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Compound Detail

CHEMBL4533184

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N#Cc1ccc2[nH]cc(CCCCN3CCN(c4c5c(nc6ccccc46)CCC5)CC3)c2c1

Basic Information

ChEMBL ID CHEMBL4533184
Phase Preclinical
Structure Type MOL
InChI Key BIULMVQRVRFGEB-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

449.6
MW (Da)
5.22
ALogP
4
HBA
1
HBD
59.0
PSA (Ų)
0.41
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H31N5
MW 449.60
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.14

Activity Summary

IC50 2 meas. best 7.12
EC50 1 meas. best 6.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL228
IC50 7.12 7.12 76.3 1
5-hydroxytryptamine receptor 1A
CHEMBL214
EC50 6.97 6.97 107.0 1
Acetylcholinesterase
CHEMBL3199
IC50 5.48 5.48 3319.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30744931 10.1016/j.bmc.2019.01.025 Acetylcholinesterase 1
30744931 10.1016/j.bmc.2019.01.025 Butyrylcholinesterase 1
30744931 10.1016/j.bmc.2019.01.025 Acetylcholinesterase and butyrylcholinesterase (AChE and BChE) 1
30744931 10.1016/j.bmc.2019.01.025 5-hydroxytryptamine receptor 1A 1
30744931 10.1016/j.bmc.2019.01.025 Sodium-dependent serotonin transporter 1

Data from ChEMBL 36 via Core Engine