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Compound Detail

CHEMBL5220446

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C/C(=N\NCCCN1C(=O)S/C(=C\c2ccc(OCc3ccccc3)cc2)C1=O)c1ccncc1

Basic Information

ChEMBL ID CHEMBL5220446
Phase Preclinical
Structure Type MOL
InChI Key LELDJCNXAPGXMU-RMYUHZIOSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

486.6
MW (Da)
5.10
ALogP
7
HBA
1
HBD
83.9
PSA (Ų)
0.19
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H26N4O3S
MW 486.60
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.46

Activity Summary

IC50 2 meas. best 7.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Amine oxidase [flavin-containing] A
CHEMBL1951
IC50 7.21 7.21 61.0 1
Amine oxidase [flavin-containing] B
CHEMBL2039
IC50 4.89 4.89 12730.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Amine oxidase [flavin-containing] A IC50 = 61.0 nM 7.21 Inhibition of human MAO-A 36162779
Amine oxidase [flavin-containing] B IC50 = 12730.0 nM 4.89 Inhibition of recombinant human MAO-B 36162779

Literature References

PubMed DOI Target Context # Activities
36162779 10.1016/j.bmcl.2022.128994 Unchecked 1
36162779 10.1016/j.bmcl.2022.128994 Amine oxidase [flavin-containing] B 1
36162779 10.1016/j.bmcl.2022.128994 Amine oxidase [flavin-containing] A 1

Data from ChEMBL 36 via Core Engine