HIT to lead activities 1
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13 Terms
what can happen if a drug is too lipophilic?
it will deposit into the fatty tissues/membrane and not partition out. also highly liphophillic drugs can have more off target side effects as binding is unselective
why is it important to test microsomal stability?
the liver will try to detoxify drugs to excrete them so this will reduce the concentration, so this assay measures compound clearance
what is Caco-2 permability
it is a model of membrane made up of epithelial mono layer, used to tested drug absorption in the gut
what is the target value for aqueous soluability?
below 100 micro molar
what is the target value for liphophilicy?
0-3
what is the target value for microsomal stability?
greater than 30 ul/min-1/mg-1
what is the target value for CYP450 inhibtion?
less than 10uM
what is the target value for Caco-2 permeability?
less than 1×10^-6cm-1
what is the target value for the MDR1MDCK permeability?
less than 10×10^-6
what can the MDR1MDCK permeability model be used to predict?
intestinal and brain permeability
what is the target value for hep g2 hepatotoxicity?
no effect at 50 times the concentration of IC50
what is the target value for cytotoxicity?
no effect at 50 times the concentration of IC50
when would you use template hopping and how does it work?
this can be used when an identified HIT compound has been patented by another company. the aim would be to keep pharmacophore but made changes to the structure that occupies a unique intellectual property (IP) space.