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Compound Detail

CHEMBL108245

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COc1cccc2c1CCCC2NCCN1CCN(c2ccccn2)CC1

Basic Information

ChEMBL ID CHEMBL108245
Phase Preclinical
Structure Type MOL
InChI Key WMEXYJKBXVWCOJ-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

366.5
MW (Da)
2.88
ALogP
5
HBA
1
HBD
40.6
PSA (Ų)
0.85
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 C22H30N4O
MW 366.51
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -1.46

Activity Summary

IC50 5 meas. best 7.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL273
IC50 7.31 7.31 49.0 1
Adrenergic receptor alpha-2
CHEMBL2093864
IC50 7.02 7.02 95.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 6.14 6.14 725.0 1
D(2) dopamine receptor
CHEMBL339
IC50 5.73 5.73 1850.0 1
Serotonin 2 (5-HT2) receptor
CHEMBL2093870
IC50 5.04 5.04 9140.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8759642 10.1021/jm960087s Unchecked 3
8759642 10.1021/jm960087s 5-hydroxytryptamine receptor 1A 1
8759642 10.1021/jm960087s Serotonin 2 (5-HT2) receptor 1
8759642 10.1021/jm960087s D(2) dopamine receptor 1
8759642 10.1021/jm960087s Adrenergic receptor alpha-1 1
8759642 10.1021/jm960087s Adrenergic receptor alpha-2 1
8759642 10.1021/jm960087s Serotonin 1a (5-HT1a) receptor/Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine