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Compound Detail

CHEMBL492648

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COC1(C2=NCCN2)COc2cccc(-c3ccccc3)c2O1

Basic Information

ChEMBL ID CHEMBL492648
Phase Preclinical
Structure Type MOL
InChI Key TVDZYHOTHAFPBR-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

310.4
MW (Da)
2.47
ALogP
5
HBA
1
HBD
52.1
PSA (Ų)
0.95
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 C18H18N2O3
MW 310.35
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness 0.52

Activity Summary

Ki 3 meas. best 6.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 6.9 6.9 125.9 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 6.61 6.61 245.5 1
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 5.97 5.97 1071.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18578476 10.1021/jm800250z Alpha-2A adrenergic receptor 2
18578476 10.1021/jm800250z Alpha-2B adrenergic receptor 2
18578476 10.1021/jm800250z Alpha-2C adrenergic receptor 2

Data from ChEMBL 36 via Core Engine