Page last updated: 2024-12-09

2-bromo-N-[3-(1-oxobutylamino)phenyl]benzamide

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 CID1048267
CHEMBL ID1411333
CHEBI ID93032
SCHEMBL ID882467

Synonyms (57)

Synonym
2-bromo-n-[3-(butanoylamino)phenyl]benzamide
OPREA1_852187
AKOS003193751
MLS000571703 ,
smr000193713
2-bromo-n-[3-(butyrylamino)phenyl]benzamide
AG-670/40910903
ml161 mls002699906
BRD-K59036917-001-05-0
MLS002699906
BRD-K59036917-001-04-3
HMS2461M06
BRD-K59036917-001-07-6
bdbm50386391
ml161
423735-93-7
STL169237
chembl1411333 ,
S2916
SCHEMBL882467
AB00101592-01
2-bromo-n-(3-butyramidophenyl)benzamide
DFOVLSMXPWPCFH-UHFFFAOYSA-N
ml 161
c17h17brn2o2
cambridge id 5946339
2-bromo-n-[3-[(1-oxobutyl)amino]phenyl]benzamide
2-bromo-n-[3-[(1-oxobutyl)amino]phenyl]-benzamide
AC-35205
J-690295
ml-161
EX-A273
DTXSID20359961
CHEBI:93032
HMS3651N10
mfcd03063772
ml-161, >=98% (hplc)
sr-01000224080
SR-01000224080-1
NCGC00371123-06
2-bromo-n-(3-butanamidophenyl)benzamide
SW219764-1
BCP08413
parmodulin 2
HY-13965
Q27164762
2-bromo-n-[3-(1-oxobutylamino)phenyl]benzamide
Z57444105
FT-0700306
AS-16666
A13495
AMY31203
CCG-268174
CS-0009021
NCGC00371123-09
YRA73593
EN300-6493078

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzamides
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency12.58930.000811.382244.6684AID686979
thioredoxin glutathione reductaseSchistosoma mansoniPotency25.11890.100022.9075100.0000AID485364
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency21.31740.01237.983543.2770AID1645841
P53Homo sapiens (human)Potency12.58930.07319.685831.6228AID504706
gemininHomo sapiens (human)Potency6.51310.004611.374133.4983AID624296
[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)
Proteinase-activated receptor 1Homo sapiens (human)IC50 (µMol)0.60350.00111.006910.0000AID1392444; AID1552683
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (46)

Processvia Protein(s)Taxonomy
connective tissue replacement involved in inflammatory response wound healingProteinase-activated receptor 1Homo sapiens (human)
negative regulation of glomerular filtrationProteinase-activated receptor 1Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processProteinase-activated receptor 1Homo sapiens (human)
inflammatory responseProteinase-activated receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayProteinase-activated receptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayProteinase-activated receptor 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProteinase-activated receptor 1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayProteinase-activated receptor 1Homo sapiens (human)
establishment of synaptic specificity at neuromuscular junctionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of cell population proliferationProteinase-activated receptor 1Homo sapiens (human)
negative regulation of cell population proliferationProteinase-activated receptor 1Homo sapiens (human)
response to woundingProteinase-activated receptor 1Homo sapiens (human)
anatomical structure morphogenesisProteinase-activated receptor 1Homo sapiens (human)
platelet activationProteinase-activated receptor 1Homo sapiens (human)
regulation of blood coagulationProteinase-activated receptor 1Homo sapiens (human)
positive regulation of blood coagulationProteinase-activated receptor 1Homo sapiens (human)
positive regulation of cell migrationProteinase-activated receptor 1Homo sapiens (human)
response to lipopolysaccharideProteinase-activated receptor 1Homo sapiens (human)
regulation of interleukin-1 beta productionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of interleukin-6 productionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of interleukin-8 productionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of collagen biosynthetic processProteinase-activated receptor 1Homo sapiens (human)
positive regulation of Rho protein signal transductionProteinase-activated receptor 1Homo sapiens (human)
dendritic cell homeostasisProteinase-activated receptor 1Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processProteinase-activated receptor 1Homo sapiens (human)
positive regulation of MAPK cascadeProteinase-activated receptor 1Homo sapiens (human)
negative regulation of neuron apoptotic processProteinase-activated receptor 1Homo sapiens (human)
positive regulation of GTPase activityProteinase-activated receptor 1Homo sapiens (human)
cell-cell junction maintenanceProteinase-activated receptor 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of vasoconstrictionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of smooth muscle contractionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATProteinase-activated receptor 1Homo sapiens (human)
regulation of synaptic plasticityProteinase-activated receptor 1Homo sapiens (human)
homeostasis of number of cells within a tissueProteinase-activated receptor 1Homo sapiens (human)
release of sequestered calcium ion into cytosolProteinase-activated receptor 1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolProteinase-activated receptor 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of calcium ion transportProteinase-activated receptor 1Homo sapiens (human)
regulation of sensory perception of painProteinase-activated receptor 1Homo sapiens (human)
platelet dense granule organizationProteinase-activated receptor 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeProteinase-activated receptor 1Homo sapiens (human)
thrombin-activated receptor signaling pathwayProteinase-activated receptor 1Homo sapiens (human)
trans-synaptic signaling by endocannabinoid, modulating synaptic transmissionProteinase-activated receptor 1Homo sapiens (human)
negative regulation of renin secretion into blood streamProteinase-activated receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
G-protein alpha-subunit bindingProteinase-activated receptor 1Homo sapiens (human)
G protein-coupled receptor activityProteinase-activated receptor 1Homo sapiens (human)
signaling receptor bindingProteinase-activated receptor 1Homo sapiens (human)
protein bindingProteinase-activated receptor 1Homo sapiens (human)
thrombin-activated receptor activityProteinase-activated receptor 1Homo sapiens (human)
G-protein beta-subunit bindingProteinase-activated receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
plasma membraneProteinase-activated receptor 1Homo sapiens (human)
extracellular regionProteinase-activated receptor 1Homo sapiens (human)
early endosomeProteinase-activated receptor 1Homo sapiens (human)
late endosomeProteinase-activated receptor 1Homo sapiens (human)
Golgi apparatusProteinase-activated receptor 1Homo sapiens (human)
plasma membraneProteinase-activated receptor 1Homo sapiens (human)
caveolaProteinase-activated receptor 1Homo sapiens (human)
cell surfaceProteinase-activated receptor 1Homo sapiens (human)
platelet dense tubular networkProteinase-activated receptor 1Homo sapiens (human)
neuromuscular junctionProteinase-activated receptor 1Homo sapiens (human)
postsynaptic membraneProteinase-activated receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (60)

