Compound Detail
CHEMBL240163
PAZUFLOXACIN 🧪 Phase III
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🧪 Phase III
Basic Information
| ChEMBL ID | CHEMBL240163 |
| Name | PAZUFLOXACIN |
| Phase | Phase III |
| Structure Type | MOL |
| InChI Key | XAGMUUZPGZWTRP-ZETCQYMHSA-N |
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
20
Publications
4
Known Names
3
Indications
2
Mechanisms
Molecular Properties
318.3
MW (Da)
1.74
ALogP
5
HBA
2
HBD
94.5
PSA (Ų)
0.88
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Bacterial DNA gyrase inhibitor | INHIBITOR | Bacterial DNA gyrase | ✓ | ✓ |
| DNA topoisomerase II inhibitor | INHIBITOR | DNA topoisomerase II | ✓ | ✓ |
Indications
Bacterial Infections Conjunctivitis, Bacterial Otitis Media
ATC Classification
J01MA18
pazufloxacin
Level 1: ANTIINFECTIVES FOR SYSTEMIC USE
Level 2: ANTIBACTERIALS FOR SYSTEMIC USE
Activity Summary
EC50 3 meas. best 5.21
IC50 1 meas. best 6.05
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Unchecked CHEMBL612545 | IC50 | 6.05 | 6.05 | 900.0 | 1 |
| Streptokinase A CHEMBL1293228 | EC50 | 5.21 | 5.21 | 6203.0 | 1 |
| Streptococcus CHEMBL612313 | EC50 | 5.17 | 5.17 | 6739.0 | 1 |
| Streptococcus sp. 'group A' CHEMBL612389 | EC50 | 5.14 | 5.14 | 7223.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Unchecked | IC50 | = | 900.0 | nM | 6.05 | PUBCHEM_BIOASSAY: A counter screen for small molecule screen for inhibitors of t... | - |
| Streptokinase A | EC50 | = | 6203.0 | nM | 5.21 | PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... | - |
| Streptococcus | EC50 | = | 6739.0 | nM | 5.17 | PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... | - |
| Streptococcus sp. 'group A' | EC50 | = | 7223.0 | nM | 5.14 | PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... | - |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 15646539 | 10.1016/s0399-8320(04)95062-2 | Unchecked | 11 |
| 15646539 | 10.1016/s0399-8320(04)95062-2 | NON-PROTEIN TARGET | 8 |
| 17548499 | 10.1128/aac.00339-07 | Escherichia coli | 7 |
| 34861348 | 10.1016/j.bmcl.2021.128484 | Staphylococcus aureus | 4 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 4 |
| 20855738 | 10.1128/aac.01054-10 | Escherichia coli | 3 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-2A adrenergic receptor | 2 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Progesterone receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2A | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Gamma-aminobutyric acid receptor subunit alpha-1 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M2 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 1A | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2B | 2 |
| 23956101 | 10.1093/toxsci/kft176 | ATP-binding cassette sub-family C member 2 | 1 |
| 23956101 | 10.1093/toxsci/kft176 | ATP-binding cassette sub-family C member 3 | 1 |
| 23956101 | 10.1093/toxsci/kft176 | Bile salt export pump | 1 |
| 15464074 | 10.1016/j.ejphar.2004.08.013 | ATP-dependent translocase ABCB1 | 1 |
| 17826097 | 10.1016/j.bmc.2007.08.031 | Klebsiella pneumoniae | 1 |
Data from ChEMBL 36 via Core Engine