Page last updated: 2024-11-13

rpx7009

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Description

RPX7009: a beta-lactamase inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	56649692
CHEMBL ID	3317857
SCHEMBL ID	620289
MeSH ID	M000608394

Synonyms (44)

Synonym
chembl3317857 ,
bdbm50089084
IOOWNWLVCOUUEX-WPRPVWTQSA-N
2-((3r,6s)-2-hydroxy-3-(2-(thiophen-2-yl)acetamido)-1,2-oxaborinan-6-yl)acetic acid
SCHEMBL620289
vaborbactam
rpx 7009
vaborbactam [usan:inn]
1360457-46-0
unii-1c75676f8v
vaborbactam component of carbavance
1,2-oxaborinane-6-acetic acid, 2-hydroxy-3-((2-(2-thienyl)acetyl)amino)-, (3r,6s)-
vaborbactam [usan]
vabomere component vaborbactam
rpx-7009
vaborbactam [orange book]
vaborbactam [mi]
1575712-03-6
rpx7009
carbavance component vaborbactam
vaborbactam [who-dd]
1C75676F8V ,
vaborbactam [inn]
HY-19930
CS-6445
D10998
vaborbactam (usan/inn)
DB12107
{(3r,6s)-2-hydroxy-3-[(thiophen-2-ylacetyl)amino]-1,2-oxaborinan-6-yl}acetic acid
AKOS032961376
mfcd28502176
EX-A2589
vaborbactam. rpx7009
gtpl10871
vabomere (vaborbactam + meropenem)
NCGC00510003-01
compound 9f [pmid: 25782055]
Q27252228
MS-24261
2-[(3r,6s)-2-hydroxy-3-[(2-thiophen-2-ylacetyl)amino]oxaborinan-6-yl]acetic acid
BV163750
DTXSID901027690
EN300-20818376
2-[(3r,6s)-2-hydroxy-3-[2-(thiophen-2-yl)acetamido]-1,2-oxaborinan-6-yl]acetic acid

Research Excerpts

Overview

RPX7009 is a novel β-lactamase inhibitor with activity against serine carbapenemases.

Excerpt	Reference	Relevance
"RPX7009 is a novel β-lactamase inhibitor with activity against serine carbapenemases."	( Activity of Meropenem Combined with RPX7009, a Novel β-Lactamase Inhibitor, against Gram-Negative Clinical Isolates in New York City. Abdallah, M; Cortes, C; Landman, D; Lapuebla, A; Olafisoye, O; Quale, J; Urban, C, 2015)	1.41

Toxicity

Excerpt	Reference	Relevance
" No subjects discontinued the study due to adverse events (AEs), and no serious AEs (SAEs) were observed."	( Phase 1 Study of the Safety, Tolerability, and Pharmacokinetics of the β-Lactamase Inhibitor Vaborbactam (RPX7009) in Healthy Adult Subjects. Dudley, MN; Durso, S; Griffith, DC; Loutit, JS; Morgan, EE, 2016)	0.65
" No subjects discontinued the study due to adverse events (AEs), and no serious AEs were observed."	( Phase 1 Study of the Safety, Tolerability, and Pharmacokinetics of Vaborbactam and Meropenem Alone and in Combination following Single and Multiple Doses in Healthy Adult Subjects. Bhavnani, SM; Dudley, MN; Griffith, DC; Loutit, JS; Morgan, EE; Rubino, CM; White, D, 2018)	0.48
" Overall, fewer adverse events were observed in the MV group than in the BAT group."	( Efficacy and Safety of Meropenem-Vaborbactam Versus Best Available Therapy for the Treatment of Carbapenem-Resistant Enterobacteriaceae Infections in Patients Without Prior Antimicrobial Failure: A Post Hoc Analysis. Bassetti, M; Giacobbe, DR; Massey, J; Patel, N; Tillotson, G, 2019)	0.51

Pharmacokinetics

Excerpt	Reference	Relevance
"Vaborbactam (formerly RPX7009) is a member of a new class of β-lactamase inhibitor with pharmacokinetic properties similar to those of many β-lactams, including carbapenems."	( Phase 1 Study of the Safety, Tolerability, and Pharmacokinetics of the β-Lactamase Inhibitor Vaborbactam (RPX7009) in Healthy Adult Subjects. Dudley, MN; Durso, S; Griffith, DC; Loutit, JS; Morgan, EE, 2016)	0.96
" The pharmacokinetics of meropenem and vaborbactam were similar when given alone or in combination; all evaluated plasma PK exposure measures (peak plasma concentration, area under the plasma concentration-time curve [AUC] from time zero to the last measurable concentration area under the plasma concentration-time curve, and AUC from time zero to infinity) were similar for the study drugs alone versus those in combination, indicating no pharmacokinetic interaction between meropenem and vaborbactam."	( Phase 1 Study of the Safety, Tolerability, and Pharmacokinetics of Vaborbactam and Meropenem Alone and in Combination following Single and Multiple Doses in Healthy Adult Subjects. Bhavnani, SM; Dudley, MN; Griffith, DC; Loutit, JS; Morgan, EE; Rubino, CM; White, D, 2018)	0.48
" Population pharmacokinetic (PK) models were developed to characterize the time course of meropenem and vaborbactam using pooled data from two phase 1 and two phase 3 studies."	( Population Pharmacokinetics of Meropenem and Vaborbactam Based on Data from Noninfected Subjects and Infected Patients. Ambrose, PG; Bhavnani, SM; Dudley, MN; Griffith, DC; Loutit, JS; Rubino, CM; Trang, M, 2021)	0.62

Compound-Compound Interactions

Excerpt	Reference	Relevance
" It is being developed in combination with meropenem."	( In vitro activity of meropenem combined with vaborbactam against KPC-producing Enterobacteriaceae in China. Chen, X; Kudinha, T; Lomovskaya, O; Sun, D; Xu, Y; Xu, Z; Yang, Q; Zhang, G; Zhou, M, 2018)	0.48
" In this study, we analyzed the in vitro activity of those novel antibacterial agents alone or in combination with polymyxin B against the CR-A."	( In vitro activity of ceftazidime/avibactam, imipenem/relebactam and meropenem/vaborbactam alone or in combination with polymyxin B against carbapenem resistant Acinetobacter baumannii. Gu, Y; Hu, D; Hu, M; Liang, R; Wang, D; Wang, M; Zhu, M, 2023)	0.91

Bioavailability

Excerpt	Reference	Relevance
" When isolated under acidic conditions, these compounds spontaneously formed a neutral cyclic anhydride (intramolecular prodrug) which was shown to have much-improved oral bioavailability (52-69%) compared to the ring-opened carboxylate salt (9%)."	( Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability. Clifton, MC; Griffith, DC; Hecker, SJ; Lomovskaya, O; Raja Reddy, K; Tarazi, Z; Totrov, M, 2022)	0.72

Dosage Studied

Excerpt	Relevance	Reference
" An understanding of the pharmacokinetics of meropenem when given in combination with vaborbactam is important to understanding the dosing of meropenem-vaborbactam."	( Pharmacokinetics of the Meropenem Component of Meropenem-Vaborbactam in the Treatment of KPC-Producing Klebsiella pneumoniae Bloodstream Infection in a Pediatric Patient. Chopra, A; Cies, JJ; Enache, A; Evangelista, AT; Hanretty, AM; Kaur, I; Moore, WS, 2018)	0.48
" Mice were inoculated with ∼1 × 107 cfu/mL in each thigh 2 h prior to dosing and both thighs were harvested at 24 h."	( Efficacy of human-simulated exposures of meropenem/vaborbactam and meropenem against OXA-48 β-lactamase-producing Enterobacterales in the neutropenic murine thigh infection model. Asempa, TE; Gill, CM; Nicolau, DP, 2021)	0.62
" Further evaluations with multiple dose in-vitro and in-vivo investigations are needed before specific MEM/VBR dosing recommendations can be made for clinical application with ECMO."	( Oxygenator impact on meropenem/vaborbactam in extracorporeal membrane oxygenation circuits. Chopra, A; Cies, JJ; Deacon, J; Enache, A; Giliam, N; Low, T; Marino, D; Moore, WS; Nikolos, P, 2022)	0.72
" pneumoniae bloodstream infection that was successfully treated with a continuous infusion of meropenem-vaborbactam at a dosage of 1 g/1 g q4h as a 4-h infusion."	( Continuous infusion of meropenem-vaborbactam for a KPC-3-producing Klebsiella pneumoniae bloodstream infection in a critically ill patient with augmented renal clearance. Bourgeois, PM; Gandon, C; Laffont-Lozes, P; Larcher, R; Magnan, C; Naciri, T; Pantel, A; Sotto, A, 2023)	0.91
" It could be appropriate for optimizing the management of critically ill patients with ARC, as it resulted in antibiotic concentrations above the minimum inhibitory concentration for susceptible carbapenem-resistant Enterobacterales (up to 8 mg/L) throughout the dosing interval."	( Continuous infusion of meropenem-vaborbactam for a KPC-3-producing Klebsiella pneumoniae bloodstream infection in a critically ill patient with augmented renal clearance. Bourgeois, PM; Gandon, C; Laffont-Lozes, P; Larcher, R; Magnan, C; Naciri, T; Pantel, A; Sotto, A, 2023)	0.91

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

Protein Targets (15)

Potency Measurements

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	39.8107	0.0096	10.5250	35.4813	AID1479145
[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)
Beta-lactamase	Escherichia coli	Ki	0.0560	0.0110	0.0335	0.0560	AID1657152
Prothrombin	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.0000	0.7107	10.0000	AID1225828
Plasminogen	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.0250	3.6280	10.0000	AID1225827
Urokinase-type plasminogen activator	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.0370	3.3859	10.0000	AID1225829
Tissue-type plasminogen activator	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.0340	2.5425	6.6000	AID1225831
Trypsin-1	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.0035	1.5321	10.0000	AID1225823
Trypsin-2	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.0035	1.5846	4.4000	AID1225823
Neutrophil elastase	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.0063	2.0734	22.3780	AID1225834
Lysosomal protective protein	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.6000	6.6000	10.0000	AID1225835
Chymase	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.0260	2.6397	10.0000	AID1225832
Trypsin-3	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.0035	1.5846	4.4000	AID1225823
Beta-lactamase	Acinetobacter baumannii	Ki	40.0000	1.7000	1.7000	1.7000	AID1657160
Dipeptidyl peptidase 2	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.0002	0.9316	6.6000	AID1225833
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (109)

