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Compound Detail

CHEMBL157046

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COc1cc2c(cc1OC)C(=O)CC(CN1CCN(c3ccccc3OC)CC1)C2

Basic Information

ChEMBL ID CHEMBL157046
Phase Preclinical
Structure Type MOL
InChI Key HOKRGWVLSKYIGL-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

410.5
MW (Da)
3.28
ALogP
6
HBA
0
HBD
51.2
PSA (Ų)
0.73
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 C24H30N2O4
MW 410.51
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.48

Activity Summary

Ki 2 meas. best 6.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL217
Ki 6.08 6.08 831.8 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 5.63 5.63 2344.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14741248 10.1016/j.bmcl.2003.11.064 5-hydroxytryptamine receptor 2A 1
14741248 10.1016/j.bmcl.2003.11.064 5-hydroxytryptamine receptor 2C 1
14741248 10.1016/j.bmcl.2003.11.064 D(2) dopamine receptor 1
14741248 10.1016/j.bmcl.2003.11.064 Serotonin 2 receptors; 5-HT2a & 5-HT2c 1
14741248 10.1016/j.bmcl.2003.11.064 Dopamine D2 receptor and serotonin 2a receptor 1

Data from ChEMBL 36 via Core Engine