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Compound Detail

CHEMBL2206528

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Cc1cccc2c1CN(C)CC2c1ccc(F)c(F)c1

Basic Information

ChEMBL ID CHEMBL2206528
Phase Preclinical
Structure Type MOL
InChI Key RUBLHLUAVCRNAN-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

273.3
MW (Da)
3.85
ALogP
1
HBA
0
HBD
3.2
PSA (Ų)
0.76
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 C17H17F2N
MW 273.33
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -0.73

Activity Summary

Ki 2 meas. best 7.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent noradrenaline transporter
CHEMBL222
Ki 7.43 7.43 37.0 1
Sodium-dependent dopamine transporter
CHEMBL238
Ki 7.24 7.24 58.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium-dependent noradrenaline transporter Ki = 37.0 nM 7.43 Inhibition of human NET 23084899
Sodium-dependent dopamine transporter Ki = 58.0 nM 7.24 Inhibition of DAT 23084899

Literature References

PubMed DOI Target Context # Activities
23084899 10.1016/j.bmcl.2012.09.050 Sodium-dependent serotonin transporter 1
23084899 10.1016/j.bmcl.2012.09.050 Sodium-dependent dopamine transporter 1
23084899 10.1016/j.bmcl.2012.09.050 Sodium-dependent noradrenaline transporter 1

Data from ChEMBL 36 via Core Engine