid amide hydrolase.
AID296670Tmax in dog at 0.3 mg/kg, po or 0.3 mg/kg, iv2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID1601281Inhibition of murine soluble epoxide hydrolase expressed in baculovirus infected Sf21 cells using NEPC as substrate by fluorescence based assay2019Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors.
AID1722864Solubility of the compound in 1% DMSO/99% PBS buffer solution measured after 2 hrs by light scattering based assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors:
AID756117Inhibition of recombinant PDPK-1 (unknown origin) at 10 uM2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID1706975Antiinflammatory activity in BALB/c mouse model of carrageenan-induced paw edema assessed as paw edema at 100 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 2 hrs by caliper method relative to control2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1601280Inhibition of recombinant human liver soluble epoxide hydrolase expressed in baculovirus infected Sf21 cells using NEPC as substrate by fluorescence based assay2019Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors.
AID296662Inhibition of dog soluble epoxide hydrolase by radioactive assay2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID1873509Inhibition of sEH (unknown origin) at 100 nM relative to control2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Synthesis and biological evaluation of new series of benzamide derivatives containing urea moiety as sEH inhibitors.
AID296658Inhibition of mouse recombinant soluble epoxide hydrolase by fluorescent assay2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID1814174Solubility of compound in PBS incubated for 2 hrs2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
From the Design to the
AID1814173Inhibition of rat recombinant sEH using CMNPC as substrate incubated for 5 mins by fluorescent based assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
From the Design to the
AID1819953Cardioprotective activity in Langendorff-perfused wild-type C57BL/6 mouse heart assessed as increase in heart rate at 3 nM2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPARγ Modulator.
AID661400Antimycobacterial activity against Mycobacterium tuberculosis H37Ra at 10 uM2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Screening a library of 1600 adamantyl ureas for anti-Mycobacterium tuberculosis activity in vitro and for better physical chemical properties for bioavailability.
AID296665Bioavailability in dog at 0.3 mg/kg, iv2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID756125Inhibition of recombinant FLT-3 (unknown origin) at 10 uM2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID296661Inhibition of cat soluble epoxide hydrolase by radioactive assay2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID1706972Antiinflammatory activity in BALB/c mouse model of carrageenan-induced paw edema assessed as paw thickness at 100 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 1 hr by caliper method (Rvb = 3.51 +/- 0.19 millimeter)2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1814171Metabolic stability in rat liver recombinant microsomes assessed as parent compound remaining measured after 60 mins in presence of NADP by UPLC-MS/MS analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
From the Design to the
AID1814178Inhibition of human COX-22021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
From the Design to the
AID1175624Stability in human liver microsomes assessed as compound remaining at 1 uM after 30 mins by mass spectrometry in presence of NADPH2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of potent inhibitors of the chicken soluble epoxide hydrolase.
AID661399Antimycobacterial activity against Mycobacterium tuberculosis H37Ra2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Screening a library of 1600 adamantyl ureas for anti-Mycobacterium tuberculosis activity in vitro and for better physical chemical properties for bioavailability.
AID756120Inhibition of recombinant PDGFRbeta (unknown origin) at 10 uM2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID592803Inhibition of human recombinant soluble epoxide hydrolase after 10 mins by fluorescent-based assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.
AID1706962Inhibition of recombinant human sEH at 100 nM using PHOME as substrate measured after 15 mins by fluorescence assay relative to control2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1373458Inhibition of human recombinant soluble epoxide hydrolase expressed in baculovirus-infected High Five cells S9 fraction using CMNPC substrate by fluorescence based assay2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Identification and optimization of soluble epoxide hydrolase inhibitors with dual potency towards fatty acid amide hydrolase.
AID1706979Antiinflammatory activity in BALB/c mouse model of carrageenan-induced paw edema assessed as paw edema at 100 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 4 hrs by caliper method relative to control2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1601283Solubility of compound in 1% DMSO : 99% PBS buffer solution at 37 degree C measured after 2 hrs by nephelometer analysis2019Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors.
AID756122Inhibition of recombinant MET (unknown origin) at 10 uM2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID1814177Inhibition of human recombinant LOX-5 preincubated for 10 mins in presence of AA and ATP measured after 20 mins by fluorescent assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
From the Design to the
AID1175626Stability in chicken liver microsomes assessed as compound remaining at 1 uM after 30 mins by mass spectrometry in presence of NADPH2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of potent inhibitors of the chicken soluble epoxide hydrolase.
AID1814169Metabolic stability in human liver recombinant microsomes assessed as parent compound remaining measured after 60 mins in presence of NADP by UPLC-MS/MS analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
From the Design to the
AID1873510Inhibition of sEH (unknown origin)2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Synthesis and biological evaluation of new series of benzamide derivatives containing urea moiety as sEH inhibitors.
AID1857694Inhibition of human recombinant sEH2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors.
AID1175623Stability in human liver microsomes assessed as compound remaining at 1 uM after 30 mins by mass spectrometry2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of potent inhibitors of the chicken soluble epoxide hydrolase.
