Page last updated: 2024-11-13

emd 534085

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

Description

EMD 534085: a kinesin-5 inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23634407
CHEMBL ID1077204
SCHEMBL ID369891
MeSH IDM0562126

Synonyms (29)

Synonym
1-(2-(dimethylamino)ethyl)-3-(((2r,4as,5r,10bs)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2h-pyrano[3,2-c]quinolin-2-yl)methyl)urea
1-[2-(dimethylamino)ethyl]-3-{[(2r,4as,5r,10bs)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2h-pyrano[3,2-c]quinolin-2-yl]methyl}urea
bdbm50313428
CHEMBL1077204 ,
emd-534085
emd 534085
emd534085
858668-07-2
BCP9000643
BCP0726000144
1035647-06-3
(-)-emd-534085
1-(2-(dimethylamino)ethyl)-3-(((2r,4as,5r,10bs)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2h-pyrano(3,2-c)quinolin-2-yl)methyl)urea
urea, n-(2-(dimethylamino)ethyl)-n'-(((2r,4as,5r,10bs)-3,4,4a,5,6,10b-hexahydro-5-phenyl-9-(trifluoromethyl)-2h-pyrano(3,2-c)quinolin-2-yl)methyl)-
al67qx8036 ,
unii-al67qx8036
DTXSID90235147
SCHEMBL369891
1-[[(2r,4as,5r,10bs)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2h-pyrano[3,2-c]quinolin-2-yl]methyl]-3-[2-(dimethylamino)ethyl]urea
mariuidcpuzlkz-fukqbsrtsa-n
CS-6279
HY-15000
EX-A2369
nsc763564
nsc-763564
Q27273980
F85521
MS-28841
AC-35806
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Kinesin-like protein KIF11Homo sapiens (human)IC50 (µMol)0.00800.00011.405710.0000AID466475
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (9)

Processvia Protein(s)Taxonomy
mitotic cell cycleKinesin-like protein KIF11Homo sapiens (human)
microtubule-based movementKinesin-like protein KIF11Homo sapiens (human)
spindle organizationKinesin-like protein KIF11Homo sapiens (human)
mitotic spindle organizationKinesin-like protein KIF11Homo sapiens (human)
mitotic centrosome separationKinesin-like protein KIF11Homo sapiens (human)
regulation of mitotic centrosome separationKinesin-like protein KIF11Homo sapiens (human)
cell divisionKinesin-like protein KIF11Homo sapiens (human)
mitotic spindle assemblyKinesin-like protein KIF11Homo sapiens (human)
spindle elongationKinesin-like protein KIF11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
microtubule motor activityKinesin-like protein KIF11Homo sapiens (human)
protein bindingKinesin-like protein KIF11Homo sapiens (human)
ATP bindingKinesin-like protein KIF11Homo sapiens (human)
microtubule bindingKinesin-like protein KIF11Homo sapiens (human)
protein kinase bindingKinesin-like protein KIF11Homo sapiens (human)
plus-end-directed microtubule motor activityKinesin-like protein KIF11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
spindle poleKinesin-like protein KIF11Homo sapiens (human)
spindle microtubuleKinesin-like protein KIF11Homo sapiens (human)
spindleKinesin-like protein KIF11Homo sapiens (human)
cytosolKinesin-like protein KIF11Homo sapiens (human)
microtubuleKinesin-like protein KIF11Homo sapiens (human)
membraneKinesin-like protein KIF11Homo sapiens (human)
mitotic spindleKinesin-like protein KIF11Homo sapiens (human)
kinesin complexKinesin-like protein KIF11Homo sapiens (human)
protein-containing complexKinesin-like protein KIF11Homo sapiens (human)
nucleusKinesin-like protein KIF11Homo sapiens (human)
mitotic spindleKinesin-like protein KIF11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (27)

Assay IDTitleYearJournalArticle
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID466494Inhibition of human KHC at 10 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466492Inhibition of human MCAK at 1 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466477Antitumor activity against human COLO205 cells xenografted in mouse assessed as tumor growth inhibition at 15 mg/kg, ip administered twice weekly relative to control2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466490Inhibition of human KIFC3 at 1 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466478Antitumor activity against human COLO205 cells xenografted in mouse assessed as tumor growth inhibition at 30 mg/kg, ip administered twice weekly relative to control2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466487Inhibition of human chromokinesin at 1 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466499Inhibition of human chromokinesin at 10 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466481Clearance in mouse2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466486Inhibition of human CENPE at 1 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466476Antiproliferative activity against human HCT116 cells after 48 hrs by crystal violet staining assay2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466484Bioavailability in mouse at >10 mg/kg2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466489Inhibition of human KIF3C at 1 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466496Inhibition of human KIFC3 at 10 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466483Half life in mouse2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466479Toxicity in mouse assessed as body weight loss at 15 mg/kg, ip administered twice weekly2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466498Inhibition of human CENPE at 10 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466485Inhibition of BimC at 1 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466480Toxicity in mouse assessed as body weight loss at 30 mg/kg, ip administered twice weekly2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466482Volume of distribution in mouse2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466493Inhibition of BimC at 10 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466488Inhibition of human KHC at 1 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466491Inhibition of human MKLP1 at 1 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466500Inhibition of human MKLP1 at 10 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466495Inhibition of human KIF3C at 10 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466475Inhibition of ATPase activity of human recombinant EG5 assessed as ATP hydrolysis by pyruvate kinase-lactate dehydrogenase coupled assay2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
AID466497Inhibition of human MCAK at 10 uM2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (80.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 13.13

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index13.13 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index5.08 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (13.13)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (20.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]