ARV-771

Description: ARV-771 is a potent BET degrader based on PROTAC technology, with Kds of 34 nM for BRD2(1), 4.7 nM for BRD2(2), 8.3 nM for BRD3(1), 7.6 nM for BRD3(2), 9.6 nM for BRD4(1), and 7.6 nM for BRD4(2), respectively[1]. Target: PROTACs, Epigenetic Reader Domain. Smiles: CC=1C2=C(N3C([C@H](CC(NCCOCCCOCC(N[C@H](C(=O)N4[C@H](C(N[C@@H](C)C5=CC=C(C=C5)C=6SC=NC6C)=O)C[C@@H](O)C4)C(C)(C)C)=O)=O)N=C2C7=CC=C(Cl)C=C7)=NN=C3C)SC1C. References: Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 201. Jun 28,113(26):7124-9.