Membrane Transporters/Ion Channels
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Protein translocation 抑制剂
Brefeldin A阻断ADP-核糖基化因子与高尔基体的结合并抑制GDP-GTP交换。
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ATPase 拮抗剂
PF 3716556是H+,K+-ATPase酶抑制剂(在人类重组离子渗漏试验中PIC50 = 6)。
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protein tyrosine phosphatases inhibitor
Sodium orthovanadate是化合物Na3VO4。 它是蛋白质酪氨酸磷酸酶，碱性磷酸酶和许多ATPase的抑制剂，很可能充当磷酸盐类似物。
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Artemisinin及其衍生物是一类药物，在所有当前针对恶性疟原虫疟疾的药物中具有最快的作用。
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Ciclopirox是一种合成的抗真菌药物。它可以抑制酵母糠醛马拉丝霉的生长，并通过中断Na+K+ ATPase来抑制膜转移系统，从而发挥作用。
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- Katsuhisa Morita, .et al. Decomposition profile data analysis of multiple drug effects identifies endoplasmic reticulum stress-inducing ability as an unrecognized factor, Sci Rep, 2020, 10: 13139 PMID: 32753643
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Pantoprazole是一种质子泵抑制剂药物，可抑制胃酸分泌。
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Bufalin是蟾酥中的有效活性成分，为有效的 Na+/K+-ATPase 抑制剂，可与其基 α1, α2 和 α3 结合，Kd 值分别为 42.5，45 和 40 nM。具有抗肿瘤活性。
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Resibufogenin是一种特异性na+/k+-ATP酶抑制剂。
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Bufotalin是一种比其他蟾毒二烯内酯更弱的na+/k+-ATP酶抑制剂。强效免疫抑制剂。
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Cinobufagin是一种特异性na+/k+-ATP酶抑制剂。大约和哇巴因一样活跃。
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a-K-ATPase 抑制剂
Ouabain是一种选择性的Na+，K+-ATPase抑制剂。
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- Paul Mark Medina, .et al. Revealing the anticancer potential of candidate drugs in vivo using Caenorhabditis elegans mutant strains, Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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ATPase 抑制剂
Oligomycin A是线粒体ATPase抑制剂。寡霉素A抑制与细胞膜结合的ATP5（线粒体ATP酶，F1F0）。
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- Makoto Kawatani, .et al. Identification of a Small-Molecule Glucose Transporter Inhibitor, Glutipyran, That Inhibits Cancer Cell Growth, ACS Chem Biol, 2021, 16, 8, 1576-1586
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ATPase 抑制剂
Omeprazole是一种可透过细胞的选择性质子泵抑制剂。
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PST-2744 (Istaroxime)是一种正性肌力药物，通过抑制钠/钾腺苷三磷酸酶（Na+/K+ ATPase）介导其作用。
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Na+/K+ ATPase modulator
Rostafuroxin (PST-2238)是一种哇巴因抑制剂，可对抗特定形式的高血压。
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myosin II 抑制剂
(-)-Blebbistcitin是有效且选择性的 myosin II 抑制剂，IC50 范围为0.5至5 μM。
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F1 Fo-ATPase 抑制剂
BTB06584是线粒体F1 Fo-ATPase的IF1依赖性选择性抑制剂。
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Na+/K+ ATPase 抑制剂
Melittin是一种Na+/K+ ATPase抑制剂。它抑制Gs并刺激Gi活性。它抑制蛋白激酶C和依赖cAMP的蛋白激酶。
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ATP synthase 抑制剂
Oligomycin是一种大环内酯类化合物，可作为线粒体ATP合酶的特异性抑制剂并阻止氧化磷酸化作用。
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SERCA 抑制剂
Cyclopiazonic acid是SERCA（内质网Ca2+ -ATPase）的抑制剂，可诱导细胞内储存的Ca2+释放，而不会增加IP3水平。
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SERCA ATPase 抑制剂
Thapsigargin是在Thapsia garganica的根中发现的一种细胞可渗透的倍半萜烯内酯。它是肿瘤的启动子，可通过抑制肌浆/内质网Ca2+ -ATPase（SERCA，IC50 = 30 nM）诱导细胞内储存的Ca2+释放，而不会水解肌醇磷脂。
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Ca 2+ /Mg 2+ -ATPase 抑制剂
Glucagon (19-29), human是有效的Ca2+/Mg2+ -ATPase抑制剂。
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CFTR 抑制剂
PTC124也称为Ataluren，是CFTR-G542X无意义等位基因抑制剂。
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- L Kadunc, .et al. Increased Gene Translation Stringency in Mammalian Cells by Nonsense Suppression at Multiple Permissive Sites With a Single Noncanonical Amino Acid, FEBS Lett, 2020, May 13 PMID: 32401336
- Caspi M, .et al. A flow cytometry-based reporter assay identifies macrolide antibiotics as nonsense mutation read-through agents, J Mol Med (Berl), 2016, Apr;94(4):469-82 PMID: 26620677
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CFTR activator
VX-770 (Ivacaftor)被称为CFTR增强剂，靶向作用于G551D-CFTR和F508del-CFTR，在fisher大鼠甲状腺细胞中EC50分别为100 nM和25 nM。
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- Okiyoneda T, .et al. Chaperone-Independent Peripheral Quality Control of CFTR by RFFL E3 Ligase, Dev Cell, 2018, Mar 26;44(6):694-708.e7 PMID: 29503157
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CFTR modulator
VX-809 (Lumacaftor)是用于治疗囊性纤维化（CF）的第二种口服研究候选化合物，通过促进突变型CFTR(F508del-CFTR)的成熟，从而纠正囊性纤维症中常见的CFTR突变，在fisher大鼠甲状腺细胞中EC50为0.1 μM。
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- Kusumika Saha, .et al. Pharmacological chaperone-rescued cystic fibrosis CFTR-F508del mutant overcomes PRAF2-gated access to endoplasmic reticulum exit sites, Cell Mol Life Sci, 2022, Sep 27;79(10):530 PMID: 36167862
- Heledd H Jarosz-Griffiths, .et al. Different CFTR Modulator Combinations Downregulate Inflammation Differently in Cystic Fibrosis, Elife, 2020, Mar 2;9:e54556 PMID: 32118580
- Okiyoneda T, .et al. Chaperone-Independent Peripheral Quality Control of CFTR by RFFL E3 Ligase, Dev Cell, 2018, Mar 26;44(6):694-708.e7 PMID: 29503157
- Junko Kido, .et al. Cystic Fibrosis Transmembrane Conductance Regulator Reduces Microtubule-Dependent Campylobacter jejuni Invasion, Infect Immun, 2017, Oct; 85(10): e00311-17 PMID: 28784926
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CFTR corrector
VX-661是另一种正在开发中的用于治疗囊性纤维化的囊性纤维化跨膜电导调节器（CFTR）校正器。
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- Kusumika Saha, .et al. Pharmacological chaperone-rescued cystic fibrosis CFTR-F508del mutant overcomes PRAF2-gated access to endoplasmic reticulum exit sites, Cell Mol Life Sci, 2022, Sep 27;79(10):530 PMID: 36167862
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K+ channel and CFTR Cl- channel blocker
Glyburide (Glibenclamide) 是一种抗糖尿病化合物，是一类磺脲类药物。
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CFTR 抑制剂
CFTR inhibitor II,也称为GlyH-101，是一种甘氨酸酰肼，可选择性和可逆地阻断CFTR通道（Ki = 4.3 uM）。
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- Dao-Lai Zhang, .et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility, eLife, 2018, 7: e33432 PMID: 29393851
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CFTR chloride channel 抑制剂
PPQ-102是一种化合物，其靶向cftr的胞内核苷酸结合结构域，并以电压依赖性和可逆的方式抑制cftr介导的氯离子电流。
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CFTR 抑制剂
Oridonin (Isodonol)是一种从鼠李木中分离出来的Entkaurane二萜类化合物，是一种重要的传统中草药。
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CFTR 抑制剂
CFTRinh-172是电压无关的选择性CFTR抑制剂。在2分钟内可逆地抑制CFTR短路电流的 Ki 值为300 nM。
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- Dao-Lai Zhang, .et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility, eLife, 2018, 7: e33432 PMID: 29393851
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F508del-CFTR trafficking corrector
KM 11060纠正了F508del-CFTR的运输，增加了质膜上功能性CFTR的量（?75％）并抑制了PDE5的活性。
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CFTR potentiator
PG 01 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. PG 01 is effective on G970R although with a significant decrease in potency relative to E193K and δF508.
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CFTR corrector
CFTR corrector 2 is a cystic fibrosis transmembrane conductance corrector (CFTR), extracted from patent US20140274933.
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CFTR potentiator
GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator, which effectively potentiates low temperature rescued F508del CFTR with an EC50 of 11.1 nM.
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CFTR potentiator
Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
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CFTR potentiator
Ivacaftor hydrate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
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intracellular Ca2+ handling modulator
Caldaret is an intracellular Ca2+ handling modulator that acts through reverse mode Na+/Ca2+ exchanger inhibition.
