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Compound Detail

CHEMBL2313969

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CCCc1nn(CN2CCN(c3cc4c(cc3F)c(=O)c(C(=O)O)cn4C3CC3)CC2)c(=S)n1-c1cccc(I)c1

Basic Information

ChEMBL ID CHEMBL2313969
Phase Preclinical
Structure Type MOL
InChI Key DVJMTNFNGYSTBI-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

688.6
MW (Da)
5.23
ALogP
9
HBA
1
HBD
88.5
PSA (Ų)
0.20
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H30FIN6O3S
MW 688.57
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.68

Activity Summary

IC50 2 meas. best 5.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA gyrase
CHEMBL2094139
IC50 5.2 5.2 6280.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA gyrase IC50 = 6280.0 nM 5.2 Inhibition of Escherichia coli DNA gyrase after 1 hr by agarose gel electrophore... 25951434

Literature References

PubMed DOI Target Context # Activities
23287058 10.1016/j.ejmech.2012.11.040 Staphylococcus aureus 4
23287058 10.1016/j.ejmech.2012.11.040 Proteus mirabilis 1
23287058 10.1016/j.ejmech.2012.11.040 Pseudomonas aeruginosa 1
23287058 10.1016/j.ejmech.2012.11.040 Escherichia coli 1
23287058 10.1016/j.ejmech.2012.11.040 Micrococcus luteus 1
23287058 10.1016/j.ejmech.2012.11.040 Bacillus cereus 1
23287058 10.1016/j.ejmech.2012.11.040 Bacillus subtilis 1
23287058 10.1016/j.ejmech.2012.11.040 Staphylococcus epidermidis 1
25951434 10.1016/j.ejmech.2015.04.058 DNA gyrase 1
25951434 10.1016/j.ejmech.2015.04.058 Unchecked 1

Data from ChEMBL 36 via Core Engine