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Compound Detail

CHEMBL218444

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COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(Br)ccc3[nH]2)CC1

Basic Information

ChEMBL ID CHEMBL218444
Phase Preclinical
Structure Type MOL
InChI Key POFDQHAFICYDAQ-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

485.4
MW (Da)
4.27
ALogP
4
HBA
2
HBD
60.6
PSA (Ų)
0.47
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29BrN4O2
MW 485.43
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.45

Activity Summary

Ki 3 meas. best 9.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 9.61 9.61 0.2 1
D(4) dopamine receptor
CHEMBL219
Ki 7.8 7.8 15.8 1
D(2) dopamine receptor
CHEMBL217
Ki 6.96 6.96 109.7 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(2) dopamine receptor 1
17266201 10.1021/jm0611152 D(3) dopamine receptor 1
17266201 10.1021/jm0611152 D(4) dopamine receptor 1

Data from ChEMBL 36 via Core Engine