slow-binding

LDN-27219 是一种人组织型转谷氨酰胺酶抑制剂(IC50:600 nM)。

SID 26681509 是可逆的，竞争性的人组织蛋白酶 L 选择性抑制剂，IC50为 56 nM。它抑制Plasmodium falciparum 的体外繁殖，IC50为15.4 μM，抑制Leishmania major，IC5012.5 μM。

AACOCF3（Arachidonyl trifluoromethyl ketone）是一种细胞可渗透的三氟甲基酮类花生四烯酸模拟物。它是一个强效且选择性的85-kDa胞质型磷脂酶A2（cPLA2）缓慢结合抑制剂。通过阻止钙离子载体挑战的血小板中花生四烯酸和12-羟基二十四碳五烯酸的生成，AACOCF3抑制了它们的合成。此外，AACOCF3还能抑制从分离的大鼠岛细胞中诱导的葡萄糖引起的胰岛素释放。鉴于其多样的应用，AACOCF3对心血管疾病研究具有潜在的应用价值。

EMD57033是一种心脏肌钙蛋白C（cTnC）激活剂，是一种显性的Ca2+增敏剂。EMD57033通过与心脏 慢速骨骼肌钙蛋白C 异构体结合从而发挥促进心脏收缩的功能。

FK706 is a slow-binding and competitive human neutrophil elastase inhibitor (IC50: 83 nM; Ki: 4.2 nM). FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase (IC50s: 22 nM and 100 nM, respectively). FK706 has an anti-inflammatory ef

DSPE-PEG(2000)-biotin 是一种对1,2-二硬脂酰-sn-甘油-3-PE进行PEG化和生物素化处理的化合物。它被广泛应用于体外和体内的脂质体输送、荧光标记纳米结构脂质载体（NLCs）的开发。此外，DSPE-PEG(2000)-biotin 也用于生成胶束，用作固定脂质体的前体，并被应用于生物层干涉测量结合实验中。当含有DSPE-PEG(2000)-biotin的脂质体内封装有多柔比星和槲皮素时，能对体外的MCF-7 adr多药耐药乳腺癌细胞产生细胞毒作用，并有效抑制MCF-7 adr小鼠移植瘤模型中的肿瘤增长。通过使用生物素偶联的FITC标记的avidin，已成功在NLCs中实现荧光标记。

L 708286 is an agent of peptide-based phenethylcarbamoyldifluoromethylene. It is a slow-binding inhibitor of human leucocyte elastase (HLE).

ONO-0300302 is a slow tight binding LPA1 antagonist (IC50: 0.16 nM) used to treat Benign Prostatic Hyperplasia. ONO-0300302 inhibits significantly an LPA-induced increase of intraurethral pressure (IUP) in rat (3 mg kg, p.o.) and dog (1 mg kg, p.o.) over

SL-25.1188 is a monoamine oxidase B (MAO-B) inhibitor. SL-25.1188 is characterized by reversible binding, high brain uptake, and very slow plasma metabolism in vivo.

UR-2922 is an oral antagonist of platelet GPIIb IIIa. UR-2922 possessed a high affinity for the human platelet receptor (K(d) <1 nM) and a slow dissociation rate (k(off)= 90 min) in vitro. UR-2922 induced no ligand-induced binding sites (LIBS) expression

Pimelic diphenylamide 106 (RGFA-8) 是一种缓慢和紧密结合的I 类HDAC 抑制剂，对HDAC1、 2和3的IC50值分别150、760和370 nM。

11-trans Leukotriene C4 (11-trans LTC4) is a C-11 double bond isomer of LTC4. LTC4 undergoes slow temperature-dependent isomerization to 11-trans LTC4 during storage. 11-trans LTC4 is produced in smaller amounts relative to LTC4 in ionophore-stimulated HMC-1 cells (a human mast cell line) and equine eosinophils, but not in human neutrophils or RBL-1 cells. It is nearly equipotent with LTC4 for contraction of guinea pig parenchymal and ileum. In a radioligand binding assay using guinea pig ileum as a cysteinyl leukotriene receptor preparation, the pKis for LTC4 and 11-trans LTC4 were determined to be 6.42 and 6.58, respectively.

Ara-F-NAD+, an arabino analogue of NAD + , is a potent, slow-binding CD38 NADase inhibitor, with a K i of 169 nM.

UCB-5307 是一种小分子化合物，可在体外抑制 TNFR1 信号转导和下游功能。 人 TNFα 的 KD 为 9 nM。 TNF 直接通过缓慢的结合动力学结合，KD = 6 nM。 UCB-5307 可以通过预制的 hTNF hTNFR1 复合物。

Tiotropium Bromide hydrate (BA-679 BR hydrate) 是长效的毒蕈碱受体拮抗剂，可用于治疗慢性阻塞性气道疾病 (COPD)。

RO-5328673 is a dual NK2 NK3 antagonist. O5328673. [(3)H]RO5328673 bound to a single saturable site on hNK2, hNK3 and gpNK3 with high-affinity. RO5328673 acted as an insurmountable antagonist at both human and guinea-pig NK3 receptors in the [(3)H]IP accumulation assay. In binding kinetic analyses, [(3)H]RO5328673 had fast association and dissociation rates at hNK2 while it had a fast association rate and a remarkably slow dissociation rate at gp and hNK3. In electrophysiological recordings of gp SNpc, RO5328673 inhibited the senktide-induced potentiation of spontaneous activity of dopaminergic neurons with an insurmountable mechanism of action. RO5328673 exhibited in-vivo activity in gerbils, robustly reversing the senktide-induced locomotor activity.

Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L. In the cathepsin L inhibition assay, The oxocarbazate caused a time-dependent 17-fold drop in IC50 from 6.9 nM (no preincubation) to 0.4 nM (4-h preincubation). Slowly reversible inhibition was demonstrated in a dilution assay. CID23631927 demonstrate activity in blocking both SARS-CoV (IC50 = 273 nM) and Ebola virus (IC50 = 193 nM) entry into human embryonic. CID 23631927 was a subnanomolar, slow-binding, reversible inhibitor of human cathepsin L that blocked SARS-CoV and Ebola pseudotype virus entry in human cells. Inhibition of cathepsin L thus holds promise for therapeutic intervention for both SARS-CoV and Ebola virus infection.

Ara-F-NAD+ sodium 是一种 NAD+的 arabino 类似物。Ara-F-NAD+ sodium 是一种有效的、可逆的、缓慢结合的CD38NADase 抑制剂。

1400W is a slow, tight-binding, and highly selective inducible nitric-oxide synthase (iNOS) inhibitor, with a K_d value ≤ 7 nM. 1400W inhibits iNOS induction in microglial cells and reduces the generation of NO, thereby mitigating oxidative stress and neuronal cell apoptosis in the rat cerebral cortex, and improving spatial memory dysfunction caused by acute hypobaric hypoxia-reoxygenation [1] [2].

HDAC6-IN-33 (compound 6) 作为一种选择性且不可逆的HDAC6抑制剂，展现出了 193 nM 的 IC50 值。该化合物对 HDAC1-4 未显示出活性。通过两步缓慢结合机制，HDAC6-IN-33 有效地抑制 HDAC6，属于紧密结合型抑制剂。

ITF5924 (compound 1) 是一种高效且极具选择性的HDAC6抑制剂，IC50为7.7 nM，对其他HDAC亚型的选择性超过104倍。ITF5924 含有二氟甲基-1,3,4-恶二唑 (DFMO) 结构，作为HDAC6缓慢结合的底物类似物，通过酶催化开环反应形成紧密且持久的酶抑制剂复合物。

MAO-A B-IN-3（Compound 12）在体外实验条件下，表现出对Caco2和MDCK细胞中等的穿透能力，其穿透性分别为16.49 nm s和103.16 nm s。此外，MAO-A B-IN-3 在血浆蛋白结合实验中显示出90.97%的高结合率，这一数值大于90%，暗示该化合物在体内可能具有较长的半衰期及缓慢的排泄速率。

Broussonin C and broussin are antifungal compounds. Broussonin C exerts simple reversible slow-binding inhibition against diphenolase.