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Compound Detail

CHEMBL515864

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O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1

Basic Information

ChEMBL ID CHEMBL515864
Phase Preclinical
Structure Type MOL
InChI Key XQWZTPWKACKUMJ-FSTJURTJSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

447.5
MW (Da)
2.15
ALogP
6
HBA
3
HBD
94.9
PSA (Ų)
0.66
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 C26H29N3O4
MW 447.54
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness 0.77

Activity Summary

Ki 3 meas. best 9.32
EC50 1 meas. best 8.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL233
Ki 9.32 9.32 0.5 1
Mu-type opioid receptor
CHEMBL233
EC50 8.9 8.9 1.3 1
Kappa-type opioid receptor
CHEMBL237
Ki 7.71 7.71 19.6 1
Delta-type opioid receptor
CHEMBL236
Ki 6.73 6.73 186.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19199782 10.1021/jm801272c Mu-type opioid receptor 4
19199782 10.1021/jm801272c Unchecked 2
19199782 10.1021/jm801272c Mus musculus 1
19199782 10.1021/jm801272c Kappa-type opioid receptor 1
19199782 10.1021/jm801272c Delta-type opioid receptor 1

Data from ChEMBL 36 via Core Engine