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Compound Detail

CHEMBL4798551

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CNc1cc(F)cc2c(NCCCN)c(C(=O)Nc3ccc(C(=O)O)cc3)c(=O)[nH]c12.O=CO

Basic Information

ChEMBL ID CHEMBL4798551
Phase Preclinical
Structure Type MOL
InChI Key QGUMEINGUYVNKR-UHFFFAOYSA-N
Parent Compound CHEMBL4804007
Active Moiety CHEMBL4804007
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

427.4
MW (Da)
2.42
ALogP
6
HBA
6
HBD
149.3
PSA (Ų)
0.30
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24FN5O6
MW 473.46
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.98

Activity Summary

IC50 1 meas. best 9.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA gyrase
CHEMBL2094139
IC50 9.28 9.28 0.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA gyrase IC50 = 0.52 nM 9.28 Inhibition of Escherichia coli DNA gyrase by measuring supercoiling activity inc... 33032189

Literature References

PubMed DOI Target Context # Activities
33032189 10.1016/j.bmc.2020.115776 Escherichia coli 2
33032189 10.1016/j.bmc.2020.115776 DNA gyrase 1
33032189 10.1016/j.bmc.2020.115776 Unchecked 1
33032189 10.1016/j.bmc.2020.115776 Staphylococcus aureus 1

Data from ChEMBL 36 via Core Engine