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Quinoline Discovery Library

160 compounds, 2 plates

The BioQuadrant quinoline discovery library currently consists of 160 substituted quinoline compounds (including KM11060), divided over two 96 polypropylene deep-well plates. Each plate can be purchased individually. Each molecule has been deposited in 1 micromole quantity per well. Adding 100 microliter of DMSO will yield a 10mM solution. Columns 1 and 12 have been left empty.

The following quinoline sub-sets are available:

Plate# BQQA     Click here to view structures. A 96-well plate of 80 compounds consisting predominantly of six different quinoline-4-carboxylic acids onto which an aryl-, alkyl- or acyl-piperazine has been attached.

Plate# BQQB     Click here to view structures. A 96-well plate with 80 compounds consisting of eleven different substituted quinolines onto which a piperazine moiety is attached. The piperazine moiety itself is further functionalized with several different sulfonyl groups.

The piperazine moiety is attached either directly onto the quinoline template, or indirectly through a carbonyl moiety.

Pharmacology of Quinolines

The Quinoline motif occurs in several approved and investigational drugs. Some examples of biologically active piperazinyl quinolines similar to those found in the BioQuadrant Quinoline Discovery Library:

Reported bioactivities (source: PubChem database) of Quinolines include -but are not limited to- the following:

• Inhibition of lung tumor cell growth
• Inhibition of transient receptor potential cation C channel C6
• Inhibition of Shiga Toxin
• Activiation of human intestinal alkaline phosphatase
• Inhibition of IMP-1 metallo-beta-lactamase
• Inhibition of respiratory syncytial virus (RSV)
• Inhibition of KLF5
• Inhibition of Alzheimer's amyloid precursor protein translation
• Modulation of D1 receptors