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Compound Detail

CHEMBL4282527

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COc1ccc2c(=O)cc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[nH]c2c1

Basic Information

ChEMBL ID CHEMBL4282527
Phase Preclinical
Structure Type MOL
InChI Key SULOYNMFUTYGFY-UHFFFAOYSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

419.5
MW (Da)
3.57
ALogP
4
HBA
2
HBD
74.4
PSA (Ų)
0.61
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29N3O3
MW 419.53
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.82

Activity Summary

IC50 3 meas. best 6.35
Ki 2 meas. best 7.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sigma non-opioid intracellular receptor 1
CHEMBL4153
Ki 7.34 7.34 45.2 1
Sigma intracellular receptor 2
CHEMBL4105864
Ki 6.42 6.42 376.0 1
Acetylcholinesterase
CHEMBL220
IC50 6.35 6.35 450.0 1
Amine oxidase [flavin-containing] B
CHEMBL2039
IC50 4.25 4.25 56400.0 1
Amine oxidase [flavin-containing] A
CHEMBL1951
IC50 4.14 4.14 72700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30025348 10.1016/j.ejmech.2018.07.026 Unchecked 2
30025348 10.1016/j.ejmech.2018.07.026 No relevant target 2
30025348 10.1016/j.ejmech.2018.07.026 Polyunsaturated fatty acid 5-lipoxygenase 2
30025348 10.1016/j.ejmech.2018.07.026 Cholinesterase 1
30025348 10.1016/j.ejmech.2018.07.026 Acetylcholinesterase 1
30025348 10.1016/j.ejmech.2018.07.026 Amine oxidase [flavin-containing] A 1
30025348 10.1016/j.ejmech.2018.07.026 Amine oxidase [flavin-containing] B 1
30025348 10.1016/j.ejmech.2018.07.026 Sigma non-opioid intracellular receptor 1 1
30025348 10.1016/j.ejmech.2018.07.026 Sigma intracellular receptor 2 1

Data from ChEMBL 36 via Core Engine