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Compound Detail

CHEMBL1084011

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O=c1c(Br)cc(Br)c2n1C[C@@H]1CNC[C@H]2C1

Basic Information

ChEMBL ID CHEMBL1084011
Phase Preclinical
Structure Type MOL
InChI Key UIRFWXCFBPYLDL-NKWVEPMBSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

348.0
MW (Da)
2.08
ALogP
3
HBA
1
HBD
34.0
PSA (Ų)
0.78
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 C11H12Br2N2O
MW 348.04
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness 0.03

Activity Summary

IC50 1 meas. best 6.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor; alpha4/beta2
CHEMBL1907596
IC50 6.43 6.43 371.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuronal acetylcholine receptor; alpha4/beta2 IC50 = 371.54 nM 6.43 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