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)
| Member | Definition | Class |
|---|---|---|
| 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. | avibactam |
| ceftriaxone | A 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 potassium | A 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 acid | Antibiotic isolated from Streptomyces clavuligerus. It acts as a suicide inhibitor of bacterial beta-lactamase enzymes. | clavulanic acid |
| nxl 104 | 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. | avibactam sodium |
| salicylsalicylic acid | A 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 |
| 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. | tazobactam |
| tazobactam sodium | An 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)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 436 (12.45) | 18.7374 |
| 1990's | 685 (19.56) | 18.2507 |
| 2000's | 742 (21.19) | 29.6817 |
| 2010's | 1,063 (30.35) | 24.3611 |
| 2020's | 576 (16.45) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 425 (10.90%) | 5.53% |
| Reviews | 259 (6.64%) | 6.00% |
| Case Studies | 382 (9.80%) | 4.05% |
| Observational | 35 (0.90%) | 0.25% |
| Other | 2,797 (71.75%) | 84.16% |
Protein Targets (100)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 17.7828 | 1 | 1 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 0.0067 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 1.2328 | 2 | 2 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 0.0237 | 1 | 1 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 13.2493 | 5 | 6 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 2.1132 | 1 | 1 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 11.8823 | 1 | 1 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 33.4915 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 0.9621 | 3 | 3 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 0.2184 | 2 | 2 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 10.1815 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 0.4872 | 3 | 3 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 0.8412 | 1 | 1 |
| progesterone receptor | Homo sapiens (human) | Potency | 0.9439 | 1 | 1 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 26.6032 | 1 | 1 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 0.3073 | 2 | 2 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 0.1068 | 2 | 2 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 4.2527 | 1 | 1 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | IC50 | 17.0333 | 3 | 3 |
| Angiotensin-converting enzyme | Rattus norvegicus (Norway rat) | IC50 | 48.0000 | 1 | 4 |
| B2 bradykinin receptor | Cavia porcellus (domestic guinea pig) | IC50 | 4.8000 | 1 | 1 |
| Beta-lactamase | Bacillus licheniformis | IC50 | 0.5100 | 1 | 1 |
| Beta-lactamase | Citrobacter freundii | IC50 | 0.9300 | 1 | 1 |
| Beta-lactamase | Enterobacter cloacae | IC50 | 63.7225 | 21 | 24 |
| Beta-lactamase | Escherichia coli K-12 | IC50 | 139.6865 | 10 | 10 |
| Beta-lactamase | Morganella morganii | IC50 | 0.1900 | 1 | 1 |
| Beta-lactamase | Pseudomonas aeruginosa PAO1 | IC50 | 20.6369 | 5 | 7 |
| Beta-lactamase | Staphylococcus aureus | IC50 | 7.6259 | 8 | 8 |
| Beta-lactamase | Enterobacter cloacae | Ki | 88.8500 | 1 | 2 |
| Beta-lactamase | Mycobacterium tuberculosis CDC1551 | Ki | 6.3000 | 1 | 1 |
| Beta-lactamase | Acinetobacter baumannii | IC50 | 1,850.0000 | 2 | 2 |
| Beta-lactamase | Acinetobacter pittii | IC50 | 1,208.6733 | 3 | 3 |
| Beta-lactamase | Burkholderia cenocepacia | IC50 | 0.5000 | 1 | 1 |
| Beta-lactamase | Citrobacter freundii | IC50 | 0.0960 | 1 | 1 |
| Beta-lactamase | Citrobacter gillenii | IC50 | 0.0245 | 1 | 2 |
| Beta-lactamase | Enterobacter cloacae | IC50 | 25.6925 | 8 | 8 |
| Beta-lactamase | Escherichia coli | IC50 | 84.9914 | 4 | 8 |
| Beta-lactamase | Klebsiella pneumoniae | IC50 | 0.6067 | 2 | 3 |
| Beta-lactamase | Pseudomonas aeruginosa | IC50 | 0.7267 | 3 | 6 |
| Beta-lactamase | Pseudomonas luteola | IC50 | 0.0380 | 1 | 2 |
| Beta-lactamase | Salmonella enterica subsp. enterica serovar Westhampton | IC50 | 0.0061 | 1 | 2 |
| Beta-lactamase | Serratia fonticola | IC50 | 39.8500 | 1 | 2 |
| Beta-lactamase | Shouchella clausii | IC50 | 0.0445 | 1 | 2 |
| Beta-lactamase | Acinetobacter baumannii | Ki | 1.7000 | 1 | 1 |
| Beta-lactamase | Escherichia coli | Ki | 0.0110 | 1 | 1 |
| Beta-lactamase OXA-1 | Escherichia coli | IC50 | 4.0000 | 2 | 2 |
| Beta-lactamase SHV-1 | Escherichia coli | IC50 | 0.1250 | 1 | 2 |
| Beta-lactamase SHV-1 | Klebsiella pneumoniae | IC50 | 0.1500 | 2 | 3 |
| Beta-lactamase SHV-1 | Klebsiella pneumoniae | Ki | 1.1100 | 1 | 2 |
| Beta-lactamase TEM | Escherichia coli | IC50 | 2.7733 | 14 | 17 |
| Beta-lactamase TEM | Escherichia coli | Ki | 0.4950 | 2 | 2 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 783.2500 | 3 | 4 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 1 |
| BlaVIM-1 | Escherichia coli | Ki | 40.0000 | 1 | 1 |
| Carbapenem-hydrolyzing beta-lactamase KPC | Klebsiella pneumoniae | IC50 | 3.7480 | 2 | 3 |
| Carbapenem-hydrolyzing beta-lactamase KPC | Klebsiella pneumoniae | Ki | 42.5000 | 1 | 2 |
| Carbonic anhydrase 1 | Homo sapiens (human) | Ki | 22.1500 | 1 | 2 |
| Carbonic anhydrase 2 | Homo sapiens (human) | Ki | 22.1500 | 1 | 2 |
| Chymotrypsinogen A | Bos taurus (cattle) | IC50 | 434.5000 | 2 | 2 |
| Class D beta-lactamase | Brachyspira pilosicoli | IC50 | 1.0800 | 1 | 2 |
| Cytochrome P450 2B6 | Homo sapiens (human) | IC50 | 0.1400 | 1 | 2 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 27.4000 | 1 | 1 |
| Cytochrome P450 2J2 | Homo sapiens (human) | IC50 | 27.4000 | 1 | 1 |
| D-amino-acid oxidase | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Glutathione peroxidase 1 | Homo sapiens (human) | Ki | 34.1000 | 1 | 1 |
| Glutathione reductase, mitochondrial | Homo sapiens (human) | Ki | 17.3400 | 1 | 1 |
| Metallo-beta-lactamase L1 type 3 | Stenotrophomonas maltophilia | IC50 | 2,100.0000 | 2 | 2 |
| Metallo-beta-lactamase type 2 | Bacillus cereus | IC50 | 200.0000 | 1 | 1 |
| Metallo-beta-lactamase type 2 | Bacteroides fragilis | IC50 | 2,260.0000 | 5 | 5 |
| Microsomal glutathione S-transferase 1 | Homo sapiens (human) | Ki | 35.4100 | 1 | 1 |
| Neutrophil elastase | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| Peptidoglycan D,D-transpeptidase MrdA | Escherichia coli K-12 | IC50 | 0.5900 | 1 | 1 |
| Solute carrier family 15 member 1 | Homo sapiens (human) | Ki | 30,000.0000 | 2 | 2 |
| Solute carrier family 15 member 2 | Rattus norvegicus (Norway rat) | Ki | 20,000.0000 | 1 | 1 |
| Solute carrier family 22 member 11 | Homo sapiens (human) | Ki | 2.3800 | 1 | 1 |
| Solute carrier family 22 member 6 | Rattus norvegicus (Norway rat) | IC50 | 840.0000 | 1 | 1 |
| Solute carrier family 22 member 6 | Homo sapiens (human) | Ki | 0.2300 | 1 | 1 |
| Solute carrier family 22 member 8 | Rattus norvegicus (Norway rat) | IC50 | 2,000.0000 | 1 | 1 |
| Solute carrier family 22 member 8 | Homo sapiens (human) | Ki | 4.3900 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1C | Homo sapiens (human) | IC50 | 153.8000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1D | Homo sapiens (human) | IC50 | 153.8000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1F | Homo sapiens (human) | IC50 | 153.8000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1S | Homo sapiens (human) | IC50 | 153.8000 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Alpha-synuclein | Homo sapiens (human) | Kd | 0.5300 | 1 | 1 |
| Excitatory amino acid transporter 2 | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Beta-lactamase | Enterobacter cloacae | K | 5.1000 | 1 | 1 |
| Beta-lactamase | Enterobacter cloacae | Km | 300.0000 | 1 | 1 |
| Beta-lactamase | Escherichia coli | Km | 300.0000 | 1 | 1 |
| Beta-lactamase | Shouchella clausii | Km | 950.0000 | 1 | 1 |
| Beta-lactamase class B VIM-2 | Pseudomonas aeruginosa | Km | 2,937.5000 | 1 | 2 |
| Beta-lactamase OXA-1 | Escherichia coli | Kinact | 380.0000 | 1 | 1 |
| Beta-lactamase TEM | Escherichia coli | Activity | 3.0000 | 1 | 1 |
| Metallo-b-lactamase | Pseudomonas aeruginosa | Km | 2,220.0000 | 1 | 2 |