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 Source	ID
PubMed CID	9803375
CHEMBL ID	367808
SCHEMBL ID	5203590
MeSH ID	M0350986

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

Excerpt	Reference	Relevance
" 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

Excerpt	Relevance	Reference
" 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

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	2.6837	0.0123	7.9835	43.2770	AID1645841
G	Vesicular stomatitis virus	Potency	3.3786	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2D6	Homo sapiens (human)	Potency	16.9330	0.0010	8.3798	61.1304	AID1645840
Interferon beta	Homo sapiens (human)	Potency	3.3786	0.0033	9.1582	39.8107	AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	3.3786	0.0123	8.9648	39.8107	AID1645842
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	3.3786	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	3.3786	0.0123	8.9648	39.8107	AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Integrin beta-2	Homo sapiens (human)	IC50 (µMol)	0.0260	0.0008	0.5905	3.7800	AID248906
Intercellular adhesion molecule 1	Homo sapiens (human)	IC50 (µMol)	0.0260	0.0030	1.2122	10.0000	AID248906
Integrin alpha-L	Homo sapiens (human)	IC50 (µMol)	0.0260	0.0008	0.6020	3.7800	AID248906
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Integrin beta-2	Homo sapiens (human)	Kd	0.0200	0.0200	0.0200	0.0200	AID238155
Intercellular adhesion molecule 1	Homo sapiens (human)	Kd	0.0200	0.0200	0.0200	0.0200	AID238155
Integrin alpha-L	Homo sapiens (human)	Kd	0.0200	0.0200	0.0200	0.0200	AID238155
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (96)

Process	via Protein(s)	Taxonomy
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA 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-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
microglial cell activation	Integrin beta-2	Homo sapiens (human)
receptor-mediated endocytosis	Integrin beta-2	Homo sapiens (human)
phagocytosis, engulfment	Integrin beta-2	Homo sapiens (human)
apoptotic process	Integrin beta-2	Homo sapiens (human)
inflammatory response	Integrin beta-2	Homo sapiens (human)
cell adhesion	Integrin beta-2	Homo sapiens (human)
leukocyte cell-cell adhesion	Integrin beta-2	Homo sapiens (human)
cell-matrix adhesion	Integrin beta-2	Homo sapiens (human)
integrin-mediated signaling pathway	Integrin beta-2	Homo sapiens (human)
cell-cell signaling	Integrin beta-2	Homo sapiens (human)
regulation of cell shape	Integrin beta-2	Homo sapiens (human)
neutrophil chemotaxis	Integrin beta-2	Homo sapiens (human)
receptor internalization	Integrin beta-2	Homo sapiens (human)
positive regulation of superoxide anion generation	Integrin beta-2	Homo sapiens (human)
heterotypic cell-cell adhesion	Integrin beta-2	Homo sapiens (human)
endodermal cell differentiation	Integrin beta-2	Homo sapiens (human)
receptor clustering	Integrin beta-2	Homo sapiens (human)
positive regulation of neutrophil degranulation	Integrin beta-2	Homo sapiens (human)
negative regulation of dopamine metabolic process	Integrin beta-2	Homo sapiens (human)
regulation of peptidyl-tyrosine phosphorylation	Integrin beta-2	Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulus	Integrin beta-2	Homo sapiens (human)
positive regulation of protein targeting to membrane	Integrin beta-2	Homo sapiens (human)
amyloid-beta clearance	Integrin beta-2	Homo sapiens (human)
cell-cell adhesion	Integrin beta-2	Homo sapiens (human)
cell-cell adhesion via plasma-membrane adhesion molecules	Integrin beta-2	Homo sapiens (human)
positive regulation of leukocyte adhesion to vascular endothelial cell	Integrin beta-2	Homo sapiens (human)
neutrophil migration	Integrin beta-2	Homo sapiens (human)
positive regulation of prostaglandin-E synthase activity	Integrin beta-2	Homo sapiens (human)
cell adhesion mediated by integrin	Integrin beta-2	Homo sapiens (human)
regulation of leukocyte mediated cytotoxicity	Intercellular adhesion molecule 1	Homo sapiens (human)
T cell activation via T cell receptor contact with antigen bound to MHC molecule on antigen presenting cell	Intercellular adhesion molecule 1	Homo sapiens (human)
T cell antigen processing and presentation	Intercellular adhesion molecule 1	Homo sapiens (human)
positive regulation of cellular extravasation	Intercellular adhesion molecule 1	Homo sapiens (human)
cell adhesion	Intercellular adhesion molecule 1	Homo sapiens (human)
heterophilic cell-cell adhesion via plasma membrane cell adhesion molecules	Intercellular adhesion molecule 1	Homo sapiens (human)
leukocyte cell-cell adhesion	Intercellular adhesion molecule 1	Homo sapiens (human)
membrane to membrane docking	Intercellular adhesion molecule 1	Homo sapiens (human)
cell adhesion mediated by integrin	Intercellular adhesion molecule 1	Homo sapiens (human)
adhesion of symbiont to host	Intercellular adhesion molecule 1	Homo sapiens (human)
symbiont entry into host cell	Intercellular adhesion molecule 1	Homo sapiens (human)
receptor-mediated virion attachment to host cell	Intercellular adhesion molecule 1	Homo sapiens (human)
leukocyte migration	Intercellular adhesion molecule 1	Homo sapiens (human)
establishment of endothelial barrier	Intercellular adhesion molecule 1	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Intercellular adhesion molecule 1	Homo sapiens (human)
cellular response to glucose stimulus	Intercellular adhesion molecule 1	Homo sapiens (human)
T cell extravasation	Intercellular adhesion molecule 1	Homo sapiens (human)
regulation of ruffle assembly	Intercellular adhesion molecule 1	Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway via death domain receptors	Intercellular adhesion molecule 1	Homo sapiens (human)
cellular response to amyloid-beta	Intercellular adhesion molecule 1	Homo sapiens (human)
cellular response to leukemia inhibitory factor	Intercellular adhesion molecule 1	Homo sapiens (human)
negative regulation of endothelial cell apoptotic process	Intercellular adhesion molecule 1	Homo sapiens (human)
T cell activation via T cell receptor contact with antigen bound to MHC molecule on antigen presenting cell	Integrin alpha-L	Homo sapiens (human)
phagocytosis	Integrin alpha-L	Homo sapiens (human)
inflammatory response	Integrin alpha-L	Homo sapiens (human)
cell adhesion	Integrin alpha-L	Homo sapiens (human)
heterophilic cell-cell adhesion via plasma membrane cell adhesion molecules	Integrin alpha-L	Homo sapiens (human)
leukocyte cell-cell adhesion	Integrin alpha-L	Homo sapiens (human)
cell-matrix adhesion	Integrin alpha-L	Homo sapiens (human)
signal transduction	Integrin alpha-L	Homo sapiens (human)
integrin-mediated signaling pathway	Integrin alpha-L	Homo sapiens (human)
memory T cell extravasation	Integrin alpha-L	Homo sapiens (human)
receptor clustering	Integrin alpha-L	Homo sapiens (human)
cell-cell adhesion	Integrin alpha-L	Homo sapiens (human)
cell adhesion mediated by integrin	Integrin alpha-L	Homo sapiens (human)
inositol phosphate metabolic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of cold-induced thermogenesis	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (30)

Process	via Protein(s)	Taxonomy
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cargo receptor activity	Integrin beta-2	Homo sapiens (human)
amyloid-beta binding	Integrin beta-2	Homo sapiens (human)
complement component C3b binding	Integrin beta-2	Homo sapiens (human)
integrin binding	Integrin beta-2	Homo sapiens (human)
protein binding	Integrin beta-2	Homo sapiens (human)
protein kinase binding	Integrin beta-2	Homo sapiens (human)
ICAM-3 receptor activity	Integrin beta-2	Homo sapiens (human)
heat shock protein binding	Integrin beta-2	Homo sapiens (human)
metal ion binding	Integrin beta-2	Homo sapiens (human)
cell adhesion molecule binding	Integrin beta-2	Homo sapiens (human)
virus receptor activity	Intercellular adhesion molecule 1	Homo sapiens (human)
transmembrane signaling receptor activity	Intercellular adhesion molecule 1	Homo sapiens (human)
integrin binding	Intercellular adhesion molecule 1	Homo sapiens (human)
protein binding	Intercellular adhesion molecule 1	Homo sapiens (human)
signaling receptor activity	Intercellular adhesion molecule 1	Homo sapiens (human)
protein binding	Integrin alpha-L	Homo sapiens (human)
ICAM-3 receptor activity	Integrin alpha-L	Homo sapiens (human)
metal ion binding	Integrin alpha-L	Homo sapiens (human)
cell adhesion molecule binding	Integrin alpha-L	Homo sapiens (human)
integrin binding	Integrin alpha-L	Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (36)

Process	via Protein(s)	Taxonomy
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	Integrin beta-2	Homo sapiens (human)
external side of plasma membrane	Integrin beta-2	Homo sapiens (human)
cell surface	Integrin beta-2	Homo sapiens (human)
membrane	Integrin beta-2	Homo sapiens (human)
integrin alphaL-beta2 complex	Integrin beta-2	Homo sapiens (human)
integrin alphaM-beta2 complex	Integrin beta-2	Homo sapiens (human)
integrin alphaX-beta2 complex	Integrin beta-2	Homo sapiens (human)
specific granule membrane	Integrin beta-2	Homo sapiens (human)
plasma membrane raft	Integrin beta-2	Homo sapiens (human)
extracellular exosome	Integrin beta-2	Homo sapiens (human)
tertiary granule membrane	Integrin beta-2	Homo sapiens (human)
ficolin-1-rich granule membrane	Integrin beta-2	Homo sapiens (human)
extracellular vesicle	Integrin beta-2	Homo sapiens (human)
integrin complex	Integrin beta-2	Homo sapiens (human)
receptor complex	Integrin beta-2	Homo sapiens (human)
focal adhesion	Integrin beta-2	Homo sapiens (human)
cell surface	Integrin beta-2	Homo sapiens (human)
immunological synapse	Intercellular adhesion molecule 1	Homo sapiens (human)
extracellular space	Intercellular adhesion molecule 1	Homo sapiens (human)
plasma membrane	Intercellular adhesion molecule 1	Homo sapiens (human)
focal adhesion	Intercellular adhesion molecule 1	Homo sapiens (human)
external side of plasma membrane	Intercellular adhesion molecule 1	Homo sapiens (human)
cell surface	Intercellular adhesion molecule 1	Homo sapiens (human)
membrane	Intercellular adhesion molecule 1	Homo sapiens (human)
membrane raft	Intercellular adhesion molecule 1	Homo sapiens (human)
collagen-containing extracellular matrix	Intercellular adhesion molecule 1	Homo sapiens (human)
extracellular exosome	Intercellular adhesion molecule 1	Homo sapiens (human)
plasma membrane	Intercellular adhesion molecule 1	Homo sapiens (human)
plasma membrane	Integrin alpha-L	Homo sapiens (human)
cell surface	Integrin alpha-L	Homo sapiens (human)
membrane	Integrin alpha-L	Homo sapiens (human)
integrin alphaL-beta2 complex	Integrin alpha-L	Homo sapiens (human)
specific granule membrane	Integrin alpha-L	Homo sapiens (human)
extracellular exosome	Integrin alpha-L	Homo sapiens (human)
integrin complex	Integrin alpha-L	Homo sapiens (human)
external side of plasma membrane	Integrin alpha-L	Homo sapiens (human)
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (10)

Assay ID	Title	Year	Journal	Article
AID247522	Concentration required to inhibit aggregation of JY cells	2004	Journal 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.
AID243308	Concentration required for irreversible binding to human liver microsomes	2004	Journal 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.
AID238155	Dissociation constant for human Lymphocyte function associated antigen 1 in LFA-1/ICAM-1 binding assay	2004	Journal 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.
AID299141	Antagonist activity at LFA1 assessed as inhibition of LFA1/ICAM interaction by HeLa/HSB assay	2007	Bioorganic & 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.
AID248906	Inhibitory concentration against leukocyte function-associated antigen-1 in HSB-2 human lymphoblast and H1HeLa cell adhesion assay	2005	Bioorganic & 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.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings 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.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings 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.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular 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)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	1 (4.17)	18.2507
2000's	17 (70.83)	29.6817
2010's	4 (16.67)	24.3611
2020's	2 (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.

Metric	This Compound (vs All)
Research Demand Index	24.37 (24.57)
Research Supply Index	3.22 (2.92)
Research Growth Index	5.22 (4.65)
Search Engine Demand Index	17.79 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (24.37)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	24 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
isoflurane Isoflurane: A stable, non-explosive inhalation anesthetic, relatively free from significant side effects.	2.15	1	organofluorine compound	inhalation 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.	2.15	1	ether; 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.	2	1	alanine 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.	2.44	2	imidazolidine-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.	2.02	1	1,4-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.	2.03	1	d-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.	2.02	1	elemental manganese; manganese group element atom	Escherichia coli metabolite; micronutrient
aziridine-2-carboxylic acid aziridine-2-carboxylic acid: structure given in first source	2.02	1
imidazolidines [no description available]	4.28	18	azacycloalkane; 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.	2.05	1

Condition	Relationship Strength	Studies
Innate Inflammatory Response [description not available]	2.42	2
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.	2.42	2
Congenital Zika Syndrome [description not available]	2.25	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.46	2
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.	2.25	1
Infectious Myelitis [description not available]	2.21	1
Nerve Pain [description not available]	2.21	1
Delayed Effects, Prenatal Exposure [description not available]	2.21	1
Neuralgia Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.	2.21	1
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	2.21	1
Kahler Disease [description not available]	2.01	1
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.	2.01	1
Leucocythaemia [description not available]	2.03	1
Germinoblastoma [description not available]	2.03	1
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)	2.03	1
Lymphoma A general term for various neoplastic diseases of the lymphoid tissue.	2.03	1
Delayed Hypersensitivity [description not available]	2	1

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