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Compound Detail

CHEMBL1083905

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CN1C[C@@H]2C[C@H](C1)c1ccc(Br)c(=O)n1C2

Basic Information

ChEMBL ID CHEMBL1083905
Phase Preclinical
Structure Type MOL
InChI Key ZUXXFRXUPFGGPW-DTWKUNHWSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

283.2
MW (Da)
1.66
ALogP
3
HBA
0
HBD
25.2
PSA (Ų)
0.72
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H15BrN2O
MW 283.17
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -0.25

Activity Summary

IC50 1 meas. best 6.99

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor; alpha4/beta2
CHEMBL1907596
IC50 6.99 6.99 102.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuronal acetylcholine receptor; alpha4/beta2 IC50 = 102.33 nM 6.99 Displacement of [3H]epibatidine from rat alpha4beta2 nAChR 20493692

Literature References

PubMed DOI Target Context # Activities
20493692 10.1016/j.bmcl.2010.04.092 Neuronal acetylcholine receptor; alpha4/beta2 1

Data from ChEMBL 36 via Core Engine