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Compound Detail

CHEMBL328377

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COc1cc2c(cc1OC)C1=NOC(CN3CCN(CC4=Cc5ccccc5C4)CC3)C1CO2

Basic Information

ChEMBL ID CHEMBL328377
Phase Preclinical
Structure Type MOL
InChI Key AQDOXXILINNVJB-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

461.6
MW (Da)
3.07
ALogP
7
HBA
0
HBD
55.8
PSA (Ų)
0.66
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H31N3O4
MW 461.56
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness 0.13

Activity Summary

Ki 4 meas. best 8.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL313
Ki 8.39 8.39 4.1 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 8.33 8.33 4.7 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 7.66 7.66 22.0 1
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 6.5 6.5 315.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12873501 10.1016/s0960-894x(03)00525-0 Sodium-dependent serotonin transporter 2
12873501 10.1016/s0960-894x(03)00525-0 Alpha-2A adrenergic receptor 1
12873501 10.1016/s0960-894x(03)00525-0 Alpha-2B adrenergic receptor 1
12873501 10.1016/s0960-894x(03)00525-0 Alpha-2C adrenergic receptor 1
12873501 10.1016/s0960-894x(03)00525-0 Adrenergic receptor alpha-2 1

Data from ChEMBL 36 via Core Engine