alisporivir: nonimmunosuppressive cyclosporin analog; structure/sequence in first source
ID Source | ID |
---|---|
PubMed CID | 11513676 |
CHEMBL ID | 1651956 |
CHEBI ID | 149837 |
SCHEMBL ID | 6850787 |
MeSH ID | M0483496 |
Synonym |
---|
debio 025 |
deb025 |
debio-025 |
alisporivir |
unil-025 |
deb-025 |
CHEBI:149837 |
CHEMBL1651956 , |
deb 025 |
(d-meala)3-(etval)4-csa |
unil 025 |
bdbm50339127 |
(3s,6s,9s,12r,15s,18s,21s,24s,27r,30s,33s)-25,30-diethyl-33-((1r,2r,e)-1-hydroxy-2-methylhex-4-enyl)-6,9,18-triisobutyl-3,21,24-triisopropyl-1,4,7,10,12,15,19,27,28-nonamethyl-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5,8,11,14,17,20,23, |
(3s,6s,9s,12r,15s,18s,21s,24s,27r,30s,33s)-25,30-diethyl-33-((1r,2r)-1-hydroxy-2-methylhex-4-enyl)-6,9,18-triisobutyl-3,21,24-triisopropyl-1,4,7,10,12,15,19,27,28-nonamethyl-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5,8,11,14,17,20,23,26 |
alisporivir (usan) |
254435-95-5 |
D10087 |
meala(3)etval(4)-cyclosporin |
unil025 |
unii-vbp9099aa6 |
alisporivir [usan:inn] |
cyclo(l-alanyl-d-alanyl-n-methyl-l-leucyl-n-methyl-l-leucyl-n-methyl-l-valyl-(2s,3r,4r,6e)-3-hydroxy-4-methyl-2-(methylamino)-6-octenoyl-(2s)-2-aminobutanoyl-n-methyl-d-alanyl-n-ethyl-l-valyl-l-valyl-n-methyl-l-leucyl) |
vbp9099aa6 , |
debio025 |
alisporivir [who-dd] |
alisporivir [inn] |
alisporivir [usan] |
SCHEMBL6850787 |
CS-7501 |
HY-12559 |
DB12139 |
Q4727236 |
MS-32057 |
(3s,6s,9s,12r,15s,18s,21s,24s,27r,30s,33s)-25,30-diethyl-33-((1r,2r,e)-1-hydroxy-2-methylhex-4-en-1-yl)-6,9,18-triisobutyl-3,21,24-triisopropyl-1,4,7,10,12,15,19,27,28-nonamethyl-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5,8,11,14,17,20, |
(3s,6s,9s,12r,15s,18s,21s,24s,27r,30s,33s)-25,30-diethyl-33-[(e,1r,2r)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,27,28-nonamethyl-6,9,18-tris(2-methylpropyl)-3,21,24-tri(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11 |
(3s,6s,9s,12r,15s,18s,21s,24s,27r,30s,33s)-25,30-diethyl-33-[(1r,2r,4e)-1-hydroxy-2-methylhex-4-en-1-yl]-1,4,7,10,12,15,19,27,28-nonamethyl-6,9,18-tris(2-methylpropyl)-3,21,24-tris(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5 |
DTXSID401027752 |
debio-025;deb-025 |
AKOS040741084 |
Alisporivir (Debio 025) is a nonimmunosuppressive analogue of cyclosporine with potent cyclophilin inhibition properties. It is an oral, host-targeting agent with pangenotypic anti-hepatitis C virus (HCV) activity and a high barrier to resistance.
Excerpt | Reference | Relevance |
---|---|---|
"Alisporivir has an excellent pharmacokinetic and safety profile." | ( Profile of alisporivir and its potential in the treatment of hepatitis C. Gallay, PA; Lin, K, 2013) | 1.5 |
Alisporivir pretreatment stimulated antigen presentation by hepatoma target cells, leading to enhancement of antigen-specific CD8(+) T cell activation by 40%. Treatment with alisporvir, but not with cyclosporin A, led to a substantial recovery of respiratory function matching improved muscle ultrastructure and survival of sapje zebrafish.
Excerpt | Reference | Relevance |
---|---|---|
"Alisporivir pretreatment stimulated antigen presentation by hepatoma target cells, leading to enhancement of antigen-specific CD8(+) T cell activation by 40%." | ( The cyclophilin-inhibitor alisporivir stimulates antigen presentation thereby promoting antigen-specific CD8(+) T cell activation. Esser-Nobis, K; Lohmann, V; Neumann-Haefelin, C; Nitschke, K; Schmidt, J; Thimme, R, 2016) | 1.46 |
"Treatment with alisporivir, but not with cyclosporin A, led to a substantial recovery of respiratory function matching improved muscle ultrastructure and survival of sapje zebrafish, a severe model of DMD where muscle defects are close to those of DMD patients." | ( Alisporivir rescues defective mitochondrial respiration in Duchenne muscular dystrophy. Argenton, F; Bernardi, P; Menazza, S; Merlini, L; Petronilli, V; Sabatelli, P; Schiavone, M; Zulian, A, 2017) | 2.24 |
Co-administration with ketoconazole (a strong CYP3A4 inhibitor) increased the Cmax , AUC and terminal elimination half-life of alisporivir.
Excerpt | Reference | Relevance |
---|---|---|
" The aim of the current work was to develop a novel physiologically based pharmacokinetic (PBPK) model to quantitatively assess the magnitude of CYP3A4 mediated drug-drug interactions with alisporivir as the substrate or victim drug." | ( Physiologically based pharmacokinetic modeling for assessing the clinical drug-drug interaction of alisporivir. Alexander, N; Barve, A; Einolf, H; Gu, H; Hanna, I; He, H; Heimbach, T; Ke, J; Mangold, JB; Sunkara, G; Wang, L; Xia, B; Zhang, T, 2014) | 0.81 |
" Co-administration with ketoconazole (a strong CYP3A4 inhibitor) increased the Cmax , AUC and terminal elimination half-life of alisporivir by approximately two-, eight- ,and threefold, respectively." | ( The effects of CYP3A4 induction and inhibition on the pharmacokinetics of alisporivir in humans. Barve, A; Crabbe, R; Dabovic, K; Dole, K; Grosgurin, P; Ke, J; Kovacs, SJ; Menetrey, A; Nicolas-Métral, V; Praestgaard, J; Stein, D; Sunkara, G; Zhang, J, 2015) | 0.85 |
Alisporivir alone or in combination with pegylated interferon (peg-IFN) was found to be effective. The aim of the current work was to develop a novel physiologically based pharmacokinetic (PBPK) model.
