Compound Detail
CHEMBL44354
CEFTAZIDIME 💊 Approved Drug
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💊 Approved Drug
CC(C)(O/N=C(\C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[n+]3ccccc3)CS[C@H]12)c1csc(N)n1)C(=O)O
Basic Information
| ChEMBL ID | CHEMBL44354 |
| Name | CEFTAZIDIME |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | ORFOPKXBNMVMKC-DWVKKRMSSA-N |
| Therapeutic | ✓ Yes |
1
Targets
3
Activities
2
Assay Types
30
PK Parameters
20
Publications
22
Known Names
15
Indications
1
Mechanisms
Molecular Properties
546.6
MW (Da)
-1.30
ALogP
11
HBA
3
HBD
191.2
PSA (Ų)
0.15
QED
2
Ro5 Violations
9
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1985 |
| 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 Infections Intraabdominal Infections Parametritis Peritonitis Pneumonia Pyelonephritis Urinary Tract Infections Enterobacteriaceae Infections Skin Diseases Staphylococcal Skin Infections Esophageal Achalasia Meningitis, Bacterial Cystic Fibrosis Osteomyelitis
ATC Classification
J01DD02
ceftazidime
Level 1: ANTIINFECTIVES FOR SYSTEMIC USE
Level 2: ANTIBACTERIALS FOR SYSTEMIC USE
Drug Warnings
Black Box Warning
General Warning
Activity Summary
Ki 2 meas. best 7.7
Kd 1 meas.
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Unchecked CHEMBL612545 | Ki | 7.7 | 7.275 | 20.0 | 2 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 14000.0 | ng.hr.mL-1 | Canis lupus familiaris |
| AUC | 14000.0 | ng.hr.mL-1 | - |
| AUC | 14000.0 | ng.hr.mL-1 | marmosets |
| CL | 2.4 | mL.min-1.kg-1 | Homo sapiens |
| CL | 5.37 | L/hr | Homo sapiens |
| CL | 6.59 | L/hr | Homo sapiens |
| CL | 8.5 | L/hr | Homo sapiens |
| CL | 7.6 | L/hr | Homo sapiens |
| CL | 8.0 | L/hr | Homo sapiens |
| CL | 101.0 | ml/min | Homo sapiens |
| CL | 2.4 | mL.min-1.kg-1 | Homo sapiens |
| Cmax | 317971.42 | nM | - |
| Cmax | 814138.57 | nM | Homo sapiens |
| Cmax | 384200.22 | nM | Homo sapiens |
| F | - | % | Homo sapiens |
| Fu | 0.79 | - | Homo sapiens |
| MRT | 1.54 | hr | Homo sapiens |
| MRT | 2.1 | hr | Homo sapiens |
| MRT | 2.2 | hr | Homo sapiens |
| T1/2 | 0.3833 | hr | Rattus norvegicus |
| T1/2 | 0.8167 | hr | Simiiformes |
| T1/2 | 1.8 | hr | Homo sapiens |
| T1/2 | 0.3817 | hr | Rattus norvegicus |
| T1/2 | 0.9333 | hr | Macaca mulatta |
| T1/2 | 0.7 | hr | Callithrix |
| T1/2 | 0.7 | hr | - |
| T1/2 | 0.4 | hr | Mus musculus |
| T1/2 | 1.96 | hr | - |
| T1/2 | 1.48 | hr | Homo sapiens |
| T1/2 | 1.94 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Unchecked | Ki | = | 20.0 | nM | 7.7 | Inhibition of Escherichia coli MC4100 Beta-Lactamase CMY-2 using cephalothin as ... | 19470510 |
| Unchecked | Ki | = | 140.0 | nM | 6.85 | Inhibition of Escherichia coli MC4100 Beta-Lactamase CMY-30 using cephalothin as... | 19470510 |
Literature References
Data from ChEMBL 36 via Core Engine