Others

Tofenacin (free base) is an antidepressant drug with a tricyclic-like structure. It acts as a serotonin-norepinephrine reuptake inhibitor, and based on its close relation to orphenadrine, may also possess anticholinergic and antihistamine properties. Tofenacin is also the major active metabolite of orphenadrine and likely plays a role in its beneficial effects against depressive symptoms seen in Parkinson's disease patients.

Infigratinib monohydrate, also known as, BGJ398 monohydrate or NVP-BGJ398 monohydrate, is a pan FGFR kinase inhibitor, and is an orally bioavailable pan inhibitor of human fibroblast growth factor receptors (FGFRs) with potential antiangiogenic and antineoplastic activities. pan FGFR kinase inhibitor BGJ398 selectively binds to and inhibits the activities of FGFRs, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. Infigratinib monohydrate was approved in 2021 to treat adults with cholangiocarcinoma whose disease meets certain criteria.

GR-92549 is an HMG-CoA reductase inhibitor.

BMS-870145 is a potent and selective P2Y1 purinergic receptor antagonist..

BW 737C89 is a highly potent dopamine D1 receptor antagonist; BW-737C is the (S)-isomer; BW-736C is the (R)-isomer.

FE-200041 is a peripheral efficacious kappa opioid agonist.

SC 53228 is a specific leukotriene B4 receptor antagonist.

8-Acetyl-2-(dipropylamino)tetralin is a 5-HT(1A) receptor agonist; both isomers are active, but the (S)-isomer is the most potent.

DB1255 is a ERG/DNA binding inhibitor which targets the DNA-binding activity of the human ERG transcription factor.

Antitumor agent-47 是一种具有抗肿瘤活性的水飞蓟宾衍生物。Antitumor agent-47 对 NCI-H1299 和 HT29 细胞具有细胞毒活性，IC50值分别为 8.07 µM 和 6.27 µM。

Cgs 25015 inhibits endothelin-converting enzyme.

Orf 17578 is a histamine H2-receptor antagonist.

SC 23133 is an antimineralocorticoid that is known to induce a marked but reversible inhibition of aldosterone biosynthesis.

Asoxime dimethanesulfonate is an oxime reactivator used for counteracting intoxication by nerve agents. It is able to reactivate acetylcholinesterase (AChE) inhibited by cytotoxic nerve agents such as sarin or soman.

Deptropine citrate is a well-known H1-histamine receptor antagonist and muscarinic receptor antagonist. It is prescribed frequently for treatment of asthma. Recently deptropine has garnered interest as a potential treatment for breast cancer. In vitro studies have shown deptropine citrate has inhibitory effects on cell viability and mammosphere formation in Breast Cancer Stem Cells (BCSCs). However, it does not seem to inhibit the self-renewal capacity of the breast cancer cell line MDA-MB-231 when it is enriched with Cancer Stem Cells.

(R)-Duloxetine Hydrochloride is a napthalenyloxy-substituted amine used in binding studies of human serum albumin along with (S)-Duloxetine. Unlike its enantiomer, it is not a very effective dual serotonin and norepinephrine reuptake inhibitor (SNRI).

OBBA is a phospholipase A2 antagonist.

GMC-1111 free base is a dopamine partial agonist and stabilizer.

AGN-190121 is a retinoic acid receptor (RAR) agonist. RAR and Retinoid X Receptor (RXR) ligands can act synergistically to induce hypertriglyceridemia through distinct mechanisms of action.

Nevirapine quinone methide is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection and AIDS.

CEP-14083 is a potent ALK inhibitor that has shown activity in an NPM/ALK–carrying T-cell lymphoma in vitro study. Presumably, this compound binds to the hinge region of the kinase in an ATP-competitive manner. CEP-14083 displays a potent activity against ALK in enzymatic assays (IC50 = 11 nmol/L). Further, CEP-14083 is also able to inhibit the insulin receptor at a concentration within a nanomolar range. In a preclinical assay, CEP-14083 showed that, via NPM/ALK TK inhibition, it could control the expression of molecules that determine T-cell identity and signaling in lymphoma cells. CEP-14083 has shown preclinical activity in both cell lines and animal models harboring ALK alteration.

(+)-JQ-1 carboxylic acid is a potent bromodomain and extra terminal domain (BET) inhibitor. (+)-JQ-1 carboxylic has potential to be used as a precursor to synthesize PROTACs and other conjugates.

HR68是一种抗癌化合物，是过氧化物酶体增殖物激活受体（PPAR）激动剂非诺贝酯的衍生物。它能降低LN-229胶质母细胞瘤细胞的存活率（IC50 = 1.17 µM）。HR68能够穿越血脑屏障，在对替莫唑胺耐药的原位患者衍生的异种移植（PDX）小鼠胶质母细胞瘤模型中发挥作用。

DW532 is one of simplified analogues of hematoxylin that has shown broad-spectrum inhibition on tyrosine kinases and in vitro anti-cancer activities. DW532 inhibited EGFR and VEGFR2 in vitro kinase activity (the IC50 values were 4.9 and 5.5 μmol/L, respectively), and suppressed their downstream signaling. DW532 dose-dependently inhibited tubulin polymerization via direct binding to tubulin, thus disrupting the mitotic spindle assembly and leading to abnormal cell division. In a panel of human cancer cells, DW532 (1 and 10 μmol/L) induced G2/M phase arrest and cell apoptosis, which subsequently resulted in cytotoxicity. Knockdown of BubR1 or Mps1, the two core proteins of the spindle assembly checkpoint dramatically decreased DW532-induced cell cycle arrest in MDA-MB-468 cells. Moreover, treatment with DW532 potently and dose-dependently suppressed angiogenesis in vitro and in vivo. ( Acta Pharmacol Sin. 2014 Jul;35(7):916-28.)

AGN-204396 is an antagonist that selectively blocks the activity of prostamides (prostaglandin-ethanolamides).

CCG-203586 is a novel potent glucosylceramide synthase (GCS) inhibitor.

FI-700 is a novel and potent FLT3 inhibitor with promising antileukemia activity. FI-700 showed a potent IC(50) value against FLT3 kinase at 20 nmol/L in an in vitro kinase assay. FI-700 showed selective growth inhibition against mutant FLT3-expressing leukemia cell lines and primary acute myeloid leukemia cells, whereas it did not affect the FLT3 ligand (FL)-driven growth of Wt-FLT3-expressing cells. Oral administration of FI-700 induced the regression of tumors in a s.c. tumor xenograft model and increased the survival of mice in an i.v. transplanted model. Furthermore, FI-700 treatment eradicated FLT3/ITD-expressing leukemia cells, both in the peripheral blood and in the bone marrow. (Source: Clin Cancer Res. 2007 Aug 1;13(15 Pt 1):4575-82.)

Scopadulciol is and enzyme and proton pump inhibitor.

Erlosiban, also known as OBE001, is a novel, orally active nonpeptide oxytocin receptor antagonist under development for the treatment of preterm labor and improvement in embryo implantation and pregnancy rate in assisted reproductive technology (ART).

(S)-(–)-Deoxyarbutin是deoxyarbutin的异构体，具有酪氨酸酶抑制作用，在74 µM的浓度下可抑制酪氨酸酶活性。

DJT06001 is a selective Factor Xa inhibitor, reducing thrombus formation with low risk of bleeding.

Vincapusine is a natural inhibitor of 3C-like protease (3CLpro), targeting SARS-CoV-2 3CLpro, SARS-CoV 3CLpro and MERS-CoV 3CLpro.

Amsacrine Isothionate is an aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S/G2 phase of the cell cycle, and cell death.

L6H9 is a novel inhibitor of myeloid differentiation factor 2 (MD2), suppressing HG-induced expression of ACE and AT1 receptor and Angiotensin II (AngII) production in renal NRK‐52E cells, resulting in the decrease in fibrosis markers such as TGF-β and collagen IV.

ddTTP 是一类双脱氧核糖核苷酸 (ddNTPs)，可作为 DNA 聚合酶链延长抑制剂用于 DNA 测序。

alpha-Clopenthixol dihydrochloride is a thioxanthene with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors.