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Compound Detail

CHEMBL159608

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Fc1ccc(C(OCCN2CCN(CCCc3cccnc3)CC2)c2ccc(F)cc2)cc1

Basic Information

ChEMBL ID CHEMBL159608
Phase Preclinical
Structure Type MOL
InChI Key YSPRAXVSVOUKSE-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

451.6
MW (Da)
4.72
ALogP
4
HBA
0
HBD
28.6
PSA (Ų)
0.45
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H31F2N3O
MW 451.56
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.97

Activity Summary

IC50 5 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent dopamine transporter
CHEMBL338
IC50 7.8 6.8967 16.0 3
Sigma non-opioid intracellular receptor 1
CHEMBL287
IC50 7.1 7.1 79.0 1
Sodium-dependent serotonin transporter
CHEMBL313
IC50 5.55 5.55 2800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9057857 10.1021/jm9606599 Sodium-dependent dopamine transporter 4
9057857 10.1021/jm9606599 Monoamine transporters; serotonin & dopamine 2
9057857 10.1021/jm9606599 Sodium-dependent serotonin transporter 1
9057857 10.1021/jm9606599 Sigma non-opioid intracellular receptor 1 1

Data from ChEMBL 36 via Core Engine