Compounds > birt 377
Page last updated: 2024-12-11

birt 377

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

Cross-References

ID SourceID
PubMed CID9803375
CHEMBL ID367808
SCHEMBL ID5203590
MeSH IDM0350986

Synonyms (17)

Synonym
(r)-5-(4-bromo-benzyl)-3-(3,5-dichloro-phenyl)-1,5-dimethyl-imidazolidine-2,4-dione
(r)-5-(4-bromobenzyl)-3-(3,5-dichlorophenyl)-1,5-dimethylimidazolidine-2,4-dione
bdbm50154496
CHEMBL367808 ,
SCHEMBL5203590
birt-377
213211-10-0
AKOS025142021
birt 377
(5r)-5-[(4-bromophenyl)methyl]-3-(3,5-dichlorophenyl)-1,5-dimethyl-2,4-imidazolidinedione
(5r)-5-[(4-bromophenyl)methyl]-3-(3,5-dichlorophenyl)-1,5-dimethylimidazolidine-2,4-dione
gtpl9720
NCGC00387192-01
birt377
MS-27955
HY-110117
CS-0032969

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" In this paper we report the discovery and characterization of (R)-5-(4-bromobenzyl)-3-(3, 5-dichlorophenyl)-1,5-dimethylimidazolidine-2,4-dione (BIRT 377), an orally bioavailable small molecule that interacts specifically with LFA-1 via noncovalent binding to the CD11a chain and prevents LFA-1 from binding to its ligand, ICAM-1."( Cutting edge: a small molecule antagonist of LFA-1-mediated cell adhesion.
Bormann, BJ; Jeanfavre, DD; Kelly, TA; Kishimoto, KM; Mainolfi, EA; McNeil, DW; Nabozny, GH; Reilly, PL; Rothlein, R; Woska, JR; Zinter, R, 1999)		0.5
"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

Dosage Studied

ExcerptRelevanceReference
" Exploiting these observations, we have designed and validated an assay that allows us to measure receptor occupancy in vitro on monkey and human peripheral blood leukocytes and ex vivo in whole blood from monkeys dosed with small molecule LFA-1 antagonists."( Small molecule LFA-1 antagonists compete with an anti-LFA-1 monoclonal antibody for binding to the CD11a I domain: development of a flow-cytometry-based receptor occupancy assay.
Caviness, GO; Fogal, SE; Giblin, PA; Jeanfavre, DD; Kelly, TA; Kishimoto, TK; Kroe, RR; Last-Barney, K; Mainolfi, EA; Panzenbeck, MJ; Reilly, PL; Rothlein, R; Woska, JR, 2003)		0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.68370.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency3.37860.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency16.93300.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency3.37860.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency3.37860.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency3.37860.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency3.37860.01238.964839.8107AID1645842
[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)
Integrin beta-2Homo sapiens (human)IC50 (µMol)0.02600.00080.59053.7800AID248906
Intercellular adhesion molecule 1Homo sapiens (human)IC50 (µMol)0.02600.00301.212210.0000AID248906
Integrin alpha-LHomo sapiens (human)IC50 (µMol)0.02600.00080.60203.7800AID248906
[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)
Integrin beta-2Homo sapiens (human)Kd0.02000.02000.02000.0200AID238155
Intercellular adhesion molecule 1Homo sapiens (human)Kd0.02000.02000.02000.0200AID238155
Integrin alpha-LHomo sapiens (human)Kd0.02000.02000.02000.0200AID238155
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (96)

