Compound Detail
CHEMBL126
LINEZOLID 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL126 |
| Name | LINEZOLID |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | TYZROVQLWOKYKF-ZDUSSCGKSA-N |
| Therapeutic | ✓ Yes |
16
Targets
53
Activities
3
Assay Types
30
PK Parameters
20
Publications
6
Known Names
20
Indications
1
Mechanisms
Molecular Properties
337.4
MW (Da)
1.12
ALogP
5
HBA
1
HBD
71.1
PSA (Ų)
0.89
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2000 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Bacterial 70S ribosome inhibitor | INHIBITOR | Bacterial 70S ribosome | ✓ | ✓ |
Indications
Bacteremia Bacterial Infections Infections Osteomyelitis Pneumonia Abscess Cellulitis Gram-Positive Bacterial Infections Optic Nerve Diseases Pneumonia, Bacterial Pneumonia, Pneumococcal Skin Diseases Staphylococcal Infections Syphilis Tuberculosis Tuberculosis, Pulmonary Cystic Fibrosis Hematologic Neoplasms Lung Diseases Meningitis
ATC Classification
J01XX08
linezolid
Level 1: ANTIINFECTIVES FOR SYSTEMIC USE
Level 2: ANTIBACTERIALS FOR SYSTEMIC USE
Activity Summary
IC50 45 meas. best 6.96
EC50 4 meas. best 6.8
Ki 4 meas. best 5.1
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Clostridioides difficile CHEMBL614965 | IC50 | 6.96 | 6.96 | 110.0 | 1 |
| Streptokinase A CHEMBL1293228 | EC50 | 6.8 | 6.01 | 158.0 | 2 |
| Streptococcus sp. 'group A' CHEMBL612389 | EC50 | 6.77 | 6.77 | 170.0 | 1 |
| Amine oxidase [flavin-containing] B CHEMBL2039 | IC50 | 6.21 | 5.646 | 619.0 | 5 |
| Streptococcus CHEMBL612313 | EC50 | 6.19 | 6.19 | 645.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 6.05 | 5.17 | 900.0 | 5 |
| Escherichia coli CHEMBL354 | IC50 | 6.02 | 5.3558 | 950.0 | 12 |
| Pseudomonas aeruginosa CHEMBL348 | IC50 | 5.77 | 4.97 | 1700.0 | 4 |
| Acinetobacter baumannii CHEMBL614425 | IC50 | 5.4 | 5.0575 | 4000.0 | 4 |
| Amine oxidase [flavin-containing] A CHEMBL1951 | IC50 | 5.19 | 4.855 | 6520.0 | 4 |
| Amine oxidase [flavin-containing] A CHEMBL1951 | Ki | 5.1 | 4.585 | 7900.0 | 4 |
| Succinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrial CHEMBL5758 | IC50 | 5.09 | 5.09 | 8190.0 | 1 |
| Prostaglandin G/H synthase 1 CHEMBL221 | IC50 | 5.09 | 5.09 | 8190.0 | 1 |
| H9c2 CHEMBL614576 | IC50 | 5.06 | 5.06 | 8710.0 | 1 |
| Calmodulin-like protein 3 CHEMBL5169127 | IC50 | 5.03 | 5.03 | 9300.0 | 1 |
| Rattus norvegicus CHEMBL376 | IC50 | 4.92 | 4.92 | 12000.0 | 1 |
| Amine oxidase [flavin-containing] B CHEMBL2993 | IC50 | 4.77 | 4.77 | 17000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 4240.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 29090.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 112020.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 45700000000.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 105000000000.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 105000.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 666000.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 260000.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 10980.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 780.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 76300.0 | ng.hr.mL-1 | Oryctolagus cuniculus |
| AUC | 136900.0 | ng.hr.mL-1 | Oryctolagus cuniculus |
| AUC | 173000.0 | ng.hr.mL-1 | Oryctolagus cuniculus |
| AUC | 334000.0 | ng.hr.mL-1 | Oryctolagus cuniculus |
| AUC | 87800.0 | ng.hr.mL-1 | Cavia porcellus |
| AUC | 118700.0 | ng.hr.mL-1 | Cavia porcellus |
| AUC | 125800.0 | ng.hr.mL-1 | Cavia porcellus |
| AUC | 84600.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 96800.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 124500.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 136400.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 60100.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 66800.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 80300.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 160700.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 2100.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 16000.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 19000.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 196080.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 412550.0 | ng.hr.mL-1 | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine