Thermo In Context

Question 1

in medicinal chemistry, how do we describe drug-ligand interactions?

Answer 1

dissociation constant.

Kd = 1/ Ka

Question 2

what will effective drugs have?

Answer 2

large negative values of delta G

high values for Ka

small values for Kd

Question 3

what is another useful measure of inhibitor potency?

Answer 3

IC50

inhibitor concentrations that reduce enzymatic activity to 50% in presence of substrate

Question 4

for enzyme inhibitors, what do we often use?

Answer 4

inhibition constant Ki

directly analogous to Kd

Question 5

hydrogen bonding is often …. in drug binding

Answer 5

thermoneutral

Question 6

change in solvent accessible surface area is a key determinant in what?

Answer 6

hydrophobic strength

Question 7

give examples of common non-covalent interactions?

Answer 7

• salt bridging
• hydrogen bonding
• van der Waals
• aromatic stacking
• hydrophobic effect

Question 8

at a pH of 7, what does an amine become?

Answer 8

ionised

Question 9

what is the distance between aromatic rings in a dna helix?

Answer 9

3.5 A

Question 10

describe the electronegative of sp and sp3 in pi stacking?

Answer 10

sp carbons more electronegative than sp3

Question 11

what is water with 4 HB?

Answer 11

ice