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59(2):205-211
ClH/c24-16-13(7-11(9-21-16)8-14-17(25)22-18(26)27-14)12-1-2-15(20-10-12)23-5-3-19-4-6-23
Smiles: CC1C=C(C=CC=1F)NC1N=C2C(C=C(C(=O)N2C)C2C(Cl)=CC=CC=2Cl)=CN=1
5-diamino-N-(N-benzylcarbamimidoyl)-6-chloropyrazine-2-carboxamide hydrochloride
and 450 nM
THS-044 thynyl Estradiol 59(2):205-211THS 044 binding stabilizes the HIF2 PAS B folded state, for regulating HIF2 activity in endogenous and clinical settings. Target: HIF2Limited trypsin proteolysis reveals that both apo and THS 044 bound protein are efficiently cut at R330 in the extended HI loop. In the THS 044 bound state, there appears no additional proteolysis at the remaining candidate trypsin sites. In contrast, these THS 044 protected sites are protease accessible in the
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