| Assay ID | Title | Year | Journal | Article |
|---|
| AID725383 | AUC in rat at 5 mg/kg, po | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Inhibitors of HIV-1 attachment. Part 11: the discovery and structure-activity relationships associated with 4,6-diazaindole cores. |
| AID446486 | Inhibition of recombinant CYP3A4 using 7-benzyloxyresorufin as substrate | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1454925 | Antiviral activity against HIV1 infected in human assessed as decrease in viral load in plasma at 800 mg bid measured on day 8 | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID763536 | Inhibition of HIV-1 gp120-CD4 (unknown origin) interaction | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15
| Molecular docking guided structure based design of symmetrical N,N'-disubstituted urea/thiourea as HIV-1 gp120-CD4 binding inhibitors. |
| AID698448 | Aqueous solubility of compound at pH 4 to pH 8 | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2 |
| AID1454911 | Inhibition of [3H]BMS-488043 binding to HIV-1 isolate JRFL gp120 assessed as dissociation half life incubated for 60 mins followed by CD4 addition by scintillation counting method | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID421178 | Antiviral activity against HIV isolate 584.000.098 by replication assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID443381 | Aqueous solubility of crystalline form of compound in buffer solution of pH 10 at 25 degC | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID698636 | Half life in high fat fed healthy human at 800 mg, po administered as capsule with high fat meal | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2 |
| AID1505625 | AUC in cynomolgus monkey at 5 mg/kg, po administered via gavage | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID1505611 | Protein binding in human plasma | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID1505634 | Antiviral activity against HIV1 infected in patients assessed as reduction in maxmum viral RNA by measuring log10 viral copies at 1800 mg, bid measured at day 8 | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID421174 | Antiviral activity against HIV isolate 584.000 054 by replication assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID1505631 | Antiviral activity against HIV1 infected in patients assessed as reduction in plasma viral load by measuring log10 viral copies at 800 mg, bid measured at day 8 (Rvb = 0.02 log10 copies/ml) | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID1505652 | Binding affinity to HIV-1 JRFL gp120 assessed as half life for dissociation | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID421176 | Antiviral activity against HIV isolate 584.000 063 by replication assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID1891850 | AUC (24 hrs) in rat at 5 mg/kg, po | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Development of Azaindole-Based Frameworks as Potential Antiviral Agents and Their Future Perspectives. |
| AID1454914 | Dissociation constant, pKa of the compound | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID446489 | Inhibition of recombinant CYP2D6 | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID698444 | Aqueous solubility of compound at pH 1.5 after 18 to 24 hrs by RP-HPLC analysis | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2 |
| AID446497 | AUC in rat at 5 mg/kg, po | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID421170 | Cytotoxicity against human U87 cells coexpressing CD4, CxCR4 receptors after 72 hrs | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID724743 | Cytotoxicity against human HeLa cells expressing CD4 assessed as cell viability after 6 days by XTT assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Inhibitors of HIV-1 attachment. Part 7: indole-7-carboxamides as potent and orally bioavailable antiviral agents. |
| AID1505624 | Oral bioavailability in cynomolgus monkey at 5 mg/kg administered via gavage | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID446487 | Inhibition of recombinant CYP3A4 using benzyloxy-4-(trifluoromethyl)coumarin as substrate | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID730253 | Antiviral activity against HIV1 JRFL infected in human HeLa67 cells after 3 days by single cycle pseudotype-based luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p |
| AID446484 | Lipophilicity, log D at pH 6.5 | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID698637 | Plasma concentration in high fat fed healthy human at 800 mg, po administered as capsule with high fat meal measured after 12 hrs | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2 |
| AID443367 | Cytotoxicity against human hepatocytes up to 200 uM in presence of CYP450 enzymes | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1454910 | Inhibition of [3H]BMS-488043 binding to HIV-1 isolate JRFL gp120 assessed as association half life after 60 mins by scintillation counting method | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID1505621 | Oral bioavailability in beagle dog at 5 mg/kg | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID421169 | Inhibition of HIV1 3B recombinant gp120/sCD4 binding interaction by ELISA | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID1891844 | Solubility of the compound at pH 4 to 8 | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Development of Azaindole-Based Frameworks as Potential Antiviral Agents and Their Future Perspectives. |
