Compounds > litronesib
Page last updated: 2024-10-14

litronesib

Description

litronesib: an Eg5 inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID25167017
CHEMBL ID2105661
SCHEMBL ID368284
MeSH IDM000598335

Synonyms (38)

Synonym
910634-41-2
D09636
litronesib (usan/inn)
(r)-n-{4-(2,2-dimethyl-propionyl)-5-((2-ethylamino-ethanesulfonylamino)-methyl)-5- phenyl-4,5-dihydro-(1,3,4)thiadiazol-2-yl}-2,2-dimethyl-propionamiden
ly 2523355
ly2523355
kf89617
(-)-n-{4-(2,2-dimethylpropanoyl)-5-(({(2-(ethylamino)ethyl)sulfonyl}amino)methyl)-5- phenyl-4,5-dihydro-1,3,4-thiadiazol-2-yl}-2,2-dimethylpropanamide
litronesib [usan:inn]
6611f8kycv ,
unii-6611f8kycv
litronesib
kf 89617
propanamide, n-(4-(2,2-dimethyl-1-oxopropyl)-5-((((2-(ethylamino)ethyl)sulfonyl) amino)methyl)-4,5-dihydro-5-phenyl-1,3,4-thiadiazol-2-yl)-2,2-dimethyl-, (-)-
propanamide, n-(4-(2,2-dimethyl-1-oxopropyl)-5-((((2-(ethylamino)ethyl)sulfonyl)amino)methyl)-4,5-dihydro-5-phenyl-1,3,4-thiadiazol-2-yl)-2,2-dimethyl-, (5r)-
(-)-n-(4-(2,2-dimethylpropanoyl)-5-((((2-(ethylamino)ethyl)sulfonyl)amino)methyl)-5- phenyl-4,5-dihydro-1,3,4-thiadiazol-2-yl)-2,2-dimethylpropanamide
litronesib [usan]
(r)-n-(4-(2,2-dimethyl-propionyl)-5-((2-ethylamino-ethanesulfonylamino)-methyl)-5- phenyl-4,5-dihydro-(1,3,4)thiadiazol-2-yl)-2,2-dimethyl-propionamide
litronesib [inn]
n-(4-(2,2-dimethylpropionyl)-(5r)-5-((2-ethylamino-ethanesulfonylamino)methyl)-5-phenyl-4,5-dihydro-(1,3,4)thiadiazol-2-yl)-2,2-dimethylpropionamide
litronesib [who-dd]
kf-89617
CHEMBL2105661
ly-2523355
CS-5194
HY-14846
SCHEMBL368284
AKOS030526983
DB11861
(r)-n-(5-((2-(ethylamino)ethylsulfonamido)methyl)-5-phenyl-4-pivaloyl-4,5-dihydro-1,3,4-thiadiazol-2-yl)pivalamide.
SB18860
nsc-789722
nsc789722
Q27263928
n-[(5r)-4-(2,2-dimethylpropanoyl)-5-[[2-(ethylamino)ethylsulfonylamino]methyl]-5-phenyl-1,3,4-thiadiazol-2-yl]-2,2-dimethylpropanamide
F85314
MS-29500
bdbm50463316
[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)0.01650.00011.405710.0000AID1398519; AID1406289
[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 (3)

Assay IDTitleYearJournalArticle
AID1398519Inhibition EG5 (unknown origin)2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design and synthesis of novel thiadiazole-thiazolone hybrids as potential inhibitors of the human mitotic kinesin Eg5.
AID1406289Inhibition of microtubule-stimulated human Eg5 ATPase activity2018European journal of medicinal chemistry, Aug-05, Volume: 156Crystal structure of the Eg5 - K858 complex and implications for structure-based design of thiadiazole-containing inhibitors.
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.
[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's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (83.33)24.3611
2020's1 (16.67)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 (16.67%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
aziridine
[no description available]		2.110azacycloalkane;
aziridines;
saturated organic heteromonocyclic parent		alkylating agent
k 858
K 858: an Eg5 inhibitor and antineoplastic agent; structure in first source		2.5820benzenes
arry 520
filanesib: a kinesin spindle protein inhibitor		2.5820
ConditionIndicatedRelationship StrengthStudiesTrials
Leukocytopenia
[description not available]		04.411
Benign Neoplasms
[description not available]		04.8121
Colorectal Cancer
[description not available]		04.411
Chemotherapy-Induced Febrile Neutropenia
FEVER accompanied by a significant reduction in NEUTROPHIL count associated with CHEMOTHERAPY.		04.411
Leukopenia
A decrease in the number of LEUKOCYTES in a blood sample below the normal range (LEUKOCYTE COUNT less than 4000).		04.411
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		18.3542
Colorectal Neoplasms
Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.		16.411