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Compound Detail

CHEMBL4448285

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COc1ccc2[nH]cc(CCNCc3ccc(-c4cnc5ccccc5c4)o3)c2c1

Basic Information

ChEMBL ID CHEMBL4448285
Phase Preclinical
Structure Type MOL
InChI Key LDFDHYVHCWAUGE-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

397.5
MW (Da)
5.32
ALogP
4
HBA
2
HBD
63.1
PSA (Ų)
0.37
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23N3O2
MW 397.48
Aromatic Rings 5
Heavy Atoms 30
NP-Likeness -0.87

Activity Summary

Ki 5 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 7.0 7.0 101.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.07 6.07 843.0 1
D(2) dopamine receptor
CHEMBL217
Ki 5.99 5.99 1025.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 5.98 5.98 1052.0 1
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 5.01 5.01 9855.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31734022 10.1016/j.ejmech.2019.111857 5-hydroxytryptamine receptor 6 1
31734022 10.1016/j.ejmech.2019.111857 5-hydroxytryptamine receptor 2A 1
31734022 10.1016/j.ejmech.2019.111857 5-hydroxytryptamine receptor 1A 1
31734022 10.1016/j.ejmech.2019.111857 5-hydroxytryptamine receptor 7 1
31734022 10.1016/j.ejmech.2019.111857 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine