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Compound Detail

CHEMBL2111530

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COc1ccc2c3c([nH]c2c1)C[C@@H]1C[C@@]3(c2cccc(O)c2)CCN1C

Basic Information

ChEMBL ID CHEMBL2111530
Phase Preclinical
Structure Type MOL
InChI Key OLISSJIVMPYVMP-IVZQSRNASA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

348.4
MW (Da)
3.82
ALogP
3
HBA
2
HBD
48.5
PSA (Ų)
0.74
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24N2O2
MW 348.45
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness 0.49

Activity Summary

IC50 4 meas. best 8.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL269
IC50 8.43 8.43 3.7 1
Delta-type opioid receptor
CHEMBL3222
IC50 7.31 7.31 49.0 1
Mu-type opioid receptor
CHEMBL270
IC50 7.18 7.18 66.4 1
Kappa-type opioid receptor
CHEMBL3952
IC50 5.93 5.93 1162.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8642567 10.1021/jm950695s Mu-type opioid receptor 2
8642567 10.1021/jm950695s Delta-type opioid receptor 2
8642567 10.1021/jm950695s Unchecked 2
8642567 10.1021/jm950695s Kappa-type opioid receptor 1
8642567 10.1021/jm950695s Opioid receptors; mu & delta 1

Data from ChEMBL 36 via Core Engine