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Compound Detail

CHEMBL5285920

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COc1cccc(C2(O)CCN(C(=O)Cc3cccc4ccccc34)CC2CN(C)C)c1

Basic Information

ChEMBL ID CHEMBL5285920
Phase Preclinical
Structure Type MOL
InChI Key GWWQSZZYTWGWRT-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

432.6
MW (Da)
3.69
ALogP
4
HBA
1
HBD
53.0
PSA (Ų)
0.65
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32N2O3
MW 432.56
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.49

Activity Summary

Ki 3 meas. best 6.45

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL2858
Ki 6.45 6.45 353.0 1
Kappa-type opioid receptor
CHEMBL237
Ki 5.77 5.77 1701.0 1
Delta-type opioid receptor
CHEMBL236
Ki 5.67 5.67 2155.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34152138 10.1021/acs.jmedchem.1c00722 Unchecked 2
34152138 10.1021/acs.jmedchem.1c00722 Mu-type opioid receptor 1
34152138 10.1021/acs.jmedchem.1c00722 Delta-type opioid receptor 1
34152138 10.1021/acs.jmedchem.1c00722 Kappa-type opioid receptor 1
34152138 10.1021/acs.jmedchem.1c00722 Mus musculus 1

Data from ChEMBL 36 via Core Engine