Page last updated: 2024-11-13

snx 2112

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

Description

SNX 2112: an orally available small molecule Hsp90 inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID24772860
CHEMBL ID561224
CHEMBL ID560895
SCHEMBL ID1219380
SCHEMBL ID1221195
SCHEMBL ID1219382
SCHEMBL ID12685879
SCHEMBL ID22667486
MeSH IDM0529257

Synonyms (65)

Synonym
HY-10214
HIE ,
4-[6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1h-indazol-1-yl]-2-[(cis-4-hydroxycyclohexyl)amino]benzamide
snx-2112 ,
pf-04928473
CHEMBL561224 ,
CHEMBL560895 ,
BRD-K71281111-001-01-9
FT-0660383
snx 2112
945626-71-1
snx2112
4-[6,6-dimethyl-4-oxo-3-(trifluoromethyl)-5,7-dihydroindazol-1-yl]-2-[(4-hydroxycyclohexyl)amino]benzamide
BCP0726000309
NCGC00346633-01
unii-10c9p3ffow
10c9p3ffow ,
benzamide, 2-((trans-4-hydroxycyclohexyl)amino)-4-(4,5,6,7-tetrahydro-6,6-dimethyl-4-oxo-3-(trifluoromethyl)-1h-indazol-1-yl)-
CS-0481
S2639
908112-43-6
4-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1h-indazol-1-yl)-2-(((1r,4r)-4-hydroxycyclohexyl)amino)benzamide
4-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1h-indazol-1-yl)-2-((1r,4r)-4-hydroxycyclohexylamino)benzamide
MLS006011082
smr004702870
4-[6,6-dimethyl-4-oxidanylidene-3-(trifluoromethyl)-5,7-dihydroindazol-1-yl]-2-[(4-oxidanylcyclohexyl)amino]benzamide
pf 04928473
e0g ,
SCHEMBL1219380
SCHEMBL1221195
SCHEMBL1219382
SCHEMBL12685879
4NH7
J-513608
AKOS027270068
HMS3656P07
4-(6,6-dimethyl-4-oxo-3-trifluoromethyl-4,5,6,7-tetrahydro-indazol-1-yl)-2-(trans-4-hydroxy-cyclohexylamino)-benzamide
4-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1h-indazol-1-yl)-2-(trans-4-hydroxycyclohexylamino)benzamide
AS-75100
4-[6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1h-indazol-1-yl]-2-[(4-hydroxycyclohexyl)amino]benzamide
bdbm50480401
NCGC00386182-02
snx-2112 (pf-04928473)
SW219742-1
bdbm50450704
AKOS032947229
mfcd16038907
snx-2112; pf-04928473
EX-A2375
pf-4928473
BCP02907
AMY24162
SB19446
SCHEMBL22667486
CCG-269392
C77089
4-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1h-indazol-1-yl)-2-((trans-4-hydroxycyclohexyl)amino)benzamide
Q27461098
Q27251134
zfvrynyopqzkdg-xbxgtlagsa-n
pf 04928473; pf-04928473; pf04928473;4-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1h-indazol-1-yl)-2-(((1r,4r)-4-hydroxycyclohexyl)amino)benzamide;4-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1h-indazol-1-yl)-2-(((1r,4r)-4-
A903360
DTXSID601025695
AC-36048
Z2235801955

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" This method was successfully applied to pharmacokinetic studies in rats after intravenous administration of SNX-2112."( Determination of SNX-2112, a selective Hsp90 inhibitor, in plasma samples by high-performance liquid chromatography and its application to pharmacokinetics in rats.
Gong, GQ; Jiang, JH; Li, YC; Liu, QY; Liu, Z; Luo, Y; Wang, QD; Wang, YF; Xia, M; Xing, GW; Zhai, QQ, 2010
)
0.36
" In the study reported here, we aimed to develop a nanocrystal formulation for SNX-2112 and to determine the pharmacokinetic behaviors of the prepared nanocrystals."( Elucidating the in vivo fate of nanocrystals using a physiologically based pharmacokinetic model: a case study with the anticancer agent SNX-2112.
Dong, D; Wang, H; Wang, X; Wang, Y; Wu, B; Zhang, X, 2015
)
0.42
" Physiologically based pharmacokinetic (PBPK) modeling was undertaken to evaluate the drug's disposition in rats following administration of drug cosolvent or nanocrystals."( Elucidating the in vivo fate of nanocrystals using a physiologically based pharmacokinetic model: a case study with the anticancer agent SNX-2112.
Dong, D; Wang, H; Wang, X; Wang, Y; Wu, B; Zhang, X, 2015
)
0.42
" The results reveal that the nanocrystals rapidly released drug molecules in vivo, accounting for their cosolvent-like pharmacokinetic behaviors."( Elucidating the in vivo fate of nanocrystals using a physiologically based pharmacokinetic model: a case study with the anticancer agent SNX-2112.
Dong, D; Wang, H; Wang, X; Wang, Y; Wu, B; Zhang, X, 2015
)
0.42

Compound-Compound Interactions

ExcerptReferenceRelevance
" In cellular models of wild-type or mutant EGFR (L858R and T790M mutations), SNX-2112 alone and in combination with erlotinib inhibited EGF activation of pAKT(473) and pSTAT3(705)."( Targeting of multiple signaling pathways by the Hsp90 inhibitor SNX-2112 in EGFR resistance models as a single agent or in combination with erlotinib.
Barabasz, A; Fadden, P; Foley, B; Hall, S; Huang, K; Rice, JW; Scott, A; Steed, P; Veal, JM, 2009
)
0.35

Bioavailability

ExcerptReferenceRelevance
" 4-[6,6-Dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]-2-[(trans-4-hydroxycyclohexyl)amino]benzamide (SNX-2112, 9) was identified as highly selective and potent (IC(50) Her2 = 11 nM, HT-29 = 3 nM); its prodrug amino-acetic acid 4-[2-carbamoyl-5-(6,6-dimethyl-4-oxo-3-trifluoromethyl-4,5,6,7-tetrahydro-indazol-1-yl)-phenylamino]-cyclohexyl ester methanesulfonate (SNX-5422, 10) was orally bioavailable and efficacious in a broad range of xenograft tumor models (e."( Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
Barabasz, AF; Barta, TE; DuBois, LG; Eaves, J; Fadden, RP; Foley, BE; Freed, T; Geng, L; Hall, SE; Hanson, GJ; Hinkley, L; Hu, M; Huang, KH; Hughes, PF; Jenks, M; Lewis, M; Ma, W; Markworth, CJ; McCall, WS; Ommen, AJ; Otto, J; Partridge, JM; Pronk, B; Rice, JW; Scott, A; Silinski, MA; Smith, ED; Steed, PM; Strachan, JP; Veal, JM; Verleysen, K; Woodward, AR, 2009
)
0.35
" We report on a novel small molecule inhibitor of Hsp90, SNX-2112, and an orally bioavailable prodrug analog, SNX-5422."( Targeting of multiple signaling pathways by the Hsp90 inhibitor SNX-2112 in EGFR resistance models as a single agent or in combination with erlotinib.
Barabasz, A; Fadden, P; Foley, B; Hall, S; Huang, K; Rice, JW; Scott, A; Steed, P; Veal, JM, 2009
)
0.35
" SNX-5542, an orally bioavailable prodrug of SNX-2112, displayed significant antitumor efficacy in vivo in nude mice bearing MET-amplified tumor xenografts."( Antitumor activity of SNX-2112, a synthetic heat shock protein-90 inhibitor, in MET-amplified tumor cells with or without resistance to selective MET Inhibition.
Bachleitner-Hofmann, T; Chen, CT; Christensen, JG; Liska, D; Mittlboeck, M; Olshen, AB; Rosen, N; Solit, DB; Sun, MY; Viale, A; Weiser, MR; Zeng, Z, 2011
)
0.37
" The promising anticancer agent SNX-2112 (a novel Hsp90 inhibitor) is poorly bioavailable after oral administration."( P-glycoprotein (P-gp)-mediated efflux limits intestinal absorption of the Hsp90 inhibitor SNX-2112 in rats.
Liu, H; Sun, H; Wu, B; Wu, Z; Zhang, X, 2014
)
0.4
"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 (17)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency23.48500.00308.794948.0869AID1347053
PPM1D proteinHomo sapiens (human)Potency0.04660.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency8.48660.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency0.10460.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
GVesicular stomatitis virusPotency6.00810.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency21.31740.00108.379861.1304AID1645840
polyproteinZika virusPotency23.48500.00308.794948.0869AID1347053
Interferon betaHomo sapiens (human)Potency1.53700.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency6.00810.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency6.00810.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency6.00810.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Corticotropin releasing hormone receptor 2Sus scrofa (pig)IC50 (µMol)0.00200.00200.00670.0140AID421314
Heat shock protein HSP 90-alphaHomo sapiens (human)IC50 (µMol)28.67960.00040.695010.0000AID1363696; AID1708083; AID421300; AID421314; AID421315; AID421316; AID716071; AID767754
Heat shock protein HSP 90-alphaHomo sapiens (human)Ki0.00400.00020.54152.7000AID1063127
Heat shock protein HSP 90-betaHomo sapiens (human)IC50 (µMol)25.81360.00100.683610.0000AID1363696; AID1708082; AID421300; AID421314; AID421315; AID421316; AID465281; AID465283; AID767753
Heat shock protein HSP 90-betaHomo sapiens (human)Ki0.00330.00010.03730.5300AID1063124; AID465289; AID465293
EndoplasminHomo sapiens (human)Ki0.48400.00401.32057.0000AID1063123
EndoplasminCanis lupus familiaris (dog)IC50 (µMol)0.53100.01000.14820.5780AID1708084; AID767752
Heat shock protein 75 kDa, mitochondrialHomo sapiens (human)IC50 (µMol)0.75850.03770.49511.5860AID1708085; AID767751
Heat shock protein 75 kDa, mitochondrialHomo sapiens (human)Ki0.79100.01600.28100.7910AID1063122
[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)
Heat shock protein HSP 90-alphaHomo sapiens (human)EC50 (µMol)0.01900.00400.13311.2000AID716076
Heat shock protein HSP 90-alphaHomo sapiens (human)Kd0.00240.00030.94889.8000AID1604479; AID780857
Heat shock protein HSP 90-betaHomo sapiens (human)Kd0.00070.00031.33309.8000AID780857
EndoplasminHomo sapiens (human)Kd0.48400.20001.93908.6000AID1604480
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (112)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
telomere maintenance via telomeraseHeat shock protein HSP 90-alphaHomo sapiens (human)
neuron migrationHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein phosphorylationHeat shock protein HSP 90-alphaHomo sapiens (human)
activation of innate immune responseHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of defense response to virus by hostHeat shock protein HSP 90-alphaHomo sapiens (human)
skeletal muscle contractionHeat shock protein HSP 90-alphaHomo sapiens (human)
mitochondrial transportHeat shock protein HSP 90-alphaHomo sapiens (human)
response to unfolded proteinHeat shock protein HSP 90-alphaHomo sapiens (human)
response to heatHeat shock protein HSP 90-alphaHomo sapiens (human)
response to coldHeat shock protein HSP 90-alphaHomo sapiens (human)
response to xenobiotic stimulusHeat shock protein HSP 90-alphaHomo sapiens (human)
response to salt stressHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of lamellipodium assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
cardiac muscle cell apoptotic processHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of protein ubiquitinationHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein polymerizationHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of interferon-beta productionHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of protein localizationHeat shock protein HSP 90-alphaHomo sapiens (human)
protein refoldingHeat shock protein HSP 90-alphaHomo sapiens (human)
response to cocaineHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein import into nucleusHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of apoptotic processHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of protein-containing complex assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
protein unfoldingHeat shock protein HSP 90-alphaHomo sapiens (human)
response to estrogenHeat shock protein HSP 90-alphaHomo sapiens (human)
protein insertion into mitochondrial outer membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of nitric oxide biosynthetic processHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein catabolic processHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of cell sizeHeat shock protein HSP 90-alphaHomo sapiens (human)
response to antibioticHeat shock protein HSP 90-alphaHomo sapiens (human)
protein stabilizationHeat shock protein HSP 90-alphaHomo sapiens (human)
chaperone-mediated protein complex assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of cardiac muscle contractionHeat shock protein HSP 90-alphaHomo sapiens (human)
chaperone-mediated autophagyHeat shock protein HSP 90-alphaHomo sapiens (human)
cellular response to virusHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of postsynaptic membrane neurotransmitter receptor levelsHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of tau-protein kinase activityHeat shock protein HSP 90-alphaHomo sapiens (human)
telomerase holoenzyme complex assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
cellular response to heatHeat shock protein HSP 90-alphaHomo sapiens (human)
protein foldingHeat shock protein HSP 90-alphaHomo sapiens (human)
telomere maintenance via telomeraseHeat shock protein HSP 90-betaHomo sapiens (human)
placenta developmentHeat shock protein HSP 90-betaHomo sapiens (human)
response to unfolded proteinHeat shock protein HSP 90-betaHomo sapiens (human)
virion attachment to host cellHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of transforming growth factor beta receptor signaling pathwayHeat shock protein HSP 90-betaHomo sapiens (human)
regulation of protein ubiquitinationHeat shock protein HSP 90-betaHomo sapiens (human)
negative regulation of proteasomal ubiquitin-dependent protein catabolic processHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activityHeat shock protein HSP 90-betaHomo sapiens (human)
regulation of protein localizationHeat shock protein HSP 90-betaHomo sapiens (human)
negative regulation of apoptotic processHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of nitric oxide biosynthetic processHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of cell differentiationHeat shock protein HSP 90-betaHomo sapiens (human)
chaperone-mediated protein complex assemblyHeat shock protein HSP 90-betaHomo sapiens (human)
regulation of cell cycleHeat shock protein HSP 90-betaHomo sapiens (human)
chaperone-mediated protein foldingHeat shock protein HSP 90-betaHomo sapiens (human)
cellular response to interleukin-4Heat shock protein HSP 90-betaHomo sapiens (human)
supramolecular fiber organizationHeat shock protein HSP 90-betaHomo sapiens (human)
negative regulation of proteasomal protein catabolic processHeat shock protein HSP 90-betaHomo sapiens (human)
telomerase holoenzyme complex assemblyHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of protein localization to cell surfaceHeat shock protein HSP 90-betaHomo sapiens (human)
cellular response to heatHeat shock protein HSP 90-betaHomo sapiens (human)
protein foldingHeat shock protein HSP 90-betaHomo sapiens (human)
protein stabilizationHeat shock protein HSP 90-betaHomo sapiens (human)
actin rod assemblyEndoplasminHomo sapiens (human)
regulation of phosphoprotein phosphatase activityEndoplasminHomo sapiens (human)
cellular response to ATPEndoplasminHomo sapiens (human)
response to hypoxiaEndoplasminHomo sapiens (human)
protein transportEndoplasminHomo sapiens (human)
retrograde protein transport, ER to cytosolEndoplasminHomo sapiens (human)
protein folding in endoplasmic reticulumEndoplasminHomo sapiens (human)
response to endoplasmic reticulum stressEndoplasminHomo sapiens (human)
ERAD pathwayEndoplasminHomo sapiens (human)
negative regulation of apoptotic processEndoplasminHomo sapiens (human)
sequestering of calcium ionEndoplasminHomo sapiens (human)
cellular response to manganese ionEndoplasminHomo sapiens (human)
protein foldingEndoplasminHomo sapiens (human)
ERAD pathwayEndoplasminCanis lupus familiaris (dog)
translational attenuationHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
chaperone-mediated protein foldingHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
negative regulation of cellular respirationHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
negative regulation of reactive oxygen species biosynthetic processHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to hydrogen peroxideHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
protein foldingHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (59)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
UTP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
CTP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
RNA bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
mRNA bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ATP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
GTP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ATP hydrolysis activityHeat shock protein HSP 90-alphaHomo sapiens (human)
sulfonylurea receptor bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
protein phosphatase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
MHC class II protein complex bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
nitric-oxide synthase regulator activityHeat shock protein HSP 90-alphaHomo sapiens (human)
TPR domain bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ubiquitin protein ligase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
dATP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
identical protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
protein homodimerization activityHeat shock protein HSP 90-alphaHomo sapiens (human)
histone deacetylase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
transmembrane transporter bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
tau protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
GTPase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
Rho GDP-dissociation inhibitor bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
DNA polymerase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
scaffold protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
disordered domain specific bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ATP-dependent protein folding chaperoneHeat shock protein HSP 90-alphaHomo sapiens (human)
protein tyrosine kinase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
unfolded protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
RNA bindingHeat shock protein HSP 90-betaHomo sapiens (human)
