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Compound Detail

CHEMBL172564

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CCC(=O)OCC1=C(C(=O)[O-])N2C(=O)/C(=C/c3ccccn3)C2S(=O)(=O)C1.[Na+]

Basic Information

ChEMBL ID CHEMBL172564
Phase Preclinical
Structure Type MOL
InChI Key JOFMJZXMMHMXFT-OZLKFZLXSA-M
Parent Compound CHEMBL1205984
Active Moiety CHEMBL1205984
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

392.4
MW (Da)
0.35
ALogP
7
HBA
1
HBD
130.9
PSA (Ų)
0.43
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H15N2NaO7S
MW 414.37
Aromatic Rings 1
Heavy Atoms 27
NP-Likeness -0.36

Activity Summary

IC50 2 meas. best 4.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-lactamase
CHEMBL4114
IC50 4.81 4.81 15400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Beta-lactamase IC50 = 15400.0 nM 4.81 Inhibition of class A beta-lactamase derived from Staphylococcus aureus strain P... 10853646

Literature References

PubMed DOI Target Context # Activities
10853646 10.1016/s0960-894x(00)00098-6 Beta-lactamase class C 2
10853646 10.1016/s0960-894x(00)00098-6 Beta-lactamase TEM 1
10853646 10.1016/s0960-894x(00)00098-6 Beta-lactamase 1

Data from ChEMBL 36 via Core Engine