GNE-9278

• 常用名: GNE-9278
• 英文名: GNE-9278
• CAS号: 2315311-83-0
• 分子量: 429.54
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₁H₂₇N₅O₃S
• 熔点: N/A
• 闪点: N/A

GNE-9278用途

GNE-9278 是 NMDAR 的高选择性正变构调节剂,可作用于 GluN1 跨膜结构域 (TMD)。 GNE-9278 作用于活化的 NMDAR,以增加峰值电流和激动剂亲和力。

GNE-9278名称

• 英文名: GNE-9278

GNE-9278生物活性

• 描述: GNE-9278 是 NMDAR 的高选择性正变构调节剂,可作用于 GluN1 跨膜结构域 (TMD)。 GNE-9278 作用于活化的 NMDAR,以增加峰值电流和激动剂亲和力。
• 相关类别:
  信号通路 >> 神经信号通路 >> iGluR
  研究领域 >> 神经疾病
  信号通路 >> 跨膜转运 >> iGluR
• 靶点实验:

  NMDAR[1]

• 体外研究: GNE-9278(50μM)通过多种激动剂(D-Glu、L-Glu和L-CCG-IV)减缓失活,并提高Glu和Gly的效力[1]。GNE-9278强烈增强了含GluN2A、2B、2C和2D的NMDAR,其EC50分别为0.74、3.07、0.47和0.32μM[1]。
• 参考文献:

  [1]. Wang TM, et, al. A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain. Neuropharmacology. . 2017 Jul 15; 121: 204-218.

GNE-9278物理化学性质

• 分子式: C₂₁H₂₇N₅O₃S
• 分子量: 429.54

GNE-9278靶点实验

查看更多实验

实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

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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：qHTS of TDP-43 Inhibitors: NCGC Sytravon Library Screen 来源：NCGC External Id：tdp43-p2-repeat

实验名称：Positive allosteric modulation of GluN2A receptor (unknown origin) expressed in xenop... 来源：ChEMBL 靶标：Glutamate receptor ionotropic, NMDA 2A External Id：CHEMBL4309009

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

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