Gingerenone A is a Nrf2-Gpx4 activator with anti-breast-cancer properties. Gingerenone A results a delayed G2/M in cancer cells, following oxidative stress and senescence responses. Gingerenone A also alleviates ferroptosis in secondary liver injury (SLI) in dextran sodium sulfate (DSS)-induced colitis mice. Gingerenone A can be isolated from Zingiber officinale.

A dual inhibitor of TNF-α and TGF-β1 by inhibiting IκB kinase phosphorylation and Smad3 phosphorylation.

Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.IC50 value: 1.3/0.7 nM(OX1/OX2 receptor) [1] [2]Target: Dual OX!/OX2 receptorin vitro: [(3)H]Almorexant bound to a single saturable site on hOX(1) and hOX(2) with high affinity (K(d) of 1.3 and 0.17 nM, respectively. In Schild analyses using the [(3)H]inositol phosphates assay, almorexant acted as a competitive antagonist at hOX(1) and as a noncompetitive-like antagonist at hOX(2). In binding kinetic analyses, [(3)H]almorexant had fast association and dissociation rates at hOX(1), whereas it had a fast association rate and a remarkably slow dissociation rate at hOX(2) [1]. in vivo: During the 12-h dark period after dosing, ALM(Almorexant) exacerbated cataplexy in TG mice and increased nonrapid eye movement sleep with heightened sleep/wake fragmentation in both genotypes. ALM showed greater hypnotic potency in WT mice than in TG mice. The 100 mg/kg dose conferred maximal promotion of cataplexy in TG mice and maximal promotion of REM sleep in WT mice. In TG mice, ALM (30 mg/ kg) paradoxically induced a transient increase in active wakefulness [3]. Almorexant 200 mg showed significantly less 'Drug Liking' than both zolpidem doses (p < 0.01), and almorexant 400 mg had smaller effects than zolpidem 20 mg (p < 0.05), while almorexant 1,000 mg was not different from either zolpidem dose [4].

trans-ACPD is a selective agonist for metabotropic glutamate receptors, acting at both group I and group II mGlu receptors.

A first-generation antihistamine that acts primarily as H1 receptor antagonist.

A first-in-class analogue of unacylated ghrelin, and unacylated ghrelin receptor agonist.

A first-in-class antitumor and antimetastatic agent that induces necrosis in breast cancer tumors, inhibits inhibit mitochondria complex I activity and reduces HIF-1α stabilization.

A first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM).

A first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM).

A first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM).

A first-in-class, selective, orally bioavailable, dual inhibitor of BTK and PI3Kδ kinases with IC50 of 32.3 nM and 16.9 nM, respectively.

A first-in-class, small molecule protein-protein inhibitor of the interaction between the E1 and E2 proteins of HPV types 6 and 11.

A form of dynorphin and an endogenous opioid peptide with the amino acid sequence: Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys..

A fourth-generation fluoroquinolone antibiotic that inhibits the bacterial DNA gyrase and topoisomerase IV.

A fourth-generation fluoroquinolone antibiotic that inhibits the bacterial DNA gyrase and topoisomerase IV.

A fourth-generation fluoroquinolone antibiotic that inhibits the bacterial DNA gyrase and topoisomerase IV.

A fourth-generation synthetic fluoroquinolone, broad-spectrum antibacterial agent that is active against both Gram-positive and Gram-negative bacteria.

A fucose analog that inhibits Dll-induced Notch signaling by reducing Notch ligand Dll1-Notch1 binding, but not Jag1.

A fungal natural product that binds to HuR and inhibits HuR-RNA interaction in vitro with IC50 of 1.2 uM.

A GABA receptor agonist and modulator of glutamatergic systems.

A GABA transport inhibitor with IC50 of 5, 21, 388 and 140 uM for hGAT-3, rGAT-2, hGAT-1 and BGT-1, respectively.

A gain-of-function ligand for PGRMC2 (progesterone receptor membrane component 2) to promote adipogenesis.

