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Compound Detail

CHEMBL379755

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CN1C2CCC1C1COC(=O)CCCCCCCCCCC(=O)Nc3ccc(cc3)C1C2

Basic Information

ChEMBL ID CHEMBL379755
Phase Preclinical
Structure Type MOL
InChI Key KZXIQLJNAIYPLZ-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

440.6
MW (Da)
5.65
ALogP
4
HBA
1
HBD
58.6
PSA (Ų)
0.53
QED
1
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H40N2O3
MW 440.63
Aromatic Rings 1
Heavy Atoms 32
NP-Likeness 0.86

Activity Summary

IC50 3 meas. best 6.41
Ki 2 meas. best 6.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL228
Ki 6.54 6.54 290.0 1
Sodium-dependent dopamine transporter
CHEMBL238
IC50 6.41 6.41 390.0 1
Sodium-dependent noradrenaline transporter
CHEMBL222
Ki 5.94 5.94 1160.0 1
Sodium-dependent serotonin transporter
CHEMBL228
IC50 5.92 5.92 1200.0 1
Sodium-dependent noradrenaline transporter
CHEMBL222
IC50 5.63 5.63 2320.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16854064 10.1021/jm060287w Sodium-dependent serotonin transporter 2
16854064 10.1021/jm060287w Sodium-dependent noradrenaline transporter 2
16854064 10.1021/jm060287w Sodium-dependent dopamine transporter 1

Data from ChEMBL 36 via Core Engine