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Compound Detail

CHEMBL521350

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COc1cccc([C@H]2CC[C@@H](N3CCN(c4ccccn4)CC3)CC2)c1

Basic Information

ChEMBL ID CHEMBL521350
Phase Preclinical
Structure Type MOL
InChI Key SHEZXZSIBXLQMP-PUZFROQSSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

351.5
MW (Da)
3.94
ALogP
4
HBA
0
HBD
28.6
PSA (Ų)
0.83
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H29N3O
MW 351.49
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.38

Activity Summary

Ki 5 meas. best 7.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 7.44 7.44 36.1 1
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase
CHEMBL5525
Ki 7.34 7.34 45.4 1
Sigma non-opioid intracellular receptor 1
CHEMBL4153
Ki 6.75 6.75 178.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 6.11 6.11 783.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 6.09 6.09 815.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19053780 10.1021/jm800965b Unchecked 3
19053780 10.1021/jm800965b 5-hydroxytryptamine receptor 1A 1
19053780 10.1021/jm800965b D(2) dopamine receptor 1
19053780 10.1021/jm800965b Adrenergic receptor alpha-1 1
19053780 10.1021/jm800965b 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase 1
19053780 10.1021/jm800965b Sigma non-opioid intracellular receptor 1 1
19053780 10.1021/jm800965b PC-3 1

Data from ChEMBL 36 via Core Engine