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Compound Detail

CHEMBL3764390

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O=C(NCCCN1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccncc1

Basic Information

ChEMBL ID CHEMBL3764390
Phase Preclinical
Structure Type MOL
InChI Key GQPZNEKXJZVZFM-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

382.5
MW (Da)
1.75
ALogP
6
HBA
1
HBD
66.9
PSA (Ų)
0.74
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H26N4O3
MW 382.46
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.29

Activity Summary

Ki 3 meas. best 10.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 10.95 10.95 0.0 1
5-hydroxytryptamine receptor 2C
CHEMBL324
Ki 8.66 8.66 2.2 1
D(1A) dopamine receptor
CHEMBL265
Ki 6.9 6.9 127.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26820556 10.1016/j.ejmech.2016.01.021 Mus musculus 7
26820556 10.1016/j.ejmech.2016.01.021 Rattus norvegicus 2
26820556 10.1016/j.ejmech.2016.01.021 5-hydroxytryptamine receptor 1A 1
26820556 10.1016/j.ejmech.2016.01.021 5-hydroxytryptamine receptor 2A 1
26820556 10.1016/j.ejmech.2016.01.021 5-hydroxytryptamine receptor 2C 1
26820556 10.1016/j.ejmech.2016.01.021 Adrenergic receptor alpha-1 1
26820556 10.1016/j.ejmech.2016.01.021 Adrenergic receptor alpha-2 1
26820556 10.1016/j.ejmech.2016.01.021 D(1A) dopamine receptor 1
26820556 10.1016/j.ejmech.2016.01.021 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine