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Compound Detail

CHEMBL5282842

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O=C(NNC(=O)[C@@H]1CC[C@@H]2CN1C(=O)N2OS(=O)(=O)O)c1cn(C2CC2)c2cc(N3CCNCC3)c(F)cc2c1=O

Basic Information

ChEMBL ID CHEMBL5282842
Phase Preclinical
Structure Type MOL
InChI Key ZWRBMILGUFADAG-KDOFPFPSSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

593.6
MW (Da)
-0.35
ALogP
10
HBA
4
HBD
182.6
PSA (Ų)
0.26
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28FN7O8S
MW 593.59
Aromatic Rings 2
Heavy Atoms 41
NP-Likeness -0.97

Activity Summary

IC50 1 meas. best 8.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metallo-beta-lactamase type 2
CHEMBL1744488
IC50 8.77 8.77 1.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Metallo-beta-lactamase type 2 IC50 = 1.69 nM 8.77 Inhibition of Bacillus cereus beta-lactamase II 37127102

Literature References

PubMed DOI Target Context # Activities
37127102 10.1016/j.bmcl.2023.129308 Escherichia coli 4
37127102 10.1016/j.bmcl.2023.129308 Klebsiella pneumoniae 4
37127102 10.1016/j.bmcl.2023.129308 Staphylococcus aureus 2
37127102 10.1016/j.bmcl.2023.129308 Acinetobacter baumannii 1
37127102 10.1016/j.bmcl.2023.129308 Metallo-beta-lactamase type 2 1
37127102 10.1016/j.bmcl.2023.129308 Unchecked 1

Data from ChEMBL 36 via Core Engine