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Compound Detail

CHEMBL562280

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CCN(CC)C(=O)c1ncc(C2=CC3(CCNCC3)Oc3ccccc32)cn1

Basic Information

ChEMBL ID CHEMBL562280
Phase Preclinical
Structure Type MOL
InChI Key XJMZTKMOFXBEGY-UHFFFAOYSA-N
2
Targets
3
Activities
3
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

378.5
MW (Da)
2.90
ALogP
5
HBA
1
HBD
67.3
PSA (Ų)
0.89
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 C22H26N4O2
MW 378.48
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.22

Activity Summary

EC50 1 meas. best 7.04
IC50 1 meas. best 4.68
Ki 1 meas. best 8.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
Ki 8.34 8.34 4.6 1
Delta-type opioid receptor
CHEMBL236
EC50 7.04 7.04 92.0 1
Cytochrome P450 2D6
CHEMBL289
IC50 4.68 4.68 21000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19694468 10.1021/jm900773n Delta-type opioid receptor 2
19694468 10.1021/jm900773n Voltage-gated inwardly rectifying potassium channel KCNH2 1
19694468 10.1021/jm900773n Cytochrome P450 2D6 1
19694468 10.1021/jm900773n Mu-type opioid receptor 1
19694468 10.1021/jm900773n Kappa-type opioid receptor 1

Data from ChEMBL 36 via Core Engine