ttr

TTR stabilizer 1 (compound 1) 作为一种甲状腺素运载蛋白 (TTR) 的稳定剂，展现出了0.031 μM的EC50值。

WT-TTR inhibitor 1 (Compound 21)作为一种野生型转甲状腺素(WT-TTR)的抑制剂，其在100 μM浓度下的抑制率达到29.05%。

Dichlorophenyl-ABA is a transthyretin (TTR) amyloid fibril formation inhibitor. It inhibits aggregate formation in more than 80% in TTR L55P-expressing cells.

L6Y is a transthyretin (TTR) stabilizer which binds to the T4 binding pocket of TTR and prevents the dissociation of TTR to monomer.

Soulattrolide是一种由Calophyllum (Calophyllaceae)雨林树叶合成的天然香豆素，作为HIV-1逆转录酶（RT-HIV-1）的强效抑制剂，并显示出对Mycobacterium tuberculosis的活性。

DefNEtTrp 是一种由 Def 和 Trp 两个基团组成的铁双螯合配体。在癌细胞系中，DefNEtTrp 展示了广谱有效的抗增殖和细胞死亡活性。该化合物能够诱导细胞凋亡(apoptosis)和铁死亡(ferroptosis)，具有显著的细胞毒性，IC50 值为 0.77 μM。

Burnettramic acid A is a fungal metabolite originally isolated fromA. burnettiithat has diverse biological activities.1It is active againstB. subtilis,S. aureus,C. albicans, andS. cerevisiae(IC50s = 2.3, 5.9, 0.5, and 0.2 μg ml, respectively). Burnettramic acid A is cytotoxic to NS-1 murine myeloma cells but not neonatal foreskin fibroblasts (IC50s = 13.8 and >100 μg ml, respectively). 1.Li, H., Gilchrist, C.L.M., Lacey, H.J., et al.Discovery and heterologous biosynthesis of the burnettramic acids: Rare PKS-NRPS-derived bolaamphiphilic pyrrolizidinediones from an Australian fungus, Aspergillus burnettiiOrg. Lett.21(5)1287-1291(2019)

Burnettramic acid A aglycone is a fungal metabolite and an aglycone form of burnettramic acid A originally isolated fromA. burnettiithat has anticancer activity.1It is cytotoxic to NS-1 murine myeloma cells but not neonatal foreskin fibroblasts (IC50s = 8.4 and >100 μg ml, respectively). 1.Li, H., Gilchrist, C.L.M., Lacey, H.J., et al.Discovery and heterologous biosynthesis of the burnettramic acids: Rare PKS-NRPS-derived bolaamphiphilic pyrrolizidinediones from an Australian fungus, Aspergillus burnettiiOrg. Lett.21(5)1287-1291(2019)

Bottromycin A2is an antibiotic originally isolated fromStreptomyces.1It blocks the binding of aminoacyl-tRNA to the A site of the 50S ribosome, inhibiting protein synthesis.2Bottromycin A2is active against clinical isolates of methicillin-resistantStaphylococcus aureus(MRSA) and vancomycin-resistantEnterococciwith MIC values of 1 and 0.5 μg ml, respectively. 1.Nakamura, S., Yajima, T., Lin, Y., et al.Isolation and characterization of bottromycins A2, B2, C2J. Antibiot. (Tokyo)20(1)1-5(1967) 2.Gouda, H., Kobayashi, Y., Yamada, T., et al.Three-dimensional solution structure of bottromycin A2: A potent antibiotic active against methicillin-resistant Staphylococcus aureus and vancomycin-resistant EnterococciChem. Pharm. Bull. (Tokyo)60(2)169-171(2012)

BML-284 (Wnt agonist 1) 是细胞通透性 Wnt 信号激活剂，能够诱导 TCF 依赖的转录活性(EC50>700 nM)。

Clovoxamine (DU 23811) 是一种 5-羟色胺再摄取、血清素和去甲肾上腺素抑制剂，具有抗抑郁和抗惊厥活性。

Ziprasidone hydrochloride (CP-88059 hydrochloride) 是一种联合 5-HT（5-羟色胺）和多巴胺受体拮抗剂，具有抗精神病活性的强效作用。它也是去甲肾上腺素再摄取抑制剂。

cis-3-Hexen-1-ol ((Z)-3-Hexen-1-ol) 是发现于许多新鲜水果和蔬菜中的一种绿色草味化合物，常用作加工食品的附加风味剂，以提供新鲜的绿色品质，也是多种昆虫的引诱剂。

Pifithrin-α, p-Nitro, Cyclic (PFN-α) 是 p53 的细胞渗透性和活性形式抑制剂。它对暴露于 Etoposide 的皮层神经元的保护作用比 Pifithrin-α 强一个数量级，ED50为30 nM。它也作为 p53 转录后的活性抑制剂。

NFAT Transcription Factor Regulator-1 是 IL-2 合成 的抑制剂，IC50 值为182 nM。

Carboprost tromethamine 是合成的前列腺素 F2α的15-甲基类似物，能有效促进子宫的规律收缩，显着减少产中及产后出血量。

Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleo

Clesacostat（PF-05221304），是一种高效且选择性的ACC抑制剂（hACC1 IC50 = 13nM；hACC2 IC50 = 9nM）。在动物模型中，PF-05221304特异性抑制肝脏的DNL，同时在非人类灵长类动物模型中展示出对血小板减少具有显著的安全裕度。

Latanoprosttris(triethylsilyl) ether 是 Latanoprost 合成的前体，它是前列腺素 F2α (PGF2α) 受体 (FP受体) 激动剂。

TCS 1102 是双食欲素受体拮抗剂，对 OX1和OX2受体的Ki 分别为3和 0.2 nM。

Neuromedin U-23 (NMU-23) is a neuropeptide involved in diverse biological processes, including smooth muscle contraction, energy homeostasis, and nociception.1It is an agonist of neuromedin-U receptor 1 (NMUR1; EC50= 0.17 nM for the human receptor in a calcium mobilization assay using HEK293 cells) and NMUR2 (EC50= ~1.4-2 nM for arachidonic acid release in CHO cells expressing the human receptor).2,3NMU-23 (1 μM) induces contractions in isolated rat colon smooth muscle strips.4It decreases body weight and food intake and increases core body temperature in mice when administered at a dose of 36 μg/animal.5Intrathecal administration of NMU-23 decreases the mechanical pain threshold in the von Frey test in rats.6 1.Mitchell, J.D., Maguire, J.J., and Davenport, A.P.Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin SBr. J. Pharmacol.158(1)87-103(2009) 2.Szekeres, P.G., Muir, A.I., Spinage, L.D., et al.Neuromedin U is a potent agonist at the orphan G protein-coupled receptor FM3J. Biol. Chem.275(27)20247-20250(2000) 3.Hosoya, M., Moriya, T., Kawamata, Y., et al.Identification and functional characterization of a novel subtype of neuromedin U receptorJ. Biol. Chem.275(38)29528-29532(2000) 4.Brighton, P.J., Wise, A., Dass, N.B., et al.Paradoxical behavior of neuromedin U in isolated smooth muscle cells and intact tissueJ. Pharmacol. Exp. Ther.325(1)154-164(2008) 5.Peier, A., Kosinski, J., Cox-York, K., et al.The antiobesity effects of centrally administered neuromedin U and neuromedin S are mediated predominantly by the neuromedin U receptor 2 (NMUR2)Endocrinology150(7)3101-3109(2009) 6.Yu, X.H., Cao, C.Q., Mennicken, F., et al.Pro-nociceptive effects of neuromedin U in ratNeuroscience120(2)467-474(2003)

Neuropeptide Y (NPY) (3-36) is a C-terminal fragment of NPY, a neuropeptide involved in controlling appetite, blood pressure, cardiac contractility, and intestinal secretion. NPY (3-36) is an endogenous peptide produced by cleavage of NPY by dipeptidyl peptidase 4 (DPP-4). It binds selectively to the NPY receptor Y2 (Ki = 0.41 nM in CHP 234 cells) over the Y1 receptor, where it does not bind at concentrations up to 1 μM. NPY (3-36) (0.1 nM) increases migration of human umbilical vein endothelial cells (HUVECs) by 80% after 12 hours in an in vitro wound closure assay. NPY (3-36) corresponds to residues 3-36 of the human and rat protein sequence.

Cortistatin-29 (1-13) is a neuropeptide and cleavage product of cortistatin-29 , which is a cleavage product of procortistatin. Cortistatin-29 (1-13) corresponds to the first 13 amino acids of cortistatin-29.

GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr- -) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003). GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr- -) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2 References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003).