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Compound Detail

CHEMBL2205824

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COc1cccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)c1

Basic Information

ChEMBL ID CHEMBL2205824
Phase Preclinical
Structure Type MOL
InChI Key LIKZWSUAMNZHAE-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

295.4
MW (Da)
1.96
ALogP
3
HBA
1
HBD
32.7
PSA (Ų)
0.93
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 C19H21NO2
MW 295.38
Aromatic Rings 1
Heavy Atoms 22
NP-Likeness 0.44

Activity Summary

Ki 5 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 7.57 7.57 26.8 1
Sigma non-opioid intracellular receptor 1
CHEMBL3602
Ki 6.49 6.49 327.0 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 5.86 5.86 1369.0 1
Mu-type opioid receptor
CHEMBL233
Ki 5.63 5.63 2330.0 1
Histamine H2 receptor
CHEMBL1941
Ki 5.01 5.01 9794.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22959245 10.1016/j.bmcl.2012.08.046 Unchecked 2
22959245 10.1016/j.bmcl.2012.08.046 Muscarinic acetylcholine receptor M3 1
22959245 10.1016/j.bmcl.2012.08.046 Sigma non-opioid intracellular receptor 1 1
22959245 10.1016/j.bmcl.2012.08.046 5-hydroxytryptamine receptor 2C 1
22959245 10.1016/j.bmcl.2012.08.046 5-hydroxytryptamine receptor 3A 1
22959245 10.1016/j.bmcl.2012.08.046 5-hydroxytryptamine receptor 5A 1
22959245 10.1016/j.bmcl.2012.08.046 5-hydroxytryptamine receptor 6 1
22959245 10.1016/j.bmcl.2012.08.046 5-hydroxytryptamine receptor 7 1
22959245 10.1016/j.bmcl.2012.08.046 Sodium-dependent serotonin transporter 1
22959245 10.1016/j.bmcl.2012.08.046 Muscarinic acetylcholine receptor M1 1
22959245 10.1016/j.bmcl.2012.08.046 Muscarinic acetylcholine receptor M2 1
22959245 10.1016/j.bmcl.2012.08.046 D(3) dopamine receptor 1
22959245 10.1016/j.bmcl.2012.08.046 Muscarinic acetylcholine receptor M4 1
22959245 10.1016/j.bmcl.2012.08.046 Muscarinic acetylcholine receptor M5 1
22959245 10.1016/j.bmcl.2012.08.046 Delta-type opioid receptor 1
22959245 10.1016/j.bmcl.2012.08.046 Kappa-type opioid receptor 1
22959245 10.1016/j.bmcl.2012.08.046 Alpha-1A adrenergic receptor 1
22959245 10.1016/j.bmcl.2012.08.046 Alpha-2C adrenergic receptor 1
22959245 10.1016/j.bmcl.2012.08.046 Histamine H2 receptor 1
22959245 10.1016/j.bmcl.2012.08.046 Sodium-dependent noradrenaline transporter 1

Data from ChEMBL 36 via Core Engine