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T-type Ca2+ channel blocker
ABT-639 hydrochloride is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
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L-type Ca2+ channel agonist
(S)-(-)-Bay-K-8644 is an agonist of L-type Ca2+ channel. (S)-(-)-Bay-K-8644 activates Ba2+ currents (IBa) (EC50=32 nM).
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T-type Ca2+ channel antagonist
TTA-Q6 is a selective T-type Ca2+ channel antagonist, used in the neurological disease.
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T-type Ca2+ channel antagonist
TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca2+ channel antagonist.
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Ca2+-dependent blocker
TV-519 free base (K201 free base) is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
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N- and P/Q-type Ca2+ channels agonist
GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.
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Calcium Channel 抑制剂
Tetrandrine (Fanchinine)是一种钙通道阻滞剂。粉防己碱具有抗炎和抗纤维化作用，使粉防己碱及其相关化合物潜在地用于治疗肺矽肺，肝硬化和类风湿性关节炎。
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Ca2+ signaling modulator
Astragaloside A是缺氧条件下人脐静脉内皮细胞HIF-1α和通过PI3K/Akt途径血管生成的一种新型调节因子。
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Myosin activator
CK-1827452 (Omecamtiv mecarbil)是选择性的心脏特异性肌球蛋白激活剂。
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- Oleg Lookin, .et al. Omecamtiv mecarbil attenuates length-tension relationship in healthy rat myocardium and preserves it in monocrotaline-induced pulmonary heart failure, Clin Exp Pharmacol Physiol, 2021, Aug 29 PMID: 34459025
- Gabor A. Fulop, .et al. Omecamtiv mecarbil evokes diastolic dysfunction and leads to periodic electromechanical alternans, Basic Res Cardiol, 2021, 116(1): 24 PMID: 33844095
- Wanjian Tang, .et al. Dilated cardiomyopathy mutation in the converter domain of human cardiac myosin alters motor activity and response to omecamtiv mecarbil, J Biol Chem, 2019, October 2 PMID: 31578282
- Thinh T. Kieu, .et al. Omecamtiv Mecarbil Slows Myosin Kinetics in Skinned Rat Myocardium at Physiological Temperature, Biophysical Journal, 2019, 2019 PMID: 31103235
- Alexandre J. S. Ribeiro, .et al. Multi-Imaging Method to Assay the Contractile Mechanical Output of Micropatterned Human iPSC-Derived Cardiac Myocytes, Circ Res, 2017, May 12; 120(10): 1572-1583 PMID: 28400398
- Anja M. Swenson, .et al. Omecamtiv Mecarbil Enhances the Duty Ratio of Human β-Cardiac Myosin Resulting in Increased Calcium Sensitivity and Slowed Force Development in Cardiac Muscle, J Biol Chem, 2017, Mar 3; 292(9): 3768-3778 PMID: 28082673
- Nánási P Jr, .et al. Omecamtiv mecarbil activates ryanodine receptors from canine cardiac but not skeletal muscle, Eur J Pharmacol, 2017, Aug 15;809:73-79 PMID: 28506910
- Horv??th B, .et al. Frequency-dependent effects of omecamtiv mecarbil on cell shortening of isolated canine ventricular cardiomyocytes, Naunyn Schmiedebergs Arch Pharmacol, 2017, Dec;390(12):1239-1246 PMID: 28940010
- Szentandrassy N, .et al. Dose-dependent electrophysiological effects of the myosin activator omecamtiv mecarbil in canine ventricular cardiomyocytes, J Physiol Pharmacol, 2016, Aug;67(4):483-489 PMID: 27779469
- L Nagy, .et al. The novel cardiac myosin activator omecamtiv mecarbil increases the calcium sensitivity of force production in isolated cardiomyocytes and skeletal muscle fibres of the rat, Br J Pharmacol, 2015, Sep; 172(18): 4506-4518 PMID: 26140433
- Larissa Butler, .et al. Enhanced characterization of contractility in cardiomyocytes during early drug safety assessment, Toxicol Sci, 2015, Jun;145(2):396-406 PMID: 25820236
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Manidipine dihydrochloride是Manidipine的HCl盐形式，Manidipine是Ca2+电流的钙通道阻滞剂，IC50为2.6 nM。
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- Noriaki Ikemura,, .et al. Inhibitory effects of antihypertensive drugs on human cytochrome P450 2J2 activity: Potent inhibition by azelnidipine and manidipine, Chem -Biol Interact, 2019, 306:1-9
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L-type calcium channel blocker
Amlodipine是一种L型钙通道阻滞剂，具有降压作用。它抑制去极化大鼠主动脉中Ca2 +诱导的收缩（IC50 = 1.9 nM），并在心血管疾病中显示出血管保护作用。
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