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Compound Detail

CHEMBL373873

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Cc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL373873
Phase Preclinical
Structure Type MOL
InChI Key AARWRAFDYZSYPD-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

501.5
MW (Da)
4.27
ALogP
6
HBA
1
HBD
66.3
PSA (Ų)
0.44
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H30Cl2N6O
MW 501.46
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -2.05

Activity Summary

Ki 5 meas. best 8.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 8.37 8.37 4.3 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 8.13 8.13 7.4 1
D(2) dopamine receptor
CHEMBL217
Ki 7.85 7.63 14.0 2
D(4) dopamine receptor
CHEMBL219
Ki 6.55 6.55 281.8 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 D(2) dopamine receptor 1
26299826 10.1016/j.bmc.2015.07.050 Unchecked 1
26299826 10.1016/j.bmc.2015.07.050 5-hydroxytryptamine receptor 2A 1

Data from ChEMBL 36 via Core Engine