Excerpt | Relevance | Reference |
---|---|---|
" The treatment of target cells with agents that disrupt CypA-CA interactions often produced biphasic dose-response curves in which viral infectivity first increased and subsequently decreased as a function of the dose used." | ( Modulation of HIV-1 infectivity and cyclophilin A-dependence by Gag sequence and target cell type. Clavel, F; Dam, E; Hance, AJ; Lecossier, D; Matsuoka, S, 2009) | 0.35 |
" We simulated virologic responses with other alisporivir dosing regimens in HCV genotype 2/3 patients using the model." | ( A pharmacokinetic-viral kinetic model describes the effect of alisporivir as monotherapy or in combination with peg-IFN on hepatitis C virologic response. Guedj, J; Levi, M; Mentré, F; Nguyen, TH; Yu, J, 2014) | 0.9 |
Role | Description |
---|---|
anticoronaviral agent | Any antiviral agent which inhibits the activity of coronaviruses. |
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Class | Description |
---|---|
homodetic cyclic peptide | A homodetic cyclic peptide is a cyclic peptide in which the ring consists solely of amino-acid residues in peptide linkages. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Bile salt export pump | Homo sapiens (human) | IC50 (µMol) | 0.1100 | 0.1100 | 7.1903 | 10.0000 | AID1168844 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 (µMol) | 0.5900 | 0.0002 | 2.3185 | 10.0000 | AID1168846 |
Peptidyl-prolyl cis-trans isomerase A | Homo sapiens (human) | Ki | 0.0003 | 0.0003 | 0.0473 | 0.2310 | AID581778 |
Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 (µMol) | 18.0000 | 2.4100 | 6.3433 | 10.0000 | AID1168843 |
Solute carrier organic anion transporter family member 1B3 | Homo sapiens (human) | IC50 (µMol) | 0.2200 | 0.1047 | 2.7195 | 7.0795 | AID1168842 |
Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 (µMol) | 2.5000 | 0.0040 | 1.9666 | 10.0000 | AID1168845 |
Solute carrier organic anion transporter family member 1B1 | Homo sapiens (human) | IC50 (µMol) | 0.4900 | 0.0500 | 2.3797 | 9.7000 | AID1168826; AID1168841 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Peptidyl-prolyl cis-trans isomerase B | Homo sapiens (human) | Kd | 0.0010 | 0.0010 | 0.0053 | 0.0098 | AID1168835 |
Peptidyl-prolyl cis-trans isomerase F, mitochondrial | Homo sapiens (human) | Kd | 0.0010 | 0.0010 | 0.0028 | 0.0042 | AID1168836 |
Peptidyl-prolyl cis-trans isomerase A | Homo sapiens (human) | Kd | 0.0066 | 0.0022 | 0.4297 | 6.4200 | AID1168824; AID719606 |
Nonstructural protein 5A | EC50 (µMol) | 0.0158 | 0.0000 | 0.1375 | 8.1000 | AID1714205 | |
RNA-directed RNA polymerase | EC50 (µMol) | 0.0158 | 0.0018 | 0.2348 | 2.8000 | AID1714203 | |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1178324 | Antiviral activity against HIV1 in HCV and HIV co-infected human patient assessed as log reduction in plasma HIV1 RNA dosed for 10 days | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | From chemical tools to clinical medicines: nonimmunosuppressive cyclophilin inhibitors derived from the cyclosporin and sanglifehrin scaffolds. |
AID573111 | Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh-Mono cells assessed as reduction in replicon RNA after 4 days by RT-qPCR analysis | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
AID581926 | Antiviral activity against RSV infected in human HeLa cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID555925 | Antiviral activity against HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID555936 | Cytotoxicity against human Huh-9-13 cells at 5 ug/ml after 3 days by MTT assay | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID1168840 | Cytotoxicity against PHA-stimulated human PBMC by 5-bromo-2'-deoxyuridine incorporation assay | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID573107 | Cytotoxicity against human Huh-Mono cells after 3 days by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
AID581785 | Antiviral activity against HIV1 subtype A 92RW016 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581958 | Cytotoxicity against human HepAD38 cells | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1168850 | AUC in dog plasma at 1 mg/kg, po after 72 hrs | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID581800 | Antiviral activity against HIV1 subtype F 93BR020 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581953 | Antiviral activity against HPV-33 infected in CK1 cells assessed as inhibition of viral replication after 7 days | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581914 | Antiviral activity against LPV, APV, ATV, IDV, NFV, RTV, SQV-resistant HIV-1 52-52 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID573106 | Cytotoxicity against human Huh-9-13 cells after 3 days by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
