Assay ID | Title | Year | Journal | Article |
AID1197829 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
AID197943 | In vitro inhibition of mutant Y181C recombinant reverse transcriptase of HIV-1 IIIB | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
| Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors. |
AID1446816 | Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID1200844 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
AID1292013 | Selectivity index, ratio of CC50 for mock infected human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/YI81C double mutant infected in human MT4 cells | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
AID484294 | Colloidal aggregation in fed state simulated intestinal fluid at 700 uM by transmission electron microscopy in presence of 3% DMSO | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
AID648424 | Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID619634 | Antiviral activity against HIV-1 3B harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID619635 | Antiviral activity against HIV-1 3B harboring RT K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID1059145 | Antiviral activity against drug-resistant HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID143391 | Inhibitory activity against non-nucleoside reverse transcriptase inhibitors (NNRTI) -resistant HIV-1 strain A17 with a Y181C mutation in RT (reverse transcriptase) | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
| Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds. |
AID197944 | In vitro inhibition of recombinant reverse transcriptase (WT) of HIV-1 IIIB | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
| Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors. |
AID82141 | Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected K103N strain | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
| Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants. |
AID235444 | Selective index as the ratio of CD50 to that of ED50 against HIV-1 HxB2 strain. | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
| Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants. |
AID1165077 | Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
AID484282 | Colloidal aggregation in fed state simulated intestinal fluid by dynamic light scattering assay in presence of 3% DMSO | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
AID484275 | Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in presence of 0.01% Triton X-100 | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
AID665551 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
| Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
AID1292011 | Cytotoxicity against mock infected human MT4 cells after 4 days by MTT assay | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
AID1446819 | Antiviral activity against HIV1 harboring E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID1197833 | Resistance index, ratio of EC50 for HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant to EC50 for wild type HIV1 3B | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
AID227244 | The compound was evaluated for antiviral activity using whole cell assay | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
| Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors. |
AID619643 | Ratio of EC50 for HIV-1 3B harboring RT L100I mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID1446811 | Antiviral activity against HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID105859 | Compound was tested for potency to achieve protection of MT-4 cells from 101E strain of HIV-1 virus | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU). |
AID105860 | Compound was tested for potency to achieve protection of MT-4 cells from 103N strain of HIV-1 virus | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU). |
AID1446820 | Antiviral activity against HIV1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID197788 | In vitro ability to inhibit wild type resistant (WT) reverse transcriptase | 2000 | Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
| Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives. |
AID484394 | Colloidal aggregation in fed state simulated intestinal fluid assessed as colloid radius at 600 uM by dynamic light scattering assay in presence of 3% DMSO | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
AID1446814 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID105862 | Compound was tested for potency to achieve protection of MT-4 cells from 181C strain of HIV-1 virus | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU). |
AID484274 | Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100 | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
AID82275 | Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected Y181C strain | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
| Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants. |
AID619638 | Antiviral activity against HIV-1 3B harboring RT Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID665552 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C RT mutant | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
| Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
AID484288 | Aggregation-based binding affinity to beta-lactamase AmpC at 700 uM in fed state simulated intestinal fluid after 30 mins by silver staining in presence of 3% DMSO | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
AID619641 | Ratio of EC50 for HIV-1 3B harboring RT K103N mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID354464 | Antiviral activity against HIV1 3B infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect after 6 days by MTS assay | 2004 | Journal of natural products, Jun, Volume: 67, Issue:6
| New 3-O-acyl betulinic acids from Strychnos vanprukii Craib. |
AID11497 | Bioavailability at an iv dose of 14 mg/Kg and po dose of 28 mg/Kg | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
| Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors. |
AID619636 | Antiviral activity against HIV-1 3B harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID1197830 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
AID619639 | Antiviral activity against HIV-1 3B harboring RT F227L and V106A mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID82277 | Inhibition of HIV-1 IIIB replication in MT-4-infected wild type cells. | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
| Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants. |
AID105863 | Compound was tested for potency to achieve protection of MT-4 cells from 188L strain of HIV-1 virus | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU). |
AID235446 | Selective index (CD50 compared to ED50 against HIV-1 IIIB strain). | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
| Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants. |
AID82276 | Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected Y181C+K103N strain | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
| Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants. |
AID198563 | The compound was evaluated for the inhibition of HIV-1 reverse transcriptase | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
| Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors. |
AID152788 | Tested for the ability to inhibit the replication of HIV-1 strain HTLV IIIB in human peripheral blood mononuclear cells (PBMC) | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
| Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds. |
