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Compound Detail

CHEMBL385289

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COc1ccccc1N1CCN(CCCCNC(=O)c2nnn(Cc3ccccc3Br)c2C)CC1

Basic Information

ChEMBL ID CHEMBL385289
Phase Preclinical
Structure Type MOL
InChI Key YFSQZKVPESKTJY-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

541.5
MW (Da)
3.74
ALogP
7
HBA
1
HBD
75.5
PSA (Ų)
0.39
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H33BrN6O2
MW 541.49
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.94

Activity Summary

Ki 5 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL217
Ki 7.77 7.49 17.0 2
D(3) dopamine receptor
CHEMBL234
Ki 7.49 7.49 32.4 1
D(4) dopamine receptor
CHEMBL219
Ki 7.04 7.04 91.2 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.82 6.82 150.0 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