AID581945 | Antiviral activity against Human cytomegalovirus Davis infected in human embryonic lung cells assessed as reduction in viral yield | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581915 | Antiviral activity against Simian immunodeficiency virus-mac 251 infected in human PBMC assessed as inhibition of viral replication by RT activity | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1168844 | Inhibition of BSEP (unknown origin) expressed in HEK293 cells using [3H]taurocholic acid substrate | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID555927 | Antiviral activity against HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication selected after 1 passages at 5 ug/ml by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID581921 | Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581767 | Immunosuppressive activity in Sprague-Dawley rat KHL model assessed as IgM level at 10 mg/kg, po administered once daily for 28 days by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581929 | Cytotoxicity against human embryonic lung cells | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1168845 | Inhibition of BCRP (unknown origin) expressed in T8 cells using Bodipy FL-prazosin substrate | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID1714205 | Inhibition of NS5A L31V mutant in HCV genotype 1b infected in HuH7.5Lcu-Neo cells assessed as reduction in viral replication by luciferase reporter gene assay | 2016 | Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22 | Design and Synthesis of Cajanine Analogues against Hepatitis C Virus through Down-Regulating Host Chondroitin Sulfate N-Acetylgalactosaminyltransferase 1. |
AID581784 | Immunosuppressive activity in Sprague-Dawley rat KHL model assessed as percent cytotoxic T cells at 50 mg/kg, po administered once daily for 28 days by flow cytometry | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID555932 | Antiviral activity against HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication selected after 3 passages at 1 ug/ml by quantitative RT-PCR in presence of G418 selection pressure | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID762651 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 to 6 days by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16 | Cyclophilin inhibitors as antiviral agents. |
AID1168834 | Dissociation constant, basic pKa of the compound | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID1168849 | AUC in dog blood at 1 mg/kg, po after 72 hrs | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID581955 | Antiviral activity against HIV-1 NL4-3 infected in human TZB cells assessed as inhibition of accumulation of late viral transcripts at 0.5 to 2.5 uM by RT-PCR | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581916 | Antiviral activity against Simian immunodeficiency virus PBj infected in human PBMC assessed as inhibition of viral replication by RT activity | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1714207 | Inhibition of NS5A in HCV genotype 1b infected in HuH7.5Lcu-Neo cells assessed as reduction in viral replication by luciferase reporter gene assay | 2016 | Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22 | Design and Synthesis of Cajanine Analogues against Hepatitis C Virus through Down-Regulating Host Chondroitin Sulfate N-Acetylgalactosaminyltransferase 1. |
AID581950 | Antiviral activity against HPV-33 infected in CK1 cells assessed as inhibition of viral replication after 3 days | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581913 | Antiviral activity against APV, ATV, IDV, LPV, NFV, RTV, SQV, AZT, ddI, 3TC, d4T-resistant HIV-1 MDR1385 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581803 | Antiviral activity against LPV, APV, ATV, IDV, NFV, RTV, SQV, AZT, ddI, 3TC, d4T-resistant HIV-1 MDR3761 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1168837 | Antiviral activity against HCV subtype 1a in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID581798 | Antiviral activity against HIV1 subtype EA CMU02 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581933 | Antiviral activity against HCV infected in human Huh 5.2 cells assessed as reduction in viral RNA level by luciferase reporter gene assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581951 | Antiviral activity against HPV-16 infected in Caski cells assessed as inhibition of viral replication after 7 days | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581791 | Antiviral activity against HIV1 subtype B 92BR014 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID555950 | Antiviral activity against compound-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID1168835 | Binding affinity to human cyclophilin B by surface plasmon resonance method | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID581944 | Antiviral activity against Human cytomegalovirus AD169 infected in human embryonic lung cells assessed as reduction in viral yield | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID555953 | Antiviral activity against R479-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID555929 | Antiviral activity against HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication selected after 2 passages at 1 ug/ml by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID581924 | Antiviral activity against influenza B virus infected in MDCK cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581804 | Antiviral activity against ABC, ddC, ddI, TDF, AZT, d4T-resistant HIV-1 G910-6 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581762 | Immunosuppressive activity in Sprague-Dawley rat KHL model assessed as percent T lymphocytes at 25 mg/kg, po administered once daily for 28 days by flow cytometry | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581920 | Cytotoxicity against african green monkey Vero cells | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1168847 | AUC in rat blood at 25 mg/kg, po after 72 hrs | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID1168846 | Inhibition of MDR1 (unknown origin) expressed in MDA T0.3 cells using rhodamine 123 substrate | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID581786 | Antiviral activity against HIV1 subtype A 92UG037 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581774 | Antiviral activity against HIV-1 SF2 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581923 | Cytotoxicity against MDCK cells | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID573109 | Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh-9-13 cells assessed as reduction in replicon RNA after 4days by RT-qPCR analysis | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
AID1168839 | Cytotoxicity against human MT4 cells by CDCF probe based assay | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID1168836 | Binding affinity to human cyclophilin F by surface plasmon resonance method | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID581801 | Antiviral activity against HIV1 subtype O BCF01 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1168848 | AUC in rat plasma at 25 mg/kg, po after 72 hrs | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID573110 | Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH6 cells assessed as reduction in replicon RNA after 4days by RT-qPCR analysis | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
AID1168841 | Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using [3H]estradiol-17beta-glucuronide substrate | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID581796 | Antiviral activity against HIV1 subtype C 92BR025 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID555939 | Antiviral activity against HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication selected after 8 passages at 0.25 ug/ml by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID581942 | Antiviral activity against Herpes simplex virus 2 Lyons infected in human embryonic lung cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581938 | Antiviral activity against Herpes simplex virus 1 F infected in human embryonic lung cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581919 | Antiviral activity against Coxsackie B3 infected in african green monkey Vero cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581934 | Antiviral activity against BVDV infected in MDCK cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581941 | Antiviral activity against Herpes simplex virus 2 196 infected in human embryonic lung cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1714203 | Inhibition of NS5B S282T mutant in HCV genotype 1b infected in HuH7.5Lcu-Neo cells assessed as reduction in viral replication by luciferase reporter gene assay | 2016 | Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22 | Design and Synthesis of Cajanine Analogues against Hepatitis C Virus through Down-Regulating Host Chondroitin Sulfate N-Acetylgalactosaminyltransferase 1. |
AID719606 | Binding affinity to human cyclophilin A by fluorescence polarization assay | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Ranking high affinity ligands of low solubility by NMR spectroscopy. |
AID581939 | Antiviral activity against Herpes simplex virus 1 McIntyre infected in human embryonic lung cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581799 | Antiviral activity against HIV1 subtype G Jv1083 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID762647 | Antiviral activity against Hepatitis C virus infected in human HuH5.2 cells after 72 hrs by luciferase reporter gene assay | 2013 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16 | Cyclophilin inhibitors as antiviral agents. |
AID581927 | Cytotoxicity against human HeLa cells | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581792 | Antiviral activity against HIV1 subtype B SLKA infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581787 | Antiviral activity against HIV1 subtype B NL4-3 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581937 | Antiviral activity against Herpes simplex virus 1 KOS infected in human embryonic lung cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581775 | Antiviral activity against HIV-1 NL4-3 infected in human TZB cells assessed as inhibitory effect on the completion of viral double stranded DNA at 0.5 to 2.5 uM by RT-PCR | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581928 | Antiviral activity against VSV infected in human embryonic lung cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID555952 | Antiviral activity against 2'-C-methyl-2'-fluoro-cytidine-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID573105 | Cytotoxicity against human HuH6 cells after 3 days by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
