Page last updated: 2024-08-05 15:25:46

EC 3.5.2.6 (beta-lactamase) inhibitor

An EC 3.5.2.* (non-peptide cyclic amide C-N hydrolase) inhibitor that interferes with the action of beta-lactamase (EC 3.5.2.6).

ChEBI ID: 35625

Members (8)

MemberDefinitionClass
avibactamA 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.avibactam
ceftriaxoneA third-generation cephalosporin compound having 2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetylamino and [(2-methyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl)sulfanyl]methyl side-groups.ceftriaxone
clavulanate potassiumA potassium salt having clavulanate as the counterion. It acts as a suicide inhibitor of bacterial beta-lactamase enzymes and has only weak anitbiotic activity when administered alone. However it can be used in combination with amoxicillin trihydrate (under the trade name Augmentin) for treatment of a variety of bacterial infections, where it prevents antibiotic inactivation by microbial lactamases.potassium clavulanate
clavulanic acidAntibiotic isolated from Streptomyces clavuligerus. It acts as a suicide inhibitor of bacterial beta-lactamase enzymes.clavulanic acid
nxl 104An 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.avibactam sodium
salicylsalicylic acidA dimeric benzoate ester obtained by intermolecular condensation between the carboxy of one molecule of salicylic acid with the phenol group of a second. It is a prodrug for salycylic acid that is used for treatment of rheumatoid arthritis and osteoarthritis and also shows activity against type II diabetes.salsalate
tazobactamA 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.tazobactam
tazobactam sodiumAn organic sodium salt having tazobactam(1-) as the counterion; used in combination with ceftolozane sulfate for treatment of complicated intra-abdominal infections and complicated urinary tract infections.tazobactam sodium

Research

Studies (3,502)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990436 (12.45)18.7374
1990's685 (19.56)18.2507
2000's742 (21.19)29.6817
2010's1,063 (30.35)24.3611
2020's576 (16.45)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials425 (10.90%)5.53%
Reviews259 (6.64%)6.00%
Case Studies382 (9.80%)4.05%
Observational35 (0.90%)0.25%
Other2,797 (71.75%)84.16%

Protein Targets (100)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency17.782811
activating transcription factor 6Homo sapiens (human)Potency0.006711
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency35.481311
AR proteinHomo sapiens (human)Potency1.232822
Cellular tumor antigen p53Homo sapiens (human)Potency0.023711
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency28.183811
Chain A, HADH2 proteinHomo sapiens (human)Potency25.118911
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency44.668411
Chain B, HADH2 proteinHomo sapiens (human)Potency25.118911
estrogen nuclear receptor alphaHomo sapiens (human)Potency13.249356
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency2.113211
farnesoid X nuclear receptorHomo sapiens (human)Potency11.882311
GLI family zinc finger 3Homo sapiens (human)Potency33.491511
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.962133
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency0.218422
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency10.181511
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency0.487233
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency0.841211
progesterone receptorHomo sapiens (human)Potency0.943911
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency26.603211
retinoid X nuclear receptor alphaHomo sapiens (human)Potency0.307322
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency0.106822
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency4.252711

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC5017.033333
Angiotensin-converting enzymeRattus norvegicus (Norway rat)IC5048.000014
B2 bradykinin receptorCavia porcellus (domestic guinea pig)IC504.800011
Beta-lactamaseBacillus licheniformisIC500.510011
Beta-lactamaseCitrobacter freundiiIC500.930011
Beta-lactamaseEnterobacter cloacaeIC5063.72252124
Beta-lactamaseEscherichia coli K-12IC50139.68651010
Beta-lactamaseMorganella morganiiIC500.190011
Beta-lactamasePseudomonas aeruginosa PAO1IC5020.636957
Beta-lactamaseStaphylococcus aureusIC507.625988
Beta-lactamaseEnterobacter cloacaeKi88.850012
Beta-lactamaseMycobacterium tuberculosis CDC1551Ki6.300011
Beta-lactamase Acinetobacter baumanniiIC501,850.000022
Beta-lactamase Acinetobacter pittiiIC501,208.673333
Beta-lactamase Burkholderia cenocepaciaIC500.500011
Beta-lactamase Citrobacter freundiiIC500.096011
Beta-lactamase Citrobacter gilleniiIC500.024512
Beta-lactamase Enterobacter cloacaeIC5025.692588
Beta-lactamase Escherichia coliIC5084.991448
Beta-lactamase Klebsiella pneumoniaeIC500.606723
Beta-lactamase Pseudomonas aeruginosaIC500.726736
Beta-lactamase Pseudomonas luteolaIC500.038012
Beta-lactamase Salmonella enterica subsp. enterica serovar WesthamptonIC500.006112
Beta-lactamase Serratia fonticolaIC5039.850012
Beta-lactamase Shouchella clausiiIC500.044512
Beta-lactamase Acinetobacter baumanniiKi1.700011
Beta-lactamase Escherichia coliKi0.011011
Beta-lactamase OXA-1Escherichia coliIC504.000022
Beta-lactamase SHV-1Escherichia coliIC500.125012
Beta-lactamase SHV-1Klebsiella pneumoniaeIC500.150023
Beta-lactamase SHV-1Klebsiella pneumoniaeKi1.110012
Beta-lactamase TEMEscherichia coliIC502.77331417
Beta-lactamase TEMEscherichia coliKi0.495022
Bile salt export pumpHomo sapiens (human)IC50783.250034
Bile salt export pumpRattus norvegicus (Norway rat)IC501,000.000011
BlaVIM-1 Escherichia coliKi40.000011
Carbapenem-hydrolyzing beta-lactamase KPCKlebsiella pneumoniaeIC503.748023
Carbapenem-hydrolyzing beta-lactamase KPCKlebsiella pneumoniaeKi42.500012
Carbonic anhydrase 1Homo sapiens (human)Ki22.150012
Carbonic anhydrase 2Homo sapiens (human)Ki22.150012
Chymotrypsinogen ABos taurus (cattle)IC50434.500022
Class D beta-lactamaseBrachyspira pilosicoliIC501.080012
Cytochrome P450 2B6Homo sapiens (human)IC500.140012
Cytochrome P450 2C9 Homo sapiens (human)IC5027.400011
Cytochrome P450 2J2Homo sapiens (human)IC5027.400011
D-amino-acid oxidaseHomo sapiens (human)IC5010.000011
Glutathione peroxidase 1Homo sapiens (human)Ki34.100011
Glutathione reductase, mitochondrialHomo sapiens (human)Ki17.340011
Metallo-beta-lactamase L1 type 3Stenotrophomonas maltophiliaIC502,100.000022
Metallo-beta-lactamase type 2Bacillus cereusIC50200.000011
Metallo-beta-lactamase type 2Bacteroides fragilisIC502,260.000055
Microsomal glutathione S-transferase 1Homo sapiens (human)Ki35.410011
Neutrophil elastaseHomo sapiens (human)IC5040.000011
Peptidoglycan D,D-transpeptidase MrdAEscherichia coli K-12IC500.590011
Solute carrier family 15 member 1Homo sapiens (human)Ki30,000.000022
Solute carrier family 15 member 2Rattus norvegicus (Norway rat)Ki20,000.000011
Solute carrier family 22 member 11Homo sapiens (human)Ki2.380011
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)IC50840.000011
Solute carrier family 22 member 6Homo sapiens (human)Ki0.230011
Solute carrier family 22 member 8Rattus norvegicus (Norway rat)IC502,000.000011
Solute carrier family 22 member 8Homo sapiens (human)Ki4.390011
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50153.800011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50153.800011
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50153.800011
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50153.800011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Alpha-synucleinHomo sapiens (human)Kd0.530011
Excitatory amino acid transporter 2Homo sapiens (human)EC5010.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Beta-lactamaseEnterobacter cloacaeK5.100011
Beta-lactamaseEnterobacter cloacaeKm300.000011
Beta-lactamase Escherichia coliKm300.000011
Beta-lactamase Shouchella clausiiKm950.000011
Beta-lactamase class B VIM-2 Pseudomonas aeruginosaKm2,937.500012
Beta-lactamase OXA-1Escherichia coliKinact380.000011
Beta-lactamase TEMEscherichia coliActivity3.000011
Metallo-b-lactamase Pseudomonas aeruginosaKm2,220.000012