minimal

Darunavir (TMC114) is an HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.

Norgestimate is an acetylated progestinused in combination with ethinyl estradiol as an oral contraceptive.

JNK-IN-8 (JNK Inhibitor XVI) is an effective JNK inhibitor that inhibits JNK1, JNK2, and JNK3 with IC₅₀ values of 4.7, 18.7, and 1 nM, respectively. JNK-IN-8 offers the advantages of minimal off-target activity, sustained inhibition, and high specificity. JNK-IN-8 primarily acts by blocking the JNK/c-Jun signaling pathway, inhibiting the phosphorylation of the downstream transcription factor c-Jun, thereby regulating the expression of genes associated with inflammatory responses, apoptosis, and stress responses. JNK-IN-8 can be used in research on tumors, inflammation, and neurological diseases.

Tarlatamab (AMG-757) is a bispecific T cell engager (BiTE) antibody targeting DLL3 and CD3, with human DLL3 and CD3 KD = 0.64 nM/14.9 nM, for use in immuno-oncology therapy of small cell lung cancer (SCLC).

TCMDC-135051 is a potent and selective PfCLK3 protein kinase inhibitor demonstrating significant antiparasiticidal activity (EC50=320 nM) while exhibiting minimal off-target toxicity. It effectively hinders the transition from trophozoite to schizont, impairs transcription, and diminishes transmission to the mosquito vector.

PF-06459988 is a novel, effective, orally active, irreversible, and selective epidermal growth factor receptor (EGFR) mutant inhibitor. PF-06459988 has high efficiency and high affinity for EGFRs double mutants containing T790M, and has minimal activity against WT EGFR. PF-06459988 makes a candidate drug for the treatment of cancer.

Vesnarinone (Arkin) (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. It also suppresses cell proliferation and induces apoptosis by inducing the expression of p21, an inhibitor of cyclin-dependent kinase activity in p53-mediated cell cycle arrest.

IMPDH2-IN-2 is a potent inhibitor of inosine 5'-monophosphate dehydrogenase (IMPDH) (Ki,app: 14 μM) and a potential anti-tuberculosis agent, exhibiting moderate antibacterial effects with MIC values of 6.3 and 11 μM in minimal GAST/Fe and rich 7H9/ADC/Tween media, respectively.

Citalopram hydrobromide (XU-62-320) , a selective serotonin reuptake inhibitor (SSRI), selectively inhibits the CNS neuronal reuptake of serotonin, thereby potentiating serotonergic activity in the central nervous system (CNS). Citalopram hydrobromide is the orally bioavailable hydrobromide salt of the racemic bicyclic phthalene derivative citalopram with antidepressant activity. This agent has minimal effects on the CNS neuronal reuptake of norepinephrine (NE) and dopamine (DA).

Pitavastatin calcium (NK-104) is a potent inhibitor of HMG-CoA reductase (Ki: 1.7 nM). It lowers both total cholesterol and low-density lipoprotein cholesterol in animals and humans. Metabolism of pitavastatin by the cytochrome P450 system is minimal, reducing the risk of drug-drug interactions.

Octanoic acid (Caprylic acid), found naturally in coconuts and breast milk, is an oily liquid with a slightly unpleasant rancid taste and minimal solubility in water. It is commercially utilized in the production of esters for perfumery and in dye manufacturing.

Fidaxomicin (Tiacumicin B) is a semisynthetic macrolide antibiotic used to treat Clostridium difficile-associated diarrhea in adults. Fidaxomicin has minimal systemic absorption and has not been linked to serum enzyme elevations during therapy or to instances of clinically apparent, acute liver injury.

Lemuteporfin is a light-activated photosensitizing agent that is rapidly internalized by viable cells, localizing within the cytoplasm and associating with mitochondria. This localization is a key characteristic that confers strong cytotoxic potential upon light activation. Lemuteporfin has demonstrated the ability to reduce sebaceous gland volume in preclinical animal studies. It is currently under investigation in relation to benign prostatic hyperplasia and in topical form for the management of androgenetic alopecia.

BK60106 is a selective inhibitor of the transmembrane protein CD99, which causes cell death in Ewing Sarcoma cells by directly binding to the extracellular structural domain of CD99.

INU-152 is a pan-RAF inhibitor. INU-152 has potent anti-tumor activity in preclinical models of BRAFV600E mutant cancer. INU-152 inhibits all RAF isoforms and inhibits MAPK pathways in mutant BRAF cells. INU-152 exhibits minimal paradoxical pathway activa

OPN-9652 is a potent and orally active covalent TEAD inhibitor, with a half-maximal inhibitory concentration (IC50) of 0.005 µM against TEAD in MSTO-211H cells, and it targets the central palmitate-binding pocket of TEAD. OPN-9652 can significantly reduce the activity of TEAD-dependent reporter genes and downregulate the expression levels of TEAD target genes (CTGF and CYR61). Notably, OPN-9652 can reverse the resistance of SOX10 knockout (SOX10 KO) resistant cells to the combination of BRAF inhibitor (BRAFi) and MAPK inhibitor (MAPKi), restoring their sensitivity to the drugs. In the xenograft mouse model of BRAF-mutant A375 cells, OPN-9652 can effectively delay the development of tumor drug resistance; specifically, this effect is manifested by a significant delay in the onset of tumor drug resistance after the combination of BRAFi and MEK inhibitor (MEKi) starting from the minimal residual disease (MRD) stage. At present, OPN-9652 can be used as a research tool for scientific research related to melanoma.

Cetirizine is a second-generation selective H1-histamine receptor antagonist with antiallergic effects that inhibits eosinophil chemotaxis during allergic reactions. Cetirizine has minimal central nervous system depressant effects.

EP4 Receptor Antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist, effective for cancer immunotherapy. It inhibits both human and mouse EP4 receptors with IC50 values of 6.1 nM and 16.2 nM, respectively, while displaying minimal activity (IC50s >10 μM) against human EP1, EP2, and EP3 receptors.

GGTI298, a CAAZ peptidomimetic and potent geranylgeranyltransferase I (GGTase I) inhibitor, efficiently blocks the processing of geranylgeranylated Rap1A while exerting minimal impact on the processing of farnesylated Ha-Ras. The inhibitor displays in vivo IC50 values of 3 μM for Rap1A and >20 μM for Ha-Ras, respectively.

GSK1059865 is a highly selective orexin-1 receptor antagonist that significantly reduces voluntary ethanol intake in ethanol-dependent mice following chronic intermittent ethanol exposure, producing dose-dependent suppression of alcohol consumption without affecting sucrose intake, while exhibiting minimal effects in non-dependent controls except at high doses, thereby highlighting its utility for investigating orexin signaling in alcohol dependence and addictive behaviors.

LY3154207 is a subtype selective, potent, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM).

CA-170 is an orally bioavailable dual inhibitor of VISTA and PD-L1 that selectively restores T-cell proliferation and effector function suppressed by immune checkpoint signaling, while demonstrating minimal off-target activity across a broad receptor and enzyme panel, making CA-170 a valuable compound for immuno-oncology research and immune checkpoint modulation studies.

Homo-PROTAC cereblon degrader 1 is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.

Biperiden Hydrochloride (KL 373 Hydrochloride) is an anticholinergic antiparkinsonian agent that selectively blocks central M1 cholinoreceptors while exerting atropine-like effects on peripheral parasympathetic structures. Biperiden Hydrochloride is approved for the adjunctive treatment of postencephalitic, idiopathic, and arteriosclerotic Parkinson’s disease, demonstrates minimal impairment of novelty preference compared with other anticholinergics in comparative cognitive studies, and is associated with known adverse effects including drowsiness, vertigo, headache, and dizziness.