Azapetine is an α-adrenergic receptor antagonist, with a IC50 of 0.205 μM against rat α1-adrenergic receptors and a IC50 of 1.3 μM against rat α2-adrenergic receptors. Azapetine blocks α1/α2-adrenergic receptor-mediated contraction of blood vessels and vascular smooth muscles. Azapetine can be used for the research of peripheral vascular diseases.

ATR-IN-31 is a selective ATR kinase inhibitor with an IC50 of 7 nM. ATR-IN-31 does not significantly inhibit ATM kinase activity. ATR-IN-31 functionally inhibits ATR kinase activity. ATR-IN-31 inhibits viability of prostate cancer cells.ATR-IN-31 can be used for the research of prostate cancer.

AT1R antagonist 4 (Example 26) is an AT1R antagonist. AT1R antagonist 4 shows excellent antagonistic activity against calcium influx in cells stably expressing AT1 receptors and ETA receptors. AT1R antagonist 4 can be used in kidney disease research.

Aromatase-IN-8 is a selective Aromatase inhibitor against an IC50 of 0.05 µM. Aromatase-IN-8 exhibits selective antiproliferative effects against estrogen receptor-positive breast cancer cell lines, while showing no toxicity toward non-tumoral cells. Aromatase-IN-8 suppresses estrogen active, increases testosterone levels, and downregulates estrogen receptor expression and phosphorylation. Aromatase-IN-8 can be used for triple negative breast cancer research.

AQ-13 (Compound 7) is a Chloroquine analogue with anti-breast cancer property. AQ-13 shows antiproliferative activities against MDA-MB231 and MCF7 with GI50 of 27.81 and 17.85 μM. AQ-13 shows low cytotoxicity against non-cancerous breast epithelial cells MCF10A (GI50 = 65.26 μM). AQ-13 can be used for the research of breast cancer.

Apoptosis inducer 56 is an apoptosis inducer. Apoptosis inducer 56 induces DNA damage (upregulation of γH2AX and p-ATM expression) by minor groove binding. Apoptosis inducer 56 induces intrinsic apoptosis (upregulation of p53 and Bax/Bcl-2 ratio, cleaved caspase-7) via S-phase cell cycle arrest. Apoptosis inducer 56 shows selectivity for cancer cells over normal breast epithelial cells. Apoptosis inducer 56 can be used for the research of breast cancer.

AP21998 is a Fv (mutant FKBP) domain-selective ligand that binds to a single FKBPv. AP21998 disrupts FKBP-mediated oligomerization, blocks the proliferation of transformed myeloid progenitors and facilitates their terminal myeloid differentiation. AP21998 disrupts aggregates of CAD-hM1 receptor fusion protein, allowing receptors to exit the ER and enter the plasma membrane. AP21998 can be used for cancer research.

Antiviral agent 75 (example D26) is a Ebolavirus (EBOV) and Bundibugyo ebolavirus (BDBV) inhibitor with IC50s of 0.11 μM and 0.75 μM, respectively. Antiviral agent 75 can be used for the study of filovirus infection.

Antitumor agent-212 is a α-exo-methylene-selenolactone derivative with prominent selective antitumor activity. Antitumor agent-212 exhibits an MIC value of 128 μg/mL against Gram-positive bacteria. Antitumor agent-212 exhibits significant antitumor effects in the U87 human glioma xenograft model. Antitumor agent-212 can be used for the study of glioma, breast cancer and non-small cell lung cancer, and antibacterial study.

Anti-Trypanosoma cruzi agent-9 is a topoisomerase II inhibitor. Anti-Trypanosoma cruzi agent-9 inhibits the growth of Trypanosoma cruzi and Leishmania donovani.

Antiproliferative agent-76 (Compound II-2) is an 8-sulfonamidoquinoline derivative and a selective anticancer agent. Antiproliferative agent-76 blocks the NF-κB and WNT signaling pathways. Antiproliferative agent-76 promotes cancer cell Apoptosis. Antiproliferative agent-76 exhibits anticancer activity against colorectal cancer and leukemia.

Antiproliferative agent-74 (Compound 19a) is an anti-proliferative agent. Antiproliferative agent-74 suppresses Twist1 expression, induces weak Apoptosis. Antiproliferative agent-74 displays anti-proliferative activity against non-small cell lung cancer cells.

Antiparasitic agent-39 (Compound 14) is a selective antiparasitic agent and Deferasirox derivative. Antiparasitic agent-39 reduces the mitochondrial membrane potential. Antiparasitic agent-39 shows antiparasitic activity against T. brucei, T. gambiense, L. Mexicana, T. gondii, B. divergens, P. falciparum with EC50s of 4.2 nM, 10.4 nM, 52.0 nM, 17.0 nM, 41.2 nM, 54.8 nM, respectively.

anti-NSCLC agent-2 (compound 6o) is a SLC7A11 and GPX4 inhibitor that reduces the expression of ferroptosis key regulators SLC7A11 and GPX4. anti-NSCLC agent-2 disrupts redox homeostasis, depletes glutathione, accumulates lipid peroxides, and induces ferroptosis in non-small cell lung cancer cells. anti-NSCLC agent-2 is applicable to research related to non-small cell lung cancer.

Antifungal agent 151 is a Prp8 intein inhibitor that inhibits the self-splicing process of the Prp8 intein, preventing maturation of the Prp8 protein. Antifungal agent 151 exerts in vitro antifungal activity against Cryptococcus neoformans and Cryptococcus gattii. Antifungal agent 151 can be used for the research of cryptococcus pneumonia.

Anticancer agent 302 (Example 1) is an anticancer agent. Anticancer agent 302 has a DC50 value of 199 nM for Cyclin E1 and an IC50 value of 133 nM for pRB. Anticancer agent 302 can be used for tumor research.

Antibacterial agent 313 (Compound 20) is a broad-spectrum antibacterial agent. Antibacterial agent 313 can be used for research of bacterial infection.

Analgesic agent-4 is an adenosine A3AR ligand with analgesic/antinociceptive activity. Analgesic agent-4 inhibits writhing responses in mice and exhibits dose-dependent activity in the acetic acid-induced mouse writhing model. Analgesic agent-4 can be used in the research of pain-related diseases.

Amorphigenin is a trothotenone compound. Amorphigenin inhibits osteoclast differentiation by suppressing the expression of c-Fos and NFATc1 in activated T cells. Amorphigenin degrades melanosome proteins by activating the AMPK-dependent autophagy pathway, but not in dependence of the mTOR pathway. Amorphigenin significantly protects bone mass and reduces bone erosion in a mouse model of inflammatory bone loss. Amorphigenin can be used to study inflammatory bone diseases, postmenopausal osteoporosis, and skin pigmentation disorders.

Aminobutane bisphosphonate is a Trypanosoma cruzi farnesyl pyrophosphate synthase (FPPS) inhibitor with an IC50 of 30.77 μM against Trypanosoma cruzi. Aminobutane bisphosphonate inhibits proliferation of intracellular amastigote Trypanosoma cruzi and lacks activity against non-infective epimastigote forms. Aminobutane bisphosphonate reduces osteoclastic bone resorption, osteoid surface extent, and osteoclast number per mm of bone surface.Aminobutane bisphosphonate alters mineral apposition rate in intact legs, inhibits immobilization-induced bone loss, and increases trabecular bone volume in Sprague-Dawley rats. Aminobutane bisphosphonate can be used for the research of american trypanosomiasis (chagas' disease) and immobilization-related bone loss.

ALK-IN-24 is an orally active ALK inhibitor with an IC50 value of 1.7 nM. ALK-IN-24 also inhibits insulin receptor kinase with an IC50 value of 6 nM. ALK-IN-24 suppresses the proliferation of lung adenocarcinoma cells. ALK-IN-24 inhibits ALK-driven tumor growth in xenograft mouse models. ALK-IN-24 can be used in research related to non-small cell lung cancer.

Alixorexton (ALKS 2680) enantiomer is the enantiomer of Alixorexton. Alixorexton is a selective, orally active and brain-penetrant agonist for orexin-2 receptor and can be used for hypersomnias research.

AldoView (Compound 3) is an intermediate. AldoView can be labeled with fluorine-18 to synthesize [18F]AldoView. [18F]AldoView is a highly selective aldosterone synthase PET imaging agent. AldoView can be used in imaging studies of primary aldosteronism.

ALC1-IN-1 (compound 1) is an ALC1 inhibitor in crystalline form that can be used in the research of cancer.

AKT1-IN-11, a Podophyllotoxin derivative, is a AKT1/tubulin dual inhibitor. AKT1-IN-11 down-regulates the phosphorylation level of AKT kinase in tumor cells, disrupting cell proliferation, causeing G2/M phase arrest and inducing apoptosis. AKT1-IN-11 also promotes tubulin depolymerization. AKT1-IN-11 can be used for the research of colorectal cancer.

AG-024104 is a CDK inhibitor with Ki values of 2.3 nM (CDK1/cyclinB), 1.8 nM (CDK2/cyclinA), and 0.67 nM (CDK4/cyclinD). AG-024104 functionally inhibits kinase activity of CDK1/cyclinB, CDK2/cyclinA, and CDK4/cyclinD. AG-024104 serves as a negative control for peripheral leukocyte toxicity studies in preclinical development.

AFP464 (NSC710464) is a prodrug of Aminoflavone and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 downregulates the expression of α6-integrin (α6-integrin), inhibits breast tumor growth, reduces the population of tumor-initiating cells, disrupts mammosphere structure, induces the formation of mucin lake clusters, triggers DNA damage, and exerts antiproliferative activity. AFP464 is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 is applicable to research related to breast cancer.

Aescigenin is a triterpenoid saponin compound that can be found in Aesculus hippocastanum. Aescigenin is the main component of sodium β-aescin, a compound that has the functions of reducing tissue edema, improving microcirculation, and anti-inflammation. It can be used in research on Bell's palsy.

ADD-196022 is an orally active antiepileptic and anticonvulsant agent. ADD-196022 shows ED50 values of 26.2 mg/kg and 5.79 mg/kg for intraperitoneal injection in mice and orally administration in rats. ADD-196022 can be used for the research of neurological disease.

ADC-VI (Compound 6) is a conjugate of a toxic molecule and a linker, in which the cytotoxin carried by CPD6 is Deruxtecan. Tricyclene is used to form an antibody-drug conjugate (ADC) by a chemical conjugation reaction through linking with an anti-FGFR2b antibody.