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Compound Detail

CHEMBL146556

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c1ccc2c(c1)CC(CN1CCN(c3ccc4c(c3)OCCO4)CC1)C2

Basic Information

ChEMBL ID CHEMBL146556
Phase Preclinical
Structure Type MOL
InChI Key CYPJMEGEBKHODC-UHFFFAOYSA-N
8
Targets
8
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

350.5
MW (Da)
2.99
ALogP
4
HBA
0
HBD
24.9
PSA (Ų)
0.85
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 C22H26N2O2
MW 350.46
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.02

Activity Summary

Ki 8 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 8.8 8.8 1.6 1
Unchecked
CHEMBL612545
Ki 8.62 8.62 2.4 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 6.6 6.6 249.0 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 6.47 6.47 336.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.27 6.27 540.0 1
D(2) dopamine receptor
CHEMBL217
Ki 6.13 6.13 738.0 1
Adrenergic receptor alpha-1
CHEMBL2094251
Ki 6.01 6.01 967.0 1
D(3) dopamine receptor
CHEMBL234
Ki 5.55 5.55 2840.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11170639 10.1021/jm0002432 Rodentia sp. 6
28489950 10.1021/acs.jmedchem.7b00151 Unchecked 1
28489950 10.1021/acs.jmedchem.7b00151 D(1A) dopamine receptor 1
28489950 10.1021/acs.jmedchem.7b00151 D(2) dopamine receptor 1
28489950 10.1021/acs.jmedchem.7b00151 D(3) dopamine receptor 1
28489950 10.1021/acs.jmedchem.7b00151 D(1B) dopamine receptor 1
28489950 10.1021/acs.jmedchem.7b00151 5-hydroxytryptamine receptor 1A 1
28489950 10.1021/acs.jmedchem.7b00151 Alpha-2A adrenergic receptor 1
28489950 10.1021/acs.jmedchem.7b00151 Alpha-2C adrenergic receptor 1
28489950 10.1021/acs.jmedchem.7b00151 Sigma non-opioid intracellular receptor 1 1
28489950 10.1021/acs.jmedchem.7b00151 Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine