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Compound Detail

CHEMBL5283662

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COc1cccc(C2(O)CCN(C(=O)Cc3cccc([N+](=O)[O-])c3)CC2CN(C)C)c1

Basic Information

ChEMBL ID CHEMBL5283662
Phase Preclinical
Structure Type MOL
InChI Key USGDSNXARSJEOU-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

427.5
MW (Da)
2.44
ALogP
6
HBA
1
HBD
96.2
PSA (Ų)
0.54
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H29N3O5
MW 427.50
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -0.85

Activity Summary

Ki 2 meas. best 7.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL2858
Ki 7.07 7.07 85.6 1
Kappa-type opioid receptor
CHEMBL237
Ki 5.7 5.7 1987.0 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