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Compound Detail

CHEMBL1276315

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CC1CN2c3ccc([N+](=O)[O-])cc3CC3(C(=O)NC(=O)NC3=O)C2C(C)O1

Basic Information

ChEMBL ID CHEMBL1276315
Phase Preclinical
Structure Type MOL
InChI Key DJZPHYIXNUOVJU-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
9
PK Parameters
14
Publications
0
Known Names

Molecular Properties

374.4
MW (Da)
0.49
ALogP
7
HBA
2
HBD
130.9
PSA (Ų)
0.42
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H18N4O6
MW 374.35
Aromatic Rings 1
Heavy Atoms 27
NP-Likeness -0.47

Activity Summary

IC50 3 meas. best 5.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 5.05 4.785 9000.0 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 31000.0 ng.hr.mL-1 Mus musculus
AUC 27600.0 ng.hr.mL-1 Mus musculus
CL 11.62 mL.min-1.kg-1 Mus musculus
Cmax 41939.36 nM Mus musculus
Cmax 41939.36 nM Mus musculus
F 94.7 % Mus musculus
T1/2 1.22 hr Mus musculus
T1/2 0.927 hr Mus musculus
Tmax 1.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18519725 10.1128/aac.00247-08 Staphylococcus aureus 28
18519725 10.1128/aac.00247-08 Mus musculus 11
18519725 10.1128/aac.00247-08 Streptococcus pneumoniae 8
18519725 10.1128/aac.00247-08 Unchecked 3
18519725 10.1128/aac.00247-08 Escherichia coli 3
18519725 10.1128/aac.00247-08 Haemophilus influenzae 2
18519725 10.1128/aac.00247-08 Staphylococcus epidermidis 1
18519725 10.1128/aac.00247-08 Streptococcus pyogenes 1
18519725 10.1128/aac.00247-08 Enterococcus faecalis 1
18519725 10.1128/aac.00247-08 Enterococcus faecium 1
18519725 10.1128/aac.00247-08 Moraxella catarrhalis 1
18519725 10.1128/aac.00247-08 Klebsiella pneumoniae 1
18519725 10.1128/aac.00247-08 Pseudomonas aeruginosa 1
18519725 10.1128/aac.00247-08 MC9 1

Data from ChEMBL 36 via Core Engine