A galactose analogue that is an UDP-glucose ceramide glucosyltransferase (UGCG/GCS) inhibitor (IC50=41.4 uM).

A glycolytic inhibitor that inhibits hexokinase II activity, suppresses ATP production, and induces endoplasmic reticulum (ER) stress.

A glycyrrhetinic acid derivative that inhibits 11β-hydroxysteroid dehydrogenase (11β-HSD), a gap junction blocker and mineralocorticoid agonist..

A glycyrrhetinic acid derivative that inhibits 11β-hydroxysteroid dehydrogenase (11β-HSD), a gap junction blocker and mineralocorticoid agonist..

A growth hormone-release inhibiting factor used in the treatment of severe, acute hemorrhages of gastroduodenal ulcers.

A HDAC inhibitor that selectively inhibits the catalytic activity of class I HDACs, and induces proteasomal degradation of HDAC2.

A HDAC inhibitor that selectively inhibits the catalytic activity of class I HDACs, and induces proteasomal degradation of HDAC2.

A herbicide agent. .

A herbicide safener for gramineous crops..

SPDP (SPDP Crosslinker) is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls. It is a glutathione cleavable ADC linker u

A heterobifunctional cross-linking reagent incorporating an extended spacer with amine and sulfhydryl reactivity.

A heterobifunctional small molecule PROTAC capable of cereblon mediated proteasomal degradation of CDK9.

PD 404182 is a high affinity inhibitor of KDO 8-P synthase (Ki = 26 nM). Also inhibits dimethylarginine dimethylaminohydrolase 1 (DDAH1). Exhibits antiangiogenic and antiviral activity in vitro. Putative antibiotic against gram-negative bacteria.

A heterocyclic quinone antibiotic that inhibits RNA synthesis in vivo and in vitro.

A high affinity, selective inhibitor of Rho family GTPases with EC50 of 16-120 uM.

A high-affinity, allosteric HIV-1 and HIV-2 reverse transcriptase inhibitor (NNRTI) with EC50 of 1 nM.

A high-affinity, selective platelet integrin αIIbβ3 receptor antagonist with IC50 of 96 nM.

A highly potent agonist of σ1 receptor with Ki of 0.8 nM.

A highly potent and competitive S-adenosylhomocysteine hydrolase inhibitor with Ki of 0.05 nM, also inhibits histone methyltransferase EZH2.

A highly potent and selective antagonist of the platelet P2Y1 receptor with Ki of 0.78 nM.

A highly potent and selective antagonist of the platelet P2Y1 receptor with Ki of 0.78 nM.

A highly potent and selective dual FAAH/MAGL inhibitor with IC50 of 1-3 nM against FAAH, inhibits mouse (IC50=410 nM) and human (IC50=1.4 uM) MAGL.

A highly potent and selective GRK2 inhibitor with IC50 of 18 nM.

A highly potent and selective inhibitor of CBP/p300 bromodomain with Kd of 0.23/0.47 uM respectively, with high selectivity over all other BD families, including the BET family.

A highly potent and selective inhibitor of the apical sodium-dependent bile acid transporter (ASBT) in development for the treatment of nonalcoholic steatohepatitis (NASH)..

A highly potent and selective inhibitor of the apical sodium-dependent bile acid transporter (ASBT) in development for the treatment of nonalcoholic steatohepatitis (NASH)..

A highly potent and selective kappa Opioid receptor (KOR) antagonist with Ki of 0.3 nM.

A highly potent and selective platelet activating factor (PAF) antagonist.

A highly potent and selective platelet activating factor (PAF) antagonist.

A highly potent and selective tankyrase inhibitor with pIC50 of 8.5 and 8.1 for TNKS1 and TNKS2, respectively.

A highly potent glucagon receptor antagonist..

A highly potent sigma receptor agonist with Ki of 1.7 nM and 25.2 nM for σ1 and σ2, respectively.

