picomolar

Capmatinib 2HCl (INC-280 2HCl) 是一种新型的 ATP 竞争性 c-MET 激酶抑制剂，IC50 为 0.13 nM。它具有皮摩尔酶效，对 c-MET 具有高度特异性，选择性超过 10, 000 倍一大组人类激酶。该抑制剂在 c-MET 依赖性肿瘤细胞系中有效阻断 c-MET 磷酸化和其关键下游效应子的激活。因此，它在体外有效抑制 c-MET 依赖性肿瘤细胞增殖和迁移，并有效诱导细胞凋亡。

A-1155463是一种高效选择性的BCL-XL 抑制剂，对 BCL-XL 具有皮摩尔的结合亲和力，在Molt-4细胞中的EC50值为70 nM。

GNE-987 is a highly active chimeric BET degrader. GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50: 4.7 and 4.4 nM, respectively). GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50: 0.03

ITI-214 free base is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).

ITI-214 是一种中枢神经系统活性抑制剂，具有口服生物活性的PDE1抑制剂 (Kiof 58 pM)，对其他 PDE 家族成员和一系列酶、受体、转运体和离子通道具有良好的选择性，在各种运动和认知功能的动物模型中显示出有效性。

RP-001 is a selective agonist of picomolar short-acting S1P1 (EDG1)(EC50 of 9 pM), has little activity on S1P2-S1P4 and only moderate affinity for S1P5.

RP-001 hydrochloride is a selective agonist of picomolar short-acting S1P1 (EDG1)(EC50 of 9 pM), has little activity on S1P2-S1P4 and only moderate affinity for S1P5.

ELQ316是一种抗寄生虫化合物。在急性和潜伏性弓形虫病的小鼠模型中，ELQ-316显示出高效的功效，并且其体外IC50值处于皮克摩尔级别。

Simufilamum（亦称PTI-125）是一种针对改变构型的filamin A的小分子口服化合物候选物。它可以结合并逆转阿尔茨海默症大脑中的支架蛋白filamin A的改变构型，从而减缓阿尔茨海默症的病理发展。此外，PTI-125还能降低tau蛋白的超磷酸化、减少Aβ42的聚集沉积、神经纤维缠结和神经炎症。该化合物在体外实验中显示，对照组和阿尔茨海默病（AD）患者死后的海马切片具有浓度依赖性的效力，起始浓度为1 picomolar（pM）。PTI-125是首个优先结合并逆转蛋白病变改变构型的治疗候选物。

Lenacapavir，又名GS-6207，是一种HIV-1 capsid抑制剂。其对23种来自不同亚型的HIV-1临床分离株表现出平均EC50为50 pM (20-160 pM)，这些测试是在周围血单核细胞（PBMCs）中进行的。Lenacapavir在体外显示出皮克摩尔级的有效性，且对现有抗逆转录病毒类化合物没有交叉抗性。此外，在HIV-1感染者中，Lenacapavir展现出强大的抗病毒活性，无论治疗历史如何，都没有发现对Lenacapavir的预存在抗性。

DH376 inhibits DAGLα in a time and dose dependent manner in mouse brain. DH376 shows picomolar activity.

BMS-639623 is a CCR3 antagonist with a picomolar inhibitory effect on eosinophilic chemotaxis and can be used in the treatment of asthma.

PB1 is a highly-effective intracellular disulfide reducing agent with notable attributes such as excellent cell permeability, the capacity to generate a substantial intracellular concentration gradient, and remarkable stability. It serves as a borane-protected TCEP (tris(2-carboxyethyl)phosphine) analogue. PB1 demonstrates the potential to enhance the survival of retinal ganglion cells following axotomy in vitro at concentrations in the nanomolar and picomolar range. Consequently, PB1 has proven instrumental in the study of neuroprotective properties[1][2][3].

PB2, a tris(2-carboxyethyl)phosphine (TCEP) analogue, enhances the survival of retinal ganglion cells (RGCs) following axotomy in vitro. Even at nanomolar and picomolar concentrations, PB2 demonstrates pronounced efficacy in promoting RGC survival. Notably, PB2 exhibits superior permeability compared to TCEP. Serving as a potent reducing agent, PB2 provides robust neuroprotection for RGCs[1].

Gnidimacrin activated HIV-1 replication and killed persistently-infected cells at picomolar concentrations. In addition to its potential to purge HIV-1 from latently infected cells, gnidimacrin potently inhibited a panel of HIV-1 R5 virus infection of peripheral blood mononuclear cells (PBMCs) at an average concentration lower than 10 pM. These results suggest that gnidimacrin could activate latent HIV-1, specifically kill HIV-1 persistently infected cells, and inhibit R5 viruses at picomolar concentrations

PSB-1901 is a potent A2B Adenosine Receptor Antagonist with Picomolar Potency (Ki 0.0835 nM, KB 0.0598 nM, human A2BAR) with >10 000-fold selectivity versus all other AR subtypes. PSB-1901 was similarly potent and selective at the mouse A2BAR, making it a promising tool for preclinical studies.

RK-52 is a synthetic inhibitor of rhodesain, characterized by an impressive ksecond value (ksecond = 67000 × 103 M−1 min−1) and by a picomolar affinity toward the trypanosomal protease (Ki = 38 pM).

(S)-Mosnodenvir是一种泛血清型登革热抗病毒药物，表现出较高的耐药性屏障，同时安全性和耐受性均优良。它通过阻断NS3-NS4B相互作用来抑制病毒复制复合体。在小鼠模型中，(S)-Mosnodenvir展示了从皮摩尔到低纳摩尔量级的体外抗病毒效能。

Brolucizumab（DLX1008）是一种具有高亲和力（KD=1.05 pM）的单链抗VEGF-A抗体片段，适用于癌症研究。

Trabikibart（CSL311）为βc特异性的全人源单克隆抗体，专一性结合人βc受体的细胞因子结合位点表位，并展现高皮摩尔级别的结合亲和力。此抗体能有效抑制IL-3、GM-CSF和IL-5在嗜酸性粒细胞存活中的协同作用，显示出治疗慢性炎症性疾病的应用潜力。

ASN 07115873为具有显著抗ZIKV活性的化合物，其半抑制浓度（IC50）为189.2 pM，适用于抗病毒研究领域。

ML2006a4 是一种口服活性 SARS-CoV-2 主要蛋白酶 (Mpro) 抑制剂，具有纳摩尔级的 IC50 值。ML2006a4 具备细胞渗透性和抗病毒活性，可在纳摩尔水平下抑制 Huh7.5.1-ACE2-TMPRSS2 (Huh7.5.1++) 细胞中的 SARS-CoV-2 复制。

Streptavidin（链霉亲和素）是从细菌中纯化出来的蛋白四聚体，对生物素具有非常高的亲和力，常用于纯化或检测各种生物分子。具有免疫活性，可抑制T细胞的IL-2 合成和 CD25 表达。

Melanocortin (MC) 3-MSH (Melanocyte-Stimulating Hormone) is believed to signal through the MC 3 receptor. It induces a sustained increase in intracellular free calcium levels ([Ca2+]i) in a subpopulation of pituitary cells. Most of the cells responding to