Compound Detail
CHEMBL9
NORFLOXACIN 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL9 |
| Name | NORFLOXACIN |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | OGJPXUAPXNRGGI-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
17
Targets
58
Activities
3
Assay Types
21
PK Parameters
20
Publications
10
Known Names
8
Indications
2
Mechanisms
Molecular Properties
319.3
MW (Da)
1.27
ALogP
5
HBA
2
HBD
74.6
PSA (Ų)
0.89
QED
0
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1986 |
| Availability | Discontinued |
| Chirality | Achiral |
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 Eye Infections Cystitis, Hemorrhagic Esophageal and Gastric Varices Liver Cirrhosis Peritonitis Hermanski-Pudlak Syndrome Osteomyelitis
ATC Classification
J01MA06
norfloxacin
Level 1: ANTIINFECTIVES FOR SYSTEMIC USE
Level 2: ANTIBACTERIALS FOR SYSTEMIC USE
S01AE02
norfloxacin
Level 1: SENSORY ORGANS
Level 2: OPHTHALMOLOGICALS
Drug Warnings
Black Box Warning
General Warning
Activity Summary
IC50 55 meas. best 7.7
Kd 2 meas. best 4.01
Ki 1 meas. best 10.05
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Unchecked CHEMBL612545 | Ki | 10.05 | 10.05 | 0.1 | 1 |
| GABA-A receptor; anion channel CHEMBL1907607 | IC50 | 7.7 | 6.295 | 20.0 | 2 |
| Unchecked CHEMBL612545 | IC50 | 7.05 | 5.9982 | 90.0 | 11 |
| DNA gyrase CHEMBL2094139 | IC50 | 6.22 | 5.2267 | 600.0 | 3 |
| Bromodomain-containing protein 4 CHEMBL1163125 | IC50 | 6.01 | 6.01 | 980.0 | 1 |
| Cytochrome P450 2J2 CHEMBL3491 | IC50 | 5.59 | 5.59 | 2560.0 | 1 |
| L6 CHEMBL614793 | IC50 | 5.46 | 5.46 | 3431.1 | 1 |
| DNA topoisomerase 4 subunit A CHEMBL4088 | IC50 | 5.46 | 5.46 | 3500.0 | 1 |
| HBL-100 CHEMBL614811 | IC50 | 4.91 | 4.91 | 12430.0 | 1 |
| Topoisomerase IV CHEMBL3038508 | IC50 | 4.9 | 4.9 | 12560.0 | 1 |
| ADMET CHEMBL612558 | IC50 | 4.86 | 4.86 | 13800.0 | 1 |
| MCF7 CHEMBL387 | IC50 | 4.71 | 4.71 | 19370.0 | 1 |
| NCI/ADR-RES CHEMBL613829 | IC50 | 4.7 | 4.7 | 20060.0 | 1 |
| Trypanosoma brucei brucei CHEMBL612851 | IC50 | 4.4 | 4.4 | 39900.0 | 1 |
| Plasmodium falciparum CHEMBL364 | IC50 | 4.27 | 4.2083 | 54000.0 | 12 |
| A-431 CHEMBL614069 | IC50 | 4.16 | 4.16 | 70000.0 | 1 |
| NCI-H460 CHEMBL396 | IC50 | 4.07 | 4.07 | 86000.0 | 1 |
| Multidrug resistance protein MdtK CHEMBL1681613 | Kd | 4.01 | 4.01 | 98400.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 6.49 | - | Rattus norvegicus |
| AUC | 3.3 | - | Rattus norvegicus |
| AUC | 1.9 | - | Rattus norvegicus |
| AUC | 22.01 | - | Rattus norvegicus |
| AUC | 8.78 | - | Rattus norvegicus |
| AUC | 980.0 | ng.hr.mL-1 | - |
| AUC | 1770.0 | ng.hr.mL-1 | - |
| AUC | 1800.0 | ng.hr.mL-1 | - |
| AUC | 6490.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 6490.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 6500.0 | ng.hr.mL-1 | - |
| AUC | 2300.0 | ng.hr.mL-1 | - |
| AUC | 10000.0 | ng.hr.mL-1 | Homo sapiens |
| Cmax | 4697.19 | nM | Homo sapiens |
| F | 62.99 | % | Eutheria |
| F | 35.0 | % | Homo sapiens |
| F | 35.0 | % | Homo sapiens |
| Fu | 0.87 | - | Rattus norvegicus |
| Fu | 0.58 | - | Rattus norvegicus |
| T1/2 | 3.0 | hr | Homo sapiens |
| Vd | 2.9 | L.kg-1 | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine