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Compound Detail

CHEMBL485554

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CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@H](N(C)C(=O)/C=C/c2ccoc2)CC[C@@]3(O)[C@H]1C5

Basic Information

ChEMBL ID CHEMBL485554
Phase Preclinical
Structure Type MOL
InChI Key PPDFJRNKNGMZKI-SCKIEVSZSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

436.5
MW (Da)
2.31
ALogP
6
HBA
2
HBD
86.4
PSA (Ų)
0.72
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 C25H28N2O5
MW 436.51
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness 1.58

Activity Summary

IC50 1 meas. best 7.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL4329
IC50 7.26 7.26 55.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ke 8.1 nM Mus musculus
Ke 33.0 nM Mus musculus
Ke 6.3 nM Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18829333 10.1016/j.bmc.2008.09.011 Kappa-type opioid receptor 2
18829333 10.1016/j.bmc.2008.09.011 Mu-type opioid receptor 1
18829333 10.1016/j.bmc.2008.09.011 Delta-type opioid receptor 1
18829333 10.1016/j.bmc.2008.09.011 Mus musculus 1

Data from ChEMBL 36 via Core Engine