Molecule Details
InChIKeySMOBCLHAZXOKDQ-ZJUUUORDSA-N
Compound NameRelebactam
Canonical SMILESO=C(NC1CCNCC1)[C@@H]1CC[C@@H]2CN1C(=O)N2OS(=O)(=O)O
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)2
Pfam Stratification Cross-Family
Avg pChEMBL6.5
SourceBindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB12377
Drug NameRelebactam
CAS Number1174018-99-5
Groups approved
ATC Codes J01DH56
DescriptionRelebactam is a diazabicyclooctane beta-lactamase inhibitor, similar in structure to [avibactam].[A181195,A181207] It includes a piperidine ring which reduces export from bacterial cells by producing a positive charge.[A181207] It is currently available in a combination product which includes [imipe...

Categories: Antibacterials for Systemic Use Antiinfectives for Systemic Use Aza Compounds Enzyme Inhibitors MATE 1 Substrates MATE 2 Substrates MATE substrates OAT3/SLC22A8 Substrates beta-Lactamase Inhibitors
Cross-references: BindingDB: 1858 CHEMBL3112741 ChemSpider: 31137585 PubChem:44129647 PubChem:347828625 RxCUI: 2268500 Wikipedia: Relebactam ZINC: ZINC000043206319
Target Activities (2)
Target Gene Organism Category Pfam pChEMBL Type Source
I7AKP2 KPC-2 Klebsiella pneumoniae Pathogen PF13354 6.7 IC50 BindingDB
Q3LG62 ampC Pseudomonas aeruginosa Pathogen PF00144 6.3 IC50 BindingDB
DrugBank Target Actions (10)
Target Gene Target Name Action Type
P00807 blaZ Beta-lactamase inhibitor targets
P05364 ampC Beta-lactamase inhibitor targets
P0AD63 bla Beta-lactamase SHV-1 inhibitor targets
P62593 bla Beta-lactamase TEM inhibitor targets
Q939N4 Q939N4 Beta-lactamase CTX-M inhibitor targets
Q93LQ9 KPC-2 Beta-lactamase inhibitor targets
Q86VL8 SLC47A2 Multidrug and toxin extrusion protein 2 substrate transporters
Q8TCC7 SLC22A8 Organic anion transporter 3 substrate transporters
Q96FL8 SLC47A1 Multidrug and toxin extrusion protein 1 substrate transporters
Q9NSA0 SLC22A11 Solute carrier family 22 member 11 substrate transporters