AID581782 | Immunosuppressive activity in Sprague-Dawley rat KHL model assessed as percent cytotoxic T cells at 10 mg/kg, po administered once daily for 28 days by flow cytometry | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581765 | Immunosuppressive activity in Sprague-Dawley rat KHL model assessed as IgM level at 25 mg/kg, po administered once daily for 28 days by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581776 | Antiviral activity against HIV-1 3B infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1168842 | Inhibition of OATP1B3 (unknown origin) expressed in HEK293 cells using [3H]estradiol-17beta-glucuronide substrate | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID581947 | Antiviral activity against Vaccinia virus infected in human embryonic lung cells assessed as reduction in viral yield measured after 3 days | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581790 | Antiviral activity against HIV1 subtype B Ba-L infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581778 | Inhibition of human recombinant cyclophilin-associted cis-trans propyl isomerase activity | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1168825 | Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID555938 | Antiviral activity against HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication selected after 7 passages at 0.25 ug/ml by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID581793 | Antiviral activity against HIV1 subtype B TEKI infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581932 | Cytotoxicity against CRFK | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1168826 | Inhibition of OATP1B1 (unknown origin) expressed in CHO cells using 8-fluorescein-cAMP substrate by fluorescent photometry | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID555935 | Cytotoxicity against human Huh-9-13 cells at 1 ug/ml after 3 days by MTT assay | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID581777 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1714206 | Inhibition of NS5A D320E/Y321N mutant in HCV genotype 1b infected in HuH7.5Lcu-Neo cells assessed as reduction in viral replication by luciferase reporter gene assay | 2016 | Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22 | Design and Synthesis of Cajanine Analogues against Hepatitis C Virus through Down-Regulating Host Chondroitin Sulfate N-Acetylgalactosaminyltransferase 1. |
AID581940 | Antiviral activity against Herpes simplex virus 2 G infected in human embryonic lung cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581771 | Cytotoxicity against human MT4 cells at 0.83 uM by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID555937 | Cytotoxicity against human Huh-9-13 cells at 30 ug/ml after 3 days by MTT assay | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID555928 | Antiviral activity against HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication selected after 2 passages at 5 ug/ml by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID581931 | Antiviral activity against Feline coronavirus infected in CRFK assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581917 | Antiviral activity against HIV-2 isolate CDC310342 infected in human PBMC assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID555955 | Antiviral activity against VX 950-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID581948 | Antiviral activity against HPV-16 infected in Caski cells assessed as inhibition of viral replication after 3 days | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581797 | Antiviral activity against HIV1 subtype D 92UG046 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581783 | Immunosuppressive activity in Sprague-Dawley rat KHL model assessed as percent cytotoxic T cells at 25 mg/kg, po administered once daily for 28 days by flow cytometry | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID573112 | Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
AID581763 | Immunosuppressive activity in Sprague-Dawley rat KHL model assessed as percent T lymphocytes at 10 mg/kg, po administered once daily for 28 days by flow cytometry | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1168827 | Kinetic solubility of the compound in pH 7.0 water | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID581795 | Antiviral activity against HIV1 subtype B WEJO infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581930 | Antiviral activity against SARS coronavirus infected in african green monkey Vero cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1178323 | Antiviral activity against HCV in HCV and HIV co-infected human patient assessed as log reduction in plasma HCV RNA dosed for 10 days | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | From chemical tools to clinical medicines: nonimmunosuppressive cyclophilin inhibitors derived from the cyclosporin and sanglifehrin scaffolds. |
AID581788 | Antiviral activity against HIV1 subtype B JR-CSF infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1168843 | Inhibition of human MRP2 expressed in Sf9 cells inside out vesicles using CDCF substrate | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID581922 | Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID573108 | Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
AID1168824 | Binding affinity to human cyclophilin A by surface plasmon resonance method | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID581952 | Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 7 days | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581789 | Antiviral activity against HIV1 subtype B SF162 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581768 | Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581925 | Antiviral activity against Parainfluenza 3 infected in african green monkey Vero cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID555954 | Antiviral activity against BILN 2061-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID581943 | Antiviral activity against VZV OKA infected in human embryonic lung cells assessed as inhibition of | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID555926 | Antiviral activity against HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication selected after 1 passages at 0.82 uM by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID1714204 | Inhibition of NS3 R155Q/A156T mutant in HCV genotype 1b infected in HuH7.5Lcu-Neo cells assessed as reduction in viral replication by luciferase reporter gene assay | 2016 | Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22 | Design and Synthesis of Cajanine Analogues against Hepatitis C Virus through Down-Regulating Host Chondroitin Sulfate N-Acetylgalactosaminyltransferase 1. |
