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Compound Detail

CHEMBL2112972

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COc1ccc2c(c1)C=C[C@@H]1C2=NO[C@H]1CN1CCN(Cc2ccc3ccccc3c2)CC1

Basic Information

ChEMBL ID CHEMBL2112972
Phase Preclinical
Structure Type MOL
InChI Key UAHLUVNKSWGJEK-SVBPBHIXSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

439.6
MW (Da)
4.41
ALogP
5
HBA
0
HBD
37.3
PSA (Ų)
0.59
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 C28H29N3O2
MW 439.56
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.36

Activity Summary

Ki 3 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL228
Ki 8.85 8.85 1.4 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 8.74 8.74 1.8 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 8.2 8.2 6.3 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