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Compound Detail

CHEMBL397306

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Cc1cccc[n+]1CCCC#Cc1cc(C#CCCC[n+]2ccccc2C)cc(C#CCCC[n+]2ccccc2C)c1.[Br-].[Br-].[Br-]

Basic Information

ChEMBL ID CHEMBL397306
Phase Preclinical
Structure Type MOL
InChI Key WKGQXDBJMCFBLN-UHFFFAOYSA-K
Parent Compound CHEMBL1185197
Active Moiety CHEMBL1185197
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

552.8
MW (Da)
5.97
ALogP
0
HBA
0
HBD
11.6
PSA (Ų)
0.14
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H42Br3N3
MW 792.50
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -0.10

Activity Summary

IC50 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.4 8.4 4.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 4.0 nM 8.4 Antagonist activity at nAChR in rat striatal slices assessed as inhibition of ni... 17977723

Literature References

PubMed DOI Target Context # Activities
17977723 10.1016/j.bmcl.2007.10.062 Unchecked 3
17977723 10.1016/j.bmcl.2007.10.062 Neuronal acetylcholine receptor; alpha4/beta2 1
17977723 10.1016/j.bmcl.2007.10.062 Neuronal acetylcholine receptor subunit alpha-7 1

Data from ChEMBL 36 via Core Engine