Page last updated: 2024-09-27

bms 195614

Description

BMS 195614 : A carboxamide resulting from the formal condensation of the carboxy group of 5,5-dimethyl-8-(quinolin-3-yl)-5,6-dihydronaphthalene-2-carboxylic acid with the amino group of p-aminobenzoic acid. It is a neutral retinoic acid receptor (RAR) alpha-selective antagonist (Ki = 2.5 nM). It displays no significant effect on nuclear receptor corepressor (NCoR) binding; moderately decreases SMRT binding to RAR. It antagonizes agonist-induced coactivator (CoA) recruitment. [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 CID445091
CHEMBL ID2385269
CHEBI ID132571
SCHEMBL ID6756065
MeSH IDM0537867

Synonyms (31)

Synonym
gtpl2643
4-[(5,5-dimethyl-8-quinolin-3-yl6h-naphthalene-2-carbonyl)amino]benzoic acid
cid:445091
CHEBI:132571
bms614
bms 195614
4-({[5,5-dimethyl-8-(quinolin-3-yl)-5,6-dihydronaphthalen-2-yl]carbonyl}amino)benzoic acid
bms-614
4-[[[5,6-dihydro-5,5-dimethyl-8-(3-quinolinyl)-2-naphthalenyl]carbonyl]amino]benzoic acid
253310-42-8
4-[(5,5-dimethyl-8-quinolin-3-yl-6h-naphthalene-2-carbonyl)amino]benzoic acid
bms-195614
bms195614
bms 614
bdbm36811
CHEMBL2385269
SCHEMBL6756065
182135-66-6
AKOS024457734
bms-195614, >=97% (hplc)
J-015939
NCGC00370906-01
Q27075359
4-[[[5,6-dihydro-5,5-dimethyl-8-(3-quinolinyl)-2-naphthalenyl]carbonyl]amino]-benzoicacid
NCGC00370906-03
4-(5,5-dimethyl-8-(quinolin-3-yl)-5,6-dihydronaphthalene-2-carboxamido)benzoic acid
AC-36959
HY-101259
CS-0021054
AT34290
DTXSID101123381

Roles (1)

RoleDescription
retinoic acid receptor alpha antagonistA retinoic acid receptor antagonist that antagonises retinoic acid receptor alpha.
[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 (3)

ClassDescription
quinolinesA class of aromatic heterocyclic compounds each of which contains a benzene ring ortho fused to carbons 2 and 3 of a pyridine ring.
benzoic acidsAny aromatic carboxylic acid that consists of benzene in which at least a single hydrogen has been substituted by a carboxy group.
secondary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1).
[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 (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency30.11160.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency21.31740.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency37.90830.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency21.31740.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency21.31740.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency21.31740.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency21.31740.01238.964839.8107AID1645842
[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)Ki0.00170.00100.94856.5000AID1799455
Retinoic acid receptor gamma Homo sapiens (human)Ki0.00170.00001.997510.0000AID1799455
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (115)

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)
negative regulation of transcription by RNA polymerase IIRetinoic acid receptor gamma Homo sapiens (human)
neural tube closureRetinoic acid receptor gamma Homo sapiens (human)
glandular epithelial cell developmentRetinoic acid receptor gamma Homo sapiens (human)
growth plate cartilage chondrocyte growthRetinoic acid receptor gamma Homo sapiens (human)
apoptotic processRetinoic acid receptor gamma Homo sapiens (human)
positive regulation of cell population proliferationRetinoic acid receptor gamma Homo sapiens (human)
negative regulation of cell population proliferationRetinoic acid receptor gamma Homo sapiens (human)
regulation of cell sizeRetinoic acid receptor gamma Homo sapiens (human)
anterior/posterior pattern specificationRetinoic acid receptor gamma Homo sapiens (human)
positive regulation of gene expressionRetinoic acid receptor gamma Homo sapiens (human)
embryonic camera-type eye developmentRetinoic acid receptor gamma Homo sapiens (human)
regulation of myelinationRetinoic acid receptor gamma Homo sapiens (human)
negative regulation of chondrocyte differentiationRetinoic acid receptor gamma Homo sapiens (human)
response to retinoic acidRetinoic acid receptor gamma Homo sapiens (human)
embryonic hindlimb morphogenesisRetinoic acid receptor gamma Homo sapiens (human)
multicellular organism growthRetinoic acid receptor gamma Homo sapiens (human)
positive regulation of apoptotic processRetinoic acid receptor gamma Homo sapiens (human)
positive regulation of programmed cell deathRetinoic acid receptor gamma Homo sapiens (human)
regulation of myeloid cell differentiationRetinoic acid receptor gamma Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIRetinoic acid receptor gamma Homo sapiens (human)
embryonic eye morphogenesisRetinoic acid receptor gamma Homo sapiens (human)
retinoic acid receptor signaling pathwayRetinoic acid receptor gamma Homo sapiens (human)
canonical Wnt signaling pathwayRetinoic acid receptor gamma Homo sapiens (human)
face developmentRetinoic acid receptor gamma Homo sapiens (human)
trachea cartilage developmentRetinoic acid receptor gamma Homo sapiens (human)
prostate gland epithelium morphogenesisRetinoic acid receptor gamma Homo sapiens (human)
Harderian gland developmentRetinoic acid receptor gamma Homo sapiens (human)
cellular response to retinoic acidRetinoic acid receptor gamma Homo sapiens (human)
stem cell proliferationRetinoic acid receptor gamma Homo sapiens (human)
cellular response to leukemia inhibitory factorRetinoic acid receptor gamma Homo sapiens (human)
negative regulation of stem cell proliferationRetinoic acid receptor gamma Homo sapiens (human)
cell differentiationRetinoic acid receptor gamma Homo sapiens (human)
hormone-mediated signaling pathwayRetinoic acid receptor gamma 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 (42)

