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Compound Detail

CHEMBL215938

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CC(=O)O[C@H]1C[C@@H](CO)[C@]2(C)CC(=O)[C@H]3CO[C@H](c4ccoc4)CC3(C)[C@H]2C1=O

Basic Information

ChEMBL ID CHEMBL215938
Phase Preclinical
Structure Type MOL
InChI Key UOHZVTISHAIGDV-OQQZPZEBSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

404.5
MW (Da)
2.47
ALogP
7
HBA
1
HBD
103.0
PSA (Ų)
0.77
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 C22H28O7
MW 404.46
Aromatic Rings 1
Heavy Atoms 29
NP-Likeness 2.46

Activity Summary

Ki 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL237
Ki 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Kappa-type opioid receptor Ki = 1000.0 nM 6.0 Inhibition of [3H]diprenorphine binding to human KOR expressed in CHO cells 16777411

Literature References

PubMed DOI Target Context # Activities
16777411 10.1016/j.bmcl.2006.05.093 Kappa-type opioid receptor 3

Data from ChEMBL 36 via Core Engine