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Compound Detail

CHEMBL4782574

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COc1ccc(C(=O)N2CCN(CC(=O)N3CCN(CCCc4c[nH]c5ccccc45)CC3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL4782574
Phase Preclinical
Structure Type MOL
InChI Key PXQJIQDRWQXKFO-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

503.6
MW (Da)
2.71
ALogP
5
HBA
1
HBD
72.1
PSA (Ų)
0.51
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H37N5O3
MW 503.65
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.15

Activity Summary

IC50 3 meas. best 4.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 4.6 4.6 25100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 25100.0 nM 4.6 Inhibition of human plasma AChE using acetylthiocholine iodide as substrate prei... 32388114

Literature References

PubMed DOI Target Context # Activities
32388114 10.1016/j.ejmech.2020.112368 No relevant target 1
32388114 10.1016/j.ejmech.2020.112368 Acetylcholinesterase 1
32388114 10.1016/j.ejmech.2020.112368 Sodium-dependent serotonin transporter 1
32388114 10.1016/j.ejmech.2020.112368 HEK293 1
32388114 10.1016/j.ejmech.2020.112368 SH-SY5Y 1

Data from ChEMBL 36 via Core Engine