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Compound Detail

CHEMBL257550

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NCC1C(c2ccccc2)C1(C(=O)N1CCc2ccccc21)c1ccccc1

Basic Information

ChEMBL ID CHEMBL257550
Phase Preclinical
Structure Type MOL
InChI Key ZAKNFBUXJCNYEX-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

368.5
MW (Da)
3.89
ALogP
2
HBA
1
HBD
46.3
PSA (Ų)
0.76
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24N2O
MW 368.48
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.21

Activity Summary

IC50 2 meas. best 6.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL228
IC50 6.25 6.25 560.0 1
Sodium-dependent dopamine transporter
CHEMBL238
IC50 5.37 5.37 4300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium-dependent serotonin transporter IC50 = 560.0 nM 6.25 Inhibition of human SERT 18445525
Sodium-dependent dopamine transporter IC50 = 4300.0 nM 5.37 Inhibition of human DAT 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