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Compound Detail

CHEMBL60322

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COc1ccccc1N1CCN(CCN2C(=O)CC3(CCCCC3)C2=O)CC1

Basic Information

ChEMBL ID CHEMBL60322
Phase Preclinical
Structure Type MOL
InChI Key LSXHXXWLWSECTR-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

385.5
MW (Da)
2.53
ALogP
5
HBA
0
HBD
53.1
PSA (Ų)
0.73
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 C22H31N3O3
MW 385.51
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness -1.11

Activity Summary

IC50 2 meas. best 7.04
Ki 2 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 8.24 8.24 5.7 1
Dopamine receptor
CHEMBL2093868
IC50 7.04 7.04 92.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 6.62 6.62 240.0 1
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 6.59 6.59 254.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
6131130 10.1021/jm00356a014 Dopamine receptor 1
6131130 10.1021/jm00356a014 Rattus norvegicus 1
6131130 10.1021/jm00356a014 Adrenergic receptor alpha-1 1
18603331 10.1016/j.ejmech.2008.05.021 5-hydroxytryptamine receptor 1A 1
18603331 10.1016/j.ejmech.2008.05.021 5-hydroxytryptamine receptor 2A 1

Data from ChEMBL 36 via Core Engine