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)
DNA-binding transcription factor activity, RNA polymerase II-specificRetinoic acid receptor gamma Homo sapiens (human)
DNA bindingRetinoic acid receptor gamma Homo sapiens (human)
chromatin bindingRetinoic acid receptor gamma Homo sapiens (human)
DNA-binding transcription factor activityRetinoic acid receptor gamma Homo sapiens (human)
protein bindingRetinoic acid receptor gamma Homo sapiens (human)
zinc ion bindingRetinoic acid receptor gamma Homo sapiens (human)
nuclear retinoid X receptor bindingRetinoic acid receptor gamma Homo sapiens (human)
sequence-specific double-stranded DNA bindingRetinoic acid receptor gamma Homo sapiens (human)
nuclear receptor activityRetinoic acid receptor gamma Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingRetinoic acid receptor gamma 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)
[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)
nucleusRetinoic acid receptor gamma Homo sapiens (human)
nucleoplasmRetinoic acid receptor gamma Homo sapiens (human)
cytoplasmRetinoic acid receptor gamma Homo sapiens (human)
membraneRetinoic acid receptor gamma Homo sapiens (human)
chromatinRetinoic acid receptor gamma Homo sapiens (human)
transcription regulator complexRetinoic acid receptor gamma Homo sapiens (human)
nucleusRetinoic acid receptor gamma 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (34)

Assay IDTitleYearJournalArticle
AID748293Inhibition of spermatogenesis in CD1 mouse assessed as asynchronization of spermatogenic cell association at 10 mg/kg, po for 7 days measured after 1 month by bright-field microscopic analysis2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Pharmacological activity of retinoic acid receptor alpha-selective antagonists
AID748296Inhibition of spermatogenesis in CD1 mouse assessed as change in sperm release at stage 9 into lumen in testes at 2 to 10 mg/kg, po for 7 days measured after 1 month by bright-field microscopic analysis relative to control2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Pharmacological activity of retinoic acid receptor alpha-selective antagonists
AID748289Toxicity in CD1 mouse assessed as change in testosterone levels at 2 to 10 mg/kg, po for 7 days by enzyme immunoassay relative to control2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Pharmacological activity of retinoic acid receptor alpha-selective antagonists
AID748292Inhibition of spermatogenesis in CD1 mouse assessed as change in morphology of caudal epididymides at 10 mg/kg, po for 7 days measured after 1 month by bright-field microscopic analysis2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Pharmacological activity of retinoic acid receptor alpha-selective antagonists
AID748291Inhibition of spermatogenesis in CD1 mouse assessed as change in motility of epididymal sperm at 10 mg/kg, po for 7 days measured after 1 month by bright-field microscopic analysis2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Pharmacological activity of retinoic acid receptor alpha-selective antagonists
AID748298Antagonist activity at human RARalpha expressed in human HeLa cells assessed as inhibition of ATRA-induced RARE-chloramphenicol acetyltransferase reporter gene expression after 24 hrs by transactivation competition assay2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Pharmacological activity of retinoic acid receptor alpha-selective antagonists
AID748299Antagonist activity at human RARalpha expressed in human HeLa cells assessed as inhibition of ATRA-induced RARE transactivation after 24 hrs by chloramphenicol acetyltransferase reporter gene assay2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Pharmacological activity of retinoic acid receptor alpha-selective antagonists
AID748294Inhibition of spermatogenesis in CD1 mouse assessed as presence of vacuolar-like spaces at 10 mg/kg, po for 7 days measured after 1 month by bright-field microscopic analysis2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Pharmacological activity of retinoic acid receptor alpha-selective antagonists
AID748297Inhibition of spermatogenesis in CD1 mouse assessed as change in alignment of step 16 spermatids at lumen in stage 8 tubules in testes at 2 to 10 mg/kg, po for 7 days measured after 1 month by bright-field microscopic analysis relative to control2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Pharmacological activity of retinoic acid receptor alpha-selective antagonists
AID748295Toxicity in CD1 mouse assessed as change in testicular weight at 2 to 10 mg/kg, po for 7 days relative to control2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Pharmacological activity of retinoic acid receptor alpha-selective antagonists
AID748290Toxicity in CD1 mouse assessed as change in body weight at 2 to 10 mg/kg, po2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Pharmacological activity of retinoic acid receptor alpha-selective antagonists
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1799455Competitive Assay from Article 10.1016/S1074-5521(99)80084-2: \\Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists.\\1999Chemistry & biology, Aug, Volume: 6, Issue:8
Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1346740Human Retinoic acid receptor-alpha (1B. Retinoic acid receptors)1999Chemistry & biology, Aug, Volume: 6, Issue:8
Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists.
AID1346740Human Retinoic acid receptor-alpha (1B. Retinoic acid receptors)2000Molecular cell, Feb, Volume: 5, Issue:2
Crystal structure of a heterodimeric complex of RAR and RXR ligand-binding domains.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (11.11)18.2507
2000's2 (22.22)29.6817
2010's3 (33.33)24.3611
2020's3 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research Highlights

Bioavailability (1)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, Volume: 96, Issue: 5
2019
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]