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Compound Detail

CHEMBL247687

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COc1ccccc1OC(c1cccc(I)c1)C1CNCCO1

Basic Information

ChEMBL ID CHEMBL247687
Phase Preclinical
Structure Type MOL
InChI Key MGRHQJGGNQRJSA-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

425.3
MW (Da)
3.41
ALogP
4
HBA
1
HBD
39.7
PSA (Ų)
0.75
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 C18H20INO3
MW 425.27
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -0.23

Activity Summary

Ki 1 meas. best 7.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Norepinephrine transporter
CHEMBL304
Ki 7.81 7.81 15.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Norepinephrine transporter Ki = 15.4 nM 7.81 Displacement of [3H]nisoxetine from NET in rat brain membranes 17095215

Literature References

PubMed DOI Target Context # Activities
17095215 10.1016/j.bmcl.2006.10.018 Norepinephrine transporter 1
17095215 10.1016/j.bmcl.2006.10.018 Sodium-dependent dopamine transporter 1
17095215 10.1016/j.bmcl.2006.10.018 Sodium-dependent serotonin transporter 1

Data from ChEMBL 36 via Core Engine