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. 2014 May 23;136(22):7877–7888. doi: 10.1021/ja502310r

Table 4. Oxopiperazine HIF Mimics Targeting the CH1 Domain of p300/CBP.

graphic file with name ja-2014-02310r_0018.jpg

mimetic R1 R2 R3 R4 Kd (μM)a
21 Leu Leu Ala Gln 0.53 ± 0.14
22 Leu Ala Ala Gln >10
23 Leu Nle Ala Gln 0.03 ± 0.01
24 Met Met Ala Gln 0.24 ± 0.04
25 Hle Hle Ala Gln 0.16 ± 0.06
a

Binding affinity for p300-CH1 was determined using an intrinsic tryptophan fluorescence assay.