Compound Detail
CHEMBL158
AZTREONAM 💊 Approved Drug
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💊 Approved Drug
C[C@H]1[C@H](NC(=O)/C(=N\OC(C)(C)C(=O)O)c2csc(N)n2)C(=O)N1S(=O)(=O)O
Basic Information
| ChEMBL ID | CHEMBL158 |
| Name | AZTREONAM |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | WZPBZJONDBGPKJ-VEHQQRBSSA-N |
| Therapeutic | ✓ Yes |
9
Targets
19
Activities
2
Assay Types
30
PK Parameters
20
Publications
11
Known Names
15
Indications
1
Mechanisms
Molecular Properties
435.4
MW (Da)
-1.17
ALogP
10
HBA
4
HBD
201.6
PSA (Ų)
0.17
QED
0
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1986 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Bacterial penicillin-binding protein inhibitor | INHIBITOR | Bacterial penicillin-binding protein | ✓ | ✓ |
Indications
Bacterial Infections Cystic Fibrosis Infections Intraabdominal Infections Pneumonia Pyelonephritis Sepsis Urinary Tract Infections Enterobacteriaceae Infections Skin Diseases Gonorrhea Gram-Negative Bacterial Infections Carcinoma, Non-Small-Cell Lung Renal Insufficiency Osteomyelitis
ATC Classification
J01DF01
aztreonam
Level 1: ANTIINFECTIVES FOR SYSTEMIC USE
Level 2: ANTIBACTERIALS FOR SYSTEMIC USE
Activity Summary
IC50 13 meas. best 8.22
Ki 6 meas. best 9.0
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Unchecked CHEMBL612545 | Ki | 9.0 | 8.4833 | 1.0 | 3 |
| Efflux transporter CHEMBL1641337 | IC50 | 8.22 | 8.22 | 6.0 | 1 |
| Class C beta-lactamase CMY-36 CHEMBL1641338 | IC50 | 8.22 | 8.22 | 6.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 8.22 | 6.9457 | 6.0 | 7 |
| Beta-lactamase ADC-33 CHEMBL1667700 | Ki | 8.15 | 8.15 | 7.0 | 1 |
| Beta-lactamase ACC-4 CHEMBL5305 | IC50 | 7.5 | 7.5 | 32.0 | 1 |
| AmpC CHEMBL1255151 | IC50 | 7.22 | 7.22 | 60.0 | 1 |
| PER-2 beta-lactamase CHEMBL5303 | Ki | 5.7 | 5.7 | 2000.0 | 1 |
| ADC-11 CHEMBL1667701 | Ki | 5.52 | 5.52 | 3000.0 | 1 |
| Penicillin-binding protein 1A CHEMBL3259512 | IC50 | 5.48 | 5.48 | 3340.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 336.7 | - | Homo sapiens |
| AUC | 414.4 | - | Homo sapiens |
| AUC | 5000.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 13000.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 13000.0 | ng.hr.mL-1 | Canis lupus familiaris |
| AUC | 2410.0 | ng.hr.mL-1 | Rattus norvegicus |
| CL | 100.1 | ml/min | Homo sapiens |
| CL | 76.2 | ml/min | Homo sapiens |
| CL | 4.59 | L/hr | Homo sapiens |
| CL | 6.052 | L/hr | Homo sapiens |
| CL | 1.84 | mL.min-1.kg-1 | Homo sapiens |
| CL | 1.31 | mL.min-1.kg-1 | Homo sapiens |
| CL | 1.5 | mL.min-1.kg-1 | Homo sapiens |
| CL | 1.5 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.5 | mL.min-1.kg-1 | Homo sapiens |
| CL | 1.3 | mL.min-1.kg-1 | Homo sapiens |
| CL | 1.5 | mL.min-1.kg-1 | Homo sapiens |
| CL | 5.0 | mL.min-1.kg-1 | Macaca |
| CL | 8.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 11.0 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 21.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 16.0 | mL.min-1.kg-1 | Mus musculus |
| CL | 13.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 4.0 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 15.2 | mL.min-1.kg-1 | Rattus norvegicus |
| F | 1.0 | % | Homo sapiens |
| F | 1.0 | % | Homo sapiens |
| F | 1.0 | % | Homo sapiens |
| F | 100.0 | % | Homo sapiens |
| Fu | 0.72 | - | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine