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更新于：2025-05-22
Insilico Medicine Shanghai Ltd
更新于：2025-05-22
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肿瘤
免疫系统疾病
消化系统疾病
小分子化药
化学药
疾病领域得分
一眼洞穿机构专注的疾病领域
技术平台
公司药物应用最多的技术
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公司最常开发的靶点
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在研机构 |
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最高研发阶段 |
首次获批国家/地区 |
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靶点 |
作用机制 |
在研机构 |
原研机构 |
在研适应症 |
非在研适应症 |
最高研发阶段 |
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首次获批日期 |
CTR20241789
一项随机、双盲、安慰剂对照的单次、多次给药剂量递增研究以及食物影响研究以评估ISM5411在中国健康受试者中的安全性、耐受性、药代动力学特征和食物影响
CTR20240727
一项评价ISM8207治疗晚期实体瘤和复发/难治性B细胞淋巴瘤受试者的安全性、耐受性、药代动力学和初步疗效的I期、开放性、多中心、首次人体研究
CTR20230776
一项评价INS018_055口服给药用于治疗特发性肺纤维化（IPF）受试者的安全性、耐受性、药代动力学和有效性的随机、双盲、安慰剂对照、IIa期研究
100 项与 英矽智能科技（上海）有限公司 相关的临床结果
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2025-04-24JOURNAL OF MEDICINAL CHEMISTRY
Discovery of WEE1 Kinase Inhibitors with Potent Activity against Patient-Derived, Metastatic Colorectal Cancer Organoids
Article
作者: Ramsay, Robert G. ; Maddern, Guy J. ; Sammour, Tarik ; Sloan, Erica K. ; Mudududdla, Ramesh ; Fenix, Kevin ; Wright, Josephine A. ; Mukherjee, Siddhartha ; Syphers, Joel L. ; Liu, Shen ; Heriot, Alexander ; Gao, Fan ; Wang, Xiaomin ; Wei, Heping ; Kelter, Gerhard ; Lawrence, Matthew J. ; Kaur, Harleen ; Huang, Fei ; Posch, Markus ; Narasimhan, Vignesh ; Priebbenow, Daniel L. ; Silva, Tharindie N. ; Woods, Susan L. ; de Nys, Rebekah ; Worthley, Daniel L. ; Maier, Armin ; Baell, Jonathan B. ; Chang, Aeson ; Tin, Teresa ; Zhavoronkov, Alex ; Lu, Hongfu ; Barratt, Kate ; Gee, Yi Sing ; Che, Da Qing ; Vrbanac, Laura
A library of potent WEE1 kinase inhibitors was synthesized based on the discontinued frontrunner clinical candidate AZD1775 (1), many of which were more selective for WEE1 over an undesirable off-target of 1, the kinase PLK1. When tested against patient-derived organoids (PDOs) grown from TP53-mutated colorectal cancer (CRC) peritoneal metastases, 34 (IC50 value of 62 nM) exhibited stronger efficacy than 1 (IC50 value of 120 nM) and the best-in-class clinical candidate ZN-c3 (IC50 value of 127 nM). Against primary CRC PDOs with TP53-WT, 34 significantly enhanced DNA damage, replication stress and apoptosis compared to 1, as well as demonstrated high selectivity over patient-matched normal healthy colon PDOs, highlighting a potential therapeutic window for cancer treatment. Overall, this investigation provides critical insight into several potent WEE1 inhibitors that exhibited exceptional efficacy against CRC PDOs and is the first to utilize a PDO platform to assess their effect on healthy and malignant cell viability.
2025-04-10JOURNAL OF MEDICINAL CHEMISTRY
Discovery of Novel SIK2/3 Inhibitors for the Potential Treatment of MEF2C+ Acute Myeloid Leukemia (AML)
Article
作者: Zhu, Wei ; Cai, Xin ; Gao, Feng ; Zhang, Man ; Aliper, Alex ; Liu, Tingting ; Ren, Feng ; Zhao, Pei ; Ding, Xiao ; Li, Qi ; Zhavoronkov, Alex
The dual inhibition of SIK2/3 has been considered as a potential treatment approach for MEF2C-high acute myeloid leukemia (AML). Although diverse scaffolds of pan-SIK or SIK2/3 inhibitors have been reported, few of them showed sufficient in vitro or in vivo antitumor activity. Based on the proposed binding mode of the hit molecule (7), chemical space in the solvent/P-loop region was explored via fragment growing/replacement, supported by the generative chemistry platform. Further SAR exploration and ADME optimization led to the discovery of 7s, which exhibited excellent potency and strong selectivity in MEF2C high-expression cell lines over MEF2C-low cell lines. Moreover, oral administration of 7s was found to demonstrate significant tumor growth inhibition in a MV4-11 AML mice CDX model without any body weight loss. This work highlights the potential of targeting MEF2C-dependent AML by selective oral SIK2/3 inhibitors, which was supported by the generative models.
2025-02-27JOURNAL OF MEDICINAL CHEMISTRY
Design, Synthesis, and Biological Evaluation of Novel Orally Available Covalent CDK12/13 Dual Inhibitors for the Treatment of Tumors
Article
作者: Lu, Hongfu ; Sun, Deheng ; Zhang, Yihong ; Wu, Jianping ; Aliper, Alex ; Cai, Xin ; Min, Lihua ; Zhavoronkov, Alex ; Zhang, Man ; Cui, Hui ; Zhang, Haoyu ; Wang, Zhen ; Ren, Feng ; Ding, Xiao
Cyclin-dependent kinases 12 and 13 (CDK12/13) safeguard genomic integrity by preferentially regulating gene expression in the DNA damage response (DDR). The CDK12/13-mediated upregulation of DDR genes and pathways significantly contributes to both tumorigenesis and the development of resistance to antitumor therapies. Thus, the functional inhibition of CDK12/13 offers an attractive strategy to combat carcinogenesis, particularly for refractory and treatment-resistant cancers. Here, we report the discovery of compound 12b as a novel, potent, orally available covalent CDK12/13 dual inhibitor with a promising safety profile and robust in vivo antitumor properties.
100 项与 英矽智能科技（上海）有限公司 相关的药物交易
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100 项与 英矽智能科技（上海）有限公司 相关的转化医学
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2025年06月23日管线快照
管线布局中药物为当前组织机构及其子机构作为药物机构进行统计，早期临床1期并入临床1期，临床1/2期并入临床2期，临床2/3期并入临床3期
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