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Compound Detail

CHEMBL290165

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CC(=O)OCC1=C(C(=O)[O-])N2C(=O)/C(=C/C(=O)[O-])[C@H]2S(=O)(=O)C1.[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL290165
Phase Preclinical
Structure Type MOL
InChI Key AEZXXIFNQPEZCP-AHSLQULLSA-L
Parent Compound CHEMBL1206642
Active Moiety CHEMBL1206642
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

345.3
MW (Da)
-1.50
ALogP
7
HBA
2
HBD
155.3
PSA (Ų)
0.35
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H9NNa2O9S
MW 389.25
Aromatic Rings 0
Heavy Atoms 23
NP-Likeness 0.43

Activity Summary

IC50 1 meas. best 6.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-lactamase TEM
CHEMBL2065
IC50 6.4 6.4 400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Beta-lactamase TEM IC50 = 400.0 nM 6.4 Inhibitory activity against beta-Lactamase enzyme derived from Escherichia coli ... -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00249-S Escherichia coli 3
- 10.1016/0960-894X(95)00249-S Beta-lactamase 2
- 10.1016/0960-894X(95)00249-S Enterobacter cloacae 2
- 10.1016/0960-894X(95)00249-S Beta-lactamase TEM 1
- 10.1016/0960-894X(95)00249-S Staphylococcus aureus 1

Data from ChEMBL 36 via Core Engine