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Compound Detail

CHEMBL395022

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COc1ccc(C2CN(C)Cc3cc(OCCCN4CCN(c5ccc(C#N)cc5)CC4)ccc32)cc1

Basic Information

ChEMBL ID CHEMBL395022
Phase Preclinical
Structure Type MOL
InChI Key LTHPEUUEWQVVRQ-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

496.7
MW (Da)
4.74
ALogP
6
HBA
0
HBD
52.0
PSA (Ų)
0.42
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H36N4O2
MW 496.66
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.90

Activity Summary

Ki 3 meas. best 8.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL313
Ki 8.48 8.48 3.3 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 8.1 8.1 8.0 1
Histamine H3 receptor
CHEMBL264
Ki 6.84 6.84 144.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17107798 10.1016/j.bmcl.2006.10.089 Sodium-dependent serotonin transporter 2
17107798 10.1016/j.bmcl.2006.10.089 Histamine H3 receptor 1

Data from ChEMBL 36 via Core Engine