A highly potent, brain-penetrating ORL1 receptor (NOP receptor) agonist with Ki of 0.76 and 0.50  nM for rat and human ORL1 receptors, respectively.

A highly potent, functionally selective mGlu2 receptor agonist with EC50 of 13.6 nM in GTPγS functional binding assay.

A highly potent, long acting muscarinic receptor M3 antagonist with pIC50 of 9.8, inhibits M3 receptor in guinea pig trachea with pA2 of 9.4.

A highly potent, long-acting, orally active DPP4 inhibitor with Ki of 0.6 nM.

A highly potent, orally active hedgehog signaling (Hh) inhibitor with IC50 of 4.4 nM in Gli-luc reporter assays.

A highly potent, orally active VEGFR-2 inhibitor with IC50 of 8.5 nM, without activity against PKA, PKCα, PDK-1 and JNK3 (IC50>1 uM).

A highly potent, orally bioavailable, pan-VEGFR inibitor with IC50 of 1, 5, 3 nM for VEGFR1, 2, 3, respectively.

A highly potent, selective 5-HT2C receptor antagonist with pKi of 8.4 and 8.5 for human and rat 5-HT2C, respectively.

A highly potent, selective and orally active antagonist of CB2 receptor with Ki of 0.6 nM.

A highly potent, selective and orally bioavailable trace amine-associated receptor 1 (TRRA1) full agonist with EC50 of 18 nM, >500-fold selectivity over human adrenergic α2A receptor.

A highly potent, selective and orally bioavailable trace amine-associated receptor 1 (TRRA1) partial agonist with EC50 of 17 nM, >1,000-fold selectivity over human adrenergic α2A receptor.

A highly potent, selective and time-dependent Cdc7 kinase inhibitor with IC50 of 0.7 nM with slow dissociation property, with 200-fold and >14,000-fold selectivity over CDK2 and ROCK1, respectively.

A highly potent, selective beta-hairpin mimetic CXCR4 inhibitor with IC50 of 1.2 nM in Ca2+ flux assay.

A highly potent, selective beta-hairpin mimetic CXCR4 inhibitor with IC50 of 1.9 nM in Ca2+ flux assay.

A highly potent, selective CGRP receptor antagonist with Ki of 21 pM in in vitro binding assay and IC50 of 0.12 nM in cell-based functional assay.

A highly potent, selective EZH2 inhibitor with biochemical IC50 of 2 nM, cellular EC50 of 32 nM.

A highly potent, selective imidazoline I2 receptor agonist with Ki of 9.8 nM, enhances supraspinal morphine analgesia in mice..

A highly potent, selective inhibitor of checkpoint kinase TTK/Mps1 with IC50 of 0.6 nM.

A highly potent, selective mutant p53 (R175H, R249S, R273H, R273C) reactivator.

A highly potent, selective P2Y1 receptor agonist with EC50 of 1.2 nM.

A highly potent, selective platelet activating factor (PAF) inhibitor with IC50 of 75 and 170 nM for aggregation inhibition of rabbit and human platelets induced by PAF.

A highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator with Ki of 0.9 nM, IC50 of 2.5 nM.

A highly potent, selective, and orally bioavailable 11β-HSD1 inhibitor with IC50 of 2.9 and 1.6 nM for hHSD1 and mHSD1, respectively.

A highly potent, selective, and orally bioavailable factor Xa (FXa) inhibitor with Ki of o.19 nM, >5,000-fold selectivity over a series of related serine proteases.

A highly potent, selective, and orally bioavailable factor Xa (FXa) inhibitor with Ki of o.19 nM, >5,000-fold selectivity over a series of related serine proteases.

A highly potent, selective, brain-penetrating and orally active phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 0.61 nM.

A highly potent, selective, orally active mGluR5 negative allosteric modulator with Ki of 5.4 nM, IC50 of 3.1 nM.

A highly potent, selective, orally active renin inhibitor with IC50 of 2.1 nM in hPRA assay.

A highly potent, selective, orally available Src family kinase inhibitor with IC50 of <0.5 nM, <0.5 nM and for Src, Yes and Fyn kinases respectively, >950-fold selectivity for Src over ABL.

A highly potent, selective, orally bioavailable HCV NS5B polymerase inhibitor with IC50 of 9, 4, and 18 nM for GT1a, GT1b, and GT1b-C316N mutant in HCV replicon assay, respectively.

A highly potent, selective, second generation prostaglandin E2 subtype 4 receptor (EP4) antagonist with Ki of 0.56 nM.

A highly potent, specific and cell permeant inhibitor of human proline endopeptidase (PE) with Ki of 1 nM.

A highly potent, subtype-selective agonist of 5-HT2C receptor with Ki of 10.5 nM, >20-fold selectivity over 5-HT2A and 5-HT2B receptor subtypes (IC50=212 and 485 nM, respectively).

A highly potent, subtype-selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 17 nM, without inhibitory activity for MCHR2 at 10 uM.

A highly selective and potent GRK2 (G protein-coupled receptor kinase 2) inhibitor with IC50 of 130 nM.

A highly selective CYP17A1 (17,20-lyase) inhibitor with IC50 of 17 nM for human 17,20-lyase.

A highly selective inhibitor of the FMN riboswitch that controls expression of de novo riboflavin (Vitamin B2) biosynthesis in Escherichia coli.

A highly selective, non-ATP competitive substrate-pocket-directed Src/pretubulin inhibitor.

A highly selective, non-peptide agonist of the δ-opioid receptor (δ-OR) with IC50/Ki of 2.73/0.18 nM.

A highly selective, potent, BBB penetrant and orally bioavailable 5-HT6R antagonist for the treatment of neurological disorders such as AD and schizophrenia.

A highly selective, potent, BBB penetrant and orally bioavailable 5-HT6R antagonist for the treatment of neurological disorders such as AD and schizophrenia.

A highly selective, small molecule inhibitor of the miRNA regulatory complex RISC subunit SND1.

A highly specific myosin II ATPase inhibitor.

A higly potent, orally bioavailable, BBB permeable 5-HT7 receptor antagonist with Ki of 153 pM, with slightly lesser potency toward 5-HT6, 5-HT2A and 5HT-2C (Ki = 1.2-2.0  nM).

A hit compound that inhibits the proliferation of human peripheral blood T cells stimulated with anti-CD3 with IC50 of <10 nM, inhibits TCR-Nck interaction..

A HIV-1 surface-membrane inhibitor, also is a Fap1-blocking small molecule that replicates SLV peptied functions.

A homogenous mixture of compound that is used to stain amyloid plaques, binds to amyloid fibrils but not monomers and gives a distinct increase in fluorescence emission..

A homoisoflavanone found in Caesalpinia sappan, a potent, selective IMPDH2 inhibitor that covalently binds to Cys140 with Kd of 3.944 nM, almost 10 times lower than the Kd of binding to IMPDH1.

CM-11 is a homo-PROTAC, bivalent small-molecule dimerizer of the VHL E3 ubiquitin ligase to induce self-degradation.

A hormonally active metabolite of vitamin D that binds to vitamin D receptor (VDR).

A hyperpolarization-activated cyclic nucleotide-gated (HCN) channel.

A imidazoline compound that stimulate insulin release by inhibition of ATP-dependent K+ channels and inducing of Ca2+ mobilization in mouse pancreatic beta-cells.

A linear sulfated polysaccharide extracted from red edible seaweeds, shows topical microbicide activity targeting HIV viruses.

A locally-acting nonsteroidal anti-inflammatory drug (NSAID) with local anaesthetic and analgesic properties for pain relief and anti-inflammatory treatment of inflammatory conditions.

A long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma.

