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Compound Detail

CHEMBL3605369

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CN1CCc2c(c3ccccc3n2CCCCCCCCCn2c3c(c4ccccc42)CN(C)CC3)C1

Basic Information

ChEMBL ID CHEMBL3605369
Phase Preclinical
Structure Type MOL
InChI Key UOUFDKZYWIUMHL-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

496.7
MW (Da)
7.00
ALogP
4
HBA
0
HBD
16.3
PSA (Ų)
0.22
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H44N4
MW 496.74
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.33

Activity Summary

IC50 4 meas. best 7.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL4078
IC50 7.78 7.78 16.8 1
Cholinesterase
CHEMBL5763
IC50 7.28 7.28 52.4 1
Amine oxidase [flavin-containing] A
CHEMBL1951
IC50 5.46 5.46 3500.0 1
Amine oxidase [flavin-containing] B
CHEMBL2039
IC50 5.41 5.41 3900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26278660 10.1021/acs.jmedchem.5b00958 Glutamate NMDA receptor; GRIN1/GRIN2A 2
26278660 10.1021/acs.jmedchem.5b00958 Glutamate NMDA receptor; GRIN1/GRIN2B 2
26278660 10.1021/acs.jmedchem.5b00958 Acetylcholinesterase 1
26278660 10.1021/acs.jmedchem.5b00958 Cholinesterase 1
26278660 10.1021/acs.jmedchem.5b00958 Amine oxidase [flavin-containing] A 1
26278660 10.1021/acs.jmedchem.5b00958 Amine oxidase [flavin-containing] B 1
34391122 10.1016/j.bmc.2021.116355 Glutamate NMDA receptor; GRIN1/GRIN2A 1
34391122 10.1016/j.bmc.2021.116355 Nicotinic acetylcholine receptor alpha6/alpha3/beta4 1
34391122 10.1016/j.bmc.2021.116355 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine