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Compound Detail

CHEMBL1258428

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O=C1NCc2cc(F)c(OCCCN3CCN(c4cccc5ccccc45)CC3)cc21

Basic Information

ChEMBL ID CHEMBL1258428
Phase Preclinical
Structure Type MOL
InChI Key MIXXVGJQYQTQIC-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

419.5
MW (Da)
3.81
ALogP
4
HBA
1
HBD
44.8
PSA (Ų)
0.62
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H26FN3O2
MW 419.50
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.01

Activity Summary

Ki 4 meas. best 9.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 9.17 9.17 0.7 1
D(2) dopamine receptor
CHEMBL217
Ki 8.05 8.05 8.9 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 7.49 7.49 32.1 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 7.26 7.26 54.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20801650 10.1016/j.bmcl.2010.08.023 D(2) dopamine receptor 2
20801650 10.1016/j.bmcl.2010.08.023 Sodium-dependent serotonin transporter 2
20801650 10.1016/j.bmcl.2010.08.023 5-hydroxytryptamine receptor 1A 1
20801650 10.1016/j.bmcl.2010.08.023 5-hydroxytryptamine receptor 2A 1
20801650 10.1016/j.bmcl.2010.08.023 Unchecked 1

Data from ChEMBL 36 via Core Engine