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Compound Detail

CHEMBL75030

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c1ccc2c(c1)CCCC2NC1=NCCO1

Basic Information

ChEMBL ID CHEMBL75030
Phase Preclinical
Structure Type MOL
InChI Key FXNNPMSELIMMHU-UHFFFAOYSA-N
4
Targets
9
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

216.3
MW (Da)
2.04
ALogP
3
HBA
1
HBD
33.6
PSA (Ų)
0.78
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H16N2O
MW 216.28
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -0.44

Activity Summary

Ki 6 meas. best 8.67
EC50 3 meas. best 8.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2A adrenergic receptor
CHEMBL1867
EC50 8.93 8.93 1.2 1
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 8.67 8.67 2.1 1
Alpha-2C adrenergic receptor
CHEMBL1916
EC50 8.66 8.66 2.2 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 8.63 8.63 2.3 1
Alpha-2B adrenergic receptor
CHEMBL1942
EC50 8.45 8.45 3.5 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 7.92 7.92 12.0 1
Alpha-1A adrenergic receptor
CHEMBL229
Ki 6.9 6.795 125.9 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(94)85032-1 Alpha-2A adrenergic receptor 2
- 10.1016/0960-894X(94)85032-1 Alpha-2B adrenergic receptor 2
- 10.1016/0960-894X(94)85032-1 Alpha-2C adrenergic receptor 2
- 10.1016/0960-894X(94)85032-1 Alpha-1A adrenergic receptor 2
- 10.1016/0960-894X(94)85032-1 Alpha-1B adrenergic receptor 1

Data from ChEMBL 36 via Core Engine