Amiloxate is a UV-filter with anti-inflammatory activity[1].
Eclitasertib (DNL-758) is a potent receptor-interacting protein kinase 1 (RIPK1) inhibitor with an IC50 of <1 µΜ (From patent WO2017136727A2, example 42)[1].
Thalidomide-5-NH2-CH2-COOH (compound 114) is a potent and selective inhibitor of tropomyosin receptor kinase (trk). Thalidomide-5-NH2-CH2-COOH is a ligand of E3 ligase. Thalidomide-5-NH2-CH2-COOH has the potential for the treatment of one or more diseases (extracted from patent WO2021170109A1) [1].
COX-2-IN-11 (compound 7b2) is a potent and selective inhibitor of COX-2. COX-2-IN-11 has the potential for the research of inflammation diseases[1].
Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor (GR) modulator with a Ki value ＜1 nM in vitro. Dazucorilant can be used for the research of neurological disorders[1][2].
WDB002, a natural product, is a member of the FK506/rapamycin family. WDB002 can target CEP250. WDB002 can be used for the research of COVID-19[1].
RP-5063 (Brilaroxazine) is a multimodal dopamine and serotonin modulator with partial agonist activity at DA D2, D3, D4, 5-HT1A, and 5-HT2ARs, and antagonist activity at 5-HT2B, 5-HT6 and 5-HT7Rs; produces dose-dependent reductions in pulmonary blood vessel wall thickness and proportion of muscular vessels, blocks MCT-induced increases in the plasma cytokines TNFα, IL-1β, and IL-6 in vivo; prevents Sugen 5416-hypoxia-induced pulmonary arterial hypertension in rats; improves declarative memory and psychosis in mouse models of schizophrenia. Schizophrenia Phase 2 Clinical
Octenyl succinic anhydride can be used to esterify Starch to yield a hydrocolloid with amphiphilic properties, octenyl succinylated starch (OS-starch). Octenyl succinic anhydride (OSA) modification affects interaction between molecules on the outer surfaces of two starch granules by altering molecular structures on the outer surfaces[1].
Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades[1].
Terevalefim (ANG-3777), an hepatocyte growth factor (HGF) mimetic, selectively activates the c-Met receptor[1][2].
TLR7 agonist 8 (compound IIb-34) is an TLR7 agonist with an EC50 value of ~4 nM[1].
(±)-Catechin (rel-Cianidanol) is the racemate of Catechin. (±)-Catechin has two steric forms of (+)-Catechin and its enantiomer (-)-Catechin. (+)-Catechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM. Anticancer, anti-obesity, antidiabetic, anticardiovascular, anti-infectious, hepatoprotective, and neuroprotective effects[1].
A-943931 (Compound 10) is a histamine H4 receptor antagonists. A-943931 has improved pharmacotropic and in vivo efficacy in models of pain and inflammation. A-943931 can be used in vivo anti-inflammatory and anti-nociception research [1].
TLR8 agonist 2 hydrochloride is a potent and selective TLR8 agonist with an EC50 of 3 nM for human TLR8. TLR8 agonist 2 hydrochloride shows less active against human TLR7 (EC50 of 33.33 μM)[1].
Fluorometholone, a synthetic glucocorticoid, is a glucocorticoid receptor agonist with anti-inflammatory and anti-allergic properties. Fluorometholone can be used in the management of dry eye[1].
Cilomilast(SB 207499; Ariflo) is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity.IC50 value: 110 nMTarget: PDE 4Cilomilast (SB-207499) inhibits HPDE4 and LPDE4 catalytic activity with equal potency (Ki ≈100 nM). SB-207499 and rolipram are equipotent against LPDE4, but Cilomilast (Ariflo, SB-207499) is 100-fold less potent against HPDE4. This profile suggests that Cilomilast (Ariflo, SB-207499) retain the anti-inflammatory activity of rolipram yet have a decreased tendency to produce side effects.
