CMX

发现CMX990：有效的SARS-COV-2 3CL蛋白酶抑制剂带有新型的共价弹头

1 4.4 N.D. N.D. 72 99.3 147.7 31.8 A- <1 a -2 3.3 14.8 n.d. 54 93.4 1109.4 47.6 a，b 50.3 1.3 a，b 1.5 3 2.8 76.3 133 133 17 7.6 173 19.3 99 39.8 34.2 45.1 38.8 25.2 21.6 7 2.6 24.0 n.d. 117 54.8 62.2-36.2 - 8 3.0 34.7 n.d. 61 43.5 26.2 53.2 C -51.3 C -9 2.0 36.5 n.d. 108 58.8 16.3-40.3--10 1.3 35.4 n.d. 346 <1 12.8 71.0 11.7 7.2 28.0 11 28.0 11 2.0 34.5 50.8 62 31.7 8.4 35.6 C 51.8 35.3 C 35.3 C 35.7 12 1.0 33.7 20.7 20.5 24 47.3 17.4 11.4 11.1 C 56.9 20.7 C 56.9 20.7 C 25.7 C 25.0 13 3.6 34.8 34.8 13 3.6 34.8 13 3.6 34.8 14 38 14 38 38 38 38 38 67.5 67.5 67.5 67.5 67.5 67.5 67.5 17.5 67.5 67.5 67.5 67.5 67.5 17.5 19.c. 15.0 2.4 35.3 14 2.0 60.1 51.8 138 34.3 12.2 107 18.4 19.0 48.7 15 0.3 15 0.3 160 N.D. 245 51.8 13.0 N.C. A 23.3 4.6 A 37.7 16 2.6 22.0 n.d. 50 50.1 14.9 19.3 c 23.7 10.2 c 57.2 CMX990 2.3 23.4 9.6 101 56.3 7.5 125 23.0 14.5 52.8 Nirmatrelvir 1.5 28.1 44.8 148 54.8 21.8 35.8 1.92 53.5 68.7 PF-00835231 1.2 101 81.4 630 77.2 13.9 86.4-1.0- a =仓鼠，B =近距离类似物的数据，C =大鼠EC 90 = 90％有效浓度，Cl int =固有清除率，Clp =血浆清除率，F =生物利用度，HLM =人肝微染色体，HPPB = HPPB = HUMEN PLASMA蛋白质结合，IV = IV = IV = inv = intravenos，iv = intravenous，n. n。 =未确定，N.C。 =未计算，po = per per os（oral）1 4.4 N.D. N.D. 72 99.3 147.7 31.8 A- <1 a -2 3.3 14.8 n.d. 54 93.4 1109.4 47.6 a，b 50.3 1.3 a，b 1.5 3 2.8 76.3 133 133 17 7.6 173 19.3 99 39.8 34.2 45.1 38.8 25.2 21.6 7 2.6 24.0 n.d. 117 54.8 62.2-36.2 - 8 3.0 34.7 n.d. 61 43.5 26.2 53.2 C -51.3 C -9 2.0 36.5 n.d. 108 58.8 16.3-40.3--10 1.3 35.4 n.d. 346 <1 12.8 71.0 11.7 7.2 28.0 11 28.0 11 2.0 34.5 50.8 62 31.7 8.4 35.6 C 51.8 35.3 C 35.3 C 35.7 12 1.0 33.7 20.7 20.5 24 47.3 17.4 11.4 11.1 C 56.9 20.7 C 56.9 20.7 C 25.7 C 25.0 13 3.6 34.8 34.8 13 3.6 34.8 13 3.6 34.8 14 38 14 38 38 38 38 38 67.5 67.5 67.5 67.5 67.5 67.5 67.5 17.5 67.5 67.5 67.5 67.5 67.5 17.5 19.c. 15.0 2.4 35.3 14 2.0 60.1 51.8 138 34.3 12.2 107 18.4 19.0 48.7 15 0.3 15 0.3 160 N.D. 245 51.8 13.0 N.C. A 23.3 4.6 A 37.7 16 2.6 22.0 n.d. 50 50.1 14.9 19.3 c 23.7 10.2 c 57.2 CMX990 2.3 23.4 9.6 101 56.3 7.5 125 23.0 14.5 52.8 Nirmatrelvir 1.5 28.1 44.8 148 54.8 21.8 35.8 1.92 53.5 68.7 PF-00835231 1.2 101 81.4 630 77.2 13.9 86.4-1.0- a =仓鼠，B =近距离类似物的数据，C =大鼠EC 90 = 90％有效浓度，Cl int =固有清除率，Clp =血浆清除率，F =生物利用度，HLM =人肝微染色体，HPPB = HPPB = HUMEN PLASMA蛋白质结合，IV = IV = IV = inv = intravenos，iv = intravenous，n. n。 =未确定，N.C。 =未计算，po = per per os（oral）