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Compound Detail

CHEMBL180322

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C=CC(=O)Oc1ccc2c(c1)OC[C@@H]1C2=NO[C@H]1CN1CCN(C/C(C)=C/c2ccccc2)CC1

Basic Information

ChEMBL ID CHEMBL180322
Phase Preclinical
Structure Type MOL
InChI Key QHCZSHHKZDDCEC-MSKIIMLESA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

473.6
MW (Da)
3.61
ALogP
7
HBA
0
HBD
63.6
PSA (Ų)
0.35
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H31N3O4
MW 473.57
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.12

Activity Summary

Ki 3 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 9.3 9.3 0.5 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 9.05 9.05 0.9 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 7.39 7.39 41.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15771448 10.1021/jm049619s Sodium-dependent serotonin transporter 2
15771448 10.1021/jm049619s Alpha-2A adrenergic receptor 1
15771448 10.1021/jm049619s Alpha-2C adrenergic receptor 1
15771448 10.1021/jm049619s Adrenergic receptor alpha-2 1

Data from ChEMBL 36 via Core Engine