PARP10-IN-1 is a PARP10 inhibitor with an IC50 of 1.8 μM, 2.7 μM, and >10-fold selectivity over most PARP family members, excluding PARP7 and PARP16.PARP10-IN-1 inhibits PARP10-mediated mono-ADP-ribosylation, including auto-MARylation of PARP10 and MARylation of its protein targets.PARP10-IN-1 is membrane permeable and inhibits PARP10-dependent MARylation in human embryonic kidney cells.PARP10-IN-1 can be used for the research of cancer.

P38α-IN-11 (Compound 16c) is a p38α inhibitor with a KD value of 586 nM. P38α-IN-11 can be used for research on cervical cancer.

p38 MAP Kinase-IN-2 (Compound 5) is a p38 MAP Kinase inhibitor. p38 MAP Kinase-IN-2 can be used for the research of cancer.

P300-IN-6 is an orally active histone acetyltransferase p300 HAT domain inhibitor with human IC50 values of 7 nM. P300-IN-6 suppresses c-Myc expression, decreases H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation.P300-IN-6 suppresses tumor growth in xenograft mouse models.P300-IN-6 can be used for the research of multiple myeloma.

P2L-003 is a selective PAR2 antagonist with an IC50 of 0.62 μM in HT-29 cells. P2L-003 blocks PAR2-mediated Ca2+ mobilization without affecting PAR1, PAR4, or ATP-mediated signaling and dose-dependently suppresses the downstream MAPK signaling cascades, including ERK1/2 and p38 phosphorylation. P2L-003 can be used for colon cancer research.

OPN-9643 is a covalent inhibitor targeting the central palmitate binding pocket of TEADs with an IC50 of 15 nM, preventing autopalmitoylation and reducing TEAD-driven luciferase activity and canonical TEAD targets, CTGF and CYR61. OPN-9643 can be used for the research of cancer, such as melanoma.

ONO-2921 is an orally active and selective N-type calcium channel blocker. ONO-2921 functionally blocks N-type calcium channels. ONO-2921 reduces paw withdrawal responses during persistent nociception and hyperalgesia to heat in neuropathic pain models. ONO-2921 can be used for research on neuropathic pain and nociceptive pain.

OK-1035 is a selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 of 100 μM.

OH14 is a cellular FLICE-like inhibitory protein (cFLIP) inhibitor and TNF-related apoptosis-inducing ligand (TRAIL) sensitizer. OH14 selectively binds to the DED1 pocket of cFLIP, disrupting its recruitment to the TRAIL-death inducing signalling complex without affecting procaspase-8 recruitment to FADD, allowing procaspase-8 activation. OH14 promotes TRAIL-mediated apoptosis and impairs cell viability in breast cancer systems when combined with TRAIL. OH14 can be used for the research of breast cancer.

Octoclothepine (Clorotepine), an analog of Clozapine, is a neuroleptic and antipsychotic agent. Octoclothepine exists in enantiomeric forms, where the (+)-form acts as an atypical antipsychotic, while the (-)-functions as a typical antipsychotic. (+)-Octoclothepine exhibits extremely high binding affinity for 5-HT₆ and 5-HT₇ receptors, with Ki values of 0.41 and 0.38 nM; the Ki values of (-)-Octoclothepine are 17.7 and 1.3 nM, respectively. Octoclothepine can be used in research related to schizophrenia.

O-1812 is a selective CB1 ligand. O-1812 is also a very weak AMT inhibitor. O-1812 can be used in the research of chronic pain, migraines, and inflammation.

NSD-IN-5 (Example 47) is a nuclear receptor-binding SET domain (NSD) inhibitor with IC5050 values ​​of 6 and < 1 nM for NSD1 and NSD2, respectively. NSD-IN-5 also exhibits inhibitory activity against Avg KMS11 cells with an IC5050 of 6 nM. NSD-IN-5 may be used in research on multiple myeloma.

NSC 1008 is a selective Ras converting enzyme 1 (Rce1) inhibitor that reduces Rce1 in vitro activity with a human IC50 of 8.9 μM. NSC 1008 demonstrates selectivity for Rce1 by not inhibiting human Ste24 or huamn FTase. NSC 1008 exhibits low cell toxicity, and induces mislocalization of EGFP-Ras from the plasma membrane in cancer cells. NSC 1008 can be used for the research of cancer.

NS-181 is a MetAP2 inhibitor and antiamebic agent with oral effectiveness.NS-181 functionally inhibits methionine aminopeptidase 2, a protein critical for Entamoeba histolytica proliferation. NS-181 exerts antiamebic activity against Entamoeba histolytica, leading to resolution of amebic liver abscess. NS-181 can be used for the research of amebiasis.

NPD15261 (MI102) is a highly selective MYCN inhibitor. NPD15261 reduces the mRNA and protein levels of MYCN in liver cancer cells, inhibits cell proliferation and colony formation, and induces Apoptosis simultaneously. NPD15261 can be used in liver cancer research.

NLRP3-IN-89 is a NOD-like receptor protein 3 (NLRP3) inflammasome inhibitor. NLRP3-IN-89 inhibits the NLRP3 inflammasome pathway, reduces IL-1β secretion, and exhibits minimal interference with the NF-κB pathway. NLRP3-IN-89 can be used for the research of Parkinson's disease, frontotemporal dementia, multiple system atrophy, Alzheimer's disease, multiple sclerosis, amyotrophic lateral sclerosis, or brain injury.

NLRP3-IN-86 (Compound 8a), a derivative of Songorine, is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-86 can reduce LPS- and Nigericin-stimulated lactate dehydrogenase (LDH) release (IC50 = 2.69 μM in THP-1 cells and 1.75 μ M in J774A.1 cells). NLRP3-IN-86 can inhibit gasdermin D (GSDMD) cleavage and IL-1β secretion. NLRP3-IN-86 can inhibit cell pyroptosis. NLRP3-IN-86 can be used for research of inflammation.

Nitramisole is a nitrobenzene-heterocycle conjugate and microfilaricide. Nitramisole kills microfilariae of Brugia malayi, Dipetalonema viteae and Litomosoides carinii. Nitramisole can be used for the research of filariasis (Brugia malayi, Dipetalonema viteae, Litomosoides carinii infections).

NFE2L1 activator-1 (Compound 5b) is a potent nuclear factor erythroid 2-related factor 1 (NFE2L1) activator (EC50 = 2.4 µM). NFE2L1 activator-1 effectively resists ferroptosis (Ferroptosis). NFE2L1 activator-1 can specifically activate the NFE2L1 signaling pathway to upregulate GPX4, PSMB7, PSMC4. NFE2L1 activator-1 can be used in cancer research.

Neuroprotective agent 15 (Compound 3e) is a neuroprotective agent. Neuroprotective agent 15 is a selective butyrylcholinesterase (BChE) inhibitor, with IC50 values of 2.6 and 114.3 μM for BChE and AChE respectively. Neuroprotective agent 15 has cannabinoid CB2 receptor (CB2 receptor) agonistic activity. Neuroprotective agent 15 can reduce cell death, LDH release and Caspase-3/7 activity, and inhibit apoptosis. Neuroprotective agent 15 can reduce the formation of superoxide free radicals, maintain cell morphology, and significantly lower oxidative stress levels. Neuroprotective agent 15 can be used in the research of neurodegenerative diseases, such as Alzheimer's disease and Parkinson's disease.

NEP108 is a GID4 E3 ligase-based BRD4 PROTAC degrader, with its DC50 value approximately 3.8 μM. NEP108 has a strong affinity for GID4, with a KD value of 0.22 μM, and the KD value of its trimeric complex is 2.85 μM. NEP108 can be used for cancer research. (Pink: BRD4 ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker).

Nebracetam (WEB 1881 FU) is an orally active M1 muscarinic receptor agonist. Nebracetam can induce an increase in intracellular Ca2+ concentration, with an EC50 value of 1.59 mM. Nebracetam exhibits neuroprotective activity and the ability to improve cognitive impairment. Nebracetam can be used in the research of neurological diseases such as Alzheimer's disease.

Nav1.7-IN-19 is a potent, selective and orally active Nav1.7 inhibitor with an IC50 of 0.49 μM. Nav1.7-IN-19 shows high selectivity for Nav1.7, with selectivities of 312-fold and 662-fold against Nav1.1 and Nav1.5 in the inactivated state. Nav1.7-IN-19 exhibits weak inhibition on hERG potassium channels. Nav1.7-IN-19 exhibits analgesic effect and can be used for the research of neurological disease.

NAT8L-IN-1 is a NAT8L inhibitor with an IC50 value of 0.3 μM. NAT8L-IN-1 can be used for the research of Canavan disease.

N19-0881 (Compound 33) is an orally active, potent and selective KDM5A/5B histone lysine demethylase inhibitor (IC50= 0.013 μM and 0.002 μM, respectively). N19-0881 is promising for research of epigenetically dysregulated tumors (e.g., breast cancer).

N,N-Di-(beta-carboethoxyethyl)methylamine is a PROTAC linker that can be used in the synthesis of PROTACs.

N-(Aminoiminomethyl)-N-methyl-D-alanine is an amino acid derivative that can be used in the research of cancer.

N-(3-Aminopropyl)-N-methylcarbamic acid tert-butyl ester is a PROTAC linker that can be used in the synthesis of PROTACs.

Multi-target kinase-IN-10 (Compound 6l) is an orally active, blood-brain barrier-permeable, selective, reversible, and competitive MAO-B inhibitor with an IC50 of 0.0053 μM. Multi-target kinase-IN-10 competes with substrates for binding to the active site of MAO-B, chelates Cu2+ ions, inhibits Cu2+-induced ROS production, and reduces the release of NO, TNF-α, and IL-1β. Multi-target kinase-IN-10 ameliorates Parkinson's disease.

MU262 is a MUS81 inhibitor with an IC50 value of 0.87 μM. MU262 directly inhibits the catalytic activity of MUS81 without interfering with DNA binding, induces genomic instability in tumor cells, and specifically inhibits the HR/BIR repair pathway. The combination of MU262 with Cisplatin significantly enhances the chemotherapeutic killing effect. MU262 serves as a chemical biology tool for studying MUS81 function, and also acts as a lead compound for the development of anticancer therapies that exploit DNA repair defects in cancer cells.