Page last updated: 2024-11-12

lb 30057

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 CID9913629
CHEMBL ID7962
MeSH IDM0299709

Synonyms (16)

Synonym
CHEMBL7962 ,
1n-cyclopentyl-1n-methyl-3-(4-carbohydrazonamidephenyl)-2-(2-naphthylsulfonamido)-(2s)-propanamide
(s)-5-(4-methylamino-phenyl)-2-(5,6,7,8-tetrahydro-naphthalene-2-sulfonylamino)-pent-4-ynoic acid cyclopentylamide
bdbm50069294
(s)-3-[4-(carbohydrazonamidol)-phenyl]-n-cyclopentyl-n-methyl-2-(naphthalene-2-sulfonylamino)-propionamide
n-methyl-n-cyclopentyl-3-(4-hydrazonoformamidephenyl)-2-[(2-naphthylsulfonyl)amino]propanamide
1n-cyclopentyl-3-[4-amino(aminoimino)methylphenyl]-2-(2-naphthylsulfinamido)propanamide
unii-if979jqu3s
lb30057
IF979JQU3S ,
lb-30057 free base
benzenecarboximidic acid, 4-((2s)-3-(cyclopentylmethylamino)-2-((2-naphthalenylsulfonyl)amino)-3-oxopropyl)-, hydrazide
pd-172524 free base
ci-1028 free base
184770-78-3
(2s)-3-[4-[(z)-c-aminocarbonohydrazonoyl]phenyl]-n-cyclopentyl-n-methyl-2-(naphthalen-2-ylsulfonylamino)propanamide

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"38 nM for human thrombin), selective (Ki = 3290 nM for bovine trypsin), and orally bioavailable (58% oral bioavailability in dogs)."( Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.
Hong, S; Hwang, SY; Kim, DS; Kim, S; Lee, CH; Lee, K; Lee, SH; Lee, SK; Lee, YH; Oh, YS; Park, HD; Shin, Y; Yoo, YJ; Yoon, KH; Yun, M, 1998
)
0.3
"3 nM) that are trypsin-selective, highly orally bioavailable in rats, and highly permeable across Caco-2 cells."( Benzylamine-based selective and orally bioavailable inhibitors of thrombin.
Hong, CY; Jung, WH; Kim, IC; Kim, S; Kim, SW; Kwon, OH; Lee, K; Lee, SH; Lee, YH; Oh, YS; Park, CW; Park, HD; Yoo, YJ, 1998
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ProthrombinHomo sapiens (human)Ki0.00040.00000.78469.0000AID210997; AID211017; AID211022; AID211037; AID211195; AID211211
Prothrombin Bos taurus (cattle)Ki0.00110.00112.06948.3700AID213271
Coagulation factor XHomo sapiens (human)Ki1.10000.00000.47089.0000AID51684
PlasminogenHomo sapiens (human)Ki47.90000.01701.15604.4000AID158142
Tissue-type plasminogen activatorHomo sapiens (human)Ki27.20000.01703.71968.6000AID228031
Cationic trypsinBos taurus (cattle)Ki12.07770.00001.07539.0000AID215186; AID215201; AID215206
Trypsin-1Homo sapiens (human)Ki3.29000.00001.76768.9000AID215016
Trypsin-2Homo sapiens (human)Ki3.29000.00430.94873.2900AID215016
Trypsin-3Homo sapiens (human)Ki3.29000.00430.94873.2900AID215016
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (64)

