human cathepsin l

SID 26681509 是可逆的，竞争性的人组织蛋白酶 L 选择性抑制剂，IC50为 56 nM。它抑制Plasmodium falciparum 的体外繁殖，IC50为15.4 μM，抑制Leishmania major，IC5012.5 μM。

Acetyl-Calpastatin (184-210)(human) acetate 是一种有效，选择性和可逆的钙蛋白酶 (calpain) 抑制剂，对 μ-钙蛋白酶和组织蛋白酶 L 的 Ki 值分别为 0.2 nM 和 6 μM。

VK13 (Compound 6) 是一种强效抑制剂，针对人cathepsin L (hCatL) 及SARS-CoV-2 3CLpro (3CL-PR)，其Ki值分别为2.6 nM 和0.55 nM。VK13 显示出抗CoV-2 活性，其EC50值为1.25 μM。

FGA145 是一种同时抑制 Mpro 和人 Cathepsin L 的抑制剂，对 Mal-Mpro、pET21-Mpro 和 Cathepsin L 的 Ki 分别为 3.71 μM、9.82 μM 和 53 nM。FGA145 显示出多靶点的抗病毒活性。

FGA146 是一种选择性的 Mpro 和人 Cathepsin L 抑制剂，对 Mal-Mpro, pET21-Mpro 和 Cathepsin L 的 Ki 值分别为 2.19 μM, 0.96 μM 和 0.87 μM。它对 SARS-CoV-2 展现出抗病毒活性。

Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V. It exhibits high affinity for these enzymes, with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Moreover, Relacatib effectively inhibits endogenous cathepsin K in situ in human osteoclasts, as well as human osteoclast-mediated bone resorption, with IC 50 values of 45 nM and 70 nM, respectively. Additionally, in vitro studies demonstrate Relacatib's inhibitory effect on bone resorption in human tissue, while in vivo studies on cynomolgus monkeys further validate its efficacy in reducing bone resorption.

SID 26681509 quarterhydrate 是可逆的、有效的、选择性的、竞争性的人组织蛋白酶 L (human cathepsin L) 抑制剂 (IC50: 56 nM)。SID 26681509 quarterhydrate 能够抑制Plasmodium falciparum 的体外繁殖 (IC50: 15.4 μM)，并抑制Leishmania major (IC50: 12.5 μM)，且不抑制组织蛋白酶 G 的活性。

Thiocarbazate, also known as CID16725315, is an inhibitor of human cathepsin L. Inhibition of cathepsin L thus holds promise for therapeutic intervention for both SARS-CoV and Ebola virus infection. With respect to the development of antiviral agents, inhibitors of human cathepsin L are not subject to resistance because of rapid mutations of the viral genome. Cathepsin L is therefore an attractive target for drug development.

Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L. In the cathepsin L inhibition assay, The oxocarbazate caused a time-dependent 17-fold drop in IC50 from 6.9 nM (no preincubation) to 0.4 nM (4-h preincubation). Slowly reversible inhibition was demonstrated in a dilution assay. CID23631927 demonstrate activity in blocking both SARS-CoV (IC50 = 273 nM) and Ebola virus (IC50 = 193 nM) entry into human embryonic. CID 23631927 was a subnanomolar, slow-binding, reversible inhibitor of human cathepsin L that blocked SARS-CoV and Ebola pseudotype virus entry in human cells. Inhibition of cathepsin L thus holds promise for therapeutic intervention for both SARS-CoV and Ebola virus infection.

SPR39 是一种有效的 SARS-CoV-2 主要蛋白酶抑制剂，对 SARS-CoV-2 Mpro, hCatL, hCatB 的 Ki 值分别为 0.252、3.38、7.88 µM。SPR39 具有抗病毒和细胞毒性。

SPR38 是一种有效的 SARS-CoV-2 主要蛋白酶 (SARS-CoV-2 main protease) 抑制剂，Ki 为 0.260 μM。SPR38 还抑制hCatL 和hCatB，Ki 值分别为 1.92 μM 和 11.1 μM。

Acetyl-Calpastatin(184-210)(human) TFA 是一种有效，选择性和可逆的钙蛋白酶 (calpain) 抑制剂，对 μ-钙蛋白酶和组织蛋白酶 L 的Ki 值分别为 0.2 nM 和 6 μM。

Olgotrelvir sodium 是一种口服活性化合物，具备双重抑制冠状病毒主蛋白酶 (Mpro) 和人细胞组织蛋白酶 (CathepsinL) 的功能。Olgotrelvir sodium 能有效地抑制SARS-CoV-2的复制并阻止其进入宿主细胞。