COX-1/2-IN-2 is a potent COX1/2 inhibitor. COX-1/2-IN-2 exhibits significant inhibitory effect against COX-1 and COX-2 inhibitor with IC50 values of 13.9 ± 3.21 µM and 6.4±0.74 µM, respectively[1].
Netakimab is an anti-IL-17 monoclonal antibody. Nerelimomab can be used for research of ankylosing spondylitis, psoriatic arthritis, moderate-to-severe plaque psoriasis[1][2].
Polyketide synthase 13-IN-3 (compound 41) is a polyketide synthase 13 inhibitor，with a MIC of 0.0625-0.125 μg/mL against the M. tuberculosis strain H37Rv[1].
Pterostilbene is a stilbenoid isolated from blueberries and Pterocarpus marsupium[1]. Shows anti-oxidant, anti-inflammatory, anti-carcinogenic, anti-diabetic and anti-obesity properties[1][4]. Pterostilbene blocks ROS production[3], also exhibits inhibitory activity against various free radicals such as DPPH, ABTS, hydroxyl, superoxide and hydrogen peroxide[4].
Amtolmetin guacil is an effective nonsteroidal anti-Inflammatory agent with pain-relieving effects. Amtolmetin guacil inhibits prostaglandin synthesis and cyclooxygenase (COX). Amtolmetin guacil can stimulate capsaicin receptors present on the gastrointestinal wall and also releases gastroprotective nitric oxide (NO). Amtolmetin guacil can be used to research knee osteoarthritis[1][2].
Peritassine A, an alkaloid that could be isolated from Tripterygium wilfordii Hook. f., possesses anti-HIV activity[1][2].
Seratrodast(AA 2414) is a potent and selective thromboxane A2 receptor (TP) antagonist.Target: Thromboxane A2 ReceptorSeratrodast, also known as AA-2414, is a potent and selective antagonist of the TXA2R (thromboxane A2 receptor). AA-2414 reduced the induction of pulmonary inflation caused by LTD4 aerosol inhalation. AA-2414 competitively inhibited the contractile response to U-46619 in guinea pig tracheal and parenchymal strips and dog saphenous vein strips with pA2 values of 7.69, 8.29 and 6.79, respectively. AA-2414, a quinone derivative, is a novel, potent and orally active antagonist of a variety of spasmogenic prostanoids [1]. AA-2414 inhibited peroxide-induced vasoconstriction in the human placenta, as well as peroxide- induced increases in the placental secretion rates of lipid peroxides and thromboxane, but only partially inhibited peroxide-induced increases in the placental secretion rate of prostacyclin [2].
Carbasalate calcium is an anti-inflammatory, antipyretic, and analgesic agent.
11-O-Galloylbergenin is a compound isolated from ethanolic extract of Mallotus philippinensis. 11-O-Galloylbergenin has analgesic and anti-inflammatory activities. 11-O-Galloylbergenin is a lead compound for management of pain and inflammation[1].
SDMA (Symmetric dimethylarginine) is an endogenous inhibitor of nitric oxide (NO) synthase activity.
IDO1/TDO-IN-4 is a potent IDO1/TDO dual inhibitor, with IC50 values of 3.53 μM (IDO1) and 1.15 μM (TDO). IDO1/TDO-IN-4 forms hydrogen bond with IDO1, and π−π stacking interaction with TDO. IDO1/TDO-IN-4 can be used in the research of depression, and depression-induced infectious, metabolic, and autoimmune disorders[1].
BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
FKGK11 is a potent and selective inhibitor of GVIA iPLA2 (Group VIA calcium-independent phospholipase A2). FKGK11 can be used for the research of ovarian cancer and neurological disorders such as peripheral nerve injury and multiple sclerosis[1][2].
c-Fms-IN-14 (Example 76) is a c-Fms inhibitor with an IC50 value of 4 nM. c-Fms-IN-14 can be used for research of cancer and autoimmune diseases[1].