Processvia Protein(s)Taxonomy
positive regulation of protein phosphorylationProthrombinHomo sapiens (human)
proteolysisProthrombinHomo sapiens (human)
acute-phase responseProthrombinHomo sapiens (human)
cell surface receptor signaling pathwayProthrombinHomo sapiens (human)
G protein-coupled receptor signaling pathwayProthrombinHomo sapiens (human)
blood coagulationProthrombinHomo sapiens (human)
positive regulation of cell population proliferationProthrombinHomo sapiens (human)
regulation of cell shapeProthrombinHomo sapiens (human)
response to woundingProthrombinHomo sapiens (human)
negative regulation of platelet activationProthrombinHomo sapiens (human)
platelet activationProthrombinHomo sapiens (human)
regulation of blood coagulationProthrombinHomo sapiens (human)
positive regulation of blood coagulationProthrombinHomo sapiens (human)
positive regulation of cell growthProthrombinHomo sapiens (human)
positive regulation of insulin secretionProthrombinHomo sapiens (human)
positive regulation of collagen biosynthetic processProthrombinHomo sapiens (human)
fibrinolysisProthrombinHomo sapiens (human)
negative regulation of proteolysisProthrombinHomo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATProthrombinHomo sapiens (human)
negative regulation of astrocyte differentiationProthrombinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolProthrombinHomo sapiens (human)
regulation of cytosolic calcium ion concentrationProthrombinHomo sapiens (human)
cytolysis by host of symbiont cellsProthrombinHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionProthrombinHomo sapiens (human)
negative regulation of fibrinolysisProthrombinHomo sapiens (human)
antimicrobial humoral immune response mediated by antimicrobial peptideProthrombinHomo sapiens (human)
neutrophil-mediated killing of gram-negative bacteriumProthrombinHomo sapiens (human)
positive regulation of lipid kinase activityProthrombinHomo sapiens (human)
negative regulation of cytokine production involved in inflammatory responseProthrombinHomo sapiens (human)
positive regulation of protein localization to nucleusProthrombinHomo sapiens (human)
positive regulation of phospholipase C-activating G protein-coupled receptor signaling pathwayProthrombinHomo sapiens (human)
ligand-gated ion channel signaling pathwayProthrombinHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processProthrombinHomo sapiens (human)
proteolysisProthrombin Bos taurus (cattle)
acute-phase responseProthrombin Bos taurus (cattle)
positive regulation of blood coagulationProthrombin Bos taurus (cattle)
protein polymerizationProthrombin Bos taurus (cattle)
proteolysisCoagulation factor XHomo sapiens (human)
blood coagulationCoagulation factor XHomo sapiens (human)
positive regulation of cell migrationCoagulation factor XHomo sapiens (human)
positive regulation of TOR signalingCoagulation factor XHomo sapiens (human)
proteolysisPlasminogenHomo sapiens (human)
blood coagulationPlasminogenHomo sapiens (human)
negative regulation of cell population proliferationPlasminogenHomo sapiens (human)
negative regulation of cell-substrate adhesionPlasminogenHomo sapiens (human)
extracellular matrix disassemblyPlasminogenHomo sapiens (human)
tissue regenerationPlasminogenHomo sapiens (human)
fibrinolysisPlasminogenHomo sapiens (human)
positive regulation of blood vessel endothelial cell migrationPlasminogenHomo sapiens (human)
myoblast differentiationPlasminogenHomo sapiens (human)
muscle cell cellular homeostasisPlasminogenHomo sapiens (human)
tissue remodelingPlasminogenHomo sapiens (human)
biological process involved in interaction with symbiontPlasminogenHomo sapiens (human)
negative regulation of fibrinolysisPlasminogenHomo sapiens (human)
positive regulation of fibrinolysisPlasminogenHomo sapiens (human)
trophoblast giant cell differentiationPlasminogenHomo sapiens (human)
labyrinthine layer blood vessel developmentPlasminogenHomo sapiens (human)
mononuclear cell migrationPlasminogenHomo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmissionPlasminogenHomo sapiens (human)
negative regulation of cell-cell adhesion mediated by cadherinPlasminogenHomo sapiens (human)
response to hypoxiaTissue-type plasminogen activatorHomo sapiens (human)
proteolysisTissue-type plasminogen activatorHomo sapiens (human)
blood coagulationTissue-type plasminogen activatorHomo sapiens (human)
negative regulation of plasminogen activationTissue-type plasminogen activatorHomo sapiens (human)
plasminogen activationTissue-type plasminogen activatorHomo sapiens (human)
protein modification processTissue-type plasminogen activatorHomo sapiens (human)
fibrinolysisTissue-type plasminogen activatorHomo sapiens (human)
negative regulation of proteolysisTissue-type plasminogen activatorHomo sapiens (human)
negative regulation of fibrinolysisTissue-type plasminogen activatorHomo sapiens (human)
prevention of polyspermyTissue-type plasminogen activatorHomo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmissionTissue-type plasminogen activatorHomo sapiens (human)
platelet-derived growth factor receptor signaling pathwayTissue-type plasminogen activatorHomo sapiens (human)
smooth muscle cell migrationTissue-type plasminogen activatorHomo sapiens (human)
proteolysisCationic trypsinBos taurus (cattle)
digestionCationic trypsinBos taurus (cattle)
digestionTrypsin-1Homo sapiens (human)
