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Compound Detail

CHEMBL316930

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C=C(C)CN1CCC23c4c5ccc(O)c4O[C@H]2c2n[nH]cc2C[C@@]3(O)C1C5

Basic Information

ChEMBL ID CHEMBL316930
Phase Preclinical
Structure Type MOL
InChI Key XYNMWXGXZKKUFD-GRDMHCDQSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

365.4
MW (Da)
1.98
ALogP
5
HBA
3
HBD
81.6
PSA (Ų)
0.71
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23N3O3
MW 365.43
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness 1.03

Activity Summary

Ki 6 meas. best 7.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL237
Ki 7.42 7.42 38.0 1
Kappa-type opioid receptor
CHEMBL3952
Ki 7.42 7.42 38.0 1
Delta-type opioid receptor
CHEMBL236
Ki 7.4 7.4 40.0 1
Delta-type opioid receptor
CHEMBL269
Ki 7.4 7.4 39.8 1
Mu-type opioid receptor
CHEMBL233
Ki 6.85 6.85 140.0 1
Mu-type opioid receptor
CHEMBL270
Ki 6.85 6.85 141.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11597422 10.1016/s0960-894x(01)00580-7 Mu-type opioid receptor 1
11597422 10.1016/s0960-894x(01)00580-7 Delta-type opioid receptor 1
11597422 10.1016/s0960-894x(01)00580-7 Kappa-type opioid receptor 1
11597422 10.1016/s0960-894x(01)00580-7 Opioid receptors; mu & delta 1
11597422 10.1016/s0960-894x(01)00580-7 Opioid receptors; delta & kappa 1
15743203 10.1021/jm049117e Delta-type opioid receptor 1
15743203 10.1021/jm049117e Mu-type opioid receptor 1
15743203 10.1021/jm049117e Kappa-type opioid receptor 1

Data from ChEMBL 36 via Core Engine