4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.

5,3-AB-CHMFUPPYCA is an analytical reference standard that is structurally classified as a synthetic cannabinoid.

5,6-Dihydro-5-azacytidine|cas 62488-57-7

5-Aminolevulinic acid HCl

5-Azacytidine is a potent growth inhibitor and a cytotoxic agent. 5-Azacytidine acts as a demethylating agent by inhibiting DNA methyltransferase (Dnmt), forming covalent adducts with cellular DNMT1 depleting enzyme activity. 5-Azacytidine also improves t

5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3).

5'-Cytidylic acid is a nucleotide that is used as a monomer in RNA.

5-FAM SE is a single isomer, it is one of the most popular green fluorescent reagents used for labeling peptides, proteins and nucleotides.

5-Fluorouracil is a potent antitumor agent that affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools.

5-Formyl-2-pyrimidinecarbonitrile is a chemical intermidate..

5'-GTP trisodium salt hydrate is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.

5-HT2C receptor antagonist that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2Breceptors respectively. Also displays selectivity over a range of other 5-HT, dopamine and adrenergic receptors. Brain penetrant; exerts anxiolytic-like activity.

5-Iodotubercidin (Itu) has been shown to inhibit mitogen-activated protein kinase (ERK2) (Ki = 525 nM), adenosine kinase (ADK) (Ki = 30 nM), casein kinases 1 & 2 (CSNK1A1 & CSNK2A1), protein kinase A (PKA) and insulin receptor kinase (IC50 ranging from 0.

5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors.

5MPN a first-in-class, selective, competitive, orally available inhibitor of PFKFB4 with Ki of 8.6 uM, does not inhibit PFK-1 or PFKFB3.

5-NIdR (5-nitro-indolyl-2'-deoxynucleoside) is a non-natural nucleotide produces cytostatic and cytotoxic effects against human leukemia cells by altering cell-cycle progression.

5-NITP (5-nitro-indolyl-2'-deoxyribose triphosphate) is a non-natural nucleotide that inhibits ribonucleotide reductase (hRR) with IC50 of 170 uM, demonstrates anti-cancer effects against leukemia cells by altering cell-cycle progression..

5-R-Rivaroxaban is (R) enantiomer of Rivaroxaban.

5S rRNA modificator is a suitable electrophile for 2’-hydroxyl acylation on structured RNA molecules, yielding accurate structural information comparable to that obtained with existing probes; 5S rRNA RNA modification.

666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM.

6-Dimethylaminopurine is a serine threonine protein kinase inhibitor. It inhibits the germinal vesicle breakdown and the meiotic maturation of oocytes.

6-Ethylthioinosine (6-ETI.

6-FABA (6-Fluoroanthranilic Acid) is a small-molecule inhibitor of MTB tryptophan synthesis that converts Mtb into a tryptophan auxotroph and restores the efficacy of a failed host defense.

6-FAM SE is another isomer of carboxyfluorescein.

6-Fluorescein isothiocyanate(6-FITC) is a derivative of fluorescein used in wide-ranging applications including flow cytometry.

6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C).

6-Hydroxybentazon is a phase I metabolite of bentazone, and bentazone is a chemical for use in herbicides.

6-Hydroxy-DL-DOPA is a small-molecule that disrupts with RAD52 oligomerization, inhibits ssDNA binding by RAD52 with IC50 of 1.1 uM and by RAD52 (1 209) with IC50 of 1.6 uM.

6-Mercaptopurine Monohydrate is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.

6-MITC is an inhibitor of viability of both PANC-1 and BxPC-3 cells. It also acts as an inhibitor of the expression of CSC signaling molecule SOX2.

6-MOMIPP is a novel microtubule disruptor that targets the colchicine binding site on β-tubulin, induces mitotic arrest, caspase activation and loss of cell viability of U251 glioblastoma in vitro.

6-OAU(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.

6-Thioguanine(6-TG) belongs to the thiopurine family of drugs that also include mercaptopurine and azathioprine, which are examples of antimetabolites; it is a purine analogue of the nucleobase guanine.

7,8-Dihydroxyflavone acts as a potent and selective small-molecule agonist of the TrkB receptor (Kd ≈ 320 nM), the main signaling receptor of brain-derived neurotrophic factor (BDNF).

7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.

7-Aminocephalosporanic acid is used for synthesis of cephalosporin antibiotics and intermediates.

7-BIA is a small molecule 7-butoxy illudalic acid analog that targets receptor-type protein tyrosine phosphatase D (PTPRD, IC50=1-3 uM) with some specificity.

7-Dehydrocholesterol is biosynthetic precursor of cholesterol and vitamin D3.

7DG (7-Desacetoxy-6,7-dehydrogedunin) is a selective inhibitor of protein kinase R (PKR) that directly interact with the C-terminal of PKR.

7-Epi 10-Desacetyl Paclitaxel is a paclitaxel impurity. The compound, originally isolated from Taxus yunnanensis, has shown potential growth inhibitory activities against human cancer cells.

7-epi-Taxol is a paclitaxel binds to tubulin, interfering with the normal function of microtubule.

8-Bromo-cAMP is a cell perbeable cyclic AMP (cAMP) analog and a PKA activator.

8-Hydroxy-efavirenz is the primary metabolite of the antiretroviral drug Efavirenz, stimulates the glycolytic flux in cultured rat astrocytes.

8-O-Acetyl shanzhiside methyl ester (ND01) is an iridoid glucoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant in Xi-zang.

8-OH-DPAT is a research chemical of the aminotetralin chemical class and has been widely used to study the function of the 5-HT1A receptor.

A 10-fold more potent lysosomal autophagy inhibitor than hydroxychloroquine (HCQ)..

A 2-cyanoaziridine derivative with antitumor activity in some types of cancer, including pancreatic, lung, breast, prostate, melanoma, and multiple myeloma.

A 385358 is a potent, selective, cell-permeable Bcl-XL inhibitor with Ki of 0.8 nM, displays >80-fold selectivity over Bcl-2 (Ki=64 nM).

A 4′-azidocytidine analogue that shows anti-HCV activity..

A 4′-azidocytidine analogue that shows anti-HCV activity..

A 419259 3Hcl is an apoptosis inducing agent that inhibits Src family kinases (c-Src).

A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.

A 922500 is a potent, selective, and orally bioavailable DGAT-1 inhibitor with IC50 values of 7 nM and 24 nM for human and mouse DGAT-1 respectively.

A angiotensin-converting enzyme (ACE) inhibitor for treatment of hypertension, heart failure, and after heart attacks..

A anti-HIV-1 compound that interferes with HIV-I integrase binding to viral DNA..

A benzodiazepine inhibitor that directly interacts with RUNX1 and CBFβ, represses RUNX1/CBFβ-dependent transactivation in reporter assays.

A benzofuran class inhibitor of M. tuberculosis Pks13 (Polyketide Synthase 13).

A benzophenone tetracarboxylic derivative that can improve the activity and stability of alkaline phosphatases from psychrophilic and mesophilic organisms..

A bioactive, specific small molecule that targets RNA of the expanded repeat (r(GGGGCC)exp) with Kd of 9.7 uM.

A biologically active natural product isolated from Streptomyces that has been shown to inhibit tumor cell migration.

A bis-anthracycline and melanoma selective agent that demonstrates anti-melanoma activity at low nanomolar concentrations.

A BIX-01294 derivative that inhibit malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death.

A B-Raf inhibitor, pyrazine and pyrrolo[2,3-b]pyridine derivatives, useful in the treatment of cancer and proliferative diseases.

A broadly selective, potent, ATP-competitive Akt kinase inhibitor with IC50 of 0.5 nM(biochemical assay), and 0.31 nM (cell function assay).

A broad-spectrum natural antifungal compound that acts as a selective and highly potent fungal Pkc1 kinase inhibitor.

A broad-spectrum RTKs inhibitor with IC50 ranging from 2 to 50 nM for VEGFR-1, VEGFR-2, PDGFRs, KIT, FLT3, and CSF1R/FMS.

A CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor that inhibits the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras (IC50s are 3 and >10 uM respectively).

Norverapamil HCl is a calcium channel blocker. It is the main active metabolite of verapamil.

A carbamate insecticide that acts as a fast-acting cholinesterase inhibitor..

A carbamate insecticide that acts as a fast-acting cholinesterase inhibitor..

A carboxamide fungicide used to control a broad spectrum of diseases on large variety of corps.

A carboxylic acid amide (CAA) fungicide..

A cardioselective beta blocker for the treatment of hypertension and arrhythmias..

Acebutolol HCl is a cardioselective beta-adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm as well as weak inherent sympathomimetic action.

A cell differentiation inducer that inhibits activation of NF-κB function, Akt and ERK/MAPK cascade.

A cell permeable CBP bromodomain inhibitor with Kd of 19 uM.

A cell permeable CBP bromodomain inhibitor with Kd of 19 uM.

A cell permeable, mechanistically unique inhibitor of protein sumoylation.

A cell-permeable benzochromene that selectively impairs the viability and growth of IGF2-overexpressing hepatocellular carcinoma cells, binds to MFP-2, stimulates the expression of IGFBP-1 and SOCS-3 through activation of STAT6.

A cell-permeable inhibitor of the KIX-KID interaction and CREB-mediated gene transcription (IC50=2.26 uM).

A cell-permeable mitochondrial calcium uptake inhibitor that binds to mitochondria with high affinity (Kd=340 pM) and blocks Ca2+ uptake into mitochondria in vitro with IC50 of 184 pM.

A cell-permeable peptide inhibitor of JNK kinase.

A cell-permeable small molecule inhibitor of Fumarase (fumarate hydratase), an enzyme of the tricarboxylic acid cycle (TCA cycle).

A cell-permeable synthetic peptide inhibitor of Bax conformational change and mitochondrial translocation.

A cell-permeable, small molecule inhibitor of the transcription factor STAT5 that exhibits anticancer activity and inhibits the growth of A549, HL-60 and K562 cells with IC50 of 8, 5 and 8 uM, respectively..

A cell-permeable, small-molecule c-Abl kinase activator with pEC50 of 6.1(EC50=794 nM).

BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca2+ release from intracellular stores or influx via Ca2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca2+ chelators.

A cellular cholesterol modifier that can form soluble inclusion complex with cholesterol.

A ceramide analog that inhibits glucosylceramide synthase (GCS), reduces the synthesis of sphingosine and its derivatives, increases cellular ceramide, and induces cell cycle arrest. .

A cerebral vasodilator that acts as a calcium blocker.

A chemical probe that consists of Ibrutinib linked to biotin via a long chain linker, has IC50 of 0.755-1.02 nM for Btk kinase.

A chemical with pesticide properties, belonging to the class of insecticides called insect growth regulators..

A class Ic antiarrhythmic agent used to prevent and treat tachyarrhythmias, works by blocking the Nav1.5 sodium channel in the heart, slowing the upstroke of the cardiac action potential.

Azimilide(NE-10064) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.

A clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux.

A clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux.

A combination of clofibrate and niacin, used to treat hyperlipidaemias

A combined adenosine receptor antagonist, p38 MAPK and PDE4 inhibitor, inhibits A1, A2b and A3 receptor (IC50=19, 21 and 80 nM), p38α, p38β and PDE4D (IC50=87, 400 and 22 nM).

A competitive inhibitor of HMG-CoA reductase that acts as a lipid-lowering agent for prevention of events associated with cardiovascular disease..

A competitive S1P receptor antagonist with pKi of 7.86 and 5.93 for S1P1 and S1P3, respectively, in radioligand binding assay.

RU-TRAAK-2 is a completely reversible TRAAK inhibitor, shows no activity for non-K2P channels (Kv1.2, Slo1 and GIRK2).

A conjugate of glucose and active alkylating moiety of ifosfamide with potentially enhanced selectivity for tumors that overexpress transmembrane glucose transporters.

A coumarin-based HIV-1 viral protein R (Vpr) inhibitor, inhibits Vpr-dependent viral infection of human macrophages.

A coumarin-based HIV-1 viral protein R (Vpr) inhibitor, inhibits Vpr-dependent viral infection of human macrophages..

A counterstain for background autofluorescence in fluorescence and immunofluorescence histochemistry, also is the first small molecule prion protein (PrP) ligand capable of inhibiting Aβ binding.

BTTAA is a Cu(I)-stabilizing ligand, whch performs potently with ubiquitin Glu18AzF.

A cyclooxygenase inhibitor. Structurally similar to Tenoxicam. An anti-inflammatory and an analgesic.

A cytokinin analog that displays potent antiproliferative activity against various human cancer cell lines.

A cytotoxic agent used in antibody-drug conjugates

A derivative of 8-hydroxyquinoline that has selectivity for rescuing the distinct toxicities caused by the expression of TDP-43, α-synuclein or polyglutamine proteins.

A derivative of EDTA that chelates iron and reduces the number of metal ions complexed with anthracycline and, consequently, decrease the formation of superoxide radicals.

A derivative of the antifungal drug itraconazole (ITA) as an inhibitor of MFB cell fate in resident fibroblasts derived from multiple murine and human tissues.

A derivative of the neurotransmitter GABA that acts as a GABAB receptor agonist.

A des acryl analogue of AZD9291 that is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant..

A diastereomer form of Taranabant, which is a potent, selective and orally active cannabinoid-1 receptor (CB1R) inverse agonist.

A dipeptide antibiotic that inhibits the initiation of protein synthesis.

A direct soluble guanylate cyclase (sGC) stimulator that acts independently of nitric oxide (NO).

A donepezil analog that can moderately inhibit acetylcholinesterase and metal-induced Aβ aggregation in vitro and shows disassembly of Aβ aggregates.

A donepezil analog that can moderately inhibit acetylcholinesterase and metal-induced Aβ aggregation in vitro and shows disassembly of Aβ aggregates.

A donepezil analog that can moderately inhibit acetylcholinesterase and metal-induced Aβ aggregation in vitro and shows disassembly of Aβ aggregates.

A doxorubicin analog that demonstrates anti-cancer activity without cardiotoxicity, does not inhibit topoisomerase IIβ activity at 100 uM.

A drug-like small molecule that prevents aminoglycoside-induced hair cell death in zebrafish and in mammals..

A drug-linker conjugate for Antibody-drug conjugates (ADCs) by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the cleavable peptide Val-Cit-PAB..

A dual action as an alkylating agent and topoisomerase inhibitor with potent activity against anthracycline- and cisplatin-resistant tumor cancer.

A dual antagonist of TP1 and EP4 receptors that inhibit TXA2-induced platelet aggregation with IC50 of 0.26 uM.

A dual inhibitor of E selectin and CXCR4 with IC50 of 3.6 uM and 1.1 uM respectively, blocks adhesion of AML blasts to E-Selectin, mobilizes human AML engrafted in mice.

A dual inhibitor of E selectin and CXCR4 with IC50 of 4.1 uM and 30 nM respectively, blocks adhesion of AML blasts to E-Selectin, mobilizes human AML engrafted in mice.

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 guanosine analogue antiviral agent used for the treatment of various herpesvirus (HSV) infections.

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 inhibitor of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.

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..