nonpeptidic

BMS-202 (PD1-PDL1 inhibitor 2) is a non-peptide PD-1/PD-L complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 binds to PD-L1 with high affinity and blocks human PD-1/PD-L interactions, exhibiting antitumor activity.

Embelin (Embelic acid), isolated from the Japanese Ardisia herb, is an inhibitor of the X-linked inhibitor of apoptosis (IC50: 4.1 uM).

AS057278 (3-Methylpyrazole-5-carboxylic acid) is an D-amino acid oxidase (DAAO) inhibitor.

SARS-CoV-2 Mpro-IN-9 (compound c7), a nonpeptidic, noncovalent inhibitor of SARS-CoV-2 main protease (Mpro), exhibits potent inhibitory action (IC50 = 0.085 μM) and improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. It effectively suppresses viral replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 1.10 μM) and demonstrates low cytotoxicity (CC50 > 50 μM) [1].

ALE-0540 is a nonpeptidic heterocyclic molecule that inhibits the binding of NGF to p75 and TrkA, as well as signal transduction and biological responses mediated by TrkA receptors.

GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM. GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist.

GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM. GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist.

IFN alpha-IFNAR-IN-1 is a nonpeptidic, low-molecular-weight inhibitor that disrupts the interaction between IFN-α and IFNAR, inhibiting MVA-induced IFN-α responses by BM-pDCs (IC50: 2-8 μM).

ML-00253764 hydrochloride is an antagonist of nonpeptidic melanocortin receptor 4 (MC4R) (Ki and IC50 of 0.16 µM and 0.103 µM, respectively).

PROTAC RIPK degrader-2 is a nonpeptidic PROTAC ,and potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.

Brilacidin is a nonpeptidic anti-infective in a new class of defensin mimetics used for the research of eye infections.

SB-267268 inhibits human and mouse αvβ3 (IC50s: 0.68 and 0.29 nM, respectively). SB-267268 is a selective and nonpeptidic alpha(v)beta3 and alpha(v)beta5 integrins antagonist (Kis: 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respective

Apogossypolone (ApoG2) is a semi-synthesized derivative of gossypol which is a nonpeptidic small molecule inhibitor targeting Bcl-2 family proteins with K i values of 35, 25 and 660 nM for Bcl-2, Mcl-1 and Bcl-X L, respectively. Apogossypolone shows antitumor activities, induces cell apoptosis [1] and autophagy [2]. Apogossypolone also has antifungal activity [3].

RID-F is an inhibitor of the nonpeptidic proteasome.

A 74273, a nonpeptidic and renin inhibitor, may be used to treat cardiovascular diseases due to renin inhibition.

JNJ 10329670 is a highly potent (Ki of approximately 30 nM), nonpeptidic, noncovalent inhibitor of human cathepsin S with immunosuppressive activity.

NS 11 is an RGD-nonpeptidic mimetic.

CAY10727 is an inhibitor of protein arginine deiminase 3 (PAD3; kinact/KI= 15,600 M-1min-1).1It is selective for PAD3 over PAD1, -2, and -4 (kinact/KIs = 360, 1,110, and 1,460 M-1min-1, respectively). 1.Jamali, H., Khan, H.A., Stringer, J.R., et al.Identification of multiple structurally distinct, nonpeptidic small molecule inhibitors of protein arginine deiminase 3 using a substrate-based fragment methodJ. Am. Chem. Soc.137(10)3616-3621(2015)

2-Fluoro-4-iodo benzonitrile is a building block.1,2It has been used in the synthesis ofL. infantumtrypanothione reductase (Li-TryR) dimerization and oxidoreductase activity inhibitors.12-Fluoro-4-iodo benzonitrile has also been used in the synthesis of transient receptor potential ankyrin 1 (TRPA1) antagonists.2 1.Revuelto, A., Ruiz-Santaquiteria, M., de Lucio, H., et al.Pyrrolopyrimidine vs imidazole-phenyl-thiazole scaffolds in nonpeptidic dimerization inhibitors of Leishmania infantum trypanothione reductaseACS Infect. Dis.5(6)873-891(2019) 2.Vallin, K.S., Sterky, K.J., Nyman, E., et al.N-1-Alkyl-2-oxo-2-aryl amides as novel antagonists of the TRPA1 receptorBioorg. Med. Chem. Lett.22(17)5485-5492(2012)

AR-M 1000390 hydrochloride (ARM-390 HCl) , also known as ARM-390, is a low-internalizing nonpeptidic δ-selective opioid receptor agonist; derivative of SNC 80. Does not trigger acute desensitization of the analgesic response; reduces CFA-induced hyperalgesia. Brain penetrant following systemic administration.

R-PSOP is a potent and selective nonpeptidic NMUR2 antagonist, exhibiting binding affinity to human and rat NMUR2 with Ki values of 52 nM and 32 nM, respectively. This compound demonstrates moderate central nervous system (CNS) penetration and is valuable in the study of eating disorders, obesity, pain, and stress-related disorders [1].

ATC0065 dihydrochloride is a novel nonpeptidic and potent melanin-concentrating hormone receptor 1 (MCHR1) selective antagonist.

SC 51316 is a nonpeptidic angiotensin II (AII) receptor antagonist.

GB-110 hydrochloride, a potent and orally active nonpeptidic agonist of the protease-activated receptor 2 (PAR2), selectively triggers PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM [1].