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)
microglial cell activationIntegrin beta-2Homo sapiens (human)
receptor-mediated endocytosisIntegrin beta-2Homo sapiens (human)
phagocytosis, engulfmentIntegrin beta-2Homo sapiens (human)
apoptotic processIntegrin beta-2Homo sapiens (human)
inflammatory responseIntegrin beta-2Homo sapiens (human)
cell adhesionIntegrin beta-2Homo sapiens (human)
leukocyte cell-cell adhesionIntegrin beta-2Homo sapiens (human)
cell-matrix adhesionIntegrin beta-2Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-2Homo sapiens (human)
cell-cell signalingIntegrin beta-2Homo sapiens (human)
regulation of cell shapeIntegrin beta-2Homo sapiens (human)
neutrophil chemotaxisIntegrin beta-2Homo sapiens (human)
receptor internalizationIntegrin beta-2Homo sapiens (human)
positive regulation of superoxide anion generationIntegrin beta-2Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-2Homo sapiens (human)
endodermal cell differentiationIntegrin beta-2Homo sapiens (human)
receptor clusteringIntegrin beta-2Homo sapiens (human)
positive regulation of neutrophil degranulationIntegrin beta-2Homo sapiens (human)
negative regulation of dopamine metabolic processIntegrin beta-2Homo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationIntegrin beta-2Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulusIntegrin beta-2Homo sapiens (human)
positive regulation of protein targeting to membraneIntegrin beta-2Homo sapiens (human)
amyloid-beta clearanceIntegrin beta-2Homo sapiens (human)
cell-cell adhesionIntegrin beta-2Homo sapiens (human)
cell-cell adhesion via plasma-membrane adhesion moleculesIntegrin beta-2Homo sapiens (human)
positive regulation of leukocyte adhesion to vascular endothelial cellIntegrin beta-2Homo sapiens (human)
neutrophil migrationIntegrin beta-2Homo sapiens (human)
positive regulation of prostaglandin-E synthase activityIntegrin beta-2Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-2Homo sapiens (human)
regulation of leukocyte mediated cytotoxicityIntercellular adhesion molecule 1Homo sapiens (human)
T cell activation via T cell receptor contact with antigen bound to MHC molecule on antigen presenting cellIntercellular adhesion molecule 1Homo sapiens (human)
T cell antigen processing and presentationIntercellular adhesion molecule 1Homo sapiens (human)
positive regulation of cellular extravasationIntercellular adhesion molecule 1Homo sapiens (human)
cell adhesionIntercellular adhesion molecule 1Homo sapiens (human)
heterophilic cell-cell adhesion via plasma membrane cell adhesion moleculesIntercellular adhesion molecule 1Homo sapiens (human)
leukocyte cell-cell adhesionIntercellular adhesion molecule 1Homo sapiens (human)
membrane to membrane dockingIntercellular adhesion molecule 1Homo sapiens (human)
cell adhesion mediated by integrinIntercellular adhesion molecule 1Homo sapiens (human)
adhesion of symbiont to hostIntercellular adhesion molecule 1Homo sapiens (human)
symbiont entry into host cellIntercellular adhesion molecule 1Homo sapiens (human)
receptor-mediated virion attachment to host cellIntercellular adhesion molecule 1Homo sapiens (human)
leukocyte migrationIntercellular adhesion molecule 1Homo sapiens (human)
establishment of endothelial barrierIntercellular adhesion molecule 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntercellular adhesion molecule 1Homo sapiens (human)
cellular response to glucose stimulusIntercellular adhesion molecule 1Homo sapiens (human)
T cell extravasationIntercellular adhesion molecule 1Homo sapiens (human)
regulation of ruffle assemblyIntercellular adhesion molecule 1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway via death domain receptorsIntercellular adhesion molecule 1Homo sapiens (human)
cellular response to amyloid-betaIntercellular adhesion molecule 1Homo sapiens (human)
cellular response to leukemia inhibitory factorIntercellular adhesion molecule 1Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntercellular adhesion molecule 1Homo sapiens (human)
T cell activation via T cell receptor contact with antigen bound to MHC molecule on antigen presenting cellIntegrin alpha-LHomo sapiens (human)
phagocytosisIntegrin alpha-LHomo sapiens (human)
inflammatory responseIntegrin alpha-LHomo sapiens (human)
cell adhesionIntegrin alpha-LHomo sapiens (human)
heterophilic cell-cell adhesion via plasma membrane cell adhesion moleculesIntegrin alpha-LHomo sapiens (human)
leukocyte cell-cell adhesionIntegrin alpha-LHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-LHomo sapiens (human)
signal transductionIntegrin alpha-LHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-LHomo sapiens (human)
memory T cell extravasationIntegrin alpha-LHomo sapiens (human)
receptor clusteringIntegrin alpha-LHomo sapiens (human)
cell-cell adhesionIntegrin alpha-LHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-LHomo 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 (30)

