T68599
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Sodium Channel
NMDAR
AChR
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Orphenadrine 是一种非竞争性的 N-甲基-D-天冬氨酸(NMDA)受体拮抗剂,以浓度依赖性方式抑制克隆的 HERG 通道,在 HEK 细胞中产生0.85μM 的 IC。Orphenadrine 是中枢和外周毒蕈碱受体的拮抗剂,通过孔残基 Y652或 F656突变阻断衰减。 Orphenadrine 具有抗痉挛、镇痛和抗胆碱能活性,对在体外和体内对谷氨酸神经毒性具有保护作用。Orphenadrine 对钠离子通道具有抑制作用,可用来治疗帕金森。 |
T32033
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GYKI-46903 is a noncompetitive 5-HT3 receptor antagonist. |
T70467
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Alinastine is a noncompetitive histamine H1 receptor antagonist. |
T38050
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Transferase
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CP-609754 是高效的、可逆的法尼基转移酶抑制剂,对重组人 H-Ras 和重组 K-Ras 法尼基化的 IC50分别为 0.57 ng/mL 和 46 ng/mL。CP-609754有潜在的抗癌作用。 |
T27452
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GSK1723980 is a novel noncompetitive rTbIPMK inhibitor. |
T25516
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I-A09 is a noncompetitive mPTPB inhibitor. |
T24604
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PDAT is a noncompetitive Indolethylamine N-methyltransferase inhibitor. |
T27674
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JNJ-27141491 is a potent, noncompetitive antagonist of human CCR2. |
T38068
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Potent and noncompetitive NMDA receptor antagonist (IC50 = 36 nM). Exhibits >70-fold selectivity for NMDA receptor over σ receptor. Neuroprotective in a rat model of focal ischemia. |
T28614
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RPC425 is a noncompetitive inhibitors of the Betaine-γ-Aminobutyric Acid Transporter 1 (BGT1). |