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Compound Detail

CHEMBL429929

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COc1cccc(C(=O)N[C@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)c1

Basic Information

ChEMBL ID CHEMBL429929
Phase Preclinical
Structure Type MOL
InChI Key MCVSUAXKBBAXPV-QLDGPFJWSA-N
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

476.6
MW (Da)
2.76
ALogP
6
HBA
3
HBD
91.3
PSA (Ų)
0.61
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32N2O5
MW 476.57
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness 0.70

Activity Summary

Ki 3 meas. best 9.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL233
Ki 9.8 9.8 0.2 1
Kappa-type opioid receptor
CHEMBL237
Ki 9.14 9.14 0.7 1
Delta-type opioid receptor
CHEMBL236
Ki 8.23 8.23 5.8 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.8167 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18298057 10.1021/jm701060e Unchecked 2
18298057 10.1021/jm701060e Mu-type opioid receptor 1
18298057 10.1021/jm701060e Delta-type opioid receptor 1
18298057 10.1021/jm701060e Kappa-type opioid receptor 1
18298057 10.1021/jm701060e Liver 1

Data from ChEMBL 36 via Core Engine