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Compound Detail

CHEMBL258450

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CCN(CC)C(=O)[C@@]1(c2ccc3occc3c2)C[C@H]1CN

Basic Information

ChEMBL ID CHEMBL258450
Phase Preclinical
Structure Type MOL
InChI Key YKZNMHWYVVPEPW-WMLDXEAASA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

286.4
MW (Da)
2.52
ALogP
3
HBA
1
HBD
59.5
PSA (Ų)
0.92
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H22N2O2
MW 286.38
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness 0.17

Activity Summary

IC50 2 meas. best 7.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent noradrenaline transporter
CHEMBL222
IC50 7.33 7.33 47.0 1
Sodium-dependent serotonin transporter
CHEMBL228
IC50 6.55 6.55 280.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium-dependent noradrenaline transporter IC50 = 47.0 nM 7.33 Inhibition of human NET 18445525
Sodium-dependent serotonin transporter IC50 = 280.0 nM 6.55 Inhibition of human SERT 18445525

Literature References

PubMed DOI Target Context # Activities
18445525 10.1016/j.bmcl.2008.04.025 Sodium-dependent noradrenaline transporter 1
18445525 10.1016/j.bmcl.2008.04.025 Sodium-dependent serotonin transporter 1
18445525 10.1016/j.bmcl.2008.04.025 Sodium-dependent dopamine transporter 1

Data from ChEMBL 36 via Core Engine