at-101

Gossypol acetic acid (AT101) 是一种从棉籽中分离出来的多酚天然产物，分别与 Bcl-xL 蛋白和 Bcl-2蛋白结合，Ki 值分别为 0.5-0.6 μM 和 0.2-0.3 mM。

(R)-(-)-Gossypol acetic acid (AT101 acetate) 是天然产物 Gossypol 的左旋异构体，与 Bcl-2、Bcl-xL 和 Mcl-1 结合，Ki 为 0.32 μM、0.48 μM 和 0.18 μM。

AT-1015 hydrochloride monohydrate is a serotonin (5-HT)2 receptor antagonist that blocks vascular and platelet 5-HT2A receptors.

AT-1015 free base is a serotonin (5-HT)2 receptor antagonist that blocks vascular and platelet 5-HT2A receptors.

AV-101 (4-Cl-KYN) 是 NMDA 受体甘氨酸位点的前药拮抗剂，具有抗抑郁活性，可减少 MPTP 猴子中左旋多巴诱导的运动障碍。

PF8380 是有效的autotaxin 抑制剂，在体外酶实验和人类全血细胞实验中的IC50分别为 2.8 nM 和 101 nM。

RB 101 suppresses enkephalinase and aminopeptidases; biologically cleaved at disulfide to produce inhibitors of both aminopeptidase N and neutral endopeptidase.

PKUMDL-LC-101-D04是一种高效的谷胱甘肽过氧化物酶4（GPX4）的异位激活剂，是一种铁死亡的调节剂。 当在无细胞试验中使用浓度为20 μM 时，GPX4活性增加到对照水平的150%；在野生型而非Gpx4- -小鼠胚胎成纤维细胞(MEF)提取物中使用浓度为61 μM 时，GPX4活性增加到对照水平的150%。PKUMDL-LC-101-D04（200 μM）能减少胆固醇过氧化氢诱导的MEF 死亡。

Ro 04-5595 is a selective antagonist of NMDA receptors NR2B subunits. Ro 04-5595 had an EC 50 of 186 ± 32 nmol L. Ro 04-5595 was predicted to bind the EVT-101 binding site, not the ifenprodil-binding site. Specific binding, defined with a new NR2B-specific antagonist Ro 04-5595 at 10 microM was fully inhibited by several compounds with the following rank order of affinities--Ro 25-6981 > CP-101,606 > Ro 04-5595 = ifenprodil >> eliprodil > haloperidol > spermine > spermidine > MgCl2 > CaCl2--and partially inhibited by competitive glutamate recognition site antagonists. Complementary high-resolution autoradiographic images using [3H]Ro04-5595 demonstrated strong binding in NR2B receptor-rich regions and low binding in cerebellum where NR2B concentration is low.

EVT-101 is a GluN2B antagonist, binding at the same GluN1 GluN2B dimer interface as ifenprodil but adopting a remarkably different binding mode involving a distinct subcavity and receptor interactions.

Kynurenic acid, an active metabolite of tryptophan, is synthesized through a kynurenine intermediate by kynurenine aminotransferases (KATs). It acts as an antagonist of both NMDA and AMPA receptors, as well as α7 nicotinic acetylcholine receptors (nAChRs; EC50s = 235, 101, and 7 µM, respectively), and functions as an agonist for the aryl hydrocarbon receptor (AhR) and G protein-coupled receptor 35 (GPR35; EC50s = 1.4 and 39 µM, respectively). In a neonatal rat model of cerebral hypoxic-ischemia, induced by carotid artery ligation, administration of kynurenic acid at 300 mg kg prevents weight loss in the lesioned hemisphere. Additionally, at concentrations of 1 and 5 mg ml, it protects against neurodegeneration in the rhabdomere of the eye in an Htt93QtransgenicDrosophila model of Huntington's disease. Elevated levels of kynurenic acid in the cerebrospinal fluid have been observed in patients with schizophrenia.