Page last updated: 2024-11-12

bms 204493

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

Description

BMS-493 : A member of the class of dihydronaphthalenes that is 1,2-dihydronaphthalene which is substituted at positions 1, 1, 4, and 6 by methyl, methyl, phenylethynyl, and 2-(p-carboxyphenyl)vinyl groups, respectively (the E isomer). [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID9909190
CHEMBL ID472172
CHEBI ID132086
SCHEMBL ID3690042
SCHEMBL ID3690047
MeSH IDM0537865

Synonyms (30)

Synonym
EQO ,
4-[(e)-2-[5,5-dimethyl-8-(2-phenylethynyl)-6h-naphthalen-2-yl]ethenyl]benzoic acid
4-{(e)-2-[5,5-dimethyl-8-(phenylethynyl)-5,6-dihydronaphthalen-2-yl]ethenyl}benzoic acid
bms 493
CHEBI:132086
bms493
bms-493
gtpl2641
4-[(e)-2-[5,5-dimethyl-8-(2-phenylethynyl)-5,6-dihydronaphthalen-2-yl]ethenyl]benzoic acid
CHEMBL472172 ,
bms-204493
4-[(1e)-2-[5,6-dihydro-5,5-dimethyl-8-(phenylethynyl)-2-naphthalenyl]ethenyl]-benzoic acid
215030-90-3
bdbm50447840
SCHEMBL3690042
SCHEMBL3690047
4-[(1e)-2-[5,6-dihydro-5,5-dimethyl-8-(2-phenylethynyl)-2-naphthalenyl]ethenyl]benzoic acid
AKOS024457650
bms 493, >=98% (hplc)
J-014108
NCGC00387103-01
HY-108529
Q27075350
CS-0029097
MS-26920
4-(2-(5,5-dimethyl-8-(phenylethynyl)-5,6-dihydronaphthalen-2-yl)vinyl)benzoic acid
2329465-40-7
(e)-4-(2-(5,5-dimethyl-8-(phenylethynyl)-5,6-dihydronaphthalen-2-yl)vinyl)benzoic acid
(e)-4-(2-(5,5-dimethyl-8-(phenylethynyl)-5,6-dihydronaphthalen-2-yl)vinyl)benzoicacid
DTXSID801034187

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]

Roles (1)

RoleDescription
retinoic acid receptor antagonistAn antagonist that acts at the retinoic acid receptor.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
benzoic acidsAny aromatic carboxylic acid that consists of benzene in which at least a single hydrogen has been substituted by a carboxy group.
stilbenoidAny olefinic compound characterised by a 1,2-diphenylethylene backbone.
dihydronaphthalenesAny carbobycyclic compound that is a dihydronaphthalene or a compound obtained from a dihydronaphthalene by formal substitution of one or more hydrogens.
acetylenic compoundAny organic molecule containing a C#C bond.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency21.31740.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency18.99910.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency18.99910.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency18.99910.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency18.99910.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency18.99910.01238.964839.8107AID1645842
[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)
Retinoic acid receptor alphaHomo sapiens (human)IC50 (µMol)0.11400.00080.93249.0000AID1069745
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (98)

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)
ureteric bud developmentRetinoic acid receptor alphaHomo sapiens (human)
neural tube closureRetinoic acid receptor alphaHomo sapiens (human)
liver developmentRetinoic acid receptor alphaHomo sapiens (human)
glandular epithelial cell developmentRetinoic acid receptor alphaHomo sapiens (human)
growth plate cartilage developmentRetinoic acid receptor alphaHomo sapiens (human)
protein phosphorylationRetinoic acid receptor alphaHomo sapiens (human)
germ cell developmentRetinoic acid receptor alphaHomo sapiens (human)
female pregnancyRetinoic acid receptor alphaHomo sapiens (human)
positive regulation of cell population proliferationRetinoic acid receptor alphaHomo sapiens (human)
negative regulation of cell population proliferationRetinoic acid receptor alphaHomo sapiens (human)
negative regulation of translationRetinoic acid receptor alphaHomo sapiens (human)
hippocampus developmentRetinoic acid receptor alphaHomo sapiens (human)
prostate gland developmentRetinoic acid receptor alphaHomo sapiens (human)
negative regulation of granulocyte differentiationRetinoic acid receptor alphaHomo sapiens (human)
embryonic camera-type eye developmentRetinoic acid receptor alphaHomo sapiens (human)
regulation of myelinationRetinoic acid receptor alphaHomo sapiens (human)
response to estradiolRetinoic acid receptor alphaHomo sapiens (human)
response to retinoic acidRetinoic acid receptor alphaHomo sapiens (human)
negative regulation of type II interferon productionRetinoic acid receptor alphaHomo sapiens (human)
negative regulation of tumor necrosis factor productionRetinoic acid receptor alphaHomo sapiens (human)
positive regulation of interleukin-13 productionRetinoic acid receptor alphaHomo sapiens (human)
positive regulation of interleukin-4 productionRetinoic acid receptor alphaHomo sapiens (human)
positive regulation of interleukin-5 productionRetinoic acid receptor alphaHomo sapiens (human)
response to vitamin ARetinoic acid receptor alphaHomo sapiens (human)
response to cytokineRetinoic acid receptor alphaHomo sapiens (human)
multicellular organism growthRetinoic acid receptor alphaHomo sapiens (human)
mRNA transcription by RNA polymerase IIRetinoic acid receptor alphaHomo sapiens (human)
regulation of apoptotic processRetinoic acid receptor alphaHomo sapiens (human)
apoptotic cell clearanceRetinoic acid receptor alphaHomo sapiens (human)
response to ethanolRetinoic acid receptor alphaHomo sapiens (human)
positive regulation of T-helper 2 cell differentiationRetinoic acid receptor alphaHomo sapiens (human)
positive regulation of neuron differentiationRetinoic acid receptor alphaHomo sapiens (human)
positive regulation of cell cycleRetinoic acid receptor alphaHomo sapiens (human)
negative regulation of DNA-templated transcriptionRetinoic acid receptor alphaHomo sapiens (human)
positive regulation of DNA-templated transcriptionRetinoic acid receptor alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIRetinoic acid receptor alphaHomo sapiens (human)
regulation of synaptic plasticityRetinoic acid receptor alphaHomo sapiens (human)
retinoic acid receptor signaling pathwayRetinoic acid receptor alphaHomo sapiens (human)
positive regulation of bindingRetinoic acid receptor alphaHomo sapiens (human)
ventricular cardiac muscle cell differentiationRetinoic acid receptor alphaHomo sapiens (human)
Sertoli cell fate commitmentRetinoic acid receptor alphaHomo sapiens (human)
limb developmentRetinoic acid receptor alphaHomo sapiens (human)
face developmentRetinoic acid receptor alphaHomo sapiens (human)
trachea cartilage developmentRetinoic acid receptor alphaHomo sapiens (human)
chondroblast differentiationRetinoic acid receptor alphaHomo sapiens (human)
negative regulation of cartilage developmentRetinoic acid receptor alphaHomo sapiens (human)
cellular response to lipopolysaccharideRetinoic acid receptor alphaHomo sapiens (human)
cellular response to retinoic acidRetinoic acid receptor alphaHomo sapiens (human)
cellular response to estrogen stimulusRetinoic acid receptor alphaHomo sapiens (human)
regulation of hematopoietic progenitor cell differentiationRetinoic acid receptor alphaHomo sapiens (human)
negative regulation of miRNA transcriptionRetinoic acid receptor alphaHomo sapiens (human)
cell differentiationRetinoic acid receptor alphaHomo sapiens (human)
hormone-mediated signaling pathwayRetinoic acid receptor alphaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIRetinoic acid receptor alphaHomo 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 (40)

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)
mRNA regulatory element binding translation repressor activityRetinoic acid receptor alphaHomo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingRetinoic acid receptor alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingRetinoic acid receptor alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificRetinoic acid receptor alphaHomo sapiens (human)
DNA-binding transcription repressor activityRetinoic acid receptor alphaHomo sapiens (human)
transcription coactivator bindingRetinoic acid receptor alphaHomo sapiens (human)
retinoic acid bindingRetinoic acid receptor alphaHomo sapiens (human)
chromatin bindingRetinoic acid receptor alphaHomo sapiens (human)
DNA-binding transcription factor activityRetinoic acid receptor alphaHomo sapiens (human)
nuclear receptor activityRetinoic acid receptor alphaHomo sapiens (human)
signaling receptor bindingRetinoic acid receptor alphaHomo sapiens (human)
protein bindingRetinoic acid receptor alphaHomo sapiens (human)
zinc ion bindingRetinoic acid receptor alphaHomo sapiens (human)
enzyme bindingRetinoic acid receptor alphaHomo sapiens (human)
protein domain specific bindingRetinoic acid receptor alphaHomo sapiens (human)
chromatin DNA bindingRetinoic acid receptor alphaHomo sapiens (human)
histone deacetylase bindingRetinoic acid receptor alphaHomo sapiens (human)
protein kinase B bindingRetinoic acid receptor alphaHomo sapiens (human)
retinoic acid-responsive element bindingRetinoic acid receptor alphaHomo sapiens (human)
mRNA 5'-UTR bindingRetinoic acid receptor alphaHomo sapiens (human)
protein kinase A bindingRetinoic acid receptor alphaHomo sapiens (human)
alpha-actinin bindingRetinoic acid receptor alphaHomo sapiens (human)
heterocyclic compound bindingRetinoic acid receptor alphaHomo sapiens (human)
sequence-specific double-stranded DNA bindingRetinoic acid receptor alphaHomo 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 (30)

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)
nucleusRetinoic acid receptor alphaHomo sapiens (human)
nucleoplasmRetinoic acid receptor alphaHomo sapiens (human)
transcription regulator complexRetinoic acid receptor alphaHomo sapiens (human)
nucleolusRetinoic acid receptor alphaHomo sapiens (human)
cytoplasmRetinoic acid receptor alphaHomo sapiens (human)
cytosolRetinoic acid receptor alphaHomo sapiens (human)
plasma membraneRetinoic acid receptor alphaHomo sapiens (human)
actin cytoskeletonRetinoic acid receptor alphaHomo sapiens (human)
dendriteRetinoic acid receptor alphaHomo sapiens (human)
perinuclear region of cytoplasmRetinoic acid receptor alphaHomo sapiens (human)
RNA polymerase II transcription regulator complexRetinoic acid receptor alphaHomo sapiens (human)
chromatinRetinoic acid receptor alphaHomo sapiens (human)
protein-containing complexRetinoic acid receptor alphaHomo sapiens (human)
nucleusRetinoic acid receptor alphaHomo 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 (20)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
AID1069744Agonist activity at recombinant GST-tagged RXRalpha LBD (unknown origin) assessed as induction of fluorescein labeled D22 coactivator recruitment after 4 hrs by TR-FRET assay relative to control2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Inhibition of IκB kinase-β and IκB kinase-α by heterocyclic adamantyl arotinoids.
AID1069747Antagonist activity at Gal4-fused RXRalpha (unknown origin) transfected in HEK293 cells assessed as CD3254-induced transcriptional activity at 4 uM by luciferase/beta-galactosidase reporter gene assay relative to CD3254-treated control2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Inhibition of IκB kinase-β and IκB kinase-α by heterocyclic adamantyl arotinoids.
AID1069748Antagonist activity at Gal4-fused RARalpha (unknown origin) transfected in HEK293 cells assessed as ATRA-induced transcriptional activity at 4 uM by luciferase/beta-galactosidase reporter gene assay relative to ATRA-treated control2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Inhibition of IκB kinase-β and IκB kinase-α by heterocyclic adamantyl arotinoids.
AID1069745Inverse agonist activity at RARalpha (unknown origin)2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Inhibition of IκB kinase-β and IκB kinase-α by heterocyclic adamantyl arotinoids.
AID1069749Agonist activity at Gal4-fused RXRalpha (unknown origin) transfected in HEK293 cells assessed as induction of transcriptional activity at 4 uM after 24 hrs by luciferase/beta-galactosidase reporter gene assay relative to control2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Inhibition of IκB kinase-β and IκB kinase-α by heterocyclic adamantyl arotinoids.
AID1069743Agonist activity at recombinant GST-tagged RXRalpha LBD (unknown origin) assessed as induction of biotinylated SRC-1-676-700 coactivator recruitment after 4 hrs by TR-FRET assay (Rvb = 148 +/- 7%)2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Inhibition of IκB kinase-β and IκB kinase-α by heterocyclic adamantyl arotinoids.
AID364889Antagonist activity at human RARbeta expressed in african green monkey CV1 cells assessed as all-trans-retinoic acid-stimulated Gal4 transactivation activity by luciferase reporter gene assay2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
Inhibition of IkappaB kinase-beta and anticancer activities of novel chalcone adamantyl arotinoids.
AID364691Antagonist activity at human RARalpha expressed in african green monkey CV1 cells assessed as all-trans-retinoic acid-stimulated Gal4 transactivation activity by luciferase reporter gene assay2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
Inhibition of IkappaB kinase-beta and anticancer activities of novel chalcone adamantyl arotinoids.
AID1069750Agonist activity at Gal4-fused RARalpha (unknown origin) transfected in HEK293 cells assessed as induction of transcriptional activity at 4 uM after 6 hrs by luciferase/beta-galactosidase reporter gene assay relative to control2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Inhibition of IκB kinase-β and IκB kinase-α by heterocyclic adamantyl arotinoids.
AID364890Antagonist activity at human RARgamma expressed in african green monkey CV1 cells assessed as all-trans-retinoic acid-stimulated Gal4 transactivation activity by luciferase reporter gene assay2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
Inhibition of IkappaB kinase-beta and anticancer activities of novel chalcone adamantyl arotinoids.
AID420861Inhibition of transactivation activity of Gal4-LBD fused human RARbeta (169 to 448) transfected in atRA-stimulated african green monkey CV1 cells after 6 hrs by Dual-light chemiluminescent assay2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Highly twisted adamantyl arotinoids: synthesis, antiproliferative effects and RXR transactivation profiles.
AID420860Inhibition of transactivation activity of Gal4-LBD fused human RARgamma (178 to 454) transfected in atRA-stimulated african green monkey CV1 cells after 6 hrs by Dual-light chemiluminescent assay2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Highly twisted adamantyl arotinoids: synthesis, antiproliferative effects and RXR transactivation profiles.
AID1346786Human Retinoic acid receptor-beta (1B. Retinoic acid receptors)2002Nature, Jan-10, Volume: 415, Issue:6868
Co-regulator recruitment and the mechanism of retinoic acid receptor synergy.
AID1346740Human Retinoic acid receptor-alpha (1B. Retinoic acid receptors)2002Nature, Jan-10, Volume: 415, Issue:6868
Co-regulator recruitment and the mechanism of retinoic acid receptor synergy.
AID1346788Human Retinoic acid receptor-gamma (1B. Retinoic acid receptors)2002Nature, Jan-10, Volume: 415, Issue:6868
Co-regulator recruitment and the mechanism of retinoic acid receptor synergy.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (42.86)29.6817
2010's2 (28.57)24.3611
2020's2 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.51

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

MetricThis Compound (vs All)
Research Demand Index12.51 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.59 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.51)

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%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]