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Compound Detail

CHEMBL64261

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COc1cc2c(cc1OC)CN(CCNC(=O)c1cc(Br)ccc1OC)CC2

Basic Information

ChEMBL ID CHEMBL64261
Phase Preclinical
Structure Type MOL
InChI Key KSANSFZVRVSECI-UHFFFAOYSA-N
5
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

449.4
MW (Da)
3.26
ALogP
5
HBA
1
HBD
60.0
PSA (Ų)
0.70
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 C21H25BrN2O4
MW 449.35
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.11

Activity Summary

Ki 6 meas. best 7.91

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 7.91 7.91 12.4 1
Sigma 2 receptor
CHEMBL613288
Ki 7.91 7.91 12.4 1
D(3) dopamine receptor
CHEMBL3138
Ki 6.31 6.31 488.0 1
D(2) dopamine receptor
CHEMBL339
Ki 5.45 5.45 3570.0 1
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 5.26 5.26 5484.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14684327 10.1016/j.bmcl.2003.09.083 Sigma non-opioid intracellular receptor 1 2
23734634 10.1021/jm301545c Unchecked 2
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 2 receptor 1
23734634 10.1021/jm301545c Sigma non-opioid intracellular receptor 1 1

Data from ChEMBL 36 via Core Engine