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Compound Detail

CHEMBL334970

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O=C(O)C[C@@H](NC(=O)c1cccc2c3c([nH]c12)[C@@H]1Oc2c(O)ccc4c2C12CCN(CC1CC1)C(C4)[C@]2(O)C3)C(=O)O

Basic Information

ChEMBL ID CHEMBL334970
Phase Preclinical
Structure Type MOL
InChI Key OPMKMCOJTGUVGA-IRECNROUSA-N
3
Targets
4
Activities
1
Assay Types
1
PK Parameters
7
Publications
0
Known Names

Molecular Properties

573.6
MW (Da)
2.23
ALogP
7
HBA
6
HBD
172.4
PSA (Ų)
0.25
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H31N3O8
MW 573.60
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness 0.86

Activity Summary

Ki 4 meas. best 9.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
Ki 9.85 9.62 0.1 2
Mu-type opioid receptor
CHEMBL4354
Ki 6.43 6.43 368.0 1
Kappa-type opioid receptor
CHEMBL3952
Ki 6.05 6.05 893.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ke 1.1 nM -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7853332 10.1021/jm00003a002 Delta-type opioid receptor 7
7853332 10.1021/jm00003a002 Mu-type opioid receptor 3
7853332 10.1021/jm00003a002 Kappa-type opioid receptor 3
7853332 10.1021/jm00003a002 Opioid receptors; mu & delta 2
7853332 10.1021/jm00003a002 Opioid receptors; delta & kappa 2
7853332 10.1021/jm00003a002 Mus musculus 2
7853332 10.1021/jm00003a002 Unchecked 1

Data from ChEMBL 36 via Core Engine