Page last updated: 2024-11-13

mk 8245

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 CID24988881
CHEMBL ID1938870
SCHEMBL ID472978
MeSH IDM0561738

Synonyms (36)

Synonym
HY-13070
bdbm50362592
mk8245
MK-8245 ,
mk 8245
1030612-90-8
CHEMBL1938870 ,
NCGC00346680-01
unii-537e7qe8lx
2h-tetrazole-2-acetic acid, 5-(3-(4-(2-bromo-5-fluorophenoxy)-1-piperidinyl)-5-isoxazolyl)-
537e7qe8lx ,
CS-0410
S1158
(5-{3-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]isoxazol-5-yl}-2h-tetrazol-2-yl)acetic acid
UJEAABFSXKCSGI-UHFFFAOYSA-N ,
MLS006011144
smr004702921
SCHEMBL472978
2-(5-(3-(4-(2-bromo-5-fluorophenoxy)piperidin-1-yl)isoxazol-5-yl)-2h-tetrazol-2-yl)acetic acid
AC-28436
DTXSID80145625
mfcd20039622
AKOS026750582
HMS3654I12
2-[5-[3-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,2-oxazol-5-yl]tetrazol-2-yl]acetic acid
NCGC00346680-05
SW220251-1
2h-tetrazole-2-acetic acid, 5-[3-[4-(2-bromo-5-fluorophenoxy)-1-piperidinyl]-5-isoxazolyl]-;2h-tetrazole-2-acetic acid, 5-[3-[4-(2-bromo-5-fluorophenoxy)-1-piperidinyl]-5-isoxazolyl]-
DB13024
EX-A2267
AS-19554
BCP02516
AMY23640
SB19577
CCG-269424
Q27261073

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (16)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency0.66190.00308.794948.0869AID1347053
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency30.11160.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency0.00470.001310.157742.8575AID1259255
GVesicular stomatitis virusPotency13.45040.01238.964839.8107AID1645842
polyproteinZika virusPotency0.66190.00308.794948.0869AID1347053
Interferon betaHomo sapiens (human)Potency13.45040.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency13.45040.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency13.45040.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency13.45040.01238.964839.8107AID1645842
[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)
Stearoyl-CoA desaturaseHomo sapiens (human)IC50 (µMol)0.53550.00100.35661.0700AID647857; AID692198; AID692201; AID692479
Acyl-CoA (8-3)-desaturaseHomo sapiens (human)IC50 (µMol)100,000.00000.01100.01100.0110AID692205
Acyl-CoA desaturase 1Rattus norvegicus (Norway rat)IC50 (µMol)0.03550.00040.15941.7100AID647858; AID692197; AID692199; AID692202
Acyl-CoA desaturase 1Mus musculus (house mouse)IC50 (µMol)0.00300.00100.68303.4000AID640649; AID692203
Acyl-CoA Rattus norvegicus (Norway rat)IC50 (µMol)100,000.00000.00840.00840.0084AID692204
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (61)

