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Compound Detail

CHEMBL5082239

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O=C(NC[C@H]1CN(c2ccc(N3CCOCC3)c(F)c2)C(=O)O1)c1cccs1

Basic Information

ChEMBL ID CHEMBL5082239
Phase Preclinical
Structure Type MOL
InChI Key QDJVUINYHZXGMP-AWEZNQCLSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

405.4
MW (Da)
2.48
ALogP
6
HBA
1
HBD
71.1
PSA (Ų)
0.83
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H20FN3O4S
MW 405.45
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -2.27

Activity Summary

IC50 1 meas. best 4.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Amine oxidase [flavin-containing] B
CHEMBL2039
IC50 4.48 4.48 33120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Amine oxidase [flavin-containing] B IC50 = 33120.0 nM 4.48 Inhibition of human recombinant MAO-B using benzylamine as substrate 38894926

Literature References

PubMed DOI Target Context # Activities
38894926 10.1021/acsmedchemlett.4c00114 Mycobacterium tuberculosis 6
34619406 10.1016/j.bmc.2021.116397 Staphylococcus aureus 4
34619406 10.1016/j.bmc.2021.116397 Enterococcus faecalis 2
34619406 10.1016/j.bmc.2021.116397 Streptococcus pneumoniae 2
34619406 10.1016/j.bmc.2021.116397 Acinetobacter baumannii 2
34619406 10.1016/j.bmc.2021.116397 Pseudomonas aeruginosa 2
34619406 10.1016/j.bmc.2021.116397 Enterococcus faecium 1
34619406 10.1016/j.bmc.2021.116397 Escherichia coli 1
38894926 10.1021/acsmedchemlett.4c00114 Amine oxidase [flavin-containing] A 1
38894926 10.1021/acsmedchemlett.4c00114 Amine oxidase [flavin-containing] B 1

Data from ChEMBL 36 via Core Engine