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Compound Detail

CHEMBL3818901

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COC(=O)c1cccn(C[C@@H]2CNCCO[C@H]2c2ccc(Cl)c(F)c2)c1=O.Cl

Basic Information

ChEMBL ID CHEMBL3818901
Phase Preclinical
Structure Type MOL
InChI Key DKYROPSEFKOOAQ-KYLFUZKPSA-N
Parent Compound CHEMBL3819687
Active Moiety CHEMBL3819687
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

394.8
MW (Da)
2.40
ALogP
6
HBA
1
HBD
69.6
PSA (Ų)
0.81
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 C19H21Cl2FN2O4
MW 431.29
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.82

Activity Summary

IC50 2 meas. best 9.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent noradrenaline transporter
CHEMBL222
IC50 9.68 9.68 0.2 1
Sodium-dependent serotonin transporter
CHEMBL228
IC50 7.27 7.27 54.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27325446 10.1016/j.bmc.2016.06.014 Sodium-dependent noradrenaline transporter 1
27325446 10.1016/j.bmc.2016.06.014 Sodium-dependent serotonin transporter 1
27325446 10.1016/j.bmc.2016.06.014 Sodium-dependent dopamine transporter 1
27325446 10.1016/j.bmc.2016.06.014 LLC-PK1 1

Data from ChEMBL 36 via Core Engine