Compound Detail
CHEMBL850
SPARFLOXACIN 💊 Approved Drug
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💊 Approved Drug
C[C@@H]1CN(c2c(F)c(N)c3c(=O)c(C(=O)O)cn(C4CC4)c3c2F)C[C@H](C)N1
Basic Information
| ChEMBL ID | CHEMBL850 |
| Name | SPARFLOXACIN |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | DZZWHBIBMUVIIW-DTORHVGOSA-N |
| Therapeutic | ✓ Yes |
3
Targets
17
Activities
2
Assay Types
18
PK Parameters
20
Publications
8
Known Names
2
Indications
2
Mechanisms
Molecular Properties
392.4
MW (Da)
2.08
ALogP
6
HBA
3
HBD
100.6
PSA (Ų)
0.69
QED
0
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1996 |
| Availability | Discontinued |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Topoisomerase IV inhibitor | INHIBITOR | Topoisomerase IV | ✓ | ✓ |
| Bacterial DNA gyrase inhibitor | INHIBITOR | Bacterial DNA gyrase | ✓ | ✓ |
Indications
Bacterial Infections Osteomyelitis
ATC Classification
J01MA09
sparfloxacin
Level 1: ANTIINFECTIVES FOR SYSTEMIC USE
Level 2: ANTIBACTERIALS FOR SYSTEMIC USE
Activity Summary
IC50 16 meas. best 4.75
Ki 1 meas. best 4.41
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 4.75 | 4.58 | 18000.0 | 11 |
| Trypanosoma brucei brucei CHEMBL612851 | IC50 | 4.73 | 4.73 | 18500.0 | 1 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | Ki | 4.41 | 4.41 | 38619.4 | 1 |
| Voltage-gated L-type calcium channel CHEMBL2095229 | IC50 | 4.05 | 4.05 | 88800.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 43000.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 20000.0 | ng.hr.mL-1 | Homo sapiens |
| CL | 2.7 | mL.min-1.kg-1 | Homo sapiens |
| CL | 2.3 | mL.min-1.kg-1 | Homo sapiens |
| CL | 2.7 | mL.min-1.kg-1 | Homo sapiens |
| CL | 2.7 | mL.min-1.kg-1 | Homo sapiens |
| Cmax | 1911.27 | nM | Mus musculus |
| Cmax | 2548.36 | nM | Homo sapiens |
| F | 92.0 | % | Homo sapiens |
| F | 92.0 | % | Homo sapiens |
| Fu | 0.26 | - | Mus musculus |
| Fu | 0.55 | - | Homo sapiens |
| Fu | 0.55 | - | Homo sapiens |
| Fu | 0.88 | - | Homo sapiens |
| MRT | 24.0 | hr | Homo sapiens |
| T1/2 | 9.8 | hr | Mus musculus |
| T1/2 | 20.0 | hr | Homo sapiens |
| T1/2 | 18.0 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine