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Compound Detail

CHEMBL564825

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O=C(c1ccccc1)c1cc(OC(=O)N2CCN3CCC2CC3)ccc1Br

Basic Information

ChEMBL ID CHEMBL564825
Phase Preclinical
Structure Type MOL
InChI Key VVRPKFMCZNMWRF-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

429.3
MW (Da)
3.96
ALogP
4
HBA
0
HBD
49.9
PSA (Ų)
0.69
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 C21H21BrN2O3
MW 429.31
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.59

Activity Summary

IC50 2 meas. best 5.86
Ki 1 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL4980
Ki 7.8 7.8 16.0 1
Neuronal acetylcholine receptor subunit alpha-3
CHEMBL3068
IC50 5.86 5.86 1390.0 1
Neuronal acetylcholine receptor; alpha4/beta2
CHEMBL1907596
IC50 5.69 5.69 2040.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19576766 10.1016/j.bmcl.2009.06.059 Neuronal acetylcholine receptor subunit alpha-7 2
19576766 10.1016/j.bmcl.2009.06.059 Neuronal acetylcholine receptor; alpha4/beta2 1
19576766 10.1016/j.bmcl.2009.06.059 Neuronal acetylcholine receptor subunit alpha-3 1
19576766 10.1016/j.bmcl.2009.06.059 Unchecked 1

Data from ChEMBL 36 via Core Engine