GMS6504
Lecture
/
Exam
/ /
2 Questions With Correct Answers
/ / / /
MODULE /4 /Drug /Targets /- /correct /answer(s) /✔✔ /
What
/are
/the /
4
/things
/that
/make
/something /
a /good /drug? /- /correct /answer(s) /✔✔ /1. /Lipinski's /Rule /of /5 /
2. /Chemical /reactivity: /good /or /bad? /
3.
/Some
/chemically /or /biologically /reactive /functional /groups /to /recognize /
4. /Choosing /a /target
What
/is
/Lipinski's
/Rule
/of /5? /- /correct /answer(s) /✔✔ /1.Molecular /mass /greater /than /500 /Da /
2.High /lipophilicity /(expressed /as /LogP /greater /than /5) /
3.More /than /5 /hydrogen /bond /donors /
,4.More /than /10 /hydrogen /bond /acceptors
Partition
/Coefficient /Definition /- /correct /answer(s) /✔✔ /P /= /Coct/Cwater
How
/big
/are
/the
/differences
/in
/the
/partition
/coefficient? /- /correct /answer(s) /✔✔ /very /large /scale, /Log10(P)
What
/are
/the
/Improvements
/on
/the
/Lipinski /Parameters /(5) /- /correct /answer(s) /✔✔ /1. /Partition /coefficient
/log /P /in /-0.4 /to /+5.6 /range /
2. /Molar /refractivity /from /40 /to /130 /
3. /Molecular /weight /from /160 /to /500 /
4. /Number /of /atoms /from /20 /to /70 /(includes /H-
bond /donors /[e.g.;OHs /and /NHs] /and /H-
bond /acceptors /[e.g.; /Ns /and /Os]) /
5. /Polar /surface /area /no /greater /than /140 /Å2
What
/are /
2
/things
, /that
/make
/chemical
/reactivity /
a
/good
/thing? /-
/correct
/answer(s)
/✔✔
/1.Modification
/of /Proteins /and/or /Nucleic /Acids /(Bad /if /unanticipated /and /non-
selective, /but /can /be /good /if /selective) /
2. /Labile /in /Biological /Systems /*Esters /*Amide /Bonds /*Disulfide /Bonds
What
/are
/some
/chemically
/reactive
/functional
/groups? /-
/correct
/answer(s) /✔✔ /Sulfonyl /Halides /- /most /halides /(R /and /X /groups)
Aldehydes
Ketones
Epoxides /- /carcinogens
What
/is
/the
/name
/of
/the
Lecture
/
Exam
/ /
2 Questions With Correct Answers
/ / / /
MODULE /4 /Drug /Targets /- /correct /answer(s) /✔✔ /
What
/are
/the /
4
/things
/that
/make
/something /
a /good /drug? /- /correct /answer(s) /✔✔ /1. /Lipinski's /Rule /of /5 /
2. /Chemical /reactivity: /good /or /bad? /
3.
/Some
/chemically /or /biologically /reactive /functional /groups /to /recognize /
4. /Choosing /a /target
What
/is
/Lipinski's
/Rule
/of /5? /- /correct /answer(s) /✔✔ /1.Molecular /mass /greater /than /500 /Da /
2.High /lipophilicity /(expressed /as /LogP /greater /than /5) /
3.More /than /5 /hydrogen /bond /donors /
,4.More /than /10 /hydrogen /bond /acceptors
Partition
/Coefficient /Definition /- /correct /answer(s) /✔✔ /P /= /Coct/Cwater
How
/big
/are
/the
/differences
/in
/the
/partition
/coefficient? /- /correct /answer(s) /✔✔ /very /large /scale, /Log10(P)
What
/are
/the
/Improvements
/on
/the
/Lipinski /Parameters /(5) /- /correct /answer(s) /✔✔ /1. /Partition /coefficient
/log /P /in /-0.4 /to /+5.6 /range /
2. /Molar /refractivity /from /40 /to /130 /
3. /Molecular /weight /from /160 /to /500 /
4. /Number /of /atoms /from /20 /to /70 /(includes /H-
bond /donors /[e.g.;OHs /and /NHs] /and /H-
bond /acceptors /[e.g.; /Ns /and /Os]) /
5. /Polar /surface /area /no /greater /than /140 /Å2
What
/are /
2
/things
, /that
/make
/chemical
/reactivity /
a
/good
/thing? /-
/correct
/answer(s)
/✔✔
/1.Modification
/of /Proteins /and/or /Nucleic /Acids /(Bad /if /unanticipated /and /non-
selective, /but /can /be /good /if /selective) /
2. /Labile /in /Biological /Systems /*Esters /*Amide /Bonds /*Disulfide /Bonds
What
/are
/some
/chemically
/reactive
/functional
/groups? /-
/correct
/answer(s) /✔✔ /Sulfonyl /Halides /- /most /halides /(R /and /X /groups)
Aldehydes
Ketones
Epoxides /- /carcinogens
What
/is
/the
/name
/of
/the
