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Compound Detail

CHEMBL3038190

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CO[C@]12C=C[C@@]3(C[C@@H]1NC(=O)CBr)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5

Basic Information

ChEMBL ID CHEMBL3038190
Phase Preclinical
Structure Type MOL
InChI Key UUROJLGOMFSTOA-DAQJRISHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

501.4
MW (Da)
2.66
ALogP
5
HBA
2
HBD
71.0
PSA (Ų)
0.48
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29BrN2O4
MW 501.42
Aromatic Rings 1
Heavy Atoms 32
NP-Likeness 1.22

Activity Summary

EC50 1 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Opioid receptor
CHEMBL2094129
EC50 8.15 8.15 7.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Opioid receptor EC50 = 7.0 nM 8.15 Displacement of [3H]dalamid ([D-Ala2,Met5] enkephalinamide) from opioid receptor... 3023609

Literature References

PubMed DOI Target Context # Activities
3023609 10.1021/jm00161a002 Mus musculus 3
3023609 10.1021/jm00161a002 Opioid receptor 1
3023609 10.1021/jm00161a002 Kappa-type opioid receptor 1

Data from ChEMBL 36 via Core Engine