| AID1505605 | AUC in Sprague-Dawley rat at 5 mg/kg, po after 24 hrs | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID730237 | Antiviral activity against X4-tropic HIV1 NL4-3 infected in MT2 cells | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p |
| AID421181 | Antiviral activity against HIV isolate 589.000 033 by replication assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID730245 | Clearance in iv dosed rat | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p |
| AID730247 | AUC in rat at 5 mg/kg, po at 24 hrs | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p |
| AID446503 | Stability at pH 2 after 48 hrs | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1891849 | Antiviral activity against HIV-1 JRFL assessed as inhibition of viral growth | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Development of Azaindole-Based Frameworks as Potential Antiviral Agents and Their Future Perspectives. |
| AID698644 | Dissociation constant, pKa of compound | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2 |
| AID446494 | Oral bioavailability in dog at 5 mg/kg | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1505626 | Total clearance in cynomolgus monkey at 1 mg/kg, iv | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID1505601 | Permeability in human Caco2 cells | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID443370 | Cmax in dog at 200 mg/kg | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID443375 | Ratio of plasma concentration in rat at 5 mg/kg, po to EC50 for HIV1 clinical isolates | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1454953 | Antiviral activity against HIV-1 JR-FL infected in human PM1 cells harboring CCR5 co-receptor after 4 to 6 days by p24 ELISA | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID1505622 | AUC in beagle dog at 5 mg/kg, po | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID446493 | Inhibition of human ERG by channel flux assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID421175 | Antiviral activity against HIV isolate 584.000 060 by replication assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID725386 | Oral bioavailability in rat at 5 mg/kg | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Inhibitors of HIV-1 attachment. Part 11: the discovery and structure-activity relationships associated with 4,6-diazaindole cores. |
| AID1454954 | Antiviral activity against HIV-1 SF-162 infected in human PM1 cells harboring CCR5 co-receptor after 4 to 6 days by p24 ELISA | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID421173 | Antiviral activity against HIV isolate 584.000 031 by replication assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID1891841 | Oral bioavailability in dog | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Development of Azaindole-Based Frameworks as Potential Antiviral Agents and Their Future Perspectives. |
| AID730246 | Cmax in rat at 5 mg/kg, po | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p |
| AID446492 | Aqueous solubility of crystalline form of compound in buffer solution of pH 6.5 at 25 degC | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID446479 | Inhibition of HIV1 JRFL gp120/CD4 interaction in human HeLa67 cells assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID724744 | Antiviral activity against HIV1 JRFL infected in human HeLa cells expressing CD4 and CCR5 assessed as inhibition of single-cycle viral replication by luciferase reporter gene assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Inhibitors of HIV-1 attachment. Part 7: indole-7-carboxamides as potent and orally bioavailable antiviral agents. |
| AID1454973 | Antiviral activity against HIV1 infected in human assessed as decrease in viral load in plasma at 1800 mg bid measured on day 8 | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID446506 | Cytotoxicity against human PBMC | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID421179 | Antiviral activity against HIV isolate 584.000 220 by replication assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID698633 | Cmax in high fat fed healthy human at 800 mg, po administered as capsule with high fat meal | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2 |
| AID698634 | Tmax in high fat fed healthy human at 800 mg, po administered as capsule with high fat meal | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2 |
| AID446491 | Inhibition of recombinant CYP1A2 | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID421177 | Antiviral activity against HIV isolate 584.000 066 by replication assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID304720 | Antiviral activity against HIV1 pseudovirus in U87 cells expressing CD4 and CCR5 after 72 hrs by M33 pseudotyped assay | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
| Design and synthesis of human immunodeficiency virus entry inhibitors: sulfonamide as an isostere for the alpha-ketoamide group. |
| AID446480 | Inhibition of HIV1 LAI gp120/CD4 interaction in human HeLa67 cells assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID698451 | Lipophilicity, log P of compound in octanol-PBS mixture at pH 6.5 by HPLC-UV analysis | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2 |
