Thiethylperazine is a phenothiazine derivative that acts as an oral dopamine D2-receptor and histamine H1-receptor antagonist. This compound functions as an ABCC1 activator and has been shown to decrease amyloid-β (Aβ) accumulation in mice. It exhibits anti-emetic, antipsychotic, and antimicrobial properties.

Opiranserin hydrochloride (VVZ-149 hydrochloride) is a non-opioid and non-NSAID analgesic that acts as a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50 of 0.86 μM and 1.3 μM, respectively.

ZPL-5212372 (PF 5212372) is a cPLA2α inhibitor (IC50 = 7 nM). ZPL-5212372 inhibits the release of prostaglandin D2 (PGD2), cysteyl leukotrienes, leukotriene B4, thromboxane A2, and PGD2 from human lung cells. ZPL-5212372 inhibits delayed bronchoconstriction and airway hyperresponsiveness in a sheep allergic inflammation model. ZPL-5212372 may be used in asthma research.

ZBP1 Covalent PROTAC-1 is a covalent Z-DNA binding protein 1 ZBP1 PROTAC degrader, with its DC50 being 25.69 nM. ZBP1 Covalent PROTAC-1 integrates the ligand that recruits the VHL E3 ubiquitin ligase and the DNA aptamer (Aptamer Z3) with the specific Zα domain that can bind to ZBP1, which has a high affinity (KD = 2.71 nM) with ZBP1. After degrading ZBP1, the phosphorylation levels of downstream signaling molecules RIPK3 and MLKL significantly decrease. ZBP1 Covalent PROTAC-1, encapsulated by nano-liposomes, significantly improves the survival rate of mice infected with influenza A virus (IAV) after administration via the trachea.

Z-13752A is a mercaptopropanoyl amino acid. Z-13752A inhibits NEP and ACE, with Ki values of 1.8 and 3.2 nM, respectively. Z-13752A decreases the arterial blood pressure and increases coronary blood flow. Z-13752A can be used in the research of coronary artery occlusion.

XAN-5 is a mitochondrial DNA G-quadruplex (mtG4) ligand with a Kd of 3.8 μM. XAN-5 selectively binds and stabilizes mtG4 structures, disrupting mitochondrial gene transcription and DNA replication. XAN-5 triggers mitochondrial dysfunction, ROS overproduction, G0 phase arrest and caspase-dependent apoptosis. XAN-5 inhibits autophagy and induces immunogenic cell death. XAN-5 inhibits tumor growth in a mouse liver cancer model while enhancing tumor-infiltrating CD4+ and CD8+ T cells. XAN-5 targets two cancer resistance mechanisms simultaneously. XAN-5 can be used for the research of liver cancer.

WWQ-03-012 is a selective deSUMOylating isopeptidases DESI2 inhibitor with an IC50 of 47.3 μM. WWQ-03-012 cans induce JAK2-V617F ubiquitination-proteasome degradation with no significant effect on wild-type JAK2. WWQ-03-012 can block JAK2-STAT3/5 signaling, inhibit cell proliferation and induce apoptosis. WWQ-03-012 has a synergistic effect in combination with Ruxolitinib, further enhancing its killing effect on JAK2 mutant cells. WWQ-03-012 can be used for the research of cancer, such as myeloproliferative neoplasms.

WCF-598 is a RXRγ (Kd: 234.2 nM) and AR-V7 PROTAC degrader. WCF-598 induces RXRγ degradation via the ubiquitin-proteasome pathway and binds directly to RXRγ. WCF-598 indirectly induces AR-V7 degradation, impairs the stability of the RXRγ-AR-V7 complex, downregulates AR-V7 levels, and inhibits the transcription of downstream target genes of AR-V7. WCF-598 induces tumor cell apoptosis, inhibits cell proliferation, activates the p53 signaling pathway, and suppresses cell cycle progression. WCF-598 can be used for the research of prostate cancer. (Pink: RXRγ Target protein ligand; Blue: Cereblon ligand ; Black: linker).

VU6052254, a derivative of VU0467319, is a selective, potent, orally active and brain-penetrant muscarinic M1 acetylcholine receptor (mAChR1) positive allosteric modulator with an EC50 of 59 nM. VU6052254 has no activity on the M2-5 receptor (EC50 > 30 μM). VU6052254 can improve memory recognition ability and reverse the cognitive impairment induced by Scopolamine with minimum effective dose both of 1 mg/kg. VU6052254 can be used for the research of neurological disease, such as Alzheimer's disease.

VKT-17-P4-23 is a blood-brain barrier-permeable DksA inhibitor. DksA is a highly conserved transcriptional regulator in Gram-negative bacteria, with a Kd of 124 μM. Through the DksA-regulated, SPI-2-dependent survival pathway, VKT-17-P4-23 exhibits antibacterial activity against both planktonic and intracellular pathogens such as Salmonella, and also effectively combats persistent bacteria that are difficult to eliminate. VKT-17-P4-23 can be used in studies of Salmonella infection.

VHR-IN-6 is a selective vaccinia H1-related (VHR) phosphatase inhibitor with an IC50 of 74 nM. VHR-IN-6 shows very weaker inhibitory activity against MKP-1 (IC50 = 0.52 μM), CD45 (IC50 = 0.50 μM), Cdc25A (IC50 = 2.8 μM), PTP1B (IC50 = 0.42 μM), and HePTP (IC50 = 0.87 μM). VHR-IN-6 inhibits the proliferation of HeLa cells. VHR-IN-6 can be used for the research of cervical cancer.

UDP-α-sulfoquinovose is a nucleoside metabolite.

Tubulin/VEGFR-2-IN-2 is an orally active tubulin and VEGFR-2 inhibitor with IC50s of 3.27 and 0.09 μM, respectively. Tubulin/VEGFR-2-IN-2 exerts the antitumor effects through multifaceted pathways, including enhancing reactive oxygen species (ROS) generation, disrupting mitochondrial membrane potential, inducing apoptosis, and arresting the cell cycle. Tubulin/VEGFR-2-IN-2 demonstrates anti-angiogenic properties by significantly impairing endothelial cell migration, invasion, and tube formation in vitro. Tubulin/VEGFR-2-IN-2 suppresses angiogenesis, tumor growth, and metastasis in vivo. Tubulin/VEGFR-2-IN-2 can be used for non-small lung cancer, breast cancer, gastric cancer and lymphoma.

tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.

TEI-6122 is a 7-thiaprostaglandin E1 derivative. TEI-6122 can reduce urinary protein and suppressthe increase of blood urea nitrogen. TEI-6122 can inhibit monocyte chemoattractant protein-1 induced chemotaxis. TEI-6122 can be used for the research of inflammation, such as nephritis.

SP187 hydrochloride (MON-DNJ hydrochloride; UV4 hydrochloride) is an orally active, host-targeting iminosaccharide against filovirus infection. SP187 hydrochloride inhibits endoplasmic reticulum glucosidase. SP187 hydrochloride exhibits antiviral and Dengue Virus activity in vivo. SP187 hydrochloride can be used in antiviral and dengue research.

Sodium Channel-IN-8 (Example 96) is a voltage-gated sodium channel (NaV1.7) inhibitor.Sodium Channel-IN-8 can be used for the research of pain.

SGK1-IN-7 is a blood-brain barrier-permeable SGK1 inhibitor with an IC50 of 0.72 μM. SGK1-IN-7 reduces the phosphorylation level of TAU protein at the Ser396 and Ser214 epitopes. SGK1-IN-7 antagonizes the toxicity induced by Okadaic acid. SGK1-IN-7 can be used in the research of Alzheimer's disease.

SCH 2047069 (MK-8267) is an orally active kinesin spindle protein (KSP) inhibitor (Kd: 0.5 nM) that can cross the blood-brain barrier. SCH 2047069 exhibits an IC50 value of ≤ 5 nM against the KSP ATPase. SCH 2047069 exhibits broad-spectrum antitumor activity. SCH 2047069 can induce mitotic arrest and apoptosis in tumor cells. SCH 2047069 can be used in the research of tumors such as ovarian cancer, colon cancer, glioblastoma, and lymphoma.

Ronomilast (Elbimilast; ELB353) is an orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 3 nM. Revamilast can be used for research to inflammation related diseases.

Rimegepant (BMS-927711) hemisulfate is a potent, orally active, selective and competitive calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor. Rimegepant hemisulfate can be used for migraine research.

Renin-IN-4 is a Renin inhibitor. Renin-IN-4 can be used for the research of cardiovascular disease.

Quinotolast is an orally active antiallergic agent. Quinotolast inhibits histamine release from rat peritoneal cells. Quinotolast inhibits cutaneous cromoglycate in guinea pig model. Quinotolast has inhibitory effect on histamine and peptide leukotrienes release from guinea pig lung fragments and mouse cultured mast cells. Quinotolast can be studied in allergy-related research.

QS-IN-1 (Compound 10 in Table 2 on page 18) is a quorum sensing (QS) inhibitor with an IC50 of 1.22 μM against agr-type QS. QS-IN-1 is applicable to the research of bacterial infections.

PU-11 is a Hsp90α/Hsp90β inhibitor with IC50 values of 18.6 μM and 89.8 μM and Kd values of 2 and 4.2 μM. PU-11 binds to the ATP-binding pocket of Hsp90α and Hsp90β and displays selective binding preference for Hsp90α over Hsp90β, mediated by the nonconserved Hsp90α Ser52 residue. PU-11 can be used for the research of neurodegenerative disorders.

PROTAC SMARCA2 degrader-36 (Compound 26) is a selective and potent SMARCA2 PROTAC degrader with a DC50 of 51 nM. PROTAC SMARCA2 degrader-36 promotes ubiquitination and degradation of SMARCA2. PROTAC SMARCA2 degrader-36 exhibits anticancer activity against non-small cell lung cancer. PROTAC SMARCA2 degrader-36 can be used in studies related to SMARCA4-deficient cancers. (Pink: Epigenetic Reader Domain Target protein ligand; Blue: Ligands for E3 Ligase and VHL ligand ; Black: linker).

PROTAC LRRK2 Degrader-3 (compound 6) is a PROTAC LRRK2 degrader with a DC50 of 0.17 nM. PROTAC LRRK2 Degrader-3 can be used for research in Parkinson’s disease and inflammation. (Pink: LRRK2 ligand ; Blue: Cereblon ligand ; Black: linker ).

PI3K/AKT/ERK/CREB activator 1 is an orally active PI3K/AKT/ERK/CREB pathway activator. PI3K/AKT/ERK/CREB activator 1 maintains neuronal survival and function, promotes neuronal proliferation, restores the viability of damaged neurons, and facilitates synapse formation. PI3K/AKT/ERK/CREB activator 1 alleviates neuroinflammation by reducing the levels of pro-inflammatory cytokines, preserves synaptic ultrastructure and restores spatial memory in Alzheimer's disease models. PI3K/AKT/ERK/CREB activator 1 can be used in research related to Alzheimer's disease.

Phenamacide hydrochloride is an anti-spasmodic agent that can be used for the study of urinary incontinence.

PF-03246799 monohydrochloride is a potent and selective 5-HT2C receptor agonist with an EC50 of 190 nM and a Ki of 160 nM. PF-03246799 monohydrochloride shows selectivity for 5-HT2C over 5-HT2A and 5-HT2B receptors. PF-03246799 monohydrochloride has the potential for stress urinary incontinence (SUI) research.