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Compound Detail

CHEMBL600424

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CNC[C@@H](O)[C@H](c1cc(F)cc(F)c1)N1CC(C)(C)c2ccccc21.Cl

Basic Information

ChEMBL ID CHEMBL600424
Phase Preclinical
Structure Type MOL
InChI Key NKULKNQOSDDCTA-VOMIJIAVSA-N
Parent Compound CHEMBL1198290
Active Moiety CHEMBL1198290
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

346.4
MW (Da)
3.38
ALogP
3
HBA
2
HBD
35.5
PSA (Ų)
0.87
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H25ClF2N2O
MW 382.88
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.08

Activity Summary

IC50 3 meas. best 8.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent noradrenaline transporter
CHEMBL222
IC50 8.39 8.29 4.1 2
Sodium-dependent serotonin transporter
CHEMBL228
IC50 5.28 5.28 5293.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20131864 10.1021/jm901559e Rattus norvegicus 4
20131864 10.1021/jm901559e Sodium-dependent noradrenaline transporter 2
20131864 10.1021/jm901559e Unchecked 2
20131864 10.1021/jm901559e Sodium-dependent serotonin transporter 1
20131864 10.1021/jm901559e Sodium-dependent dopamine transporter 1
20131864 10.1021/jm901559e 5-hydroxytryptamine receptor 2B 1
20131864 10.1021/jm901559e D(2) dopamine receptor 1
20131864 10.1021/jm901559e 5-hydroxytryptamine receptor 6 1
20131864 10.1021/jm901559e Mus musculus 1

Data from ChEMBL 36 via Core Engine