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Compound Detail

CHEMBL3357983

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Cc1noc2c(F)c3c(cc12)CC1(C(=O)NC(=O)NC1=O)[C@H]1[C@H](C)O[C@@H](C)CN31

Basic Information

ChEMBL ID CHEMBL3357983
Phase Preclinical
Structure Type MOL
InChI Key FWKBFPFKHVTISW-RWNMLDIDSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
8
Publications
0
Known Names

Molecular Properties

402.4
MW (Da)
1.17
ALogP
7
HBA
2
HBD
113.8
PSA (Ų)
0.64
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H19FN4O5
MW 402.38
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.34

Activity Summary

IC50 1 meas. best 7.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA gyrase
CHEMBL2094139
IC50 7.58 7.58 26.0 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.051 - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA gyrase IC50 = 26.0 nM 7.58 Inhibition of Escherichia coli DNA gyrase using fluorescence-tagged DNA by fluor... 25286019

Literature References

PubMed DOI Target Context # Activities
25286019 10.1021/jm501174m Escherichia coli 2
25286019 10.1021/jm501174m Staphylococcus aureus 2
25286019 10.1021/jm501174m Haemophilus influenzae 1
25286019 10.1021/jm501174m Streptococcus pyogenes 1
25286019 10.1021/jm501174m Streptococcus pneumoniae 1
25286019 10.1021/jm501174m No relevant target 1
25286019 10.1021/jm501174m Plasma 1
25286019 10.1021/jm501174m DNA gyrase 1

Data from ChEMBL 36 via Core Engine