Processvia Protein(s)Taxonomy
unsaturated fatty acid biosynthetic processStearoyl-CoA desaturaseHomo sapiens (human)
positive regulation of cold-induced thermogenesisStearoyl-CoA desaturaseHomo sapiens (human)
monounsaturated fatty acid biosynthetic processStearoyl-CoA desaturaseHomo sapiens (human)
response to fatty acidStearoyl-CoA desaturaseHomo sapiens (human)
unsaturated fatty acid biosynthetic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
long-chain fatty acid biosynthetic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
regulation of DNA-templated transcriptionAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
unsaturated fatty acid biosynthetic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
cell-cell signalingAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
phospholipid biosynthetic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
cellular response to starvationAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
alpha-linolenic acid metabolic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
linoleic acid metabolic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
regulation of cell differentiationAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
icosanoid biosynthetic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
lipid metabolic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
arachidonic acid metabolite production involved in inflammatory responseAcyl-CoA 6-desaturaseHomo sapiens (human)
unsaturated fatty acid biosynthetic processAcyl-CoA 6-desaturaseHomo sapiens (human)
alpha-linolenic acid metabolic processAcyl-CoA 6-desaturaseHomo sapiens (human)
linoleic acid metabolic processAcyl-CoA 6-desaturaseHomo sapiens (human)
positive regulation of cellular response to oxidative stressAcyl-CoA 6-desaturaseHomo sapiens (human)
lipid metabolic processAcyl-CoA 6-desaturaseHomo 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)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
stearoyl-CoA 9-desaturase activityStearoyl-CoA desaturaseHomo sapiens (human)
iron ion bindingStearoyl-CoA desaturaseHomo sapiens (human)
protein bindingStearoyl-CoA desaturaseHomo sapiens (human)
oxidoreductase activityStearoyl-CoA desaturaseHomo sapiens (human)
palmitoyl-CoA 9-desaturase activityStearoyl-CoA desaturaseHomo sapiens (human)
C-5 sterol desaturase activityAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
linoleoyl-CoA desaturase activityAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
oxidoreductase activityAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
omega-6 fatty acid desaturase activityAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
acyl-CoA delta5-desaturase activityAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
oxidoreductase activity, acting on paired donors, with oxidation of a pair of donors resulting in the reduction of molecular oxygen to two molecules of waterAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
stearoyl-CoA 9-desaturase activityAcyl-CoA 6-desaturaseHomo sapiens (human)
linoleoyl-CoA desaturase activityAcyl-CoA 6-desaturaseHomo sapiens (human)
oxidoreductase activity, acting on paired donors, with oxidation of a pair of donors resulting in the reduction of molecular oxygen to two molecules of waterAcyl-CoA 6-desaturaseHomo 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)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
omega-6 fatty acid desaturase activityAcyl-CoA 6-desaturase Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
nucleolusStearoyl-CoA desaturaseHomo sapiens (human)
endoplasmic reticulumStearoyl-CoA desaturaseHomo sapiens (human)
endoplasmic reticulum membraneStearoyl-CoA desaturaseHomo sapiens (human)
membraneStearoyl-CoA desaturaseHomo sapiens (human)
endoplasmic reticulum membraneStearoyl-CoA desaturaseHomo sapiens (human)
mitochondrionAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
endoplasmic reticulum membraneAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
membraneAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
intracellular membrane-bounded organelleAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
endoplasmic reticulum membraneAcyl-CoA 6-desaturaseHomo sapiens (human)
plasma membraneAcyl-CoA 6-desaturaseHomo sapiens (human)
membraneAcyl-CoA 6-desaturaseHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
endoplasmic reticulum membraneAcyl-CoA 6-desaturase Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (122)

Assay IDTitleYearJournalArticle
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347157Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347164384 well plate NINDS Rhodamine confirmatory qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347161Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347163384 well plate NINDS AMC confirmatory qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID1347169Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID692234Ratio drug uptake in liver to plasma of female rhesus monkey at 5 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID640645Drug level in plasma of C57BL/6 mouse at 10 mg/kg, po measured 6 hrs post dosing2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series.
AID692220Drug uptake in eye of female rhesus monkey at 5 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692429Transport by human OATP1B1 stably transfected in butyrate treated dog MDCK2 cells at 10 uM after 3 hrs by scintillation counting in presence of 100 uM OATP inhibitor sulfobromophthalein2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692207Inhibition of human delta6 desaturase activity expressed in human HEpG2 cells2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692206Inhibition of rat delta-6 desaturase activity expressed in human HEpG2 cells2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692226Ratio drug uptake in liver to skin of female rhesus monkey at 5 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID647878Drug uptake in mouse shaved skin at 10 mg/kg, po after 6 hrs2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
AID692479Inhibition of SCD-1 activity in human Hepatocytes expressing organic anion transporting polypeptides assessed as reduction in [I-14C] stearoyl CoA desaturation after 1 hr by scintillation counting2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692230Ratio drug uptake in liver to harderian gland of female rhesus monkey at 5 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692480Antidiabetic activity in diet-induced obese C57BL6 mouse assessed as reduction in liver steatosis at 20 to 60 mg/kg, po BID measured on day 282011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692456Antidiabetic activity in diet-induced obese C57BL6 mouse assessed as reduction in liver triglyceride level at 20 mg/kg, po BID2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692472Inhibition of SCD activity in liver of diet-induced obese C57BL6 mouse assessed as reduction in desaturation induces at 20 mg/kg, po BID administered for 4 weeks2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692221Drug uptake in liver of Beagle dog at 5 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692453Antidiabetic activity in diet-induced obese C57BL6 mouse assessed as reduction in body weight gain at 20 mg/kg, po BID2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692203Inhibition of mouse SCD-12011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID640646Drug level in harderian gland of C57BL/6 mouse at 10 mg/kg, po measured 6 hrs post dosing2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series.
AID692475Drug level in harderian gland of diet-induced obese C57BL6 mouse at 20 mg/kg, po BID2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692211Oral bioavailability in dog2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692237Transport mediated by human OATP1B3 stably transfected in butyrate treated dog MDCK2 cells at 10 uM after 3 hrs by scintillation counting2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692227Ratio drug uptake in liver to skin of Beagle dog at 5 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692222Drug uptake in skin of Beagle dog at 5 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID647872Inhibition of SCD1 in mouse liver assessed as reduction in conversion of [14C]stearic acid to [14C]oleic acid at 2 mg/kg, po measured after 3 hrs2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
AID692202Inhibition of rat SCD-12011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID640644Drug level in liver of C57BL/6 mouse at 10 mg/kg, po measured 6 hrs post dosing2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series.
AID692215Drug uptake in liver of Sprague-Dawley rat at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692431Antidiabetic activity in po dosed diet-induced obese fasted C57BL6 mouse assessed as increase in glucose clearance administered 1 hr before glucose challenge measured 12 hrs thereafter by OGTT2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692225Ratio drug uptake in liver to skin of Sprague-Dawley rat at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692223Drug uptake in eye of Beagle dog at 5 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692231Ratio drug uptake in liver to harderian gland of Beagle dog at 5 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692219Drug uptake in skin of female rhesus monkey at 5 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID640639Antidiabetic activity in C57BL/6 mouse LPD model assessed as reduction in liver SCD activity at 1.6 uM liver concentration dosed at 0.4 mg/kg, po measured 3 hrs post dosing2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series.
AID692463Toxicity in diet-induced obese C57BL6 mouse assessed as adverse effect in eye at 20 to 60 mg/kg, po BID measured within 4 weeks2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692218Drug uptake in liver of female rhesus monkey at 5 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692208Apparent permeability across pig LLC-PK1 cells2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692435Antidiabetic activity in diet-induced obese C57BL6 mouse assessed as reduction in glucose AUC at 3 to 7 mg/kg, po administered 1 hr before oral glucose administration measured 2 hrs thereafter2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692216Drug uptake in skin of Sprague-Dawley rat at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692204Inhibition of rat delta-5 desaturase activity expressed in human HEpG2 cells2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692430Transport by human OATP1B3 stably transfected in butyrate treated dog MDCK2 cells at 10 uM after 3 hrs by scintillation counting in presence of 100 uM OATP inhibitor sulfobromophthalein2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692477Ratio drug uptake in liver to harderian gland in diet-induced C57BL6 mouse at 20 mg/kg, po measured after 4 weeks of dosing2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID640650Antidiabetic activity in po dosed C57BL/6 mouse LPD model assessed as reduction in liver SCD activity measured 6 hrs post dosing2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series.
AID647881Inhibition of SCD1 in mouse liver assessed as reduction in conversion of [14C]stearic acid to [14C]oleic acid after at 0.4 mg/kg, po after 3 hrs2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