Process	via Protein(s)	Taxonomy
positive regulation of protein phosphorylation	Prothrombin	Homo sapiens (human)
proteolysis	Prothrombin	Homo sapiens (human)
acute-phase response	Prothrombin	Homo sapiens (human)
cell surface receptor signaling pathway	Prothrombin	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Prothrombin	Homo sapiens (human)
blood coagulation	Prothrombin	Homo sapiens (human)
positive regulation of cell population proliferation	Prothrombin	Homo sapiens (human)
regulation of cell shape	Prothrombin	Homo sapiens (human)
response to wounding	Prothrombin	Homo sapiens (human)
negative regulation of platelet activation	Prothrombin	Homo sapiens (human)
platelet activation	Prothrombin	Homo sapiens (human)
regulation of blood coagulation	Prothrombin	Homo sapiens (human)
positive regulation of blood coagulation	Prothrombin	Homo sapiens (human)
positive regulation of cell growth	Prothrombin	Homo sapiens (human)
positive regulation of insulin secretion	Prothrombin	Homo sapiens (human)
positive regulation of collagen biosynthetic process	Prothrombin	Homo sapiens (human)
fibrinolysis	Prothrombin	Homo sapiens (human)
negative regulation of proteolysis	Prothrombin	Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STAT	Prothrombin	Homo sapiens (human)
negative regulation of astrocyte differentiation	Prothrombin	Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosol	Prothrombin	Homo sapiens (human)
regulation of cytosolic calcium ion concentration	Prothrombin	Homo sapiens (human)
cytolysis by host of symbiont cells	Prothrombin	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Prothrombin	Homo sapiens (human)
negative regulation of fibrinolysis	Prothrombin	Homo sapiens (human)
antimicrobial humoral immune response mediated by antimicrobial peptide	Prothrombin	Homo sapiens (human)
neutrophil-mediated killing of gram-negative bacterium	Prothrombin	Homo sapiens (human)
positive regulation of lipid kinase activity	Prothrombin	Homo sapiens (human)
negative regulation of cytokine production involved in inflammatory response	Prothrombin	Homo sapiens (human)
positive regulation of protein localization to nucleus	Prothrombin	Homo sapiens (human)
positive regulation of phospholipase C-activating G protein-coupled receptor signaling pathway	Prothrombin	Homo sapiens (human)
ligand-gated ion channel signaling pathway	Prothrombin	Homo sapiens (human)
positive regulation of reactive oxygen species metabolic process	Prothrombin	Homo sapiens (human)
proteolysis	Plasminogen	Homo sapiens (human)
blood coagulation	Plasminogen	Homo sapiens (human)
negative regulation of cell population proliferation	Plasminogen	Homo sapiens (human)
negative regulation of cell-substrate adhesion	Plasminogen	Homo sapiens (human)
extracellular matrix disassembly	Plasminogen	Homo sapiens (human)
tissue regeneration	Plasminogen	Homo sapiens (human)
fibrinolysis	Plasminogen	Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration	Plasminogen	Homo sapiens (human)
myoblast differentiation	Plasminogen	Homo sapiens (human)
muscle cell cellular homeostasis	Plasminogen	Homo sapiens (human)
tissue remodeling	Plasminogen	Homo sapiens (human)
biological process involved in interaction with symbiont	Plasminogen	Homo sapiens (human)
negative regulation of fibrinolysis	Plasminogen	Homo sapiens (human)
positive regulation of fibrinolysis	Plasminogen	Homo sapiens (human)
trophoblast giant cell differentiation	Plasminogen	Homo sapiens (human)
labyrinthine layer blood vessel development	Plasminogen	Homo sapiens (human)
mononuclear cell migration	Plasminogen	Homo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmission	Plasminogen	Homo sapiens (human)
negative regulation of cell-cell adhesion mediated by cadherin	Plasminogen	Homo sapiens (human)
positive regulation of cell migration	Urokinase-type plasminogen activator	Homo sapiens (human)
response to hypoxia	Urokinase-type plasminogen activator	Homo sapiens (human)
proteolysis	Urokinase-type plasminogen activator	Homo sapiens (human)
chemotaxis	Urokinase-type plasminogen activator	Homo sapiens (human)
signal transduction	Urokinase-type plasminogen activator	Homo sapiens (human)
blood coagulation	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of signaling receptor activity	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of plasminogen activation	Urokinase-type plasminogen activator	Homo sapiens (human)
negative regulation of plasminogen activation	Urokinase-type plasminogen activator	Homo sapiens (human)
smooth muscle cell migration	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of smooth muscle cell migration	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of cell adhesion	Urokinase-type plasminogen activator	Homo sapiens (human)
plasminogen activation	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of cell adhesion mediated by integrin	Urokinase-type plasminogen activator	Homo sapiens (human)
urokinase plasminogen activator signaling pathway	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of cell population proliferation	Urokinase-type plasminogen activator	Homo sapiens (human)
fibrinolysis	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of fibrinolysis	Urokinase-type plasminogen activator	Homo sapiens (human)
negative regulation of fibrinolysis	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of wound healing	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of smooth muscle cell-matrix adhesion	Urokinase-type plasminogen activator	Homo sapiens (human)
response to hypoxia	Tissue-type plasminogen activator	Homo sapiens (human)
proteolysis	Tissue-type plasminogen activator	Homo sapiens (human)
blood coagulation	Tissue-type plasminogen activator	Homo sapiens (human)
negative regulation of plasminogen activation	Tissue-type plasminogen activator	Homo sapiens (human)
plasminogen activation	Tissue-type plasminogen activator	Homo sapiens (human)
protein modification process	Tissue-type plasminogen activator	Homo sapiens (human)
fibrinolysis	Tissue-type plasminogen activator	Homo sapiens (human)
negative regulation of proteolysis	Tissue-type plasminogen activator	Homo sapiens (human)
negative regulation of fibrinolysis	Tissue-type plasminogen activator	Homo sapiens (human)
prevention of polyspermy	Tissue-type plasminogen activator	Homo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmission	Tissue-type plasminogen activator	Homo sapiens (human)
platelet-derived growth factor receptor signaling pathway	Tissue-type plasminogen activator	Homo sapiens (human)
smooth muscle cell migration	Tissue-type plasminogen activator	Homo sapiens (human)
digestion	Trypsin-1	Homo sapiens (human)
extracellular matrix disassembly	Trypsin-1	Homo sapiens (human)
proteolysis	Trypsin-1	Homo sapiens (human)
proteolysis	Trypsin-2	Homo sapiens (human)
digestion	Trypsin-2	Homo sapiens (human)
antimicrobial humoral response	Trypsin-2	Homo sapiens (human)
extracellular matrix disassembly	Trypsin-2	Homo sapiens (human)
positive regulation of cell growth	Trypsin-2	Homo sapiens (human)
collagen catabolic process	Trypsin-2	Homo sapiens (human)
positive regulation of cell adhesion	Trypsin-2	Homo sapiens (human)
proteolysis	Neutrophil elastase	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Neutrophil elastase	Homo sapiens (human)
response to yeast	Neutrophil elastase	Homo sapiens (human)
leukocyte migration involved in inflammatory response	Neutrophil elastase	Homo sapiens (human)
biosynthetic process of antibacterial peptides active against Gram-negative bacteria	Neutrophil elastase	Homo sapiens (human)
proteolysis	Neutrophil elastase	Homo sapiens (human)
intracellular calcium ion homeostasis	Neutrophil elastase	Homo sapiens (human)
response to UV	Neutrophil elastase	Homo sapiens (human)
extracellular matrix disassembly	Neutrophil elastase	Homo sapiens (human)
protein catabolic process	Neutrophil elastase	Homo sapiens (human)
response to lipopolysaccharide	Neutrophil elastase	Homo sapiens (human)
negative regulation of chemokine production	Neutrophil elastase	Homo sapiens (human)
negative regulation of interleukin-8 production	Neutrophil elastase	Homo sapiens (human)
positive regulation of interleukin-8 production	Neutrophil elastase	Homo sapiens (human)
defense response to bacterium	Neutrophil elastase	Homo sapiens (human)
positive regulation of MAP kinase activity	Neutrophil elastase	Homo sapiens (human)
positive regulation of smooth muscle cell proliferation	Neutrophil elastase	Homo sapiens (human)
negative regulation of inflammatory response	Neutrophil elastase	Homo sapiens (human)
positive regulation of immune response	Neutrophil elastase	Homo sapiens (human)
negative regulation of chemotaxis	Neutrophil elastase	Homo sapiens (human)
pyroptosis	Neutrophil elastase	Homo sapiens (human)
neutrophil-mediated killing of gram-negative bacterium	Neutrophil elastase	Homo sapiens (human)
neutrophil-mediated killing of fungus	Neutrophil elastase	Homo sapiens (human)
positive regulation of leukocyte tethering or rolling	Neutrophil elastase	Homo sapiens (human)
phagocytosis	Neutrophil elastase	Homo sapiens (human)
acute inflammatory response to antigenic stimulus	Neutrophil elastase	Homo sapiens (human)
proteolysis	Lysosomal protective protein	Homo sapiens (human)
intracellular protein transport	Lysosomal protective protein	Homo sapiens (human)
regulation of protein stability	Lysosomal protective protein	Homo sapiens (human)
regulation of chaperone-mediated autophagy	Lysosomal protective protein	Homo sapiens (human)
negative regulation of chaperone-mediated autophagy	Lysosomal protective protein	Homo sapiens (human)
angiotensin maturation	Chymase	Homo sapiens (human)
peptide metabolic process	Chymase	Homo sapiens (human)
extracellular matrix disassembly	Chymase	Homo sapiens (human)
protein catabolic process	Chymase	Homo sapiens (human)
midbrain development	Chymase	Homo sapiens (human)
basement membrane disassembly	Chymase	Homo sapiens (human)
positive regulation of angiogenesis	Chymase	Homo sapiens (human)
regulation of inflammatory response	Chymase	Homo sapiens (human)
cellular response to glucose stimulus	Chymase	Homo sapiens (human)
cytokine precursor processing	Chymase	Homo sapiens (human)
proteolysis	Trypsin-3	Homo sapiens (human)
digestion	Trypsin-3	Homo sapiens (human)
antimicrobial humoral response	Trypsin-3	Homo sapiens (human)
zymogen activation	Trypsin-3	Homo sapiens (human)
endothelial cell migration	Trypsin-3	Homo sapiens (human)
proteolysis	Dipeptidyl peptidase 2	Homo sapiens (human)
lysosomal protein catabolic process	Dipeptidyl peptidase 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (30)

Process	via Protein(s)	Taxonomy
lipopolysaccharide binding	Prothrombin	Homo sapiens (human)
serine-type endopeptidase activity	Prothrombin	Homo sapiens (human)
signaling receptor binding	Prothrombin	Homo sapiens (human)
calcium ion binding	Prothrombin	Homo sapiens (human)
protein binding	Prothrombin	Homo sapiens (human)
growth factor activity	Prothrombin	Homo sapiens (human)
heparin binding	Prothrombin	Homo sapiens (human)
thrombospondin receptor activity	Prothrombin	Homo sapiens (human)
protease binding	Plasminogen	Homo sapiens (human)
endopeptidase activity	Plasminogen	Homo sapiens (human)
serine-type endopeptidase activity	Plasminogen	Homo sapiens (human)
signaling receptor binding	Plasminogen	Homo sapiens (human)
protein binding	Plasminogen	Homo sapiens (human)
serine-type peptidase activity	Plasminogen	Homo sapiens (human)
enzyme binding	Plasminogen	Homo sapiens (human)
kinase binding	Plasminogen	Homo sapiens (human)
protein domain specific binding	Plasminogen	Homo sapiens (human)
apolipoprotein binding	Plasminogen	Homo sapiens (human)
protein-folding chaperone binding	Plasminogen	Homo sapiens (human)
protein antigen binding	Plasminogen	Homo sapiens (human)
serine-type endopeptidase activity	Urokinase-type plasminogen activator	Homo sapiens (human)
protein binding	Urokinase-type plasminogen activator	Homo sapiens (human)
serine-type endopeptidase activity	Tissue-type plasminogen activator	Homo sapiens (human)
signaling receptor binding	Tissue-type plasminogen activator	Homo sapiens (human)
protein binding	Tissue-type plasminogen activator	Homo sapiens (human)
phosphoprotein binding	Tissue-type plasminogen activator	Homo sapiens (human)
serine-type endopeptidase activity	Trypsin-1	Homo sapiens (human)
metal ion binding	Trypsin-1	Homo sapiens (human)
metalloendopeptidase activity	Trypsin-2	Homo sapiens (human)
serine-type endopeptidase activity	Trypsin-2	Homo sapiens (human)
calcium ion binding	Trypsin-2	Homo sapiens (human)
protein binding	Trypsin-2	Homo sapiens (human)
serine-type peptidase activity	Trypsin-2	Homo sapiens (human)
protease binding	Neutrophil elastase	Homo sapiens (human)
transcription corepressor activity	Neutrophil elastase	Homo sapiens (human)
endopeptidase activity	Neutrophil elastase	Homo sapiens (human)
serine-type endopeptidase activity	Neutrophil elastase	Homo sapiens (human)
protein binding	Neutrophil elastase	Homo sapiens (human)
heparin binding	Neutrophil elastase	Homo sapiens (human)
peptidase activity	Neutrophil elastase	Homo sapiens (human)
cytokine binding	Neutrophil elastase	Homo sapiens (human)
carboxypeptidase activity	Lysosomal protective protein	Homo sapiens (human)
serine-type carboxypeptidase activity	Lysosomal protective protein	Homo sapiens (human)
enzyme activator activity	Lysosomal protective protein	Homo sapiens (human)
endopeptidase activity	Chymase	Homo sapiens (human)
serine-type endopeptidase activity	Chymase	Homo sapiens (human)
serine-type peptidase activity	Chymase	Homo sapiens (human)
peptide binding	Chymase	Homo sapiens (human)
serine-type endopeptidase activity	Trypsin-3	Homo sapiens (human)
calcium ion binding	Trypsin-3	Homo sapiens (human)
protein binding	Trypsin-3	Homo sapiens (human)
serine-type peptidase activity	Trypsin-3	Homo sapiens (human)
aminopeptidase activity	Dipeptidyl peptidase 2	Homo sapiens (human)
serine-type peptidase activity	Dipeptidyl peptidase 2	Homo sapiens (human)
serine-type exopeptidase activity	Dipeptidyl peptidase 2	Homo sapiens (human)
dipeptidyl-peptidase activity	Dipeptidyl peptidase 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (39)

Process	via Protein(s)	Taxonomy
external side of plasma membrane	Prothrombin	Homo sapiens (human)
collagen-containing extracellular matrix	Prothrombin	Homo sapiens (human)
extracellular region	Prothrombin	Homo sapiens (human)
extracellular space	Prothrombin	Homo sapiens (human)
endoplasmic reticulum lumen	Prothrombin	Homo sapiens (human)
Golgi lumen	Prothrombin	Homo sapiens (human)
plasma membrane	Prothrombin	Homo sapiens (human)
extracellular exosome	Prothrombin	Homo sapiens (human)
blood microparticle	Prothrombin	Homo sapiens (human)
collagen-containing extracellular matrix	Prothrombin	Homo sapiens (human)
extracellular space	Prothrombin	Homo sapiens (human)
extracellular region	Plasminogen	Homo sapiens (human)
extracellular space	Plasminogen	Homo sapiens (human)
plasma membrane	Plasminogen	Homo sapiens (human)
external side of plasma membrane	Plasminogen	Homo sapiens (human)
cell surface	Plasminogen	Homo sapiens (human)
platelet alpha granule lumen	Plasminogen	Homo sapiens (human)
collagen-containing extracellular matrix	Plasminogen	Homo sapiens (human)
extracellular exosome	Plasminogen	Homo sapiens (human)
blood microparticle	Plasminogen	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Plasminogen	Homo sapiens (human)
glutamatergic synapse	Plasminogen	Homo sapiens (human)
extracellular space	Plasminogen	Homo sapiens (human)
extracellular region	Urokinase-type plasminogen activator	Homo sapiens (human)
extracellular space	Urokinase-type plasminogen activator	Homo sapiens (human)
plasma membrane	Urokinase-type plasminogen activator	Homo sapiens (human)
focal adhesion	Urokinase-type plasminogen activator	Homo sapiens (human)
external side of plasma membrane	Urokinase-type plasminogen activator	Homo sapiens (human)
cell surface	Urokinase-type plasminogen activator	Homo sapiens (human)
specific granule membrane	Urokinase-type plasminogen activator	Homo sapiens (human)
extracellular exosome	Urokinase-type plasminogen activator	Homo sapiens (human)
tertiary granule membrane	Urokinase-type plasminogen activator	Homo sapiens (human)
serine protease inhibitor complex	Urokinase-type plasminogen activator	Homo sapiens (human)
protein complex involved in cell-matrix adhesion	Urokinase-type plasminogen activator	Homo sapiens (human)
serine-type endopeptidase complex	Urokinase-type plasminogen activator	Homo sapiens (human)
extracellular space	Urokinase-type plasminogen activator	Homo sapiens (human)
collagen-containing extracellular matrix	Tissue-type plasminogen activator	Homo sapiens (human)
extracellular region	Tissue-type plasminogen activator	Homo sapiens (human)
cytoplasm	Tissue-type plasminogen activator	Homo sapiens (human)
cell surface	Tissue-type plasminogen activator	Homo sapiens (human)
secretory granule	Tissue-type plasminogen activator	Homo sapiens (human)
apical part of cell	Tissue-type plasminogen activator	Homo sapiens (human)
extracellular exosome	Tissue-type plasminogen activator	Homo sapiens (human)
serine protease inhibitor complex	Tissue-type plasminogen activator	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Tissue-type plasminogen activator	Homo sapiens (human)
glutamatergic synapse	Tissue-type plasminogen activator	Homo sapiens (human)
extracellular space	Tissue-type plasminogen activator	Homo sapiens (human)
extracellular region	Trypsin-1	Homo sapiens (human)
collagen-containing extracellular matrix	Trypsin-1	Homo sapiens (human)
blood microparticle	Trypsin-1	Homo sapiens (human)
extracellular space	Trypsin-1	Homo sapiens (human)
extracellular region	Trypsin-2	Homo sapiens (human)
extracellular space	Trypsin-2	Homo sapiens (human)
extracellular matrix	Trypsin-2	Homo sapiens (human)
azurophil granule lumen	Trypsin-2	Homo sapiens (human)
extracellular space	Trypsin-2	Homo sapiens (human)
extracellular region	Neutrophil elastase	Homo sapiens (human)
extracellular space	Neutrophil elastase	Homo sapiens (human)
cytoplasm	Neutrophil elastase	Homo sapiens (human)
cytosol	Neutrophil elastase	Homo sapiens (human)
cell surface	Neutrophil elastase	Homo sapiens (human)
secretory granule	Neutrophil elastase	Homo sapiens (human)
azurophil granule lumen	Neutrophil elastase	Homo sapiens (human)
specific granule lumen	Neutrophil elastase	Homo sapiens (human)
phagocytic vesicle	Neutrophil elastase	Homo sapiens (human)
collagen-containing extracellular matrix	Neutrophil elastase	Homo sapiens (human)
extracellular exosome	Neutrophil elastase	Homo sapiens (human)
transcription repressor complex	Neutrophil elastase	Homo sapiens (human)
extracellular space	Neutrophil elastase	Homo sapiens (human)
lumenal side of lysosomal membrane	Lysosomal protective protein	Homo sapiens (human)
extracellular region	Lysosomal protective protein	Homo sapiens (human)
lysosome	Lysosomal protective protein	Homo sapiens (human)
endoplasmic reticulum	Lysosomal protective protein	Homo sapiens (human)
membrane	Lysosomal protective protein	Homo sapiens (human)
azurophil granule lumen	Lysosomal protective protein	Homo sapiens (human)
lysosomal lumen	Lysosomal protective protein	Homo sapiens (human)
intracellular membrane-bounded organelle	Lysosomal protective protein	Homo sapiens (human)
extracellular exosome	Lysosomal protective protein	Homo sapiens (human)
collagen-containing extracellular matrix	Chymase	Homo sapiens (human)
extracellular region	Chymase	Homo sapiens (human)
cytosol	Chymase	Homo sapiens (human)
secretory granule	Chymase	Homo sapiens (human)
cytoplasmic ribonucleoprotein granule	Chymase	Homo sapiens (human)
collagen-containing extracellular matrix	Chymase	Homo sapiens (human)
extracellular space	Chymase	Homo sapiens (human)
intracellular membrane-bounded organelle	Chymase	Homo sapiens (human)
cytoplasm	Chymase	Homo sapiens (human)
extracellular region	Trypsin-3	Homo sapiens (human)
extracellular space	Trypsin-3	Homo sapiens (human)
tertiary granule lumen	Trypsin-3	Homo sapiens (human)
extracellular space	Trypsin-3	Homo sapiens (human)
virion membrane	Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus
extracellular region	Dipeptidyl peptidase 2	Homo sapiens (human)
Golgi apparatus	Dipeptidyl peptidase 2	Homo sapiens (human)
azurophil granule lumen	Dipeptidyl peptidase 2	Homo sapiens (human)
intracellular membrane-bounded organelle	Dipeptidyl peptidase 2	Homo sapiens (human)
extracellular exosome	Dipeptidyl peptidase 2	Homo sapiens (human)
vesicle	Dipeptidyl peptidase 2	Homo sapiens (human)
vesicle	Dipeptidyl peptidase 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (272)