double-stranded RNA bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP hydrolysis activityHeat shock protein HSP 90-betaHomo sapiens (human)
protein kinase regulator activityHeat shock protein HSP 90-betaHomo sapiens (human)
kinase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein kinase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
MHC class II protein complex bindingHeat shock protein HSP 90-betaHomo sapiens (human)
nitric-oxide synthase regulator activityHeat shock protein HSP 90-betaHomo sapiens (human)
TPR domain bindingHeat shock protein HSP 90-betaHomo sapiens (human)
heat shock protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ubiquitin protein ligase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
peptide bindingHeat shock protein HSP 90-betaHomo sapiens (human)
identical protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein homodimerization activityHeat shock protein HSP 90-betaHomo sapiens (human)
histone deacetylase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP-dependent protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein folding chaperoneHeat shock protein HSP 90-betaHomo sapiens (human)
cadherin bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein dimerization activityHeat shock protein HSP 90-betaHomo sapiens (human)
tau protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
DNA polymerase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
disordered domain specific bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP-dependent protein folding chaperoneHeat shock protein HSP 90-betaHomo sapiens (human)
receptor ligand inhibitor activityHeat shock protein HSP 90-betaHomo sapiens (human)
histone methyltransferase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
unfolded protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
RNA bindingEndoplasminHomo sapiens (human)
calcium ion bindingEndoplasminHomo sapiens (human)
protein bindingEndoplasminHomo sapiens (human)
ATP bindingEndoplasminHomo sapiens (human)
ATP hydrolysis activityEndoplasminHomo sapiens (human)
protein phosphatase bindingEndoplasminHomo sapiens (human)
low-density lipoprotein particle receptor bindingEndoplasminHomo sapiens (human)
ATP-dependent protein folding chaperoneEndoplasminHomo sapiens (human)
unfolded protein bindingEndoplasminHomo sapiens (human)
ATP bindingEndoplasminCanis lupus familiaris (dog)
ATP hydrolysis activityEndoplasminCanis lupus familiaris (dog)
ATP-dependent protein folding chaperoneEndoplasminCanis lupus familiaris (dog)
RNA bindingHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
tumor necrosis factor receptor bindingHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
protein bindingHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
ATP bindingHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
ATP hydrolysis activityHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
protein kinase bindingHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
ATP-dependent protein folding chaperoneHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
unfolded protein bindingHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (56)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular regionHeat shock protein HSP 90-alphaHomo sapiens (human)
nucleusHeat shock protein HSP 90-alphaHomo sapiens (human)
nucleoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
cytoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
mitochondrionHeat shock protein HSP 90-alphaHomo sapiens (human)
cytosolHeat shock protein HSP 90-alphaHomo sapiens (human)
plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
cell surfaceHeat shock protein HSP 90-alphaHomo sapiens (human)
membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
basolateral plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
apical plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
brush border membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
secretory granule lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
melanosomeHeat shock protein HSP 90-alphaHomo sapiens (human)
neuronal cell bodyHeat shock protein HSP 90-alphaHomo sapiens (human)
lysosomal lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
dendritic growth coneHeat shock protein HSP 90-alphaHomo sapiens (human)
axonal growth coneHeat shock protein HSP 90-alphaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
collagen-containing extracellular matrixHeat shock protein HSP 90-alphaHomo sapiens (human)
extracellular exosomeHeat shock protein HSP 90-alphaHomo sapiens (human)
endocytic vesicle lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
sperm mitochondrial sheathHeat shock protein HSP 90-alphaHomo sapiens (human)
sperm plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
ficolin-1-rich granule lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
protein-containing complexHeat shock protein HSP 90-alphaHomo sapiens (human)
plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
neuronal cell bodyHeat shock protein HSP 90-alphaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
myelin sheathHeat shock protein HSP 90-alphaHomo sapiens (human)
cytosolHeat shock protein HSP 90-alphaHomo sapiens (human)
nucleusHeat shock protein HSP 90-alphaHomo sapiens (human)
COP9 signalosomeHeat shock protein HSP 90-betaHomo sapiens (human)
protein folding chaperone complexHeat shock protein HSP 90-betaHomo sapiens (human)
extracellular regionHeat shock protein HSP 90-betaHomo sapiens (human)
nucleusHeat shock protein HSP 90-betaHomo sapiens (human)
nucleoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
cytoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
mitochondrionHeat shock protein HSP 90-betaHomo sapiens (human)
cytosolHeat shock protein HSP 90-betaHomo sapiens (human)
cell surfaceHeat shock protein HSP 90-betaHomo sapiens (human)
membraneHeat shock protein HSP 90-betaHomo sapiens (human)
secretory granule lumenHeat shock protein HSP 90-betaHomo sapiens (human)
melanosomeHeat shock protein HSP 90-betaHomo sapiens (human)
neuronal cell bodyHeat shock protein HSP 90-betaHomo sapiens (human)
dendritic growth coneHeat shock protein HSP 90-betaHomo sapiens (human)
axonal growth coneHeat shock protein HSP 90-betaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
extracellular exosomeHeat shock protein HSP 90-betaHomo sapiens (human)
dynein axonemal particleHeat shock protein HSP 90-betaHomo sapiens (human)
ficolin-1-rich granule lumenHeat shock protein HSP 90-betaHomo sapiens (human)
protein-containing complexHeat shock protein HSP 90-betaHomo sapiens (human)
aryl hydrocarbon receptor complexHeat shock protein HSP 90-betaHomo sapiens (human)
HSP90-CDC37 chaperone complexHeat shock protein HSP 90-betaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
plasma membraneHeat shock protein HSP 90-betaHomo sapiens (human)
cytosolHeat shock protein HSP 90-betaHomo sapiens (human)
extracellular regionEndoplasminHomo sapiens (human)
nucleusEndoplasminHomo sapiens (human)
endoplasmic reticulumEndoplasminHomo sapiens (human)
endoplasmic reticulum lumenEndoplasminHomo sapiens (human)
endoplasmic reticulum membraneEndoplasminHomo sapiens (human)
smooth endoplasmic reticulumEndoplasminHomo sapiens (human)
cytosolEndoplasminHomo sapiens (human)
focal adhesionEndoplasminHomo sapiens (human)
membraneEndoplasminHomo sapiens (human)
midbodyEndoplasminHomo sapiens (human)
sarcoplasmic reticulum lumenEndoplasminHomo sapiens (human)
melanosomeEndoplasminHomo sapiens (human)
perinuclear region of cytoplasmEndoplasminHomo sapiens (human)
collagen-containing extracellular matrixEndoplasminHomo sapiens (human)
extracellular exosomeEndoplasminHomo sapiens (human)
endocytic vesicle lumenEndoplasminHomo sapiens (human)
sperm plasma membraneEndoplasminHomo sapiens (human)
protein-containing complexEndoplasminHomo sapiens (human)
endoplasmic reticulum chaperone complexEndoplasminHomo sapiens (human)
endoplasmic reticulumEndoplasminHomo sapiens (human)
perinuclear region of cytoplasmEndoplasminHomo sapiens (human)
sarcoplasmic reticulum lumenEndoplasminCanis lupus familiaris (dog)
melanosomeEndoplasminCanis lupus familiaris (dog)
nucleoplasmHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
mitochondrionHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
mitochondrial inner membraneHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
mitochondrial intermembrane spaceHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
mitochondrial matrixHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
membraneHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
cell peripheryHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
mitochondrial inner membraneHeat shock protein 75 kDa, mitochondrialHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (133)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS 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.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS 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.
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.
AID1347415qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: tertiary screen by RT-qPCR2020ACS 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.
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.
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.
AID421316Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID697737Cytotoxicity against african green monkey Vero cells assessed as inhibition of cell viability after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Anti-herpes simplex virus efficacies of 2-aminobenzamide derivatives as novel HSP90 inhibitors.
AID716064Intrinsic clearance in human liver microsomes2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID1363694Inhibition of FITC-geldanamycin binding to dog GST-tagged GRP94 N41 deletion mutant (69 to 337 residues) expressed in Escherichia coli BL21star (DE3) after 4 hrs by GM-FITC-based FP assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis.
AID421319Solubility of the compound2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID697736Antiviral activity against HSV1 strain F ATCC VR733 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Anti-herpes simplex virus efficacies of 2-aminobenzamide derivatives as novel HSP90 inhibitors.
AID697722Antiviral activity against HSV1 infected herpes simplex keratitis New zealand rabbit model assessed as reduction in viral DNA level in corneal sample compound administered twice daily as gel 24 hrs post inoculation measured on day 9 post infection by RT-P2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Anti-herpes simplex virus efficacies of 2-aminobenzamide derivatives as novel HSP90 inhibitors.
AID1491574Antileishmanial activity against Leishmania donovani axenic amastigotes infected in mouse J774 cells after 72 hrs by Draq5 staining based assay2017ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
Synthesis and Activity of a New Series of Antileishmanial Agents.
AID421306Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID465293Binding affinity to HSP90 under non-reducing conditions in absence of TECP2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Heat shock protein 90: inhibitors in clinical trials.
AID697732Antiviral activity against HSV2 strain 333 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect at 4 uM after 48 hrs by plaque reduction assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Anti-herpes simplex virus efficacies of 2-aminobenzamide derivatives as novel HSP90 inhibitors.
AID1708084Inhibition of FITC-GDA binding to dog GRP94 incubated for 2 hrs by fluorescence polarization assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
The Development of Hsp90β-Selective Inhibitors to Overcome Detriments Associated with
AID716069Fraction unbound at mouse plasma2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID716066Intrinsic clearance in mouse liver microsomes2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID421309Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID716065Intrinsic clearance in rat liver microsomes2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID1708085Inhibition of FITC-GDA binding to human TRAP1 incubated for 2 hrs by fluorescence polarization assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
The Development of Hsp90β-Selective Inhibitors to Overcome Detriments Associated with
AID421312Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID421300Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID716068Fraction unbound at rat plasma2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID465289Binding affinity to HSP90 under reducing conditions in presence of TECP2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Heat shock protein 90: inhibitors in clinical trials.
AID780857Displacement of FITC-Geldanamycin from Hsp90 (unknown origin) after 18 hrs by fluorescence polarization assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).
AID1708083Inhibition of FITC-GDA binding to human HSP90-alpha incubated for 2 hrs by fluorescence polarization assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
The Development of Hsp90β-Selective Inhibitors to Overcome Detriments Associated with
AID421308Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID465362Half life in plasma of mouse bearing human MM1S cells at 50 mg/kg2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Heat shock protein 90: inhibitors in clinical trials.
AID421299Oral bioavailability in mouse2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID1491576Inhibition of human Hsp90 by fluorescence polarization analysis2017ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
Synthesis and Activity of a New Series of Antileishmanial Agents.
AID697735Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Anti-herpes simplex virus efficacies of 2-aminobenzamide derivatives as novel HSP90 inhibitors.
AID697727Antiviral activity against HSV1 infected herpes simplex keratitis New zealand rabbit model at 0.025% to 0.1% administered twice daily as gel 24 hrs post inoculation measured on day 9 post infection2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Anti-herpes simplex virus efficacies of 2-aminobenzamide derivatives as novel HSP90 inhibitors.
AID1063122Binding affinity to human recombinant TRAP1 after 3 hrs by fluorescence polarization assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases.
AID697733Antiviral activity against HSV1 strain F ATCC VR733 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect at 4 uM after 48 hrs by plaque reduction assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Anti-herpes simplex virus efficacies of 2-aminobenzamide derivatives as novel HSP90 inhibitors.
AID421314Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID697723Antiviral activity against HSV1 infected herpes simplex keratitis New zealand rabbit model assessed as reduction in viral DNA level in corneal sample at 0.025% to 0.1% administered twice daily as gel 24 hrs post inoculation measured on day 9 post infectio2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Anti-herpes simplex virus efficacies of 2-aminobenzamide derivatives as novel HSP90 inhibitors.
AID421315Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID421318Metabolic stability in human liver S9 fraction assessed as drug remaining at 1 uM after 1 hr2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID1491573Antileishmanial activity against Leishmania donovani axenic amastigotes after 72 hrs by CellTiter reagent based assay2017ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
Synthesis and Activity of a New Series of Antileishmanial Agents.
AID1604479Displacement of FITC-geldanamycin from HSP90alpha (unknown origin) after 5 hrs by fluorescence polarization assay2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions.
AID421304Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID421303Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID716071Inhibition of Hsp90alpha2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID697728Selectivity index, ratio of CC50 for african green monkey Vero cells to EC50 for HSV2 strain 333 infected in african green monkey Vero cells2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Anti-herpes simplex virus efficacies of 2-aminobenzamide derivatives as novel HSP90 inhibitors.
AID767754Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from HSP90alpha (unknown origin) after 24 hrs by fluorescence polarization assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.
AID767751Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from recombinant human Trap-1 after 24 hrs by fluorescence polarization assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.
