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Compound Detail

CHEMBL566533

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CCOC(=O)c1cc2cc(OCCCN3CCN(c4cccc(Cl)c4)CC3)ccc2[nH]1

Basic Information

ChEMBL ID CHEMBL566533
Phase Preclinical
Structure Type MOL
InChI Key QSFMQTFAVWMEGW-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

442.0
MW (Da)
4.59
ALogP
5
HBA
1
HBD
57.8
PSA (Ų)
0.41
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28ClN3O3
MW 441.96
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.60

Activity Summary

Ki 6 meas. best 8.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL324
Ki 8.89 8.89 1.3 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.48 7.48 32.9 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 7.41 7.41 39.0 1
D(1A) dopamine receptor
CHEMBL265
Ki 5.97 5.97 1070.0 1
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 5.87 5.87 1350.0 1
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19954866 10.1016/j.ejmech.2009.11.023 D(2) dopamine receptor 1
19954866 10.1016/j.ejmech.2009.11.023 Adrenergic receptor alpha-2 1
19954866 10.1016/j.ejmech.2009.11.023 D(1A) dopamine receptor 1
19954866 10.1016/j.ejmech.2009.11.023 Adrenergic receptor alpha-1 1
19954866 10.1016/j.ejmech.2009.11.023 5-hydroxytryptamine receptor 1A 1
19954866 10.1016/j.ejmech.2009.11.023 5-hydroxytryptamine receptor 2C 1
19954866 10.1016/j.ejmech.2009.11.023 5-hydroxytryptamine receptor 2A 1

Data from ChEMBL 36 via Core Engine