Advancing the activity cliff concept

Advancing the activity cliff concept

The activity cliff concept has experienced increasing interest in medicinal chemistry and chemoinformatics. Activity cliffs have originally been defined as pairs of structurally similar compounds that are active against the same target but have a large difference in potency. Activity cliffs are relevant for structure-activity relationship (SAR) analysis and compound optimization because small c...

Follow up: Advancing the activity cliff concept, part II

We present a follow up contribution to further complement a previous commentary on the activity cliff concept and recent advances in activity cliff research. Activity cliffs have originally been defined as pairs of structurally similar compounds that display a large difference in potency against a given target. For medicinal chemistry, activity cliffs are of high interest because structure-acti...

Role the TICE?: advancing the concept of transintestinal cholesterol excretion.

Cliff hangers

The peregrine falcon holds a special place in the minds of environmentalists and conservation biologists. The crash in its population throughout the 1950s and 60s was linked to the rapidly increasing use of agricultural organochlorine pesticides which led to a thinning of the birds’ eggshells and dramatic breeding failure. Since the widespread ban on the use of these chemicals, populations have...

Cliff hanger

The asparagus season has recently ended for northern hemisphere crops. Tradition has it that, at the summer solstice, growers stop cutting spears to allow the plant to grow and produce enough resources to generate spears for the next spring’s crop. The plant is becoming increasingly fashionable and production is increasing to meet demand. But the cultivated asparagus has a wild relative that is...