Pegcantratinib (CT327) is a potent and selective TRKA antagonist with activity against TRKB and TRKC. Pegcantratinib can be used for research of CYLD cutaneous syndrome (CCS) and inflammatory dermatoses, such as psoriasis and concomitant pruritus.

PD-L1-IN-8 is a PD-L1 inhibitor (IC50 = 0.89 nM). PD-L1-IN-8 shows low CYP inhibition and minimal hERG activity. PD-L1-IN-8 can be used for the study of colon cancer.

PDL1 degrader-3 (comppund e24) is a CSN5-binding antitumor immunomodulator with a human CSN5 Kd of 4.53 μM. PDL1 degrader-3 inhibits CSN5 enzymatic activity, increases PD-L1 ubiquitination, and induces PD-L1 degradation via the ubiquitin-proteasome pathway, reducing PD-L1 expression on tumor cell membranes. PDL1 degrader-3 blocks PD-1/PD-L1 interaction, activates the tumor immune microenvironment, enhances tumor-infiltrating T-cell immunity, and inhibits activation of immunosuppressive MDSCs and Tregs. PDL1 degrader-3 exerts antitumor effects in mouse tumor models. PDL1 degrader-3 can be used for the research of colorectal cancer, lung cancer.

PDI-IN-5 (compound 30z) is an allosteric-covalent inhibitor targeting protein disulfide isomerase (PDI) with a 2-chloro-pyrrolopyrimidin-4-one scaffold, with an IC50 of 0.4 μM. PDI-IN-5 exhibits selectivity for ERp57 and GPX4, and inhibits glioblastoma. PDI-IN-5 can be used in glioblastoma-related research.

PDE5/CA-IN-1 is a dual PDE5 and carbonic anhydrase (CA) inhibitor, with IC50 values of 0.41, 38.4, and 9.1 nM against PDE5, hCA II, and hCA VA, respectively. PDE5/CA-IN-1 inhibits multiple hCA subtypes associated with Alzheimer's disease. As a cytoprotective agent and oxidative stress alleviator, PDE5/CA-IN-1 reduces oxidative stress, and prevents recognition memory and working memory impairments. PDE5/CA-IN-1 is available for the research of Alzheimer's disease.

PDE4-IN-33 is a phosphodiesterase 4 (PDE4) inhibitor. PDE4-IN-33 reduces uric acid levels. PDE4-IN-33 PDE4-IN-33 can be used for the research of hyperuricemia and gout.

PDE4-IN-32 (Compound B05) is a selective, blood-brain barrier permeable PDE4B and PDE4D inhibitor with IC50 values of 13.7 nM and 23.8 nM, respectively. PDE4-IN-32 promotes the recovery of motor and cognitive function in MCAO/R mouse models. PDE4-IN-32 reduces cerebral edema. PDE4-IN-32 can be used for the research of ischemic stroke.

PDE4B/D-IN-5 (Compound P32) is a peripherally restricted, oral active inhibitor of PDE4B and PDE4D with extremely low blood-brain barrier penetration, with IC50 values of 3.4 nM and 2.2 nM, respectively. PDE4B-IN-8 inhibits the production of TNF-α. PDE4B/D-IN-5 significantly reduces the Bax/Bcl2 ratio, and alleviates oxidative stress by decreasing MPO activity and NO levels. PDE4B/D-IN-5 exhibits anti-inflammatory, antioxidant, and anti-apoptotic activities. PDE4B/D-IN-5 can be used for the research of acute lung injury.

PDE4/5-IN-1 is a selective phosphodiesterase 4/5 (PDE4/5) dual inhibitor. PDE4/5-IN-1 functionally inhibits PDE5, PDE4B2, and PDE4D2 activity. PDE4/5-IN-1 relaxes isolated rat prostate tissue, enhances nitric oxide-induced relaxation in isolated rat prostate tissue, and reduces alpha-1 adrenoceptor-mediated contractile responses in isolated rat prostate tissue. PDE4/5-IN-1 inhibits proliferation of human hyperplastic prostate cells. PDE4/5-IN-1 can be used for the research of benign prostatic hyperplasia.

PDE3/4-IN-4 is an orally active PDE3A and PDE4B inhibitor with IC50 values of 10 nM and 9.4 nM, respectively. PDE3/4-IN-4 shows selective activity relative to most other PDE family members. PDE3/4-IN-4 modulates the cAMP/PKA/CREB signaling pathway. PDE3/4-IN-4 inhibits pro-inflammatory factor IL-6. PDE3/4-IN-4 reduces expression of inflammatory markers in liver tissue. PDE3/4-IN-4 attenuates liver fibrosis. PDE3/4-IN-4 limits liver damage in cholestatic and sepsis-induced liver disease mice models. PDE3/4-IN-4 can be used for the research of liver injury, cholestatic liver diseases, sepsis-induced liver injury.

PDE1-IN-12 (P78, the first compound in 12) is a PDE1 inhibitor. PDE1-IN-12 inhibits PDEl-mediated suppression of the dopamine D1 receptor intracellular pathway and can be used for narcolepsy.

PDE1-IN-11 (Compound 5cc) is an orally active and highly selective PDE1A1 inhibitor. PDE1-IN-11 increases intracellular cAMP and cGMP levels, activating the PKA-CREB and NO-cGMP-PKG signaling pathways, promoting osteoblast differentiation and bone formation, while suppressing osteoclastogenesis and bone resorption. PDE1-IN-11 is promising for research of postmenopausal osteoporosis (PMO) and other bone metabolism disorders.

PDE10A-IN-1 is a phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 250 nM and the ability to cross the blood-brain barrier. PDE10A-IN-1 can be used in research on neurological disorders such as schizophrenia.

PD-143188 (CI 1007) is a selective agonist targeting dopamine (DA) receptors, with Ki values of 25.5 nM and 16.6 nM for human D2 and D3 receptors, respectively and lower affinity for D4.2 receptors (Ki=90.9 nM). PD-143188 inhibits DA release, synthesis and metabolism, while reducing cellular cyclic AMP levels, exerting antipsychotic activity. PD-143188 is promising for research of psychopharmacology.

PD-1/PD-L1-IN-61 is a PD-1/PD-L1 interaction inhibitor with a human IC50 of 5.3 nM. PD-1/PD-L1-IN-61 embeds into the hydrophobic pocket at the PD-L1 dimer interface, stabilizing binding through hydrogen bonds and π-π stacking with PD-L1 residues. PD-1/PD-L1-IN-61 acts as an immune activator, enhances immune-killing activity of peripheral blood mononuclear cells against cancer cells, restores T-cell immune function, and promotes IFN-γ secretion. PD-1/PD-L1-IN-61 can be used for the research of triple-negative breast cancer.

PD-1/PD-L1-IN-60 is the counterpart of the small-molecule immuno-probe [18F] LG‑8, and the two together enable integrated immuno-diagnosis and therapy. PD-1/PD-L1-IN-60 exhibits potent anti-tumor activity in mouse models of melanoma and lung cancer with high PD‑L1 uptake. PD-1/PD-L1-IN-60 can be used for relevant research on melanoma and lung cancer.

PD 168368 derivative-1 (Compound 16) is a derivative of PD 168368, with Ki values of 0.46 and 3.7 nM for the subtypes of bombesin receptor (BB₁ and BB₂). PD 168368 derivative-1 can be used for the study of various diseases, such as cancer, depression, and eating disorders.

PC6-VC-PAB-MMAE is a Drug-Linker Conjugates for ADC. PC6-VC-PAB-MMAE consists of the ADC Cytotoxin MMAE and a linker. PC6-VC-PAB-MMAE can be used for synthesis of ADCs.

PB2-IN-3 (Compound 11) is a PB2 inhibitor. PB2-IN-3 exhibits antiviral activity against Influenza A H1N1 and H3N2 strains. PB2-IN-3 can be used in studies related to influenza A virus infection.

PAT-347 sodium is an Autotaxin (ATX) inhibitor. ATX is a secretory enzyme that hydrolyzes lysophosphatidylcholine (LPC) and regulates lysophosphatidic acid (LPA) production in the blood.

PAT-078 is a type II autotaxin (ATX) inhibitor. PAT-078 mainly occupies the hydrophobic pocket of ATX, blocks the bottleneck region between the hydrophobic channel and the catalytic site, and does not interact with the zinc ion at the catalytic site.

Parsalmide is an orally active non-steroidal anti-inflammatory drug and gastroprotective agent, with an IC50 of 9.92 μM against COX-1 and 155 μM against COX-2. Parsalmide prevents gastric injury and reduces edema. Parsalmide can be used in the research of arthritis.

PARP1-IN-56 (Compound RCY) is an I-labeled poly(ADP−ribose) polymerase (PARP1) inhibitor. PARP1-IN-56 can be radiolabeled with 211At or 125I for use as an α-emitting radiotherapeutic agent. PARP1-IN-56 can be used for the research of cancer.

PARP1-IN-55 is a potent and selective PARP1 inhibitor with an IC50 value of 0.019 μM. PARP1-IN-55 exhibits anti-proliferative selective activity against MCF-7 breast cancer cells (IC50 = 3.6 μM). PARP1-IN-55 inhibits the PARP1-mediated DNA damage repair pathway, induces ROS accumulation, disrupts mitochondrial membrane potential, induced apoptosis and suppresses cancer cell migration, invasion, and colony formation. PARP1-IN-55 can be used for the study of breast cancer.

PARP1-IN-53 (Compound 328) is a quinazolinone derivative and PARP1 inhibitor with a PARP1 IC50 of 0.1 nM and selectivity over PARP2, which has a PARP2 IC50 of 23 nM.PARP1-IN-53 can be used for the research of cancer.

PARP1-IN-51 (P55 the second compound in the fifth row) is a PARP1 inhibitor. PARP1-IN-51 can be used for the research of cancer, such as breast cancer.

PARP1-IN-50 is a selective and orally active PARP-1 inhibitor with an IC50 of 64.98 nM. PARP1-IN-50 can inhibit PAR formation and induce DNA double strand breaks, thereby causing DNA damage. PARP1-IN-50 can induce G2/M phase arrest and cancer cells apoptosis. PARP1-IN-50 demonstrates significant antiproliferative activity against various cancer cells. PARP1-IN-50 can be used for the research of cancer, such as breast cancer.

PARP1-IN-48 (Compound 61) is a highly selective PARP1 (PARP1 IC50 = 3 nM, PARP2 IC50 = 170 nM) inhibitor. PARP1-IN-48 can be used for research on cancer, viral infections, and metabolic conditions.

PARP1-IN-47 (Compound 35) is a highly selective PARP1 inhibitor (IC50 <100 nM). PARP1-IN-47 blocks poly(ADP-ribosyl)ation and disrupts DNA damage repair pathways to induce tumor cell apoptosis. PARP1-IN-47 is promising for research of solid tumors and hematological malignancies.

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.