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Compound Detail

CHEMBL64176

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COc1cc2c(cc1OC)CN(CCNC(=O)c1cc(Br)cc(OC)c1OC)CC2

Basic Information

ChEMBL ID CHEMBL64176
Phase Preclinical
Structure Type MOL
InChI Key GSHZYENJHIPEJJ-UHFFFAOYSA-N
6
Targets
7
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

479.4
MW (Da)
3.27
ALogP
6
HBA
1
HBD
69.3
PSA (Ų)
0.63
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 C22H27BrN2O5
MW 479.37
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.86

Activity Summary

Ki 7 meas. best 7.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 7.79 7.79 16.4 1
Sigma 2 receptor
CHEMBL613288
Ki 7.79 7.79 16.4 1
D(3) dopamine receptor
CHEMBL3138
Ki 7.67 7.67 21.4 1
D(4) dopamine receptor
CHEMBL219
Ki 6.58 6.58 265.0 1
D(2) dopamine receptor
CHEMBL339
Ki 6.15 6.15 714.0 1
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 5.53 5.53 2932.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
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 Dopamine receptor D2 and D3 1
14684327 10.1016/j.bmcl.2003.09.083 D(4) 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
14684327 10.1016/j.bmcl.2003.09.083 Dopamine receptors; D3 & D4 1
23734634 10.1021/jm301545c Sigma non-opioid intracellular receptor 1 1

Data from ChEMBL 36 via Core Engine