Page last updated: 2024-11-13

a-1155463

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Description

A-1155463: a Bcl-X(L) inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID59447577
CHEMBL ID3342332
SCHEMBL ID2501550
MeSH IDM000612786

Synonyms (22)

Synonym
bdbm50030754
chembl3342332 ,
S7800
SCHEMBL2501550
3cq ,
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1h)-yl]-5-(3-{4-[3-(dimethylamino)prop-1-yn-1-yl]-2-fluorophenoxy}propyl)-1,3-thiazole-4-carboxylic acid
a-1155463
1235034-55-5
HY-19725
CS-5398
EX-A1060
AKOS030526342
2-[8-[(2-benzothiazolylamino)carbonyl]-3,4-dihydro-2(1h)-isoquinolinyl]-5-[3-[4-[3-(dimethylamino)-1-propyn-1-yl]-2-fluorophenoxy]propyl]-4-thiazolecarboxylic acid
mfcd29924714
2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1h)-yl)-5-(3-(4-(3-(dimethylamino)prop-1-yn-1-yl)-2-fluorophenoxy)propyl)thiazole-4-carboxylic acid
a1155463
BCP18309
BS-14688
a 1155463
CCG-270355
Q27453707
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1h-isoquinolin-2-yl]-5-[3-[4-[3-(dimethylamino)prop-1-ynyl]-2-fluorophenoxy]propyl]-1,3-thiazole-4-carboxylic acid
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (11)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Apoptosis regulator Bcl-2Homo sapiens (human)IC50 (µMol)0.38200.00100.57634.3000AID1791972; AID1914432
Apoptosis regulator Bcl-2Homo sapiens (human)Ki0.07800.00000.19012.9000AID1168932; AID1293719; AID1914433
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki0.79400.00000.21085.6234AID1914437
Translocator proteinRattus norvegicus (Norway rat)Ki0.79410.00010.65108.9300AID1794444
Delta-type opioid receptorHomo sapiens (human)Ki2.12490.00000.59789.9300AID1794423; AID1914426
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki1.11890.00000.74119.9000AID1794410; AID1914438
Bcl-2-like protein 1Homo sapiens (human)IC50 (µMol)0.00050.00031.04829.5400AID1791971; AID1913236
Bcl-2-like protein 1Homo sapiens (human)Ki0.00000.00000.45819.0000AID1168930; AID1168931; AID1293720
Induced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)Ki0.44000.00101.46539.5400AID1168941
Sigma intracellular receptor 2Homo sapiens (human)Ki0.80840.00010.83604.6005AID1794446; AID1914439
Bcl-2-like protein 2Homo sapiens (human)Ki0.01900.00101.25908.1900AID1168940
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.13590.00000.490110.0000AID1794447; AID1914434
Histamine H3 receptorHomo sapiens (human)Ki1.81110.00010.33998.5110AID1794428; AID1914424
[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)
Bcl-2-like protein 1Homo sapiens (human)EC50 (µMol)0.06500.01000.03370.0650AID1912781
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (204)

Processvia Protein(s)Taxonomy
protein polyubiquitinationApoptosis regulator Bcl-2Homo sapiens (human)
apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsApoptosis regulator Bcl-2Homo sapiens (human)
response to xenobiotic stimulusApoptosis regulator Bcl-2Homo sapiens (human)
response to toxic substanceApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of cell growthApoptosis regulator Bcl-2Homo sapiens (human)
response to cytokineApoptosis regulator Bcl-2Homo sapiens (human)
B cell proliferationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
regulation of calcium ion transportApoptosis regulator Bcl-2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandApoptosis regulator Bcl-2Homo sapiens (human)
G1/S transition of mitotic cell cycleApoptosis regulator Bcl-2Homo sapiens (human)
ossificationApoptosis regulator Bcl-2Homo sapiens (human)
ovarian follicle developmentApoptosis regulator Bcl-2Homo sapiens (human)
metanephros developmentApoptosis regulator Bcl-2Homo sapiens (human)
branching involved in ureteric bud morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
behavioral fear responseApoptosis regulator Bcl-2Homo sapiens (human)
B cell homeostasisApoptosis regulator Bcl-2Homo sapiens (human)
B cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
release of cytochrome c from mitochondriaApoptosis regulator Bcl-2Homo sapiens (human)
regulation of cell-matrix adhesionApoptosis regulator Bcl-2Homo sapiens (human)
lymphoid progenitor cell differentiationApoptosis regulator Bcl-2Homo sapiens (human)
B cell lineage commitmentApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of B cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
response to ischemiaApoptosis regulator Bcl-2Homo sapiens (human)
renal system processApoptosis regulator Bcl-2Homo sapiens (human)
melanin metabolic processApoptosis regulator Bcl-2Homo sapiens (human)
regulation of nitrogen utilizationApoptosis regulator Bcl-2Homo sapiens (human)
autophagyApoptosis regulator Bcl-2Homo sapiens (human)
humoral immune responseApoptosis regulator Bcl-2Homo sapiens (human)
DNA damage responseApoptosis regulator Bcl-2Homo sapiens (human)
actin filament organizationApoptosis regulator Bcl-2Homo sapiens (human)
axonogenesisApoptosis regulator Bcl-2Homo sapiens (human)
female pregnancyApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of cell population proliferationApoptosis regulator Bcl-2Homo sapiens (human)
male gonad developmentApoptosis regulator Bcl-2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to oxidative stressApoptosis regulator Bcl-2Homo sapiens (human)
response to radiationApoptosis regulator Bcl-2Homo sapiens (human)
response to xenobiotic stimulusApoptosis regulator Bcl-2Homo sapiens (human)
response to toxic substanceApoptosis regulator Bcl-2Homo sapiens (human)
post-embryonic developmentApoptosis regulator Bcl-2Homo sapiens (human)
response to iron ionApoptosis regulator Bcl-2Homo sapiens (human)
response to UV-BApoptosis regulator Bcl-2Homo sapiens (human)
response to gamma radiationApoptosis regulator Bcl-2Homo sapiens (human)
regulation of gene expressionApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of autophagyApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of calcium ion transport into cytosolApoptosis regulator Bcl-2Homo sapiens (human)
regulation of glycoprotein biosynthetic processApoptosis regulator Bcl-2Homo sapiens (human)
mesenchymal cell developmentApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of neuron maturationApoptosis regulator Bcl-2Homo sapiens (human)
smooth muscle cell migrationApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of smooth muscle cell migrationApoptosis regulator Bcl-2Homo sapiens (human)
cochlear nucleus developmentApoptosis regulator Bcl-2Homo sapiens (human)
gland morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
regulation of transmembrane transporter activityApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of ossificationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of cell growthApoptosis regulator Bcl-2Homo sapiens (human)
melanocyte differentiationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of cell migrationApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of B cell proliferationApoptosis regulator Bcl-2Homo sapiens (human)
hair follicle morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
axon regenerationApoptosis regulator Bcl-2Homo sapiens (human)
regulation of protein stabilityApoptosis regulator Bcl-2Homo sapiens (human)
endoplasmic reticulum calcium ion homeostasisApoptosis regulator Bcl-2Homo sapiens (human)
glomerulus developmentApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of cellular pH reductionApoptosis regulator Bcl-2Homo sapiens (human)
regulation of protein localizationApoptosis regulator Bcl-2Homo sapiens (human)
myeloid cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of myeloid cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
T cell differentiation in thymusApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationApoptosis regulator Bcl-2Homo sapiens (human)
osteoblast proliferationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of osteoblast proliferationApoptosis regulator Bcl-2Homo sapiens (human)
response to nicotineApoptosis regulator Bcl-2Homo sapiens (human)
organ growthApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of multicellular organism growthApoptosis regulator Bcl-2Homo sapiens (human)
cellular response to glucose starvationApoptosis regulator Bcl-2Homo sapiens (human)
response to hydrogen peroxideApoptosis regulator Bcl-2Homo sapiens (human)
neuron maturationApoptosis regulator Bcl-2Homo sapiens (human)
T cell homeostasisApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
CD8-positive, alpha-beta T cell lineage commitmentApoptosis regulator Bcl-2Homo sapiens (human)
ear developmentApoptosis regulator Bcl-2Homo sapiens (human)
regulation of viral genome replicationApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of melanocyte differentiationApoptosis regulator Bcl-2Homo sapiens (human)
retinal cell programmed cell deathApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of retinal cell programmed cell deathApoptosis regulator Bcl-2Homo sapiens (human)
regulation of mitochondrial membrane permeabilityApoptosis regulator Bcl-2Homo sapiens (human)
focal adhesion assemblyApoptosis regulator Bcl-2Homo sapiens (human)
spleen developmentApoptosis regulator Bcl-2Homo sapiens (human)
thymus developmentApoptosis regulator Bcl-2Homo sapiens (human)
digestive tract morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
oocyte developmentApoptosis regulator Bcl-2Homo sapiens (human)
skeletal muscle fiber developmentApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of skeletal muscle fiber developmentApoptosis regulator Bcl-2Homo sapiens (human)
pigment granule organizationApoptosis regulator Bcl-2Homo sapiens (human)
stem cell developmentApoptosis regulator Bcl-2Homo sapiens (human)
homeostasis of number of cells within a tissueApoptosis regulator Bcl-2Homo sapiens (human)
B cell receptor signaling pathwayApoptosis regulator Bcl-2Homo sapiens (human)
response to glucocorticoidApoptosis regulator Bcl-2Homo sapiens (human)
neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
defense response to virusApoptosis regulator Bcl-2Homo sapiens (human)
establishment of localization in cellApoptosis regulator Bcl-2Homo sapiens (human)
regulation of mitochondrial membrane potentialApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of mitochondrial depolarizationApoptosis regulator Bcl-2Homo sapiens (human)
hematopoietic stem cell differentiationApoptosis regulator Bcl-2Homo sapiens (human)
calcium ion transport into cytosolApoptosis regulator Bcl-2Homo sapiens (human)
T cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of T cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
cellular response to organic substanceApoptosis regulator Bcl-2Homo sapiens (human)
cellular response to hypoxiaApoptosis regulator Bcl-2Homo sapiens (human)
reactive oxygen species metabolic processApoptosis regulator Bcl-2Homo sapiens (human)
dendritic cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
motor neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
cell-cell adhesionApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorApoptosis regulator Bcl-2Homo sapiens (human)
epithelial cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of epithelial cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of G1/S transition of mitotic cell cycleApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of dendritic cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of motor neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of anoikisApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of apoptotic signaling pathwayApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayApoptosis regulator Bcl-2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageApoptosis regulator Bcl-2Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandApoptosis regulator Bcl-2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3AHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
response to cytokineBcl-2-like protein 1Homo sapiens (human)
negative regulation of apoptotic processBcl-2-like protein 1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway via death domain receptorsBcl-2-like protein 1Homo sapiens (human)
ovarian follicle developmentBcl-2-like protein 1Homo sapiens (human)
in utero embryonic developmentBcl-2-like protein 1Homo sapiens (human)
release of cytochrome c from mitochondriaBcl-2-like protein 1Homo sapiens (human)
endocytosisBcl-2-like protein 1Homo sapiens (human)
germ cell developmentBcl-2-like protein 1Homo sapiens (human)
spermatogenesisBcl-2-like protein 1Homo sapiens (human)
male gonad developmentBcl-2-like protein 1Homo sapiens (human)
apoptotic mitochondrial changesBcl-2-like protein 1Homo sapiens (human)
fertilizationBcl-2-like protein 1Homo sapiens (human)
regulation of cytokinesisBcl-2-like protein 1Homo sapiens (human)
positive regulation of mononuclear cell proliferationBcl-2-like protein 1Homo sapiens (human)
ectopic germ cell programmed cell deathBcl-2-like protein 1Homo sapiens (human)
regulation of growthBcl-2-like protein 1Homo sapiens (human)
negative regulation of apoptotic processBcl-2-like protein 1Homo sapiens (human)
negative regulation of neuron apoptotic processBcl-2-like protein 1Homo sapiens (human)
dendritic cell proliferationBcl-2-like protein 1Homo sapiens (human)
response to cycloheximideBcl-2-like protein 1Homo sapiens (human)
regulation of mitochondrial membrane permeabilityBcl-2-like protein 1Homo sapiens (human)
epithelial cell proliferationBcl-2-like protein 1Homo sapiens (human)
negative regulation of developmental processBcl-2-like protein 1Homo sapiens (human)
neuron apoptotic processBcl-2-like protein 1Homo sapiens (human)
defense response to virusBcl-2-like protein 1Homo sapiens (human)
regulation of mitochondrial membrane potentialBcl-2-like protein 1Homo sapiens (human)
cellular response to amino acid stimulusBcl-2-like protein 1Homo sapiens (human)
cellular response to alkaloidBcl-2-like protein 1Homo sapiens (human)
cellular response to gamma radiationBcl-2-like protein 1Homo sapiens (human)
apoptotic process in bone marrow cellBcl-2-like protein 1Homo sapiens (human)
negative regulation of release of cytochrome c from mitochondriaBcl-2-like protein 1Homo sapiens (human)
dendritic cell apoptotic processBcl-2-like protein 1Homo sapiens (human)
hepatocyte apoptotic processBcl-2-like protein 1Homo sapiens (human)
negative regulation of execution phase of apoptosisBcl-2-like protein 1Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damageBcl-2-like protein 1Homo sapiens (human)
negative regulation of endoplasmic reticulum stress-induced intrinsic apoptotic signaling pathwayBcl-2-like protein 1Homo sapiens (human)
negative regulation of protein localization to plasma membraneBcl-2-like protein 1Homo sapiens (human)
negative regulation of reproductive processBcl-2-like protein 1Homo sapiens (human)
negative regulation of dendritic cell apoptotic processBcl-2-like protein 1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandBcl-2-like protein 1Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayBcl-2-like protein 1Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageBcl-2-like protein 1Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandBcl-2-like protein 1Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processBcl-2-like protein 1Homo sapiens (human)
DNA damage responseInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
response to cytokineInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
cell fate determinationInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of autophagyInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
cellular homeostasisInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
positive regulation of apoptotic processInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of apoptotic processInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
protein transmembrane transportInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
positive regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathwayInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of anoikisInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
mitochondrial fusionInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
release of cytochrome c from mitochondriaInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
regulation of cell growthSigma intracellular receptor 2Homo sapiens (human)
regulation of intracellular lipid transportSigma intracellular receptor 2Homo sapiens (human)
regulation of intracellular cholesterol transportSigma intracellular receptor 2Homo sapiens (human)
cholesterol homeostasisSigma intracellular receptor 2Homo sapiens (human)
positive regulation of wound healingSigma intracellular receptor 2Homo sapiens (human)
positive regulation of lipoprotein transportSigma intracellular receptor 2Homo sapiens (human)
response to ischemiaBcl-2-like protein 2Homo sapiens (human)
spermatogenesisBcl-2-like protein 2Homo sapiens (human)
negative regulation of mitochondrial membrane permeabilityBcl-2-like protein 2Homo sapiens (human)
regulation of apoptotic processBcl-2-like protein 2Homo sapiens (human)
negative regulation of apoptotic processBcl-2-like protein 2Homo sapiens (human)
Sertoli cell proliferationBcl-2-like protein 2Homo sapiens (human)
cellular response to estradiol stimulusBcl-2-like protein 2Homo sapiens (human)
negative regulation of release of cytochrome c from mitochondriaBcl-2-like protein 2Homo sapiens (human)
cellular response to amyloid-betaBcl-2-like protein 2Homo sapiens (human)
cellular response to glycineBcl-2-like protein 2Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandBcl-2-like protein 2Homo sapiens (human)
release of cytochrome c from mitochondriaBcl-2-like protein 2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageBcl-2-like protein 2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processBcl-2-like protein 2Homo sapiens (human)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
neurotransmitter secretionHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H3 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H3 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (36)

Processvia Protein(s)Taxonomy
protease bindingApoptosis regulator Bcl-2Homo sapiens (human)
protein bindingApoptosis regulator Bcl-2Homo sapiens (human)
channel activityApoptosis regulator Bcl-2Homo sapiens (human)
channel inhibitor activityApoptosis regulator Bcl-2Homo sapiens (human)
ubiquitin protein ligase bindingApoptosis regulator Bcl-2Homo sapiens (human)
identical protein bindingApoptosis regulator Bcl-2Homo sapiens (human)
sequence-specific DNA bindingApoptosis regulator Bcl-2Homo sapiens (human)
protein heterodimerization activityApoptosis regulator Bcl-2Homo sapiens (human)
BH3 domain bindingApoptosis regulator Bcl-2Homo sapiens (human)
protein phosphatase 2A bindingApoptosis regulator Bcl-2Homo sapiens (human)
molecular adaptor activityApoptosis regulator Bcl-2Homo sapiens (human)
DNA-binding transcription factor bindingApoptosis regulator Bcl-2Homo sapiens (human)
BH domain bindingApoptosis regulator Bcl-2Homo sapiens (human)
GABA receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
protein bindingBcl-2-like protein 1Homo sapiens (human)
protein kinase bindingBcl-2-like protein 1Homo sapiens (human)
identical protein bindingBcl-2-like protein 1Homo sapiens (human)
BH3 domain bindingBcl-2-like protein 1Homo sapiens (human)
BH domain bindingBcl-2-like protein 1Homo sapiens (human)
protein bindingInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
protein transmembrane transporter activityInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
protein heterodimerization activityInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
BH3 domain bindingInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
channel activityInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
BH domain bindingInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
protein bindingSigma intracellular receptor 2Homo sapiens (human)
oxysterol bindingSigma intracellular receptor 2Homo sapiens (human)
cholesterol bindingSigma intracellular receptor 2Homo sapiens (human)
protein bindingBcl-2-like protein 2Homo sapiens (human)
identical protein bindingBcl-2-like protein 2Homo sapiens (human)
protein-containing complex bindingBcl-2-like protein 2Homo sapiens (human)
disordered domain specific bindingBcl-2-like protein 2Homo sapiens (human)
BH domain bindingBcl-2-like protein 2Homo sapiens (human)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
histamine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (52)

Processvia Protein(s)Taxonomy
mitochondrial outer membraneApoptosis regulator Bcl-2Homo sapiens (human)
endoplasmic reticulum membraneApoptosis regulator Bcl-2Homo sapiens (human)
nucleusApoptosis regulator Bcl-2Homo sapiens (human)
cytoplasmApoptosis regulator Bcl-2Homo sapiens (human)
mitochondrionApoptosis regulator Bcl-2Homo sapiens (human)
mitochondrial outer membraneApoptosis regulator Bcl-2Homo sapiens (human)
endoplasmic reticulumApoptosis regulator Bcl-2Homo sapiens (human)
cytosolApoptosis regulator Bcl-2Homo sapiens (human)
membraneApoptosis regulator Bcl-2Homo sapiens (human)
nuclear membraneApoptosis regulator Bcl-2Homo sapiens (human)
myelin sheathApoptosis regulator Bcl-2Homo sapiens (human)
BAD-BCL-2 complexApoptosis regulator Bcl-2Homo sapiens (human)
protein-containing complexApoptosis regulator Bcl-2Homo sapiens (human)
pore complexApoptosis regulator Bcl-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
cleavage furrow5-hydroxytryptamine receptor 3AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3AHomo sapiens (human)
cytoplasmBcl-2-like protein 1Homo sapiens (human)
mitochondrionBcl-2-like protein 1Homo sapiens (human)
mitochondrial outer membraneBcl-2-like protein 1Homo sapiens (human)
mitochondrial inner membraneBcl-2-like protein 1Homo sapiens (human)
mitochondrial matrixBcl-2-like protein 1Homo sapiens (human)
endoplasmic reticulumBcl-2-like protein 1Homo sapiens (human)
centrosomeBcl-2-like protein 1Homo sapiens (human)
cytosolBcl-2-like protein 1Homo sapiens (human)
synaptic vesicle membraneBcl-2-like protein 1Homo sapiens (human)
nuclear membraneBcl-2-like protein 1Homo sapiens (human)
Bcl-2 family protein complexBcl-2-like protein 1Homo sapiens (human)
mitochondrial outer membraneBcl-2-like protein 1Homo sapiens (human)
nucleusInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
nucleoplasmInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
cytoplasmInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
mitochondrionInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
mitochondrial outer membraneInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
cytosolInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
membraneInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
Bcl-2 family protein complexInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
mitochondrial outer membraneInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
endoplasmic reticulumSigma intracellular receptor 2Homo sapiens (human)
lysosomeSigma intracellular receptor 2Homo sapiens (human)
endoplasmic reticulumSigma intracellular receptor 2Homo sapiens (human)
rough endoplasmic reticulumSigma intracellular receptor 2Homo sapiens (human)
plasma membraneSigma intracellular receptor 2Homo sapiens (human)
rough endoplasmic reticulum membraneSigma intracellular receptor 2Homo sapiens (human)
nuclear membraneSigma intracellular receptor 2Homo sapiens (human)
cytosolBcl-2-like protein 2Homo sapiens (human)
Bcl-2 family protein complexBcl-2-like protein 2Homo sapiens (human)
mitochondrial outer membraneBcl-2-like protein 2Homo sapiens (human)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
presynapseHistamine H3 receptorHomo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
synapseHistamine H3 receptorHomo sapiens (human)
dendriteHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID1168936Cmax in SCID-Beige mouse at 5 mg/kg, ip2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
AID1853850Cytotoxicity against human MOLT-4 cells assessed as cell growth inhibition incubated for 72 hrs2022European journal of medicinal chemistry, Mar-15, Volume: 232Trends in targeting Bcl-2 anti-apoptotic proteins for cancer treatment.
AID1168931Inhibition of BCL-XL (unknown origin) incubated for 1 hr in presence of 1% human serum by TR-FRET assay2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
AID1168932Inhibition of BCL-2 (unknown origin) incubated for 1 hr by TR-FRET assay2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
AID1168939Drug concentration in SCID-Beige mouse at 5 mg/kg, ip after 12 hrs2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
AID1853851Cytotoxicity against human platelets assessed as cell growth inhibition incubated for 24 hrs2022European journal of medicinal chemistry, Mar-15, Volume: 232Trends in targeting Bcl-2 anti-apoptotic proteins for cancer treatment.
AID1168940Binding affinity to BCL-W (unknown origin)2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
AID1168938AUC in SCID-Beige mouse at 5 mg/kg, ip2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
AID1168937Tmax in SCID-Beige mouse at 5 mg/kg, ip2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
AID1168942Reduction in platelets count in SCID-Beige mouse at 5 mg/kg, ip after 6 hrs2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
AID1293724Cytotoxicity against human Bcl-XL dependant MOLT4 cells by cell based assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity.
AID1168935Cytotoxicity against BCL-XL-dependent human NCI-H146 cells in presence of 10% human serum incubated for 48 hrs by Cell titerGlo reagent based assay2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
AID1293725Cytotoxicity against human Bcl-2 dependant RS4:11 cells by cell based assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity.
AID1293720Binding affinity to Bcl-XL (unknown origin) by FRET assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity.
AID1168933Selectivity index, ratio of Ki for BCL-2 (unknown origin) to Ki for BCL-XL (unknown origin)2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
AID1293719Binding affinity to Bcl-2 (unknown origin) by FRET assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity.
AID1168930Inhibition of BCL-XL (unknown origin) incubated for 1 hr by TR-FRET assay2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
AID1168941Binding affinity to MCL1 (unknown origin)2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
AID1168944Antitumor activity against BCL-XL-dependent human NCI-H146 cells xenografted in SCID-Beige mouse assessed as tumor growth inhibition at 5 mg/kg, ip for 14 days2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
AID1168943Reduction in platelets count in SCID-Beige mouse at 5 mg/kg, ip after 72 hrs2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's10 (66.67)24.3611
2020's5 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.46

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 Index23.46 (24.57)
Research Supply Index2.77 (2.92)
Research Growth Index4.59 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.46)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (13.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (86.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]