AID716070Efflux ratio of apparent permeability from basolateral to apical side to apical to basolateral side of human Caco2 cells2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID716052Half life in CD-1 mouse at 25 mg/kg, po2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID421302Binding affinity to pig spleen Hsp90 ATPase pocket by Bradford assay2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID421307Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID697729Selectivity index, ratio of CC50 for african green monkey Vero cells to EC50 for HSV1 strain F ATCC VR733 infected in african green monkey Vero cells2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Anti-herpes simplex virus efficacies of 2-aminobenzamide derivatives as novel HSP90 inhibitors.
AID1063124Binding affinity to human N-terminal polyHis-tagged HSP90beta (D9 to E236) expressed in insect sf9 cells after 3 hrs by fluorescence polarization assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases.
AID697734Antiviral activity against HSV2 strain 333 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Anti-herpes simplex virus efficacies of 2-aminobenzamide derivatives as novel HSP90 inhibitors.
AID716061Tmax in CD-1 mouse at 25 mg/kg, po2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID421317Metabolic stability in human liver microsomes at 1 uM after 1 hr2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID1363696Inhibition of FITC-geldanamycin binding to human His-tagged HSP90alpha N-terminal domain (1 to 236 residues) expressed in Escherichia coli BL21star (DE3) after 4 hrs by FP assay relative to control2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis.
AID465281Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Heat shock protein 90: inhibitors in clinical trials.
AID1708082Inhibition of FITC-GDA binding to human HSP90-beta incubated for 2 hrs by fluorescence polarization assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
The Development of Hsp90β-Selective Inhibitors to Overcome Detriments Associated with
AID716077Apparent permeability from apical to basolateral side of human Caco2 cells2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID1604480Displacement of FITC-geldanamycin from GRP94 (unknown origin) after 5 hrs by fluorescence polarization assay2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions.
AID1491575Cytotoxicity against mouse J774.A1 cells after 72 hrs by MTS assay2017ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
Synthesis and Activity of a New Series of Antileishmanial Agents.
AID767752Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from dog Grp94 after 24 hrs by fluorescence polarization assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.
AID716076Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-22012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID716078Initial Cmax in CD-1 mouse at 25 mg/kg, po2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID1063123Binding affinity to human N-terminal polyHis-tagged GRP94 (L69 to N337) expressed in Escherichia coli BL21(DE3) after 3 hrs by fluorescence polarization assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases.
AID465363Half life in tumor of mouse bearing human MM1S cells at 50 mg/kg2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Heat shock protein 90: inhibitors in clinical trials.
AID1063127Binding affinity to human N-terminal polyHis-tagged HSP90alpha (D9 to E236) alpha-helix conformation expressed in insect sf9 cells after 3 hrs by fluorescence polarization assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases.
AID421313Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID767753Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from recombinant HSP90beta (unknown origin) after 24 hrs by fluorescence polarization assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.
AID1363693Inhibition of FITC-geldanamycin binding to dog GST-tagged GRP94 N41 deletion mutant (69 to 337 residues) expressed in Escherichia coli BL21star (DE3) at 100 uM after 4 hrs by FP assay relative to control2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis.
AID421311Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID716067Fraction unbound at human plasma2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID421310Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID716058AUC in CD-1 mouse at 25 mg/kg, po2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID421320Aqueous solubility in phosphate-buffered saline at pH 7.42009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID465283Inhibition of HSP90-mediated client protein HER2 degradation2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Heat shock protein 90: inhibitors in clinical trials.
AID1170902Increase in oxygen consumption rate/extracellular acidification rate ratio in human NCI-H1299 cells at incubated for 12 hrs2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of 4,5-diarylisoxazoles as potent dual inhibitors of pyruvate dehydrogenase kinase and heat shock protein 90.
AID697724Antiviral activity against HSV1 infected herpes simplex keratitis New zealand rabbit model assessed as reduction in corneal epithelia involvement score at 0.025% to 0.1% administered twice daily as gel 24 hrs post inoculation measured on day 9 post infect2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Anti-herpes simplex virus efficacies of 2-aminobenzamide derivatives as novel HSP90 inhibitors.
AID716055Dose normalized AUC in CD-1 mouse at 25 mg/kg, po2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
EC144 is a potent inhibitor of the heat shock protein 90.
AID421305Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (58)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (6.90)29.6817
2010's44 (75.86)24.3611
2020's10 (17.24)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (1.72%)5.53%
Reviews1 (1.72%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other56 (96.55%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]