AID719605 | Binding affinity to human cyclophilin A assessed as compound-enzyme complex formation at 1:1 protein to compound ratio by NMR analysis | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Ranking high affinity ligands of low solubility by NMR spectroscopy. |
AID581949 | Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 3 days | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581764 | Immunosuppressive activity in Sprague-Dawley rat KHL model assessed as IgM level at 50 mg/kg, po administered once daily for 28 days by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID555934 | Antiviral activity against HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication selected after 7 passages at 30 ug/ml by quantitative RT-PCR in presence of G418 selection pressure | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID555933 | Antiviral activity against HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication selected after 7 passages at 5 ug/ml by quantitative RT-PCR in presence of G418 selection pressure | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID581954 | Antiviral activity against HIV-1 NL4-3 infected in human TZB cells assessed as inhibition of accumulation of early viral transcripts at 0.5 to 2.5 uM by RT-PCR | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581918 | Antiviral activity against HIV-2 isolate CDC310319 infected in human PBMC assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1168833 | Lipophilicity, log D of the compound | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID581935 | Antiviral activity against Yellow fever virus 17D infected in african green monkey Vero cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581779 | Immunosuppressive activity in Sprague-Dawley rat KHL model assessed as percent T-helper cells at 10 mg/kg, po administered once daily for 28 days by flow cytometry | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581957 | Antiviral activity against HIV-1 NL4-3 cells infected in human TZB cells assessed as degradation of cDNA at 0.5 to 2.5 uM after 6 hrs postinfection by RT-PCR | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581761 | Immunosuppressive activity in Sprague-Dawley rat KHL model assessed as percent T lymphocytes at 50 mg/kg, po administered once daily for 28 days by flow cytometry | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID1168838 | Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene in presence of 40% human serum | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
AID581770 | Cytotoxicity against human PBMC at 0.83 uM by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581802 | Antiviral activity against APV, ATV, LPV, IDV, NFV, RTV, SQV-resistant HIV-1 1064-52 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581794 | Antiviral activity against HIV1 subtype B ROJO infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID555951 | Antiviral activity against cyclosporine-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
AID581946 | Antiviral activity against HBV infected in human hepAD38 cells assessed as inhibition of viral replication | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581781 | Immunosuppressive activity in Sprague-Dawley rat KHL model assessed as percent T-helper cells at 50 mg/kg, po administered once daily for 28 days by flow cytometry | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581780 | Immunosuppressive activity in Sprague-Dawley rat KHL model assessed as percent T-helper cells at 25 mg/kg, po administered once daily for 28 days by flow cytometry | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581773 | Immunosuppressive activity in human Jurkat cells assessed as inhibition of PHA-phorbol myristate acetate induced beta-galactosidase activity at 21.5 uM | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581956 | Antiviral activity against HIV-1 NL4-3 infected in human TZB cells assessed as inhibition of viral entry at 0.5 to 2.5 uM after 2 hrs by RT-PCR | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581936 | Cytotoxicity against human Huh 5.2 cells | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
AID581805 | Antiviral activity against APV, ATV, IDV, LPV, NFV, RTV, SQV, 3TC, FTC, ABC, AZT, d4T, ddC, ddI, TDF, EFV, DLV, NVP-resistant HIV-1 MDR769 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 17 (20.99) | 29.6817 |
2010's | 52 (64.20) | 24.3611 |
2020's | 12 (14.81) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (29.41) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 9 (11.11%) | 5.53% |
Reviews | 13 (16.05%) | 6.00% |
Case Studies | 1 (1.23%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 58 (71.60%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |