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Compound Detail

CHEMBL50017

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CN1CCN(c2ncccc2Br)CC1

Basic Information

ChEMBL ID CHEMBL50017
Phase Preclinical
Structure Type MOL
InChI Key UQIOJCBARSSJKK-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

256.1
MW (Da)
1.60
ALogP
3
HBA
0
HBD
19.4
PSA (Ų)
0.76
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 C10H14BrN3
MW 256.15
Aromatic Rings 1
Heavy Atoms 14
NP-Likeness -1.42

Activity Summary

Kd 2 meas. best 7.6
Ki 2 meas. best 8.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2A adrenergic receptor
CHEMBL4744
Ki 8.54 8.54 2.9 1
Adrenergic receptor alpha-2
CHEMBL2093864
Kd 7.6 7.6 25.1 1
Alpha-1A adrenergic receptor
CHEMBL4892
Ki 6.8 6.8 160.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Kd 6.5 6.5 316.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
6139479 10.1021/jm00366a007 Adrenergic receptor alpha-2 2
6139479 10.1021/jm00366a007 Alpha-2A adrenergic receptor 1
6139479 10.1021/jm00366a007 Alpha-1A adrenergic receptor 1
6139479 10.1021/jm00366a007 Adrenergic receptor alpha-1 1
6139479 10.1021/jm00366a007 Cerebral cortex alpha adrenergic receptor 1
6139479 10.1021/jm00366a007 Adrenergic receptor alpha 1

Data from ChEMBL 36 via Core Engine