Page last updated: 2024-11-13

at 406

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

Cross-References

ID SourceID
PubMed CID25022340
CHEMBL ID2158051
SCHEMBL ID2724374
MeSH IDM0558791

Synonyms (63)

Synonym
1071992-99-8
AT-406 ,
at 406
at406
debio-1143
xevinapant
CHEMBL2158051 ,
debio 1143
iap inhibitor at-406
sm-406
bdbm50393505
HY-15454
CS-0962
NCGC00346675-01
D-1143 ,
(5s,8s,10ar)-n-benzhydryl-5-((s)-2-(methylamino)propanamido)-3-(3-methylbutanoyl)-6-oxodecahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide
QCR-136 ,
S2754
(5s,8s,10ar)-n-(diphenylmethyl)-5-[(2s)-2-(methylamino)propanamido]-3-(3-methylbutanoyl)-6-oxodecahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide
pyrrolo[1,2-a][1,5]diazocine-8-carboxamide, n-(diphenylmethyl)decahydro-5-[[(2s)-2-(methylamino)-1-oxopropyl]amino]-3-(3-methyl-1-oxobutyl)-6-oxo-, (5s,8s,10ar)-
msc2735845a
xevinapant [usan]
xevinapant [who-dd]
xevinapant [inn]
N65WC8PXDD ,
sm 406
debio1143
(5s,8s,10ar)-n-benzhydryl-5-[[(2s)-2-(methylamino)propanoyl]amino]-3-(3-methylbutanoyl)-6-oxo-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide
gtpl7729
SCHEMBL2724374
(5s,8s,10ar)-n-(diphenylmethyl)decahydro-5-[[(2s)-2-(methylamino)-1-oxopropyl]amino]-3-(3-methyl-1-oxobutyl)-6-oxopyrrolo[1,2-a][1,5 ]diazocine-8-carboxamide
J-501625
AC-30282
unii-n65wc8pxdd
(5s,8s,10ar)-n-(diphenylmethyl)-5-[(n-methyl-l-alanyl)amino]-3-(3-methylbutanoyl)-6-oxodecahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide
DTXSID50648496
EX-A104
AKOS027250726
(5s,8s,10ar)-n-(diphenylmethyl)decahydro-5-(((2s)-2-(methylamino)-1-oxopropyl)amino)-3-(3-methyl-1-oxobutyl)-6-oxopyrrolo(1,2-a)(1,5)diazocine-8-carboxamide
d 1143
mfcd22124467
NCGC00346675-03
at406 (sm-406, arry-334543)
BCP04668
1071992-99-8, 1071992-57-8 (hcl)
Q27074566
CCG-270056
debio-1143 (at-406)
1071992-99-8 (free base)
AS-56453
at-406(at406)
nsc-764757
nsc764757
Z2740129972
(5s,8s,10ar)-n-(diphenylmethyl)-5-[(2s)-2-(methylamino)propanamido]-3-(3-methylbutanoyl)-6-oxo-decahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide
EN300-25327900
iaps inhibitor debio 1143
smac mimetic debio 1143
second mitochondrial-derived activator of caspases mimetic debio 1143
d1143
iaps antagonist debio 1143
pyrrolo(1,2-a)(1,5)diazocine-8-carboxamide, n-((1,1'-biphenyl)-2-ylmethyl)decahydro-5-(((2s)-2-(methylamino)-1-oxopropyl)amino)-3-(3-methyl-1-oxobutyl)-6-oxo-, (5s,8s,10ar)
pyrrolo(1,2-a)(1,5)diazocine-8-carboxamide, n-(diphenylmethyl)decahydro-5-(((2s)-2-(methylamino)-1-oxopropyl)amino)-3-(3-methyl-1-oxobutyl)-6-oxo-, (5s,8s,10ar)-

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"We report the discovery and characterization of SM-406 (compound 2), a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs)."( A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
Cai, Q; Guo, M; Kang, S; Leopold, L; Liu, L; Lu, J; McEachern, D; Miller, R; Nikolovska-Coleska, Z; Peng, Y; Qiu, S; Sun, D; Sun, H; Wang, S; Yang, CY; Yang, D; Yi, H; Zhang, T, 2011
)
0.37
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.77240.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency34.52270.001310.157742.8575AID1259252; AID1259253; AID1259256
[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)
Genome polyprotein Zika virusIC50 (µMol)4.10001.10001.94004.1000AID1659171
Genome polyprotein Zika virusKi13.50000.80000.80000.8000AID1659171
E3 ubiquitin-protein ligase XIAPHomo sapiens (human)IC50 (µMol)0.10490.00750.62274.1000AID1616477; AID1616478; AID695455
E3 ubiquitin-protein ligase XIAPHomo sapiens (human)Ki0.06640.00200.10670.4000AID695455
Baculoviral IAP repeat-containing protein 3Homo sapiens (human)IC50 (µMol)0.06640.00850.08930.6900AID1616476; AID1616483; AID695457
Baculoviral IAP repeat-containing protein 3Homo sapiens (human)Ki0.00510.00201.93049.6000AID695457
Baculoviral IAP repeat-containing protein 2Homo sapiens (human)IC50 (µMol)0.02710.00040.31212.7200AID1616481; AID1616482; AID695456
Baculoviral IAP repeat-containing protein 2Homo sapiens (human)Ki0.00190.00050.00440.0170AID695456
[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)
Genome polyprotein Zika virusKd9.00009.00009.00009.0000AID1659181
E3 ubiquitin-protein ligase XIAPHomo sapiens (human)EC50 (µMol)0.03400.01500.17340.5000AID1239111
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (52)

Processvia Protein(s)Taxonomy
regulation of apoptotic processE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
DNA damage responseE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
negative regulation of tumor necrosis factor-mediated signaling pathwayE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
Wnt signaling pathwayE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
regulation of BMP signaling pathwayE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
positive regulation of protein ubiquitinationE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
positive regulation of type I interferon productionE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
regulation of cell population proliferationE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
defense response to bacteriumE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
negative regulation of apoptotic processE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
regulation of innate immune responseE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
positive regulation of JNK cascadeE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
regulation of inflammatory responseE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
neuron apoptotic processE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
copper ion homeostasisE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
regulation of apoptosis involved in tissue homeostasisE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
regulation of nucleotide-binding domain, leucine rich repeat containing receptor signaling pathwayE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
nucleotide-binding oligomerization domain containing 1 signaling pathwayE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
nucleotide-binding oligomerization domain containing 2 signaling pathwayE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
protein K63-linked ubiquitinationE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
inhibition of cysteine-type endopeptidase activityE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
positive regulation of protein linear polyubiquitinationE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
regulation of cell cycleE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
apoptotic processBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
cell surface receptor signaling pathwayBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
canonical NF-kappaB signal transductionBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
spermatogenesisBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
positive regulation of protein ubiquitinationBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
regulation of toll-like receptor signaling pathwayBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
non-canonical NF-kappaB signal transductionBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
regulation of RIG-I signaling pathwayBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
regulation of apoptotic processBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
regulation of innate immune responseBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
regulation of inflammatory responseBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
regulation of necroptotic processBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
regulation of nucleotide-binding domain, leucine rich repeat containing receptor signaling pathwayBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
regulation of cysteine-type endopeptidase activityBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
regulation of cell cycleBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
negative regulation of apoptotic processBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
negative regulation of necroptotic processBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
protein polyubiquitinationBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
response to hypoxiaBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
placenta developmentBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
apoptotic processBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
cell surface receptor signaling pathwayBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
canonical NF-kappaB signal transductionBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
regulation of toll-like receptor signaling pathwayBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
non-canonical NF-kappaB signal transductionBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
regulation of RIG-I signaling pathwayBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
regulation of cell population proliferationBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
regulation of apoptotic processBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
negative regulation of apoptotic processBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
regulation of innate immune responseBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
response to ethanolBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
regulation of cell differentiationBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
regulation of inflammatory responseBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
response to cAMPBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
regulation of cell cycleBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
regulation of necroptotic processBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
necroptotic processBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
regulation of nucleotide-binding domain, leucine rich repeat containing receptor signaling pathwayBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
regulation of non-canonical NF-kappaB signal transductionBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
negative regulation of ripoptosome assembly involved in necroptotic processBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
positive regulation of protein K63-linked ubiquitinationBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
positive regulation of protein K48-linked ubiquitinationBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
positive regulation of protein monoubiquitinationBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
regulation of cysteine-type endopeptidase activityBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
regulation of reactive oxygen species metabolic processBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
positive regulation of protein ubiquitinationBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
negative regulation of necroptotic processBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
ubiquitin-protein transferase activityE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
cysteine-type endopeptidase inhibitor activityE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
protein bindingE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
identical protein bindingE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic processE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
metal ion bindingE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
endopeptidase regulator activityE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
ubiquitin protein ligase activityE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
protein serine/threonine kinase bindingE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
ubiquitin-protein transferase activityBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
protein bindingBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
transferase activityBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
protein-containing complex bindingBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
metal ion bindingBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic processBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
ubiquitin protein ligase activityBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
transcription coactivator activityBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
ubiquitin-protein transferase activityBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
protein bindingBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
zinc ion bindingBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
transferase activityBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
identical protein bindingBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
ubiquitin bindingBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
protein-containing complex bindingBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
protein-folding chaperone bindingBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
FBXO family protein bindingBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
ubiquitin protein ligase activityBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic processBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
cytoplasmE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
nucleusE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
nucleoplasmE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
cytoplasmE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
cytosolE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
nucleusE3 ubiquitin-protein ligase XIAPHomo sapiens (human)
nucleusBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
nucleoplasmBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
cytoplasmBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
cytosolBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
protein-containing complexBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
nucleusBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
cytoplasmBaculoviral IAP repeat-containing protein 3Homo sapiens (human)
XY bodyBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
nucleusBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
cytoplasmBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
cytosolBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
cytoplasmic side of plasma membraneBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
CD40 receptor complexBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
nucleusBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
cytoplasmBaculoviral IAP repeat-containing protein 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (139)

Assay IDTitleYearJournalArticle
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
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.
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.
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.
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.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary 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.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1616481Inhibition of N-terminal 6x-His-tagged recombinant human cIAP1-BIR3 (258 to 363 residues) expressed in Escherichia coli incubated for 2 hrs without 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695638Antitumor activity against human MDA-MB-231 cells xenografted in SCID mouse assessed inhibition of tumor growth at 100 mg/kg, po administered daily for 5 days/week for 2 weeks2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695651Tmax in human MDA-MB-231 cells xenografted SCID mouse plasma at 30 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695456Competitive inhibition of human cIAP1 BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1616496Cytotoxicity in human SK-MEL-28 cells assessed as reduction in cell viability in presence of 1 ng/mL TNFlpha measured every 3 hrs for 4 days by IncuCyteS3 live-cell analysis system based assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID1239121Antitumor activity against human MDA-MB-231 cells xenografted in Balb/c SCID mouse assessed as tumor growth inhibition at 100 mg/kg, po qd measured every 3 days2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.
AID695668AUC (0 to t) in human MDA-MB-231 cells xenografted SCID mouse tumor at 100 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695659AUC (0 to t) in human MDA-MB-231 cells xenografted SCID mouse tumor at 10 mg/kg, iv administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1616489Induction of cIAP1 degradation in human A549 cells assessed as reduction in cIAP1 protein level at 1 uM incubated for 3 hrs by Western blot analysis2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695655Cmax in human MDA-MB-231 cells xenografted SCID mouse plasma at 100 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695635Toxicity in human MDA-MB-231 cells xenografted in SCID mouse at 100 mg/kg, po administered daily for 5 days/week for 2 to 3 weeks2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695670Tmax in human MDA-MB-231 cells xenografted SCID mouse tumor at 100 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1616497Cytotoxicity in human A549 cells assessed as reduction in cell viability in presence of 1 ng/mL TNFlpha measured every 3 hrs for 4 days by IncuCyteS3 live-cell analysis system based assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695677Inhibition of human ERG at 30 uM2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695653Oral bioavailability in human MDA-MB-231 cells xenografted SCID mouse plasma at 30 mg/kg administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695455Competitive inhibition of human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695676Inhibition of Cytochrome P4502011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1659181Binding affinity to N-terminal His-tagged Zika virus NS2B-NS3 protease (1 to 187 residues) using Boc-Gly-Arg-Arg-AMC as substrate2020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Inhibitors of the Zika virus protease NS2B-NS3.
AID1616494Induction of apoptosis in human SK-MEL-28 cells assessed as increase in caspase-3/7 activity at 2.5 uM incubated for 36 hrs in presence of 1 ng/mL TNFlpha by IncuCyteS3 caspase-3/7 fluorescence-based apoptosis assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695646Tmax in human MDA-MB-231 cells xenografted SCID mouse plasma at 10 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695675Antitumor activity against human MDA-MB-231 cells xenografted in SCID mouse assessed inhibition of tumor growth at 100 mg/kg, po administered daily for 5 days/week for 2 weeks measured on day 36 relative to untreated control2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1616490Induction of cIAP2 degradation in human SK-MEL-28 cells assessed as reduction in cIAP2 protein level at 1 uM incubated for 3 hrs by Western blot analysis2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695663Cmax in human MDA-MB-231 cells xenografted SCID mouse tumor at 10 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695661Tmax in human MDA-MB-231 cells xenografted SCID mouse tumor at 10 mg/kg, iv administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1239110Cytotoxicity against human insensitive HCT116 cells assessed as inhibition of cell growth after 72 hrs by Alamar Blue assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.
AID1659171Inhibition of N-terminal His-tagged Zika virus NS2B-NS3 protease (1 to 187 residues) using Boc-Gly-Arg-Arg-AMC as substrate2020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Inhibitors of the Zika virus protease NS2B-NS3.
AID1616480Binding affinity to N-terminal His-tagged human XIAP-BIR3 (253 to 347 residues) expressed in Escherichia coli BL21-Gold(DE3) pLysS assessed as change in melting temperature incubated for for 6 hrs at 37 degC by SYPRO orange dye based thermal shift assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695644AUC (0 to t) in human MDA-MB-231 cells xenografted SCID mouse plasma at 10 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1616495Induction of apoptosis in human A549 cells assessed as increase in caspase-3/7 activity at 2.5 uM incubated for 36 hrs in presence of 1 ng/mL TNFlpha by IncuCyteS3 caspase-3/7 fluorescence-based apoptosis assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695642Cmax in human MDA-MB-231 cells xenografted SCID mouse plasma at 10 mg/kg, iv administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1616492Induction of apoptosis in human SK-MEL-28 cells assessed as increase in caspase-3/7 activity at 2.5 uM incubated for 36 hrs by IncuCyteS3 caspase-3/7 fluorescence-based apoptosis assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695672Induction of cell death in human MDA-MB-231 cells incubated for 24 hrs by trypan blue exclusion assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695664Tmax in human MDA-MB-231 cells xenografted SCID mouse tumor at 10 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695470Induction of apoptosis in human MDA-MB-231 cells assessed as activation of caspase-3 activity at 1.5 uM after 12 hrs by Western blot analysis2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695647Half life in human MDA-MB-231 cells xenografted SCID mouse plasma at 10 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1239107Antagonist activity at cIAP1-BIR3 domain (unknown origin) assessed as inhibition of interaction with SMAC at 0.01 uM by fluorescence polarization assay relative to control2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.
AID695669Cmax in human MDA-MB-231 cells xenografted SCID mouse tumor at 100 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695662AUC (0 to t) in human MDA-MB-231 cells xenografted SCID mouse tumor at 10 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1616488Induction of cIAP1 degradation in human SK-MEL-28 cells assessed as reduction in cIAP1 protein level at 1 uM incubated for 3 hrs by Western blot analysis2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695658Oral bioavailability in human MDA-MB-231 cells xenografted SCID mouse plasma at 100 mg/kg administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695472Toxicity in human MCF12F cells assessed as induction of cell death at 10 uM after 48 hrs by trypan blue exclusion assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1616479Binding affinity to N-terminal His-tagged human XIAP-BIR3 (253 to 347 residues) expressed in Escherichia coli BL21-Gold(DE3) pLysS assessed as change in melting temperature incubated for for 2 hrs at room temperature by SYPRO orange dye based thermal shif2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695657Half life in human MDA-MB-231 cells xenografted SCID mouse plasma at 100 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695648Oral bioavailability in human MDA-MB-231 cells xenografted SCID mouse plasma at 10 mg/kg administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695468Growth inhibition of human SKOV3 cells after 4 days by WST8 assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695457Competitive inhibition of human cIAP2 BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1239108Cytotoxicity against human sensitive EVSA-T cells assessed as inhibition of cell growth after 72 hrs by Alamar Blue assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.
AID1616476Inhibition of N-terminal 6x-His-tagged recombinant human cIAP2-BIR3 (244 to 349 residues) expressed in Escherichia coli incubated for 2 hrs without 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695641AUC (0 to t) in human MDA-MB-231 cells xenografted SCID mouse plasma at 10 mg/kg, iv administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695643Half life in human MDA-MB-231 cells xenografted SCID mouse plasma at 10 mg/kg, iv administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695654AUC (0 to t) in human MDA-MB-231 cells xenografted SCID mouse plasma at 100 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1239105Antagonist activity at XIAP-BIR3 domain (unknown origin) assessed as inhibition of interaction with SMAC at 0.05 uM by fluorescence polarization assay relative to control2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.
AID1616477Inhibition of N-terminal His-tagged human XIAP-BIR3 (253 to 347 residues) expressed in Escherichia coli BL21-Gold(DE3) pLysS incubated for 2 hrs without 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695678Toxicity in dog assessed as drug tolerability2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1239111Antagonist activity at full-length FLAG-tagged XIAP (unknown origin) transfected in HEK293 cells assessed as inhibition of interaction with caspase 9 after 2 hrs by immunoprecipitation assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.
AID695469Induction of cell death in human MDA-MB-231 cells at 1 uM by trypan blue exclusion assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695471Induction of apoptosis in human MDA-MB-231 cells assessed as activation of PARP cleavage at 1.5 uM after 12 hrs by Western blot analysis2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1616487Covalent binding affinity to HA-BIR3 domain of XIAP (unknown origin) expressed in HEK293T cells assessed as increase in band intensity at 10 uM incubated for 6 hrs by Western blot analysis2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID1616478Inhibition of N-terminal His-tagged human XIAP-BIR3 (253 to 347 residues) expressed in Escherichia coli BL21-Gold(DE3) pLysS incubated for 2 hrs after 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695460Antagonist activity at human XIAP BIR3 domain assessed as restoration of caspase 9 activity using human MDA-MB-231 cells lysates using Z-LEHD-AFC by fluorescence assay based cell-free assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695649AUC (0 to t) in human MDA-MB-231 cells xenografted SCID mouse plasma at 30 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1616493Induction of apoptosis in human A549 cells assessed as increase in caspase-3/7 activity at 2.5 uM incubated for 36 hrs by IncuCyteS3 caspase-3/7 fluorescence-based apoptosis assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID1616483Inhibition of N-terminal 6x-His-tagged recombinant human cIAP2-BIR3 (244 to 349 residues) expressed in Escherichia coli incubated for 2 hrs after 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695660Cmax in human MDA-MB-231 cells xenografted SCID mouse tumor at 10 mg/kg, iv administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695652Half life in human MDA-MB-231 cells xenografted SCID mouse plasma at 30 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1616491Induction of cIAP2 degradation in human A549 cells assessed as reduction in cIAP2 protein level at 1 uM incubated for 3 hrs by Western blot analysis2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695666Cmax in human MDA-MB-231 cells xenografted SCID mouse tumor at 30 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695673Induction of cell death in human MDA-MB-231 cells at 1 uM incubated for 24 hrs by trypan blue exclusion assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1616486Stability in mouse plasma assessed as half life at 200 uM at 37 degC incubated up to 120 mins by mass spectrometry2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695679Aqueous solubility of the compound2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695674Antitumor activity against human MDA-MB-231 cells xenografted in SCID mouse assessed inhibition of tumor growth at 100 mg/kg, po administered daily for 5 days/week for 2 weeks measured on day 50 relative to untreated control2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1616482Inhibition of N-terminal 6x-His-tagged recombinant human cIAP1-BIR3 (258 to 363 residues) expressed in Escherichia coli incubated for 2 hrs after 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
AID695473Toxicity in in human prostate epithelial cells assessed as induction of cell death at 10 uM after 48 hrs by trypan blue exclusion assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695462Induction of degradation of cIAP1 in human MDA-MB-231 cells at 100 nM after 15 mins by Western blot analysis2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695656Tmax in human MDA-MB-231 cells xenografted SCID mouse plasma at 100 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695650Cmax in human MDA-MB-231 cells xenografted SCID mouse plasma at 30 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695667Tmax in human MDA-MB-231 cells xenografted SCID mouse tumor at 30 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695645Cmax in human MDA-MB-231 cells xenografted SCID mouse plasma at 10 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1239109Cytotoxicity against human sensitive MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by Alamar Blue assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.
AID695637Antitumor activity against human MDA-MB-231 cells xenografted in SCID mouse assessed inhibition of tumor growth at 30 mg/kg, po administered daily for 5 days/week for 2 weeks2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695461Induction of degradation of cIAP1 in human MDA-MB-231 cells at 10 nM by Western blot analysis2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695467Growth inhibition of human MDA-MB-231 cells after 4 days by WST8 assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695636Antitumor activity against human MDA-MB-231 cells xenografted in SCID mouse assessed inhibition of tumor growth at 10 mg/kg, po administered daily for 5 days/week for 2 weeks2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID695665AUC (0 to t) in human MDA-MB-231 cells xenografted SCID mouse tumor at 30 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1346238Human baculoviral IAP repeat containing 3 (Inhibitors of apoptosis (IAP) protein family)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1346249Human baculoviral IAP repeat containing 2 (Inhibitors of apoptosis (IAP) protein family)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
AID1346157Human X-linked inhibitor of apoptosis (Inhibitors of apoptosis (IAP) protein family)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (41.67)24.3611
2020's7 (58.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 24.89

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 Index24.89 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.54 (4.65)
Search Engine Demand Index25.99 (26.88)
Search Engine Supply Index2.57 (0.95)

This Compound (24.89)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (8.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (91.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]