Page last updated: 2024-11-13

a-1331852

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Description

A-1331852: 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 CID71565985
CHEMBL ID3793424
SCHEMBL ID14859048
SCHEMBL ID24034646
MeSH IDM000612787

Synonyms (27)

Synonym
chembl3793424 ,
bdbm50162797
S7801
SCHEMBL14859048
a-1331852
1430844-80-6
EX-A1061
gtpl11102
3-[1-(1-adamantylmethyl)-5-methylpyrazol-4-yl]-6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1h-isoquinolin-2-yl]pyridine-2-carboxylic acid
AKOS030573295
CS-5565
HY-19741
BCP18310
a 1331852
a1331852
3-(1-(adamantan-1-ylmethyl)-5-methyl-1h-pyrazol-4-yl)-6-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1h)-yl)picolinicacid
A900598
3-(1-(((3r,5r,7r)-adamantan-1-yl)methyl)-5-methyl-1h-pyrazol-4-yl)-6-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1h)-yl)picolinic acid
AC-36132
nsc797172
nsc-797172
mfcd30532662
3-(1-(adamantan-1-ylmethyl)-5-methyl-1h-pyrazol-4-yl)-6-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1h)-yl)picolinic acid
3-{1-[(adamantan-1-yl)methyl]-5-methyl-1h-pyrazol-4-yl}-6-{8-[(1,3-benzothiazol-2-yl)carbamoyl]-1,2,3,4-tetrahydroisoquinolin-2-yl}pyridine-2-carboxylic acid
EN300-26927815
AS-82460
SCHEMBL24034646

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" In this study, we show that the orally bioavailable XPO1 inhibitor KPT-330 reduced Mcl-1 protein level, by which it synergized with Bcl-xL inhibitor A-1331852 to induce apoptosis in cancer cells."( XPO1 inhibitor KPT-330 synergizes with Bcl-xL inhibitor to induce cancer cell apoptosis by perturbing rRNA processing and Mcl-1 protein synthesis.
Liu, JW; Xiong, ZQ; Yang, C; Zhao, M; Zhu, ZC, 2019
)
0.71
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Apoptosis regulator Bcl-2Homo sapiens (human)Ki0.00600.00000.19012.9000AID1293719; AID1724942
Bcl-2-like protein 1Homo sapiens (human)Ki0.00000.00000.45819.0000AID1293720; AID1599455; AID1724940
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (154)

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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (18)

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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (26)

Assay IDTitleYearJournalArticle
AID1724950Oral bioavailability in Sprague-Dawley rat at 5 mg/kg administered via gavage2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724955AUC in CD1 mouse at 5 mg/kg, iv2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724946Clearance in Sprague-Dawley rat plasma at 5 mg/kg, iv administered as bolus dose2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724954Clearance in CD1 mouse plasma at 5 mg/kg, iv2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1599455Inhibition of Bcl-xL (unknown origin)2019European journal of medicinal chemistry, Sep-01, Volume: 177The chemical biology of apoptosis: Revisited after 17 years.
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.
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.
AID1724959Antitumor activity against human COLO205 cells xenografted in SCID/beige mouse assessed as tumor growth inhibition at 25 mg/kg/day, po qd for 14 days relative to control2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724944Half life in Sprague-Dawley rat at 5 mg/kg, iv administered as bolus dose2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724951Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 48 hrs in presence of 10% human serum by CellTiter-Glo luminescent assay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724952Half life in CD1 mouse at 5 mg/kg, iv2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724949AUC in Sprague-Dawley rat at 5 mg/kg, po administered via gavage2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724961Antitumor activity against human COLO205 cells xenografted in SCID/beige mouse assessed as tumor growth inhibition at 25 mg/kg/day, po qd for 14 days co-administered with 30 mg/kg irinotecan relative to control2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724948Cmax in Sprague-Dawley rat at 5 mg/kg, po administered via gavage2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724947AUC in Sprague-Dawley rat at 5 mg/kg, iv administered as bolus dose2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724958Oral bioavailability in CD1 mouse at 5 mg/kg2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724940Inhibition of F-Bak (GQVGRQLAIIGDK(6-FAM)INR-amide probe binding to BCL-xl (unknown origin) incubated for 1 hr by TR-FRET assay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724945Volume of distribution at steady state in Sprague-Dawley rat at 5 mg/kg, iv administered as bolus dose2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724953Volume of distribution at steady state in CD1 mouse at 5 mg/kg, iv2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
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.
AID1724962Antitumor activity against human COLO205 cells xenografted in SCID/beige mouse assessed as tumor growth delay at 25 mg/kg/day, po qd for 14 days co-administered with 30 mg/kg irinotecan relative to control2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724943Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability after 48 hrs in presence of 10% human serum by CellTiter-Glo luminescent assay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724956Cmax in CD1 mouse at 5 mg/kg, po2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724942Inhibition of F-Bak (GQVGRQLAIIGDK(6-FAM)INR-amide) F-Bak(GQVGRQLAIIGDK(6-FAM)INR-amide) binding to BCL2 (unknown origin) incubated for 1 hr by TR-FRET assay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
AID1724957AUC in CD1 mouse at 5 mg/kg, po2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's12 (75.00)24.3611
2020's4 (25.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.54

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 Index27.54 (24.57)
Research Supply Index2.83 (2.92)
Research Growth Index4.58 (4.65)
Search Engine Demand Index31.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (27.54)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (12.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other14 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]