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Compound Detail

CHEMBL487852

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CCNC(=O)Nc1nc2cc(-c3cccnc3)cc(-n3cccn3)c2[nH]1

Basic Information

ChEMBL ID CHEMBL487852
Phase Preclinical
Structure Type MOL
InChI Key DIIRMLRBGBCXMK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

347.4
MW (Da)
2.95
ALogP
5
HBA
3
HBD
100.5
PSA (Ų)
0.53
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 C18H17N7O
MW 347.38
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -2.11

Activity Summary

Ki 2 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA gyrase
CHEMBL3038482
Ki 7.82 7.82 15.0 1
Unchecked
CHEMBL612545
Ki 7.34 7.34 46.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA gyrase Ki = 15.0 nM 7.82 Inhibition of Staphylococcus aureus DNA gyrase 18690678
Unchecked Ki = 46.0 nM 7.34 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
24685546 10.1016/j.bmcl.2014.03.022 Staphylococcus aureus 2
25317480 10.1021/jm500563g Staphylococcus aureus 2
18690678 10.1021/jm800318d Haemophilus influenzae 1
18690678 10.1021/jm800318d Streptococcus pneumoniae 1
18690678 10.1021/jm800318d DNA gyrase 1
25317480 10.1021/jm500563g Streptococcus pneumoniae 1
25317480 10.1021/jm500563g Enterococcus faecalis 1
25317480 10.1021/jm500563g Enterococcus faecium 1
25317480 10.1021/jm500563g Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine