entry

GRP-60367 is the first small molecule rabies virus (RABV) entry inhibitor, which has nanomolar effect on some RABV strains.

EBOVentry-IN-1 (compound Hu7) is an inhibitor of EBOV virus entry, with an IC50 of 1.50 μM.

K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.

IQP-0528 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) that has potential for the treatment of HIV infection by blocking viral entry and shows antiviral activity as a microbicidal gel. . IQP-0528 showed inhibition of both HIV-1 and HIV-2, with an EC50 of 0.2 nM for HIV-1 and 100 nM for HIV-2.

Flunarizine dihydrochloride (R14950) is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. Flunarizine dihydrochloride (R14950) is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.

L-Carnitine (L(-)-Carnitine) is an amino acid derivative. L-Carnitine facilitates long-chain fatty acid entry into mitochondria, delivering substrate for oxidation and subsequent energy production. Fatty acids are utilized as an energy substrate in all tissues except the brain.

Isradipine (PN 200-110) is a dihydropyridine calcium channel blocker with antihypertensive and vasodilator activities. Isradipine blocks calcium entry through calcium ion channels in coronary and peripheral vascular smooth muscle, dilating coronary arteries and peripheral arterioles. This action increases oxygen delivery by enhancing blood flow and decreases oxygen requirements by reducing total peripheral resistance.

Beclometasone dipropionate (Vancenase) is the dipropionate ester of a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. After cell surface receptor attachment and cell entry, beclomethasone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production.

TBMP (butylated hydroxyanisole) is the viral envelope protein hemagglutinin (HA)-mediated entry novel inhibitor.

L-Lysine (Aminutrin) is one of nine essential amino acids in humans required for growth and tissue repair, Lysine is supplied by many foods, especially red meats, fish, and dairy products. Lysine seems to be active against herpes simplex viruses and present in many forms of diet supplements. The mechanism underlying this effect is based on the viral need for amino acid arginine; lysine competes with arginine for absorption and entry into cells. Lysine inhibits HSV growth by knocking out arginine.

CPDS is a non permeant thiol agent which affects several mitochondrial functions. In rat liver mitochondria, CPDS inhibits only the Pi OH- carrier; both CPDS and n-butylmalonate are necessary to inhibit completely Pi entry.

YYA-021 inhibits HIV entry, with high anti-HIV activity and low cytotoxicity.

N-(1-benzyl-4-piperidyl)adamantane-1-carboxamide inhibiting the entry of Ebola virus in host cells by binding to the surface glycoprotein, the compound inhibited the Ebola virus with EC50 of 3.9 μM.

MBX2329 is a specific inhibitor of HA-mediated viral entry that inhibits H1N1 virus strain high pathogenic avian influenza H5N1 virus strain.

Triamcinolone (Aristocort) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B.

Mefloquine (Ro 215998), a quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1 minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus, and cancer research.

1-Docosanol (Behenic alcohol) is a saturated 22-carbon aliphatic alcohol with antiviral activity. 1-Docosanol has a distinct mechanism of action and inhibits fusion between the plasma membrane and the herpes simplex virus envelope, thereby preventing viral entry into cells and subsequent viral activity and replication. 1-Docosanol is used topically in the treatment of recurrent herpes simplex labialis episodes and relieves associated pain and may help heal sores faster.

Dooku1 is an analog of Yoda1 and a selective antagonist of endogenous Piezo1 channels. Dooku1 inhibits Ca2+ entry induced by 2μMYoda1 with IC50 values of 1.3μM (in HEK 293 cells) and 1.5μM (in HUVEC). Dooku1 inhibits Yoda1-induced aortic relaxation.

Filipin complex is a 28-membered cyclopentene macrolide antifungal antibiotic produced by a mixture of S. filipinensis, S. avermitilis, and S. miharaensis that inhibits the entry of PRRSV viruses into cells.

MRS1845 is an ORAI1 inhibitor and calcium entry (SOCE) blocker that blocks VP-induced SOCE, OS, and Ca(2+) deposition.

Naphthoquine phosphate is a broad-spectrum 4-aminoquinoline antimalarial compound with oral activity that may affect viral entry and post-entry replication.Naphthoquine phosphate has hepatic vascular center toxicity and is often used with artemisinin to treat malaria.

SOCE inhibitor 1 is a inhibitor of store-operated calcium entry (SOCE)(IC50 of 4.4 μM).

Synta66 is a store-operated calcium entry channel Orai inhibitor, and used for the research of neurological disease.

Vapendavir diphosphate (BTA798 diphosphate) is a rhinoceros/enterovirus inhibitor that targets the hydrophobic pocket in the viral capsid and is a capsid-binding agent with antiviral activity that prevents viral entry into the cell. Vapendavir diphosphate inhibits EV71 replication.