Assay IDTitleYearJournalArticle
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID1392444Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluor2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells.
AID669691Inhibition of U46619-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin at 3 uM after 20 mins by flow cytometry2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID669705Inhibition of thrombin-stimulated PAR1-mediated platelet aggregation in human washed platelets at 3 uM by ChronoLog 680 aggregation system analysis2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID669698Metabolic stability in mouse plasma assessed as compound remaining at 5 uM after 5 hrs2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID669707Inhibition of thromboxane-stimulated PAR1-mediated platelet aggregation in human washed platelets at 3 uM by ChronoLog 680 aggregation system analysis2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID1552682Inhibition of rat PBR at 10 uM2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID669708Inhibition of ADP-stimulated PAR1-mediated platelet aggregation in human washed platelets at 3 uM by ChronoLog 680 aggregation system analysis2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID669700Plasma protein binding in human2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID669699Inhibition of thrombin-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID1552684Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization at 10 uM incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay relative 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID1552698Cytotoxicity against human HepG2 cells assessed as reduction in cell viability2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID1552702Stability in mouse plasma at 10 uM measured at 4 hrs by LC-MS analysis2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID669706Inhibition of AYPGFK-stimulated PAR1-mediated platelet aggregation in human washed platelets at 3 uM by ChronoLog 680 aggregation system analysis2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID669702Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet aggregation in platelet-rich human plasma assessed as granule secretion2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID669690Inhibition of AYPGKF-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin at 3 uM after 20 mins by flow cytometry2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID1552695Inhibition of serotonin transporter (unknown origin) at 10 uM2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID1552688Reversible inhibition of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization at 10 uM incubated for 15 mins and washed in buffer followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence ass2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID1552683Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID1552699Solubility in 2.5% DMSO2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID669703Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet aggregation in platelet-rich human plasma assessed as shape changes2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID669696Solubility of the compound in phosphate buffered saline2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID669692Inhibition of collagen-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin at 3 uM after 20 mins by flow cytometry2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID1552681Antiplatelet activity in human platelet rich plasma assessed as inhibition of SFLLRN-NH2-induced platelet aggregation at 10 uM incubated for 2 mins followed by SFLLRN-NH2 addition and monitored for 5 mins by lumi-aggregometery2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID669689Inhibition of PMA-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin at 3 uM after 20 mins by flow cytometry2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID1392450Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization at 10 uM pretreated for 20 to 30 mins followed by compound washout and subsequent incubation for 10 mins prior to2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells.
AID669688Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID669693Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin at 10 uM after 20 mins by flow cytometry2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID669704Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet aggregation in human washed platelets at 3 uM by ChronoLog 680 aggregation system analysis2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID1392446Antagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization at 10 uM pretreated for 15 mins followed by SLIGKV-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye ba2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells.
AID669694Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin at 3 uM after 20 mins by flow cytometry2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID1552694Inhibition of beta3 adrenoceptor (unknown origin) at 10 uM by radio ligand binding assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID1552689Antiinflammatory activity in human EAhy926 cells assessed as inhibition of TNFalpha-induced TF expression at 10 uM preincubated for 1 hr followed by TNFalpha addition and measured after 3 hrs by qPCR analysis2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID669701Plasma protein binding in mouse2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID669697Metabolic stability in human plasma assessed as compound remaining at 5 uM after 5 hrs2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID1552693Inhibition of beta1 adrenoceptor (unknown origin) at 10 uM by radio ligand binding assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID1552687Negative allosteric modulation of PAR2 in human EAhy926 cells assessed as reduction in SLIGKV-NH2-induced intracellular calcium mobilization at 0.316 to 10 uM incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID1552692Stability in human microsomes for 1 hr2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID1552703Stability in human plasma at 10 uM measured at 4 hrs by LC-MS analysis2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
AID669695Inhibition of PDE3A2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159537qHTS screening for TAG (triacylglycerol) accumulators in algae2017Plant physiology, Aug, Volume: 174, Issue:4
Identification and Metabolite Profiling of Chemical Activators of Lipid Accumulation in Green Algae.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (7.14)29.6817
2010's9 (64.29)24.3611
2020's4 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.03

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 Index12.03 (24.57)
Research Supply Index2.71 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.03)

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%
Other14 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]