BMS-229724 is an orally active and tight-binding cytosolic phospholipase A2 (cPLA2) inhibitor with an IC50 of 2.8 μM. BMS-229724 can inhibit the production of arachidonic acid and eicosanoids in U937 cells, neutrophils, platelets, and other cells. BMS-229724 has anti-inflammatory activity and can be used in the research of diseases such as skin inflammation.

LXT34 (Example 2) is a GPR120 agonist. LXT34 has an anti-inflammatory activity. LXT34 promotes GLP-1 formation in the gastrointestinal tract and improves insulin resistance in macrophages and pancreas cells. LXT34 can be used for inflammatory diseases, such as type 2 diabetes, obesity and non-alcoholic fatty liver research.

Dopamine D4 receptor ligand 3 (Compound 16) is a dopamine D4 receptor (D4R) antagonist (pKi: 8.86). Dopamine D4 receptor ligand 3 has pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 sensors in HEK-293T cells, respectively. Dopamine D4 receptor ligand 3 inhibits the viability of three human glioma cell lines, U87 MG, T98G, and U251 MG. Dopamine D4 receptor ligand 3 induces ROS production and mitochondrial dysfunction in glioma cells.

SAR216471 is a P2Y12 receptor antagonist. SAR216471 reversibly blocks the binding of 2MeSADP to P2Y12 receptors in vitro with an IC50 of 17 nM. SAR216471 can result in the inhibition of platelet aggregation. SAR216471 exhibits anti-thrombotic activity in rat model. SAR216471 can be studied in research on thrombosis.

TriOncoFAP-GlyPro-MMAE is a small molecule drug conjugate (SMDC) targeting fibroblast activation protein (FAP) with an IC50 of 13 pmol/L. TriOncoFAP-GlyPro-MMAE combines a FAP-targeting ligand (TriOnco), a cleavable glycine-proline linker, and a cytotoxic payload (MMAE).

YZ-35 is a STAT3 inhibitor, with a Ki value of 0.38 μM. YZ-35 binds directly to STAT3 with high affinity, exhibiting a dissociation constant (Kd) of 190 nM. YZ-35 directly attenuates the dual phosphorylation of STAT3 (Tyr705 and Ser727). YZ-35 suppresses colony formation, cellular migration, and induces apoptosis in breast cancer cell lines (BCSC). YZ-35 selectively suppresses BCSC self-renewal. YZ-35 inhibits tumor growth in the BCSC xenograft models. YZ-35 can be used for the study of breast cancer.

CCI17464 is a selective, orally active EP4 agonist. CCI17464 can be used in a Freund's complete adjuvant (FCA) acute rat inflammatory pain model and shows complete reversal of allergic reactions.

LY2457546 is a potent and orally active multi-targeted anti-angiogenic tyrosine kinases inhibitor. LY2457546 demonstrates potent activity against targets that include VEGFR2, PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. LY2457546 can be used for the research of cancer, such as leukemia.

MOL-6131 is a highly selective, reversible tryptase inhibitor, with a Ki of 45 nM. MOL-6131 significantly reduces the following features of allergic airway inflammation: eosinophil infiltration in lung tissue, goblet cell hyperplasia and mucus occlusion of airways.

IHMT-15130 is a highly potent irreversible BMX kinase inhibitor (IC50=1.47 nM). IHMT-15130 inhibits the secretion of inflammatory cytokines, blocks inflammatory signaling pathways, and alleviates Angiotensin II-induced myocardial hypertrophy in mice. IHMT-15130 is promising for research of myocardial hypertrophy.

TcO-ABX474 (TcO-5) is a potent prostate-specific membrane antigen (PSMA) inhibitor with a Kd value of 6.1 nM. TcO-ABX474 inhibits prostate cancer cell growth and metastasis. TcO-ABX474 is promising for research of prostate cancer.

RS 93427-007 is an orally active prostacyclin stable mimetic agent. RS 93427-007 can be used for the research of cardiovascular disease, such as atherosclerosis.

SM1-71-R is a reversible analog o SM1-71). SM1-71-R lacks the acrylamide warhead and therefore cannot form a covalent bond with the kinase. SM1-71-R can be used as a control compound for SM1-71.

CC-3052 is a phosphodiesterase 4 (PDE4) inhibitor with immunomodulatory activities. CC-3052 reduces neutrophil apoptosis in HIV⁺. CC-3052 is promising for research of HIV-related diseases.

Dimephosphon is an anti-inflammatory agent with antihistamine and antiserotonin activities. Dimephosphon helps maintain the conduction function of the spinal cord and reduces the excitability of spinal motor neurons in the area surrounding the lesion. Dimephosphon directly activates lymphatic vessel movement and improves lymphatic circulation. Dimephosphon can be used for the study of inflammatory edema, acute spinal cord injury and lymphatic circulation disorders.

IDN-1965 is an irreversible, broad-spectrum caspase inhibitor. IDN-1965 prevents downstream apoptotic events (such as DNase activation) and significantly delays cytochrome c release by inhibiting caspase activity. IDN-1965 significantly delayed death in mice with cardiomyocyte apoptosis. IDN-1965 completely prevents left ventricular dilation, systolic dysfunction, and fibrosis in mice with dilated cardiomyopathy. IDN-1965 can be used to study apoptosis-related diseases such as heart failure and the mechanisms of apoptosis initiation.

GLK7-001 is a Trypanosoma cruzi glucokinase (TcGlcK) inhibitor. GLK7-001 has in vitro trypanocidal activity.

HOE-288 is an orally active angiotensin-converting enzyme (ACE) inhibitor. HOE-288 can be used for the research of neurological disease.

α-Synuclein inhibitor 15 (Compound 1) is an inhibitor targeting the fibrillation growth of α-synuclein (IC50=18 μM). α-Synuclein inhibitor 15 is promising for research of neurodegenerative diseases, such as Parkinson's disease (PD) and Lewy body dementia (LBD).

(Rac)-TUL01101 (Compound I) is a selective JAK kinase inhibitor. (Rac)-TUL01101 can be used in the research of various diseases such as rheumatoid arthritis, atopic dermatitis, and alopecia areata.

YM-50001 is a potent and selective dopamine D4 receptor antagonist with a Ki 5.62 nM. YM-50001 can be used for the research of neurological disease .

FCE-20696 (hydrochloride) is an orally active immunomodulator. FCE-20696 (hydrochloride) also shows anti-inflammation and anti-infection effects. FCE-20696 (hydrochloride) can be used for the researches of infection, inflammation and immunology, such as adjuvant arthritis.

RS-86 is a potent, central acting, and selective muscarinic acetylcholine receptor agonist. RS-86 exhibits typical cholinergic excitatory effects, such as inducing smooth muscle contraction, ganglion depolarization, central hypothermia, etc. RS-86 can be used for research on Alzheimer's disease.

SQ 26490 is an active corticoid, moderate-potency edema formation inhibitor. SQ 26490 inhibits edema formation in rats.

PY-PAP is a photoactivatable affinity probe and a derivative of PY-60). PY-PAP retains the cellular function of activating YAP transcriptional activity. In 293A cells, PY-PAP can label cathepsin D (CTSD) and annexin A2 (ANXA2) through ultraviolet crosslinking and click reactions. PY-PAP plays a key role in identifying ANXA2 as the specific target of PY-60.

MU876 (Compound 32) is a MUS81 inhibitor with an IC50 of 0.5  μM. MU876 effectively inhibits MUS81-dependent homologous recombination (HR) and break-induced replication (BIR) pathways. MU876 sensitizes cancer cells to DNA-damaging agents, such as Cisplatin, through impairing their ability to repair DNA lesions. MU876 can be used for cancers chemotherapy research.

BLX-2477 is a potent and selective 15-lipoxygenase-1 (15-LOX-1) inhibitor with an IC50 value of 99 nM. BLX-2477 can inhibit the generation of inflammatory lipid mediators such as 15-hydroxy-eicosatetraenoic acid (15-HETE). BLX-2477 can be used for the research of inflammation and immunology.

SR 142948 TFA is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 TFA antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 TFA blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 TFA shows blood-brain permeability and can be used in study of psychiatric disorders.

Midobrutinib (Example 13) is a BTK inhibitor (IC50: 0.813 nM). Midobrutinib can be used for research of diseases involving BTK, particularly cancer.

GT-02216 can bind to GCase allosterically and enhance its activity. GT-02216 enhances the activity of GCase in primary human fibroblasts dose-dependently reduces the accumulation of its substrate, hexosylsphingosine (HexCer). GT-02216 reduces the Tau accumulation in mutant GBA1 fibroblasts. GT-02216 can be used for the study of Parkinson’s disease.