Assay ID	Title	Year	Journal	Article
AID1225915	Inhibition of Klebsiella pneumoniae KP1004 TEM-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1588035	Inhibition of recombinant bacterial L1 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1559335	Inhibition of KPC-2/SHV12/TEM-1 in Klebsiella pneumoniae CDC-0361 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 32 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225780	Inhibition of Enterobacter cloacae ECL1003 TEM assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559327	Inhibition of KPC-2/SHV12/TEM-1 in Klebsiella pneumoniae CDC-0361 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225857	Clearance in human at 1 g administered as 3 hrs of infusion	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1832299	Inhibition of Pseudomonas aeruginosa PBP3 using bocillin FL as a fluorogenic substrate assessed as residual activity at 1 mM preincubated for 1 hr followed by substrate addition measured after 30 mins by fluorescence anisotropy assay relative to control	2021	Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15	High-Throughput Crystallography Reveals Boron-Containing Inhibitors of a Penicillin-Binding Protein with Di- and Tricovalent Binding Modes.
AID1471284	Inhibition of bacterial CTX-M by measuring nitrocefin degradation	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Pharmaceutical Approaches to Target Antibiotic Resistance Mechanisms.
AID1588033	Inhibition of recombinant bacterial VIM-2 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1864429	Inhibition of NLRP3 inflammasome activation in LPS-primed mouse J774.A1 cells assessed as reduction in IL-1beta secretion at 1 uM relative to control	2022	Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18	Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity.
AID1225912	Inhibition of Klebsiella oxytoca KX1017 OXA-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1891032	Potentiation of aztreonam-induced antibacterial activity against Escherichia coli 1010 producing CMY-6 assessed as concentration required to reduce aztreonam MIC to 4 ug/ml by CLSI based broth microdilution method	2022	Bioorganic & medicinal chemistry, 05-15, Volume: 62	Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability.
AID1891021	Potentiation of aztreonam-induced antibacterial activity against Escherichia coli 308 producing SHV-5 assessed as concentration required to reduce aztreonam MIC to 4 ug/ml by CLSI based broth microdilution method	2022	Bioorganic & medicinal chemistry, 05-15, Volume: 62	Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability.
AID1657154	Inhibition of recombinant Escherichia coli NDM-1 using imipenem as substrate preincubated for 10 mins followed by substrate addition and measured every 30 secs for 30 mins by spectrophotometric analysis	2020	Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14	Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases.
AID1559329	Inhibition of KPC-2/PDC-42 in Pseudomonas aeruginosa CDC-0457 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 64 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225764	Inhibition of Escherichia coli recombinant CMY-2 assessed as substrate nitrocefin degradation preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559308	Inhibition of bacterial KPC-2 using imipenem as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1695048	Irreversible inhibition of beta lactamase KPC-2 in Klebsiella pneumoniae assessed as off-rate constant using nitrocefin as substrate preincubated for 30 mins followed by substrate addition	2020	RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4	Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition.
AID1225825	Cmax in rat at 100 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225937	Inhibition of Klebsiella oxytoca KX1019 KPC-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225753	Inhibition of Klebsiella pneumoniae KP1088 KPC-3 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225827	Inhibition of plasmin (unknown origin) using H-D-VLK-pNA as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1471283	Inhibition of bacterial KPC by measuring nitrocefin degradation	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Pharmaceutical Approaches to Target Antibiotic Resistance Mechanisms.
AID1225747	Inhibition of Klebsiella pneumoniae KP1008 KPC-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559343	Inhibition of KPC-2/SHV12/TEM-1 in Klebsiella pneumoniae CDC-0361 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 16 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225758	Antibacterial activity against Klebsiella pneumoniae KP1004 by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559341	Inhibition of OXA-232/OXA-9/TEM-1A/CTX-M-15/OXA-1 in Klebsiella pneumoniae CDC-0066 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 32 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225925	Inhibition of Klebsiella pneumoniae KP1088 TEM-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225891	Inhibition of Klebsiella pneumoniae KP1088 SHV-11 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225918	Inhibition of Klebsiella pneumoniae KP1082 KPC-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225812	Inhibition of Enterobacter cloacae ECL1058 TEM-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225907	Inhibition of Enterobacter cloacae ECL1058 SHV-11 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225928	Inhibition of Klebsiella pneumoniae KP1084 TEM-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1471285	Inhibition of bacterial SHV by measuring nitrocefin degradation	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Pharmaceutical Approaches to Target Antibiotic Resistance Mechanisms.
AID1225833	Inhibition of dipeptidyl peptidase 7 (unknown origin) using H-Lys-Pro-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1525845	Inhibition of bacterial class B1 metallo beta-lactamase NDM-1 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method	2019	Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18	Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.
AID1525846	Inhibition of bacterial class B1 metallo beta-lactamase VIM-1 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method	2019	Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18	Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.
AID1225820	Inhibition of Klebsiella pneumoniae KP1084 TEM-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225892	Inhibition of Klebsiella pneumoniae KP1088 TEM-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225848	Clearance in rat at 1000 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225870	Inhibition of Enterobacter cloacae EC1010 CMY-6 assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225824	Inhibition of chymotrypsin (unknown origin) using Suc-AAPF-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225943	Inhibition of Klebsiella pneumoniae KP1004 TEM-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225809	Inhibition of Klebsiella oxytoca KX1017 OXA-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225858	Volume of distribution at steady state in human at 1 g administered as 3 hrs of infusion	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225894	Inhibition of Klebsiella pneumoniae KP1083 TEM-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1695046	Inhibition of beta lactamase KPC-2 in Klebsiella pneumoniae assessed as apparent inhibition constant using nitrocefin as substrate measured without preincubation by Dixon plot analysis	2020	RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4	Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition.
AID1225830	Inhibition of elastase (unknown origin) using Suc-AAPA-pNA as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1525843	Inhibition of bacterial class A serine beta-lactamase TEM-116 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method	2019	Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18	Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.
AID1588027	Inhibition of Escherichia coli TEM-116 assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1225823	Inhibition of trypsin (unknown origin) using N-Bz-R-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225883	Inhibition of Klebsiella pneumoniae KP1004 SHV-11 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1588044	Inhibition of NDM1 in Klebsiella pneumoniae B64 clinical isolate assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC at 8 ug/ml by broth microdilution method (Rvb > 64 ug/ml)	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1225846	Half life in rat at 1000 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559323	Inhibition of VIM-27/CTX-M-15/SHV-11/OXA-1 in Klebsiella pneumoniae CDC-0040 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225813	Inhibition of Enterobacter cloacae ECL1058 SHV-11 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225899	Inhibition of Klebsiella pneumoniae KP1084 SHV-11 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1588029	Inhibition of recombinant bacterial KPC-2 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1225835	Inhibition of cathepsin A (unknown origin) using MCA-RPPGFSAFK-Dnp as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1529342	Inhibition of beta lactamase KPC in Enterobacteriaceae assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC by broth microdilution method	2018	MedChemComm, Sep-01, Volume: 9, Issue:9	β-lactam/β-lactamase inhibitor combinations: an update.
AID1225933	Inhibition of Escherichia coli EC1007 KPC-3 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225941	Inhibition of Klebsiella oxytoca KX1017 SHV-30 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1588042	Inhibition of NDM1 in Escherichia coli S117 clinical isolate assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC at 8 ug/ml by broth microdilution method (Rvb > 64 ug/ml)	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1225923	Inhibition of Klebsiella pneumoniae KP1088 KPC-3 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1183472	Inhibition of beta-lactamase (unknown origin)	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Confronting the challenges of discovery of novel antibacterial agents.
AID1225917	Inhibition of Klebsiella pneumoniae KP1008 KPC-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1588034	Inhibition of recombinant bacterial CphA expressed in Escherichia coli assessed as reduction in hydrolysis of meropenem by UV spectrophotometeric analysis	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1525848	Inhibition of Aeromonas hydrophila class B2 metallo beta-lactamse CphA assessed as reduction in meropenem hydrolysis after 10 mins by UV absorbance method	2019	Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18	Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.
AID1225800	Inhibition of Klebsiella pneumoniae KP1083 KPC-3 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225888	Inhibition of Klebsiella pneumoniae KP1083 SHV-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1588043	Inhibition of NDM1 in Escherichia coli IR57 clinical isolate assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC at 8 ug/ml by broth microdilution method (Rvb > 64 ug/ml)	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1559320	Inhibition of bacterial NDM-1 using cefepime as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225930	Inhibition of Klebsiella pneumoniae KP1087 CTX-M-15 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225804	Inhibition of Klebsiella pneumoniae KP1004 SHV-11 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225808	Inhibition of Klebsiella oxytoca KX1017 KPC-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225901	Inhibition of Klebsiella pneumoniae KP1087 KPC-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1525854	Inhibition of bacterial class D serine beta-lactamase OXA-48 assessed as reduction in breakdown of cephalosporin FC-5 in presence of aqueous sodium bicarbonate after 10 mins by fluorescence method	2019	Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18	Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.
AID1225863	Inhibition of Klebsiella pneumoniae KP1005 CTX-M-14 assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225748	Inhibition of Klebsiella pneumoniae KP1082 KPC-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225851	In vivo inhibition of KPC in Klebsiella pneumoniae KP1074 in Swiss webster neutropenic mouse lung infection model assessed as biapenem deltalog10CFU in lung at 50 mg/kg, ip administered every 2 hrs starting at 2 hrs postinfection measured after 24 hrs	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225836	Half life in rat at 100 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225898	Inhibition of Klebsiella pneumoniae KP1084 KPC-3 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225842	Volume of distribution in rat at 300 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225900	Inhibition of Klebsiella pneumoniae KP1084 TEM-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1529341	Inhibition of beta lactamase KPC in Klebsiella pneumoniae BAA-1705 assessed as potentiation of meropenem-induced antibacterial activity by measuring fold reduction in meropenem MIC90 by checkerboard microdilution assay relative to meropenem alone	2018	MedChemComm, Sep-01, Volume: 9, Issue:9	β-lactam/β-lactamase inhibitor combinations: an update.
AID1225822	Inhibition of Klebsiella pneumoniae KP1084 SHV-11 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225940	Inhibition of Klebsiella oxytoca KX1017 OXA-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1471286	Inhibition of bacterial CMY by measuring nitrocefin degradation	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Pharmaceutical Approaches to Target Antibiotic Resistance Mechanisms.
AID1225871	Inhibition of Klebsiella oxytoca KX1001 OXA-2 assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225862	Inhibition of Escherichia coli EC1008 CTX-M-3 assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225803	Inhibition of Klebsiella pneumoniae KP1008 KPC-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225868	Inhibition of Enterobacter cloacae ECL1061 AmpC assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1657157	Inhibition of recombinant Escherichia coli SHV-12 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis	2020	Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14	Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases.
AID1225840	AUC (0 to infinity) in rat at 300 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1695050	Potentiation of cefepime-induced antibacterial activity against Klebsiella pneumoniae Ecl8 transfected with pUBYT vector expressing KPC-2 assessed as cefepime MIC measured after 18 to 24 hrs by CLSI protocol based broth microdilution assay (Rvb >=256 ug/m	2020	RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4	Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition.
AID1225872	Inhibition of Enterobacter aerogenes EA1028 OXA-30 assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1695047	Inhibition of beta lactamase KPC-2 in Klebsiella pneumoniae assessed as apparent second order rate constant K2/K using nitrocefin as substrate	2020	RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4	Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition.
AID1225875	Inhibition of Enterobacter cloacae ECL1058 TEM-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225854	Cmax in human at 1 g administered as 3 hrs of infusion	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225935	Inhibition of Enterobacter cloacae ECL1058 SHV-11 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225893	Inhibition of Klebsiella pneumoniae KP1083 SHV-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1529340	Inhibition of beta lactamase KPC in Klebsiella pneumoniae BAA-1705 assessed as potentiation of meropenem-induced antibacterial activity by measuring fold reduction in meropenem MIC50 by checkerboard microdilution assay relative to meropenem alone	2018	MedChemComm, Sep-01, Volume: 9, Issue:9	β-lactam/β-lactamase inhibitor combinations: an update.
AID1225884	Inhibition of Klebsiella pneumoniae KP1008 KPC-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225887	Inhibition of Klebsiella pneumoniae KP1083 KPC-3 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1588047	Inhibition of NDM1 in Escherichia coli 91N clinical isolate assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC at 8 ug/ml by broth microdilution method (Rvb > 64 ug/ml)	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1559345	Inhibition of KPC-2/PDC-42 in Pseudomonas aeruginosa CDC-0457 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 128 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1657155	Inhibition of recombinant Escherichia coli CTX-M-14 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis	2020	Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14	Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases.
AID1225914	Inhibition of Klebsiella pneumoniae KP1004 KPC-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1657156	Inhibition of recombinant Escherichia coli TEM-10 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis	2020	Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14	Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases.
AID1225942	Inhibition of Klebsiella pneumoniae KP1004 KPC-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225903	Inhibition of Klebsiella pneumoniae KP1087 SHV-11 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559317	Inhibition of bacterial CTX-M-15 using cefotaxime as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1559342	Inhibition of KPC-2/PDC-42 in Pseudomonas aeruginosa CDC-0356 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 32 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225845	AUC (0 to infinity) in rat at 1000 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225880	Inhibition of Klebsiella oxytoca KX1017 SHV-30 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1891030	Potentiation of aztreonam-induced antibacterial activity against Klebsiella pneumoniae 1004 producing KPC assessed as concentration required to reduce aztreonam MIC to 4 ug/ml by CLSI based broth microdilution method	2022	Bioorganic & medicinal chemistry, 05-15, Volume: 62	Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability.
AID1225761	Inhibition of Escherichia coli recombinant SHV-12 assessed as substrate nitrocefin degradation preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225882	Inhibition of Klebsiella pneumoniae KP1004 TEM-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1657161	Inhibition of recombinant Escherichia coli VIM-1 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis	2020	Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14	Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases.
AID1225779	Inhibition of Escherichia coli EC1011 TEM-26 assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225843	Clearance in rat at 300 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225806	Inhibition of Klebsiella pneumoniae KP1004 KPC-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559337	Inhibition of KPC-2/PDC-42 in Pseudomonas aeruginosa CDC-0457 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 16 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1525844	Inhibition of bacterial class B1 metallo beta-lactamase IMP-1 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method	2019	Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18	Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.
AID1225817	Inhibition of Klebsiella pneumoniae KP1087 SHV-11 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225756	In vivo inhibition of KPC in Klebsiella pneumoniae KP1074 in Swiss webster neutropenic mouse lung infection model assessed as meropenem deltalog10CFU in lung at 50 mg/kg, ip administered every 2 hrs starting at 2 hrs postinfection measured after 24 hrs	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1588031	Inhibition of recombinant bacterial NDM-1 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1588038	Inhibition of recombinant Escherichia coli OXA-10 assessed as reduction in breakdown of cephalosporin FC-5 in presence of 100 mM NaHCO3 by fluorescence method	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1225876	Inhibition of Klebsiella oxytoca KX1019 KPC-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225926	Inhibition of Klebsiella pneumoniae KP1084 KPC-3 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225909	Inhibition of Klebsiella oxytoca KX1019 KPC-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559309	Inhibition of bacterial AmpC using nitrocefin as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1559316	Inhibition of bacterial SHV-5 using cefotaxime as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225896	Inhibition of Klebsiella pneumoniae KP1088 SHV-11 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1695045	Inhibition of beta lactamase KPC-2 in Klebsiella pneumoniae using nitrocefin as substrate preincubated for 10 mins followed by substrate addition	2020	RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4	Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition.
AID1225905	Inhibition of Escherichia coli EC1007 KPC-3 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225844	Cmax in rat at 1000 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225819	Inhibition of Klebsiella pneumoniae KP1087 KPC-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1891031	Potentiation of aztreonam-induced antibacterial activity against Enterobacter cloacae 1002 producing AmpC assessed as concentration required to reduce aztreonam MIC to 4 ug/ml by CLSI based broth microdilution method	2022	Bioorganic & medicinal chemistry, 05-15, Volume: 62	Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability.
AID1225749	Inhibition of Klebsiella pneumoniae KP1082 SHV-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225754	Inhibition of Klebsiella pneumoniae KP1088 SHV-11 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225796	Inhibition of Klebsiella pneumoniae KP1087 CTX-M-15 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1695049	Inhibition of beta lactamase KPC-2 in Klebsiella pneumoniae assessed as irreversible covalent complex formation by measuring half life using nitrocefin as substrate	2020	RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4	Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition.
AID1588030	Inhibition of recombinant bacterial IMP-1 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1559339	Inhibition of VIM-27/CTX-M-15/SHV-11/OXA-1 in Klebsiella pneumoniae CDC-0040 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225807	Inhibition of Klebsiella oxytoca KX1017 SHV-30 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1695051	Potentiation of meropenem-induced antibacterial activity against Klebsiella pneumoniae Ecl8 transfected with pUBYT vector expressing KPC-2 assessed as meropenem MIC measured after 18 to 24 hrs by CLSI protocol based broth microdilution assay (Rvb = 16 ug/	2020	RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4	Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition.
AID1225798	Inhibition of Klebsiella pneumoniae KP1087 TEM-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225861	Inhibition of Enterobacter cloacae ECL1003 SHV assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1588037	Inhibition of recombinant bacterial OXA-10 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1225794	Inhibition of Klebsiella pneumoniae KP1084 TEM-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225834	Inhibition of neutrophil elastase (unknown origin) using MeOSuc-AAVP-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225810	Inhibition of Klebsiella oxytoca KX1019 OXA-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1657158	Inhibition of recombinant Escherichia coli AmpC using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis	2020	Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14	Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases.
AID1525849	Inhibition of Stenotrophomonas maltophilia class B3 metallo beta-lactamse L1 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method	2019	Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18	Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.
AID1225847	Volume of distribution in rat at 1000 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1657160	Inhibition of Acinetobacter baumannii OXA-23 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis	2020	Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14	Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases.
AID1559319	Inhibition of bacterial OXA-1 using nitrocefin as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225760	Inhibition of Escherichia coli recombinant CTX-M-15 assessed as substrate nitrocefin degradation preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225913	Inhibition of Klebsiella oxytoca KX1017 SHV-30 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225866	Inhibition of Klebsiella pneumoniae KP1010 SHV-12 assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225885	Inhibition of Klebsiella pneumoniae KP1082 KPC-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225752	Inhibition of Klebsiella pneumoniae KP1083 TEM-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225757	Inhibition of Klebsiella pneumoniae KP1004 KPC 2 carbapenemase assessed as minimum concentration required to reduce biapenem MIC from 32 ug/ml to 1 ug/mL by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559333	Inhibition of OXA-232/OXA-9/TEM-1A/CTX-M-15/OXA-1 in Klebsiella pneumoniae CDC-0066 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1588032	Inhibition of recombinant bacterial VIM-1 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1225904	Inhibition of Klebsiella pneumoniae KP1087 TEM-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225816	Inhibition of Klebsiella pneumoniae KP1087 TEM-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225877	Inhibition of Klebsiella oxytoca KX1019 OXA-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559336	Inhibition of NDM in Escherichia coli CDC-0452 assessed as cefepime antibacterial activity after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 64 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225879	Inhibition of Klebsiella oxytoca KX1017 OXA-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225890	Inhibition of Klebsiella pneumoniae KP1088 KPC-3 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225908	Inhibition of Enterobacter cloacae ECL1058 TEM-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559325	Inhibition of OXA-232/OXA-9/TEM-1A/CTX-M-15/OXA-1 in Klebsiella pneumoniae CDC-0066 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1832314	Inhibition of Pseudomonas aeruginosa PBP3 using bocillin FL as a fluorogenic substrate assessed as inhibition constant at 1 to 1024 uM preincubated for 1 hr followed by substrate addition measured after 30 mins by fluorescence anisotropy assay	2021	Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15	High-Throughput Crystallography Reveals Boron-Containing Inhibitors of a Penicillin-Binding Protein with Di- and Tricovalent Binding Modes.
AID1225792	Inhibition of Klebsiella pneumoniae KP1084 KPC-3 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1588045	Inhibition of NDM1 in Klebsiella pneumoniae B68-1 clinical isolate assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC at 8 ug/ml by broth microdilution method (Rvb > 64 ug/ml)	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1525850	Inhibition of Pseudomonas aeruginosa class C serine beta-lactamase AmpC assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method	2019	Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18	Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.
AID1225799	Inhibition of Escherichia coli EC1007 KPC-3 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559321	Inhibition of bacterial IMP-1 using nitrocefin as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225881	Inhibition of Klebsiella pneumoniae KP1004 KPC-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225821	Inhibition of Klebsiella pneumoniae KP1084 KPC-3 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225916	Inhibition of Klebsiella pneumoniae KP1004 SHV-11 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225763	Inhibition of Escherichia coli recombinant P99 assessed as substrate nitrocefin degradation preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225829	Inhibition of urokinase (unknown origin) using NGK-pNA as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559338	Inhibition of KPC-2 in Klebsiella pneumoniae ATCC BAA 1705 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 16 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225755	Inhibition of Klebsiella pneumoniae KP1088 TEM-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225931	Inhibition of Klebsiella pneumoniae KP1087 SHV-11 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1588036	Inhibition of recombinant bacterial AmpC expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1225828	Inhibition of thrombin (unknown origin) using Benz-FVR-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225865	Inhibition of Klebsiella pneumoniae KP1011 SHV5 assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1588041	Inhibition of bacterial expressed in Escherichia coli OXA-10 assessed as reduction in breakdown of cephalosporin FC-5 at 400 uM by fluorescence method	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1559330	Inhibition of KPC-2 in Klebsiella pneumoniae ATCC BAA 1705 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 16 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1525847	Inhibition of bacterial class B1 metallo beta-lactamse VIM-2 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method	2019	Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18	Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.
AID1225906	Inhibition of Enterobacter cloacae ECL1058 KPC-3 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225938	Inhibition of Klebsiella oxytoca KX1019 OXA-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225814	Inhibition of Enterobacter cloacae ECL1058 KPC-3 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225751	Inhibition of Klebsiella pneumoniae KP1083 SHV-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225811	Inhibition of Klebsiella oxytoca KX1019 KPC-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225895	Inhibition of Klebsiella pneumoniae KP1088 KPC-3 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225852	Toxicity in Swiss webster neutropenic mouse lung infection model up to 1000 mg/kg, administered every 2 hrs starting at 2 hrs	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225927	Inhibition of Klebsiella pneumoniae KP1084 SHV-11 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225853	Toxicity in human at 250 to 1500 mg administered as 3 hrs of infusion	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1657152	Inhibition of recombinant Escherichia coli KPC-2 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition and measured every 10 secs for 10 mins by spectrophotometric analysis	2020	Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14	Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases.
AID1559332	Inhibition of NDM-1/CMY-6/OXA-1 in Escherichia coli CDC-0055 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 128 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225795	Inhibition of Klebsiella pneumoniae KP1087 KPC-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225746	Inhibition of Klebsiella pneumoniae KP1004 SHV-11 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1891047	Oral bioavailability in rat	2022	Bioorganic & medicinal chemistry, 05-15, Volume: 62	Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability.
AID1657162	Inhibition of recombinant Escherichia coli IMP-1 using imipenem as substrate preincubated for 10 mins followed by substrate addition measured every 30 secs for 30 mins by spectrophotometrically analysis	2020	Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14	Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases.
AID1225805	Inhibition of Klebsiella pneumoniae KP1004 TEM-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225801	Inhibition of Klebsiella pneumoniae KP1082 SHV-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559340	Inhibition of NDM-1/CMY-6/OXA-1 in Escherichia coli CDC-0055 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 32 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225939	Inhibition of Klebsiella oxytoca KX1017 KPC-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1891028	Potentiation of aztreonam-induced antibacterial activity against Klebsiella pneumoniae 1009 producing class A CTX-M-14 assessed as concentration required to reduce aztreonam MIC to 4 ug/ml by CLSI based broth microdilution method	2022	Bioorganic & medicinal chemistry, 05-15, Volume: 62	Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability.
AID1225855	Half life in human at 1 g administered as 3 hrs of infusion	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1657159	Inhibition of Acinetobacter baumannii OXA-48 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis	2020	Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14	Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases.
AID1225869	Inhibition of Enterobacter cloacae ECL1061 KPC-3 assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225897	Inhibition of Klebsiella pneumoniae KP1088 TEM-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225924	Inhibition of Klebsiella pneumoniae KP1088 SHV-11 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225815	Inhibition of Escherichia coli EC1007 KPC-3 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225874	Inhibition of Enterobacter cloacae ECL1058 SHV-11 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559326	Inhibition of KPC-2/PDC-42 in Pseudomonas aeruginosa CDC-0356 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1832301	Inhibition of Pseudomonas aeruginosa PBP3 using (2-((benzoyl-D-alanyl)thio)acetic acid) as a substrate assessed as residual activity by measuring substrate turnover at 1 mM incubated for 1 hr followed by substrate addition by absorbance based assay relati	2021	Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15	High-Throughput Crystallography Reveals Boron-Containing Inhibitors of a Penicillin-Binding Protein with Di- and Tricovalent Binding Modes.
AID1225919	Inhibition of Klebsiella pneumoniae KP1082 SHV-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225902	Inhibition of Klebsiella pneumoniae KP1087 CTX-M-15 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225826	AUC (0 to infinity) in rat at 100 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559331	Inhibition of VIM-27/CTX-M-15/SHV-11/OXA-1 in Klebsiella pneumoniae CDC-0040 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1559344	Inhibition of NDM in Escherichia coli CDC-0452 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 32 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225818	Inhibition of Klebsiella pneumoniae KP1087 CTX-M-15 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225832	Inhibition of chymase (unknown origin) using Suc-AAPF-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225841	Half life in rat at 300 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225922	Inhibition of Klebsiella pneumoniae KP1083 TEM-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559322	Inhibition of KPC-2 in Klebsiella pneumoniae ATCC BAA 1705 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225762	Inhibition of Escherichia coli recombinant TEM-10 assessed as substrate nitrocefin degradation preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559328	Inhibition of NDM in Escherichia coli CDC-0452 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1588039	Inhibition of recombinant Escherichia coli OXA-48 assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1225797	Inhibition of Klebsiella pneumoniae KP1087 SHV-11 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225936	Inhibition of Enterobacter cloacae ECL1058 TEM-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225837	Volume of distribution in rat at 100 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1588046	Inhibition of NDM1 in Klebsiella pneumoniae IR43 clinical isolate assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC at 8 ug/ml by broth microdilution method (Rvb > 64 ug/ml)	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1225838	Clearance in rat at 100 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225889	Inhibition of Klebsiella pneumoniae KP1083 TEM-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225934	Inhibition of Enterobacter cloacae ECL1058 KPC-3 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559311	Inhibition of bacterial VIM-2 using nitrocefin as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225778	Inhibition of Escherichia coli EC1009 TEM-10 assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225929	Inhibition of Klebsiella pneumoniae KP1087 KPC-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225856	AUC in human at 1 g administered as 3 hrs of infusion	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1525851	Inhibition of bacterial class D serine beta-lactamase OXA-10 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method	2019	Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18	Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.
AID1225759	Inhibition of Escherichia coli recombinant KPC-2 assessed as substrate nitrocefin degradation preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225910	Inhibition of Klebsiella oxytoca KX1019 OXA-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225839	Cmax in rat at 300 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225921	Inhibition of Klebsiella pneumoniae KP1083 SHV-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225878	Inhibition of Klebsiella oxytoca KX1017 KPC-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559324	Inhibition of NDM-1/CMY-6/OXA-1 in Escherichia coli CDC-0055 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1891029	Potentiation of aztreonam-induced antibacterial activity against Escherichia coli 302 producing TEM-10 assessed as concentration required to reduce aztreonam MIC to 4 ug/ml by CLSI based broth microdilution method	2022	Bioorganic & medicinal chemistry, 05-15, Volume: 62	Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability.
AID1588040	Inhibition of recombinant Escherichia coli OXA-48 assessed as reduction in breakdown of cephalosporin FC-5 in presence of 100 mM NaHCO3 by fluorescence method	2019	Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15	Profiling interactions of vaborbactam with metallo-β-lactamases.
AID1559310	Inhibition of bacterial OXA-48 using nitrocefin as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225802	Inhibition of Klebsiella pneumoniae KP1082 KPC-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225873	Inhibition of Enterobacter cloacae ECL1058 KPC-3 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225886	Inhibition of Klebsiella pneumoniae KP1082 SHV-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1525852	Inhibition of bacterial class D serine beta-lactamase OXA-10 assessed as reduction in breakdown of cephalosporin FC-5 in presence of aqueous sodium bicarbonate after 10 mins by fluorescence method	2019	Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18	Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.
AID1559318	Inhibition of bacterial CMY-2 using nitrocefin as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1225793	Inhibition of Klebsiella pneumoniae KP1084 SHV-11 assessed as biapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225867	Inhibition of Enterobacter cloacae ECL1002 AmpC assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225750	Inhibition of Klebsiella pneumoniae KP1083 KPC-3 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225932	Inhibition of Klebsiella pneumoniae KP1087 TEM-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225831	Inhibition of tissue plasminogen activator (unknown origin) using GK-pNA as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225920	Inhibition of Klebsiella pneumoniae KP1083 KPC-3 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225864	Inhibition of Klebsiella pneumoniae KP1009 CTX-M-15 assessed as cefepime MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1559334	Inhibition of KPC-2/PDC-42 in Pseudomonas aeruginosa CDC-0356 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml)	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
AID1525853	Inhibition of bacterial class D serine beta-lactamase OXA-48 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method	2019	Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18	Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.
AID1225911	Inhibition of Klebsiella oxytoca KX1017 KPC-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (99)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	36 (36.36)	24.3611
2020's	63 (63.64)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.76

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	17.76 (24.57)
Research Supply Index	4.65 (2.92)
Research Growth Index	4.79 (4.65)
Search Engine Demand Index	15.26 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (17.76)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	4 (4.00%)	5.53%
Reviews	14 (14.00%)	6.00%
Case Studies	3 (3.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	79 (79.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
aztreonam Aztreonam: A monocyclic beta-lactam antibiotic originally isolated from Chromobacterium violaceum. It is resistant to beta-lactamases and is used in gram-negative infections, especially of the meninges, bladder, and kidneys. It may cause a superinfection with gram-positive organisms.. aztreonam : A synthetic monocyclic beta-lactam antibiotic (monobactam), used primarily to treat infections caused by Gram-negative bacteria. It inhibits mucopeptide synthesis in the bacterial cell wall, thereby blocking peptidoglycan crosslinking.	3.33	4	0
cefuroxime Cefuroxime: Broad-spectrum cephalosporin antibiotic resistant to beta-lactamase. It has been proposed for infections with gram-negative and gram-positive organisms, GONORRHEA, and HAEMOPHILUS.. cefuroxime : A 3-(carbamoyloxymethyl)cephalosporin compound having a 7-(2Z)-2-(furan-2-yl)-2-(methoxyimino)acetamido side chain.	2.25	1	0	carbamate ester; cephalosporin
isoniazid Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC).	2.6	1	0	carbohydrazide	antitubercular agent; drug allergen
metronidazole Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death.	2.17	1	0	C-nitro compound; imidazoles; primary alcohol	antiamoebic agent; antibacterial drug; antimicrobial agent; antiparasitic agent; antitrichomonal drug; environmental contaminant; prodrug; radiosensitizing agent; xenobiotic
reserpine Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.	2.15	1	0	alkaloid ester; methyl ester; yohimban alkaloid	adrenergic uptake inhibitor; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; first generation antipsychotic; plant metabolite; xenobiotic
oxacillin Oxacillin: An antibiotic similar to FLUCLOXACILLIN used in resistant staphylococci infections.. oxacillin : A penicillin antibiotic carrying a 5-methyl-3-phenylisoxazole-4-carboxamide group at position 6beta.	2.25	1	0	penicillin	antibacterial agent; antibacterial drug
penicillanic acid Penicillanic Acid: A building block of penicillin, devoid of significant antibacterial activity. (From Merck Index, 11th ed). penicillanic acid : A penam that consists of 3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane bearing a carboxy group at position 2 and having (2S,5R)-configuration.	4.48	1	1	penicillanic acids
quinazolines Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.	2.17	1	0	azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines
azomycin azomycin: RN given refers to parent cpd with specified locant; structure	3.73	2	0	C-nitro compound; imidazoles	antitubercular agent
phenyl acetate phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid.	2.17	1	0	benzenes; phenyl acetates
benzonidazole benzonidazole: used in treatment of Chagas' disease. benznidazole : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2-nitroimidazol-1-yl)acetic acid with the aromatic amino group of benzylamine. Used for treatment of Chagas disease.	2.17	1	0	C-nitro compound; imidazoles; monocarboxylic acid amide	antiprotozoal drug
sisomicin Sisomicin: Antibiotic produced by Micromonospora inyoensis. It is closely related to gentamicin C1A, one of the components of the gentamicin complex (GENTAMICINS).	4.54	3	0	amino cyclitol glycoside; aminoglycoside antibiotic; beta-L-arabinoside; monosaccharide derivative
piperacillin Piperacillin: Semisynthetic, broad-spectrum, AMPICILLIN derived ureidopenicillin antibiotic proposed for PSEUDOMONAS infections. It is also used in combination with other antibiotics.. piperacillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-[(4-ethyl-2,3-dioxopiperazin-1-yl)carboxamido]-2-phenylacetamido group.	5.2	3	1	penicillin allergen; penicillin	antibacterial drug
cephalosporin c cephalosporin C: RN given refers to parent cpd; structure in Merck, 9th ed, #1937. cephalosporin C : A cephalosporin antibiotic carrying a 3-acetoxymethyl substituent and a 6-oxo-N(6)-L-lysino group at position 7.	5.05	9	0	cephalosporin	fungal metabolite
benzeneboronic acid [no description available]	2.25	1	0	boronic acids
ljc 10627 biapenem: structure given in first source. biapenem : A carbapenem antibiotic in which the azetidine and pyrroline rings carry 1-hydroxymethyl and pyrazolo[1,2-a][1,2,4]triazolium-6-ylthio substituents respectively.	2.11	1	0	carbapenems; organic sulfide; pyrazolotriazole	antibacterial drug
secnidazole [no description available]	2.17	1	0	C-nitro compound; imidazoles; secondary alcohol	epitope
doripenem Doripenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS.	2.6	1	0	carbapenems
imipenem, anhydrous Imipenem: Semisynthetic thienamycin that has a wide spectrum of antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, including many multiresistant strains. It is stable to beta-lactamases. Clinical studies have demonstrated high efficacy in the treatment of infections of various body systems. Its effectiveness is enhanced when it is administered in combination with CILASTATIN, a renal dipeptidase inhibitor.. imipenem : A broad-spectrum, intravenous beta-lactam antibiotic of the carbapenem subgroup.	6.41	22	0	beta-lactam antibiotic allergen; carbapenems; zwitterion	antibacterial drug
tazobactam Tazobactam: A penicillanic acid and sulfone derivative and potent BETA-LACTAMASE inhibitor that enhances the activity of other anti-bacterial agents against beta-lactamase producing bacteria.. tazobactam : A member of the class of penicillanic acids that is sulbactam in which one of the exocyclic methyl hydrogens is replaced by a 1,2,3-triazol-1-yl group; used (in the form of its sodium salt) in combination with ceftolozane sulfate for treatment of complicated intra-abdominal infections and complicated urinary tract infections.	5.04	10	0	penicillanic acids; triazoles	antiinfective agent; antimicrobial agent; EC 3.5.2.6 (beta-lactamase) inhibitor
pyrrolomycin d pyrrolomycin D: from Streptomyces strain SF-2080; structure given in first source	2.15	1	0
carbapenems [no description available]	4.37	14	0
beta-lactams 2-azetidinone: structure in first source. azetidin-2-one : An unsubstituted beta-lactam compound.. beta-lactam : A lactam in which the amide bond is contained within a four-membered ring, which includes the amide nitrogen and the carbonyl carbon.	2.66	2	0	beta-lactam antibiotic allergen; beta-lactam
ertapenem Ertapenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of Gram-positive and Gram-negative bacterial infections including intra-abdominal infections, acute gynecological infections, complicated urinary tract infections, skin infections, and respiratory tract infections. It is also used to prevent infection in colorectal surgery.. ertapenem : Meropenem in which the one of the two methyl groups attached to the amide nitrogen is replaced by hydrogen while the other is replaced by a 3-carboxyphenyl group. The sodium salt is used for the treatment of moderate to severe susceptible infections including intra-abdominal and acute gynaecological infections, pneumonia, and infections of the skin and of the urinary tract.	2.11	1	0	carbapenemcarboxylic acid; pyrrolidinecarboxamide	antibacterial drug
moxifloxacin Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.	2.6	1	0	aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone	antibacterial drug
bortezomib [no description available]	2.41	1	0	amino acid amide; L-phenylalanine derivative; pyrazines	antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor
meropenem Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively.	12.82	82	3	alpha,beta-unsaturated monocarboxylic acid; carbapenemcarboxylic acid; organic sulfide; pyrrolidinecarboxamide	antibacterial agent; antibacterial drug; drug allergen
linezolid [no description available]	2.6	1	0	acetamides; morpholines; organofluorine compound; oxazolidinone	antibacterial drug; protein synthesis inhibitor
phenylalanine arginine beta-naphthylamide phenylalanine arginine beta-naphthylamide: a drug efflux pump inhibitor; structure in first source	2.15	1	0	peptide
fosfomycin Fosfomycin: An antibiotic produced by Streptomyces fradiae.. fosfomycin : A phosphonic acid having an (R,S)-1,2-epoxypropyl group attached to phosphorus.	2.6	1	0	epoxide; phosphonic acids	antimicrobial agent; EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor
pa 824 pretomanid: nitroimidazopyran derived from 5-nitroimidazoles; a prodrug that requires activation by a bacterial F420-depedent glucose-6-phosphate dehydrogenase (Fgd) and nitroreductase to activate components that then inhibit bacterial mycolic acid and protein synthesis; structure in first source	3.41	1	0
abt 492 WQ 3034: structure in first source	4.03	3	0
1-(1-naphthylmethyl)piperazine [no description available]	2.15	1	0
capsaicin ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief. capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers.	2.15	1	0	capsaicinoid	non-narcotic analgesic; TRPV1 agonist; voltage-gated sodium channel blocker
clavulanic acid Clavulanic Acid: A beta-lactam antibiotic produced by the actinobacterium Streptomyces clavuligerus. It is a suicide inhibitor of bacterial beta-lactamase enzymes. Administered alone, it has only weak antibacterial activity against most organisms, but given in combination with other beta-lactam antibiotics it prevents antibiotic inactivation by microbial lactamase.. clavulanate : The conjugate base of clavulanic acid.. clavulanic acid : Antibiotic isolated from Streptomyces clavuligerus. It acts as a suicide inhibitor of bacterial beta-lactamase enzymes.	2.57	2	0	oxapenam	antibacterial drug; anxiolytic drug; bacterial metabolite; EC 3.5.2.6 (beta-lactamase) inhibitor
bedaquiline bedaquiline: a diarylquinoline Antitubercular Agent. bedaquiline : A quinoline-based antimycobacterial drug used (as its fumarate salt) for the treatment of pulmonary multi-drug resistant tuberculosis by inhibition of ATP synthase, an enzyme essential for the replication of the mycobacteria.	2.6	1	0	aromatic ether; naphthalenes; organobromine compound; quinolines; tertiary alcohol; tertiary amino compound	antitubercular agent; ATP synthase inhibitor
cefepime Cefepime: A fourth-generation cephalosporin antibacterial agent that is used in the treatment of infections, including those of the abdomen, urinary tract, respiratory tract, and skin. It is effective against PSEUDOMONAS AERUGINOSA and may also be used in the empiric treatment of FEBRILE NEUTROPENIA.. cefepime : A cephalosporin bearing (1-methylpyrrolidinium-1-yl)methyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton.	3.33	5	0	cephalosporin; oxime O-ether	antibacterial drug
aztreonam [no description available]	2.41	1	0	beta-lactam antibiotic allergen; monobactam	antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor
cilastatin [no description available]	2.31	1	0	carboxamide; L-cysteine derivative; non-proteinogenic L-alpha-amino acid; organic sulfide	EC 3.4.13.19 (membrane dipeptidase) inhibitor; environmental contaminant; protease inhibitor; xenobiotic
avibactam avibactam : A member of the class of azabicycloalkanes that is (2S,5R)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamide in which the amino hydrogen at position 6 is replaced by a sulfooxy group. Used (in the form of its sodium salt) in combination with ceftazidime pentahydrate for the treatment of complicated urinary tract infections including pyelonephritis.	5.55	15	0	azabicycloalkane; hydroxylamine O-sulfonic acid; monocarboxylic acid amide; ureas	antibacterial drug; antimicrobial agent; EC 3.5.2.6 (beta-lactamase) inhibitor
mcc-950 [no description available]	2.41	1	0
tavaborole tavaborole: has antifungal activity; structure in first source. tavaborole : A member of the class of benzoxaboroles that is 1,3-dihydro-1-hydroxy-2,1-benzoxaborole substituted at position 5 by a fluoro group. A topical antifungal agent used for the treatment of onychomycosis (fungal infection of the toenails and fingernails).	2.41	1	0	benzoxaborole; organofluorine compound	antifungal agent; EC 6.1.1.4 (leucine--tRNA ligase) inhibitor; protein synthesis inhibitor
piperacillin, tazobactam drug combination Piperacillin, Tazobactam Drug Combination: An antibiotic combination product of piperacillin and tazobactam, a penicillanic acid derivative with enhanced beta-lactamase inhibitory activity, that is used for the intravenous treatment of intra-abdominal, pelvic, and skin infections and for community-acquired pneumonia of moderate severity. It is also used for the treatment of PSEUDOMONAS AERUGINOSA INFECTIONS.	5.98	2	1
nxl 104 avibactam sodium : An organic sodium salt that is the monosodium salt of avibactam. Used in combination with ceftazidime pentahydrate for the treatment of complicated urinary tract infections including pyelonephritis.	3.66	2	0	organic sodium salt	antibacterial drug; antimicrobial agent; EC 3.5.2.6 (beta-lactamase) inhibitor
ixazomib ixazomib: a proteasome inhibitor with antineoplastic activity; MLN2238 is the biologically active form of MLN9708; structure in first source. ixazomib : A glycine derivative that is the amide obtained by formal condensation of the carboxy group of N-(2,5-dichlorobenzoyl)glycine with the amino group of [(1R)-1-amino-3-methylbutyl]boronic acid. The active metabolite of ixazomib citrate, it is used in combination therapy for treatment of multiple myeloma.	2.41	1	0	benzamides; boronic acids; dichlorobenzene; glycine derivative	antineoplastic agent; apoptosis inducer; drug metabolite; orphan drug; proteasome inhibitor
achn 490 plazomicin: structure in first source	4.54	3	0
mk-7655 relebactam: structure in first source	6.37	21	0
piperidines Piperidines: A family of hexahydropyridines.	2.31	1	0
an2728 crisaborole: NSAID, Dermatologic Agent; structure in first source. crisaborole : A member of the class of benzoxaboroles that is 5-hydroxy-1,3-dihydro-2,1-benzoxaborole in which the phenolic hydrogen has been replaced by a 4-cyanophenyl group. A phosphodiesterase 4 inhibitor that is used for treatment of mild to moderate atopic dermatitis in children and adults.	2.41	1	0	aromatic ether; benzoxaborole; nitrile	antipsoriatic; non-steroidal anti-inflammatory drug; phosphodiesterase IV inhibitor
letermovir letermovir: has antiviral activity; structure in first source	2.17	1	0
colistin Colistin: Cyclic polypeptide antibiotic from Bacillus colistinus. It is composed of Polymyxins E1 and E2 (or Colistins A, B, and C) which act as detergents on cell membranes. Colistin is less toxic than Polymyxin B, but otherwise similar; the methanesulfonate is used orally.. colistin : A multi-component mixture comprising mostly of colistin A (R = Me) and B (R = H), with small amounts of colistin C and other polymyxins, produced by certain strains of Bacillus polymyxa var. colistinus. An antibiotic, it is used as its sulfate salt (for oral or topical use) or as the sodium salt of the N-methylsulfonic acid derivative (the injectable form) in the treatment of severe Gram-negative infections, partiularly those due to Pseudomonas aeruginosa.	2.31	1	0
fr 264205 ceftolozane: cephalosporin anti-bacterial agent with enhanced activity against Pseudomonas aeruginosa. ceftolozane : A fifth-generation cephalosporin antibiotic having (5-amino-4-{[(2-aminoethyl)carbamoyl]amino}-1-methyl-1H-pyrazol-2-ium-2-yl)methyl and [(2Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-{[(2-carboxypropan-2-yl)oxy]imino}acetyl]amino side groups located at positions 3 and 7 respectively; developed for the treatment of infections with gram-negative bacteria that have become resistant to conventional antibiotics.	3.49	5	0
eravacycline eravacycline: has antibacterial activity	4.78	4	0	tetracyclines
agar Agar: A complex sulfated polymer of galactose units, extracted from Gelidium cartilagineum, Gracilaria confervoides, and related red algae. It is used as a gel in the preparation of solid culture media for microorganisms, as a bulk laxative, in making emulsions, and as a supporting medium for immunodiffusion and immunoelectrophoresis.. agar : A complex mixture of polysaccharides extracted from species of red algae. Its two main components are agarose and agaropectin. Agarose is the component responsible for the high-strength gelling properties of agar, while agaropectin provides the viscous properties.	2.6	1	0
rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)	2.6	1	0	cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion	angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor
ceftobiprole ceftobiprole: BAL5788 is Ceftobiprole medocaril sodium. ceftobiprole : A fifth-generation cephalosporin antibiotic having (E)-[(3'R)-2-oxo[1,3'-bipyrrolidin]-3-ylidene]methyl and [(2Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(hydroxyimino)acetyl]amino side groups located at positions 3 and 7 respectively; developed for the treatment of hospital-acquired pneumonia (HAP, excluding ventilator-associated pneumonia, VAP) and community-acquired pneumonia (CAP).	2.25	1	0	cephalosporin; thiadiazoles	antimicrobial agent
abaloparatide abaloparatide: synthetic analog of human PTHrP (Parathyroid Hormone-Related Protein)	2.17	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Infections, Pseudomonas [description not available]	0	3.7	7	0
Cronobacter Infections [description not available]	0	5.19	9	0
Enterobacteriaceae Infections Infections with bacteria of the family ENTEROBACTERIACEAE.	0	5.19	9	0
Pseudomonas Infections Infections with bacteria of the genus PSEUDOMONAS.	0	3.7	7	0
Bacterial Disease [description not available]	0	3.53	2	0
Bacterial Infections Infections by bacteria, general or unspecified.	1	5.53	2	0
Infections, Klebsiella [description not available]	0	5.1	12	0
Klebsiella Infections Infections with bacteria of the genus KLEBSIELLA.	0	5.1	12	0
Infections, Soft Tissue [description not available]	0	2.31	1	0
Soft Tissue Infections Infections of non-skeletal tissue, i.e., exclusive of bone, ligaments, cartilage, and fibrous tissue. The concept is usually referred to as skin and soft tissue infections and usually subcutaneous and muscle tissue are involved. The predisposing factors in anaerobic infections are trauma, ischemia, and surgery. The organisms often derive from the fecal or oral flora, particularly in wounds associated with intestinal surgery, decubitus ulcer, and human bites. (From Cecil Textbook of Medicine, 19th ed, p1688)	0	2.31	1	0
Bacteremia The presence of viable bacteria circulating in the blood. Fever, chills, tachycardia, and tachypnea are common acute manifestations of bacteremia. The majority of cases are seen in already hospitalized patients, most of whom have underlying diseases or procedures which render their bloodstreams susceptible to invasion.	0	2.76	2	0
2019 Novel Coronavirus Disease [description not available]	0	2.41	1	0
Experimental Lung Inflammation Inflammation of any part, segment or lobe, of the lung parenchyma.	0	3.64	2	0
Pneumonia Infection of the lung often accompanied by inflammation.	0	3.64	2	0
Critical Illness A disease or state in which death is possible or imminent.	0	3.22	3	0
Urinary Tract Infections Inflammatory responses of the epithelium of the URINARY TRACT to microbial invasions. They are often bacterial infections with associated BACTERIURIA and PYURIA.	1	10.67	12	1
Blood Poisoning [description not available]	0	2.6	1	0
Sepsis Systemic inflammatory response syndrome with a proven or suspected infectious etiology. When sepsis is associated with organ dysfunction distant from the site of infection, it is called severe sepsis. When sepsis is accompanied by HYPOTENSION despite adequate fluid infusion, it is called SEPTIC SHOCK.	0	2.6	1	0
Tuberculosis, Drug-Resistant [description not available]	0	2.6	1	0
Tuberculosis, Multidrug-Resistant Tuberculosis resistant to chemotherapy with two or more ANTITUBERCULAR AGENTS, including at least ISONIAZID and RIFAMPICIN. The problem of resistance is particularly troublesome in tuberculous OPPORTUNISTIC INFECTIONS associated with HIV INFECTIONS. It requires the use of second line drugs which are more toxic than the first line regimens. TB with isolates that have developed further resistance to at least three of the six classes of second line drugs is defined as EXTENSIVELY DRUG-RESISTANT TUBERCULOSIS.	0	2.6	1	0
Ventilator-Associated Pneumonia [description not available]	0	2.82	2	0
Pneumonia, Ventilator-Associated Serious INFLAMMATION of the LUNG in patients who required the use of PULMONARY VENTILATOR. It is usually caused by bacterial CROSS INFECTION in hospitals.	0	2.82	2	0
Cystic Fibrosis of Pancreas [description not available]	0	2.66	2	0
Cystic Fibrosis An autosomal recessive genetic disease of the EXOCRINE GLANDS. It is caused by mutations in the gene encoding the CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR expressed in several organs including the LUNG, the PANCREAS, the BILIARY SYSTEM, and the SWEAT GLANDS. Cystic fibrosis is characterized by epithelial secretory dysfunction associated with ductal obstruction resulting in AIRWAY OBSTRUCTION; chronic RESPIRATORY INFECTIONS; PANCREATIC INSUFFICIENCY; maldigestion; salt depletion; and HEAT PROSTRATION.	0	2.66	2	0
Infections, Serratia [description not available]	0	2.25	1	0
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	2.25	1	0
Clostridioides difficile Infection [description not available]	0	3.23	1	0
Neisseria gonorrhoeae Infection [description not available]	0	3.23	1	0
Clostridium Infections Infections with bacteria of the genus CLOSTRIDIUM and closely related CLOSTRIDIOIDES species.	0	3.23	1	0
Gonorrhea Acute infectious disease characterized by primary invasion of the urogenital tract. The etiologic agent, NEISSERIA GONORRHOEAE, was isolated by Neisser in 1879.	0	3.23	1	0
Bacterial Infections, Gram-Negative [description not available]	0	2.87	3	0
Gram-Negative Bacterial Infections Infections caused by bacteria that show up as pink (negative) when treated by the gram-staining method.	0	2.87	3	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.17	1	0
Necrotizing Pyelonephritis [description not available]	0	6.09	3	1
Pyelonephritis Inflammation of the KIDNEY involving the renal parenchyma (the NEPHRONS); KIDNEY PELVIS; and KIDNEY CALICES. It is characterized by ABDOMINAL PAIN; FEVER; NAUSEA; VOMITING; and occasionally DIARRHEA.	0	6.09	3	1
Acute Disease Disease having a short and relatively severe course.	0	4.48	1	1
Adverse Drug Event [description not available]	0	2.17	1	0
Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.	0	2.17	1	0
Atypical Mycobacterial Infection, Disseminated [description not available]	0	2.21	1	0
Endotoxin Shock [description not available]	0	2.21	1	0
Shock, Septic Sepsis associated with HYPOTENSION or hypoperfusion despite adequate fluid resuscitation. Perfusion abnormalities may include but are not limited to LACTIC ACIDOSIS; OLIGURIA; or acute alteration in mental status.	0	2.21	1	0
Intra-Abdominal Infections [description not available]	0	3.09	1	0
Intraabdominal Infections Infection within the PERITONEAL CAVITY. A frequent cause is an ANASTOMOTIC LEAK following surgery.	0	3.09	1	0

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