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Compound Detail

CHEMBL4545050

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C[C@H]1[C@H]2Cc3ccc(O)cc3[C@]1(C)CCN2CCC(=O)N1CCc2ccccc2C1c1ccccc1

Basic Information

ChEMBL ID CHEMBL4545050
Phase Preclinical
Structure Type MOL
InChI Key ONHACLFIIHPLGZ-IQACEWDJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

480.6
MW (Da)
5.48
ALogP
3
HBA
1
HBD
43.8
PSA (Ų)
0.54
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H36N2O2
MW 480.65
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness 0.33

Activity Summary

Ki 1 meas. best 7.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL233
Ki 7.02 7.02 96.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mu-type opioid receptor Ki = 96.0 nM 7.02 Displacement of [3H]DAMGO from MOR in HEK293 cells 27624520

Literature References

PubMed DOI Target Context # Activities
27624520 10.1016/j.bmc.2016.08.057 Unchecked 2
27624520 10.1016/j.bmc.2016.08.057 Mu-type opioid receptor 1
27624520 10.1016/j.bmc.2016.08.057 Kappa-type opioid receptor 1
27624520 10.1016/j.bmc.2016.08.057 Delta-type opioid receptor 1

Data from ChEMBL 36 via Core Engine