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Compound Detail

CHEMBL537959

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COc1cc(Cc2cnc(N)nc2N)cc(/C=C/C(=O)N2N=Cc3ccccc3C2c2ccccc2CN(C)C)c1OC

Basic Information

ChEMBL ID CHEMBL537959
Phase Preclinical
Structure Type MOL
InChI Key XZAWIWOWJUQKJE-BUHFOSPRSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

577.7
MW (Da)
4.29
ALogP
9
HBA
2
HBD
132.2
PSA (Ų)
0.28
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H35N7O3
MW 577.69
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -0.30

Activity Summary

IC50 1 meas. best 6.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bacillus anthracis
CHEMBL613904
IC50 6.4 6.4 400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bacillus anthracis IC50 = 400.0 nM 6.4 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