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Compound Detail

CHEMBL181941

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CN(C(=O)CNC(=O)c1ccc(Cl)c(Cl)c1)[C@H](CN1CC[C@@H](O)C1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL181941
Phase Preclinical
Structure Type MOL
InChI Key HWEZMDZRYSNGGK-YLJYHZDGSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

450.4
MW (Da)
2.99
ALogP
4
HBA
2
HBD
72.9
PSA (Ų)
0.68
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25Cl2N3O3
MW 450.37
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.27

Activity Summary

EC50 1 meas. best 9.12
Ki 1 meas. best 9.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL237
EC50 9.12 9.12 0.8 1
Kappa-type opioid receptor
CHEMBL237
Ki 9.08 9.08 0.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15713370 10.1016/j.bmcl.2005.01.038 Kappa-type opioid receptor 2
15713370 10.1016/j.bmcl.2005.01.038 Opioid receptors; mu & kappa 2

Data from ChEMBL 36 via Core Engine