A loop diuretic used to treat high blood pressure and the swelling, a novel ligand and inhibitor of MAP2K6 kinase that inhibits MAP2K6 in part through alkylation of a nonconserved cysteine residue.

A low micromolar (EC50=9.7 uM, K2P2.1), selective activator of temperature- and mechano-sensitive K2P potassium channels.

A macrolide antibiotic that effectively inhibits tumor angiogenesis by suppressing VEGFR2-mediated signaling pathways in lung cancer.

A Mannich base compound, selective and orally active JAK3 inhibitor that blocks IL-2-induced activation of JAK3 and downstream substrates STAT5a/b.

A marine sponge alkaloid that inhibits Chk1 and Chk2 with IC50 of 3 and 3.5 uM, respectively.

A melanoma-selective anticancer agent (IC50=30 nM, Malme-3M cell line), induces cell death by autophagocytosis, targeting the cancer-protective protein dermcidin.

A melatonin receptor agonist of MT1 (Ki=0.1nM) and MT2 (Ki=0.12nM), and a 5-HT2C (Ki=631nM) receptor antagonist.

A melatonin receptor agonist of MT1 (Ki=0.1nM) and MT2 (Ki=0.12nM), and a 5-HT2C (Ki=631nM) receptor antagonist.

A membrane permeable IP3 receptor antagonist and broad TRP channels (TRPC5, TRPM2) blcoker.

A membrane-impermeable sodium channel blocker, blocks sodium current in voltage-clamped nociceptive DRG neurons.

A metabolite of Gefitinib, which is a potent inhibitor of tyrosine phosporylation in EGFR..

A metabolite of ST1535, which is potent, selective A2A adenosine receptor antagonist with Ki of 6.6 nM..

A metabolite of tamoxifen, orally active non-steroidal selective estrogen receptor modulator (SERM) for the treatment of estrogen receptor-positive breast cancer..

A mitochondriotoxic small molecule that selectively inhibits proliferation of mammary epithelial, neu-overexpressing cells, as well as a variety of mouse mammary tumor and human breast cancer cell lines.

A moderately potent, but highly selective α2-adrenoceptor antagonist, the only reported selective antagonist at the α2B-adrenoceptor not having potent α1-adrenoceptor antagonist activity.

A multichannel blocker agent that has antiarrhythmic activity.

A mycotoxin produced from F. moniliforme, and an inhibitor of ceramide synthase (sphingosine N-acyltransferase/CerS).

A nanomolar potent, selective, and orally bioavailable glycine transporter type-1 (GlyT1) inhibitor for the treatment of negative symptoms associated with schizophrenia.

Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice.

Dip G is a natural compound, novel chemical probe reciprocally stabilizes ERβ and destabilizes ERα in breast cancer cells; targets CHIP ubiquitin E3 ligase to modulate ER protein stability, enhances the transcription and anti-proliferative activities of ERβ, while attenuating the transcription and proliferative effects of ERα; the first small molecule that can restore the balance of ERα and ERβ.

A natural furanocoumarin that is found to be a potent inhibitor of debenzylation activity of CYP3A4 enzyme with IC50 of 24.92 uM.

A natural poduct that functions as a splicing inhibitor with IC50 of 35 uM, blocks a late stage of spliceosome assembly..

A natural tetranortriterpenoid compound that inhibits Hsp90 and induce the degradation of Hsp90-dependent client proteins.

A naturally occurring nucleoside analog that possesses antitumor activity, also is a potent and efficacious readthrough agent.

A naturally occurring tetranortriterpenoid that has been found to act as a potent, selective, small-molecule agonist of TrkB with Kd of 1.4 uM.

A negative allosteric modulator of the Frizzled4 (Fzd4) receptor and a Wnt/β-catenin pathway inhibitor with pEC50 value of 5.74 for inhibition of Wnt antagonism.

A negative control of VU-WS113, which is a potent inhibitor of Wnt signaling with EC50 of 80 nM that selectively potentiates CK1α kinase activity..

A neuropeptide derived from the same precursor polypeptide as neurotensin, and with similar but subtly distinct expression and effects..

A new broad spectrum industrial microbicide with applications in material and coating preservation. .

A new compound which is similar with +JQ-1，BET bromodomain inhibitor

A new-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of HIV-1 infections, the prodrug of the active compound VM-1500A..

A newly identified, small molecule HuR inhibitor that disrupts HuR multimerization modules and reduces tumor cell survival and proliferation..

A noncovalent small molecule binder to Keap1 (Kd=6 uM) and selective activator of Nrf2 signaling.

A non-immunosuppressive FTY720 analogue, PKCδ activator with higher antiproliferative potency with IC50 of 2.4, 2.4, and 3.5 uM in Huh7, Hep3B, and PLC5 cells, respectively.

A non-ionic emulsifying agent that can modulate multidrug resistance and enhances antitumor activity of vinblastine sulfate by modulating substrate-stimulated P-gp ATPase activity.

A nonnucleoside, competitive, small-molecule inhibitor of human ribonucleotide reductase (hRR) that binds to the large subunit hRRM1 at the catalytic site (C-site) with Kd of 37.4 uM, IC50 of 32 uM.

A non-peptide small molecule agonist of the PTH1 receptor, activates both the cAMP and calcium signaling pathways..

A nonpeptide, cell-permeable STAT3 inhibitor that binds directly to the pTyr705 binding site of the STAT3 monomer.

A non-peptide, centrally-penetrant and selective agonist of GHSR with appetite-enhancing and anabolic effects.

A non-peptide, selective RGS4 inhibitor that inhibits RGS4/Gα(o) binding with 3 to 5 uM potency.

A nonpeptidic, selective, brain-penetrant agonist of nociceptin/orphanin FQ receptor (NOP receptor/ORL1) with pKi of 9.41.

A nonpeptidyl small molecule agonist of GDNF family receptor α1 (GFRα-1).

A non-planar analogue of fascaplysin that selectively inhibits CDK4/cyclin D1 with IC50 of 5.5 uM.

A non-selective agonist of Adenosine A3 receptor.

A non-selective agonist of the dopamine D3 receptor (Ki=0.71 nM).

A non-selective agonist of the dopamine D3 receptor (Ki=0.71 nM).

A non-selective beta blocker used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent..

A non-selective group I/group II metabotropic glutamate receptor (mGluR) antagonist..

A nonselective inhibitor of UBL protein-activating E1 enzymes that forms covalent adducts with UBL proteins SUMO1, ubiquitin, Nedd8, ISG15, and GABARAP in the presence of ATP and E1 enzymes in vitro.

A non-steroidal anti-inflammatory drug (NSAID).

A nonsteroidal selective estrogen receptor modulator (SERM) that shows 10- to 60-fold increased affinity for the estrogen receptor compared with Tamoxifen.

A non-steroidal sulphamate analogue of 2-methoxyoestradiol (2ME2) and microtubule disruptor, shows anti-proliferative activity against NCI 60 cell lines with mean GI50 of 50 nM.

A nontoxic heat shock protein (HSP) coinducer and potentiator of the heat shock response.

A nontoxic, orally active heat shock protein (HSP) coinducer and potentiator of the heat shock response.

A nootropic agent that enhances high-affinity choline uptake.

A nove potent, dual FGFR and PIK3C3 inhibitor with Kd of 0.53 nM for PIK3C3.

A nove potent, selective and reversible SHP2 inhibitor with Ki of 0.51 uM.

A novel 5-HT receptor antagonist for the treatment of Parkinson's disease..

A novel a potent, selective inhibitor of BRD4 with Kd of 550 nM, cellular IC50 of 724 nM.

A novel allosteric, noncompetitive dual CXCR1/2 inhibitor that inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 in vitro with IC50 of 0.7 nM.

