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Compound Detail

CHEMBL204136

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C[C@@H]1CN([C@H](c2ccc(-c3ccccc3C(=O)O)cc2)c2cccc(O)c2)[C@@H](C)CN1Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL204136
Phase Preclinical
Structure Type MOL
InChI Key DSURCNIRDBYQFH-MKVNITDJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

506.6
MW (Da)
6.44
ALogP
4
HBA
2
HBD
64.0
PSA (Ų)
0.30
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H34N2O3
MW 506.65
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -0.36

Activity Summary

IC50 1 meas. best 10.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL3222
IC50 10.7 10.7 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Delta-type opioid receptor IC50 = 0.01995 nM 10.7 Agonist activity at delta opioid receptor in mouse vas deferens 16290934

Literature References

PubMed DOI Target Context # Activities
16290934 10.1016/j.bmcl.2005.10.102 Caco-2 2
16290934 10.1016/j.bmcl.2005.10.102 Delta-type opioid receptor 1
16290934 10.1016/j.bmcl.2005.10.102 No relevant target 1

Data from ChEMBL 36 via Core Engine