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Compound Detail

CHEMBL218732

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COc1ccc2ccccc2c1OCCNC[C@@H]1COc2cc3c(cc2O1)CCCC3.Cl

Basic Information

ChEMBL ID CHEMBL218732
Phase Preclinical
Structure Type MOL
InChI Key BXAUNYRCMJYSAD-ZMBIFBSDSA-N
Parent Compound CHEMBL1182196
Active Moiety CHEMBL1182196
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

419.5
MW (Da)
4.54
ALogP
5
HBA
1
HBD
49.0
PSA (Ų)
0.57
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 C26H30ClNO4
MW 455.98
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.02

Activity Summary

Ki 4 meas. best 6.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 6.49 6.49 323.6 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 6.26 6.26 549.5 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 6.02 6.02 955.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 5.44 5.44 3630.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17125266 10.1021/jm060358r Alpha-1A adrenergic receptor 1
17125266 10.1021/jm060358r Alpha-1B adrenergic receptor 1
17125266 10.1021/jm060358r Alpha-1D adrenergic receptor 1
17125266 10.1021/jm060358r 5-hydroxytryptamine receptor 1A 1
17125266 10.1021/jm060358r Alpha adrenergic receptor (1a and 1d) 1
17125266 10.1021/jm060358r Adrenergic receptors; alpha-1 A & B 1
17125266 10.1021/jm060358r Unchecked 1

Data from ChEMBL 36 via Core Engine