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Compound Detail

CHEMBL4238919

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CNc1cc(F)cc2c1[nH]c1nc(CNC(=O)c3cocn3)nc(N3CCC(N)C3)c12

Basic Information

ChEMBL ID CHEMBL4238919
Phase Preclinical
Structure Type MOL
InChI Key WRRYWYLIRTYXGI-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

424.4
MW (Da)
1.75
ALogP
8
HBA
4
HBD
138.0
PSA (Ų)
0.38
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 C20H21FN8O2
MW 424.44
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.20

Activity Summary

IC50 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA gyrase subunit A/DNA gyrase subunit B
CHEMBL3430898
IC50 8.3 7.95 5.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30122228 10.1016/j.bmcl.2018.05.049 Mycobacterium tuberculosis 4
30122228 10.1016/j.bmcl.2018.05.049 DNA gyrase subunit A/DNA gyrase subunit B 2
30122228 10.1016/j.bmcl.2018.05.049 Enterococcus faecalis 1
30122228 10.1016/j.bmcl.2018.05.049 Staphylococcus aureus 1
30122228 10.1016/j.bmcl.2018.05.049 Unchecked 1
30122228 10.1016/j.bmcl.2018.05.049 HepG2 1
30122228 10.1016/j.bmcl.2018.05.049 Staphylococcus epidermidis 1
30122228 10.1016/j.bmcl.2018.05.049 Streptococcus pneumoniae 1
30122228 10.1016/j.bmcl.2018.05.049 Haemophilus influenzae 1
30122228 10.1016/j.bmcl.2018.05.049 Pseudomonas aeruginosa 1
30122228 10.1016/j.bmcl.2018.05.049 Acinetobacter baumannii 1
30122228 10.1016/j.bmcl.2018.05.049 Mycolicibacterium smegmatis 1
30122228 10.1016/j.bmcl.2018.05.049 Escherichia coli 1

Data from ChEMBL 36 via Core Engine