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Compound Detail

CHEMBL471319

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CCNC(=O)Nc1nc2cc(-n3cnc(C(=O)NC4CC4)c3)c(F)cc2[nH]1

Basic Information

ChEMBL ID CHEMBL471319
Phase Preclinical
Structure Type MOL
InChI Key ULFIHHOZULSWER-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

371.4
MW (Da)
1.92
ALogP
5
HBA
4
HBD
116.7
PSA (Ų)
0.55
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 C17H18FN7O2
MW 371.38
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.87

Activity Summary

Ki 2 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA gyrase
CHEMBL3038482
Ki 8.0 8.0 10.0 1
Unchecked
CHEMBL612545
Ki 7.11 7.11 78.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA gyrase Ki = 10.0 nM 8.0 Inhibition of Staphylococcus aureus DNA gyrase 18690678
Unchecked Ki = 78.0 nM 7.11 Inhibition of Escherichia coli topoisomerase 4 18690678

Literature References

PubMed DOI Target Context # Activities
18690678 10.1021/jm800318d Staphylococcus aureus 2
18690678 10.1021/jm800318d Unchecked 2
18690678 10.1021/jm800318d Haemophilus influenzae 1
18690678 10.1021/jm800318d Streptococcus pneumoniae 1
18690678 10.1021/jm800318d DNA gyrase 1

Data from ChEMBL 36 via Core Engine