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Compound Detail

CHEMBL455461

RADEZOLID
🧪 Phase II
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🧪 Phase II
CC(=O)NC[C@H]1CN(c2ccc(-c3ccc(CNCc4cnn[nH]4)cc3)c(F)c2)C(=O)O1

Basic Information

ChEMBL ID CHEMBL455461
Name RADEZOLID
Phase Phase II
Structure Type MOL
InChI Key BTTNOGHPGJANSW-IBGZPJMESA-N

Known Names

Radezolid RX-013 RX-01_667 RX-103 RX-1741 RX-O1_667
1
Targets
2
Activities
1
Assay Types
3
PK Parameters
20
Publications
6
Known Names
1
Indications
1
Mechanisms

Molecular Properties

438.5
MW (Da)
2.36
ALogP
6
HBA
3
HBD
112.2
PSA (Ų)
0.50
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -zolid
USAN Year 2008

Extended Properties

Molecular Formula C22H23FN6O3
MW 438.46
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.36

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Bacterial 70S ribosome inhibitor INHIBITOR Bacterial 70S ribosome

Indications

Pneumonia

Activity Summary

IC50 2 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.7 7.61 20.0 2

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.1 hr Homo sapiens
T1/2 0.1 hr Mus musculus
T1/2 0.1 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20385852 10.1128/aac.01724-09 Staphylococcus aureus 68
18316525 10.1128/aac.01383-07 Staphylococcus aureus 19
18316525 10.1128/aac.01383-07 Streptococcus pneumoniae 18
18316525 10.1128/aac.01383-07 Enterococcus faecium 17
20385873 10.1128/aac.01723-09 THP-1 13
18316525 10.1128/aac.01383-07 Enterococcus faecalis 13
20837755 10.1128/aac.00714-10 Staphylococcus aureus 11
20385852 10.1128/aac.01724-09 ADMET 8
18316525 10.1128/aac.01383-07 Streptococcus pyogenes 6
18316525 10.1128/aac.01383-07 Haemophilus influenzae 5
20385852 10.1128/aac.01724-09 Staphylococcus epidermidis 5
20385852 10.1128/aac.01724-09 Legionella pneumophila 5
20385852 10.1128/aac.01724-09 Listeria monocytogenes 5
20385873 10.1128/aac.01723-09 J774 4
18947996 10.1016/j.bmcl.2008.10.011 Haemophilus influenzae 4
18316525 10.1128/aac.01383-07 Moraxella catarrhalis 3
18316525 10.1128/aac.01383-07 Mycoplasmoides pneumoniae 3
18316525 10.1128/aac.01383-07 Legionella pneumophila 3
18947996 10.1016/j.bmcl.2008.10.011 Streptococcus pneumoniae 3
18663023 10.1128/aac.01193-07 Unchecked 3

Data from ChEMBL 36 via Core Engine