at 1001

GL-1001 disodium tetrahydrate is an ACE2 inhibitor.

Kahweol oleate is emi-syntetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1 induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.

AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal preparation, AT-1001 inhibits nicotine-induced [³H]dopamine release poorly and at significantly higher concentrations compared with mecamylamine and conotoxin MII.

3-Aminobenzamide (PARP-IN-1) 是一种有效的 PARP 抑制剂，在 CHO 细胞中，对 PARP 的 IC50值约为 50 nM。它是再灌注过程中氧化剂诱导的肌细胞功能障碍的介质。

ORY1001 (ORY 1001) 是一种具有口服活性的选择性赖氨酸特异性去甲基化酶 LSD1 KDM1A 抑制剂，对相关的 FAD 依赖性氨氧化酶具有高选择性，IC50 <20 nM。

BMS-1001 是一种有效的 PD-1 PD-L1 相互作用抑制剂（IC50：2.25 nM，在均相时间分辨荧光结合试验中）。

ORY-1001 is a KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A B, IL4I1, KDM1B >100uM, SMOX 7uM). Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time dose dependent me2H3K4 accumulation a

F594-1001 (compound 6) 作为一种强效且高选择性的SARS-CoV-2 Mac1-ADP-核糖抑制剂，其在 AS、FP 及 FRET 测试中显示出对 SARS-CoV-2 的杰出抑制效果，IC50 值分别为 8.5 μM、68 μM 和 45 μM。此化合物能够直接与 SARS-CoV-2 Mac1 结合，并以剂量依赖的方式抑制 Mac1 ADP-核糖基水解酶的活性。

JAMI1001A is a positive allosteric modulator of the AMPA receptor, effectively modulating the deactivation and desensitization of both flip and flop receptor isoforms.

DPM-1001 is an orally bioavailable and non-competitive protein-tyrosine phosphatase (PTP1B) inhibitor (IC50: 100 nM) with the anti-diabetic property.

(S)-BI-1001 is an active S-enantiomer of BI-1001. (S)-BI-1001 has antiviral potency against HIV-1 integrase (IC50: 28 nM, and EC50: 450 nM and a Kd: 4.7 μM).

KTX-1001，亦称为NSD2 inhibitor 161，是一种新型且有效的核SET结构域含蛋白2（NSD2）抑制剂。该化合物专一性地结合NSD2，抑制其催化活性以及组蛋白H3赖氨酸36（H3K36）的单和双甲基化作用。此作用调控涉及细胞过程的基因表达，包括细胞增殖，进而可能导致癌细胞生长减缓。NSD2是NSD家族组蛋白赖氨酸甲基转移酶中的一员，该酶类在许多癌症类型中表达过量且调控失常。

ATM-1001 is an inhibitor of the cancer-associated tropomyosin 3.1 (Tpm3.1), suppressing glucose-stimulated insulin secretion (GSIS) from the pancreatic islets.

T1001 is an antagonist of hypoxia-inducible factor-2α subunit (HIF-2α) which displaces residue M252 from inside the HIF-2α PAS-B pocket toward the ARNT subunit to weaken heterodimerization.

INO-1001 是一种有效的、选择性聚 (ADP-核糖) 聚合酶 (PARP) 抑制剂，具有抗肿瘤活性。INO-1001 是一种有效的辐射敏感性增强剂，能够利用干扰 DNA 修复机制，进而提高辐射诱导的细胞杀伤，使坏死细胞死亡。

SR1001 是选择性RORα及RORγt 的反向激动剂，其Ki 分别为 172 和 111 nM。

GL-1001 sodium salt is an ACE2 inhibitor.

DS-1001b 是IDH-1(异柠檬酸脱氢酶-1) 突变体抑制剂。

pJAK2(1001–1013) 是一种 SOCS1 3 拮抗剂，通过抑制 SOCS 蛋白的负调控作用，增强 JAK STAT 信号传导，从而在抗病毒免疫反应中起积极作用。

INO-1001 methanesulfonate is an isoindolinone derivative and potent inhibitor of the nuclear enzyme poly (ADP-ribose) polymerase (PARP) with chemosensitization and radiosensitization properties.

DPM-1001 trihydrochloride 是一种有效的，特异性的，具有口服活性的，且非竞争性的蛋白酪氨酸磷酸酶 (PTP1B) 抑制剂，其 IC50为 100 nM。DPM-1001 trihydrochloride 是特异性 PTP1B 抑制剂 MSI-1436 (IC50=600 nM) 的类似物。DPM-1001 trihydrochloride 具有抗糖尿病特性。

Iadademstat dihydrochloride (ORY-1001(trans)) 是一种不可逆的选择性赖氨酸特异性脱甲基酶 1A(KDM1A LSD1) 抑制剂，用于治疗急性白血病。

BMS-1001 hydrochloride 是一种人 PD-L1 PD-1免疫检查点的抑制剂，具有口服活性且细胞毒性低。

M1001 是较弱的HIF-2α激动剂，直接与 HIF-2α PAS-B 结构域结合，Kd=667 nM，能够提高 HIF-2α-ARNT 复合体之间的稳定性。