Page last updated: 2024-12-08

zosuquidar trihydrochloride

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Cross-References

ID SourceID
PubMed CID153997
CHEMBL ID2074689
MeSH IDM0250672

Synonyms (56)

Synonym
zosuquidar (trihydrochloride)
HY-50671
rs-33295-198
nsc-725086
167465-36-3
zosuquidar trihydrochloride (usan)
D06387
(r)-4-((1ar,6r,10bs)-1,2-difluoro-1,1a,6,10b-tetrahydrodibenzo(a,e)cyclopropa(c)cycloheptan-6-yl)-alpha-((5-quinoloyloxy)methyl)-1-piperazineethanol trihydrochloride
zosuquidar hcl
nsc 725086
unii-813agy3126
813agy3126 ,
zosuquidar trihydrochloride [usan]
ly 335979
(r)-4-((1ar,6r,10bs)-1,2-difluoro-1,1a,6,10b-tetrahydrodibenzo(a,e)cyclopropa(c)cycloheptan-6-yl)-alpha-((5-quinoloyloxy)methyl)-1-piperazineethanol, trihydrochloride
1-piperazineethanol, 4-(1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo(a,e)cyclopropa(c)cycloheptan-6-yl)-alpha-1((5-quinolinyloxy)methyl-, trihydrochloride, (6(r)-(1alpha,6alpha,10balpha))-
LY335979 - ZOSUQUIDAR TRIHYDROCHLORIDE
CHEMBL2074689
CS-0275
S1481
(2r)-1-{4-[(1ar,6r,10bs)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]piperazin-1-yl}-3-(quinolin-5-yloxy)propan-2-ol trihydrochloride
(r)-4-[(1ar,6r,10bs)-1,2-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cycloheptan-6-yl]-alpha-[(5-quinoloyloxy)methyl]-1-piperazineethanol trihydrochloride
zosuquidar trihydrochloride [who-dd]
zosuquidar trihydrochloride [mi]
dtxcid2031451
dtxsid1057662 ,
tox21_113964
ly335979 trihydrochloride
cas-167465-36-3
J-500909
(2r)-1-{4-[(1ar,6r,10bs)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]piperazin-1-yl}-3-(quinolin-5-y loxy)propan-2-ol trihydrochloride
zosuquidar 3hcl
zosuquidar (ly335979) 3hcl
(?r)-4-[(1a?,6?,10b?)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-?-[(5-quinolinyloxy)methyl]-1-piperazineethanol trihydrochloride
AKOS025293500
AC-32884
(r)-1-(4-((1ar,6r,10bs)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c][7]annulen-6-yl)piperazin-1-yl)-3-(quinolin-5-yloxy)propan-2-ol trihydrochloride
ly335979 (zosuquidar 3hcl)
rs 33295-198 trihydrochloride
ly-335979 trihydrochloride
rs 33295-198 (d06387) 3hcl
mfcd00942300
SW219884-1
ly335979 (zosuquidar trihydrochloride)
EX-A2191
zosuquidar trihydrochloride; ly-335979 trihydrochloride
zosuquidr.3hcl (ly335979)
CCG-270305
Q27269191
V10115
(2r)-1-{4-[(1ar,6r,10bs)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]piperazin-1-yl-3-(quinolin-5-yloxy)propan-2-ol, 3hcl
(2r)-1-[4-[(2r,4s)-3,3-difluoro-11-tetracyclo[10.4.0.02,4.05,10]hexadeca-1(16),5,7,9,12,14-hexaenyl]piperazin-1-yl]-3-quinolin-5-yloxypropan-2-ol;trihydrochloride
A855894
zpfvqkpwgdrlhl-witooocmsa-n
zosuquidartrihydrochloride
(alphar)-4-[(1aalpha,6alpha,10balpha)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-alpha-[(5-quinolinyloxy)methyl]-1-piperazineethanol hydrochloride (1:3)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (19)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency30.10653.189029.884159.4836AID1224846
RAR-related orphan receptor gammaMus musculus (house mouse)Potency29.84930.006038.004119,952.5996AID1159523
GLI family zinc finger 3Homo sapiens (human)Potency15.55670.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency18.52170.000221.22318,912.5098AID1259243; AID1259247
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency16.78550.000657.913322,387.1992AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency3.34910.001022.650876.6163AID1224838
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency31.72090.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency9.80260.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency12.04810.001530.607315,848.9004AID1224841; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency23.41050.375827.485161.6524AID743217; AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency1.18830.005428.02631,258.9301AID1346982
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency33.48890.001024.504861.6448AID743215
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency7.49720.001019.414170.9645AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency33.48890.023723.228263.5986AID743222
thyroid stimulating hormone receptorHomo sapiens (human)Potency12.11560.001628.015177.1139AID1224843; AID1224895
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency26.832519.739145.978464.9432AID1159509
heat shock protein beta-1Homo sapiens (human)Potency29.84700.042027.378961.6448AID743210
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency33.48890.000627.21521,122.0200AID743202
[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)
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)2.30060.00022.318510.0000AID1530709; AID1530710; AID680133; AID680477; AID681144; AID681358
[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)
ATP-dependent translocase ABCB1Homo sapiens (human)Kd0.07300.07305.798110.0000AID680155
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (17)

Processvia Protein(s)Taxonomy
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID681144TP_TRANSPORTER: cell accumulation of calcein in L-MDR1 cells2003The Journal of pharmacology and experimental therapeutics, Apr, Volume: 305, Issue:1
Inhibition of P-glycoprotein by newer antidepressants.
AID680155TP_TRANSPORTER: binding in membrane vesicle from CEM/VLB100 cells1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities.
AID680802TP_TRANSPORTER: inhibition of LTC4 uptake (LTC4: 0.05 uM, LY335979: 10 uM) in membrane vesicles from MRP2-expressing MDCK cells1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities.
AID680133TP_TRANSPORTER: inhibition of Indinavir transepithelial transport (basal to apical) (Indinavir: 0.05 uM) in Caco-2 cells2000Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 28, Issue:6
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.
AID1530710Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 5 uM after 72 hrs by MTT assay (Rvb = 398.34 +/- 0.58 uM)2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents.
AID682086TP_TRANSPORTER: cell accumulation in CCRF-CEM and CEM/VLB100 cells1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities.
AID680901TP_TRANSPORTER: drug resistance (mitozantrone) in MDR1-expressing HL60/Vinc cells2003International journal of cancer, Jan-01, Volume: 103, Issue:1
Modulation of P-glycoprotein but not MRP1- or BCRP-mediated drug resistance by LY335979.
AID1530711Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold reduction in paclitaxel IC50 at 10 uM after 72 hrs by MTT assay relative to paclitaxel alone2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents.
AID679262TP_TRANSPORTER: transepithelial transport (basal to apical) in Caco-2 cells1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities.
AID680892TP_TRANSPORTER: drug resistance (vinorelbine) in MDR1-expressing HL60/Vinc cells2003International journal of cancer, Jan-01, Volume: 103, Issue:1
Modulation of P-glycoprotein but not MRP1- or BCRP-mediated drug resistance by LY335979.
AID1530709Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 398.34 +/- 0.58 uM)2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents.
AID1530712Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold reduction in paclitaxel IC50 at 5 uM after 72 hrs by MTT assay relative to paclitaxel alone2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents.
AID680803TP_TRANSPORTER: inhibition of Fluo-3 secretion into apical vacuoles (Fluo-3: 1 uM, LY335979: 10 uM) in Hep G2 cells2000American journal of physiology. Gastrointestinal and liver physiology, Apr, Volume: 278, Issue:4
MRP2, a human conjugate export pump, is present and transports fluo 3 into apical vacuoles of Hep G2 cells.
AID680477TP_TRANSPORTER: inhibition of Nelfinavir transepithelial transport (basal to apical) (Nelfinavir: 0.02 uM) in Caco-2 cells2000Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 28, Issue:6
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.
AID681358TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells2000Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 28, Issue:6
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (16.67)18.2507
2000's4 (66.67)29.6817
2010's1 (16.67)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 33.82

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 Index33.82 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.31 (4.65)
Search Engine Demand Index39.83 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (33.82)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]