Table 4. Oxopiperazine HIF Mimics Targeting the CH1 Domain of p300/CBP.
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 |
Binding affinity for p300-CH1 was determined using an intrinsic tryptophan fluorescence assay.