A novel allosteric, noncompetitive dual CXCR1/2 inhibitor that inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 in vitro with IC50 of 0.7 nM.

A novel and highly selective 5-HT6 receptor small molecule antagonist with Ki of 2.34 nM.

A novel and irreversible inhibitor of mutant K-ras G12C..

A novel and irreversible inhibitor of mutant K-ras G12C..

A novel and irreversible inhibitor of mutant K-ras G12C..

FT011 is an anti-fibrotic agent, reduces mRNA expression of collagens I and III and inhibits collagen synthesis.

A novel antifolate modulator compound..

Olorofim (F901318) selectively inhibits fungal dihydroorotate dehydrogenase (DHODH), a key enzyme in the pyrimidine biosynthesis pathway. Olorofim (F901318). Olorofim exhibits excellent activity against A. fumigatus and other Aspergillus spp.

A novel antiprion compound with EC50 of 68 nM, significantly increases monoglycosylated/diglycosylated PrPSc..

A novel anti-TB agent that has an MIC range of 0.06-0.5 ug/mL..

A novel anti-TB agent that has an MIC range of 0.06-0.5 ug/mL..

A novel bifunctional PDE4 inhibitor (IC50=5 nM) and long acting β2-adrenoceptor agonist (EC50=8 nM).

A novel brain penetrant antiprion compound with EC50 of 57 nM, prevents both PrP(Sc) accumulation and astrocytic gliosis in the cerebrum.

A novel bromodomain BRD4 inhibitor that significantly induces HIV-1 reactivation.

A novel cardiotonic agent that acts as a calcium sensitizer with no chronotropic activity in mammalian cardiac muscle, elicits positive inotropic effect in dog and rabbit ventricular muscles (EC50=9.2 uM).

A novel cell membrane impermeable smoothened antagonist with IC50 of 7.6 nM in Hh-dependent Gli transcriptional activity assay.

A novel cell permeable smoothened antagonist with IC50 of 3.1 nM in Hh-dependent Gli transcriptional activity assay.

A novel chemical probe that enable selective 2’-hydroxyl acylation for accurate RNA structural analysis in living cells..

A novel compound that disrupts the HIV-1 integrase LEDGF interaction.

Dotinurad is a novel compound that exhibits a remarkable uric acid excretion-promoting action.

A novel conformational modulator of α-synuclein with EC50 of 105 uM, potentially outcompetes spermine in binding to α-synuclein.

GB111-NH2 (Z-Phe-Lys-AOMK) is a novel cysteine cathepsin inhibitor that blocks the activity of cathepsins B, L and S. GB111-NH2 (Z-Phe-Lys-AOMK) inhibits autophagy and increases oxidative stress, specifically trigger macrophage cell death.

A novel dansylated analog of purvalanol B, and a CDK inhibitor that inhibits cell cycle progression and proliferation in prostate and breast cancer cells more effectively than purvalanol B.

A novel diaryldiamine that inhibits bacterial methionyl-tRNA synthetases in Gram-positive bacteria as a novel agent to treat Clostridium difficile infection (CDI).

A novel dual inhibitor of mTOR and DNA-PK with IC50 of 21 nM and 13 nM, respectively.

A novel dual-acting steroid sulfatase inhibitor (IC50=0.1 uM) and selective ERα modulator (SERM).

Benzenepentacarboxylic acid is a fluorescent dye that detects and scavenge HO radicals.

A novel FTY720 analog that acts as PP2A activator, disrupts the SET/PP2A interaction devoid of immunosuppressive effects leads to the reactivation of PP2A.

A novel highly potent, selective, long acting muscarinic receptor M3 antagonist with pIC50 of 9.8, 10-fold selectivity over M2 (pIC50=9.0).

A novel histamine H3 receptor inverse agonist for the treatment of sleep apnoea syndrome.

A novel HIV-1 non-catalytic-site integrase inhibitor (NCINI).