tr 1

TR antagonist 1 是一种高效甲状腺激素受体（TR）拮抗剂（对 TRα 和 TRβ 的 IC50 分别为 36 和 22 nM），可用于研究内分泌异常引起的疾病。

TRβ agonist 1 为一种选择性且对突变敏感的甲状腺激素受体 β (TRβ) 激动剂，其EC50值为21 nM。该化合物适用于血脂异常、非酒精性脂肪性肝炎 (NASH) 与甲状腺激素抵抗 (RTH) 研究。

Meclinertant (SR 48692) 是神经降压素受体-1（NT1）拮抗剂，可阻断神经降压素诱导的兴奋，可用于研究神经系统疾病。

7-Amino-4-(trifluoromethyl)coumarin (Coumarin 151) 是一种荧光标记物，其激发和发射波长分别为400和500 nm，可用来灵敏的检测蛋白酶。

TbPTR1 inhibitor 2 被确定为改进的蝶啶还原酶-1 (PTR1) 抑制剂和抗锥虫药物的新发展。

MK 571 (L660711) 是一种具有口服活性的 CysLT1 受体拮抗剂。

Aristolochic acid A (TR 1736) 是植物提取物 Aristolochic acids 的主要成分，主要存在于 Aristolochia 和 Asarum 草本植物中。它降低人细胞中膀胱癌相关BLCAP 基因表达。它显著降低激活蛋白1 (AP-1) 和NF-κB 活性。

YTR107 是一种有效的放射增敏剂,通过与核磷蛋白 1 (NPM1) 结合,抑制其五聚体的形成.该化合物阻止核磷蛋白向 DNA 损伤部位的聚集,从而抑制 DNA 双链断裂修复过程,增强了放射治疗的疗效.

TR-107 (Anticancer agent 230) 是一种具有选择性和高效性的线粒体蛋白酶 ClpP 激活剂，抑制 MDA-MB-231 异种移植模型中的肿瘤生长。

SR-33805 is a calcium channel antagonist potentially for the treatment of atherosclerosis and heart failure. SR-33805 restored the MI-altered cell shortening without affecting the Ca(2+) transient amplitude, suggesting an increase of myofilament Ca(2+) sensitivity in MI myocytes. A SR33805-induced sensitization of myofilament activation was found to be associated with a slight increase in myosin light chain-2 phosphorylation and a more significant decrease on troponin I (TnI) phosphorylation. Decreased TnI phosphorylation was related to inhibition of protein kinase A activity by SR-33805.

TbPTR1 inhibitor 1 (compound 5d) 是有效的动基体蝶啶还原酶 1 (PTR1)抑制剂。TbPTR1 inhibitor 1抑制布氏锥虫 PTR1 (TbPTR1) 的 IC50<0.1 nM，抑制布氏锥虫 (Trypanosoma brucei) 活性的 EC50=0.66 μM。

Nevanimibe hydrochloride (PD-132301 hydrochloride) 是一种口服有效的，选择性酰基辅酶 A：胆固醇 O-酰基转移酶 1 抑制剂，EC50为 9 nM。它抑制 ACAT2，EC50为 368 nM。它诱导细胞凋亡，具有抗肾上腺皮质癌的潜力。

Protectin conjugates in tissue regeneration 1 (PCTR1) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid . DHA is oxidized to 16S,17S-epoxy-protectin, which is then converted to PCTR1 by glutathione S-transferase. PCTR1 levels increase during resolution of acute microbial-induced peritonitis in mice. PCTR1 (30 ng, i.p.) administration 12 hours post-infection increases macrophage numbers and activity and shortens the resolution phase of inflammation by 57%. It also reduces the levels of PGE2 , PGD2 , and TXB2 in peritoneal exudates.

Maresin conjugates in tissue regeneration 1 (MCTR1) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages at the site of inflammation. DHA is oxidized to maresin 1 , which is then converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase. MCTR1 accelerates tissue regeneration in planaria (1 and 100 nM). Pretreatment with MCTR1 (50 ng mouse, i.p.) prior to E. coli administration reduces neutrophil infiltration, shortens the inflammatory resolution period, and increases phagocytosis of E. coli by macrophages. When administered at a dose of 100 ng 12h post E. coli infection in a mouse model of peritonitis, MCTR1 reduces the amount of eicosanoids in the exudate.

Naloxegol (NKTR-118; AZ-13337019) is an opioid-receptor antagonist[1]. [1]. Yoon SC, et al. Naloxegol in opioid-induced constipation: a new paradigm in the treatment of a common problem. Patient Prefer Adherence. 2017 Jul 24;11:1265-1271.

LZTR1-KRAS modulator 1 作为一种KRAS-LZTR1相互作用的调节剂，能够促进LZTR1-KRAS复合物的聚集。

BTR-1 (5-Benzylidene-3-ethyl rhodanine) 是一种活性抗癌剂， 可激活细胞凋亡并诱导细胞死亡。它能够诱导细胞周期 S 期停滞，影响 DNA 复制。

FTR1335 is a CaNMT inhibitor (IC50 = 0.49 nM) with good fungal selectivity. CaNMT inhibitors are fungicidal and show antifungal activity against Candida (especially fluconazole-resistant strains). They function by inhibiting N-myristoyltransferase (NMT), which catalyzes the transfer of a C14 fatty acif from myristoyl-CoA to the N-terminal of glycine in many fungal proteins. Without this process, fungi can die. This process also occurs in humans, and as such selectivity is an important characteristic of these drugs.

DB2313 is a first-in-class potent small-molecule inhibitor of PU.1. DB2313 disrupts the interaction of PU.1 with target gene promoters and leads to down-regulation of canonical PU.1 transcriptional targets.

TR-14035 (MDK-1191) 是一种具有口服活性的 α4β7 α4β1整合素双重抑制剂，对 α4β7和 α4β1作用的 IC50值分别为 7 和 87 nM，可用于炎症和自体免疫疾病的研究。

Resolvin conjugate in tissue regeneration 1 (RCTR1) is a specialized pro-resolving mediator (SPM) biosynthesized from docosahexaenoic acid by isolated human macrophages and apoptotic polymorphonuclear (PMN) neutrophils.1It has been found in human spleen and bone marrow.2RCTR1 is produced via lipoxygenase-mediated oxidation of DHA to 7(S)-8-epoxy-17(S)-HDHA, which is conjugated to glutathione.1,2,3RCTR1 (10 nM) increases phagocytosis ofE. colior apoptotic neutrophils in isolated human monocyte-derived macrophages.2It decreases chemotaxis induced by leukotriene B4in isolated human neutrophils when used at a concentration of 10 nM. RCTR1 (1 and 10 nM) accelerates tissue regeneration in planaria. Intraperitoneal administration of RCTR1 (100 ng/animal) shortens the inflammatory resolution period and decreases inflammatory exudate neutrophil infiltration in a mouse model ofE. coli-induced peritonitis. 1.Dalli, J., Ramon, S., Norris, P.C., et al.Novel proresolving and tissue-regenerative resolvin and protectin sulfido-conjugated pathwaysFASEB J.29(5)2120-2136(2015) 2.de la Rosa, X., Norris, P.C., Chiang, N., et al.Identification and complete stereochemical assignments of the new resolvin conjugates in tissue regeneration in human tissues that stimulate proresolving phagocyte functions and tissue regenerationAm. J. Pathol.188(4)950-966(2018) 3.Rodriguez, A.R., and Spur, B.W.First total synthesis of pro-resolving and tissue-regenerative resolvin sulfido-conjugatesTetrahedron Lett.58(16)1662-1668(2017)

MTR-105 is a nitric oxide synthase inhibitor.

Vadaclidine is an orally acting antinociceptive muscarinic agonist.

GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively).