Page last updated: 2024-11-12

bms 309403

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Cross-References

ID SourceID
PubMed CID16122583
CHEMBL ID247920
SCHEMBL ID1066736
MeSH IDM0558971

Synonyms (50)

Synonym
bms 309403
CHEMBL247920 ,
bms-309403
[2''-(5-ethyl-3,4-diphenyl-pyrazol-1-yl)-biphenyl-3-yloxy]-acetic acid
bdbm50212873
((2''-(5-ethyl-3,4-diphenyl-1h-pyrazol-1-yl)-3-biphenylyl)oxy)acetic acid
t4b ,
((2'-(5-ethyl-3,4-diphenyl-1h-pyrazol-1-yl)-3-biphenylyl)oxy)acetic acid
300657-03-8
[2'-(5-ethyl-3,4-diphenyl-pyrazol-1-yl)-biphenyl-3-yloxy]acetic acid
2-((2'-(5-ethyl-3,4-diphenyl-1h-pyrazol-1-yl)-[1,1'-biphenyl]-3-yl)oxy)acetic acid
AKOS016003010
BCP9000677
S6622
2-((2'-(5-ethyl-3,4-diphenyl-1h-pyrazol-1-yl)-[1,1'-biphenyl]-3-yl)oxy)acet ic acid
gtpl6735
bms309403
2-[3-[2-[5-ethyl-3,4-di(phenyl)pyrazol-1-yl]phenyl]phenoxy]acetic acid
680998-70-3
unii-m5x9xsu6j5
acetic acid, ((2'-(5-ethyl-3,4-diphenyl-1h-pyrazol-1-yl)(1,1'-biphenyl)-3-yl)oxy)-
((2'-(5-ethyl-3,4-diphenyl-1h-pyrazol-1-yl)-1,1'-biphenyl-3-yl)oxy)acetic acid
2-((2'-(5-ethyl-3,4-diphenyl-1h-pyrazol-1-yl)(1,1'-biphenyl)-3-yl)oxy)-acetic acid
acetic acid, 2-((2'-(5-ethyl-3,4-diphenyl-1h-pyrazol-1-yl)(1,1'-biphenyl)-3-yl)oxy)-
m5x9xsu6j5 ,
SCHEMBL1066736
[2'-(5-ethyl-3,4-diphenyl-pyrazol-1-yl)-biphenyl-3-yloxy]-acetic acid
fabp4 inhibitor
mfcd09991687
c31h26n2o3
2-[[2'-(5-ethyl-3,4-diphenyl-1h-pyrazol-1-yl)[1,1'-biphenyl]-3-yl]oxy]-acetic acid
2-[[2'-(5-ethyl-3,4-diphenyl-1h-pyrazol-1-yl)[1,1'-biphenyl]-3-yl]oxy]- acetic acid
bms-309403, >=98% (hplc)
EX-A1147
CS-6876
HY-101903
((2'-(5-ethyl-3,4-diphenyl-1h-pyrazol-1-yl)(1,1'-biphenyl)-3-yl)oxy)-acetic acid
J-505200
NCGC00387254-02
{[2'-(5-ethyl-3,4-diphenyl-1h-pyrazol-1-yl)biphenyl-3-yl]oxy}acetic acid
NCGC00387254-01
DS-18592
Q27075342
BCP02448
HMS3866M13
2-[3-[2-(5-ethyl-3,4-diphenylpyrazol-1-yl)phenyl]phenoxy]acetic acid
HMS3740I19
2-(5-ethyl-3,4-diphenyl-pyrazol-1-yl)-biphenyl-3-yloxy]aceticacid
2-((2'-(5-ethyl-3,4-diphenyl-1h-pyrazol-1-yl)-[1,1'-biphenyl]-3-yl)oxy)aceticacid
AC-36146

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

Dosage Studied

ExcerptRelevanceReference
" Oral administration of 12b at a dosage of 50 mg/kg effectively reduced the levels of plasma blood glucose, triglycerides, insulin, total cholesterol and alanine aminotransferase in high-fat/diet-induced obesity model."( Design, synthesis and biological evaluation of thiazole- and indole-based derivatives for the treatment of type II diabetes.
Cao, D; Chen, J; Chen, L; Chen, T; Huang, L; Liang, X; Liu, J; Ma, L; Peng, A; Peng, F; Qiu, J; Qiu, N; Wang, G; Wei, Y; Xiang, M; Xu, Q; Yang, Z, 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)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency9.52210.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency37.90830.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency37.90830.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency37.90830.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency37.90830.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency37.90830.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency37.90830.01238.964839.8107AID1645842
[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)
Fatty acid-binding protein, heartHomo sapiens (human)IC50 (µMol)14.70000.36700.84181.0000AID733214
Fatty acid-binding protein, heartHomo sapiens (human)Ki3.72330.25005.90809.3000AID1648408; AID307908; AID601695
Fatty acid-binding protein, liverMus musculus (house mouse)Ki0.03650.02100.34832.0000AID1802031
Fatty acid-binding protein, adipocyteHomo sapiens (human)IC50 (µMol)0.22100.22101.22532.7500AID733213
Fatty acid-binding protein, adipocyteHomo sapiens (human)Ki0.10960.00200.92916.8000AID1305257; AID1312065; AID1648406; AID307907; AID307910; AID601694
Somatostatin receptor type 2Rattus norvegicus (Norway rat)Ki0.25000.25000.25000.2500AID307908
Fatty acid-binding protein, adipocyteRattus norvegicus (Norway rat)Ki0.02900.02900.02900.0290AID660106
Fatty acid-binding protein 5Homo sapiens (human)Ki4.79500.24802.77129.3700AID1648409; AID307909
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fatty acid-binding protein, adipocyteHomo sapiens (human)Kd1.15130.15000.65822.0500AID1312067; AID1648407
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (74)

Processvia Protein(s)Taxonomy
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)
negative regulation of cell population proliferationFatty acid-binding protein, heartHomo sapiens (human)
long-chain fatty acid transportFatty acid-binding protein, heartHomo sapiens (human)
intracellular lipid transportFatty acid-binding protein, heartHomo sapiens (human)
cholesterol homeostasisFatty acid-binding protein, heartHomo sapiens (human)
regulation of fatty acid oxidationFatty acid-binding protein, heartHomo sapiens (human)
brown fat cell differentiationFatty acid-binding protein, heartHomo sapiens (human)
phospholipid homeostasisFatty acid-binding protein, heartHomo sapiens (human)
positive regulation of phospholipid biosynthetic processFatty acid-binding protein, heartHomo sapiens (human)
positive regulation of long-chain fatty acid import into cellFatty acid-binding protein, heartHomo sapiens (human)
regulation of phosphatidylcholine biosynthetic processFatty acid-binding protein, heartHomo sapiens (human)
response to bacteriumFatty acid-binding protein, adipocyteHomo sapiens (human)
long-chain fatty acid transportFatty acid-binding protein, adipocyteHomo sapiens (human)
cholesterol homeostasisFatty acid-binding protein, adipocyteHomo sapiens (human)
negative regulation of DNA-templated transcriptionFatty acid-binding protein, adipocyteHomo sapiens (human)
positive regulation of inflammatory responseFatty acid-binding protein, adipocyteHomo sapiens (human)
white fat cell differentiationFatty acid-binding protein, adipocyteHomo sapiens (human)
brown fat cell differentiationFatty acid-binding protein, adipocyteHomo sapiens (human)
cellular response to lithium ionFatty acid-binding protein, adipocyteHomo sapiens (human)
cellular response to tumor necrosis factorFatty acid-binding protein, adipocyteHomo sapiens (human)
positive regulation of cold-induced thermogenesisFatty acid-binding protein, adipocyteHomo sapiens (human)
fatty acid transportFatty acid-binding protein, adipocyteHomo sapiens (human)
glucose metabolic processFatty acid-binding protein 5Homo sapiens (human)
lipid metabolic processFatty acid-binding protein 5Homo sapiens (human)
phosphatidylcholine biosynthetic processFatty acid-binding protein 5Homo sapiens (human)
epidermis developmentFatty acid-binding protein 5Homo sapiens (human)
negative regulation of glucose transmembrane transportFatty acid-binding protein 5Homo sapiens (human)
long-chain fatty acid transportFatty acid-binding protein 5Homo sapiens (human)
regulation of prostaglandin biosynthetic processFatty acid-binding protein 5Homo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayFatty acid-binding protein 5Homo sapiens (human)
glucose homeostasisFatty acid-binding protein 5Homo sapiens (human)
regulation of sensory perception of painFatty acid-binding protein 5Homo sapiens (human)
regulation of retrograde trans-synaptic signaling by endocanabinoidFatty acid-binding protein 5Homo sapiens (human)
positive regulation of cold-induced thermogenesisFatty acid-binding protein 5Homo sapiens (human)
lipid transport across blood-brain barrierFatty acid-binding protein 5Homo sapiens (human)
fatty acid transportFatty acid-binding protein 5Homo 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
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)
protein bindingFatty acid-binding protein, heartHomo sapiens (human)
cytoskeletal protein bindingFatty acid-binding protein, heartHomo sapiens (human)
long-chain fatty acid bindingFatty acid-binding protein, heartHomo sapiens (human)
oleic acid bindingFatty acid-binding protein, heartHomo sapiens (human)
long-chain fatty acid transmembrane transporter activityFatty acid-binding protein, adipocyteHomo sapiens (human)
long-chain fatty acid bindingFatty acid-binding protein, adipocyteHomo sapiens (human)
hormone receptor bindingFatty acid-binding protein, adipocyteHomo sapiens (human)
fatty acid bindingFatty acid-binding protein, adipocyteHomo sapiens (human)
retinoic acid bindingFatty acid-binding protein 5Homo sapiens (human)
long-chain fatty acid transmembrane transporter activityFatty acid-binding protein 5Homo sapiens (human)
fatty acid bindingFatty acid-binding protein 5Homo sapiens (human)
protein bindingFatty acid-binding protein 5Homo sapiens (human)
lipid bindingFatty acid-binding protein 5Homo sapiens (human)
identical protein bindingFatty acid-binding protein 5Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
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)
extracellular spaceFatty acid-binding protein, heartHomo sapiens (human)
cytosolFatty acid-binding protein, heartHomo sapiens (human)
extracellular exosomeFatty acid-binding protein, heartHomo sapiens (human)
nucleusFatty acid-binding protein, heartHomo sapiens (human)
cytosolFatty acid-binding protein, heartHomo sapiens (human)
nucleusFatty acid-binding protein, adipocyteHomo sapiens (human)
cytoplasmFatty acid-binding protein, adipocyteHomo sapiens (human)
lipid dropletFatty acid-binding protein, adipocyteHomo sapiens (human)
cytosolFatty acid-binding protein, adipocyteHomo sapiens (human)
extracellular exosomeFatty acid-binding protein, adipocyteHomo sapiens (human)
cytosolFatty acid-binding protein, adipocyteHomo sapiens (human)
nucleusFatty acid-binding protein, adipocyteHomo sapiens (human)
lipid dropletFatty acid-binding protein, adipocyteRattus norvegicus (Norway rat)
extracellular regionFatty acid-binding protein 5Homo sapiens (human)
nucleusFatty acid-binding protein 5Homo sapiens (human)
nucleoplasmFatty acid-binding protein 5Homo sapiens (human)
cytoplasmFatty acid-binding protein 5Homo sapiens (human)
cytosolFatty acid-binding protein 5Homo sapiens (human)
plasma membraneFatty acid-binding protein 5Homo sapiens (human)
postsynaptic densityFatty acid-binding protein 5Homo sapiens (human)
secretory granule membraneFatty acid-binding protein 5Homo sapiens (human)
azurophil granule lumenFatty acid-binding protein 5Homo sapiens (human)
synapseFatty acid-binding protein 5Homo sapiens (human)
extracellular exosomeFatty acid-binding protein 5Homo sapiens (human)
cytosolFatty acid-binding protein 5Homo sapiens (human)
nucleusFatty acid-binding protein 5Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (148)

Assay IDTitleYearJournalArticle
AID319458Effect on TNF expression in mouse aP2-/- macrophage cells relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319416Effect on triglyceride level in 5-week old apoE-/- C57BL/6J mouse fed on western diet and 15 mg/kg/day, po drug simultaneously in 5-11 week early intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319442Effect on hormone-sensitive lipase in mouse aP2-/- macrophage cells at 25 uM after 24 hrs2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID601695Displacement of fluorescent 1-anilinonapthalene 8-sulfonic acid from human h-FABP by fluorescence spectrophotometry2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
New aromatic substituted pyrazoles as selective inhibitors of human adipocyte fatty acid-binding protein.
AID1312067Direct binding to His6-tagged FABP4 (unknown origin) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biological evaluation.
AID733213Inhibition of human FABP4 by 8-anilino-1-naphthalenesulfonic acid based fluorescence displacement assay2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Structure-guided design, synthesis and in vitro evaluation of a series of pyrazole-based fatty acid binding protein (FABP) 3 ligands.
AID1648441Antiinflammatory activity in C57BL/6J mouse assessed as reduction in LPS-induced IL6 secretion at 50 mg/kg, ig administered 1 hr before LPS stimulation and measured after 5 hrs by ELISA2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319419Effect on adiponectin level in 5-week old apoE-/- C57BL/6J mouse fed on western diet and 15 mg/kg/day, po drug simultaneously in 5-11 week early intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648452Reduction in LPS-induced spleen damage in C57BL/6J mouse at 25 mg/kg, ig administered for 4 days and measured by H and E staining-based microscopy analysis2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319461Decrease in fatty acid uptake in FABP-deficient mouse adipocytes reconstituted with exogenous aP2 after 24 hrs2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID660105Inhibition of LPS-stimulated TNFalpha production in mouse RAW264.7 cells at 10 umol/ml dosed simultaneously with LPS measured 24 hrs post dose by ELISA2012European journal of medicinal chemistry, Jun, Volume: 52Design, synthesis and biological evaluation of thiazole- and indole-based derivatives for the treatment of type II diabetes.
AID319425Effect on free fatty acid level in 5-week old apoE-/- C57BL/6J mouse fed on western diet and administered with 15 mg/kg/day, po drug at 12 week in 12-18 week late intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319449Reduction of IL1-beta expressed in mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID601696Antiinflammatory activity in rat RAW264.7 cells assessed as inhibition of lipopolysaccharide induced TNF-alpha mRNA expression by PCR2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
New aromatic substituted pyrazoles as selective inhibitors of human adipocyte fatty acid-binding protein.
AID319447Reduction of IL1-beta expression in human THP1 cells expressing aP2 relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319451Reduction of IL6 expression in human THP1 cells expressing aP2 relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319445Reduction of Mcp1 expression mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319407Decrease in MCP1 production in mouse aP2+/+ macrophage cells after 24 hrs2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648415Cytotoxicity against mouse 3T3L1 cells assessed as reduction in cell viability at 20 and 50 uM incubated for 24 hrs by CCK8 assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319473Suppression of clamp hepatic glucose production in ob/ob mouse at 40 mg/kg/day, po after 4 weeks by hyperinsulinemic-euglycaemic clamp studies2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319427Effect on adiponectin level in 5-week old apoE-/- C57BL/6J mouse fed on western diet and administered with 15 mg/kg/day, po drug at 12 week in 12-18 week late intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319444Reduction of Mcp1 expression mouse aP2+/+ macrophage cells relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1312066Binding affinity to His6-tagged FABP4 (unknown origin) expressed in Escherichia coli BL21(DE3) cells assessed as change in melting temperature at 50 uM after 30 mins by SYPRO orange dye based thermal stability shift assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biological evaluation.
AID1648408Displacement of 1,8-ANS from recombinant human 6His-tagged FABP3 expressed in Escherichia coli BL21 DE3 incubated for 15 mins followed by 1,8-ANS addition and measured after 3 mins by fluorescence based assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID1648413Antiinflammatory activity in human THP1 cells assessed as reduction in LPS-induced IL6 secretion at 20 uM incubated for 18 hrs followed by LPS stimulation and measured after 6 hrs by ELISA2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319429Reduction of cholesterol ester accumulation in human THP1 cells at 25 uM after 4 days relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648450Reduction in LPS-induced liver damage in C57BL/6J mouse at 25 mg/kg, ig administered for 4 days and measured by H and E staining-based microscopy analysis2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319485Attenuation of JNK1 activity in ob/ob mouse adipose tissue at 40 mg/kg/day, po2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319459Decrease in fatty acid uptake in wild type mouse aP2+/+ mal1+/+ preadipocytes after 24 hrs2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID733214Inhibition of human FABP3 by 8-anilino-1-naphthalenesulfonic acid based fluorescence displacement assay2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Structure-guided design, synthesis and in vitro evaluation of a series of pyrazole-based fatty acid binding protein (FABP) 3 ligands.
AID319488Effect on aP2 level in ob/ob mouse adipose tissue at 40 mg/kg/day, po after 6 weeks2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319493Decrease in Fasn expression in liver of ob/ob mouse at 40 mg/kg/day, po2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319440Effect on hormone-sensitive lipase in mouse aP2+/+ macrophage cells at 25 uM after 24 hrs2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319472Effect on glycerol level in ob/ob mouse at 40 mg/kg/day, po after 6 weeks relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319415Effect on cholesterol level in 5-week old apoE -/- C57BL/6J mouse fed on western diet and 15 mg/kg/day, po drug simultaneously in 5-11 week early intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319448Reduction of IL1-beta expressed in mouse aP2+/+ macrophage cells relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319433Increase in APOA1-mediated cholesterol in human THP1 cells at 25 uM relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319454Effect on IL6 expression mouse aP2-/- macrophage cells relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319496Increase in insulin-stimulated IRbeta tyrosine 1162/1163 phosphorylation in ob/ob mouse liver at 40 mg/kg/day, po relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319420Effect on body weight in 5-week old apoE-/- C57BL/6J mouse fed on western diet and administered with 15 mg/kg/day, po drug at 12 week in 12-18 week late intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319428Reduction of transformation of human THP1 cells to foam cells at 25 uM after 3 days relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648407Binding affinity at recombinant human 6His-tagged FABP4 expressed in Escherichia coli BL21 DE3 by isothermal titration calorimetry2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319476Increase in glucose uptake in epididymal fat in ob/ob mouse at 40 mg/kg/day, po after 4 weeks by hyperinsulinemic-euglycaemic clamp studies relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319483Decrease in IL6 expression in ob/ob mouse adipose tissue at 40 mg/kg/day, po2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID733212Selectivity ratio of IC50 for human FABP4 over IC50 for human FABP32013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Structure-guided design, synthesis and in vitro evaluation of a series of pyrazole-based fatty acid binding protein (FABP) 3 ligands.
AID319455Reduction of TNF expression in human THP1 cells expressing aP2 relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319412Effect on body weight in 5-week old apoE-/- C57BL/6J mouse fed on western diet and 15 mg/kg/day, po drug simultaneously in 5-11 week early intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319437Increase in cholesterol efflux in mouse aP2-/-R macrophage cells (re-expression of aP2) at 25 uM relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319446Effect on Mcp1 expression mouse aP2-/- macrophage cells relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319434Increase in ABCA1 mRNA level in human THP1 cells at 25 uM relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648453Hepatoprotective activity in C57BL/6J mouse assessed as reduction in LPS-induced AST level at 25 mg/kg, ig administered before LPS stimulation for 4 days and measured on day 52020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319406Decrease in MCP1 production in human THP1 cells expressing aP2 after 24 hrs2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648449Reduction in LPS-induced lung damage in C57BL/6J mouse at 25 mg/kg, ig administered for 4 days and measured by H and E staining-based microscopy analysis2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID601694Displacement of fluorescent 1-anilinonapthalene 8-sulfonic acid from human a-FABP by fluorescence spectrophotometry2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
New aromatic substituted pyrazoles as selective inhibitors of human adipocyte fatty acid-binding protein.
AID319443Reduction of Mcp1 expression in human THP1 cells expressing aP2 relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319471Increase in free fatty acid level in ob/ob mouse at 40 mg/kg/day, po after 6 weeks relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319414Effect on insulin level in 5-week old apoE-/- C57BL/6J mouse fed on western diet and 15 mg/kg/day, po drug simultaneously in 5-11 week early intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648406Displacement of 1,8-ANS from recombinant human 6His-tagged FABP4 expressed in Escherichia coli BL21 DE3 incubated for 15 mins followed by 1,8-ANS addition and measured after 3 mins by fluorescence based assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319430Reduction in total cholesterol ester content in mouse aP2+/+ macrophage cells at 25 uM relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319478Decrease in glucose level in FABP-deficient mouse fed on high fat diet after 4 weeks by glucose tolerance test relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319481Decrease in Mcp1 expression in ob/ob mouse adipose tissue at 40 mg/kg/day, po2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319463Decrease in blood glucose level in fasted ob/ob mouse at 40 mg/kg/day, po after 6 weeks2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID307909Displacement of 1,8-ANS from eFABP by fluorescence based-assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).
AID319453Reduction of IL6 expression mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1312068Inhibition of FABP4 in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production after 24 hrs by ELISA2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biological evaluation.
AID307910Displacement of [3H]2,3-bis[(2,4-dichlorobenzyl)oxy]benzoic acid from aFABP2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).
AID319474Increase in whole body glucose disposal and glucose infusion rate in ob/ob mouse at 40 mg/kg/day, po after 4 weeks by hyperinsulinemic-euglycaemic clamp studies2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319487Increase in insulin-stimulated AKT serine 473 phosphorylation in ob/ob mouse adipose tissue at 40 mg/kg/day, po relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648440Antiinflammatory activity in C57BL/6J mouse assessed as reduction in LPS-induced MCP1 secretion at 50 mg/kg, ig administered 1 hr before LPS stimulation and measured after 5 hrs by ELISA2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319479Decrease in F4/80 (Emr1) expression in ob/ob mouse adipose tissue at 40 mg/kg/day, po2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319422Effect on insulin level in 5-week old apoE-/- C57BL/6J mouse fed on western diet and administered with 15 mg/kg/day, po drug at 12 week in 12-18 week late intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID660106Inhibition of rat ap2 by fluorescent 1,8-anilino-8-naphthalene sulfonate assay2012European journal of medicinal chemistry, Jun, Volume: 52Design, synthesis and biological evaluation of thiazole- and indole-based derivatives for the treatment of type II diabetes.
AID319468Decrease in insulin level in ob/ob mouse plasma at 40 mg/kg/day, po after 6 weeks relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319408Effect on MCP1 production in mouse aP2-/- macrophage cells after 24 hrs2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319432Effect on cholesterol ester content in mouse aP2-/- macrophages at 25 uM relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319435Increase in ABCA1 protein level in human THP1 cells at 25 uM relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319494Decrease in Acaca expression in liver of ob/ob mouse at 40 mg/kg/day, po2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319492Decrease in Scd1 expression in liver of ob/ob mouse at 40 mg/kg/day, po2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319423Effect on cholesterol level in 5-week old apoE-/- C57BL/6J mouse fed on western diet and administered with 15 mg/kg/day, po drug at 12 week in 12-18 week late intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319462Decrease in blood glucose level in fed ob/ob mouse at 40 mg/kg/day, po after 2 weeks2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319470Increase in adiponectin level in ob/ob mouse plasma at 40 mg/kg/day, po after 6 weeks relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1305257Binding affinity to His-tagged human recombinant FABP4 expressed in Escherichia coli BL21 (DE3) by fluorescence assay2016ACS medicinal chemistry letters, Apr-14, Volume: 7, Issue:4
Interaction Analysis of FABP4 Inhibitors by X-ray Crystallography and Fragment Molecular Orbital Analysis.
AID319477Decrease in glucose level in wild type mouse fed on high fat diet after 4 weeks by glucose tolerance test relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319417Effect on free fatty acid level in 5-week old apoE-/- C57BL/6J mouse fed on western diet and 15 mg/kg/day, po drug simultaneously in 5-11 week early intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319467Effect on cholesterol level in ob/ob mouse at 40 mg/kg/day, po after 6 weeks relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1312065Displacement of 1,8-ANS from His6-tagged FABP4 (unknown origin) expressed in Escherichia coli BL21(DE3) cells by fluorescence assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biological evaluation.
AID601697Antiinflammatory activity in rat RAW264.7 cells assessed as inhibition of lipopolysaccharide induced MCP-1/CCL2 mRNA expression by PCR2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
New aromatic substituted pyrazoles as selective inhibitors of human adipocyte fatty acid-binding protein.
AID319450Effect on IL1-beta expressed in mouse aP2-/- macrophage cells relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648412Antiinflammatory activity in human THP1 cells assessed as reduction in LPS-induced MCP1 secretion at 20 uM incubated for 18 hrs followed by LPS stimulation and measured after 6 hrs by ELISA2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319497Increase in insulin-stimulated AKT serine 473 phosphorylation in ob/ob mouse liver at 40 mg/kg/day, po relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648455Nephroprotective activity in C57BL/6J mouse assessed as reduction in LPS-induced BUN level at 25 mg/kg, ig administered before LPS stimulation for 4 days and measured on day 52020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319436Increase in cholesterol efflux in mouse aP2+/+ macrophage cells at 25 uM relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319457Reduction of TNF expression mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319413Effect on glucose level in 5-week old apoE -/- C57BL/6J mouse fed on western diet and 15 mg/kg/day, po drug simultaneously in 5-11 week early intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648454Hepatoprotective activity in C57BL/6J mouse assessed as reduction in LPS-induced ALT level at 25 mg/kg, ig administered before LPS stimulation for 4 days and measured on day 52020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319421Effect on glucose level in 5-week old apoE-/- C57BL/6J mouse fed on western diet and administered with 15 mg/kg/day, po drug at 12 week in 12-18 week late intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319480Decrease in Cd68 expression in ob/ob mouse adipose tissue at 40 mg/kg/day, po2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319456Reduction of TNF expression in mouse aP2+/+ macrophage cells relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319486Increase in insulin-stimulated IRbeta tyrosine 1162/1163 phosphorylation in ob/ob mouse adipose tissue at 40 mg/kg/day, po relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1312070Inhibition of FABP4 in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 expression after 24 hrs by qPCR method2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biological evaluation.
AID319460Effect on fatty acid uptake in FABP-deficient mouse aP2-/- mal1-/- preadipocytes after 24 hrs2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319464Increase in glucose metabolism in ob/ob mouse at 40 mg/kg/day, po after 4 weeks by glucose tolerance test2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319439Effect on hormone-sensitive lipase in human THP1 cells expressing aP2 at 25 uM after 24 hrs2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID307907Displacement of 1,8-ANS from aFABP by fluorescence based-assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).
AID1312069Inhibition of FABP4 in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha expression after 24 hrs by qPCR method2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biological evaluation.
AID1648409Displacement of 1,8-ANS from recombinant human 6His-tagged FABP5 expressed in Escherichia coli BL21 DE3 incubated for 15 mins followed by 1,8-ANS addition and measured after 3 mins by fluorescence based assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319431Reduction in total cholesterol ester content in mouse aP2-/-R macrophage cells (re-expression of aP2) at 25 uM relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319484Decrease in TNF expression in ob/ob mouse adipose tissue at 40 mg/kg/day, po2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319438Increase in cholesterol efflux in mouse aP2-/- macrophage cells at 25 uM relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648410Selectivity index, ratio of Ki for recombinant human 6His-tagged FABP3 expressed in Escherichia coli BL21 DE3 to Ki for recombinant human 6His-tagged FABP4 expressed in Escherichia coli BL21 DE32020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319475Increase in glucose uptake in gastrocnemius muscle in ob/ob mouse at 40 mg/kg/day, po after 4 weeks by hyperinsulinemic-euglycaemic clamp studies relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319418Effect on glycerol level in 5-week old apoE-/- C57BL/6J mouse fed on western diet and 15 mg/kg/day, po drug simultaneously in 5-11 week early intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648451Reduction in LPS-induced kidney damage in C57BL/6J mouse at 25 mg/kg, ig administered for 4 days and measured by H and E staining-based microscopy analysis2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319482Decrease in IL1-beta expression in ob/ob mouse adipose tissue at 40 mg/kg/day, po2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319466Effect on pancreatic morphology in ob/ob mouse at 40 mg/kg/day, po2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319452Reduction of IL6 expression mouse aP2+/+ macrophage cells relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319490Attenuation of fatty infiltration of liver in ob/ob mouse at 40 mg/kg/day, po2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319411Inhibition of aP2 in 5-week old apoE-/- C57BL/6J mouse fed on western diet and administered with 15 mg/kg/day, po drug at 12 week in late intervention study assessed as reduction of atherosclerotic lesion in en face aorta relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319426Effect on glycerol level in 5-week old apoE-/- C57BL/6J mouse fed on western diet and administered with 15 mg/kg/day, po drug at 12 week in 12-18 week late intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319409Decrease in MCP1 production in mouse aP2-/-R macrophage cells (re-expression of aP2) after 24 hrs2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319489Effect on mal1 protein level in ob/ob mouse adipose tissue at 40 mg/kg/day, po after 6 weeks2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319441Effect on hormone-sensitive lipase in mouse aP2-/-R macrophage cells (re-expression of aP2) at 25 uM after 24 hrs2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319495Inhibition of JNK1 activity in ob/ob mouse liver at 40 mg/kg/day, po relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319469Decrease in triglyceride level in ob/ob mouse at 40 mg/kg/day, po after 6 weeks relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID1648416Inhibition of FABP4 in mouse 3T3L1 cells assessed as inhibition of forskolin-stimulated lipolysis by measuring free glycerol at 1 to 25 uM incubated for 24 hrs followed by forskolin stimulation and measured after 2 hrs2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
AID319491Reduction of total liver triglyceride level in ob/ob mouse at 40 mg/kg/day, po2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319410Inhibition of aP2 in 5-week old apoE -/- C57BL/6J mouse fed on western diet and 15 mg/kg/day, po drug simultaneously in early intervention study assessed as reduction of atherosclerotic lesion in en face aorta relative to control2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID319465Increase in insulin sensitivity in ob/ob mouse at 40 mg/kg/day, po after 5 weeks by insulin tolerance test2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
AID307908Displacement of 1,8-ANS from mFABP by fluorescence based-assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).
AID319424Effect on triglyceride level in 5-week old apoE-/- C57BL/6J mouse fed on western diet and administered with 15 mg/kg/day, po drug at 12 week in 12-18 week late intervention study2007Nature, Jun-21, Volume: 447, Issue:7147
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
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.
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.
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.
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.
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.
AID1347149Furin counterscreen 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.
AID1347168HepG2 cells viability 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.
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.
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.
AID1347167Vero cells viability 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.
AID1347152Confirmatory screen NINDS 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.
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.
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.
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.
AID1347153Confirmatory 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.
AID1802031FABP1 Fluorescent Ligand Displacement Assay from Article 10.1021/acs.biochem.6b00446: \\FABP1: A Novel Hepatic Endocannabinoid and Cannabinoid Binding Protein.\\2016Biochemistry, 09-20, Volume: 55, Issue:37
FABP1: A Novel Hepatic Endocannabinoid and Cannabinoid Binding Protein.
AID1347158ZIKV-mCherry secondary 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.
AID1347156DAPI mCherry counterscreen 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (16.67)29.6817
2010's7 (58.33)24.3611
2020's3 (25.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.28

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 Index20.28 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index5.21 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.28)

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%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]