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Compound Detail

CHEMBL434111

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CN(CC(=O)NC12CC3CC(CC(C3)C1)C2)C(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC[S+](C)[O-])NC(=O)[C@@H](N)Cc1ccc(O)cc1

Basic Information

ChEMBL ID CHEMBL434111
Phase Preclinical
Structure Type MOL
InChI Key KGWSFJNQXKRONL-JLCMKISKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

679.9
MW (Da)
1.79
ALogP
7
HBA
5
HBD
176.9
PSA (Ų)
0.18
QED
1
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H49N5O6S
MW 679.88
Aromatic Rings 2
Heavy Atoms 48
NP-Likeness -0.30

Activity Summary

IC50 1 meas. best 7.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Opioid receptors; mu/kappa/delta
CHEMBL2095181
IC50 7.59 7.59 25.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Opioid receptors; mu/kappa/delta IC50 = 25.5 nM 7.59 In vitro opioid inhibitory activity against in guinea pig ileum 2872334

Literature References

PubMed DOI Target Context # Activities
2872334 10.1021/jm00156a003 Mus musculus 4
2872334 10.1021/jm00156a003 Opioid receptors; mu/kappa/delta 3

Data from ChEMBL 36 via Core Engine