AID1446813 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID153129 | Cytotoxic concentration was determined | 2000 | Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
| Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives. |
AID1059141 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for drug-resistant HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID106769 | Cytotoxic dose required to reduce the viability of normal uninfected MT-4 cells by 50% | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
| Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants. |
AID484280 | Colloidal aggregation in fed state simulated intestinal fluid by dynamic light scattering assay in presence of 0.5% DMSO | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
AID105866 | Compound was tested for potency to achieve protection of MT-4 cells from LAI strain of HIV-1 virus | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU). |
AID484286 | Colloidal aggregation in fed state simulated intestinal fluid assessed as critical aggregation concentration by UV-visible spectrophotometry in presence of 0.35% DMSO | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
AID354455 | Antiviral activity against HIV1 3B infected in human HOG.R5 cells after 4 days | 2004 | Journal of natural products, Jun, Volume: 67, Issue:6
| New 3-O-acyl betulinic acids from Strychnos vanprukii Craib. |
AID1446815 | Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID1292012 | Selectivity index, ratio of CC50 for mock infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
AID484385 | Colloidal aggregation in fed state simulated intestinal fluid assessed as colloid radius at 100 uM by dynamic light scattering assay in presence of 1% DMSO | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
AID1200845 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
AID1165075 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
AID82272 | Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected wild type cells | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
| Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants. |
AID11496 | Bioavailability at an iv dose of 14 mg/Kg and po dose of 15 mg/Kg | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
| Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors. |
AID648422 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID619640 | Antiviral activity against HIV-1 3B harboring RT K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID1197831 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
AID665553 | Fold resistance, ratio of EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C RT mutant to EC50 for wild type HIV1 3B | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
| Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
AID1200846 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
AID1292009 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as cell viability after 4 days by MTT assay | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
AID1059146 | Antiviral activity against HIV1 3B infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1059144 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1165074 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
AID484295 | Colloidal aggregation in phosphate buffer at 200 uM by transmission electron microscopy in presence of 0.2% DMSO | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
AID1200847 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
AID1446812 | Antiviral activity against HIV-2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID153130 | Effective dose for inhibition of viral replication in cell culture of 0.1 uM | 2000 | Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
| Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives. |
AID11014 | Clearance at an iv dose of 14 mg/Kg and po dose of 15 mg/Kg | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
| Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors. |
AID354458 | Cytotoxicity against human CEM-SS cells at 40 ug/ml after 6 days by MTS assay | 2004 | Journal of natural products, Jun, Volume: 67, Issue:6
| New 3-O-acyl betulinic acids from Strychnos vanprukii Craib. |
AID105864 | Compound was tested for potency to achieve protection of MT-4 cells from 190A strain of HIV-1 virus | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU). |
AID484390 | Colloidal aggregation in fed state simulated intestinal fluid by dynamic light scattering-based beads autocorrelation assay in presence of 1% DMSO | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
AID665547 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
| Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
AID1197834 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
AID354454 | Cytotoxicity against human HOG.R5 cells at 40 ug/ml after 4 days | 2004 | Journal of natural products, Jun, Volume: 67, Issue:6
| New 3-O-acyl betulinic acids from Strychnos vanprukii Craib. |
AID105858 | Compound was tested for potency to achieve protection of MT-4 cells from 100I strain of HIV-1 virus | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU). |
AID197941 | In vitro inhibition of mutant P236L recombinant reverse transcriptase of HIV-1 IIIB | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
| Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors. |
AID1446818 | Antiviral activity against HIV1 harboring Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID82271 | Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected Y181C strain | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
| Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants. |
AID1059143 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID665550 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
| Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
AID619642 | Ratio of EC50 for HIV-1 3B harboring RT E138K mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID665549 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
| Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
AID1165078 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
AID648421 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1165076 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
AID619637 | Antiviral activity against HIV-1 3B harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID1197832 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
AID1446817 | Antiviral activity against HIV1 harboring Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID1200843 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
AID484290 | Binding affinity to beta-lactamase AmpC at 700 uM after 30 mins by SDS-PAGE | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
AID648420 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID105861 | Compound was tested for potency to achieve protection of MT-4 cells from 106A strain of HIV-1 virus | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU). |
AID197787 | In vitro ability to inhibit mutant P236L reverse transcriptase | 2000 | Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
| Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives. |
AID143390 | Inhibitory activity against non-nucleoside reverse transcriptase inhibitors (NNRTI) -resistant HIV-1 strain A17 variant with Y181C plus K103N mutations in RT (reverse transcriptase) | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
| Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds. |
AID1292010 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/YI81C double mutant infected in human MT4 cells assessed as cell viability after 4 days by MTT assay | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |