MolPort-010-778-422 is a high-affinity inhibitor targeting the ACE2 receptor of SARS-CoV-2 virus. MolPort-010-778-422 demonstrates excellent antiviral activity (IC50=8.9 nM). MolPort-010-778-422 is promising for research of SARS-CoV-2.

APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research.

BAL-1516 is a brain-penetrant and highly selective NLRP3 inhibitor (IC50=14.2 nM). BAL-1516 significantly suppresses IL-1β and IL-18 release in microglial neuroinflammation models (IC50=11-59 nM). BAL-1516 is promising for research of neurodegenerative diseases (e.g., Alzheimer’s, Parkinson’s) and systemic inflammatory disorders.

NZ-107 is an orally active leukotriene receptor antagonist. NZ-107 can inhibit anaphylaxis reaction. NZ-107 can be used for the researches of inflammation and immunology.

MG-HuR2 is a molecular glue degrader targeting the oncogenic RNA-binding protein HuR (IC50=0.5 μM). MG-HuR2 is promising for research of HuR-overexpressing malignancies (e.g., breast cancer).

Wy 27569 is an orally active vascular selective calcium channel blocker that can effectively lower blood pressure. Wy 27569 is a thromboxane synthase inhibitor that can reshape prostaglandin balance, reduce pro thrombotic TXA2, and increase anti thrombotic PGI2. Wy 27569 can be used for research on cardiovascular diseases such as hypertension and angina.

TEI-2306 is a precursor of glutathione biosynthesis. TEI-2306 possesses a unique anti-HIV-1 activity in both chronically and acutely infected cells, and even for free viruses. TEI-2306 can be used for the study of myocardial ischaemia.

Emvistegrast is a quinolone derivative. Emvistegrast is an antagonist of α4β7 integrin. Emvistegrast can be studied in research for diseases that are mediated by α4β7 integrin, such as infkammatory bowel disease.

NSC 303861 is an L-glutamine antagonist. NSC 303861 selectively inhibits glutamine dependent enzymes in purine nucleotide synthesis without affecting pyrimidine synthase. NSC 303861 has significant cytotoxicity against liver cancer 3924A cells (LC50 = 6 µM). NSC 303861 can be used for cancer research.

diABZI-i is a orthosteric STING inhibitor. diABZI-i significantly inhibits cGAMP-induced IFNβ in PBMCs with an IC50 of 49 nM. diABZI-i also activates V155M SAVI constitutive signaling in STING V155M THP-1 cells model with potent agonism (EC50: 17  nM). diABZI-i can be used for monogenic autoinflammatory disease like SAVI disease research.

diABZI-a1 is a orthosteric STING agonist with EC50 of 117 nM for IFNβ in human PBMCs. diABZI-a1 can be used for monogenic autoinflammatory disease like SAVI disease research.

AP-503 is a selective GPR133/ADGRD1 agonist with an EC50 of 1.21 nM. AP-503 is used in research on the prevention of muscle-related diseases and vestibular dysfunction.

DNH28 is a potent NF-κB and MAPK inhibitor with an IC50 of 0.93 μM against HepG2 cells. DNH28 promotes apoptosis by down-regulating the expression of Bcl-2, up-regulating the expression of BAX and Cleaved-caspase-3. DNH28 blocks the cell cycle and inhibits migration. DNH28 can be used for the study of hepatocellular carcinoma (HCC).

CGP-74514 dihydrochloride is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor (IC50=25 nM). CGP-74514 dihydrochloride inhibits CDK1/cyclin B complex activity, arrests the cell cycle at G2/M phase and induces tumor cell apoptosis. CGP-74514 dihydrochloride is promising for research of bladder cancer.

BMS-341400 is an orally active selective phosphodiesterase 5 (PDE5) inhibitor with an IC50 value of 0.3 nM. BMS-341400 reduces the degradation of cyclic guanosine monophosphate (cGMP), thereby enhancing nitric oxide (NO)-mediated relaxation of the smooth muscle of the corpus cavernosum and promoting erection. BMS-341400 can be used to study erectile dysfunction.

CDK12-Cyclin K Ligand-Linker Conjugates 1 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for CDK12-Cyclin K and a PROTAC linker, which recruits E3 ligases. CDK12-Cyclin K Ligand-Linker Conjugates 1 can be used for synthesis of PROTAC PP-C8

MDL 27266 is an orally active NMDA receptor antagonist with neuroprotective effect. MDL 27266 is a broad-spectrum anticonvulsant agent.

SEP-4199 is a nonracemic 85:15 ratio of Aramisulpride and Esamisulpride. SEP-4199 exhibits significant differences in relative potency at two different receptors (5-HT7R and D2R) compared to the racemate. SEP-4199 exhibits antidepressant effects.

NK7-902 TFA is a CRBN molecular glue degrader of NEK7. NK7-902 TFA fully degrades NEK7 in human primary monocytes and whole blood but only partially inhibits NLRP3-dependent IL-1β production. NK7-902 TFA leads to profound and long-lasting NEK7 degradation but only transiently blocks NLRP3 inflammasome activation in non-human primates by oral administration. NK7-902 TFA shows activity in murine systems.

Aramisulpride (hydrochloride) is a 5-HT7 receptor antagonist with a Ki value of 22 nM. Aramisulpride (hydrochloride) is a D2/D3 receptor antagonist with a Ki value of 140 nM for D2R and a Ki value of 13.9 nM for D3R. Aramisulpride (hydrochloride) can be used in psychiatric research.

Zocainone is an antiarrhythmic agent. Zocainone blocks sodium channels in cardiac tissue, stabilizing the cardiac action potential and reducing abnormal electrical activity. Zocainone is promising for research of cardiac arrhythmias.

T 588 is an orally active neuroprotective agent. T 588 can increase acetylcholine release from the frontal cortex and hippocampus and meliorate cognitive dysfunction. T 588 can protect cerebellar granule cells from glutamate neurotoxicity. T 588can be used for the research of neurological disease, such as Alzheimer's disease.

Methyltetrazine-DBCO TEA is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Methyltetrazine-DBCO TEA is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups. Methyltetrazine-DBCO TEA also contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.

AD109 is a combination of the selective norepinephrine reuptake inhibitor atomoxetine and the antimuscarinic agent aroxybutynin. AD109 shows orally active significantly and reduce the apnea–hypopnea index.

AZD-2327 is a potent and selective δ-opioid receptor agonist. AZD-2327 binds to the human opioid receptor (Ki = 0.49 and 0.75 nM and EC50 = 24 and 9.2 nM at the C27 and F27 isoforms, respectively). AZD-2327 shows selectivity of >1000-fold over the human μ- and κ-opioid receptor subtypes as well as >130 other receptors and channels. AZD-2327 exhibits antidepressant and anxiolytic activities and can be used for the research of neurological disease.

MK 287 is a potent, selective and orally active antagonist of platelet-activating factor receptor (PAFR). MK 287 can inhibit [3H]C18-PAF binding to human platelet, polymorphonuclear leukocyte (PMN) and lung membranes with K1 values of 6.1, 3.2, and 5.49 nM, respectively. MK 287 can inhibit PAF-induced aggregation of platelets in plasma or gel-filtered platelets and elastase release from PMNs with ED50 values of 56, 1.5 and 4.4 nM. MK 287 can be used for the research of cardiovascular disease, such as thrombosis.

CGS 15873A is an orally active benzopyranopyridine derivative. CGS 15873A has selective dopamine receptor activation activity. CGS 15873A can be used for research on schizophrenia or Parkinson's disease.

CQP-201403 is a dopamine receptor agonist. CQP-201403 can be used for the research of neurological disease.

FPFS-1169 (hydrochloride) is a proto-oncogene protein c-bcl-2 stimulant. FPFS-1169 (hydrochloride) can increase the impulse-evoked release of monoamine neurotransmitters. FPFS-1169 (hydrochloride) can be studied in research on Parkinson’s disease.

A-620223 is a PARP-1 inhibitor with a Ki of 8 nM against PARP-1 and EC50 of 3 nM in a whole cell assay. A-620223 demonstrates good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with Temozolomide (TMZ) and in an MX-1 breast xenograph model in combination with Cisplatin. A-620223 can be used for the studies of melanoma and breast cancer.