Capsid

Cetylpyridinium Chloride (Hexadecylpyridinium Chloride) is a cationic quaternary ammonium compound used as oropharyngeal antiseptic.

Lenacapavir (GS-6207) is the first HIV-1 capsid inhibitor approved by the U.S. Food and Drug Administration, the European Medicines Agency, and Health Canada for the treatment of MDR HIV-1 infection.[3]

NVR 3-778 is a first-in-class, orally bioavailable HBV CAM belonging to the SBA class, exhibiting anti-HBV activity.

HIVCapsid-IN-2 (Compound IC-2b4) is a potent inhibitor of the HIV-1 capsid protein (CA). It effectively inhibits both HIV-1, with an EC50 of 0.08 μM, and HIV-2. HIVCapsid-IN-2 operates by directly stabilizing the binding to HIV-1 CA, exerting its inhibitory effects in both early and late stages of infection.

Capsid assembly inhibitor is a 12-mer peptide that binds to the Gag capsid (CA) domain, effectively inhibiting the assembly of both immature and mature-like HIV-1 capsid particles in vitro.

Isothiafludine (NZ-4) is an orally active anti-HBV compound that acts by blocking the encapsulation of pre-genomic RNA (pgRNA) and interfering with nucleosome capsid assembly, and is used in the study of HBV infections.

I-XW-053 is a micromolar affinity inhibitor of capsid-targeted HIV-1 replication, utilizing a hybrid structure-based method to block the interface between CA N-terminal domains (NTD-NTD interface).

BA-53038B is an HBV core protein allosteric modulator (CpAM), binding to the HAP pocket and modulating HBV capsid assembly in a distinct manner (EC50: 3.32 μM).

Pleconaril (VP 63843) is a capsid inhibitor used previously to treat enterovirus infections. Pleconaril is effective in inhibiting replication (IC50: 50 nM).

PF-3450074 (PF-74) acts at an early stage of HIV-1 infection inhibits viral replication by directly competing with the binding of CPSF6 (nuclear host factors cleavage and polyadenylation specific factor 6) and NUP153 (nucleoporin 153), and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle. PF-3450074 is a specifical inhibitor of HIV-1 capsid protein (CA) and shows a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM).

Pocapavir (SCH-48973) is an investigational enterovirus (EV) capsid inhibitor.

CA inhibitor 1 (GS-6207 analog) is a potent inhibitor of the HIV capsid.

GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools. GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC50=3 nM), and reduces cccDNA by >90% at 1

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.

Vapendavir is a potent enteroviral capsid binder. Vapendavir has an effective antiviral activity for enterovirus 71 replication (EC50: 0.5-1.4 μM in different EV71 strains).

Pirodavir (R77975) (R 77975), the prototype of broad-spectrum anti-picornavirus compounds, is a potent human rhinovirus (HRV) capsid-binding inhibitor.

Lenacapavir, also known as GS-6207, is an HIV-1 capsid inhibitor. It demonstrates an average EC50 of 50 pM (ranging from 20-160 pM) against 23 clinical isolates of HIV-1 from diverse subtypes, with tests performed in peripheral blood mononuclear cells (PBMCs). In vitro, Lenacapavir exhibits picomolar potency and shows no cross-resistance with existing antiretroviral compounds. Furthermore, Lenacapavir displays significant antiviral activity in individuals with HIV-1, regardless of prior treatment history, with no pre-existing resistance detected.

BA-AZT1 acts as an inhibitor of HBV polymerase (HBV polymerase) and sodium taurocholate cotransporting polypeptide (NTCP). It hinders the secretion of viral capsid proteins HBsAg and HBeAg, with IC50 values of 0.65 µM and 13.42 µM, respectively, and inhibits HBV DNA replication with an IC50 of 0.70 µM.

ALG-000184, a prodrug of the potent HBV capsid assembly modulator ALG-001075, shows potential for use in HBV infection research.

HR-568 displays broad-spectrum anti-enterovirus activity. It inhibits enterovirus strains EV-A71, E30, and CVA24 in MRC-5 cells, with EC50 values of 1.53 μM, 0.4 μM, and 1.22 μM, respectively. HR-568 targets the hydrophobic pocket on enterovirus capsid proteins, thereby hindering viral replication.

KR019 is a potent hepatitis B virus (HBV) capsid assembly modulator that demonstrates significant antiviral activity in HBV cells. It binds to the hydrophobic pocket at the core protein dimer-dimer interface, redirecting capsid assembly into genome-free capsids, thereby inhibiting viral replication.

HBV-IN-51 (Compound 17e) is an effective hepatitis B virus (HBV) capsid assembly modulator. It demonstrates significant anti-HBV activity with an EC50 value of 0.033 μM in HepAD38 cells. HBV-IN-51 exhibits good metabolic stability in plasma and is rapidly metabolized in human liver microsomes.

AIC263282 is a potent capsid assembly modulator for the hepatitis B virus (HBV) with an EC50 of 3.8 nM. It exhibits an IC50 of 61 nM against hERG and effectively inhibits viral replication and hepatitis B surface antigen (HBsAG) in primary human hepatocytes.

HEC72702 is a novel Hepatitis B virus capsid inhibitor, based on clinical candidate GLS4. HEC72702 was found to display no induction of the CYP1A2, CYP3A4, or CYP2B6 enzyme at the high concentration of 10 μM.