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Compound Detail

CHEMBL610046

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O=C1[C@@H](Cc2ccccc2)C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5

Basic Information

ChEMBL ID CHEMBL610046
Phase Preclinical
Structure Type MOL
InChI Key ZLMLSUIQTYFLKF-XKVUGNILSA-N
4
Targets
4
Activities
1
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

431.5
MW (Da)
2.99
ALogP
5
HBA
2
HBD
70.0
PSA (Ų)
0.78
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 C27H29NO4
MW 431.53
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness 1.23

Activity Summary

Ki 4 meas. best 9.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
Ki 9.92 9.92 0.1 1
Delta-type opioid receptor
CHEMBL269
Ki 9.07 9.07 0.9 1
Mu-type opioid receptor
CHEMBL233
Ki 8.85 8.85 1.4 1
Kappa-type opioid receptor
CHEMBL3952
Ki 7.6 7.6 25.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ke 1.5 nM -
Ke 21.0 nM Cavia porcellus
Ke - - Cavia porcellus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8126697 10.1021/jm00031a006 Delta-type opioid receptor 4
8126697 10.1021/jm00031a006 Mu-type opioid receptor 3
8126697 10.1021/jm00031a006 Kappa-type opioid receptor 3
22818080 10.1016/j.bmcl.2012.06.085 Glutathione reductase, putative 2
8126697 10.1021/jm00031a006 Opioid receptors; mu & delta 1

Data from ChEMBL 36 via Core Engine