extracellular matrix disassemblyTrypsin-1Homo sapiens (human)
proteolysisTrypsin-1Homo sapiens (human)
proteolysisTrypsin-2Homo sapiens (human)
digestionTrypsin-2Homo sapiens (human)
antimicrobial humoral responseTrypsin-2Homo sapiens (human)
extracellular matrix disassemblyTrypsin-2Homo sapiens (human)
positive regulation of cell growthTrypsin-2Homo sapiens (human)
collagen catabolic processTrypsin-2Homo sapiens (human)
positive regulation of cell adhesionTrypsin-2Homo sapiens (human)
proteolysisTrypsin-3Homo sapiens (human)
digestionTrypsin-3Homo sapiens (human)
antimicrobial humoral responseTrypsin-3Homo sapiens (human)
zymogen activationTrypsin-3Homo sapiens (human)
endothelial cell migrationTrypsin-3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
lipopolysaccharide bindingProthrombinHomo sapiens (human)
serine-type endopeptidase activityProthrombinHomo sapiens (human)
signaling receptor bindingProthrombinHomo sapiens (human)
calcium ion bindingProthrombinHomo sapiens (human)
protein bindingProthrombinHomo sapiens (human)
growth factor activityProthrombinHomo sapiens (human)
heparin bindingProthrombinHomo sapiens (human)
thrombospondin receptor activityProthrombinHomo sapiens (human)
serine-type endopeptidase activityProthrombin Bos taurus (cattle)
calcium ion bindingProthrombin Bos taurus (cattle)
protein bindingProthrombin Bos taurus (cattle)
fibrinogen bindingProthrombin Bos taurus (cattle)
serine-type endopeptidase activityCoagulation factor XHomo sapiens (human)
calcium ion bindingCoagulation factor XHomo sapiens (human)
protein bindingCoagulation factor XHomo sapiens (human)
phospholipid bindingCoagulation factor XHomo sapiens (human)
protease bindingPlasminogenHomo sapiens (human)
endopeptidase activityPlasminogenHomo sapiens (human)
serine-type endopeptidase activityPlasminogenHomo sapiens (human)
signaling receptor bindingPlasminogenHomo sapiens (human)
protein bindingPlasminogenHomo sapiens (human)
serine-type peptidase activityPlasminogenHomo sapiens (human)
enzyme bindingPlasminogenHomo sapiens (human)
kinase bindingPlasminogenHomo sapiens (human)
protein domain specific bindingPlasminogenHomo sapiens (human)
apolipoprotein bindingPlasminogenHomo sapiens (human)
protein-folding chaperone bindingPlasminogenHomo sapiens (human)
protein antigen bindingPlasminogenHomo sapiens (human)
serine-type endopeptidase activityTissue-type plasminogen activatorHomo sapiens (human)
signaling receptor bindingTissue-type plasminogen activatorHomo sapiens (human)
protein bindingTissue-type plasminogen activatorHomo sapiens (human)
phosphoprotein bindingTissue-type plasminogen activatorHomo sapiens (human)
endopeptidase activityCationic trypsinBos taurus (cattle)
serine-type endopeptidase activityCationic trypsinBos taurus (cattle)
protein bindingCationic trypsinBos taurus (cattle)
metal ion bindingCationic trypsinBos taurus (cattle)
serpin family protein bindingCationic trypsinBos taurus (cattle)
serine-type endopeptidase activityTrypsin-1Homo sapiens (human)
metal ion bindingTrypsin-1Homo sapiens (human)
metalloendopeptidase activityTrypsin-2Homo sapiens (human)
serine-type endopeptidase activityTrypsin-2Homo sapiens (human)
calcium ion bindingTrypsin-2Homo sapiens (human)
protein bindingTrypsin-2Homo sapiens (human)
serine-type peptidase activityTrypsin-2Homo sapiens (human)
serine-type endopeptidase activityTrypsin-3Homo sapiens (human)
calcium ion bindingTrypsin-3Homo sapiens (human)
protein bindingTrypsin-3Homo sapiens (human)
serine-type peptidase activityTrypsin-3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Processvia Protein(s)Taxonomy
external side of plasma membraneProthrombinHomo sapiens (human)
collagen-containing extracellular matrixProthrombinHomo sapiens (human)
extracellular regionProthrombinHomo sapiens (human)
extracellular spaceProthrombinHomo sapiens (human)
endoplasmic reticulum lumenProthrombinHomo sapiens (human)
Golgi lumenProthrombinHomo sapiens (human)
plasma membraneProthrombinHomo sapiens (human)
extracellular exosomeProthrombinHomo sapiens (human)
blood microparticleProthrombinHomo sapiens (human)
collagen-containing extracellular matrixProthrombinHomo sapiens (human)
extracellular spaceProthrombinHomo sapiens (human)
extracellular regionCoagulation factor XHomo sapiens (human)
endoplasmic reticulum lumenCoagulation factor XHomo sapiens (human)
Golgi lumenCoagulation factor XHomo sapiens (human)
plasma membraneCoagulation factor XHomo sapiens (human)
external side of plasma membraneCoagulation factor XHomo sapiens (human)
extracellular spaceCoagulation factor XHomo sapiens (human)
extracellular regionPlasminogenHomo sapiens (human)
extracellular spacePlasminogenHomo sapiens (human)
plasma membranePlasminogenHomo sapiens (human)
external side of plasma membranePlasminogenHomo sapiens (human)
cell surfacePlasminogenHomo sapiens (human)
platelet alpha granule lumenPlasminogenHomo sapiens (human)
collagen-containing extracellular matrixPlasminogenHomo sapiens (human)
extracellular exosomePlasminogenHomo sapiens (human)
blood microparticlePlasminogenHomo sapiens (human)
Schaffer collateral - CA1 synapsePlasminogenHomo sapiens (human)
glutamatergic synapsePlasminogenHomo sapiens (human)
extracellular spacePlasminogenHomo sapiens (human)
collagen-containing extracellular matrixTissue-type plasminogen activatorHomo sapiens (human)
