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Compound Detail

CHEMBL4215892

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CN1CC2OCCN(C(=O)Cc3ccc(Cl)c(Cl)c3)C2C(N2CCCC2)C1

Basic Information

ChEMBL ID CHEMBL4215892
Phase Preclinical
Structure Type MOL
InChI Key DCWGNIFKBNPDLA-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

412.4
MW (Da)
2.54
ALogP
4
HBA
0
HBD
36.0
PSA (Ų)
0.76
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H27Cl2N3O2
MW 412.36
Aromatic Rings 1
Heavy Atoms 27
NP-Likeness -0.63

Activity Summary

Ki 1 meas. best 6.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL3952
Ki 6.54 6.54 286.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Kappa-type opioid receptor Ki = 286.0 nM 6.54 Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig brain memb... -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C6MD00441E Delta-type opioid receptor 1
- 10.1039/C6MD00441E Mu-type opioid receptor 1
- 10.1039/C6MD00441E Kappa-type opioid receptor 1
- 10.1039/C6MD00441E Sigma non-opioid intracellular receptor 1 1
- 10.1039/C6MD00441E Sigma intracellular receptor 2 1

Data from ChEMBL 36 via Core Engine