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Compound Detail

CHEMBL358895

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COc1ccccc1N1CCN(CC2CC(=O)c3ccoc3C2)CC1

Basic Information

ChEMBL ID CHEMBL358895
Phase Preclinical
Structure Type MOL
InChI Key KDVQFYXINILZBG-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

340.4
MW (Da)
2.86
ALogP
5
HBA
0
HBD
45.9
PSA (Ų)
0.86
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 C20H24N2O3
MW 340.42
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.53

Activity Summary

Kd 2 meas. best 6.19
Ki 2 meas. best 5.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2B
CHEMBL323
Kd 6.19 6.19 645.6 2
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 5.64 5.64 2290.9 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 4.89 4.89 12882.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11754579 10.1021/jm011014y 5-hydroxytryptamine receptor 2A 2
11754579 10.1021/jm011014y 5-hydroxytryptamine receptor 2B 1
11754579 10.1021/jm011014y 5-hydroxytryptamine receptor 2C 1
11754579 10.1021/jm011014y Serotonin receptor 2a and 2b (5HT2A and 5HT2B) 1
11754579 10.1021/jm011014y Serotonin receptor 2a and 2c (5HT2A and 5HT2C) 1
11101359 10.1021/jm0009890 5-hydroxytryptamine receptor 2A 1
11101359 10.1021/jm0009890 5-hydroxytryptamine receptor 2C 1
11101359 10.1021/jm0009890 D(1A) dopamine receptor 1
11101359 10.1021/jm0009890 D(2) dopamine receptor 1
11101359 10.1021/jm0009890 Unchecked 1
11101359 10.1021/jm0009890 Dopamine D2 receptor and serotonin 2a receptor 1
11101359 10.1021/jm0009890 5-hydroxytryptamine receptor 2B 1

Data from ChEMBL 36 via Core Engine