| AID1505599 | Half life in human liver microsomes | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID421172 | Antiviral activity against HIV isolate 584.000 030 by replication assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID730234 | Antiviral activity against R5-tropic HIV1 JRFL infected in PM1 cells | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p |
| AID446501 | Solubility at pH 1.5 | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1891840 | Oral bioavailability in rat | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Development of Azaindole-Based Frameworks as Potential Antiviral Agents and Their Future Perspectives. |
| AID1454924 | Inhibition of [3H]BMS-488043 binding to HIV-1 isolate JRFL gp120 after 60 mins by scintillation counting method | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID730249 | Oral bioavailability in rat at 5 mg/kg | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p |
| AID1454958 | Antiviral activity against HIV-1 isolate MN infected in human MT2 cells harboring CXCR4 co-receptor after 4 to 6 days | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID698443 | Toxicity in HIV 1-infected human assessed as adverse events at 1800 mg, po bid for 8 days measured upto 14 days | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2 |
| AID443372 | Cytotoxicity against human neuronal tumor cells | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID443377 | Ratio of plasma concentration in monkey at 5 mg/kg, po to EC50 for HIV1 clinical isolates | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1505632 | Antiviral activity against HIV1 infected in patients assessed as reduction in plasma viral load by measuring log10 viral copies at 1800 mg, bid measured at day 8 | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID446495 | Oral bioavailability in monkey at 5 mg/kg | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID446481 | Metabolic stability in human liver microsomes assessed as half life | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1505630 | Antiviral activity against ENV pseudotyped CCR5-tropic HIV1 JFRL infected in human HeLa67 cells after 3 days by luciferase reporter gene assay | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID1454915 | Protein binding in human plasma | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID443366 | Cytotoxicity against HEK cells | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID730236 | Antiviral activity against R5-tropic HIV1 BAL infected in PM1 cells | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p |
| AID698449 | Antiviral activity against HIV 1-infected human assessed as reduction in viral load at 1800 mg, po bid for 8 days measured upto 14 days | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2 |
| AID698445 | Aqueous solubility of compound at pH 10 | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2 |
| AID730235 | Antiviral activity against X4-tropic HIV1 MN infected in MT2 cells | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p |
| AID421168 | Antiviral activity against HIV1 expressed in 293T cells assessed as protection against viral M33 envelope infection in human U87 cells coexpressing CD4, CCR5 receptors after 72 hrs by luciferase reporter gene pseudoviral assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID421180 | Antiviral activity against HIV isolate 584.000 227 by replication assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID1505607 | Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID304721 | Cytotoxicity against human U87 cells expressing CD4 and CXCR4 | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
| Design and synthesis of human immunodeficiency virus entry inhibitors: sulfonamide as an isostere for the alpha-ketoamide group. |
| AID421171 | Antiviral activity against HIV isolate 584.000 017 by replication assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID446482 | Cytotoxicity against human MT2 cells after 3 days by XTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID443369 | Cardiotoxicity in dog assessed as changes in ECG at 200 mg/kg | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1454957 | Antiviral activity against HIV-1 NL4 - 3 infected in human MT2 cells harboring CXCR4 co-receptor after 4 to 6 days | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID1454959 | Antiviral activity against HIV-1 3B infected in human MT2 cells harboring CXCR4 co-receptor after 4 to 6 days | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID446490 | Inhibition of recombinant CYP2C19 | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1505635 | Inhibition of [3H]BMS-488043 binding to HIV-1 JRFL gp120 after 1 hr by scintillation counting method | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID443373 | Cytotoxicity against human cervical cancer cells | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1505604 | Oral bioavailability in Sprague-Dawley rat at 5 mg/kg | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID1505633 | Antiviral activity against HIV1 infected in patients assessed as reduction in maxmum viral RNA by measuring log10 viral copies at 800 mg, bid measured at day 8 | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID1891851 | Cmax in rat at 5 mg/kg, po | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Development of Azaindole-Based Frameworks as Potential Antiviral Agents and Their Future Perspectives. |
| AID1295703 | Aqueous solubility of the compound at pH 4 to 8 | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends. |
| AID1454955 | Antiviral activity against HIV-1 Bal infected in human PM1 cells harboring CCR5 co-receptor after 4 to 6 days by p24 ELISA | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID446499 | Oral bioavailability in rat at 5 mg/kg administered as solution in 90% PEG400/10% EtOH | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID730244 | Volume of distribution at steady state in iv dosed rat | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p |
| AID1891852 | Clearance in rat administered intravenously | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Development of Azaindole-Based Frameworks as Potential Antiviral Agents and Their Future Perspectives. |
| AID730252 | Cytotoxicity against human HeLa cells | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p |
| AID1505651 | Selectivity ratio of EC50 for ENV pseudotyped CCR5-tropic HIV1 JFRL in presence of 40%human serum to EC50 for ENV pseudotyped CCR5-tropic HIV1 JFRL in absence of 40%human serum | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID698453 | Permeability across human Caco2 cells at pH 6.5 | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2 |
| AID443380 | Aqueous solubility of crystalline form of compound in buffer solution of pH 1.5 at 25 degC | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID443376 | Ratio of plasma concentration in dog at 5 mg/kg, po to EC50 for HIV1 clinical isolates | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID421182 | Antiviral activity against HIV isolate 584.000 058 by replication assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Heterobiaryl human immunodeficiency virus entry inhibitors. |
| AID446496 | Cmax in rat at 5 mg/kg, po | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID446505 | Cytotoxicity against human T cell | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1454923 | Competitive inhibition of soluble CD4 binding to HIV-1 gp120 after 2 hrs by ELISA | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID446502 | Solubility at pH 4 to 8 | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1891842 | Oral bioavailability in monkey | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Development of Azaindole-Based Frameworks as Potential Antiviral Agents and Their Future Perspectives. |
| AID730238 | Antiviral activity against X4-tropic HIV1 LAI infected in MT2 cells | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p |
| AID443365 | Cytotoxicity against human lung cancer cell | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID443368 | Cytotoxicity against human hepatocytes up to 200 uM in absence of CYP450 enzymes | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1454961 | Antiviral activity against HIV-1 89.6 infected in human PM1 cells harboring dual co-receptors after 4 to 6 days by p24 ELISA | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID698635 | AUC (infinity) in high fat fed healthy human at 800 mg, po administered as capsule with high fat meal | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2 |
| AID725384 | Clearance in rat at 1 mg/kg, iv | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Inhibitors of HIV-1 attachment. Part 11: the discovery and structure-activity relationships associated with 4,6-diazaindole cores. |
| AID443371 | Cytotoxicity against human hepatic cancer cells | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1454916 | Aqueous solubility of the compound at pH 6.5 | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID1505598 | Cytotoxicity against human MT2 cells assessed as decrease in cell viability after 3 days by XTT assay | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID446485 | Antiviral activity against HIV1 clinical isolates | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID446488 | Inhibition of recombinant CYP2C9 | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1505606 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID1454929 | Half life in human administered as capsule | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID443374 | Cytotoxicity against human larynx cancer cells | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1454956 | Antiviral activity against HIV-1 LAI infected in human MT2 cells harboring CXCR4 co-receptor after 4 to 6 days | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID1505608 | Half life in Sprague-Dawley rat at 1 mg/kg, iv | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| AID1454960 | Antiviral activity against HIV-1 RF infected in human MT2 cells harboring CXCR4 co-receptor after 4 to 6 days | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir. |
| AID446500 | Oral bioavailability in rat at 5 mg/kg administered as crystalline suspension | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID446498 | Terminal half life in rat at 5 mg/kg, iv | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID446504 | Stability at pH 7 after 48 hrs | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID446483 | Permeability across human Caco-2 cell membrane at pH 6.5 | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug ca |
| AID1505623 | Total clearance in beagle dog at 1 mg/kg, iv | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |