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Compound Detail

CHEMBL2310919

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C=CCN1CC[C@]23c4c5ccc(O)c4O[C@H]2C2(OC)C=C[C@@]3(C[C@@H]2N=S)[C@H]1C5.O=C(O)C(=O)O

Basic Information

ChEMBL ID CHEMBL2310919
Phase Preclinical
Structure Type MOL
InChI Key JIBAJFBVXOHFNE-ISQFUXSMSA-N
Parent Compound CHEMBL2365486
Active Moiety CHEMBL2365486
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

396.5
MW (Da)
2.65
ALogP
6
HBA
1
HBD
54.3
PSA (Ų)
0.79
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H26N2O7S
MW 486.55
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness 1.71

Activity Summary

EC50 1 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Opioid receptor
CHEMBL2094129
EC50 7.0 7.0 100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Opioid receptor EC50 = 100.0 nM 7.0 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