SCH-202676

• 常用名: SCH-202676
• 英文名: SCH-202676
• CAS号: 70375-43-8
• 分子量: 348.26100
• 密度: N/A
• 沸点: 392ºC at 760 mmHg
• 分子式: C₁₅H₁₄BrN₃S
• 熔点: 240.0-240.8ºC(lit.)
• 闪点: 190.9ºC

SCH-202676用途

SCH-202676是G蛋白偶联受体(GPCR)和腺苷受体(AR)的变构调节剂。SCH-202676具有抗病毒活性,以时间依赖的方式抑制3CLpro,IC50值为0.655µM[1][2][3][4]。

SCH-202676名称

• 英文名: (Z)-N-(2,3-diphenyl-1,2,4-thiadiazol-5(2H)-ylidene)methanamine

SCH-202676生物活性

• 描述: SCH-202676是G蛋白偶联受体(GPCR)和腺苷受体(AR)的变构调节剂。SCH-202676具有抗病毒活性,以时间依赖的方式抑制3CLpro,IC50值为0.655µM[1][2][3][4]。
• 相关类别:
  信号通路 >> 抗感染 >> 流感病毒
  研究领域 >> 感染
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> GPCR19
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 腺苷受体
• 靶点实验:

  Adenosine A3 receptor

• 体外研究: SCH-202676(化合物6a)具有抗病毒活性并以时间依赖的方式抑制 3CLpro在 0、5、10 和 20分钟的 国际50值分别为 0.409、0.302、0.206 和 0.191µM[1]SCH-202676(10μM；90分钟)加强了大鼠前脑膜中 [35S]GTPγS的标记[2]。 表-202676抑制激动剂 [3H]UK-14304(HY-B0659)和拮抗剂 [3H]育亨宾 (育亨宾,HY-12715)与 α2a肾上腺素能受体的结合[3]。 SCH-202676(10μM)选择性地加速了激动剂在腺苷 第3页受体上的解离,减慢了拮抗剂在腺苷 艾岛受体上的解离,或加速了拮抗剂在腺苷 AzA公司受体上的解离[4]。
• 参考文献:

  [1]. Ren P, et al. Discovery, synthesis and mechanism study of 2,3,5-substituted [1,2,4]-thiadiazoles as covalent inhibitors targeting 3C-Like protease of SARS-CoV-2. Eur J Med Chem. 2023 Jan 18;249:115129.

  [2]. Lewandowicz AM, et al. The 'allosteric modulator' SCH-202676 disrupts G protein-coupled receptor function via sulphydryl-sensitive mechanisms. Br J Pharmacol. 2006 Feb;147(4):422-9.

  [3]. Fawzi A B, et al. SCH-202676: an allosteric modulator of both agonist and antagonist binding to G protein-coupled receptors[J]. Molecular Pharmacology, 2001, 59(1): 30-37.

  [4]. Gao ZG, et al. Effects of the allosteric modulator SCH-202676 on adenosine and P2Y receptors. Life Sci. 2004 May 7;74(25):3173-80.

SCH-202676物理化学性质

• 沸点: 392ºC at 760 mmHg
• 熔点: 240.0-240.8ºC(lit.)
• 分子式: C₁₅H₁₄BrN₃S
• 分子量: 348.26100
• 闪点: 190.9ºC
• 精确质量: 347.00900
• PSA: 58.42000
• LogP: 4.08940
• InChIKey: FFUBTEITUNMMOK-UHFFFAOYSA-N
• SMILES: CN=c1nc(-c2ccccc2)n(-c2ccccc2)s1

SCH-202676安全信息

• 危害码 (欧洲): Xi
• 风险声明 (欧洲): 36/37/38
• 安全声明 (欧洲): 26-36

SCH-202676靶点实验

查看更多实验

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfect... 来源：Broad Institute 靶标：N/A External Id：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfected HEK293 cells Inhibition - 7011-01_Antagonist_SinglePoint_HTS_Activity

实验名称：Tocris HTS for Inhibitors of Aerobactin Synthetase lucA 来源：23265 External Id：IucA Pilot Assay Tocris Library

实验名称：Dicer-mediated maturation of pre-microRNA 来源：Center for Chemical Genomics, University of Michigan 靶标：N/A External Id：TargetID_659_CEMA

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify pos... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_PAM_FLUO8_1536_1X%ACT PRUN

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=Sialate O-acetylesterase; AltName: Full=H-Lse; AltName: Full=Sialic acid-specific 9-O-acetylesterase; Flags: Precursor [Homo sapiens] External Id：SIAE_INH_FP_1536_1X%INH PRUN

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SCH-202676英文别名

• aurora ka-7903