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Compound Detail

CHEMBL127802

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CCCCN1CCC(=C(c2ccccc2)c2ccc(C(=O)N(CC)CC)cc2)CC1

Basic Information

ChEMBL ID CHEMBL127802
Phase Preclinical
Structure Type MOL
InChI Key IBGYSLZJAPQZEL-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

404.6
MW (Da)
5.87
ALogP
2
HBA
0
HBD
23.6
PSA (Ų)
0.55
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H36N2O
MW 404.60
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.93

Activity Summary

IC50 3 meas. best 8.19
EC50 1 meas. best 7.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
IC50 8.19 8.19 6.5 1
Delta-type opioid receptor
CHEMBL236
EC50 7.34 7.34 46.0 1
Mu-type opioid receptor
CHEMBL233
IC50 5.38 5.38 4130.0 1
Kappa-type opioid receptor
CHEMBL237
IC50 5.37 5.37 4270.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11052794 10.1021/jm000229p Delta-type opioid receptor 3
11052794 10.1021/jm000229p Mu-type opioid receptor 1
11052794 10.1021/jm000229p Kappa-type opioid receptor 1
11052794 10.1021/jm000229p Opioid receptors; mu & delta 1
11052794 10.1021/jm000229p Opioid receptors; delta & kappa 1

Data from ChEMBL 36 via Core Engine