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Compound Detail

CHEMBL2113654

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C=CCN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(OCC)[C@H]1C5

Basic Information

ChEMBL ID CHEMBL2113654
Phase Preclinical
Structure Type MOL
InChI Key DIAAKKARDRDKAQ-NVSKSXHLSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

428.5
MW (Da)
4.39
ALogP
4
HBA
2
HBD
57.7
PSA (Ų)
0.61
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H28N2O3
MW 428.53
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness 1.29

Activity Summary

Ki 4 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
Ki 9.0 9.0 1.0 1
Delta-type opioid receptor
CHEMBL269
Ki 8.59 8.59 2.6 1
Kappa-type opioid receptor
CHEMBL3952
Ki 6.46 6.46 349.0 1
Mu-type opioid receptor
CHEMBL270
Ki 5.86 5.86 1368.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12431065 10.1021/jm020940p Delta-type opioid receptor 2
12431065 10.1021/jm020940p Mu-type opioid receptor 2
12431065 10.1021/jm020940p Kappa-type opioid receptor 2
12431065 10.1021/jm020940p Opioid receptors; mu & delta 1
12431065 10.1021/jm020940p Unchecked 1

Data from ChEMBL 36 via Core Engine