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
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
Chemistry
10th Edition
ISBN:9781305957404
Author:Steven S. Zumdahl, Susan A. Zumdahl, Donald J. DeCoste
Publisher:Steven S. Zumdahl, Susan A. Zumdahl, Donald J. DeCoste
Chapter1: Chemical Foundations
Section: Chapter Questions
Problem 1RQ: Define and explain the differences between the following terms. a. law and theory b. theory and...
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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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