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Compound Detail

CHEMBL303418

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NC(=O)[C@@H]1CC(=O)NCCC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N1

Basic Information

ChEMBL ID CHEMBL303418
Phase Preclinical
Structure Type BOTH
InChI Key YHLQBUMFTKANHO-LRSLUSHPSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

583.6
MW (Da)
-1.35
ALogP
9
HBA
7
HBD
248.9
PSA (Ų)
0.14
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H33N7O8
MW 583.60
Aromatic Rings 2
Heavy Atoms 42
NP-Likeness 0.30

Activity Summary

Ki 2 meas. best 6.56
IC50 1 meas. best 5.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL270
Ki 6.56 6.56 273.0 1
Mu-type opioid receptor
CHEMBL4354
IC50 5.63 5.63 2340.0 1
Delta-type opioid receptor
CHEMBL269
Ki 5.3 5.3 5060.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2822930 10.1021/jm00394a027 Mu-type opioid receptor 4
2822930 10.1021/jm00394a027 Delta-type opioid receptor 4
2822930 10.1021/jm00394a027 Opioid receptors; mu & delta 1
2822930 10.1021/jm00394a027 Unchecked 1

Data from ChEMBL 36 via Core Engine