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Compound Detail

CHEMBL218351

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CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccc(OC)cc1

Basic Information

ChEMBL ID CHEMBL218351
Phase Preclinical
Structure Type MOL
InChI Key VNQMWRQYPRIJGM-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

520.7
MW (Da)
3.63
ALogP
8
HBA
1
HBD
84.8
PSA (Ų)
0.34
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H40N6O3
MW 520.68
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.62

Activity Summary

Ki 5 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL217
Ki 8.15 7.76 7.1 2
D(3) dopamine receptor
CHEMBL234
Ki 7.89 7.89 12.9 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 7.54 7.54 29.0 1
D(4) dopamine receptor
CHEMBL219
Ki 6.89 6.89 128.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17266201 10.1021/jm0611152 Dopamine receptors; D2 & D3 1
17266201 10.1021/jm0611152 Dopamine receptors; D3 & D4 1
17266201 10.1021/jm0611152 D(3) dopamine receptor 1
17266201 10.1021/jm0611152 D(4) dopamine receptor 1
17266201 10.1021/jm0611152 D(2) dopamine receptor 1
26299826 10.1016/j.bmc.2015.07.050 Unchecked 1
26299826 10.1016/j.bmc.2015.07.050 D(2) dopamine receptor 1
26299826 10.1016/j.bmc.2015.07.050 5-hydroxytryptamine receptor 2A 1

Data from ChEMBL 36 via Core Engine