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Compound Detail

CHEMBL264666

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c1nc(N2CCCCC2)c2nc[nH]c2n1

Basic Information

ChEMBL ID CHEMBL264666
Phase Preclinical
Structure Type MOL
InChI Key OXCZAXJFRBPQRP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

203.2
MW (Da)
1.34
ALogP
4
HBA
1
HBD
57.7
PSA (Ų)
0.76
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H13N5
MW 203.25
Aromatic Rings 2
Heavy Atoms 15
NP-Likeness -1.28

Activity Summary

IC50 2 meas. best 4.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase kinase kinase 5
CHEMBL5285
IC50 4.77 4.77 17000.0 1
RAC-beta serine/threonine-protein kinase
CHEMBL2431
IC50 4.23 4.23 59000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29598912 10.1016/j.bmcl.2018.03.046 Staphylococcus aureus 4
21134755 10.1016/j.bmc.2010.11.004 Mitogen-activated protein kinase kinase kinase 5 2
- 10.6019/CHEMBL3301361 No relevant target 2
29598912 10.1016/j.bmcl.2018.03.046 Escherichia coli 2
29598912 10.1016/j.bmcl.2018.03.046 Pseudomonas aeruginosa 2
29598912 10.1016/j.bmcl.2018.03.046 Candida albicans 2
18345609 10.1021/jm701437d RAC-beta serine/threonine-protein kinase 1
18345609 10.1021/jm701437d Unchecked 1
18345609 10.1021/jm701437d NON-PROTEIN TARGET 1
18345609 10.1021/jm701437d Glycogen synthase kinase-3 beta 1
29598912 10.1016/j.bmcl.2018.03.046 Enterococcus faecalis 1
29598912 10.1016/j.bmcl.2018.03.046 Klebsiella pneumoniae 1
29598912 10.1016/j.bmcl.2018.03.046 Acinetobacter baumannii 1
29598912 10.1016/j.bmcl.2018.03.046 Candida tropicalis 1
29598912 10.1016/j.bmcl.2018.03.046 Aspergillus fumigatus 1
29598912 10.1016/j.bmcl.2018.03.046 Candida parapsilosis 1

Data from ChEMBL 36 via Core Engine