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Compound Detail

CHEMBL319119

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COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4cc(F)ccc4F)CC3)[C@@H]1CO2

Basic Information

ChEMBL ID CHEMBL319119
Phase Preclinical
Structure Type MOL
InChI Key NDIXVNRNAFQAJZ-HNQXZTCOSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

499.6
MW (Da)
3.81
ALogP
7
HBA
0
HBD
55.8
PSA (Ų)
0.58
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 C27H31F2N3O4
MW 499.56
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness -0.50

Activity Summary

Ki 3 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 9.7 9.7 0.2 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 9.52 9.52 0.3 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 8.49 8.49 3.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15125959 10.1016/j.bmcl.2004.03.031 Sodium-dependent serotonin transporter 2
15125959 10.1016/j.bmcl.2004.03.031 Alpha-2A adrenergic receptor 1
15125959 10.1016/j.bmcl.2004.03.031 Alpha-2C adrenergic receptor 1
15125959 10.1016/j.bmcl.2004.03.031 Adrenergic receptor alpha-2 1

Data from ChEMBL 36 via Core Engine