NSD2 Degrader CSV,,,,
Compound number,Structure,Activity in reducing the NSD2 protein level in 293FT cells by western blotting,Kd (μM),NSD2: DC50 μM
1,O=C(C1=CC=C(C=C1)NC(C(C=C2)=CC=C2CN(C(C3=CC=C4NC(COC4=C3)=O)=O)C5CC5)=O)NCCOCCOCCC(N[C@@H](C(C)(C)C)C(N6[C@H](C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C6)=O)=O,Yes,Not determined,Not determined
2,O=C(C1=CC=C(C=C1)NC(C(C=C2)=CC=C2CN(C(C3=CC=C4NC(COC4=C3)=O)=O)C5CC5)=O)NCCCCCC(N[C@H](C(N6C[C@@H](C[C@H]6C(NCC(C=C7)=CC=C7C8=C(N=CS8)C)=O)O)=O)C(C)(C)C)=O,No,Not determined,Not determined
3,O=C(C1=CC=C(C=C1)NC(C(C=C2)=CC=C2CN(C(C3=CC=C4NC(COC4=C3)=O)=O)C5CC5)=O)NCCOCCOCCOCCNC6=CC=CC(C(N7C8C(NC(CC8)=O)=O)=O)=C6C7=O,No,Not determined,Not determined
4,O=C(C1=CC=C(C=C1)NC(C(C=C2)=CC=C2CN(C(C3=CC=C4NC(COC4=C3)=O)=O)C5CC5)=O)NCCNC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O,No,Not determined,Not determined
5,O=C1COC2=CC(C(N(CC3=CC=C(C(NC(C=C4)=NC=C4OCCCNC(CCOCCOCCOCCC(N[C@H](C(N5C[C@@H](C[C@H]5C(NCC(C=C6)=CC=C6C7=C(N=CS7)C)=O)O)=O)C(C)(C)C)=O)=O)=O)C=C3)C8CC8)=O)=CC=C2N1,No,Not determined,Not determined
6,O=C1COC2=CC(C(N(CC3=CC=C(C(NC(C=C4)=NC=C4OCCCNC(CCCC(N[C@H](C(N5C[C@@H](C[C@H]5C(NCC(C=C6)=CC=C6C7=C(N=CS7)C)=O)O)=O)C(C)(C)C)=O)=O)=O)C=C3)C8CC8)=O)=CC=C2N1,No,Not determined,Not determined
7,O=C1COC2=CC(C(N(CC3=CC=C(C(NC(C=C4)=NC=C4OCCCNC(CCOCCOCCNC5=CC=CC6=C5C(N(C6=O)C7CCC(NC7=O)=O)=O)=O)=O)C=C3)C8CC8)=O)=CC=C2N1,No,Not determined,Not determined
8,O=C1COC2=CC(C(N(CC3=CC=C(C(NC(C=C4)=NC=C4OCCCNC(CCCCCCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)=O)=O)C=C3)C8CC8)=O)=CC=C2N1,No,Not determined,Not determined
9 (MS159),O=C1COC2=CC(C(N(CC3=CC=C(C(NC(C=C4)=NC=C4OCCCNC(CNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)=O)=O)C=C3)C8CC8)=O)=CC=C2N1,Yes,1.1 ± 0.4,5.2 ± 0.9
10,O=C1COC2=CC(C(N(CC3=CC=C(C(NC(C=C4)=NC=C4OCCCNC(CCOCCOCCOCCNC(C=C5)=CC6=C5C(N(C6=O)C7CCC(NC7=O)=O)=O)=O)=O)C=C3)C8CC8)=O)=CC=C2N1,No,Not determined,Not determined
11,O=C(N1)CCC(N(C2=O)C(C3=C2C=CC(NCCCCC(NCCCOC4=CN=C(C=C4)NC(C(C=C5)=CC=C5CN(C(C6=CC=C7NC(COC7=C6)=O)=O)C8CC8)=O)=O)=C3)=O)C1=O,No,Not determined,Not determined
17 (MS159N1),O=C1COC2=CC(C(N(CC3=CC=C(C(NC(C=C4)=NC=C4OCCCNC(CNC5=CC=CC(C(N6C7C(N(C)C(CC7)=O)=O)=O)=C5C6=O)=O)=O)C=C3)C8CC8)=O)=CC=C2N1,No,0.9 ± 0.3,Not determined
18 (MS159N2),O=C1COC2=CC(C(N(CC3=CC=C(C(NC(C=C4)=NC=C4OCCCNC(CNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)=O)=O)C=C3)C(C)C)=O)=CC=C2N1,No,Not determined,Not determined