AID756124Inhibition of recombinant FLT-1 (unknown origin) at 10 uM2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID756113Cytotoxicity against human HuH7 cells by MTT assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID1601282Microsomal stability in human microsomes assessed as parent compound remaining in presence of NADP, glucose-6-phosphate and glucose-6-phosphate dehydrogenase measured after 60 mins by UPLC-MS/MS analysis2019Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors.
AID592808Antiallodynic activity in Sprague-Dawley rat von Frey hair mechanically-stimulated neuropathic pain model assessed as reversal of LPS-induced decrease in paw withdrawal latency at 10 mg/kg, sc administered 60 mins before LPS challenge2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.
AID1722867Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in human Caco-2 cells at 10 uM measured after 2 hrs by LC-MS/MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors:
AID1601284Apparent permeability across apical to basolateral membrane in human Caco2 cells at 10 uM measured after 2 hrs by UPLC-MS/MS analysis2019Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors.
AID1814175Apparent permeability of compound across apical to basolateral side in human Caco2 cells at 10 uM incubated for 2 hrs treated with Lucifer Yellow by UPLC-MS/MS analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
From the Design to the
AID755350Inhibition of human recombinant soluble epoxide hydrolase using ((3-phenyl-oxiranyl)-acetic acid cyano-(6-methoxy-naphthalen-2-yl)-methyl ester) as substrate at 10 nM preincubated for 5 mins prior to substrate addition measured after 60 mins by fluorescen2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides.
AID1601286Efflux ratio of apparent permeability across basolateral to apical membrane over apical to basolateral membrane in human Caco2 cells at 10 uM measured after 2 hrs by UPLC-MS/MS analysis2019Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors.
AID1706977Antiinflammatory activity in BALB/c mouse model of carrageenan-induced paw edema assessed as paw edema at 100 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 3 hrs by caliper method relative to control2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1722865Apparent permeability across apical to basolateral side in human Caco-2 cells at 10 uM measured after 2 hrs by LC-MS/MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors:
AID1814176Cytotoxicity against human SH-SY5Y cells assessed as lethal dose measured after 24 hrs by propidium iodide staining based fluorescent assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
From the Design to the
AID1814167Apparent permeability of compound across basolateral to apical side in human Caco2 cells at 10 uM incubated for 2 hrs treated with Lucifer Yellow by UPLC-MS/MS analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
From the Design to the
AID1706978Antiinflammatory activity in BALB/c mouse model of carrageenan-induced paw edema assessed as paw thickness at 100 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 4 hrs by caliper method (Rvb = 3.60 +/- 0.12 millimeter)2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1551776Inhibition of soluble epoxide hydrolase (unknown origin)2019European journal of medicinal chemistry, Jul-01, Volume: 173Multitarget PPARγ agonists as innovative modulators of the metabolic syndrome.
AID1819948Cardioprotective activity in Langendorff-perfused wild-type C57BL/6 mouse heart assessed as increase in heart rate at 30 nM2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPARγ Modulator.
AID756116Inhibition of full length recombinant c-RAF (unknown origin) using MEK1 as substrate after 1 hr by luminescence assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID756123Inhibition of recombinant FGFR-2 (unknown origin) at 10 uM2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID661405Inhibition of human recombinant soluble epoxide hydrolase using CMNPC as substrate assessed as appearance of 6-methoxy-2-naphthaldehyde after 10 mins by fluorescence analysis2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Screening a library of 1600 adamantyl ureas for anti-Mycobacterium tuberculosis activity in vitro and for better physical chemical properties for bioavailability.
AID1706973Antiinflammatory activity in BALB/c mouse model of carrageenan-induced paw edema assessed as paw edema at 100 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 1 hr by caliper method relative to control2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1814172Inhibition of mouse recombinant sEH using CMNPC as substrate incubated for 5 mins by fluorescent based assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
From the Design to the
AID296656Metabolic stability in human liver microsomes2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
AID1175622Solubility of the compound in 0.1 M sodium phosphate buffer at pH 7.4 containing 1% DMSO by turbidity method2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of potent inhibitors of the chicken soluble epoxide hydrolase.
AID756118Inhibition of recombinant KDR (unknown origin) at 10 uM2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID1601285Apparent permeability across basolateral to apical membrane in human Caco2 cells at 10 uM measured after 2 hrs by UPLC-MS/MS analysis2019Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors.
AID756112Antiproliferative activity against HUVEC after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID756114Cytotoxicity against human HepG2 cells by MTT assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
AID1798579Mtb EHB Inhibition Assay from Article 10.1016/j.jmb.2008.06.030: \\The molecular structure of epoxide hydrolase B from Mycobacterium tuberculosis and its complex with a urea-based inhibitor.\\2008Journal of molecular biology, Sep-12, Volume: 381, Issue:4
The molecular structure of epoxide hydrolase B from Mycobacterium tuberculosis and its complex with a urea-based inhibitor.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structural insights into binding of inhibitors to soluble epoxide hydrolase gained by fragment screening and X-ray crystallography.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (23)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (13.04)29.6817
2010's12 (52.17)24.3611
2020's8 (34.78)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.65

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 Index11.65 (24.57)
Research Supply Index3.18 (2.92)
Research Growth Index4.83 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.65)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.35%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other22 (95.65%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]