magnitude

MRS-1706 是一种选择性A2B 腺苷受体的反向激动剂，对人 A2B、A2A、A1和 A3受体的Ki 值分别为 1.39、112、157 和 230 nM。

Venetoclax (ABT-199) 是一种 Bcl-2 抑制剂 (Ki<0.01 nM)，具有高效性、选择性和口服活性。Venetoclax 与 Bcl-xL 和 Bcl-W 的亲和力降低了 3 个数量级（Kis=48 245 nM）。Venetoclax 可以诱导自噬和凋亡。

γ-Hexalactone (γ-caprolactone) 是一种存在成熟水果中的 gamma 内酯。它会导致 DNA 损伤，可用作对氧磷酶 1 的底物 (PON1)。

The endocannabinoids, 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide (AEA), are biologically active lipids that regulate diverse neurological and metabolic functions by activating the cannabinoid receptors, central cannabinoid (CB1) and peripheral cannabinoid (CB2). Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH) hydrolyze 2-AG and AEA, respectively, thus terminating their biological function. IDFP is an organophosphorus compound that dually inhibits MAGL and FAAH with IC50 values of 0.8 and 3 nM, respectively. At 10 mg/kg, IDFP elevates brain levels of 2-AG and AEA more than 10-fold, and decreases levels of arachidonic acid by a similar magnitude.

N-acetyl Leukotriene E4（N-乙酰白三烯 E4）是Leukotriene E4的内源性代谢物，主要通过胆汁排泄，其活性比Leukotriene E4低1~3个数量级，能引起气管的收缩。

Tiliroside (Tribuloside) 是糖苷类黄酮，是 α-淀粉酶的非竞争性抑制剂(Ki:84.2 μM)。它抑制胃肠道中碳水化合物的消化和葡萄糖的吸收，具有抗糖尿病作用。

PBS-1086 is a novel dual inhibitor of the canonical and noncanonical NF-κB pathways, increasing the magnitude and duration of initial EGFR inhibitor response in multiple NSCLC models, decreasing PDHK1 expression, and suppressing phosphorylation of the PDHK1 protein substrate PDHA1 in a panel of PTEN-deficient cell lines.

Covidcil-19 binds to the revised attenuator hairpin structure of the SARS-CoV-2 frameshifting element (FSE) with high affinity (Kd = 11 nM). It stabilizes the hairpin's folded state and reduces frameshifting efficiency in cells. Covidcil-19 inhibits viral propagation and reduces viral infectivity by > 3.5 orders of magnitude.

Cryptophycin analog 1, an ADC payload, exhibits anticancer activity and demonstrates cellular potency an order of magnitude greater than the approved ADC payloads MMAE and DM1 [1].

Selective NaV1.7 channel blocker. Shifts activation gating positively and decreases current magnitude. Displays 100-fold selectivity over other sodium channel subtypes.

Amyloid A proteins (H2N-Ala-Gly-Leu-Pro-Glu-Lys-Tyr-OH) are a family of apolipoproteins associated with high-density lipoprotein in plasma. Different isoforms of SAA are expressed constitutively at different levels or in response to inflammatory stimuli.