KI-7 is an adenosine A2B receptor positive allosteric modulator.

Amiloride hydrochloride (Amiloride HCl) is an effective sodium channel blocker of epithelial.

HS 014 acetate is a potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake in rats and nociception in mice following central

Lys-[Des-Arg9]Bradykinin acetate is an endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9]-Bradykinin.

Novokinin acetate exhibited an affinity for the AT2 receptor with Ki of 7 nM, and its antihypertensive and vasorelaxing activities were blocked by PD123319, an AT2 receptor antagonist.

(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) acetate is a highly potent antagonist of parathyroid hormone (PTH) The Ki value is 69 nM in bovine renal cortical membrane.

M40 acetate is a potent, non-selective galanin receptor antagonist (Ki values are 1.82 and 5.1 nM at GAL1 and GAL2 respectively) that inhibits galanin (1-29) binding in rat brain in vitro (IC50 = 3 - 15 nM). Attenuates the antidepressant effects of fluoxetine and blocks galanin-induced food intake in vivo. Also exhibits weak partial agonist activity at peripheral GAL2 receptors at doses > 100 nM.

PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR. PI3Kα/mTOR-IN-1 shows an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 12.5 nM and 10.6 nM for mTOR and PI3Kα in a cell free assay , respectively.

Lys-[Des-Arg9]Bradykinin,TFA is Endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9]-Bradykinin.

Orphanin FQ(1-11) acetate(178249-41-7 free base) is a peptide fragment containing amino acids 1-11 of Nociceptin. Orphanin FQ(1-11) acetate(178249-41-7 free base) is a potent agonist of the ORL1/KOR-3 receptor (Ki = 55 nM) and displays no affinity for opioid receptors, including μ, δ, κ1 and κ3 receptors (Ki >1000 nM). Orphanin FQ(1-11) acetate(178249-41-7 free base) displays analgesic properties in CD-1 mice.

YM90K (6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-) hydrochloride is an antagonist of AMPA receptor.

CRA-026440 hydrochloride is a potent and broad-spectrum HDAC inhibitor. CRA-026440 hydrochloride exhibits Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4 nM, 14 nM, 11 nM, 15 nM, 7 nM, and 20 nM, respectively. CRA-026440 hydrochloride exhibits antitumor and antiangiogenic activities.

7-Chlorokynurenic acid (7-chloro-4-hydroxy-2-carboxyquinoline) is an effecitve and selective antagonist of NMDA receptor with IC50 of 0.56 μM for the glycine B coagonist site. 7-Chlorokynurenic acid inhibits the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM and shows antinociceptive actions after neuraxial delivery.

1400W dihydrochloride (N-(3-(Aminomethyl)benzyl)acetamidine) is a highly effective and specific inhibitor of inducible NOS2 (iNOS).

ML-7 hydrochloride (ML-7 HCl) is a cell-permeable, reversible, effective, ATP-competitive, and specific inhibitor of myosin light chain kinase (Ki: 300 nM); also inhibits smooth-muscle myosin light chain kinase, PKA, and PKC.

Capromorelin Tartrate (CP 424391-18) is a potent, orally active growth hormone secretagogue receptor (GHSR) agonist (Ki: 7 nM for hGHS-R1a).

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg/ml) and Gram-negative bacteria (MICs = 136-200 µg/ml), as well as yeasts (MICs = 10-20 µg/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16/BL6 mouse model of melanoma when administered at a dose of 25 mg/kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg/kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg/ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg/kg.3Ajoene (25 mg/kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16/BL6 melanoma cells in C57BL/6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)

Nebentan (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2]. Nebentan inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB receptors in a concentration dependent manner,Ki values are 0.697 nM and 1.53 nM for human and rat endothelin ETA receptors, respectively. In contrast, YM598 exhibits low affinities for human and rat endothelin ETB receptors, with Ki values of 569 nM and 155 nM,respectively[1].In measurement of intracellular Ca2+ concentration, Nebentan concentration-dependently inhibits the increase in [Ca2+]i induced by 10 nM endothelin-1 in both CHO cells and A10 cells, the IC50 values are 26.2 nM for CHO cells and 26.7 nM for A10 cells, respectively[1]. Nebentan (oral administration; 0.1-1 mg/kg; 4 weeks) significantly inhibits the progression of pulmonary hypertension and the development of right ventricular hypertrophy[2].Nebentan (oral administration; 1 mg/kg; 30 weeks) significantly ameliorates the poor survival rate of CHF rats, it markedly reduces the hypertrophy of both ventricles as well as pulmonary congestion[2]. [1]. Hironori Yuyama, et al. Pharmacological Characterization of YM598, an Orally Active and Highly Potent Selective Endothelin ET(A) Receptor Antagonist. Eur J Pharmacol. 2003 Sep 30;478(1):61-71. [2]. Akira Fujimori, et al. YM598, an Orally Active ET(A) Receptor Antagonist, Ameliorates the Progression of Cardiopulmonary Changes and Both-Side Heart Failure in Rats With Cor Pulmonale and Myocardial Infarction. J Cardiovasc Pharmacol. 2004 Nov;44 Suppl 1:S354-7.

3-Cyano-7-hydroxycoumarin (3-Cyanoumbelliferone) is a macrophage inhibitor of macrophage inhibitory factor (MIF) interconjugate isomerase with a Ki of 2.9 μM. 3-Cyano-7-hydroxycoumarin belongs to the group of coumarin derivatives, which can be used as molecular probes and fluorescent dyes.

BIBS 39 is a new nonpeptide angiotensin II (AII) receptor antagonist.

Protein kinase inhibitor H-7 (5-(2-methylpiperazine-1-sulfonyl)isoquinoline) is a potent inhibitor of protein kinase C (PKC) with a Ki of 6 μM. Protein kinase inhibitor H-7 is also a cyclic nucleotide dependent protein kinase inhibitor.

CAIX Inhibitor S4 (S4) is an effective inhibitor of carbonic anhydrase IX/XII with a Ki of 7 nM and 2 nM, respectively. The Kis for CA II and CA I are 546 and 5600 nM.

1. N-Methylcytisine (Caulophylline)'s nicotinic receptors have high affinity (KD = 5 nM)to nAChR from squid optical ganglia. 2. N-Methylcytisine and N, N-dimethylcytisine did not displace 14C-tubocurarine at a concentration of .1 mM, cytisine was the only effective inhibitor of 14C-tubocurarine specific binding (Ki=7 nM).

Ac-DNLD-CHO (Ac-Asp-Asn-Leu-Asp-CHO) is an inhibitor of Caspase-3/7, exhibiting IC50 values of 9.89 nM and 245 nM, and approximate Ki values of 0.68 nM and 55.7 nM, respectively. This compound is utilized in the study of diseases associated with caspase-mediated apoptosis, including neurodegenerative and viral infection diseases [1].

The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2. CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM. The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-prostaglandin D2 with an IC50 value of 40 nM.

CXCR7 modulator 2 is a 7-type C-X-C chemokine receptor (CXCR7) modulator with a Ki of 13 nM.

Telaprevir (Incivek) (VX-950) is an effective inhibitor of HCV NS3-4A serine protease (IC50: 0.35 μM).

Vortioxetine hydrobromide (Lu AA21004 hydrobromide) is a serotonin (5-HT) modulator and stimulator (SMS), inhibits 5-HT1A/1B/3A/7 receptor and SERT (IC50: 15/33/3.7/19/1.6 nM).

GDC-0623 (RG 7421) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.

Navoximod (GDC-0919) (NLG- 919, GDC-0919) is a potent indoleamine-(2,3)-dioxygenase (IDO) pathway inhibitor (Ki/EC50: 7 nM/75 nM).

Lanicemine (AZD6765) dihydrochloride is a low-trapping blocker of the NMDA channel with Ki of 0.56-2.1 μM for NMDA receptor and IC 50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively. Lanicemine (AZD6765) dihydrochloride has sustained antidepressant efficacy [1].

(Rac)-Lanicemine ((Rac)-AZD6765) is the racemate of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker with Ki of 0.56-2.1 μM for NMDA receptor; IC 50 s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively. Lanicemine shows antidepressant effects [1].

RG-12525（NID 525） is an orally available, selective and competitive leukotriene D (LTD) antagonist that inhibits LTC4, LTD4 and LTE4-induced contraction of guinea pig thin-walled bands, with IC50 values of 2.6 nM, 2.5 nM, and 7 nM, respectively.RG-12525 inhibits CYP3A4, with a Ki value of 0.5 µM. RG-12525 is a novel and potent PPAR-γ agonist (IC50 value of about 60 nM) with species specificity for the study of asthma.

CAY10406 is a trifluoromethyl analog of an isatin sulfonamide compound that selectively inhibits caspases 3 and 7. The non-trifluoromethyl compound exhibits Ki values of 1.2 nM and 6 nM for caspases 3 and 7, respectively. For all of the other caspases tested, it is 100 to 1,000 times less potent. Caspases 3 and 7 are 'effector caspases' that are downstream from the initiating steps of apoptosis, and are implicated in the main proteolytic processing of the apoptotic signal. No data is currently available for caspase inhibition by CAY10406.

Reboxetine-d5 Mesylate is a deuterated compound of Reboxetine Mesylate. Reboxetine Mesylate has a CAS number of 98769-84-7. Reboxetine is a norepinephrine reuptake inhibitor (Ki: 8.2 nM).

Febuxostat-d7 is a deuterated compound of Febuxostat. Febuxostat has a CAS number of 144060-53-7. Febuxostat is a xanthine oxidase Inhibitor.

7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2.with anti-inflammatory activity

ONX-0914 (PR-957) TFA is a selective, noncompetitive, irreversible inhibitor targeting the chymotrypsin-like subunit (LMP7) of the immunoproteasome, effectively blocking cytokine production and mitigating the progression of experimental arthritis. With a K_i value of 5.2 μM against the mycobacterial proteasome, ONX-0914 TFA also facilitates the reactivation of latent HIV-1 by inducing p-TEFb activation through HSF-1 mediation [1] [2] [3].

Cercosporamide is a ATP-competitive Pkc1 kinase inhibitor (IC50 <50 nM; Ki <7 nM). It also is a unique Mnk inhibitor.

IRE1α kinase-IN-5 (compound 7) is a potent inhibitor of IRE1α (Ki: 98 nM) and is an ATP-competitive ligand for IRE1α.

hCAIX/XII-IN-1, a potent inhibitor of both CAIX and CAXII, exhibits KI values of 0.48 μM for CAIX and 0.83 μM for CAXII, respectively. This compound demonstrates antiproliferative activity in vitro and induces apoptosis in MCF-7 cells [1].

APJ receptor agonist 7 (compound 37) is an orally active APJ (apelin receptor) agonist (Ki: 0.059 μM). arrestin (EC50: 0.063 μM).

SKF89976A is a potent GABA uptake inhibitor, which is selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). SKF89976A inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). It is able to pass the blood-brain barrier after systemic administration and is active in vivo.

7-Deaza-2',3'-dideoxyguanosine (7-Deaza-ddG) is a 2′,3′-dideoxynucleoside 5′-triphosphate that inhibits HIV-1 reverse transcriptase with a Ki of 25 nM [1].

Ac-DEVD-CHO is a specific Caspase-3 inhibitor (Ki: 230 pM).Ac-DEVD-CHO has an inhibitory effect in SLNT-induced apoptosis.

AZD8797 (KAND567) is an orally available, selective and potent human CX3CR1-converting antagonist with inhibitory effects on CX3CR1 and CXCR2, and potentially protects against SARS-CoV-2-induced neuronal damage, preventing worsening of nociceptive sensitization and microglial activation in a migraine model of rats following seizures.

Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 microM), while not affecting ADP- or arachidonic acid-induced platelet aggregation [1]. The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7+/-0.4 microM, 3.2+/-0.7 microM and 1.5+/-0.4 microM, respectively whereas for loratadine the IC50 was 2.1+/-0.9 microM, 4.0+/-1.3 M and 1.7+/-0.5 microM. SR-27417A exhibited no inhibitory effect [2].in vivo: Rupatadine blocked histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 micrograms/kg i.v.). Moreover, it potently inhibited PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg/kg i.v.) [1]. rupatadine treatment improved the declined lung function and significantly decreased animal death. Moreover, rupatadine was able not only to attenuate silica-induced silicosis but also to produce a superior therapeutic efficacy compared to pirfenidone, histamine H1 antagonist loratadine, or PAF antagonist CV-3988 [3]. [1]. Merlos M, et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21. [2]. Queralt M, et al. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60. [3]. Lv XX, et al. Rupatadine protects against pulmonary fibrosis by attenuating PAF-mediated senescence in rodents. PLoS One. 2013 Jul 15;8(7):e68631.

CKI-7 free base is a potent and ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.

Merestinib dihydrochloride is an effective and orally bioavailable c-Met inhibitor (Ki=2 nM). It has anti-tumor activities and also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), RO

PCI-24781 (Abexinostat (PCI24781)) is a new pan-HDAC inhibitor mainly targeting HDAC1 (Ki: 7 nM), also have moderate inhibitory for HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2.