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Compound Detail

CHEMBL5426766

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Cl.O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2cc(Br)[nH]c12

Basic Information

ChEMBL ID CHEMBL5426766
Phase Preclinical
Structure Type MOL
InChI Key FNXKUVSFZIJUJO-MARJHAEGSA-N
Parent Compound CHEMBL5499905
Active Moiety CHEMBL5499905
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

564.5
MW (Da)
4.00
ALogP
5
HBA
4
HBD
97.8
PSA (Ų)
0.38
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H31BrClN3O4
MW 600.94
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness 0.80

Activity Summary

Ki 3 meas. best 9.32
EC50 1 meas. best 6.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL2858
Ki 9.32 9.32 0.5 1
Kappa-type opioid receptor
CHEMBL4329
Ki 8.82 8.82 1.5 1
Delta-type opioid receptor
CHEMBL236
Ki 8.17 8.17 6.7 1
Mu-type opioid receptor
CHEMBL2858
EC50 6.63 6.63 236.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36538027 10.1021/acs.jmedchem.2c01499 Mu-type opioid receptor 3
36538027 10.1021/acs.jmedchem.2c01499 Unchecked 2
36538027 10.1021/acs.jmedchem.2c01499 Kappa-type opioid receptor 1
36538027 10.1021/acs.jmedchem.2c01499 Delta-type opioid receptor 1
36538027 10.1021/acs.jmedchem.2c01499 Mus musculus 1

Data from ChEMBL 36 via Core Engine