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Compound Detail

CHEMBL174569

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CCN(CC)C(=O)c1ccc(N(c2cccc(OC)c2)[C@@H]2CCN(CC3CC3)C[C@@H]2C)cc1

Basic Information

ChEMBL ID CHEMBL174569
Phase Preclinical
Structure Type MOL
InChI Key KEHOXWIRLSRNHN-KDYSTLNUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

449.6
MW (Da)
5.44
ALogP
4
HBA
0
HBD
36.0
PSA (Ų)
0.51
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H39N3O2
MW 449.64
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.08

Activity Summary

Ki 1 meas. best 7.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL269
Ki 7.44 7.44 36.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Delta-type opioid receptor Ki = 36.0 nM 7.44 Affinity of [H]DADLE to the delta opioid receptor from rat brain 11300879

Literature References

PubMed DOI Target Context # Activities
11300879 10.1021/jm000427g Mu-type opioid receptor 1
11300879 10.1021/jm000427g Delta-type opioid receptor 1
11300879 10.1021/jm000427g Kappa-type opioid receptor 1
11300879 10.1021/jm000427g Opioid receptors; mu & delta 1
11300879 10.1021/jm000427g Unchecked 1

Data from ChEMBL 36 via Core Engine