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Compound Detail

CHEMBL425567

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COc1ccccc1N1CCN(CCCNc2ccn3c(n2)nc2c3c(=O)n(C)c(=O)n2C)CC1

Basic Information

ChEMBL ID CHEMBL425567
Phase Preclinical
Structure Type MOL
InChI Key XIXQLRQXQQAYSG-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

478.6
MW (Da)
0.91
ALogP
11
HBA
1
HBD
101.9
PSA (Ų)
0.39
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30N8O3
MW 478.56
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.61

Activity Summary

Ki 5 meas. best 7.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.48 7.48 33.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 7.47 7.47 34.0 1
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 6.08 6.08 835.0 1
D(2) dopamine receptor
CHEMBL339
Ki 5.93 5.93 1175.0 1
Unchecked
CHEMBL612545
Ki 5.93 5.93 1174.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15115407 10.1021/jm030946u 5-hydroxytryptamine receptor 1A 2
15115407 10.1021/jm030946u 5-hydroxytryptamine receptor 2A 2
15115407 10.1021/jm030946u D(2) dopamine receptor 1
15115407 10.1021/jm030946u Adrenergic receptor alpha-1 1
15808487 10.1016/j.bmcl.2005.02.012 Unchecked 1

Data from ChEMBL 36 via Core Engine