GSK805 is a potent, orally bioavailable RORγγ Inhibitor with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay.
RORγt Inverse agonist 2 is a selective, orally active RORγt inverse agonist with an EC50 of 119 nM[1].
Ilexoside O is a triterpene saponin isolated from the roots of Ilex pubescens. Ilexoside O exhibits weak xanthine oxidase (XOD) inhibitory activity (IC50=53.05 μM)[1].
Lenercept (Ro 45-2081) is a recombinant fusion protein that consists of the soluble TNF-receptor (p55) linked to the Fc portion of human IgG1[1].
Fluticasone propionate is a high affinity, selective GR (glucocorticoid receptor) agonist which is derived from fluticasone used to treat asthma and allergic rhinitis.Target: Glucocorticoid ReceptorFluticasone propionate is a corticosteroid derived from fluticasone used to treat asthma and allergic rhinitis. It is also used to treat eosinophilic esophagitis. Fluticasone propionate is a synthetic trifluorinated glucocorticoid. It is highly lipophilic (logp octanol/water 3.69). In studies the topical drug has been associated with burning, stinging, skin irritation, blisters, dryness, skin infection, infected eczema, viral warts,impetigo, atopic dermatitis, pruritus, exacerbation of pruritus, exacerbation of eczema, erythema, and folliculitis.There are also numerous side effects associated with the oral version of this medication including headache, stuffy or runny nose, difficulty speaking, sore or irritated throat and painful white patches in the mouth or throat. Candidiasis of mouth and throat is reported as a "very common" side effect indicating that it occurs with a frequency greater than 1 in 10.Hoarseness is "common" indicating a frequency from 1 in 10 to 1 in 100. In both instances rinsing the mouth with water immediately after inhalation is recommended.
Afelimomab (MAK 195F) is an anti-tumor necrosis factor F(ab')2 monoclonal antibody fragment. Afelimomab can be used for the research of sepsis[1].
Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651 IC50=309 nM).
GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.
Bifarcept is a recombinant antibody of interferon receptor type I (IFN-RI). Bifarcept can bind IFN-β and prolong its serum half-life[1].
Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It acts on the spinal cord by depressing reflexes.Chlorzoxazone is currently being used as a marker substrate in vitro/vivo studies to quantify cytochrome P450 2E1 (CYP2E1) activity in humans.
KSPWFTTL is an immunodominant Kb-restricted epitope from the p15E transmembrane protein. KSPWFTTL can restore susceptibility of a tumor line to anti-AKR/Gross MuLV cytotoxic T lymphocytes[1][2].
ZINC49534341 is a MRGPRX2 antagonist, with a Ki of 32 nM[1].
Thonzylamine is an orally active H1 histamine receptor antagonist, exhibits good antihistaminic and antianaphylactic properties. Thonzylamine can be used for the research of hypersensitivity diseases, nasal congestion, allergic conjunctivitis and other allergic diseases[1][2].
PTPN22-IN-1 is a potent PTPN22 inhibitor (IC50=1.4 µM; Ki=0.50 µM). PTPN22-IN-1 exhibits >7-10 fold selectivity for PTPN22 over similar phosphatases. PTPN22-IN-1 augments antitumor immune responses[1]. From WO2021007491A1 compound L-1.
PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader[1].
Beclometasone dipropionate monohydrate, the prodrug of Beclometasone, is an orally active and potent glucocorticoid recepter agonist. Beclometasone dipropionate monohydrate acts via a glucocorticoid receptor and suppresses inflammation and hyperproliferation. Beclometasone dipropionate monohydrate can be used for asthma [1][2].
Heptadecan-9-yl 8-((6-(decyloxy)-6-oxohexyl)(2-hydroxyethyl)amino)octanoate can be used in lipid nanoparticles (LNP) delivery systems for mRNA vaccine delivery[1].
Baloramotide is a recombinant NY-ESO-1 protein containing 182 amino acids. Baloramotide increases the immune response against tumors[1].
SYK/JAK-IN-1 is dual SYK/JAK inhibitor with IC50s of <5 nM for SYK and JAK2, respectively[1].
Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry[1].
Azapropazone is a nonsteroidal anti-inflammatory drug (NSAID). Azapropazone can be used for the research of rheumatoid arthritis and other rheumatoid conditions[1].
Valziflocept (BAX1810; TAK-752) is a recombinant soluble human FcγRIIb receptor that targets Fc and FcγR. FcγRs bind and neutralize pathogenic IgG, thus forming a "decoy" or "scavenger" receptor that can reduce the severity of autoimmune diseases. Valziflocept can be used in studies of autoimmune diseases such as systemic lupus erythematosus (SLE)[1].
Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis[1].
PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity[1].
Chamaechromone is a biflavonoid ingredient isolated from the roots of Stellera chamaejasme L. (Thymelaeaceae). Chamaechromone possesses anti-hepatitis B virus (HBV) effects against the surface antigen of HBV (HBsAg) secretion and has insecticidal activities[1].
Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with Ki values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity[1].
RXFP1 receptor agonist-6 (Example 7) is a RXFP1 receptor agonist. RXFP1 receptor agonist-6 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 12 nM[1].
Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
DPLG3 is a specific chymotryptic-like β5i subunits inhibitor. DPLG3 inhibits mouse i-20S with IC50 of 9.4 nM. DPLG3 can be used for immune disease research[1].