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Compound Detail

CHEMBL287935

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COc1cccc(OC)c1OCCNC[C@H]1Oc2ccccc2O[C@@H]1c1ccccc1

Basic Information

ChEMBL ID CHEMBL287935
Phase Preclinical
Structure Type MOL
InChI Key UVEKKXRFQCNLQE-DNQXCXABSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

421.5
MW (Da)
4.25
ALogP
6
HBA
1
HBD
58.2
PSA (Ų)
0.52
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27NO5
MW 421.49
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness 0.40

Activity Summary

Kd 4 meas. best 8.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Kd 8.59 8.49 2.6 2
Adrenergic receptor alpha-2
CHEMBL2093864
Kd 4.22 4.2 60256.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8098772 10.1021/jm00063a002 Adrenergic receptor alpha-1 1
8098772 10.1021/jm00063a002 Adrenergic receptor alpha-2 1
8098772 10.1021/jm00063a002 Adrenergic receptor alpha 1
1977906 10.1021/jm00173a004 Adrenergic receptor alpha-1 1
1977906 10.1021/jm00173a004 Adrenergic receptor alpha-2 1
1977906 10.1021/jm00173a004 Unchecked 1
10425105 10.1021/jm9910324 Alpha-1A adrenergic receptor 1
10425105 10.1021/jm9910324 Alpha-1B adrenergic receptor 1
10425105 10.1021/jm9910324 Alpha-1D adrenergic receptor 1

Data from ChEMBL 36 via Core Engine