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Compound Detail

CHEMBL60140

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COc1cc2c(cc1OC)CN(CCNC(=O)c1cc(Br)c3ccccc3c1OC)CC2

Basic Information

ChEMBL ID CHEMBL60140
Phase Preclinical
Structure Type MOL
InChI Key NJTZXTZDMKNNIW-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

499.4
MW (Da)
4.42
ALogP
5
HBA
1
HBD
60.0
PSA (Ų)
0.52
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27BrN2O4
MW 499.41
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.73

Activity Summary

Ki 4 meas. best 7.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sigma 2 receptor
CHEMBL613288
Ki 7.67 7.67 21.2 1
D(3) dopamine receptor
CHEMBL3138
Ki 6.9 6.9 126.5 1
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 6.72 6.72 189.1 1
D(2) dopamine receptor
CHEMBL339
Ki 6.62 6.62 240.5 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