extracellular regionTissue-type plasminogen activatorHomo sapiens (human)
cytoplasmTissue-type plasminogen activatorHomo sapiens (human)
cell surfaceTissue-type plasminogen activatorHomo sapiens (human)
secretory granuleTissue-type plasminogen activatorHomo sapiens (human)
apical part of cellTissue-type plasminogen activatorHomo sapiens (human)
extracellular exosomeTissue-type plasminogen activatorHomo sapiens (human)
serine protease inhibitor complexTissue-type plasminogen activatorHomo sapiens (human)
Schaffer collateral - CA1 synapseTissue-type plasminogen activatorHomo sapiens (human)
glutamatergic synapseTissue-type plasminogen activatorHomo sapiens (human)
extracellular spaceTissue-type plasminogen activatorHomo sapiens (human)
serine protease inhibitor complexCationic trypsinBos taurus (cattle)
extracellular regionTrypsin-1Homo sapiens (human)
collagen-containing extracellular matrixTrypsin-1Homo sapiens (human)
blood microparticleTrypsin-1Homo sapiens (human)
extracellular spaceTrypsin-1Homo sapiens (human)
extracellular regionTrypsin-2Homo sapiens (human)
extracellular spaceTrypsin-2Homo sapiens (human)
extracellular matrixTrypsin-2Homo sapiens (human)
azurophil granule lumenTrypsin-2Homo sapiens (human)
extracellular spaceTrypsin-2Homo sapiens (human)
extracellular regionTrypsin-3Homo sapiens (human)
extracellular spaceTrypsin-3Homo sapiens (human)
tertiary granule lumenTrypsin-3Homo sapiens (human)
extracellular spaceTrypsin-3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID9515Half life was evaluated in dog1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.
AID210997Binding affinity towards human thrombin1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Benzylamine-based selective and orally bioavailable inhibitors of thrombin.
AID7811Apparent permeability coefficient (Papp) was determined in human Caco-2 cell monolayer (n = 3)1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Benzylamine-based selective and orally bioavailable inhibitors of thrombin.
AID215016Compound was tested for inhibitory activity against bovine trypsin1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.
AID211195In vitro inhibition of human thrombin.2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Noncovalent thrombin inhibitors incorporating an imidazolylethynyl P1.
AID211017Compound was evaluated for its inhibitory activity against human thrombin1998Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
Potent and efficacious thienylamidine-incorporated thrombin inhibitors.
AID12133Absorption behavior was judged by the area under the curve, determined after oral dose of 30 mg/kg in rats.1999Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17
Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.
AID211211Inhibitory constant against human thrombin was determined in vitro.1999Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17
Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.
AID11396Absorption behavior was judged by the peak blood concentration determined after oral dose of 30 mg/kg in rats.1999Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17
Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.
AID215186Compound was evaluated for its inhibitory activity against bovine trypsin1998Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
Potent and efficacious thienylamidine-incorporated thrombin inhibitors.
AID89356Concentration of inhibitor in human plasma required to double the activated partial thromboplastin time (aPTT)2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Noncovalent thrombin inhibitors incorporating an imidazolylethynyl P1.
AID211037Compound was tested for inhibitory activity against human thrombin1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.
AID211022Binding affinity against human thrombin2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1.
AID228031The compound was tested for inhibitory activity against tissue plasminogen activator1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.
AID213271Compound was tested for inhibitory activity against bovine thrombin1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.
AID8500Compound was tested for percent of oral bioavailability at 10 mg/ml dose in dogs1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.
AID51684The compound was tested for inhibitory activity against Coagulation factor X1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.
AID215206Inhibitory constant against bovine trypsin was determined in vitro.1999Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17
Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.
AID158142The compound was tested for inhibitory activity against human plasmin1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.
AID215201Inhibitory activity against Bovine Trypsin2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Noncovalent thrombin inhibitors incorporating an imidazolylethynyl P1.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (66.67)18.2507
2000's2 (33.33)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.24

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 Index12.24 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.18 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.24)

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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]