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Compound Detail

CHEMBL60133

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COc1c(C(=O)NCCN2CCc3ccccc3C2)cc(Br)c2ccccc12

Basic Information

ChEMBL ID CHEMBL60133
Phase Preclinical
Structure Type MOL
InChI Key LQOYFQQIZFEVDY-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

439.4
MW (Da)
4.40
ALogP
3
HBA
1
HBD
41.6
PSA (Ų)
0.64
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H23BrN2O2
MW 439.35
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.96

Activity Summary

Ki 4 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 7.82 7.82 15.1 1
Sigma 2 receptor
CHEMBL613288
Ki 7.32 7.32 47.7 1
D(3) dopamine receptor
CHEMBL3138
Ki 7.09 7.09 81.6 1
D(2) dopamine receptor
CHEMBL339
Ki 6.88 6.88 131.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14684327 10.1016/j.bmcl.2003.09.083 D(2) dopamine receptor 1
14684327 10.1016/j.bmcl.2003.09.083 D(3) dopamine receptor 1
14684327 10.1016/j.bmcl.2003.09.083 Sigma non-opioid intracellular receptor 1 1
14684327 10.1016/j.bmcl.2003.09.083 Sigma 2 receptor 1

Data from ChEMBL 36 via Core Engine