AID692224Ratio drug uptake in liver to skin of C57BL6 mouse at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692459Toxicity in diet-induced obese C57BL6 mouse assessed as reduction in food intake at 20 to 60 mg/kg, po BID2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692233Ratio drug uptake in liver to plasma of Sprague-Dawley rat at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692236Transport mediated by human OATP1B1 butyrate treated stably transfected in dog MDCK2 cells at 10 uM after 3 hrs by scintillation counting2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692457Antidiabetic activity in diet-induced obese C57BL6 mouse assessed as reduction in liver triglyceride level at 60 mg/kg, po BID2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692232Ratio drug uptake in liver to plasma of C57BL6 mouse at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692205Inhibition of human delta-5 desaturase activity expressed in human HEpG2 cells2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID640648Ratio of drug uptake in liver to harderian gland of C57BL/6 mouse at 10 mg/kg, po measured 6 hrs post dosing2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series.
AID647879Drug uptake in mouse harderian glands at 10 mg/kg, po after 6 hrs2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
AID692476Ratio drug uptake in liver to harderian gland in diet-induced C57BL6 mouse at 20 mg/kg, po measured after single dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692200Ratio IC50 for SCD-1 activity in organic anion transporting polypeptides-deficient human HepG2 cells to IC50 for SCD-1 activity in Sprague-Dawley rat Hepatocytes expressing organic anion transporting polypeptides2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692478Ratio drug uptake in liver to harderian gland in diet-induced C57BL6 mouse at 20 mg/kg, po measured after 1 weeks of dosing2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692229Ratio drug uptake in liver to harderian gland of Sprague-Dawley rat at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692209Oral bioavailability in mouse2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692473Inhibition of SCD activity in harderian gland of diet-induced obese C57BL6 mouse assessed as reduction in desaturation induces at 20 mg/kg, po BID administered for 4 weeks2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID647877Drug uptake in mouse plasma at 10 mg/kg, po after 6 hrs2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
AID692462Toxicity in diet-induced obese C57BL6 mouse assessed as adverse effect in skin at 20 to 60 mg/kg, po BID measured within 4 weeks2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692235Ratio drug uptake in liver to plasma of Beagle dog at 5 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692199Inhibition of SCD-1 activity in Sprague-Dawley rat Hepatocytes expressing organic anion transporting polypeptides assessed as reduction in [I-14C] stearoyl CoA desaturation by scintillation counting2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID640647Ratio of drug uptake in liver to plasma of C57BL/6 mouse at 10 mg/kg, po measured 6 hrs post dosing2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series.
AID640638Antidiabetic activity in C57BL/6 mouse LPD model assessed as reduction in liver SCD activity at 4.9 uM liver concentration dosed at 2 mg/kg, po measured 3 hrs post dosing2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series.
AID692197Inhibition of SCD-1 activity in Sprague-Dawley rat microsome assessed as reduction in [I-14C] stearoyl CoA desaturation by scintillation counting2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692474Drug level in liver of diet-induced obese C57BL6 mouse at 20 mg/kg, po BID2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID647882Drug uptake in mouse liver at 0.4 mg/kg, po after 3 hrs2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
AID692212Drug uptake in liver of C57BL6 mouse at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692436Antidiabetic activity in diet-induced obese C57BL6 mouse assessed as reduction in glucose AUC at 7 to 10 mg/kg, po administered 1 hr before oral glucose administration measured 2 hrs thereafter2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692454Antidiabetic activity in diet-induced obese C57BL6 mouse assessed as reduction in body weight gain at 60 mg/kg, po BID2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692437Antidiabetic activity in diet-induced obese C57BL6 mouse assessed as reduction in glucose AUC at 7 to 30 mg/kg, po administered 1 hr before oral glucose administration measured 2 hrs thereafter2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692213Drug uptake in skin of C57BL6 mouse at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692210Oral bioavailability in rat2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID647876Drug metabolism in rat hepatocytes assessed as 2-(5-(3-amino-3-(4-(2-bromo-5-fluorophenoxy)piperidin-1-yl)acryloyl)-2H-tetrazol-2-yl)acetic acid level2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
AID640649Inhibition of mouse SCD-12012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series.
AID692217Drug uptake in eye of Sprague-Dawley rat at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692198Inhibition of SCD-1 activity in organic anion transporting polypeptides-deficient human HepG2 cells assessed as reduction in [I-14C] stearoyl CoA desaturation by scintillation counting2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID647867Drug uptake in mouse liver at 10 mg/kg, po after 6 hrs2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
AID692201Inhibition of human SCD-12011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID647857Inhibition of SCD1 in OATP-deficient human HepG2 cells by whole cell assay2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
AID647873Drug uptake in mouse liver at 2 mg/kg, po measured after 3 hrs2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
AID692228Ratio drug uptake in liver to harderian gland of C57BL6 mouse at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692214Drug uptake in eye of C57BL6 mouse at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID647858Inhibition of SCD1 in rat hepatocytes expressing OATP2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
AID1347170Vero cells viability counterscreen for qRT-PCR qHTS assay of selected Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347172Secondary qRT-PCR qHTS assay for selected Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

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 (45.45)24.3611
2020's6 (54.55)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.61

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index25.61 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index22.84 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (25.61)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]