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Compound Detail

CHEMBL537843

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CN1CCC(C#N)(c2ccc(F)cc2)CC1.Cl

Basic Information

ChEMBL ID CHEMBL537843
Phase Preclinical
Structure Type MOL
InChI Key ARCQPYKYHNUIAO-UHFFFAOYSA-N
Parent Compound CHEMBL324885
Active Moiety CHEMBL324885
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

218.3
MW (Da)
2.31
ALogP
2
HBA
0
HBD
27.0
PSA (Ų)
0.72
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H16ClFN2
MW 254.74
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -1.00

Activity Summary

Ki 2 meas. best 5.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL313
Ki 5.0 5.0 10100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium-dependent serotonin transporter Ki = 10100.0 nM 5.0 Inhibition of [3H]paroxetine binding to rat serotonin transporter 15743177

Literature References

PubMed DOI Target Context # Activities
15743177 10.1021/jm0401614 Sodium-dependent dopamine transporter 2
15743177 10.1021/jm0401614 Sodium-dependent serotonin transporter 1
15743177 10.1021/jm0401614 Norepinephrine transporter 1
15743177 10.1021/jm0401614 Mu-type opioid receptor 1

Data from ChEMBL 36 via Core Engine