reference to table 1, discuss the structure activity relationships related to the nature of the substituent R1 and linker group L. In your answer, aim not just to identify trends, but to give possible explanations to them. Include as much detail as possible.

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Publisher:Matthew Douglas, Jung Choi, Mary Ann Clark
Chapter9: Cell Communication
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A range of substituted biphenyls have been evaluated as antagonists of the GPCR neurokinin-1 (NK1) , a target for the treatment of cancer chemotherapy endured nausea and vomiting. With reference to table 1, discuss the structure activity relationships related to the nature of the substituent R1 and linker group L. In your answer, aim not just to identify trends, but to give possible explanations to them. Include as much detail as possible.
Table 1. Effect of biphenyl substituent R¹ and linker group L on human NK₁ inhibitory
activity.
R¹
CF3
R¹
hNK₁ K₁
hNK₁ K₁
Com-
pound
(nM)
(nM)
1
51
295
2
17
>10,000
22
562
45
68
> 10,000
1,380
3
4
5
H
CH3
CI
Br
H
O
www
O
w
O
L
m
CF3
Com-
pound
6
7
8
9
10
R¹
H
H
H
H
H
L
2X
ex
NN
www.
mj
IZ ₂₂
O
Transcribed Image Text:Table 1. Effect of biphenyl substituent R¹ and linker group L on human NK₁ inhibitory activity. R¹ CF3 R¹ hNK₁ K₁ hNK₁ K₁ Com- pound (nM) (nM) 1 51 295 2 17 >10,000 22 562 45 68 > 10,000 1,380 3 4 5 H CH3 CI Br H O www O w O L m CF3 Com- pound 6 7 8 9 10 R¹ H H H H H L 2X ex NN www. mj IZ ₂₂ O
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