Compound 1 Kd = 20 nM Compound 2 K= 35 mM O There is an important hydrophobic interaction at the binding region. O There is not much space at the binding region, so removing the aromatic ring increases affinity. The removed aromatic ring is not part of the pharmacophore. The removed aromatic ring was getting metabolized and subsequently easily eliminated. O Changing the methoxy group for an electron withdrawing group will result in decrease of affinity

Organic Chemistry
9th Edition
ISBN:9781305080485
Author:John E. McMurry
Publisher:John E. McMurry
Chapter23: Carbonyl Condensation Reactions
Section23.SE: Something Extra
Problem 35MP: Isoleucine, another of the twenty amino acids found in proteins, is metabolized by a pathway that...
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What can be a reasonable hypothesis from the following observed in vitro data?
Compound 1
Kd = 20 nM
Compound 2
K₁ = 35 mM
There is an important hydrophobic interaction at the binding region.
There is not much space at the binding region, so removing the aromatic ring increases affinity.
O The removed aromatic ring is not part of the pharmacophore.
O The removed aromatic ring was getting metabolized and subsequently easily eliminated.
O Changing the methoxy group for an electron withdrawing group will result in decrease of affinity.
Transcribed Image Text:What can be a reasonable hypothesis from the following observed in vitro data? Compound 1 Kd = 20 nM Compound 2 K₁ = 35 mM There is an important hydrophobic interaction at the binding region. There is not much space at the binding region, so removing the aromatic ring increases affinity. O The removed aromatic ring is not part of the pharmacophore. O The removed aromatic ring was getting metabolized and subsequently easily eliminated. O Changing the methoxy group for an electron withdrawing group will result in decrease of affinity.
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