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Compound Detail

CHEMBL517730

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COc1cccc2c1C1CCN(CCCCNC(=O)C3=Cc4ccccc4CN3)CC1=N2

Basic Information

ChEMBL ID CHEMBL517730
Phase Preclinical
Structure Type MOL
InChI Key ULYVPXBJTVSSBH-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

430.6
MW (Da)
3.61
ALogP
5
HBA
2
HBD
66.0
PSA (Ų)
0.66
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 C26H30N4O2
MW 430.55
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.42

Activity Summary

Ki 5 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 8.22 8.22 6.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 6.93 6.93 118.0 1
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 6.83 6.83 149.0 1
Unchecked
CHEMBL612545
Ki 6.36 6.36 434.0 1
D(2) dopamine receptor
CHEMBL339
Ki 5.19 5.19 6475.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19072656 10.1021/jm800689g Voltage-gated inwardly rectifying potassium channel KCNH2 1
19072656 10.1021/jm800689g Unchecked 1
19072656 10.1021/jm800689g 5-hydroxytryptamine receptor 2A 1
19072656 10.1021/jm800689g 5-hydroxytryptamine receptor 1A 1
19072656 10.1021/jm800689g D(3) dopamine receptor 1
19072656 10.1021/jm800689g D(2) dopamine receptor 1
19072656 10.1021/jm800689g D(1A) dopamine receptor 1

Data from ChEMBL 36 via Core Engine