Compound Detail
CHEMBL1257051
TEDIZOLID 🧪 Phase III
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🧪 Phase III
Basic Information
| ChEMBL ID | CHEMBL1257051 |
| Name | TEDIZOLID |
| Phase | Phase III |
| Structure Type | MOL |
| InChI Key | XFALPSLJIHVRKE-GFCCVEGCSA-N |
| Therapeutic | ✓ Yes |
3
Targets
3
Activities
1
Assay Types
9
PK Parameters
20
Publications
3
Known Names
2
Indications
1
Mechanisms
Molecular Properties
370.3
MW (Da)
1.40
ALogP
8
HBA
1
HBD
106.3
PSA (Ų)
0.74
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Bacterial 70S ribosome inhibitor | INHIBITOR | Bacterial 70S ribosome | ✓ | ✓ |
Indications
Bacterial Infections Infections
ATC Classification
J01XX11
tedizolid
Level 1: ANTIINFECTIVES FOR SYSTEMIC USE
Level 2: ANTIBACTERIALS FOR SYSTEMIC USE
Activity Summary
IC50 3 meas. best 5.45
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Clostridioides difficile CHEMBL614965 | IC50 | 5.45 | 5.45 | 3590.0 | 1 |
| Amine oxidase [flavin-containing] B CHEMBL2039 | IC50 | 5.24 | 5.24 | 5700.0 | 1 |
| Amine oxidase [flavin-containing] A CHEMBL1951 | IC50 | 5.06 | 5.06 | 8700.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 103000.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 49800.0 | ng.hr.mL-1 | Mus musculus |
| CL | 1.61 | mL.min-1.kg-1 | Mus musculus |
| Cmax | 12475.02 | nM | Mus musculus |
| F | 48.5 | % | Mus musculus |
| F | 91.0 | % | Rattus norvegicus |
| T1/2 | 3.49 | hr | Mus musculus |
| T1/2 | 3.12 | hr | Mus musculus |
| Tmax | 2.0 | hr | Mus musculus |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Clostridioides difficile | IC50 | = | 3590.0 | nM | 5.45 | Antibacterial activity against Clostridioides difficile assessed as inhibition o... | 38753983 |
| Amine oxidase [flavin-containing] B | IC50 | = | 5700.0 | nM | 5.24 | Reversible inhibition of human MAO-B | 26536532 |
| Amine oxidase [flavin-containing] A | IC50 | = | 8700.0 | nM | 5.06 | Reversible inhibition of human MAO-A | 26536532 |
Literature References
Data from ChEMBL 36 via Core Engine