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Compound Detail

CHEMBL403677

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Cn1c2ccccc2n2cc(/C=C3/C(=O)N4C(C(=O)[O-])=CS[C@H]34)nc12.[Na+]

Basic Information

ChEMBL ID CHEMBL403677
Phase Preclinical
Structure Type MOL
InChI Key SOBDJICXYDBRSQ-PKCBAQMVSA-M
Parent Compound CHEMBL1207412
Active Moiety CHEMBL1207412
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

352.4
MW (Da)
2.05
ALogP
6
HBA
1
HBD
79.8
PSA (Ų)
0.56
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H11N4NaO3S
MW 374.36
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -0.65

Activity Summary

IC50 3 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.8 7.5733 16.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 16.0 nM 7.8 Inhibition of AmpC beta-lactamase 18061461
Unchecked IC50 = 24.0 nM 7.62 Inhibition of TEM1 beta-lactamase 18061461
Unchecked IC50 = 50.0 nM 7.3 Inhibition of Imi1 beta lactamase 18061461

Literature References

PubMed DOI Target Context # Activities
18061461 10.1016/j.bmc.2007.11.006 Escherichia coli 11
18061461 10.1016/j.bmc.2007.11.006 Enterobacter cloacae 4
18061461 10.1016/j.bmc.2007.11.006 Unchecked 3
18061461 10.1016/j.bmc.2007.11.006 Serratia marcescens 2
18061461 10.1016/j.bmc.2007.11.006 Pseudomonas aeruginosa 1
18061461 10.1016/j.bmc.2007.11.006 Stenotrophomonas maltophilia 1
18061461 10.1016/j.bmc.2007.11.006 Staphylococcus aureus 1

Data from ChEMBL 36 via Core Engine