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Compound Detail

CHEMBL109124

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COc1cccc(C23CCN(C)C(C2)/C(=C\c2ccccc2)C(=O)C3)c1

Basic Information

ChEMBL ID CHEMBL109124
Phase Preclinical
Structure Type MOL
InChI Key QZJJWXHOVZHRTH-DEDYPNTBSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

347.5
MW (Da)
4.08
ALogP
3
HBA
0
HBD
29.5
PSA (Ų)
0.78
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25NO2
MW 347.46
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness 0.40

Activity Summary

Ki 6 meas. best 7.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sigma 2 receptor
CHEMBL613288
Ki 7.28 7.185 52.0 2
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 6.86 6.8533 137.7 3
Muscarinic acetylcholine receptor
CHEMBL1907609
Ki 4.94 4.94 11600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7490727 10.1021/jm00024a005 Sigma 2 receptor 4
7490727 10.1021/jm00024a005 Sigma non-opioid intracellular receptor 1 2
7490727 10.1021/jm00024a005 Mu-type opioid receptor 2
7490727 10.1021/jm00024a005 Delta-type opioid receptor 2
7490727 10.1021/jm00024a005 Kappa-type opioid receptor 2
7932540 10.1021/jm00045a022 Sigma non-opioid intracellular receptor 1 1
7932540 10.1021/jm00045a022 Glutamate NMDA receptor 1
7932540 10.1021/jm00045a022 Muscarinic acetylcholine receptor 1

Data from ChEMBL 36 via Core Engine