modest

Losulazine is a peripheral sympathetic antihypertensive compound that can be taken orally. Losulazine causes relatively modest, transient depletion of dopamine and norepinephrine in brain regions protected by the blood-brain barrier.

Dolutegravir sodium (GSK-1349572A) salt(DTG; GSK1349572) is an HIV integrase inhibitor(IC50: 2.7 nM), modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S Q148H.

A-674563 2HCl is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.

EB-47 mimics the substrate NAD+ and extends from the nicotinamide to the adenosine subsite.EB-47, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM.

OXFBD04 is a potent and selective BRD4 inhibitor (IC50= 166 nM), a BET bromodomain ligand with modest affinity for the CREBBP bromodomain, and exhibits anti-cancer activity.

Firategrast (SB 683699) is an orally active and specific α4β1 α4β7 integrin antagonist that reduces the transport of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity. It is used in relapsing-remitting multiple sclerosis, associated with modest reductions in CD4, CD8, and CD19 lymphocyte counts in cerebrospinal fluid.

Vesnarinone (Arkin) (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. It also suppresses cell proliferation and induces apoptosis by inducing the expression of p21, an inhibitor of cyclin-dependent kinase activity in p53-mediated cell cycle arrest.

Homodestcardin is a cyclic depsipeptide fungal metabolite that has been found in T. roseum and has immunosuppressant activity. It inhibits concanavalin A-induced proliferation of isolated mouse T cells.

Quisinostat (JNJ-26481585) (JNJ-26481585) is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7.

Pictilisib dimethanesulfonate (GDC-0941 2 MeSO3H salt) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

Quisinostat dihydrochloride (JNJ26854165(Quisinostat) 2HCl) is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2.

Aloveroside A, a triglucosylnaphthalene derivative extracted from Aloe vera using ethanol, exhibits modest inhibitory activity against bACE, demonstrating approximately 18.68% inhibition at a concentration of 100 μg/mL [1].

CAF-382 (compound B1), an analog of SNS-032, functions as a CDKL5 and pan-CDK inhibitor, exhibiting modest inhibitory activity against GSK3α/β with an affinity greater than 1.8 μM. It effectively inhibits CDKL5 and impedes the phosphorylation of the CDKL5 E2 domain [1].

Topoisomerase IIα-IN-8 (compound 15) serves as a modest inhibitor of human DNA topoisomerase IIα (htIIα), exhibiting an inhibitory concentration (IC50) of 462 ± 38.0 μM [1].

A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.

11-Oxomogroside II A1 (compound 7), an oxidized cucurbitin derived from the ethanol extract of Rohanberry fruit, inhibits the activation of Epstein-Barr virus (EBV) early antigen (EBV-EA) induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) and modestly inhibits the activation of (±)-(E)-methyl-2-[(E)-hydroxyimino]-5-nitro-6-methoxy-3-hexemide (NOR 1), a nitric oxide (NO) donor [1].

NEU-730, a novel inhibitor of TbrPDEB1, shows modest inhibition of T. brucei proliferation.

MOG (92–106), mouse, rat, is a biologically active peptide corresponding to the fragment of amino acids 92 to 106 in myelin oligodendrocyte glycoprotein (MOG) from mice and rats. Mice subjected to MOG (92–106)-induced experimental autoimmune encephalomyelitis show substantial B cell reactivity to secondary myelin antigens. Although this MOG fragment elicits only modest T cell responses, the resultant autoimmunity is profoundly severe. The peptide demonstrates encephalitogenic properties in various species, including SJL mice, DA rats, and rhesus monkeys.

Atrial natriuretic factor (1-28) from both human and porcine sources is a potent suppressor of pro-opiomelanocortin (POMC) mRNA, exerting only a modest inhibitory effect on βEP-LI release.

LP-935509 is highly brain-penetrant and reverses fully established pain behavior following the SNL procedure. LP-935509 is also an effective inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 is a selective, ATP-competit

Tetrahdroxysqualene shows antimycobacterial activity with an MIC of 10.0 microg/mL, while showing only modest cytotoxicity.

AI-4-57 Hydrochloride is a ligand to the CBFß. AI-4-57 Hydrochloride is a modest potency inhibitor of the binding of wildtype CBFß to the RUNX1 Runt domain.

Nicotelline, also known as Nicotellin, is an alkaloid associated with nicotine and acts as a modest inhibitor of the enzyme human cDNA-expressed cytochrome P-450 2A6 (CYP2A6), which is responsible for coumarin 7-hydroxylation. However, Nicotelline does not show inhibitory effects at a concentration of 300 μM. It serves as a tracer and biomarker for particulate matter (PM) originating from tobacco smoke [1] [2].

Ivachtin (Caspase-3 Inhibitor VII) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor(IC50 = 23 nM) and is a modest inhibitor of the remaining caspases.

Rucaparib hydrochloride, also known as AG014699, is a powerful and orally active compound that inhibits PARP proteins including PARP-1, PARP-2, and PARP-3 with a Ki value of 1.4 nM for PARP1. Additionally, Rucaparib hydrochloride acts as a modest inhibitor of hexose-6-phosphate dehydrogenase (H6PD). This compound shows potential in research for castration-resistant prostate cancer (CRPC) [1] [2] [3] [4].

SHP244 is an allosteric inhibitor of SHP2 with modest thermal stabilization of the enzyme.

VMY-1-101 is a synthesized fluorescent CDK inhibitor. VMY-1-101 demonstrates potent CDK inhibitory activity, enhanced induction of G2/M arrest and modest apoptosis as compared to purvalanol B.

L 653328 is an ocular hypotensive agent that has modest beta-receptor blocking activity.

Compound 11, labeled as a weak Hepatoprotective agent-1, is a naturally occurring substance extracted from the fruits of Arctium lappa L. It demonstrates modest hepatoprotective effects when applied at a concentration of 10 μM [1].

1,1′-Disinomenine, an alkaloid extracted from the stems of Sinomenium acutum, exhibits modest inhibitory activity against A549 and Hela cells [1].

Leriglitazone (Hydroxypioglitazone) hydrochloride, a pioglitazone metabolite, acts as a PPARγ agonist, effectively stabilizing the PPARγ activation function-2 (AF-2) co-activator binding surface to enhance co-activator binding, which results in a modest improvement in transcriptional efficacy. It binds to the PPARγ C-terminal ligand-binding domain (LBD) with a dissociation constant (K i) of 1.2 μM and demonstrates transcriptional efficacy with an effective concentration (EC 50) of 680 nM [1].

Harzianum A, a trichothecene isolated from the soil-borne fungus Trichoderma harzianum, exhibits no cytotoxicity against baby hamster kidney cells and lacks activity against both Gram-negative and Gram-positive bacteria. However, it demonstrates modest antifungal activity at a concentration of 100 μg/mL [1].

BMS-536924 (BMS 536924) is an ATP-competitive IGF-1R IR inhibitor with IC50 of 100 nM 73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1 2.

MKC3946 is an effective and soluble IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.

Coronarin B has cytotoxic activity, it also has modest antiplasmodial activity.

Przewalskin A and Przewalskin B showed modest anti-HIV-1 activity with EC50 = 41 and 30 microg/mL, respectively.

Ilexoside O, a triterpene saponin derived from Ilex pubescens roots, demonstrates modest inhibition of xanthine oxidase (XOD) activity with an IC50 value of 53.05 μM.

Azapropazone is anti-inflammatory agent. Azapropazone has uricosuric properties used to treat rheumatoid arthritis and ankylosing spondylitis. Azapropazone lowered plasma uric acid but exerted only a modest and variable uricosuric effect without altering

Icariside F2 shows modest α-glucosidase inhibitory (4.60±1.74% to 11.97±3.30%) and antioxidant activities. It also displays potent NF-κB inhibitory effects, with the IC50 value of 16.25 ± 2.19 uM.