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Compound Detail

CHEMBL559830

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COc1cc(Cc2cnc(N)nc2N)cc(/C=C/C(=O)N2N=Cc3ccccc3C2c2ccc(CO)cc2)c1O

Basic Information

ChEMBL ID CHEMBL559830
Phase Preclinical
Structure Type MOL
InChI Key PVLCYETZWWPUKN-ZHACJKMWSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

536.6
MW (Da)
3.42
ALogP
9
HBA
4
HBD
160.2
PSA (Ų)
0.26
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H28N6O4
MW 536.59
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness 0.01

Activity Summary

IC50 1 meas. best 7.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bacillus anthracis
CHEMBL613904
IC50 7.16 7.16 69.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bacillus anthracis IC50 = 69.0 nM 7.16 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