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Compound Detail

CHEMBL539445

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COc1ncc(C2c3ccccc3C=NN2C(=O)/C=C/c2cc(Cc3cnc(N)nc3N)cc(OC)c2OC)c(OC)n1

Basic Information

ChEMBL ID CHEMBL539445
Phase Preclinical
Structure Type MOL
InChI Key OVPKOULLSONDRW-MDZDMXLPSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

582.6
MW (Da)
3.04
ALogP
12
HBA
2
HBD
173.2
PSA (Ų)
0.28
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H30N8O5
MW 582.62
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -0.27

Activity Summary

IC50 1 meas. best 6.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bacillus anthracis
CHEMBL613904
IC50 6.22 6.22 600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bacillus anthracis IC50 = 600.0 nM 6.22 Inhibition of histidine-tagged Bacillus anthracis Sterne recombinant DHFR expres... 17875993

Literature References

PubMed DOI Target Context # Activities
17875993 10.1128/aac.00628-07 Bacillus anthracis 2
17875993 10.1128/aac.00628-07 Dihydrofolate reductase 1
17875993 10.1128/aac.00628-07 Unchecked 1

Data from ChEMBL 36 via Core Engine