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Compound Detail

CHEMBL424328

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O=C(CCCCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3

Basic Information

ChEMBL ID CHEMBL424328
Phase Preclinical
Structure Type MOL
InChI Key WFMQFEDXEBTDHZ-NTASORKHSA-N
3
Targets
5
Activities
3
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

817.2
MW (Da)
11.82
ALogP
6
HBA
0
HBD
59.1
PSA (Ų)
0.09
QED
2
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C54H76N2O4
MW 817.21
Aromatic Rings 2
Heavy Atoms 60
NP-Likeness 0.30

Activity Summary

Ki 3 meas. best 8.96
EC50 1 meas. best 8.09
IC50 1 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL237
Ki 8.96 8.96 1.1 1
Mu-type opioid receptor
CHEMBL233
Ki 8.74 8.74 1.8 1
Kappa-type opioid receptor
CHEMBL237
EC50 8.09 8.09 8.1 1
Delta-type opioid receptor
CHEMBL236
Ki 7.09 7.09 82.0 1
Mu-type opioid receptor
CHEMBL233
IC50 7.0 7.0 100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14613319 10.1021/jm030139v Mu-type opioid receptor 5
14613319 10.1021/jm030139v Kappa-type opioid receptor 4
14613319 10.1021/jm030139v Delta-type opioid receptor 1
14613319 10.1021/jm030139v Opioid receptors; mu & kappa 1
14613319 10.1021/jm030139v Opioid receptors; delta & kappa 1

Data from ChEMBL 36 via Core Engine