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)
cargo receptor activityIntegrin beta-2Homo sapiens (human)
amyloid-beta bindingIntegrin beta-2Homo sapiens (human)
complement component C3b bindingIntegrin beta-2Homo sapiens (human)
integrin bindingIntegrin beta-2Homo sapiens (human)
protein bindingIntegrin beta-2Homo sapiens (human)
protein kinase bindingIntegrin beta-2Homo sapiens (human)
ICAM-3 receptor activityIntegrin beta-2Homo sapiens (human)
heat shock protein bindingIntegrin beta-2Homo sapiens (human)
metal ion bindingIntegrin beta-2Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-2Homo sapiens (human)
virus receptor activityIntercellular adhesion molecule 1Homo sapiens (human)
transmembrane signaling receptor activityIntercellular adhesion molecule 1Homo sapiens (human)
integrin bindingIntercellular adhesion molecule 1Homo sapiens (human)
protein bindingIntercellular adhesion molecule 1Homo sapiens (human)
signaling receptor activityIntercellular adhesion molecule 1Homo sapiens (human)
protein bindingIntegrin alpha-LHomo sapiens (human)
ICAM-3 receptor activityIntegrin alpha-LHomo sapiens (human)
metal ion bindingIntegrin alpha-LHomo sapiens (human)
cell adhesion molecule bindingIntegrin alpha-LHomo sapiens (human)
integrin bindingIntegrin alpha-LHomo 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 (36)

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)
plasma membraneIntegrin beta-2Homo sapiens (human)
external side of plasma membraneIntegrin beta-2Homo sapiens (human)
cell surfaceIntegrin beta-2Homo sapiens (human)
membraneIntegrin beta-2Homo sapiens (human)
integrin alphaL-beta2 complexIntegrin beta-2Homo sapiens (human)
integrin alphaM-beta2 complexIntegrin beta-2Homo sapiens (human)
integrin alphaX-beta2 complexIntegrin beta-2Homo sapiens (human)
specific granule membraneIntegrin beta-2Homo sapiens (human)
plasma membrane raftIntegrin beta-2Homo sapiens (human)
extracellular exosomeIntegrin beta-2Homo sapiens (human)
tertiary granule membraneIntegrin beta-2Homo sapiens (human)
ficolin-1-rich granule membraneIntegrin beta-2Homo sapiens (human)
extracellular vesicleIntegrin beta-2Homo sapiens (human)
integrin complexIntegrin beta-2Homo sapiens (human)
receptor complexIntegrin beta-2Homo sapiens (human)
focal adhesionIntegrin beta-2Homo sapiens (human)
cell surfaceIntegrin beta-2Homo sapiens (human)
immunological synapseIntercellular adhesion molecule 1Homo sapiens (human)
extracellular spaceIntercellular adhesion molecule 1Homo sapiens (human)
plasma membraneIntercellular adhesion molecule 1Homo sapiens (human)
focal adhesionIntercellular adhesion molecule 1Homo sapiens (human)
external side of plasma membraneIntercellular adhesion molecule 1Homo sapiens (human)
cell surfaceIntercellular adhesion molecule 1Homo sapiens (human)
membraneIntercellular adhesion molecule 1Homo sapiens (human)
membrane raftIntercellular adhesion molecule 1Homo sapiens (human)
collagen-containing extracellular matrixIntercellular adhesion molecule 1Homo sapiens (human)
extracellular exosomeIntercellular adhesion molecule 1Homo sapiens (human)
plasma membraneIntercellular adhesion molecule 1Homo sapiens (human)
plasma membraneIntegrin alpha-LHomo sapiens (human)
cell surfaceIntegrin alpha-LHomo sapiens (human)
membraneIntegrin alpha-LHomo sapiens (human)
integrin alphaL-beta2 complexIntegrin alpha-LHomo sapiens (human)
specific granule membraneIntegrin alpha-LHomo sapiens (human)
extracellular exosomeIntegrin alpha-LHomo sapiens (human)
integrin complexIntegrin alpha-LHomo sapiens (human)
external side of plasma membraneIntegrin alpha-LHomo 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 (10)

Assay IDTitleYearJournalArticle
AID247522Concentration required to inhibit aggregation of JY cells2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives.
AID243308Concentration required for irreversible binding to human liver microsomes2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives.
AID238155Dissociation constant for human Lymphocyte function associated antigen 1 in LFA-1/ICAM-1 binding assay2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives.
AID299141Antagonist activity at LFA1 assessed as inhibition of LFA1/ICAM interaction by HeLa/HSB assay2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Design of LFA-1 antagonists based on a 2,3-dihydro-1H-pyrrolizin-5(7aH)-one scaffold.
AID248906Inhibitory concentration against leukocyte function-associated antigen-1 in HSB-2 human lymphoblast and H1HeLa cell adhesion assay2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
De novo design, synthesis, and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (24)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (4.17)18.2507
2000's17 (70.83)29.6817
2010's4 (16.67)24.3611
2020's2 (8.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 24.37

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index24.37 (24.57)
Research Supply Index3.22 (2.92)
Research Growth Index5.22 (4.65)
Search Engine Demand Index17.79 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (24.37)

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%
Other24 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
isoflurane
Isoflurane: A stable, non-explosive inhalation anesthetic, relatively free from significant side effects.		2.1510organofluorine compoundinhalation anaesthetic
sevoflurane
Sevoflurane: A non-explosive inhalation anesthetic used in the induction and maintenance of general anesthesia. It does not cause respiratory irritation and may also prevent PLATELET AGGREGATION.. sevoflurane : An ether compound having fluoromethyl and 1,1,1,3,3,3-hexafluoroisopropyl as the two alkyl groups.		2.1510ether;
organofluorine compound		central nervous system depressant;
inhalation anaesthetic;
platelet aggregation inhibitor
alanine
Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.		210alanine zwitterion;
alanine;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid		EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor;
fundamental metabolite
hydantoins
Hydantoins: Compounds based on imidazolidine dione. Some derivatives are ANTICONVULSANTS.. imidazolidine-2,4-dione : An imidazolidinone with oxo groups at position 2 and 4.		2.4420imidazolidine-2,4-dione
dithiothreitol
1,4-dimercaptobutane-2,3-diol : A glycol that is butane-2,3-diol in which a hydrogen from each of the methyl groups is replaced by a thiol group.. 1,4-dithiothreitol : The threo-diastereomer of 1,4-dimercaptobutane-2,3-diol.		2.02101,4-dimercaptobutane-2,3-diol;
butanediols;
dithiol;
glycol;
thiol		chelator;
human metabolite;
reducing agent
lutetium
Lutetium: An element of the rare earth family of metals. It has the atomic symbol Lu, atomic number 71, and atomic weight 175.		2.0310d-block element atom;
lanthanoid atom
manganese
Manganese: A trace element with atomic symbol Mn, atomic number 25, and atomic weight 54.94. It is concentrated in cell mitochondria, mostly in the pituitary gland, liver, pancreas, kidney, and bone, influences the synthesis of mucopolysaccharides, stimulates hepatic synthesis of cholesterol and fatty acids, and is a cofactor in many enzymes, including arginase and alkaline phosphatase in the liver. (From AMA Drug Evaluations Annual 1992, p2035). manganese(4+) : A manganese cation that is monoatomic and has a formal charge of +4.		2.0210elemental manganese;
manganese group element atom		Escherichia coli metabolite;
micronutrient
aziridine-2-carboxylic acid
aziridine-2-carboxylic acid: structure given in first source		2.0210
imidazolidines
[no description available]		4.28180azacycloalkane;
imidazolidines;
saturated organic heteromonocyclic parent
muramidase
Muramidase: A basic enzyme that is present in saliva, tears, egg white, and many animal fluids. It functions as an antibacterial agent. The enzyme catalyzes the hydrolysis of 1,4-beta-linkages between N-acetylmuramic acid and N-acetyl-D-glucosamine residues in peptidoglycan and between N-acetyl-D-glucosamine residues in chitodextrin. EC 3.2.1.17.		2.0510
ConditionIndicatedRelationship StrengthStudiesTrials
Innate Inflammatory Response
[description not available]		02.4220
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.4220
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.4620
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Infectious Myelitis
[description not available]		02.2110
Nerve Pain
[description not available]		02.2110
Delayed Effects, Prenatal Exposure
[description not available]		02.2110
Neuralgia
Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.		02.2110
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		02.2110
Kahler Disease
[description not available]		02.0110
Multiple Myeloma
A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.		02.0110
Leucocythaemia
[description not available]		02.0310
Germinoblastoma
[description not available]		02.0310
Leukemia
A progressive, malignant disease of the blood-forming organs, characterized by distorted proliferation and development of leukocytes and their precursors in the blood and bone marrow. Leukemias were originally termed acute or chronic based on life expectancy but now are classified according to cellular maturity. Acute leukemias consist of predominately immature cells; chronic leukemias are composed of more mature cells. (From The Merck Manual, 2006)		02.0310
Lymphoma
A general term for various neoplastic diseases of the lymphoid tissue.		02.0310
Delayed Hypersensitivity
[description not available]		0210