Assay ID | Title | Year | Journal | Article |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
| Identification of potent Yes1 kinase inhibitors using a library screening approach. |
AID1798816 | Reverse Transcriptase Assay from Article 10.1021/jm801395v: \\Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations.\\ | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
AID1795395 | HIV-1 RT Assay from Article 10.1021/jm0211063: \\Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.\\ | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
| Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies. |
AID1795743 | HIV-1 RT Assay from Article 10.1016/j.bmc.2004.08.050: \\Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides.\\ | 2004 | Bioorganic & medicinal chemistry, Dec-01, Volume: 12, Issue:23
| Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides. |
AID1795423 | HIV-1 RT Assay from Article 10.1021/jm990095j: \\Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.\\ | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
| Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues. |
AID1802513 | DNA Polymerase Assay from Article 10.1002/cbic.201600592: \\Natural Product Kuwanon-L Inhibits HIV-1 Replication through Multiple Target Binding.\\ | 2017 | Chembiochem : a European journal of chemical biology, 02-16, Volume: 18, Issue:4
| Natural Product Kuwanon-L Inhibits HIV-1 Replication through Multiple Target Binding. |
AID1801910 | HIV-1 RT Colorimetric Assay from Article 10.1016/j.bioorg.2016.05.009: \\Rational design, synthesis, anti-HIV-1 RT and antimicrobial activity of novel 3-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-1-(piperazin-1-yl)propan-1-one derivatives.\\ | 2016 | Bioorganic chemistry, 08, Volume: 67 | Rational design, synthesis, anti-HIV-1 RT and antimicrobial activity of novel 3-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-1-(piperazin-1-yl)propan-1-one derivatives. |
AID1795438 | HIV-1 RT Assay from Article 10.1016/S0960-894X(01)00331-6: \\Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.\\ | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
| Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors. |
AID1795433 | HIV-1 RT Assay from Article 10.1021/jm990580e: \\Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.\\ | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID1802514 | RNAse H-Polymerase-Independent Cleavage Assay from Article 10.1002/cbic.201600592: \\Natural Product Kuwanon-L Inhibits HIV-1 Replication through Multiple Target Binding.\\ | 2017 | Chembiochem : a European journal of chemical biology, 02-16, Volume: 18, Issue:4
| Natural Product Kuwanon-L Inhibits HIV-1 Replication through Multiple Target Binding. |
AID1795727 | HIV-1 RT Assay from Article 10.1016/j.bmc.2004.11.045: \\Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives.\\ | 2005 | Bioorganic & medicinal chemistry, Feb-15, Volume: 13, Issue:4
| Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives. |
AID1795435 | HIV-1 RT Assay from Article 10.1016/s0960-894x(99)00486-2: \\Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors.\\ | 1999 | Bioorganic & medicinal chemistry letters, Oct-04, Volume: 9, Issue:19
| Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors. |
AID1795437 | HIV-1 RT Assay from Article 10.1016/s0960-894x(00)00321-8: \\Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.\\ | 2000 | Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
| Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors. |
AID1798815 | Reverse Transcriptase Assay from Article 10.1021/jm801322h: \\Novel Indazole Non-Nucleoside Reverse Transcriptase Inhibitors Using Molecular Hybridization Based on Crystallographic Overlays (dagger).\\ | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays. |
AID1795436 | HIV-1 RT Assay from Article 10.1016/s0960-894x(99)00565-x: \\Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA).\\ | 1999 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
| Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA). |
AID1801530 | In-vitro HIV-1 RT Screening from Article 10.1016/j.bioorg.2015.12.005: \\Design, synthesis and in-vitro evaluation of novel tetrahydroquinoline carbamates as HIV-1 RT inhibitor and their antifungal activity.\\ | 2016 | Bioorganic chemistry, Feb, Volume: 64 | Design, synthesis and in-vitro evaluation of novel tetrahydroquinoline carbamates as HIV-1 RT inhibitor and their antifungal activity. |
AID1801804 | RNA-dependent DNA Polymerase (RDDP) Assay from Article 10.1002/cbic.201500668: \\Inhibition of HIV-1 Reverse Transcriptase Dimerization by Small Molecules.\\ | 2016 | Chembiochem : a European journal of chemical biology, Apr-15, Volume: 17, Issue:8
| Inhibition of HIV-1 Reverse Transcriptase Dimerization by Small Molecules. |
AID1802605 | HIV-1 RT In-Vitro Assay from Article 10.1016/j.bioorg.2017.03.013: \\Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives.\\ | 2017 | Bioorganic chemistry, 06, Volume: 72 | Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives. |
AID1795434 | HIV-1 RT Assay from Article 10.1016/s0960-894x(01)00239-6: \\4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.\\ | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
| 4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID586360 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T66I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vir | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
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. |
AID248880 | Inhibitory concentration against human immunodeficiency virus type 1 (with K103N/Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2. |
AID587749 | Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as inhibition of 2 mins magnetic nanopartials-medated infectiv | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
AID342718 | Inhibition of HIV1 reverse transcriptase RNA-dependent DNA polymerase activity assessed as incorporation of radioactive dTTP into poly(rA)/oligo(DT) | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors. |
AID1212882 | Drug metabolism in microsomes expressing CYP2B6.1 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in presence of Cyt b5 coexpression | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID1457056 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID1884225 | Antiviral activity against HIV-1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID1729149 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID557040 | Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1435502 | Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | | | |
AID416758 | Antiviral activity against HIV1 with reverse transcriptase Y181I mutation in human CEM cells assessed as protection against virus-induced cytopathicity | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus. |
AID586486 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E138A/S147G/Q148R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunod | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1348220 | Antiviral activity against HIV1 pNL4-3 infected in HEK293 cells assessed as reduction in viral transcription by measuring decrease in luciferase activity at 1 uM after 20 hrs by luciferase reporter gene assay | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12
| Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities. |
AID279397 | Antiviral activity against HIV1 isolate with RT 188L mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1157592 | Antiviral activity against 6-[(3,5-Dimethylphenyl)fluoromethyl]-5-ethyl-1-{[[4-(3-hydroxyprop-1-ynyl)benzyl]oxy]methyl}pyrimidine-2,4(1H,3H)-dione-resistant HIV1 harboring RT 106I, 181C mutant infected in human MT4 cells assessed as inhibition of virus-in | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID1171588 | Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-3 | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID522368 | Antiviral activity against wild type HIV1 infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID1069710 | Inhibition of GST-tagged recombinant wild type HIV-1 reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli JM109 using dTTP as substrate after 40 mins by spectrofluorometric analysis | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
| Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
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. |
AID709836 | Ratio of EC50 for HIV1 expressing wild type reverse transcriptase in presence of human serum albumin and human alpha-1 acid glycoprotein to EC50 for HIV1 expressing wild type reverse transcriptase | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1784586 | Inhibition of HIV-1 reverse transcriptase using Cy5-CAGGAAACAGCTATGAC/3'-GTCCTTTGTCGATACTGTTTTTTT-5' as primer/template at 5 to 50 uM preincubated for 20 min followed by dATP addition measured after 5 to 10 mins by gel electrophoresis analysis | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Exploring the dNTP -binding site of HIV-1 reverse transcriptase for inhibitor design. |
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. |
AID496630 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase Y181C/V35T, V60I, I135V, S162A, K173T, Q174K, N175Y, D177E, T200A, Q207E, R211K, H221Y mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID523481 | Antiviral activity against HIV1 with RT connection domain G190S/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID1574388 | Resistance index, ratio of ID50 for recombinant HIV-1 His-tagged reverse transcriptase p66/p51 K103N mutant to ID50 for recombinant wild type HIV-1 reverse transcriptase His-tagged p66/p51 | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID557019 | Inhibition of HIV1 isolate R8 reverse transcriptase after 90 mins | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID248261 | In vitro inhibitory concentration against HIV L100I mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
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. |
AID266347 | Inhibition of HIV1 reverse transcriptase Y181C mutant in 293T cells | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity. |
AID293563 | Antiviral activity against HIV1 LAI with RT L100I and K103N mutation in MT4 cells by EGFP based replication assay | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5
| Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains. |
AID279472 | Antiviral activity against HIV1 isolate with RT 103S mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID247500 | Inhibitory activity against HIV-1 mutant strain 179E | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID527562 | Antiviral activity against HIV1 NL4-3 containing reverse transcriptase K103N mutation infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1057040 | Antiviral activity against wild-type HIV1 3B infected in MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
| Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs. |
AID508752 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID141359 | Potency of second-generation NNRTIs against Mutant HIV-1 sV179D/L100I/Y181C free drug | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID1572525 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
AID1457069 | Downregulation of iNOS mRNA levels in C57BL/6 mouse BV2 cells at 1000 nM after 24 hrs by RT-PCR assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID698299 | Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4-3 | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID199980 | Inhibitory activity against human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations. |
AID1750721 | Inhibition of HIV-1 p66/p51 reverse transcriptase E138K mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID443680 | Antiviral activity against HIV with reverse transcriptase Y188L mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
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. |
AID443684 | Antiviral activity against HIV with reverse transcriptase K103N/Y181C double mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID519866 | Antiviral activity against HIV1 subtype B-93US143 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID1729153 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID1884223 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against wildtype HIV-1 3B infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID1435505 | Antiviral activity against HIV1 expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | | | |
AID541171 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring L74M and E92V mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1198749 | Inhibition of HIV1 reverse transcriptase-associated RNA-dependent DNA polymerase activity after 30 mins | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase. |
AID361920 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase P225H mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1773458 | Resistance factor, ratio of EC50 for HIV1 harboring K103N mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells | | | |
AID1456310 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. |
AID361924 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/V108I mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID496624 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/A33E, V35T, T39A, D123E, S162A, Q174G, T200E, I202V, Q207E mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID241472 | Inhibitory concentration against HIV-1 mutant reverse transcriptase (Y181C) | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
| Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives. |
AID1561717 | Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of (E)-4-((4-((4-(4-(2-Cyanovinyl)-2,6-dimethylphenoxy)thieno[2,3- d]pyrimidin-2-yl)amino)piperidin-1-yl)methyl)benzenesulfonamide assessed as protection ag | | | |
AID446239 | Cytotoxicity against human SupT1 cells | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
AID698300 | Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4-3 | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1815390 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 of Anti-HIV activity against HIV-1 IIIB infected in human MT4 | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID279480 | Antiviral activity against HIV1 isolate with RT 100F mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1750719 | Inhibition of HIV-1 p66/p51 reverse transcriptase Y181C mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID1264550 | Selectivity ratio for antiviral activity against HIV-1 expressing reverse transcriptase K101P mutant to HIV-1 expressing wild-type reverse transcriptase | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
| Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance. |
AID1750723 | Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase L100I mutant | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID541167 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring Q148K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID519891 | Selectivity ratio of EC50 for 0.02 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.02 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
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. |
AID519876 | Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID508768 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID386492 | Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Parallel synthesis, molecular modelling and structure-activity relationship studies on analogues of O-(2-phenylethyl)-N-phenylthiocarbamate. |
AID665272 | Antiviral activity against HIV1 RES056 harboring K103N/Y181C RT mutant infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID1884489 | Antiviral activity against drug-resistant HIV-1 L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID490362 | Antiviral activity against wild type HIV1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect in presence of 10 % fetal bovine serum | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses. |
AID1880374 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Structure-Based Discovery of Novel NH |
AID573246 | Cmin in HIV-1 infected children at 10 to 15 mg/kg, po administered once daily by HPLC | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID508769 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase H221Y mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID253493 | Dose required to inhibit HIV-1 reverse transcriptase activity (Y181I mutant) by 50% | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
| Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation. |
AID347607 | Antiviral activity against wild type HIV HXB2 in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay in presence of 40% human serum | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID448395 | Inhibition of wild type HIV reverse transcriptase in presence of poly(rA) 300 template, (dT) 16 primer | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 3: optimisation of physicochemical properties. |
AID1157580 | Cytotoxicity against human MT4 cells after 96 hrs by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID1171593 | Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in enzyme activity | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1736361 | Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase V108I/K103N double mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hr | | | |
AID508758 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, Y181I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1316335 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1583022 | Selectivity index, ratio of CC50 for cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
| Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel. |
AID1815400 | Inhibition of HIV1 reverse transcriptase Y188L mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1212918 | Drug metabolism in microsomes expressing CYP2B6.6 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in absence of Cyt b5 coexpression | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID279464 | Antiviral activity against HIV1 isolate with RT 101Q, 103N, 225H mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1379964 | Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 assessed as reduction in biotin-dUTP incorporation incubated for 40 mins using poly(rA) template and oligo(dT)16 primer by picogreen dye based spectrofluorometry | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs. |
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. |
AID523356 | Antiviral activity against HIV1 with RT connection domain Y181C/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID302270 | Resistance index, ratio of Ki for HIV1 reverse transcriptase Y181I mutant to Ki for wild type HIV1 3B reverse transcriptase | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
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. |
AID1069707 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
| Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1435504 | Antiviral activity against HIV1 expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | | | |
AID1316336 | Antiviral activity against HIV1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID586367 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase F121Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1731747 | Inhibition of reverse transcriptase K103N mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID368569 | Inhibition of HIV1 recombinant reverse transcriptase K103N mutant-DNA-dNTP ternary complex expressed in Escherichia coli BL21 | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID562698 | Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as decrease in virus production at 2 times EC90 after 72 hrs by beta-galactosidase reporter gene assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation. |
AID698303 | Cytotoxicity against mock-infected human MT4 cells measured after 5 days by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID464767 | Binding affinity to human serum albumin | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1352318 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID293176 | Antiviral activity against HIV1 RT 181C mutant assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method | 2007 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
| Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity. |
AID391224 | Antiviral activity against wild type HIV1 infected in human MT4 cells after 72 hrs in presence of 10% fetal bovine serum | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
| Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses. |
AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID152959 | Antiviral activity of Protein Binding of compound was evaluated for Thai 9466 virus expressed PBMC by P24 | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID1171597 | Inhibition of wild type HIV1 reverse transcriptase V106A mutant assessed as reduction in enzyme activity | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1186000 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/P225H double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID650690 | Inhibition of HIV 1 reverse transcriptase Y181I mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT) | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID1261312 | Antiviral activity against BVDV infected in MDBK cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
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. |
AID1736349 | Inhibition of RNase H activity of HIV-1 reverse transcriptase using DNA/RNA hybrid as substrate incubated for 30 mins by fluorescence based analysis | | | |
AID464765 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1653628 | Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) F416A mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID476471 | Cytotoxicity against human MT2 cells infected with HIV1 harboring reverse transcriptase Y181C mutation by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
| Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives. |
AID1457057 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID240140 | Concentration required to inhibit HIV-1 reverse transcriptase activity (wild-type) by 50% | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
| Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation. |
AID572179 | Antiviral activity against HIV-1 subtype O V029524 harboring NNRTI A98G, V179E and Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1157581 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
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. |
AID1773459 | Resistance factor, ratio of EC50 for HIV1 harboring Y18IC mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells | | | |
AID298079 | Antiviral activity against HIV1 RT 112 mutant in lymphocytes assessed as reduction of p24 antigen production | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. |
AID263513 | Antiviral activity against HIV1 K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2. |
AID279488 | Antiviral activity against HIV1 isolate with RT G190S mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
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. |
AID279402 | Antiviral activity against HIV1 isolate with RT 103N, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID508658 | Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF03 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1880380 | Antiviral activity against HIV-1 IIIB harboring reverse transcriptase E138K mutant infected in human MT4 cells by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Structure-Based Discovery of Novel NH |
AID1736348 | Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase K103N mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hrs post-infect | | | |
AID279414 | Antiviral activity against HIV1 isolate with RT 108I, 181C mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1750716 | Selectivity index, ratio of CC50 for human MT-4 cells to EC50 for HIV-1 infected in MT-4 cells | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID1773446 | Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | | | |
AID1609105 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 of antiviral activity against HIV-1 IIIB infected in human MT4 cells | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID508756 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179D, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID576026 | Half life in healthy human plasma at 400 mg, po measured on day 1 post dose by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID465423 | Volume of distribution at steady state in Beagle dog at 0.5 mg/kg, iv or. 5 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID519874 | Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID573982 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for Simian immunodeficiency virus MAC 251 | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID247501 | Inhibitory activity against HIV-1 mutant strain 181C | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID523482 | Antiviral activity against HIV1 with RT connection domain G190S/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID226236 | Fold resistance (L100I/ WT) (as per ref 10 in the article) | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
| Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs. |
AID576048 | Reduction in ABCC1 mRNA expression in healthy human at 400 mg, po qd for 14 days by RT-PCR | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID519962 | Selectivity ratio of EC50 for 0.05 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by MTS assay to EC50 for 0.05 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID586384 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase N155S mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1379961 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by measuring virus-induced syncytium formation by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs. |
AID293558 | Antiviral activity against HIV1 LAI with RT L100I mutation in MT4 cells by EGFP based replication assay | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5
| Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains. |
AID269686 | Antiviral activity against HIV1 NNTRI resistant Y188L mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269686 | Antiviral activity against HIV1 NNTRI resistant Y188L mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269686 | Antiviral activity against HIV1 NNTRI resistant Y188L mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1731745 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB | | | |
AID267859 | Cytotoxicity against MT4 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1773449 | Antiviral activity against wild type HIV1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | | | |
AID464772 | Oral bioavailability in Beagle dog at 4 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID366557 | Antiviral activity against HIV1 with reverse transcriptase G190A mutation in human MT4 cells assessed as reduction of virus-induced cytopathic effect | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1596751 | Antiviral activity against wild type HIV-1 3B infected in MT4 cells measured after 5 days by MTT assay | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains. |
AID508830 | Antiviral activity against Human immunodeficiency virus 1 subtype B isolate WEJO infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1357795 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID443699 | Antiviral activity against HIV with reverse transcriptase G190S mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID1212893 | Drug metabolism in human liver microsomes harboring CYP2B6*1/*1 genotype assessed as CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation measured per mg protein after 15 mins by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID449492 | Selective index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
| Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1435509 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | | | |
AID1457058 | Antiviral activity against HIV1 harboring reverse transcriptase K103N /Y1881C double mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID1126506 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
| Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1558855 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID1653620 | Inhibition of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli at 60 to 100 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-ma | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID298081 | Selectivity index, ratio of TC50 for lymphocytes to ED50 for HIV1 3B | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. |
AID1435516 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase E138K mutant | | | |
AID508782 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138Q mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1609110 | Inhibition of recombinant HIV-1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye based spectrofluorometric assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID607875 | Cytotoxic activity against human MT4 cells assessed as viability of mock-infected cells after 5 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
| Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1736357 | Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase K103N/Y181C double mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hr | | | |
AID541170 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring N155S mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1212915 | Drug metabolism in microsomes expressing CYP2B6.1 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in absence of Cyt b5 coexpression | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID1736346 | Selectivity index, ratio of CC50 for human HEK 293T cells to EC50 for VSVG/wild type HIV1 infected in human HEK 293T cells | | | |
AID573985 | Antiviral activity against Reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID557025 | Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N and G190A mutant relative to drug-sensitive HIV1 CNDO | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID443704 | Antiviral activity against HIV with reverse transcriptase K103N/P225H double mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID587739 | Cytotoxicity against human HeLaT4 cells by WST-1 assay | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
AID675390 | Antiviral activity against HIV1 infected in human MT4 cells assessed as virus-induced cytopathogenicity after 4 days by MTT assay | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Disubstituted thiourea derivatives and their activity on CNS: synthesis and biological evaluation. |
AID556525 | Antiviral activity against Human immunodeficiency virus 1 clone 38086 harboring K49R, V60I, I135V, Q145M, Q174H, G196E, Q207E, R211K, V245K mutation in reverse transcriptase by phenosense assay relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility. |
AID1390711 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
| First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain. |
AID1220368 | Drug metabolism in human seminal plasma assessed as formation of N- and O-linked glucuronidated metabolite at 100 mg administered every 4 hrs by UPLC-MS/MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
| Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid. |
AID1815402 | Inhibition of HIV1 reverse transcriptase F227L/V106A double mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1736367 | Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase G190A/K103N double mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cel | | | |
AID519877 | Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID622058 | Ratio of Ki for HIV1 RT p66/p66 homodimer K103N/Y181C double mutant to Ki for wild-type HIV1 RT p66/p66 homodimer | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID82967 | Inhibitory activity against HIV-1 reverse transcriptase | 1999 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
| Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA). |
AID1750726 | Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase Y188L mutant | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID1754639 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Antiviral activity against HIV-1 IIIB infected in human MT4 cells | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
AID1884486 | Antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID1418468 | Inhibition of recombinant wild-type HIV1 GST-fused reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in biotin-dUTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 | 2018 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 28, Issue:22
| Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine. |
AID658566 | Resistance factor, ratio of EC50 for multidrug-resistant HIV1 695-RT infected in HEK293T cells to wildtype HIV1 infected in HEK293T cells | 2012 | Journal of natural products, Mar-23, Volume: 75, Issue:3
| Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium. |
AID370724 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 expressed in Escherichia coli JM109 | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
AID82461 | Antiviral activity against K103N/L100I strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1316346 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID583847 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I, E138K mutant infected in human SupT1 cells derived from 9 viral passages with lersivirine assessed as inhibition of viral replication after 21 days relative to drug sensitive HIV | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID1163230 | Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei brucei Squib427 assessed as reduction in parasite growth after 72 hrs | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
AID738333 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs. |
AID1057036 | Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
| Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs. |
AID1457065 | Inhibition of HIV1 reverse transcriptase p66 Y181I mutant associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintillation counting | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID1212895 | Drug metabolism in human liver microsomes harboring CYP2B6*6/*6 genotype assessed as CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation measured per mg protein after 15 mins by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID279407 | Antiviral activity against HIV1 isolate with RT 98G, 103N mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID572176 | Antiviral activity against HIV-1 subtype H V022827 harboring NNRTI V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1168820 | Activity of CYP2B6 (unknown origin) assessed as maximum depletion rate constant pre-incubated for 5 mins in presence of NADPH by uHPLC-MS/MS based substrate depletion kinetics assay | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Structure-Activity Studies Reveal the Oxazinone Ring Is a Determinant of Cytochrome P450 2B6 Activity Toward Efavirenz. |
AID635346 | Cytotoxicity against human MT4 cells measured by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
AID1212894 | Drug metabolism in human liver microsomes harboring CYP2B6*1/*6 genotype assessed as CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation measured per mg protein after 15 mins by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID523350 | Antiviral activity against HIV1 with RT connection domain K103N/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID1763906 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID738334 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs. |
AID586371 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Y143C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID263518 | Antiviral activity against HIV1 V179E mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2. |
AID1198753 | Inhibition of HIV1 reverse transcriptase Lys103Asn mutant-associated DNA polymerase-independent RNase H activity after 1 hr | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase. |
AID313876 | Antiviral activity against HIV1 in MT4 cells | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase--structure-activity relationships and crystallographic analysis. |
AID1483285 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase F227L/V106A double mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID1077223 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
AID328844 | Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay | 2007 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
| Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors. |
AID361918 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K101E mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID527376 | Toxicity in human CEM-SS cells | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1155819 | Fold resistance, ratio of ID50 for HIV-1 recombinant NNTRI-resistant reverse transcriptase L100I mutant to ID50 for wild type HIV-1 recombinant reverse transcriptase | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID1565090 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID1572530 | Inhibition of HIV1 reverse transcriptase p66/p51 using poly(rA)/oligo(dT)16 as template/primer measured after 40 mins by pico-green based spectrofluorometric analysis | | | |
AID1357798 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID1156488 | Selectivity index, ratio of CC50 for human MT4 cells to IC50 for wild type HIV1 3B | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors. |
AID279466 | Antiviral activity against HIV1 isolate with RT 103N, 190S mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID293565 | Antiviral activity against HIV1 LAI with RT F227C and V106A mutation in MT4 cells by EGFP based replication assay | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5
| Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains. |
AID246343 | Effective concentration of the compound to inhibit HIV-1 mutant K103N+Y181C replication in HIV-infected MT-4 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID584046 | Ratio of IC50 for HIV1 reverse transcriptase F227C mutant to IC50 for wild type HIV1 reverse transcriptase | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID1435503 | Antiviral activity against HIV1 expressing reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | | | |
AID279438 | Antiviral activity against HIV1 isolate with RT 98G, 103N, 108I mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1741390 | Inhibition of reverse transcriptase in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID1327987 | Antiviral activity against VSV-G pseudotyped HIV1 infected in human SupT1 cells after 48 hrs by luciferase reporter gene assay | 2016 | Journal of natural products, 09-23, Volume: 79, Issue:9
| Eremophilane Sesquiterpenes from an Endophytic Fungus Periconia Species. |
AID613687 | Antitumor activity against human A375 cells xenografted in athymic nude Harlan mouse assessed as reduced tumor growth at 20 mg/kg, ip administered daily 5 days pre week measured every day | 2011 | Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16
| Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors. |
AID1157598 | Antiviral activity against HIV1 MP1308 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID576041 | Drug concentration in PBMCs of healthy human at 400 mg, po measured after 5 hrs on day 1 post dose by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID269797 | Antiviral activity against HIV1 I135V mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269797 | Antiviral activity against HIV1 I135V mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269797 | Antiviral activity against HIV1 I135V mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID279453 | Antiviral activity against HIV1 isolate with RT 98G, 100I, 103N mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID440082 | Antiviral activity against HIV1 HXB2 harboring 190S mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID1705188 | Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID1594861 | Inhibition of HIV1 reverse transcriptase | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic. |
AID573989 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for non nucleoside reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID522374 | Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106A mutant clone to EC50 for wild type HIV1 | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID1653636 | Binding affinity to recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli in absence of substrate at 24 degC by stopped-flow spectrophotometric method | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID279460 | Antiviral activity against HIV1 isolate with RT 103N, 108I, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1483269 | Antiviral activity against wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID263507 | Antiviral activity against HIV1 in HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2. |
AID663313 | Resistance ratio of ID50 for HIV1 reverse transcriptase Y181I mutant to ID50 HIV1 wild type reverse transcriptase | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID1884230 | Inhibition of wild type HIV-1 reverse transcriptase assessed as reduction of biotin-dUTP incorporation into protein using ABTS as substrate incubated for 1 hrs by ELISA analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID766431 | Cytotoxicity against human MT2 cells by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
| Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility. |
AID246244 | Effective concentration against human immunodeficiency virus type 1 wild type srtain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). |
AID279509 | Antiviral activity against HIV1 isolate with RT F227L mutation in Hela-JC-53 cells | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase 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. |
AID263517 | Antiviral activity against HIV1 E138K mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2. |
AID368556 | Inhibition of HIV1 recombinant reverse transcriptase K103N mutant-mediated RNA-dependent DNA polymerase activity expressed in Escherichia coli BL21 assessed as [3H]dTTP incorporation by cell free-based scintillation counting | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID1763900 | Antiviral activity against HIV-1 IIIB harboring RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID82470 | Antiviral activity against V106I strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID105693 | Anti-HIV-1 activity against K1001 strain was determined in MT-4 cells by the MTT method | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
| 3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1784587 | Inhibition of HIV-1 reverse transcriptase using 5'-Cy5CAGGAAACAGCTATGAC/3'-GTCCTTTGTCGATACTGTTTTTTT-5' as primer/template at 0.5 uM preincubated for 20 min followed by dATP addition measured after 5 to 10 mins by gel electrophoresis analysis | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Exploring the dNTP -binding site of HIV-1 reverse transcriptase for inhibitor design. |
AID88370 | Antiviral activity against K103N/Y181C mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1773840 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies. |
AID1331267 | Inhibition of HIV-1 reverse transcriptase assessed as reduction in biotin-labeled dNTP incorporation using streptavidine bound template measured after 1 hr by ELISA | 2017 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1
| Design, synthesis and anti-HIV-1 RT evaluation of 2-(benzyl(4-chlorophenyl)amino)-1-(piperazin-1-yl)ethanone derivatives. |
AID88377 | Antiviral activity against V106A mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1687686 | Cytotoxicity against human MT4 cells assessed as inhibition of cell viability by measuring reduction in absorbance at OD540 by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID586379 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase I151L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1316338 | Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1171411 | Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay | 2014 | ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
| Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers. |
AID1705194 | Inhibition of RNA-dependent DNA polymerase activity of wild type recombinant HIV-1 His-tagged p66/p51 reverse transcriptase assessed as inhibition of [3H]dTTP incorporation using poly(rA)/oligo(dT) as templates incubated for 15 mins by MicroBeta scintilla | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID523483 | Antiviral activity against HIV1 with RT connection domain L100I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID302253 | Antiviral activity against HIV1 with reverse transcriptase K103N mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID1264540 | Antiviral activity against HIV-1 X4 expressing reverse transcriptase K103N mutant infected in human CD4+ T cells for 3 days by FACS analysis | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
| Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance. |
AID1884490 | Antiviral activity against drug-resistant HIV-1 K103 N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID253490 | Dose required to inhibit HIV-1 reverse transcriptase activity (K103N mutant) by 50% | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
| Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation. |
AID246393 | Effective concentration against human immunodeficiency virus type 1 mutated at 103N+181C | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID366517 | Antiviral activity against HIV1 NL4-3 in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID1165079 | Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(rA)-oligo(dT) as template/primer and digoxigenin-/biotin-labeled dUTP nucleotides incubated for 1 hr | 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. |
AID1691436 | Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as reduction in virus-induced cell death incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP. |
AID105543 | Inhibition of wild type HIV-1 in MT-4 cell culture (human T cell line) | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
| Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues. |
AID1888691 | Toxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay | | | |
AID1163255 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O positive erythrocyte assessed as reduction in parasitemia after 72 hrs | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
AID1286670 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor. |
AID1572522 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | | | |
AID1761018 | Antiviral activity against HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID1157599 | Antiviral activity against NRTI-resistant HIV1 MP1315 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID198385 | Inhibitory concentration for 50% inhibition of HIV-1 reverse transcriptase | 2000 | Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
| Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors. |
AID1191668 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenic effect | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
| Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs. |
AID541159 | Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 8 passages to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1335213 | Antiviral activity against HIV-1 NL4-3 harboring RT-Y188L mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID523357 | Antiviral activity against HIV1 with RT connection domain G190A mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID248491 | In vitro inhibitory concentration against HIV F227L and V106A mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID1206935 | Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection from virus-induced cytopathicity after 4 days by MTT assay | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1750717 | Inhibition of HIV-1 p66/p51 reverse transcriptase L100I mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID586376 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Q148H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1729151 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID1761014 | Antiviral activity against HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID1743618 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID279479 | Antiviral activity against HIV1 isolate with RT 179D, 181C mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID419085 | Inhibition of HIV1 replication in human 293T cells preincubated 15 mins prior to infection measured after 48 hrs postinfection by luciferase reporter gene assay | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
| Synthesis and biological evaluation of N4-(hetero)arylsulfonylquinoxalinones as HIV-1 reverse transcriptase inhibitors. |
AID573975 | Antiretroviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID1636930 | Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against viral infection by MTT method | 2016 | Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
| Computer-aided discovery of anti-HIV agents. |
AID1847040 | Inhibition of HIV-1 reverse transcriptase associated RNA-dependent DNA polymerase activity using poly(A)-oligo(dT) as template/primer incubated for 30 mins by multilabel counter plate reader analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
| Quinolinonyl Non-Diketo Acid Derivatives as Inhibitors of HIV-1 Ribonuclease H and Polymerase Functions of Reverse Transcriptase. |
AID490368 | Antiviral activity against HIV1 expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses. |
AID508648 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, T386A mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
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. |
AID1357790 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID614139 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 IIIB infected in human MT4 cells | 2011 | Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17
| Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs. |
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. |
AID1220370 | Blood plasma protein binding in human at 100 mg administered every 4 hrs by ultrafiltration method | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
| Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid. |
AID1574374 | Antiviral activity against HIV-1 IRLL98 harboring reverse transcriptase M41L, D67N, Y181C, M184V, R211K, and T215Y mutants infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID1888697 | Antiviral activity against HIV1 with RT Y188L mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
AID1773830 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 infected in human MT4 cells | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies. |
AID1335201 | Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/V108I double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID541164 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1627029 | Inhibition of HIV1 RT using 17-mer DNA/Alexa Fluor 488 5'-end labeled DNA/Alexa Fluor 555-aha-dUTP as primer/template/substrate preincubated for 10 mins followed substarte addition measured after 30 mins by FRET assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID279446 | Antiviral activity against HIV1 isolate with RT 101Q, 181C mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1126511 | Inhibition of wild-type HIV1 reverse transcriptase p66/p51 after 40 mins by spectrophotometry | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
| Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
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. |
AID1457066 | Inhibition of HIV1 reverse transcriptase p66 K103N/Y1881C double mutant associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintilla | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID198237 | Inhibitory activity against HIV-1 reverse transcriptase | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| Synthesis and biological activities of potential metabolites of the non-nucleoside reverse transcriptase inhibitor efavirenz. |
AID1773835 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies. |
AID541156 | Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 5 passages to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID496620 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase K101E/K30E, I31P, V35Q, T39S, E44G, E53G, A62G, N81H, Q91H,I135V,S162A, K173S, Q174R, D177E, V179I, T200I, Q207N, R211K, F214L mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID247620 | Inhibitory activity against HIV-1 double mutants strain 227L and 106A | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID448401 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with Y188C mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 3: optimisation of physicochemical properties. |
AID1316334 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1456307 | Inhibition of HIV-1 reverse transcriptase 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 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. |
AID1731748 | Inhibition of reverse transcriptase Y183C mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID1888696 | Antiviral activity against HIV1 with RT Y181C mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
AID1357804 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase Y188L mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID1069709 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
| Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID586478 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase G140S/Q148R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1596755 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in MT4 cells | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains. |
AID257165 | Inhibition of Y181I mutant HIV1 reverse transcriptase by [3H]-dTTP poly(rA)/oligo(dT) incorporation | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
| Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity. |
AID591356 | Antiviral activity against wild type HIV1 3B infected in human CEM cells assessed as inhibition of virus-induced cytopathicity after 4 days by microscopic analysis | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide. |
AID247498 | Inhibitory activity against HIV-1 mutant strain 106A | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID518734 | Inhibition of RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by filter-based filtration assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID1653619 | Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mass spec | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID508831 | Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 92BR025 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID279427 | Antiviral activity against HIV1 isolate with RT 103R, 179D, 188L mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase 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. |
AID492278 | Antiviral activity against HIV1 with reverse transcriptase K103N, Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy. |
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | | | |
AID257164 | Inhibition of K103N mutant HIV1 reverse transcriptase by [3H]-dTTP poly(rA)/oligo(dT) incorporation | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
| Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity. |
AID1326644 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by cell titer glo based luciferase reporter gene assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1. |
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. |
AID443705 | Antiviral activity against HIV with reverse transcriptase K101E/G190A double mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID583854 | Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.5 multiplicities of infection after 6 days | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID1220363 | Drug level in human cerebrospinal fluid | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
| Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid. |
AID576031 | AUC (0 to 24 hrs) in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID1185996 | Antiviral activity against HIV1 harboring reverse transcriptase L1001/K103N double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID446410 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with L234I mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
AID1637393 | Antiviral activity against human HIV-1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID519873 | Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID1773439 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | | | |
AID446256 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with Y188C mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
AID508784 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138G mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID616199 | Antiviral activity against vesicular stomatitis virus G-pseudotyped Human immunodeficiency virus 1 NL4-3 infected in human MT2 cells assessed as inhibition of viral replication after 48 hrs by luciferase activity reporter gene assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis of new 2'-deoxy-2'-fluoro-4'-azido nucleoside analogues as potent anti-HIV agents. |
AID1212897 | Drug metabolism in human liver microsomes harboring CYP2B6*1/*6 genotype assessed as CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | | | |
AID298062 | Antiviral activity against HIV2 ROD in human MT4 cells by XTT assay | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability. |
AID573475 | Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5331 by cell based assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1069122 | Antiviral activity against HIV harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
| Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses. |
AID152958 | Antiviral activity of Protein Binding of compound was evaluated for A 018C virus expressed PBMC by P24 | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID1736354 | Antiviral activity against VSVG/wild-type HIV-1 infected in human HEK 293T cells assessed as time during which compound exhibits 50% virologic failure at 1 uM treated at post-viral infection and measured at 48 hrs post-infection by luciferase reporter gen | | | |
AID718372 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach. |
AID88382 | Antiviral activity against Y188C mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1157596 | Antiviral activity against HIV1 W5269 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID271413 | Antiviral activity against wild type HIV1 in HeLa-JC53 cells | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
| Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase. |
AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID279398 | Antiviral activity against HIV1 isolate with RT 103N, 108I mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1741398 | Inhibition of reverse transcriptase F227L and V106A mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID1379962 | Cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs. |
AID82463 | Antiviral activity against K103N/V108I strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1421325 | Inhibition of wild-type HIV1 3B reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase 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. |
AID1141964 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1298247 | Inhibition of HIV1 wild type reverse transcriptase p66/p51 using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
AID1627027 | Cytotoxicity against HIV1 infected human CEM cells assessed as reduction in cell viability after 7 days by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID508792 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101P mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID541166 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring G140S mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID523349 | Antiviral activity against HIV1 with RT connection domain K103N mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID1161107 | Cytotoxicity against human MT4 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors. |
AID1503321 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 96 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Inhibitors of Yellow Fever Virus replication based on 1,3,5-triphenyl-4,5-dihydropyrazole scaffold: Design, synthesis and antiviral evaluation. |
AID541152 | Selectivity ratio of EC50 for antiviral activity against EFV-resistant HIV1 selected after 3 passages to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID431619 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
| Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1811038 | Inhibition of recombinant wild-type HIV1 p66/p51 reverse transcriptase assessed as inhibition of [3H]dGTP incorporation using poly (rA) as templates incubated for 40 mins by spectrofluorometer | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID1168821 | Activity of CYP2B6 (unknown origin) assessed per pmol protein pre-incubated for 5 mins in presence of NADPH by uHPLC-MS/MS based substrate depletion kinetics assay | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Structure-Activity Studies Reveal the Oxazinone Ring Is a Determinant of Cytochrome P450 2B6 Activity Toward Efavirenz. |
AID279473 | Antiviral activity against HIV1 isolate with RT 230L mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1882468 | Antiviral activity against wild type HIV-1 IIIB infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors. |
AID584084 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase Y181C mutant infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID279515 | Antiviral activity against HIV1 isolate with RT V106I, D123G, Y181C, F227L, T369I mutation in Hela-JC-53 cells | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1141969 | Ratio of EC50 for HIV1 harboring reverse transcriptase K103N/Y181C double mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1157593 | Antiviral activity against MC1220-resistant HIV1 harboring RT 100I, 179D, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID1884228 | Antiviral activity against HIV-1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID1206934 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection from virus-induced cytopathicity after 4 days by MTT assay | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1286671 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor. |
AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1572520 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | | | |
AID1773453 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring Y18IC mutant infected in human MT4 cells | | | |
AID246780 | Compound concentration required to reduce the amount of p24 by 90% in wtIIIBinfected C8166 cells | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives. |
AID650541 | Resistance ratio of EC50 for multidrug-resistant HIV 1 IRLL98 harboring reverse transcriptase K101Q/Y181C/G190a mutant to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID143396 | Compound was evaluated for its ability to inhibit the mutant K103N L1001 NNRTI HIV-1 enzyme | 2001 | Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
| Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase. |
AID508653 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID771796 | Cytotoxicity against human MT4 cells after 96 hrs by MTT assay | 2014 | Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 23 | Synthesis and structure evaluation of new complex butylarylpiperazin-1-yl derivatives. |
AID347796 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 181I mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID632796 | Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral infection | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents. |
AID299022 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase | 2007 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
| Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains. |
AID1574378 | Antiviral activity against HIV-1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID1335219 | Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/Y181C double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID371906 | Antiviral activity against HIV1 NL4-3 with K103N/V108I double mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID1141959 | Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
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. |
AID508826 | Antiviral activity against Human immunodeficiency virus 1 subtype B isolate 93BR021 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID198768 | Binding affinity towards L100I mutant HIV-1 reverse transcriptase (as per ref 10 in the article) | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
| Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs. |
AID1168819 | Activity of CYP2B6 (unknown origin) pre-incubated for 5 mins in presence of NADPH by uHPLC-MS/MS based substrate depletion kinetics assay | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Structure-Activity Studies Reveal the Oxazinone Ring Is a Determinant of Cytochrome P450 2B6 Activity Toward Efavirenz. |
AID368561 | Antiviral activity against HIV1 reverse transcriptase Y188L mutant infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID197777 | Compound was evaluated for its ability to inhibit HIV-1 Reverse Transcriptase in an in vitro enzyme assay | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
| 4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors. |
AID1884222 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID88367 | Antiviral activity against K103N/L100I mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID623214 | Antiviral activity against HIV1 3B expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID282738 | Inhibition of HIV1 RT V106A mutant | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity. |
AID347619 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 138K mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID508645 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, G190S mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1561721 | Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide to EC | | | |
AID496632 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, T39L, K122E, D123N, S162A, E169T, K173E, Q174E, D177E,T200A, I202V, Q207E mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID730232 | Antiviral activity Vesicular stomatitis virus pseudotype | 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 |
AID1222793 | Dissociation constant, pKa of the compound | 2013 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
| Which metabolites circulate? |
AID562697 | Antiviral activity against HIV1 NL4-3 infected in human HeLa cells assessed as decrease in single-cycle viral infection after 72 hrs by beta-galactosidase reporter gene assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation. |
AID269685 | Antiviral activity against HIV1 | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269685 | Antiviral activity against HIV1 | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269685 | Antiviral activity against HIV1 | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID416755 | Antiviral activity against HIV1 with reverse transcriptase L100I mutation in human CEM cells assessed as protection against virus-induced cytopathicity | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus. |
AID279491 | Antiviral activity against HIV1 isolate with RT K101E mutant | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1457061 | Ratio of EC50 for HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID519875 | Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID1157586 | Antiviral activity against MDR-resistant HIV1 harboring 41L, 74V, 106A, 215Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID508640 | Antiviral activity against Human immunodeficiency virus 1 subtype BG infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID370732 | Cytotoxicity against human C8166 cells by MTT method | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
AID571979 | Antiviral activity against HIV-1 subtype B V022811 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1373161 | Inhibition of reverse transcriptase E138K mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Structural optimization of N |
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. |
AID293178 | Antiviral activity against HIV1 RT 100I mutant assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method | 2007 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
| Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity. |
AID293175 | Antiviral activity against HIV1 with RT 103N mutant assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method | 2007 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
| Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity. |
AID279410 | Antiviral activity against HIV1 isolate with RT 179E mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1298253 | Inhibition of HIV1 3B reverse transcriptase p66/p51 K103N/Y181C mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
AID586370 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase G140S mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID709868 | Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID94445 | Potency of second-generation NNRTIs against Mutant HIV-1 K103N plasma; Vlaue ranges from 3400-8100 | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID246344 | Effective concentration of the compound to inhibit HIV-1 mutant L100I+K103N replication in HIV-infected MT-4 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID587740 | Selectivity index, ratio of CC50 for human HeLa-T4 cells to EC50 for single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
AID457956 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed inhibition of viral-induced cytopathic effect after 5 days | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
| Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID586901 | Activity at MRP1 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Interaction potential of etravirine with drug transporters assessed in vitro. |
AID441314 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with K101E mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 1: design and initial optimisation of a novel template. |
AID1212884 | Drug metabolism in microsomes expressing CYP2B6.6 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by HPLC/UV system in presence of Cyt b5 coexpression | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID1326643 | Inhibition of wild type HIV-1 3B reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 5 days by cell titer glo based luciferase reporter gene assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1. |
AID1561718 | Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide assessed as protection against virus-indu | | | |
AID1304409 | Antiviral activity against HIV-1 3B expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID1157582 | Antiviral activity against efavirenz-resistant HIV1 harboring RT 100I, 103R, 179D, 225H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID508798 | Ratio of EC50 for HIV1 in presence of 50% human serum to EC50 for HIV1 in absence of serum proteins by GFP assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1060628 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs. |
AID1186328 | Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
| Antiviral activity of benzimidazole derivatives. III. Novel anti-CVB-5, anti-RSV and anti-Sb-1 agents. |
AID366524 | Antiviral activity against HIV1 isolates with reverse transcriptase Y188L mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID368557 | Inhibition of HIV1 recombinant reverse transcriptase Y181I mutant-mediated RNA-dependent DNA polymerase activity assessed as [3H]dTTP incorporation by cell free-based scintillation counting | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID279393 | Antiviral activity against HIV1 isolate with RT 106I mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID522577 | Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106I mutant clone to EC50 for wild type HIV1 | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID263152 | Antiviral activity against HIV1 in HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID263152 | Antiviral activity against HIV1 in HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID263152 | Antiviral activity against HIV1 in HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1157595 | Antiviral activity against TMC125-resistant HIV1 harboring RT 109M, 138K, 190E mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID361912 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase G190A mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID267650 | Antiviral activity against HIV1 K103N/L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID586378 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Q148R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1335209 | Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/V108I double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID1565098 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID508763 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID557022 | Antiviral activity against HIV1 CRF01_AE harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1884226 | Antiviral activity against HIV-1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID1379959 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by measuring virus-induced syncytium formation by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs. |
AID1884539 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 K103 N mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID302256 | Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT K103N mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID650543 | Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID440079 | Antiviral activity against HIV1 HXB2 harboring 138K mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID279498 | Antiviral activity against HIV1 isolate with RT K103N-V108I-A98G mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1212896 | Drug metabolism in human liver microsomes harboring CYP2B6*1/*1 genotype assessed as CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID1574380 | Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV-1 NL4-3 | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID465421 | Binding affinity to human serum albumin | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID666972 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors. |
AID541157 | Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 6 low passages to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1572526 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
AID88381 | Antiviral activity against Y181C mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID328845 | Inhibition of human MRP3 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay | 2007 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
| Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors. |
AID573254 | Apparent oral clearance in HIV-1 infected children at 12 mg/kg, po administered once daily by HPLC | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID279523 | Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID665274 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID279404 | Antiviral activity against HIV1 isolate with RT 103N, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID106069 | Inhibitory activity against 188L strain of HIV-I in MT-4 cells | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. |
AID698306 | Antiviral activity against HIV1 containing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1357803 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase Y181C mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID508650 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID279318 | Inhibition of HIV1 RT assessed as natural endogenous reverse transcription at 50 nM | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification. |
AID457955 | Inhibition of RNA-dependent DNA polymerase activity of HIV1 reverse transcriptase using poly(rA)/pligo(dT) template | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
| Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID613677 | Antiproliferative activity against human A375 cells assessed as cell growth at 15 uM after 96 hrs by trypan blue assay | 2011 | Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16
| Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors. |
AID299025 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 | 2007 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
| Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains. |
AID443676 | Antiviral activity against HIV with reverse transcriptase CNDO mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID718370 | Cytotoxicity against HIV1 3B infected in human MT4 cells by MTT assay | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach. |
AID1773461 | Resistance factor, ratio of EC50 for HIV1 harboring E138K mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells | | | |
AID443702 | Antiviral activity against HIV with reverse transcriptase K103N/G190A double mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID299026 | Antiviral activity against HIV1 3B in CEM cells assessed as inhibition of virus-induced giant cell formation | 2007 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
| Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains. |
AID106049 | Inhibitory activity against 100I strain and 103N strain of HIV-I in MT-4 cells | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. |
AID1609107 | Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1574383 | Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase K103N/Y181C double mutant to EC50 for wild type HIV-1 NL4-3 | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID271415 | Antiviral activity against HIV1 Y188L mutant in HeLa-JC53 cells | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
| Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase. |
AID342719 | Antiviral activity against HIV1 3B in human MT4 cells assessed as virus-induced cytopathogenicity after 5 days | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors. |
AID248016 | Inhibitory concentration against wild-type HIV-1 LAI Virus was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity. |
AID1483279 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID1767121 | Ratio of antiviral activity against HIV1 NL4-3 Env-deficient VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production when host cells were infected with compound pretreated viral particles to antiviral a | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase. |
AID302254 | Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID605181 | Antiviral activity against HIV1 R8 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral spread in presence of 10% fetal bovine serum | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif. |
AID496627 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K32R, V35E, T39S, S48T, V60I, D121Y, K122E, I135T, S162A, K173A, Q174K, D177E, V179I, T200E, Q207D, R211K mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID279411 | Antiviral activity against HIV1 isolate with RT 103N, 108I, 181C mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID519967 | Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells by phenosense assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID269690 | Antiviral activity against HIV1 NNTRI resistant K103N/L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269690 | Antiviral activity against HIV1 NNTRI resistant K103N/L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269690 | Antiviral activity against HIV1 NNTRI resistant K103N/L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1736364 | Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase K103N/Y181C double mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cel | | | |
AID586479 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Y143H/N155H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID449489 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus induced cytotoxicity after 5 days by MTT assay | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
| Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID541169 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring N155H mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1141968 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1574371 | Therapeutic index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 NL4-3 infected in human MT4 cells | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
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. |
AID105325 | Inhibition of Efavirenz resistant HIV-1 (Y181C) induced cytopathicity in MT-4 cells. | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations. |
AID557044 | Inhibition of HIV1 isolate R8 reverse transcriptase K103N mutant after 90 mins by electrochemiluminescence analysis | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID257173 | Cytotoxicity against MT4 cells by MTT method | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
| Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity. |
AID267851 | Inhibition of wild type HIV1 reverse transcriptase | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
AID81591 | Antiviral activity against HIV-1 using antiinfectivity assay | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
| Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors. |
AID1231486 | Antiviral activity against HIV1 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action. |
AID492046 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors. |
AID366559 | Antiviral activity against HIV1 with reverse transcriptase K103N/Y181C mutation in human MT4 cells assessed as reduction of virus-induced cytopathic effect | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID508766 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230V mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID105202 | Antiviral activity against MT-4 cells infected with Nev-R strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1457071 | Effect on CD163 mRNA levels in C57BL/6 mouse BV2 cells at 1000 nM after 24 hrs by RT-PCR assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID1485966 | Inhibition of recombinant wild-type HIV-1 reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli JM109 assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by Pi | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Searching for novel N |
AID1743637 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID586910 | Induction of BCRP activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Interaction potential of etravirine with drug transporters assessed in vitro. |
AID279443 | Antiviral activity against HIV1 isolate with RT 106A, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID368567 | Inhibition of HIV1 recombinant free reverse transcriptase K103N mutant expressed in Escherichia coli BL21 | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | | | |
AID269799 | Antiviral activity against HIV1 L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269799 | Antiviral activity against HIV1 L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269799 | Antiviral activity against HIV1 L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1763904 | Antiviral activity against HIV-1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID1212919 | Drug metabolism in microsomes expressing CYP2B6.6 (unknown origin) assessed as intrinsic clearance for enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in absence of Cyt b5 coexpression | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID83552 | Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr188Leu | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
| Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian |
AID541131 | Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RT-6TAMs mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID313877 | Selectivity index, ratio of EC50 for MT4 cells to EC50 for HIV1 | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase--structure-activity relationships and crystallographic analysis. |
AID82460 | Antiviral activity against K103N/G190A strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID440086 | Antiviral activity against HIV1 HXB2 harboring K103N and Y181C mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID573998 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for CHI/1043-resistant Human immunodeficiency virus harboring T66I and Q146K mutations in integrase | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID583853 | Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.05 multiplicities of infection after 6 days | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID88378 | Antiviral activity against V106A/Y181C mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1304400 | Antiviral activity against HIV-1 RF infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID1171578 | Cytotoxic activity against human MT4 cells by MTT assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID699541 | Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID663905 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 5-acetyl-2-arylbenzimidazoles as antiviral agents. Part 4. |
AID611909 | Antiviral activity against Human immunodeficiency virus 1 NL 4.3 harboring reverse transcriptase Y181C mutant pseudotyped with VSV-G envelope co-transfected with luciferase gene infected in 293T cells assessed as inhibition of HIV1 replication administere | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Lindenane disesquiterpenoids with anti-HIV-1 activity from Chloranthus japonicus. |
AID622049 | Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer Y181C mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID448402 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with K101E mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 3: optimisation of physicochemical properties. |
AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID263512 | Antiviral activity against HIV1 L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2. |
AID269794 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269794 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269794 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID519871 | Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID699540 | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID370727 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 Y181I mutant expressed in Escherichia coli JM109 | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
AID562703 | Antiviral activity against HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation. |
AID1245795 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 96 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
| Isolation and anticancer, anthelminthic, and antiviral (HIV) activity of acylphloroglucinols, and regioselective synthesis of empetrifranzinans from Hypericum roeperianum. |
AID279490 | Antiviral activity against HIV1 isolate with RT Y188L mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1884487 | Cytotoxicity against human MT4 cells assessed as cell growth inhibition incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID476473 | Cytotoxicity against human MT2 cells infected with HIV1 harboring reverse transcriptase K103N/Y181C mutation by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
| Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives. |
AID1637399 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring L100I mutant infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID279507 | Antiviral activity against HIV1 isolate with RT D123G mutation in Hela-JC-53 cells | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID767497 | Cytotoxicity against human MT2 cells assessed as growth inhibition | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
| Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility. |
AID572173 | Antiviral activity against HIV-1 subtype CRF05_DF V022824 harboring NNRTI V106I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID248846 | Inhibitory concentration against human immunodeficiency virus type 1 (with Y188C resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2. |
AID366518 | Cytotoxicity against human MT4 cells by MTT assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID1731749 | Inhibition of reverse transcriptase Y188L mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID371901 | Antiviral activity against HIV1 NL4-3 with Y181C mutant in human MT4 cells assessed as inhibition of virus-induced cytopathicity after 5 days by multiple round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID457957 | Cytotoxicity in human MT4 cells assessed as reduction in cell viability | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
| Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1574386 | Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 Y181I mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID1637389 | Antiviral activity against human HIV-1 3B harboring RES056 mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID386498 | Antiviral activity against HIV1 with reverse transcriptase K103N/Y181C mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Parallel synthesis, molecular modelling and structure-activity relationship studies on analogues of O-(2-phenylethyl)-N-phenylthiocarbamate. |
AID302263 | Inhibition of HIV1 reverse transcriptase V179D mutant | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID279527 | Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells in the presence of 30% human serum after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1811034 | Anti-viral activity against HIV1 harboring RT E138K mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID1565097 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID279448 | Antiviral activity against HIV1 isolate with RT 101H, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1637395 | Antiviral activity against human HIV-1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID508636 | Antiviral activity against Human immunodeficiency virus 1 subtype G infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID508629 | Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR029 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID443695 | Antiviral activity against HIV with reverse transcriptase K103N mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID698144 | Inhibition of HIV1 reverse transcriptase L100I mutant RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID441316 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with V108I mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 1: design and initial optimisation of a novel template. |
AID1763898 | Antiviral activity against HIV-1 IIIB harboring RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID443678 | Antiviral activity against HIV with reverse transcriptase K103N mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID508647 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, E138G mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID519884 | Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID621981 | Resistance index, ratio of EC50 for HIV1 3B expressing reverse transcriptase K103N/Y181C double mutant to EC50 for wild-type HIV1 3B | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID508773 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181V mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID492045 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors. |
AID267651 | Selectivity for wild type HIV1 virus over HIV1 K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID302250 | Selectivity index, ratio of CC50 for MT4 cells to EC50 for HIV1 NL43 infected MT4 cells | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID293556 | Cytotoxicity against human MT4 cells after 3 days by EGFP based replication assay | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5
| Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains. |
AID1636146 | Antiviral activity against wild type HIV1 NL4-3 | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors. |
AID255644 | Effective concentration required to inhibit HTLV-III B induced cytopathicity in human CEM cells | 2005 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
| Synthesis and evaluation of anti-HIV activity of isatin beta-thiosemicarbazone derivatives. |
AID253494 | Dose required to inhibit HIV-1 reverse transcriptase activity (Y188L mutant) by 50% | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
| Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation. |
AID347089 | Metabolic stability in human liver microsomes assessed as half life | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays. |
AID571982 | Antiviral activity against HIV-1 subtype B V022814 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID427975 | Antiviral activity against HIV1 infected in human HeLa cells expressing CD4-LTR assessed as inhibition of viral entry-related beta galactosidase expression treated for 2 hrs measured after 48 hrs by MAGI assay | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
| Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2. |
AID1171579 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1348212 | Antiviral activity against wild-type VSV-G pseudotyped HIV1 infected in HEK293 cells at 10 uM pretreated for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene assay relative to control | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12
| Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities. |
AID82457 | Antiviral activity against G190A strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1348214 | Antiviral activity against VSV-G pseudotyped HIV1 infected in human MT2 cells pretreated for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene assay | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12
| Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities. |
AID1435511 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase | | | |
AID279493 | Antiviral activity against HIV1 isolate V106I-Y188L mutant | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID330489 | Antiviral activity against HIV1 RES056 infected in MT4 cells by MTT | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID302257 | Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT Y181C mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID621980 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing reverse transcriptase K103N/Y181C double mutant | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID141362 | Ratio of Inhibitory activity against mutant K103N HIV-1 Reverse transcriptase to mutant L1001 HIV-1 Reverse transcriptase | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
| Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors. |
AID685335 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B | 2012 | Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors. |
AID1815393 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase E138K mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1249723 | Antiviral activity against HIV1 expressing reverse transcriptase F227L + V106A mutant | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID143398 | Compound was evaluated for its ability to inhibit the mutant K103N NNRTI HIV-1 enzyme | 2001 | Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
| Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase. |
AID1552555 | Antiviral activity against HIV1 YU2 pseudovirus infected in human TZM-bl cells assessed as inhibition of viral infection incubated for 20 mins prior to infection and measured after 48 hrs post infection by bright Glo-luciferase reporter gene assay | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
| Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline. |
AID1552557 | Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
| Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline. |
AID1736359 | Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase Y188L mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hrs post-infect | | | |
AID473115 | Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
| Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV. |
AID573481 | Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 8117 harboring A98S, G190A mutation in reverse transcriptase to wild-type | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1261813 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 4 days by MTT assay | 2015 | European journal of medicinal chemistry, Nov-13, Volume: 105 | Synthesis, cytotoxicity and antiviral evaluation of new series of imidazo[4,5-g]quinoline and pyrido[2,3-g]quinoxalinone derivatives. |
AID523346 | Antiviral activity against HIV1 with RT connection domain T369V mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID665273 | Antiviral activity against HIV2 ROD mutant infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase 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. |
AID632799 | Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of viral infection | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents. |
AID541154 | Selectivity ratio of EC50 for antiviral activity against APV-resistant HIV1 selected after 2 passages to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID586481 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase N155H/G163K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1761020 | Antiviral activity against HIV-1 harboring reverse transcriptase RES056 mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID665275 | Selectivity index ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID1773451 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring L1001 mutant infected in human MT4 cells | | | |
AID366550 | Inhibition of HIV1 reverse transcriptase Y181C mutant by scintillation counting assay | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1171415 | Aqueous solubility of the compound at pH 6.5 after 48 hrs by shake-flask method | 2014 | ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
| Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers. |
AID430054 | Inhibition of HIV1 recombinant RNA-dependent DNA polymerase activity of reverse transcriptase assessed as incorporation of radioactive dTTP into poly(rA)/oligo(dT) | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
| Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents. |
AID279451 | Antiviral activity against HIV1 isolate with RT 101E, 108I, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID508641 | Antiviral activity against Human immunodeficiency virus 1 subtype AG infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID492287 | Antiviral activity against HIV1 with reverse transcriptase F227L, V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy. |
AID197932 | HIV-1 reverse transcriptase inhibitory activity against Cys181 mutant using (poly)rC600*(oligo)dGT as template primer. | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
| Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues. |
AID605176 | Inhibition of wild type HIV1 reverse transcriptase by SPA assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif. |
AID573997 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for MK-0518-resistant Human immunodeficiency virus harboring G140S and Q148H mutations in integrase | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID246265 | Effective concentration against human immunodeficiency virus type 1 G190S mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). |
AID440670 | Antiviral activity against NNRTI-resistant HIV1 N119 with reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
| Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants. |
AID496633 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, E36D, K43R, V60I, K101R, K122E, D123S, I135V, S162A, K173T, Q174K, D177E, V179I, G196E, T200A, Q207E mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID88368 | Antiviral activity against K103N/P225H mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID246359 | Protection of infected MT-4 cells from wtIIIB-HIV-1-induced cytopathogenicity | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives. |
AID226171 | Compound was evaluated for the inhibition of wilde-type RF strain of HIV-1 | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID1141975 | Inhibition of HIV1 wild-type reverse transcriptase using [3H]dTTP by scintillation counting | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1155813 | Inhibition of wild type HIV-1 recombinant reverse transcriptase assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:1 | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID718369 | Selectivity index, ratio of CC50 for HIV1 3B infected in human MT4 cells to EC50 for HIV1 3B | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach. |
AID1750725 | Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase Y181C mutant | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID508635 | Antiviral activity against Human immunodeficiency virus 1 subtype (H) infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1352322 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID523484 | Antiviral activity against HIV1 with RT connection domain L100I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID1750715 | Cytotoxicity against in human MT-4 cells after 5 days by MTT assay | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID279431 | Antiviral activity against HIV1 isolate with RT 103S, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1773455 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring E138K mutant infected in human MT4 cells | | | |
AID666973 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors. |
AID1815380 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID368562 | Cytotoxicity against human MT4 cells by MTT assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID1320867 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
AID1483280 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase L100I mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID1743629 | Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID675389 | Cytotoxicity against human MT4 cells after 96 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Disubstituted thiourea derivatives and their activity on CNS: synthesis and biological evaluation. |
AID1391085 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID766430 | Aqueous solubility of the compound at pH 6.5 by shake-flask method | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
| Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility. |
AID279482 | Antiviral activity against HIV1 isolate with RT K103N mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID508796 | Ratio of EC50 for HIV1 in presence of 1 mg/ml alpha-1 acid-glycoprotein to EC50 for HIV1 in absence of serum proteins by GFP assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1435517 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase F227L/V106A double mutant | | | |
AID82467 | Antiviral activity against P236L strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID490372 | Antiviral activity against HIV1 expressing reverse transcriptase V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses. |
AID496616 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, T39M, K46Q, V60I, S68G, D123E, I135V, S162A, K173A, Q174K,D177E, T200A, Q207E, R211K mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID252950 | Selectivity index of cytotoxic activity (CC50) to inhibitory activity (IC50) relative to LAI cell line | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID1565099 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID1693799 | Antiviral activity against HIV-3B infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C. |
AID1485967 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Searching for novel N |
AID465422 | Half life in Beagle dog at 0.5 mg/kg, iv or. 5 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID757624 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID267647 | Antiviral activity against HIV1 K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID1335204 | Ratio of IC50 for HIV-1 NL4-3 harboring RT-Y188L mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID1152370 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
| Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1285844 | Antiviral activity against HIV1 A17 infected in human C8166 cells assessed as reduction in p24 antigen level incubated for 4 hrs followed by cell plating for 72 hrs by ELISA method | 2016 | Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
| Design, synthesis and anti-HIV-1 evaluation of hydrazide-based peptidomimetics as selective gelatinase inhibitors. |
AID1736345 | Cytotoxicity against human HEK 293T cells assessed as reduction in cell viability measured after 48 hrs by Celltiter-glo assay | | | |
AID1443670 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID557041 | Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1687691 | Inhibition of HIV-1BH10 reverse transcriptase expressed in Escherichia coli assessed as polymerization by real time FRET assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Rational design and Structure-Activity relationship of coumarin derivatives effective on HIV-1 protease and partially on HIV-1 reverse transcriptase. |
AID279391 | Antiviral activity against HIV1 isolate with RT 181C mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1248226 | Antiviral activity against wild type HIV 2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
| A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities. |
AID1220383 | Antiviral activity against HIV1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
| Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid. |
AID1483273 | Inhibition of HIV1 3B reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID279522 | Antiviral activity against wild type HIV1 NL4-3 in Hela-JC53 cells in the presence of 50% human serum after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID541162 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring L74M mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID263508 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2. |
AID541133 | Selectivity ratio of EC50 for antiviral activity against NNRTI-resistant HIV1 harboring RTY181C mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID571977 | Antiviral activity against HIV-1 subtype B V022809 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID508639 | Antiviral activity against Human immunodeficiency virus 1 subtype C infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1729163 | Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into template incubated for 1 hr by ELISA | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID1763897 | Antiviral activity against HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID279324 | Inhibition of reverse transcriptase activity in HIV1 NL4-3 infected MT4 cells after dialysis | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification. |
AID519861 | Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID586483 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase N155H/D232N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1352314 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID1565088 | Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into template incubated for 1 hr by ELISA | | | |
AID779524 | Inhibition of recombinant wild type HIV-1 reverse transcriptase p66/p51 expressed in Escherichia coli JM109 using poly(rA)/oligo(dT)16 (1:1.2) as template/primer after 40 mins by spectrofluorometric analysis | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
AID1298252 | Inhibition of HIV1 reverse transcriptase p66/p51 G190A mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
AID584083 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase K103N mutant infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4
| DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
AID1705186 | Antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID1743620 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID1261315 | Antiviral activity against human CVB5 infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity after 3 days by plaque reduction assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
AID106609 | Cytotoxic concentration that reduces the MT-4 cell viability by 50% | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
| 5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series. |
AID366529 | Inhibition of RNA dependent DNA polymerase activity of HIV1 reverse transcriptase Y181I mutant | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID519859 | Antiviral activity against HIV1 subtype B-RF infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID572169 | Antiviral activity against HIV-1 subtype D V022832 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID508624 | Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 92TH006 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1743631 | Antiviral activity against HIV1 harboring RT F227L/V106Amutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID1741397 | Inhibition of reverse transcriptase E138K mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID416757 | Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in human CEM cells assessed as protection against virus-induced cytopathicity | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus. |
AID248069 | Inhibitory concentration against 103N and 181C mutant strains was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity. |
AID508656 | Antiviral activity against Human immunodeficiency virus 1 subtype O misolate BCF01 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID523477 | Antiviral activity against HIV1 with RT connection domain G190A/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID586373 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Y143R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | | | |
AID571986 | Antiviral activity against HIV-1 subtype C V022829 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1212914 | Drug metabolism in microsomes expressing CYP2B6.1 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by HPLC/UV system in absence of Cyt b5 coexpression | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
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. |
AID1435508 | Antiviral activity against HIV1 expressing reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | | | |
AID508764 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K101E mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID82606 | The effect of protein binding on the antiviral activity versus wild type virus strain K103N was tested in the presence of acid glycoprotein in HeLa MAGI assay | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID562704 | Selectivity ratio of EC50 for HIV1 harboring capsid I201V mutant protein infected in human HeLa cells to EC50 for wild type HIV1 infected in human HeLa cells | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation. |
AID1637402 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring Y188L mutant infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID508634 | Antiviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1773443 | Selectivity ratio of CC50 for human MT4 cells to IC50 for HIV-1 3B infected in MT4 cells | | | |
AID620437 | Inhibition of wild type HIV1 reverse transcriptase | 2011 | Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
| Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs). |
AID1653618 | Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mass spectrometry | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID583863 | Inhibition of HIV1 HXB2 reverse transcriptase K103N mutant activity by primer extension assay | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID726438 | Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
| Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency. |
AID279435 | Antiviral activity against HIV1 isolate with RT 101Q, 103R mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID573480 | Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 8116 harboring A98S, G190A mutation in reverse transcriptase to wild-type | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1220380 | Drug metabolism of the compound assessed as CYP2B6 (unknown origin)-mediated formation of metabolites with retention time of 1.92 mins at 5 uM by UPLC-MS/MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
| Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid. |
AID573472 | Antiviral activity of wild-type Human immunodeficiency virus 1 infected in human TZM-bl cells human assessed as inhibition of viral replication by luciferase reporter gene assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID276232 | Cytotoxicity against MT2 cells | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
| Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
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. |
AID1743638 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT E138K mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID1822283 | Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID509268 | Inhibition of HIV1 RT by ELISA | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Antiviral efficacy of the novel compound BIT225 against HIV-1 release from human macrophages. |
AID492044 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors. |
AID253492 | Dose required to inhibit HIV-1 reverse transcriptase activity (V179D mutant) by 50% | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
| Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation. |
AID698146 | Inhibition of wild type HIV1 reverse transcriptase RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID476472 | Antiviral activity against HIV1 reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as inhibition of viral replication by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
| Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives. |
AID1320866 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1754637 | Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured after 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
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. |
AID1261308 | Cytotoxicity against human MT4 cells assessed as cell viability after 96 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
AID370730 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 Y188L mutant expressed in Escherichia coli JM109 | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
AID572178 | Antiviral activity against HIV-1 subtype H V029523 harboring NNRTI K101Q and V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1761015 | Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID1884493 | Antiviral activity against drug-resistant HIV-1 E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID1754647 | Antiviral activity against HIV1 harboring RT RES056 mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
AID573996 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for L-870,810-resistant Human immunodeficiency virus harboring L74M, E92Q and S230N mutations in integrase | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID1141973 | Ratio of EC50 for HIV1 harboring reverse transcriptase L1001 mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID247504 | Inhibitory activity against HIV-1 mutant strain 190S | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID82462 | Antiviral activity against K103N/P225H strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID508630 | Antiviral activity against Human immunodeficiency virus 1 subtype G isolate G3 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1822282 | Antiviral activity against HIV-1 harboring RES056 mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID430055 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
| Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents. |
AID443433 | Cytotoxicity against human MT4 cells assessed as reduction of cell viability after 96 hrs by MTT assay | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
| Synthesis, pharmacological and antiviral activity of 1,3-thiazepine derivatives. |
AID573976 | Antiretroviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID328842 | Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence by CMFDA assay | 2007 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
| Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors. |
AID572189 | Antiviral activity against HIV-1 SM058 harboring NNTRI 227L and 106A mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1320865 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
AID650696 | Ratio of ID50 for HIV 1 reverse transcriptase K103N mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID371911 | Antiviral activity against HIV1 NL4-3 with Y181C mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID443683 | Antiviral activity against HIV with reverse transcriptase L100I/K103N double mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID508637 | Antiviral activity against Human immunodeficiency virus 1 subtype D infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1348217 | Antiviral activity against wild-type VSV-G pseudotyped HIV1 infected in HEK293 cells assessed as time of 50% failure at 1 uM measured at 48 hrs post infection by luciferase reporter gene assay | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12
| Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities. |
AID571983 | Antiviral activity against HIV-1 subtype B V022815 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID464771 | Volume of distribution at steady state in Beagle dog at 0.5 mg/kg, iv or 0.5 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID622050 | Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer Y188L mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID519023 | Antiviral activity against Human immunodeficiency virus 1 NL432 infected in human MT-4 cells assessed as increase in viral two-LTR circles | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
| The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral. |
AID279477 | Antiviral activity against HIV1 isolate with RT 181V mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID576032 | AUC (0 to infinity) in healthy human plasma at 400 mg, measured on day 1 post dose by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID1811045 | Cytotoxicity against mock infected human MT4 cells by MTT assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID1185992 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID571967 | Antiviral activity against HIV-1 subtype CRF02_AG V022808 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1653637 | Binding affinity to substrate bound recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli assessed as Kon rate of cholesterol by stopped-flow spectrophotometric method | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID1171587 | Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase K103N-Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID366530 | Resistance index, ratio of ID50 for reverse transcriptase Y181I mutant to IC50 for wild-type HIV1 reverse transcriptase | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID279458 | Antiviral activity against HIV1 isolate with RT 103Q mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID347612 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 225H mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID573474 | Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5269 by cell based assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | | | |
AID508623 | Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG035 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1316332 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID279481 | Antiviral activity against HIV1 isolate with RT 101E mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1335214 | Antiviral activity against HIV-1 NL4-3 harboring RT-L100I/K103N double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID368559 | Antiviral activity against HIV1 reverse transcriptase K103N mutant infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID440087 | Antiviral activity against HIV1 HXB2 harboring 227L and 106A mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID440072 | Selectivity index, ratio of CC50 for human MT4 cells to IC50 for HIV-1 LAI harboring wild type reverse transcriptase infected in human MT4 cells | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID1880369 | Inhibition of HIV-1 reverse transcriptase using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorometric analysis | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Structure-Based Discovery of Novel NH |
AID1773447 | Antiviral activity against wild type HIV1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | | | |
AID94449 | Inhibitory concentration against wild-type virus K103N/L1001 and HIV-1 RT double mutant in whole cell antiviral assay | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
| 3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors. |
AID586474 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E138K/Q148R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID96295 | Potency of second-generation NNRTIs against Mutant HIV-1 sL100I plasma; Value ranges from 6600-15700 | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID1637390 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction of cell viability after 5 days by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID248354 | Concentration required to inhibit 50% viral production of human immunodeficiency virus type 1 (HIV-1-IIIB) | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
| Hierarchical database screenings for HIV-1 reverse transcriptase using a pharmacophore model, rigid docking, solvation docking, and MM-PB/SA. |
AID1653622 | Binding affinity to recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli in absence of substrate by UV-spectrophotometric method | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID267653 | Selectivity for wild type HIV1 virus over HIV1 L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID1261313 | Antiviral activity against YFV infected in BHK-21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
AID347618 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 236L mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID573477 | Antiviral activity of Human immunodeficiency virus 1 isolate 8116 harboring A98S, G190A mutation in reverse transcriptase by cell based assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID443703 | Antiviral activity against HIV with reverse transcriptase Y181C/G190A double mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID1443667 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID1773442 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay | | | |
AID328846 | Inhibition of human MRP1 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay | 2007 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
| Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors. |
AID368565 | Inhibition of wild type HIV1 reverse transcriptase-DNA binary complex | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID83554 | Potency evaluated against wild type HIV-1 strain IIIB | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
| Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian |
AID94314 | Antiviral activity against HIV-1 K103N mutant virus. | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID508628 | Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR020 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID440077 | Antiviral activity against HIV1 HXB2 harboring 101E mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID519868 | Antiviral activity against HIV1 subtype B-92US076 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID571972 | Antiviral activity against HIV-1 subtype CRF01_AE V022821 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID541126 | Cytotoxicity against human SupT1 cells infected with HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1198751 | Inhibition of HIV1 reverse transcriptase Tyr181Cys mutant-associated DNA polymerase-independent RNase H activity after 1 hr | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase. |
AID557043 | Inhibition of HIV1 isolate R8 reverse transcriptase Y181C mutant after 90 mins by electrochemiluminescence analysis | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID267854 | Antiviral activity against wild type HIV1 NL4-3 in MT4 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
AID709870 | Antiviral activity against HIV1 expressing wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID366549 | Inhibition of HIV1 reverse transcriptase K103N mutant by scintillation counting assay | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1220367 | Drug metabolism in human blood plasma assessed as formation of N- and O-linked glucuronidated metabolite at 100 mg administered every 4 hrs by UPLC-MS/MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
| Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid. |
AID302255 | Antiviral activity against HIV1 with reverse transcriptase Y188L mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID82603 | The effect of protein binding on the antiviral activity versus wild type virus strain HXB2 was tested in the presence of acid glycoprotein in HeLa MAGI assay | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID443686 | Antiviral activity against HIV with reverse transcriptase Y181C/G190A double mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID279437 | Antiviral activity against HIV1 isolate with RT 103N, 108I, 225H mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside 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. |
AID1535529 | Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(A)/oligo(dT)15 as template/primer after 1 hr by ELISA | 2019 | Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
| Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs. |
AID298089 | Inhibition of HIV1 RT Y181I mutant | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. |
AID279454 | Antiviral activity against HIV1 isolate with RT 100I, 103N, 108I mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID105535 | Inhibitory activity against HIV-1 Asn 103 mutant in MT-4 cells. | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
| Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues. |
AID586386 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T66I/L74M mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficienc | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1373163 | Inhibition of reverse transcriptase K103N/Y181C double mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Structural optimization of N |
AID298059 | Inhibition of HIV1 reverse transcriptase | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability. |
AID1275552 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID1729157 | Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID465420 | Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT2 cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID279471 | Antiviral activity against HIV1 isolate with RT 103N, 238N mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID571981 | Antiviral activity against HIV-1 subtype B V022813 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID576038 | Ratio of drug concentration in PBMCs to plasma of healthy human administered at 400 mg, po measured after 24 hrs on day 1 post dose | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID299029 | Antiviral activity against HIV1 with reverse transcriptase E138K mutation in CEM cells assessed as inhibition of virus-induced giant cell formation | 2007 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
| Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains. |
AID649488 | Inhibition of ribonuclease H activity of wild type Human immunodeficiency virus 1 reverse transcriptase | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach. |
AID508777 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1572518 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
AID299030 | Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in CEM cells assessed as inhibition of virus-induced giant cell formation | 2007 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
| Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains. |
AID200153 | Inhibition of HIV-1 reverse transcriptase. | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
| Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors. |
AID247618 | Inhibitory activity against HIV-1 double mutants strain 101E and 103N | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID441313 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with Y188C mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 1: design and initial optimisation of a novel template. |
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. |
AID1535527 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 RES056 containing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells | 2019 | Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
| Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs. |
AID1298245 | Cytotoxicity against human MT4 cells after 5 days MTT assay | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
AID279470 | Antiviral activity against HIV1 isolate with RT 238T mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID256325 | Percentage inhibition of proliferation against alive human A-375 cells treated with DMSO (control) at a concentration of 15 uM | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| 6-[1-(2,6-difluorophenyl)ethyl]pyrimidinones antagonize cell proliferation and induce cell differentiation by inhibiting (a nontelomeric) endogenous reverse transcriptase. |
AID1245796 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
| Isolation and anticancer, anthelminthic, and antiviral (HIV) activity of acylphloroglucinols, and regioselective synthesis of empetrifranzinans from Hypericum roeperianum. |
AID709867 | Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID440076 | Antiviral activity against HIV1 HXB2 harboring 100I mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID83550 | Potency evaluated against NNRTI-Resistant HIV-1 strain Lys103Asn | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
| Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian |
AID699539 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID1069123 | Antiviral activity against HIV harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
| Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses. |
AID1357805 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase F227L/V106A mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID573473 | Antiviral activity of wild-type Human immunodeficiency virus 1 harboring Y181C mutation in reverse transcriptase infected in human TZM-bl cells human assessed as inhibition of viral replication by luciferase reporter gene assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1880379 | Antiviral activity against HIV-1 IIIB harboring reverse transcriptase Y188L mutant infected in human MT4 cells by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Structure-Based Discovery of Novel NH |
AID1185993 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay relative HIV1 | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID1558848 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID1357784 | Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID508649 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, V179L mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1815384 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1687682 | Antiviral activity against HIV-1 Y181C mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID242820 | Dose required to inhibit HIV-1 reverse transcriptase activity (wild-type) by 50% | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
| Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation. |
AID256475 | Ratio of CC50 required to reduce the viability of mock-infected human CEM cells to EC50 required to inhibit HTLV-III B induced cytopathicity in that cells | 2005 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
| Synthesis and evaluation of anti-HIV activity of isatin beta-thiosemicarbazone derivatives. |
AID573977 | Antiretroviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID508762 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101E, K103N mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID517493 | Antiviral activity against wild type HIV1 infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 40% human serum | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses. |
AID1407645 | Cytotoxicity against human CEM-GFP cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors. |
AID1320869 | Inhibition of recombinant wild type HIV1 p66/p51 using poly(rA) template/oligo(dT)16 primer after 40 mins by PicoGreen-based spectrofluorometric method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
AID1729161 | Antiviral activity against HIV1 harboring F227L/V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID246799 | Compound concentration required to reduce the amount of p24 by 90% in C8166 cells infected with an efavirenz-resistant strain EFVR carrying mutations K103R, V179D, and P225H | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives. |
AID279450 | Antiviral activity against HIV1 isolate with RT 98G, 103N, 181C mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID586475 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase G140C/Q148R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID82465 | Antiviral activity against L100I strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID658564 | Antiviral activity against multidrug-resistant HIV1 695-RT infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay | 2012 | Journal of natural products, Mar-23, Volume: 75, Issue:3
| Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium. |
AID1198752 | Inhibition of HIV1 reverse transcriptase Tyr181Cys mutant-associated RNA-dependent DNA polymerase activity after 30 mins | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase. |
AID198911 | Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution K103N | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. |
AID279474 | Antiviral activity against HIV1 isolate with RT 101R, 103N, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID586473 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E138K/Q148K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | | | |
AID448399 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with F227L mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 3: optimisation of physicochemical properties. |
AID298078 | Antiviral activity against wild type HIV1 3B in lymphocytes assessed as reduction of p24 antigen production | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. |
AID198106 | Inhibitory activity against R172A mutant reverse transcriptase | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase. |
AID508770 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase G190S mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1249714 | Antiviral activity against HIV1 3B expressing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by MTT method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID1653634 | Binding affinity to recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli at 50 uM in presence of substrate by UV-spectrophotometric method | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID1687684 | Antiviral activity against HIV-1 RES056 mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID508787 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V106M mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID293560 | Antiviral activity against HIV1 LAI with RT K103N mutation in MT4 cells by EGFP based replication assay | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5
| Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains. |
AID1750724 | Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase K103N mutant | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID1815392 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID279399 | Antiviral activity against HIV1 isolate with RT 179D mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1057039 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
| Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs. |
AID361910 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase Y188L mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID726436 | Cytotoxicity in human MT2 cells assessed as inhibition of cell growth | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
| Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency. |
AID1212898 | Drug metabolism in human liver microsomes harboring CYP2B6*6/*6 genotype assessed as CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID767495 | Aqueous solubility of the compound in Britton-Robinson buffer at pH 6.5 after 48 hrs by shake-flask method | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
| Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility. |
AID1157587 | Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID361914 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase G190E mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID82456 | Antiviral activity against E138K strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1407641 | Inhibition of recombinant HIV-1 reverse transcriptase RNA-dependent DNA polymerase activity at 1 ug/ml using poly(rA)/oligo(dT)16 as template/primer preincubated for 5 to 10 mins followed by template/primer addition and measured after 16 hrs by colorimetr | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors. |
AID427973 | Antiviral activity against HIV1 infected in human HeLa cells expressing CD4-LTR assessed as inhibition of viral entry-related beta galactosidase expression at 0.2 to 0.4 uM followed by drug wash out and viral infection measured after 48 hrs by MAGI assay | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
| Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2. |
AID517492 | Antiviral activity against wild type HIV1 infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses. |
AID1637404 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring F227L/V106A double mutant infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID241471 | Inhibitory concentration against HIV-1 mutant reverse transcriptase (K103R) | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
| Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives. |
AID247497 | Inhibitory activity against HIV-1 mutant strain 103N | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID143402 | Compound was evaluated for its ability to inhibit the mutant K103N V1081NNRTI HIV-1 enzyme | 2001 | Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
| Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase. |
AID1888693 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT L100I mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
AID1183081 | Antiviral activity against HIV-13B infected in MT4 cells assessed as protection from virus-induced cytopathogenicity after 4 days by MTT method | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis and antiviral activity of new phenylimidazopyridines and N-benzylidenequinolinamines derived by molecular simplification of phenylimidazo[4,5-g]quinolines. |
AID1736365 | Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase L100I/K103N double mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cel | | | |
AID1741396 | Inhibition of reverse transcriptase Y188L mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID1261324 | Antiviral activity against HIV-1 infected in MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
AID1457063 | Inhibition of HIV1 NL4-3 reverse transcriptase His-tagged p66/p51 associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintillation c | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID269800 | Antiviral activity against HIV1 V106A mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269800 | Antiviral activity against HIV1 V106A mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269800 | Antiviral activity against HIV1 V106A mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID88369 | Antiviral activity against K103N/V108I mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID293557 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 LAI | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5
| Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains. |
AID404605 | Inhibition of HIV1 virion-associated reverse transcriptase | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
| Parallel one-pot synthesis and structure-activity relationship study of symmetric formimidoester disulfides as a novel class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID247619 | Inhibitory activity against HIV-1 double mutants strain 103N and 181C | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID519881 | Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID557038 | Antiviral activity against HIV1 isolate R8 harboring wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID279424 | Antiviral activity against HIV1 isolate with RT 103N, 106A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID371914 | Antiviral activity against HIV1 NL4-3 with double K103N/L100I mutant in human MT4 cells assessed as inhibition of virus-induced cytopathicity after 5 days by multiple round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID1736363 | Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase Y181C mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cells | | | |
AID1248223 | Cytotoxicity against uninfected human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
| A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities. |
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. |
AID1457062 | Ratio of EC50 for HIV-1 harboring reverse transcriptase K103N/Y1881C double mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID1636147 | Antiviral activity against NNRTI resistant HIV1 harboring reverse transcriptase V106I/Y181C/G190A/H221Y mutant assessed as inhibition of viral infection in human TZM-bl cells after 48 hrs by luciferase reporter gene assay | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors. |
AID576028 | Volume of distribution in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID279423 | Antiviral activity against HIV1 isolate with RT 106I, 188L mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1773452 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring K103N mutant infected in human MT4 cells | | | |
AID302259 | Inhibition of wild type HIV1 3B reverse transcriptase | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID313193 | Antiviral activity against HIV1 Y181C mutant | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Synthesis and antiviral activity of new dimeric inhibitors against HIV-1. |
AID1815382 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1171586 | Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID658571 | Antiviral activity against wild type Human immunodeficiency virus 1 NL4-3 pseudotyped with VSV envelope infected in human HeLa-SxR5 cells assessed as inhibition of viral replication at 65 nM after 3 days by beta-galactosidase assay | 2012 | Journal of natural products, Mar-23, Volume: 75, Issue:3
| Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium. |
AID473117 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
| Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV. |
AID519858 | Antiviral activity against HIV1 subtype B-HXB2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID1741392 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID576039 | Ratio of drug concentration in PBMCs to plasma of healthy human administered at 400 mg, po measured after 5 hrs on day 1 post dose | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID1320864 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
AID1304405 | Selectivity index, ratio of CC50 for cytotoxicity against mock-infected human MT4 cells to EC50 for antiviral activity against HIV-1 3B | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID1391077 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID361906 | Antiviral activity against wild type HIV1 in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID370731 | Antiviral activity against HIV1 3B infected human C8166 cells assessed as inhibition of syncytia formation by p24 antigen based assay | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
AID1763902 | Antiviral activity against HIV-1 IIIB harboring RT E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
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. |
AID1457060 | Ratio of EC50 for HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID1815381 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1357797 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID663308 | Inhibition of HIV1 recombinant reverse transcriptase Y181I mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT) | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID1880372 | Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Structure-Based Discovery of Novel NH |
AID82605 | The effect of protein binding on the antiviral activity versus wild type virus strain HXB2 was tested in the presence of human serum in HeLa MAGI assay | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1231487 | Inhibition of wild-type HIV1 Reverse transcriptase p66/p51 assessed as relative fluorescence signal after 40 mins | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action. |
AID1457073 | Cytotoxicity against C57BL/6 mouse BV2 cells assessed as effect on cell proliferation rate at 10 to 10000 nM up to 48 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID557049 | Antiviral activity against HIV1 clade G harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1457055 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID1056584 | Antiviral activity against wild-type HIV-1 infected in HEK293T cells co-transfected with VSVG protein assessed as time required for 50% failure of viral replication at 10 uM by luciferase reporter gene assay | 2013 | Journal of natural products, Dec-27, Volume: 76, Issue:12
| Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73. |
AID718368 | Cytotoxicity against HIV2 ROD infected in human MT4 cells by MTT assay | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach. |
AID279440 | Antiviral activity against HIV1 isolate with RT 101R, 103N mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID735081 | Antiviral activity against HIV harboring reverse transcriptase Y181C mutant by cell based assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
| Synthesis and biological evaluation of phosphonate analogues of nevirapine. |
AID573245 | Cmin in HIV-1 infected children at 13.9 mg/kg, po administered once daily by HPLC | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID1750722 | Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID541174 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V, G140S and V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1261309 | Cytotoxicity against MDBK cells assessed as cell viability after 48 to 96 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
AID1565095 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID541134 | Selectivity ratio of EC50 for antiviral activity against PI-resistant HIV1 harboring RTI84V, L90M mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID622048 | Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer V106A mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID246283 | Effective concentration of the compound to inhibit HIV-1 mutant LAI replication in HIV-infected MT-4 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID736038 | Inhibition of HIV1 reverse transcriptase p66/p51 K103N/Y181C mutant after 30 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID523353 | Antiviral activity against HIV1 with RT connection domain Y181C mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID583865 | Inhibition of HIV1 histidine-tagged reverse transcriptase L100I mutant activity by primer extension assay | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID586385 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase N155T mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID241665 | Inhibitory concentration against HIV-1 mutant reverse transcriptase (K103N+Y181C) | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
| Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives. |
AID1750718 | Inhibition of HIV-1 p66/p51 reverse transcriptase K103N mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID584081 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I, H221Y, F227F/L, M230M/I mutant infected in human SupT1 cells derived from 11 viral passages with lersivirine assessed as inhibition of viral replication after 21 days relative to | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID586387 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T66I/E92Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficienc | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID586466 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase L74M/N155H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficien | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1057038 | Antiviral activity against HIV2 ROD infected in MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
| Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs. |
AID1754644 | Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
AID255623 | Concentration required to reduce the viability of mock-infected human CEM cells | 2005 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
| Synthesis and evaluation of anti-HIV activity of isatin beta-thiosemicarbazone derivatives. |
AID1316342 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1884494 | Inhibition of recombinant wild-type p66/p51 HIV-1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID279436 | Antiviral activity against HIV1 isolate with RT 103R, 179D mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID105704 | Anti-HIV-1 activity against Y181C strain, in MT-4 cells by the MTT method | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
| 3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID508757 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138K, M230L mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID106053 | Inhibitory activity against 100I strain of HIV-I in MT-4 cells | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. |
AID587738 | Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
AID607876 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type Human immunodeficieny virus 1 3B infected in human MT4 cells | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
| Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID88366 | Antiviral activity against K103N mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID586383 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase N155H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1326646 | Inhibition of HIV-1 3B reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by cell titer glo based luciferase reporter gene assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1. |
AID141361 | Inhibitory activity against mutant K103N HIV-1 Reverse transcriptase | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
| Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors. |
AID576027 | Apparent oral clearance in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID313189 | Protection against HIV1 HTLV 3B-induced cytopathogenicity in human MT4 cells by MTT assay | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Synthesis and antiviral activity of new dimeric inhibitors against HIV-1. |
AID1736362 | Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase K103N mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cells | | | |
AID404607 | Antiviral activity against HIV1 with reverse transcriptase K103R mutation | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
| Parallel one-pot synthesis and structure-activity relationship study of symmetric formimidoester disulfides as a novel class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | | | |
AID279499 | Antiviral activity against HIV1 isolate with RT A98G mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID269802 | Antiviral activity against HIV1 Y188L mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269802 | Antiviral activity against HIV1 Y188L mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269802 | Antiviral activity against HIV1 Y188L mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID416759 | Antiviral activity against HIV1 with reverse transcriptase Y188L mutation in human CEM cells assessed as protection against virus-induced cytopathicity | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus. |
AID1483281 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase K103N mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID1574376 | Antiviral activity against HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID522378 | Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106I/V179D mutant clone to EC50 for wild type HIV1 | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID443688 | Antiviral activity against HIV with reverse transcriptase K101E/G190A double mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID279447 | Antiviral activity against HIV1 isolate with RT 236L mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID105203 | Antiviral activity against MT-4 cells infected with wild-type HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID573978 | Antiretroviral activity against Human immunodeficiency virus 2 EHO infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID1186001 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/P225H double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay r | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID1161106 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors. |
AID1815389 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID305058 | Cytotoxicity against HEK293T cells after 48 hrs | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
| 4-Aminopyrimidines as novel HIV-1 inhibitors. |
AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1
| Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID632804 | Cytotoxicity against human MT2 cells infected with HIV1 NL4.3 by MTT assay | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents. |
AID1186008 | Antiviral activity against HIV1 infected in 293T cells assessed as time of 50% failure | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID279508 | Antiviral activity against HIV1 isolate with RT Y181C mutation in Hela-JC-53 cells | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1822273 | Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID1155812 | Fold resistance, ratio of EC50 for HIV-1 harboring NNTRI-resistant reverse transcriptase Y188L mutant infected in human MT4 cells to EC50 for wild type HIV-1 NL4-3 infected in human MT4 cells | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID368558 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID279444 | Antiviral activity against HIV1 isolate with RT 101Q, 181C, 190S mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID448398 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with Y181C mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 3: optimisation of physicochemical properties. |
AID1736366 | Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase Y188L mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cells | | | |
AID1729156 | Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID1186002 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/G190A double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID81765 | Compound was evaluated for its ability to inhibit a virus containing the clinically relevant K103N mutation | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
| 4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors. |
AID1483271 | Inhibition of HIV1 3B reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID1763901 | Antiviral activity against HIV-1 IIIB harboring RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID1157601 | Antiviral activity against HIV1 CRF02 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID247499 | Inhibitory activity against HIV-1 mutant strain 138K | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID257167 | Antiviral activity against HIV1 IRLL98 mutant strain infected MT4 cells by MTT method | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
| Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity. |
AID1335205 | Ratio of IC50 for HIV-1 NL4-3 harboring RT-L100I/K103N double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID282737 | Inhibition of HIV1 RT K103N mutant | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity. |
AID1483277 | Inhibition of HIV1 3B reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID508832 | Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93IN101 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID361915 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106M mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID562701 | Antiviral activity against wild type HIV1 infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation. |
AID519890 | Selectivity ratio of EC50 for 0.01 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.01 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID649487 | Inhibition of RNA-dependent DNA polymerase activity of Human immunodeficiency virus 1 reverse transcriptase Tyr181Cys mutant | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach. |
AID1335210 | Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/G190A double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID1884542 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 E138K mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID105326 | Inhibition of HIV-1 (IIIB) induced cytopathicity in MT-4 cells. | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations. |
AID389379 | Cytotoxicity against human MT4 cells | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
| 1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID397177 | Antiviral activity against HIV1 3B expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5
| Parallel synthesis, molecular modelling and further structure-activity relationship studies of new acylthiocarbamates as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID279518 | Antiviral activity against HIV1 NL4-3 in Hela-JC53 cells in the presence of 10% human serum after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID106065 | Inhibitory activity against 181C strain of HIV-I in MT-4 cells | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. |
AID440081 | Antiviral activity against HIV1 HXB2 harboring 190A mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID586369 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID302258 | Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT Y188L mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID1583021 | Cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
| Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel. |
AID276231 | Antiviral activity against HIV1 3B in MT2 cells | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
| Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1191401 | Antiviral activity against wild type HIV-2 ROD infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
| Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1191404 | Inhibition of wild type HIV1 p66/p51 reverse transcriptase by spectrofluorometry | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
| Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID88380 | Antiviral activity against V108I/Y181C mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID348906 | Antiviral activity against drug-resistant HIV1 with reverse transcriptase Y181C mutant infected in human MT4 cells assessed as virus-induced cell death by MTT method | 2008 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
| Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies. |
AID572182 | Antiviral activity against HIV-1 SM012 harboring NNTRI 108I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1379963 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs. |
AID611907 | Antiviral activity against wild type Human immunodeficiency virus 1 NL 4.3 pseudotyped with VSV-G envelope co-transfected with luciferase gene infected in human 293T cells assessed as inhibition of HIV1 replication administered 15 mins prior to infection | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Lindenane disesquiterpenoids with anti-HIV-1 activity from Chloranthus japonicus. |
AID508772 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y188L mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1485969 | Inhibition of HIV-1 reverse transcriptase L100I mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Searching for novel N |
AID508774 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1249722 | Antiviral activity against HIV1 expressing reverse transcriptase Y188L mutant | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID298074 | Antiviral activity against HIV1 3B in MT4 cells by MTT assay | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. |
AID279325 | Inhibition of reverse transcriptase activity in HIV1 NL4-3 infected MT4 cells before dialysis | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification. |
AID299027 | Antiviral activity against HIV1 with reverse transcriptase L100I mutation in CEM cells assessed as inhibition of virus-induced giant cell formation | 2007 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
| Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains. |
AID649486 | Inhibition of RNA-dependent DNA polymerase activity of Human immunodeficiency virus 1 reverse transcriptase Lys103Asn mutant | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach. |
AID279452 | Antiviral activity against HIV1 isolate with RT 103N, 108I, 238T mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID605178 | Inhibition of HIV1 reverse transcriptase Y181C mutant by SPA assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif. |
AID104802 | In vitro cytotoxicity against mock infected MT-4 cells. | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations. |
AID666971 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors. |
AID642209 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Quinoline tricyclic derivatives. Design, synthesis and evaluation of the antiviral activity of three new classes of RNA-dependent RNA polymerase inhibitors. |
AID105700 | Anti-HIV-1 activity against K103N+Y181C strain was determined in MT-4 cells by the MTT method | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
| 3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID573479 | Antiviral activity of Human immunodeficiency virus 1 isolate 9225 harboring A98S, G190A mutation in reverse transcriptase by cell based assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID105701 | Anti-HIV-1 activity against LAI strain in MT-4 cells by the MTT method | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
| 3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID573464 | Inhibition of RNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase by filter-based filtration assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID443706 | Antiviral activity against HIV with reverse transcriptase K101E/Y181C/G190A mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID347610 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 100I mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID650545 | Antiviral activity against HIV 1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | | | |
AID1815385 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID508621 | Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG001 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID572180 | Antiviral activity against HIV-1 SM002 harboring NNTRI 181C mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1691437 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP. |
AID391221 | Inhibition of wild type HIV1 RT polymerase by SPA | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
| Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses. |
AID105537 | Inhibitory activity against HIV-1 Cys 181 mutant in MT-4 cells. | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
| Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues. |
AID541127 | Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of late RT products after 12 hrs | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID573249 | Cmax in HIV-1 infected children at 10 to 15 mg/kg, po administered once daily by HPLC | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID1731751 | Inhibition of reverse transcriptase F227L/V106A double mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID1743619 | Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID279419 | Antiviral activity against HIV1 isolate with RT 101Q, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID508755 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179E, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID247617 | Inhibitory activity against HIV-1 double mutants strain 100I and 103N | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID371909 | Antiviral activity against HIV1 NL4-3 with L100I mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID1552560 | Antiviral activity against HIV1 LAI infected in human LC5 cells expressing DsRed1 reporter gene assessed as inhibition of viral infection measured after 48 hrs post infection by reporter gene based luminescence assay | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
| Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline. |
AID1822278 | Antiviral activity against HIV-1 harboring Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID248068 | Inhibitory concentration against 100I and 103N mutant strains was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity. |
AID519965 | Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID1483282 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase Y181C mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID279468 | Antiviral activity against HIV1 isolate with RT 98G, 108I, 181C mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1637396 | Antiviral activity against human HIV-1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID649489 | Inhibition of ribonuclease H activity of Human immunodeficiency virus 1 reverse transcriptase Lys103Asn mutant | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach. |
AID279320 | Inhibition of reverse transcriptase assessed as decrease in ssDNA level in cell free virion HIV1 by NERT-based real-time PCR at 250 uM | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification. |
AID1204077 | Cytotoxicity against human MT4 cells assessed as cell viability after 96 hrs by MTT method | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
| N-((1,3-Diphenyl-1H-pyrazol-4-yl)methyl)anilines: A novel class of anti-RSV agents. |
AID361928 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V108I/Y181C mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID557035 | Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1888692 | Selectivity index, ratio of CC50 for toxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells cells assessed as protection against viral-induc | | | |
AID557047 | Antiviral activity against HIV1 clade D harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1535523 | Antiviral activity against HIV1 RES056 containing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2019 | Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
| Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs. |
AID496615 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, K64R, K102Q, D123E, S162A, K173T, Q174K, D177E, G196E,T200A, Q207E, R211K mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID1069126 | Antiviral activity against wild-type HIV infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
| Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses. |
AID1624241 | Binding affinity to HIV1 cYTA48P envelope glycoprotein gp120 infected in human TZM-b1 cells assessed as induction of conformational changes measured after 48 hrs | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5
| Soluble-type small-molecule CD4 mimics as HIV entry inhibitors. |
AID476469 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus replication by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
| Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives. |
AID1729159 | Antiviral activity against HIV1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID584237 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I mutant derived from 17 days viral passages with lersivirine infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type HIV1 NL4- | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID269689 | Antiviral activity against HIV1 NNTRI resistant L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269689 | Antiviral activity against HIV1 NNTRI resistant L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269689 | Antiviral activity against HIV1 NNTRI resistant L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID386623 | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. |
AID1348213 | Antiviral activity against wild-type VSV-G pseudotyped HIV1 infected in HEK293 cells pretreated for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene assay | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12
| Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities. |
AID83547 | Potency evaluated against NNRTI-Resistant HIV-1 strain Gly190Ala | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
| Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian |
AID279528 | Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells in the presence of 40% human serum after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1457054 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID635302 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
AID298061 | Antiviral activity against HIV1 3B in human MT4 cells by XTT assay | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability. |
AID1191402 | Cytotoxicity against human MT4 cells after 5 days MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
| Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID465424 | Oral bioavailability in Beagle dog at 4 mg/kg | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1171595 | Inhibition of wild type HIV1 reverse transcriptase Y181I/Y181C mutant assessed as reduction in enzyme activity | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1180486 | Antiviral activity against VSV-G protein pseudotyped HIV1 infected in 293T cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter assay | 2014 | Journal of natural products, Jul-25, Volume: 77, Issue:7
| Uralsaponins M-Y, antiviral triterpenoid saponins from the roots of Glycyrrhiza uralensis. |
AID1888704 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT F227L + V106A mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
AID586482 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase N155H/G163R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1773450 | Antiviral activity against HIV1 harboring F227L/V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | | | |
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. |
AID1126508 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
| Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1171412 | Antiviral activity against wild type HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay | 2014 | ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
| Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers. |
AID1822281 | Antiviral activity against HIV-1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID1261812 | Cytotoxicity against human MT4 cells assessed as reduction in cell proliferation after 96 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Nov-13, Volume: 105 | Synthesis, cytotoxicity and antiviral evaluation of new series of imidazo[4,5-g]quinoline and pyrido[2,3-g]quinoxalinone derivatives. |
AID557039 | Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID279525 | Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells in the presence of 10% human serum after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID361913 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase G190S mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID650548 | Resistance ratio of EC50 for HIV 1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | | | |
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. |
AID1231485 | Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action. |
AID440669 | Cytotoxicity against human MT4 cells assessed as reduction of cell viability after 4 days by MTT assay | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
| Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants. |
AID1316341 | Antiviral activity against HIV1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID583869 | Inhibition of HIV1 histidine-tagged reverse transcriptase V108I mutant activity by primer extension assay | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID370728 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 V106A mutant expressed in Escherichia coli JM109 | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
AID523479 | Antiviral activity against HIV1 with RT connection domain G190S mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID508754 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1373162 | Inhibition of reverse transcriptase F227L/V106A double mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Structural optimization of N |
AID265471 | Activity against HIV1 3B assessed by inhibition of p24 production in human lymphocytes | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide. |
AID573248 | Cmax in HIV-1 infected children at 12 mg/kg, po administered once daily by HPLC | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID366527 | Inhibition of RNA dependent DNA polymerase activity of HIV1 reverse transcriptase K103N mutant | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID492286 | Antiviral activity against HIV1 with reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy. |
AID523354 | Antiviral activity against HIV1 with RT connection domain Y181C/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID583852 | Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.005 multiplicities of infection after 6 days | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID576029 | Apparent oral clearance in healthy human plasma at 400 mg, po measured on day 1 post dose by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID586382 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase M154I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID650688 | Inhibition of HIV 1 reverse transcriptase L100I mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT) | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID1815387 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase L100I mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | | | |
AID267652 | Selectivity for wild type HIV1 virus over HIV1 Y181C mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID1126507 | Antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
| Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID576037 | Half life in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID1320863 | Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
AID1235381 | Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 assessed as reduction in biotin deoxyuridine triphosphate (biotin-dUTP) incorporation using poly(rA)/oligo (dT)16 template and primer by spectrofluorometry | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1888694 | Antiviral activity against HIV1 with RT L100I mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
AID586467 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E92Q/N155H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficien | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1272056 | Inhibition of HIV1 reverse transcriptase | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry. |
AID1627026 | Cytotoxicity against HIV1 infected human PBMC cells assessed as reduction in cell viability after 7 days by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID519961 | Selectivity ratio of EC50 for 0.02 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by MTS assay to EC50 for 0.02 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID496742 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/V35T, K122E, I135V, T139A, S162A, K173T, Q174K, N175Y, D177E, T200A, Q207E, R211K mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID1220382 | Antiviral activity against HIV1 expressing Env-green fluorescent fusion protein infected in PBMC assessed as inhibition of viral activity after 72 hrs by flow cytometry analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
| Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid. |
AID464768 | Half life in human microsomes | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1171585 | Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID573468 | Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase DNA-dependent DNA polymerase activity by gel-based primer extension assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1822279 | Antiviral activity against HIV-1 harboring Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID247505 | Inhibitory activity against HIV-1 mutant strain 227C | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID1743634 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT L100I mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID698302 | Antiviral activity against HIV1 containing reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1391086 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID1888703 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT E138K mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
AID1410483 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
AID1155816 | Inhibition of HIV-1 recombinant NNTRI-resistant reverse transcriptase L100I mutant assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:1 | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID586363 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E92Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vir | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID508797 | Ratio of EC50 for HIV1 in presence of 45 mg/ml HSA to EC50 for HIV1 in absence of serum proteins by GFP assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1220372 | Seminal plasma protein binding in human at 100 mg administered every 4 hrs by ultrafiltration method | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
| Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid. |
AID1705189 | Antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID1558857 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID252955 | Ratio of CC50 and EC50 against wild type human immunodeficiency virus type 1 LAI strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID198917 | Inhibition of HIV-1 wild-type RT | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. |
AID573469 | Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1335220 | Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/Y188L double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID1357792 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID1185995 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay relative HIV1 | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID248258 | In vitro inhibitory concentration against HIV G190S mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID1637403 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring E138K mutant infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID347085 | Inhibition of RNA-dependent DNA polymerase activity of wild type HIV1 reverse transcriptase | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays. |
AID508827 | Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG037 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID88364 | Antiviral activity against E138K mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID361926 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106A/Y181C mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1390715 | Resistance index, ratio of EC50 for HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
| First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain. |
AID1636148 | Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase A98G/K101E/Y181C/G190A mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors. |
AID269798 | Antiviral activity against HIV1 K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269798 | Antiviral activity against HIV1 K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269798 | Antiviral activity against HIV1 K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1815397 | Inhibition of HIV1 reverse transcriptase L100I mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1767116 | Inhibition of wild type HIV-1 NL4-3 reverse transcriptase using random mRNA as template and GADPH as primer measured at 42 degreeC for 5 mins, 95 degreeC for 10sec and 60 degreeC for 60 sec by qRT-PCR analysis | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase. |
AID650546 | Antiviral activity against HIV 1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
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. |
AID1535525 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2019 | Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
| Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs. |
AID1410482 | Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
AID371897 | Selectivity index, ratio of CC50 for human TZM-b1 cells to EC50 for HIV1 NL4-3 | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID348904 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as virus-induced cell death by MTT method | 2008 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
| Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies. |
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. |
AID366558 | Antiviral activity against HIV1 with reverse transcriptase K103N/L100I mutation in human MT4 cells assessed as reduction of virus-induced cytopathic effect | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID571975 | Antiviral activity against HIV-1 subtype CRF01_AE V029525 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID347617 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 227L mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID1609108 | Antiviral activity against HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID263153 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID263153 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID263153 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1583023 | Selectivity index, ratio of CC50 for cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay to EC50 for antiviral activity against NNRTI-resistant HIV1 RES056 containing reverse transcriptas | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
| Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel. |
AID279465 | Antiviral activity against HIV1 isolate with RT 98G, 103N, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1565093 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB | | | |
AID698294 | Antiviral activity against HIV1 IRLL98 containing reverse transcriptase K101Q, Y181C and G190A mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID767498 | Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
| Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility. |
AID1163234 | Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by WST1 assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
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. |
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. |
AID279412 | Antiviral activity against HIV1 isolate with RT 103N, 188L mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1705190 | Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID105205 | Potency against non nucleoside reverse transcriptor was determined in MT-4 cells | 2004 | Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
| Threshold interaction energy of NRTI's (2'-deoxy 3'-substituted nucleosidic analogs of reverse transcriptase inhibitors) to undergo competitive inhibition. |
AID1286677 | Aqueous solubility of the compound at pH 7 | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor. |
AID584047 | Ratio of IC50 for HIV1 reverse transcriptase Y181C, Y188C mutant to IC50 for wild type HIV1 reverse transcriptase | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID248648 | Inhibitory concentration against wild type human immunodeficiency virus type 1 was determined by recombinant virus assay | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2. |
AID572170 | Antiviral activity against HIV-1 subtype D V022818 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1171413 | Antiviral activity against wild type HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay | 2014 | ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
| Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers. |
AID1558847 | Antiviral activity against HIV1 3B infected in human MT4 cells incubated assessed as reduction in virus-induced cytopathic effect for 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID1171589 | Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4-3 | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1335211 | Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/Y188L double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID1198754 | Inhibition of HIV1 reverse transcriptase Lys103Asn mutant-associated RNA-dependent DNA polymerase activity after 30 mins | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase. |
AID1627030 | Antiviral activity against HIV-1 LAI infected in human PBM cells after 7 days | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1565091 | Antiviral activity against drug resistant HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID106949 | Anti-HIV-1 activity against WTIIIB HIV-1 strain in MT-4 cells | 2001 | Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
| Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID143395 | Antiviral activity against HIV-1 in MT-2 (human leukemia) cells in vitro. | 2001 | Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
| Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase. |
AID1316339 | Antiviral activity against HIV1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1352312 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID279430 | Antiviral activity against HIV1 isolate with RT 103N, 106I mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1373158 | Inhibition of reverse transcriptase L100I mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Structural optimization of N |
AID263516 | Antiviral activity against HIV1 I135V mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2. |
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | | | |
AID1275550 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID298090 | Inhibition of HIV1 RT L100I mutant | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. |
AID441311 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with F227L mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 1: design and initial optimisation of a novel template. |
AID508785 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138A mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID279511 | Antiviral activity against HIV1 isolate with RT V106I, Y181C mutation in Hela-JC-53 cells | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1693802 | Inhibition of recombinant HIV-1 BH10 reverse transcriptase using D38/[32P]25PGA as template-primer at 100 uM incubated for 5 mins followed by dTTP addition and measured after 15 to 30 sec by nucleotide incorporation assay relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C. |
AID247503 | Inhibitory activity against HIV-1 mutant strain 190A | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID496618 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, E36D, V60I, K122E, D123S, I135V, E138D, S162A, K173T,Q174S, D177E, I178M, V189I, T200A, I202V, Q207E, F214L, V245Q mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID279517 | Antiviral activity against wild type HIV1 NL4-3 in Hela-JC53 cells in the presence of 5% human serum after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID371903 | Antiviral activity against HIV1 NL4-3 with L100I/V108I double mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID82961 | Inhibitory activity against HIV-1 reverse transcriptase | 1999 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
| Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA). |
AID621974 | Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID1242376 | Resistance index, ratio of EC50 for NRTI-resistant HIV containing reverse transcriptase K103N/Y181C mutation to EC50 for wild type HIV | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
| Pyrazolo-Piperidines Exhibit Dual Inhibition of CCR5/CXCR4 HIV Entry and Reverse Transcriptase. |
AID571978 | Antiviral activity against HIV-1 subtype B V022810 harboring NNRTI A98S andK101R mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1249715 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by MTT method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID698145 | Inhibition of HIV1 reverse transcriptase K103N mutant RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID248494 | In vitro inhibitory concentration against HIV L100I and K103N mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID1736344 | Antiviral activity against VSVG/wild-type HIV-1 infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hrs post-infection by luciferase reporter gene ass | | | |
AID650542 | Antiviral activity against multidrug-resistant HIV 1 IRLL98 harboring reverse transcriptase K101Q/Y181C/G190a mutant infected in human MT4 cells assessed as virus-induced cytopathic effect after 5 days by MTT assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID1443660 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID591355 | Antiviral activity against HIV2 isolate ROD infected in human CEM cells assessed as inhibition of virus-induced cytopathicity after 4 days by microscopic analysis | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide. |
AID621978 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID366556 | Antiviral activity against HIV1 in human MT4 cells assessed as reduction of viral-induced cytopathic effect in presence of human serum | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID592540 | Cytotoxicity against human CEM cells by coulter counter analysis | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide. |
AID1316337 | Antiviral activity against HIV1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
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. |
AID1815398 | Inhibition of HIV1 reverse transcriptase K103N mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1773456 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring F227L/V106A double mutant infected in human MT4 cells | | | |
AID508644 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1773839 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies. |
AID279489 | Antiviral activity against HIV1 isolate with RT K103N-V108I-P225H mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1483283 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase Y188L mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID265470 | Cytotoxicity against human lymphocytes | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide. |
AID562119 | Apparent oral clearance in patient with HIV infection at 600 mg/kg, iv QD | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
| Influence of the cytochrome P450 2B6 genotype on population pharmacokinetics of efavirenz in human immunodeficiency virus patients. |
AID541132 | Selectivity ratio of EC50 for antiviral activity against NNRTI-resistant HIV1 harboring RTK103N mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID576040 | Ratio of drug concentration in PBMCs to plasma of healthy human administered at 400 mg, po qd for 14 days measured after 5 hrs post last dose | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID265474 | Selectivity index, TC50 for human lymphocytes/EC50 for HIV1 3B | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide. |
AID267862 | Inhibition of HIV1 reverse transcriptase K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
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. |
AID1316340 | Antiviral activity against HIV1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1884488 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against NNRTI resistant HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID635347 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
AID522373 | Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106I/V179D mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID1485973 | Inhibition of HIV-1 reverse transcriptase Y181C mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Searching for novel N |
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AID386493 | Inhibition of HIV1 recombinant wild type reverse transcriptase | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Parallel synthesis, molecular modelling and structure-activity relationship studies on analogues of O-(2-phenylethyl)-N-phenylthiocarbamate. |
AID82474 | Antiviral activity against Y181C strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID717257 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs. |
AID1352315 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID1391076 | Inhibition of wild type HIV1 reverse transcriptase using poly (A)/oligo (dT)15 as template/primer assessed as decrease in biotin-dUTP incorporation after 1 hr by ELISA | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID508783 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138K mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID519863 | Antiviral activity against HIV1 subtype B-NL4-3 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID573482 | Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 9225 harboring A98S, G190A mutation in reverse transcriptase to wild-type | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1335216 | Antiviral activity against HIV-1 NL4-3 harboring RT-K103N mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID1212900 | Drug metabolism in human liver microsomes harboring CYP2B6*1/*6 genotype assessed as intrinsic clearance for CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation measured per mg protein after 15 mins by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID269687 | Antiviral activity against HIV1 NNTRI resistant Y181C mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269687 | Antiviral activity against HIV1 NNTRI resistant Y181C mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269687 | Antiviral activity against HIV1 NNTRI resistant Y181C mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID573247 | Cmin in HIV-1 infected children at 14.4 mg/kg, po administered once daily by HPLC | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID106950 | Anti-HIV-1 activity against Y181C HIV-1 strain in MT-4 cells | 2001 | Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
| Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID82604 | The effect of protein binding on the antiviral activity versus wild type virus strain HXB2 was tested in the presence of both acid glycoprotein and human serum in HeLa MAGI assay | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID247495 | Inhibitory activity against HIV-1 mutant strain 100I | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID241533 | Inhibitory concentration against HIV-1 wild type reverse transcriptase (IIIB) | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
| Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives. |
AID573478 | Antiviral activity of Human immunodeficiency virus 1 isolate 8117 harboring A98S, G190A mutation in reverse transcriptase by cell based assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1761019 | Antiviral activity against HIV-1 harboring reverse transcriptase F227L/V106A mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID246394 | Effective concentration against human immunodeficiency virus type 1 mutated at 227L+106A | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
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AID1636931 | Aqueous solubility of compound in pH 6.5 solution by shake flask method | 2016 | Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
| Computer-aided discovery of anti-HIV agents. |
AID757622 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1636149 | Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase K103N/V179F/Y181C mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors. |
AID1316344 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
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| Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs. |
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| Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues. |
AID1304401 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID374090 | Antiviral activity against HIV1 3B Y181C resistant mutant in human MT4 cells assessed as protection against viral induced cytopathogenicity by MTT assay | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
| Novel modifications in the series of O-(2-phthalimidoethyl)-N-substituted thiocarbamates and their ring-opened congeners as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
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| Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
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| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID508825 | Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG029 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
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| Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID44797 | In vitro reduction of p24 by 90% in Efavirenz resistant HIV-1 (K103R, V179D, P225H) infected C8166 cells. | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations. |
AID508788 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V106A mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID508793 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101E mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID105698 | Anti-HIV-1 activity against K103N+K1001 strain was determined in MT-4 cells by the MTT method | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
| 3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
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| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
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| Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors. |
AID1457052 | Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
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| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
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| Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents. |
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| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
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| Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors. |
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| Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
AID1558854 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID1391079 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID279461 | Antiviral activity against HIV1 isolate with RT 179D, 188L mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
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AID279439 | Antiviral activity against HIV1 isolate with RT 101P, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
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AID446255 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with V106A mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
AID1335203 | Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/P225H double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID1335212 | Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/P225H double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID298075 | Antiviral activity against HIV1 RT Y181C mutant in MT4 cells by MTT assay | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. |
AID614140 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17
| Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs. |
AID1815394 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase F227L/V106A double mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID298087 | Inhibition of wild type HIV1 RT | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. |
AID573979 | Antiretroviral activity against Simian immunodeficiency virus MAC 251 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
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| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID347086 | Inhibition of RNA-dependent DNA polymerase activity of HIV1 reverse transcriptase K103N mutant | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays. |
AID519964 | Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID293559 | Antiviral activity against HIV1 LAI with RT Y188L mutation in MT4 cells by EGFP based replication assay | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5
| Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains. |
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AID141360 | Potency of second-generation NNRTIs against Mutant HIV-1 sV179D/L100I/Y181C plasma; value ranges from 130000-309500 | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID1884229 | Antiviral activity against HIV-1 RES056 infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID266346 | Inhibition of HIV1 reverse transcriptase K103N mutant in 293T cells | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity. |
AID253332 | Cytotoxic concentration against wild type human immunodeficiency virus type 1 LA1 strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID611908 | Antiviral activity against Human immunodeficiency virus 1 NL 4.3 harboring reverse transcriptase K103N mutant pseudotyped with VSV-G envelope co-transfected with luciferase gene infected in 293T cells assessed as inhibition of HIV1 replication administere | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Lindenane disesquiterpenoids with anti-HIV-1 activity from Chloranthus japonicus. |
AID465418 | Antiviral activity against wild type HIV1 infected in human MT2 cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID508790 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID269804 | Antiviral activity against HIV1 Y181H mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269804 | Antiviral activity against HIV1 Y181H mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269804 | Antiviral activity against HIV1 Y181H mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID198070 | Inhibitory activity against E138K mutant reverse transcriptase | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase. |
AID1352323 | Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 using poly (rA)/anoligo (dT)16 as template/primer assessed as inhibition of biotin-dUTP incorporation after 40 mins by Pico-Green staining based fluorescence assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID1272057 | Tmax in human plasma after the first dose of drug | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry. |
AID361927 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106I/Y181C mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1264541 | Antiviral activity against HIV-1 X4 expressing reverse transcriptase Y181C mutant infected in human CD4+ T cells for 3 days by FACS analysis | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
| Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance. |
AID1811035 | Anti-viral activity against HIV1 harboring RT Y188L mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID557021 | Antiviral activity against HIV1 CRF02_AG harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID347608 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 190A mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID509269 | Inhibition of HIV1 RT at 20 to 0.625 uM by ELISA | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Antiviral efficacy of the novel compound BIT225 against HIV-1 release from human macrophages. |
AID279422 | Antiviral activity against HIV1 isolate with RT 190E mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID508781 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138R mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID517495 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses. |
AID1316360 | Fold resistance, ratio of IC50 for recombinant HIV1 reverse transcriptase K103N/Y181C double mutant to IC50 for wild type HIV1 reverse transcriptase | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1888695 | Antiviral activity against HIV1 with RT K103N mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
AID1636150 | Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase L100I/K103N/H221Y mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors. |
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. |
AID1691435 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cell death incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP. |
AID1141971 | Ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1687681 | Antiviral activity against HIV-1 K103N mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID1880373 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Structure-Based Discovery of Novel NH |
AID1156485 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors. |
AID508626 | Antiviral activity against Human immunodeficiency virus 1 subtype E isolate CMU08 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1316328 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID348907 | Ratio of ED50 for drug resistant HIV1 with reverse transcriptase K103N mutant to wild type HIV1 NL4-3 | 2008 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
| Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies. |
AID1705193 | Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID573253 | AUC (0 to t) in HIV-1 infected children at 14.4 mg/kg, po administered once daily by HPLC | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID82476 | Antiviral activity against wild-type HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID767501 | Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
| Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility. |
AID106074 | Inhibitory activity against LAI strain of HIV-I in MT-4 cells | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. |
AID574002 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for wild-type Human immunodeficiency virus 2 ROD | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID1773445 | Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | | | |
AID386489 | Antiviral activity against HIV1 with reverse transcriptase K103N/Y181C mutation in human MT4 cells assessed as reduction of virus-induced cytopathogenicity by MTT assay | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Parallel synthesis, molecular modelling and structure-activity relationship studies on O-[2-(hetero)arylethyl]-N-phenylthiocarbamates. |
AID496626 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K22N, V35T, T39A, K122E, I135V, T139A, S162A, K173T, Q174A, D177E, T200A, Q207E, R211K, F214L mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID1248225 | Antiviral activity against HIV 1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
| A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities. |
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. |
AID557037 | Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID518741 | Antiviral activity against HIV 1 subtype B harboring reverse transcriptase M230L mutant infected in human TZM-bl cells assessed as inhibition of viral growth by luciferase reporter gene assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID366523 | Resistance index, ratio of EC50 for drug-resistant HIV1 isolate with reverse transcriptase Y181C mutation to EC50 for wild type HIV1 NL4-3 | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID492043 | Inhibition of HIV1 reverse transcriptase | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors. |
AID440074 | Antiviral activity against HIV1 HXB2 harboring Y181C mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID1171582 | Antiviral activity against HIV2 ROD infected in human CEM cells assessed as protection against virus-induced cytopathicity by giant cell formation assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1191399 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
| Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID622053 | Ratio of Ki for HIV1 RT p66/p66 homodimer L100I mutant to Ki for wild-type HIV1 RT p66/p66 homodimer | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID361919 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase E138K mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID104408 | Antiviral activity of Protein Binding of compound was evaluated for HIV-2 virus expressed MT-2 by yield | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID246511 | Compound concentration required to achieve 50% protection of infected MT-4 cells from K103N-Y181C strain was determined by the MTT method | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives. |
AID371902 | Antiviral activity against wild type HIV1 NL4-3 in human MT4 cells assessed as inhibition of virus-induced cytopathicity after 5 days by multiple round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID519860 | Antiviral activity against HIV1 subtype B-SF-2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID443677 | Antiviral activity against HIV with reverse transcriptase L100I mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID443675 | Antiviral activity against HIV with reverse transcriptase MDRC4 mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID1168822 | Inhibition of CYP2B6 (unknown origin) assessed as reduction in hydroxybupropion formation at 10 uM incubated for 10 mins by uHPLC-MS/MS method | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Structure-Activity Studies Reveal the Oxazinone Ring Is a Determinant of Cytochrome P450 2B6 Activity Toward Efavirenz. |
AID1156487 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors. |
AID248257 | In vitro inhibitory concentration against HIV G190A mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID476468 | Cytotoxicity against human MT2 cells by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
| Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives. |
AID1212885 | Drug metabolism in microsomes expressing CYP2B6.6 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in presence of Cyt b5 coexpression | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID1574372 | Antiviral activity against wild type HIV 1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID1391080 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID397176 | Inhibition of wild-type HIV1 reverse transcriptase | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5
| Parallel synthesis, molecular modelling and further structure-activity relationship studies of new acylthiocarbamates as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1561720 | Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of (E)-4-((4-((4-(4-(2-Cyanovinyl)-2,6-dimethylphenoxy)thieno[2,3- d]pyrimidin-2-yl)amino)piperidin-1-yl)methyl)benzenes | | | |
AID1687683 | Antiviral activity against HIV-1 E138K mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID557048 | Antiviral activity against HIV1 clade F1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID347090 | Metabolic stability in human hepatocytes assessed as half life | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays. |
AID1736360 | Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase G190A/K103N double mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hr | | | |
AID557068 | Plasma protein binding in healthy human at 200 mg/kg | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1298249 | Inhibition of HIV1 reverse transcriptase p66/p51 K103N mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
AID1155809 | Antiviral activity against HIV-1 harboring NNTRI-resistant reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID586477 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase G140S/Q148K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1220381 | Drug metabolism of the compound assessed as CYP2C8 (unknown origin)-mediated formation of dihydroxylated metabolites with retention time of 1.92 mins at 5 uM by UPLC-MS/MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
| Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid. |
AID257166 | Antiviral activity against wild type HIV1 NL4-3 infected MT4 cells by MTT method | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
| Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity. |
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | | | |
AID1456306 | Inhibition of HIV-1 3B wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. |
AID366519 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID1186005 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/V108I double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay r | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID736440 | Non-competitive inhibition of wild type HIV1 reverse transcriptase p66/p51 after 30 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID267648 | Antiviral activity against HIV1 Y181C mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID443691 | Antiviral activity against HIV with reverse transcriptase V106A/G190A/F227L mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID757625 | Antiviral activity against HIV1 RES056 expressing RT K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID81627 | Antiviral activity was evaluated against K103N mutant HIV-1 virus | 2001 | Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9
| Synthesis and evaluation of efavirenz (Sustiva) analogues as HIV-1 reverse transcriptase inhibitors: replacement of the cyclopropylacetylene side chain. |
AID313190 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Synthesis and antiviral activity of new dimeric inhibitors against HIV-1. |
AID496622 | Antiviral activity against HIV-1 subtype CRF06_cpx ontaining reverse transcriptase V106I/V21I, V35T, V60I, K122T, D123R, I135V, S162A, K173T, Q174K, D177E, I178L, T200A, Q207D, R211K, V245Q, E248D mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID370726 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 K103N mutant expressed in Escherichia coli JM109 | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
AID1357785 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID508753 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID279455 | Antiviral activity against HIV1 isolate with RT 103N, 188H mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID620429 | Antiviral activity against wild type HIV1 BaL in human TZM-b1 cells after 48 hrs by luciferase assay | 2011 | Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
| Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs). |
AID1352317 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID1731752 | Inhibition of reverse transcriptase RES056 mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID1261316 | Antiviral activity against human RSV infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by plaque reduction assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
AID1811037 | Anti-viral activity against HIV1 harboring RT K103N mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID1687687 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells reduction in cell viability by MTT assay to EC50 for antiviral activity against wild type HIV-1 strain IIIB infected in human MT4 cells assessed as reduction in virus-induced cytopa | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID573466 | Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID556524 | Antiviral activity against Human immunodeficiency virus 1 clone pNL4-3-Q145M harboring K102Q, Q145M, S162C, K277R, I293V mutation in reverse transcriptase by phenosense assay relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility. |
AID508642 | Antiviral activity against Human immunodeficiency virus 1 subtype AE infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1410405 | Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as decrease in biotin-dUTP incorporation using DIG-labeled dUTP/biotin-labeled dUTP and dTTP as template and viral nucleotides after 1 hr by ELISA | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site. |
AID105539 | Inhibitory activity against HIV-1 Ile 100 mutant in MT-4 cells. | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
| Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues. |
AID1653625 | Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) R415A mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID248316 | In vitro inhibitory concentration against HIV-1 Y181C mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID279462 | Antiviral activity against HIV1 isolate with RT 103N, 108I, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1155814 | Inhibition of HIV-1 recombinant NNTRI-resistant reverse transcriptase K103N mutant assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:1 | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1535522 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2019 | Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
| Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs. |
AID279418 | Antiviral activity against HIV1 isolate with RT 98G, 181C mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1558853 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID1763903 | Antiviral activity against HIV-1 IIIB harboring RT F227L/V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID519867 | Antiviral activity against HIV1 subtype B-ASM 034 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID244633 | Selective index value (ratio of CC50 to IC50 value)against HIV LAI cell line | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID304872 | Antiviral activity against HIV1 with reverse transcriptase IRLL98 mutation in MT4 cells after 5 days by MTT method relative to wild type NL4-3 | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
| Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants. |
AID1483286 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID522377 | Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106A/V179D mutant clone to EC50 for wild type HIV1 | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID663301 | Resistance ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-3 | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID347615 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 108I mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID440073 | Antiviral activity against HIV1 HXB2 harboring K103N mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID1206937 | Cytotoxicity against human MT4 cells assessed as reduction of cell viability after 4 days by MTT assay | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1637391 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID1304406 | Inhibition of wild type HIV-1 BH10 recombinant reverse transcriptase expressed in Escherichia coli assessed as incorporation of [32P]GTP into poly(rA)/oligo(dT) as template primer | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID104412 | Antiviral activity of Protein Binding of compound was evaluated for RF virus expressed MT-2 by yield | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID650694 | Ratio of ID50 for HIV 1 reverse transcriptase Y181I mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID508771 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase G190A mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID389378 | Antiviral activity against HIV1 3B in human MT4 cells assessed as protection of cell against virus-induced cytopathogenicity | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
| 1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID573990 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for non nucleoside Protease inhibitor-resistant Human immunodeficiency virus 1 | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID1483276 | Inhibition of HIV1 3B reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID1373155 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Structural optimization of N |
AID1637397 | Antiviral activity against human HIV-1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID246267 | Effective concentration against human immunodeficiency virus type 1 L100I mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). |
AID1558856 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID1767118 | Antiviral activity against HIV1 NL4-3 Env-deficient VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production when host cells were infected with compound pretreated viral particles at 10 uM measured after | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase. |
AID508631 | Antiviral activity against Human immunodeficiency virus 1 subtype G isolate JV1083 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
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. |
AID1503322 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 4 days by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Inhibitors of Yellow Fever Virus replication based on 1,3,5-triphenyl-4,5-dihydropyrazole scaffold: Design, synthesis and antiviral evaluation. |
AID269801 | Antiviral activity against HIV1 Y181C mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269801 | Antiviral activity against HIV1 Y181C mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269801 | Antiviral activity against HIV1 Y181C mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID265473 | Activity against HIV-AB1 assessed by inhibition of p24 production in human lymphocytes | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide. |
AID1298251 | Inhibition of HIV1 reverse transcriptase p66/p51 Y181C mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
AID1743626 | Antiviral activity against HIV1 harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID717258 | Cytotoxicity against human MT4 cells by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs. |
AID1691438 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP. |
AID1316359 | Inhibition of recombinant HIV1 reverse transcriptase K103N/Y181C double mutant using DIG-dUTP/biotin-dUTP/dTTP assessed as suppression of biotin-dUTP incorporation after 1 hr by ELISA | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1155807 | Antiviral activity against HIV-1 harboring NNTRI-resistant reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID663295 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID1731743 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID279417 | Antiviral activity against HIV1 isolate with RT 106A, F227L mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID572171 | Antiviral activity against HIV-1 subtype D V022819 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID198913 | Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution V106A | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. |
AID1773838 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies. |
AID298080 | Antiviral activity against HIV1 RT AB1 mutant in lymphocytes assessed as reduction of p24 antigen production | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. |
AID1880378 | Antiviral activity against HIV-1 IIIB harboring reverse transcriptase Y181C mutant infected in human MT4 cells by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Structure-Based Discovery of Novel NH |
AID347614 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 106A mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID246482 | Effective concentration for the inhibition of wild type human immunodeficiency virus type 1 LAI strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID293564 | Antiviral activity against HIV1 LAI with RT K103N and Y181C mutation in MT4 cells by EGFP based replication assay | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5
| Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains. |
AID279526 | Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells in the presence of 20% human serum after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1485968 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Searching for novel N |
AID279513 | Antiviral activity against HIV1 isolate with RT V106I, Y181C, F227L, T369I mutation in Hela-JC-53 cells | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1624242 | Cytotoxicity against human TZM-b1 cells assessed as reduction in cell viability by CCK8 assay | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5
| Soluble-type small-molecule CD4 mimics as HIV entry inhibitors. |
AID1574377 | Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID1653638 | Binding affinity to substrate bound recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli assessed as Koff rate of cholesterol by stopped-flow spectrophotometric method | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID1731753 | Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into wild type RT measured after 1 hr by ELISA | | | |
AID298076 | Antiviral activity against HIV1 RT K103N-Y181C mutant in MT4 cells by MTT assay | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. |
AID1155805 | Cytotoxicity against human MT4 cells assessed as induction of cell death by MTT method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
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. |
AID1457053 | Antiviral activity against HIV1 NL4-3 infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID1693803 | Inhibition of recombinant HIV-1 BH10 reverse transcriptase using D38/[32P]25PGA as template-primer incubated for 5 mins in presence of DTT followed by dTTP addition and measured after 15 to 30 sec by nucleotide incorporation assay | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C. |
AID1882476 | Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors. |
AID279395 | Antiviral activity against HIV1 isolate with RT 101Q mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID342720 | Cytotoxicity against human MT4 cells | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors. |
AID1352319 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID1529939 | Inhibition of recombinant HIV-1 M:B reverse transcriptase RNA-dependent DNA polymerase activity expressed in Escherichia coli M15 using poly(A)/oligo(dT)16 as template/primer measured after 30 mins by picogreen dye based assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Novel natural non-nucleoside inhibitors of HIV-1 reverse transcriptase identified by shape- and structure-based virtual screening techniques. |
AID767499 | Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
| Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility. |
AID650691 | Inhibition of wild type HIV1 NL4-3 reverse transcriptase assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT) | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID1773826 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies. |
AID572174 | Antiviral activity against HIV-1 subtype CRF05_DF V022833 harboring NNRTI V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1060626 | Fold resistance, ratio of EC50 for HIV1 RES056 expressing K103N/Y181C mutant infected in human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs. |
AID584080 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I, E138K, F227F/L mutant infected in human SupT1 cells derived from 11 viral passages with lersivirine assessed as inhibition of viral replication after 21 days relative to drug sen | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID508651 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID605180 | Antiviral activity against HIV1 R8 harboring reverse transcriptase infected in human MT4 cells assessed as inhibition of viral spread in presence of 50% normal human serum | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif. |
AID1298243 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
AID279433 | Antiviral activity against HIV1 isolate with RT 179T mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID443682 | Antiviral activity against HIV with reverse transcriptase G190S mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID104410 | Antiviral activity of Protein Binding of compound was evaluated for PB shift virus expressed MT-2 by RNA | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID1741399 | Inhibition of reverse transcriptase RES056 mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID391226 | Antiviral activity against HIV1 with reverse transcriptase Y181C mutant infected in human MT4 cells after 72 hrs in presence of 10% fetal bovine serum | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
| Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses. |
AID1729150 | Antiviral activity against HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID1261314 | Antiviral activity against Reo-1 virus infected in BHK-21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
AID198916 | Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution Y188L | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. |
AID1565094 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV RES056 | | | |
AID347088 | Antiviral activity against HIV1 NL4-3 in HeLaP4 reporter cell assessed as virus replication by FluorAceTM beta-galactosidase reporter assay | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays. |
AID523347 | Antiviral activity against HIV1 with RT connection domain N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID1141960 | Antiviral activity against HIV1 NL4.3 infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID508791 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101Q mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID771795 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 23 | Synthesis and structure evaluation of new complex butylarylpiperazin-1-yl derivatives. |
AID143399 | Compound was evaluated for its ability to inhibit the mutant K103N P225H NNRTI HIV-1 enzyme | 2001 | Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
| Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase. |
AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID1574381 | Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase Y188L mutant to EC50 for wild type HIV-1 NL4-3 | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID257917 | Antiviral activity against HIV1 Y181C mutant using HeLa MAGI assay | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor. |
AID586374 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase P145S mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID736039 | Inhibition of HIV1 reverse transcriptase p66/p51 G190A mutant after 30 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1161104 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors. |
AID1357796 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase E138K mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID663306 | Inhibition of HIV1 recombinant reverse transcriptase K103N mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT) | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID197783 | Compound was evaluated for the inhibition of HIV-1 Reverse transcriptase | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID1561719 | Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-[4-[2-cyanovinyl]-2,6-dimethylphenoxy]thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide assessed as protection against v | | | |
AID1264539 | Antiviral activity against HIV-1 X4 expressing reverse transcriptase K101P mutant infected in human CD4+ T cells for 3 days by FACS analysis | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
| Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance. |
AID257916 | Antiviral activity against HIV1 K103N mutant using HeLa MAGI assay | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor. |
AID106061 | Inhibitory activity against 103N strain of HIV-I in MT-4 cells | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. |
AID248263 | In vitro inhibitory concentration against HIV V179E mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID247724 | Inhibitory concentration against 103N mutant was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity. |
AID440084 | Antiviral activity against HIV1 HXB2 harboring 100I and K103N mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID1485975 | Inhibition of HIV-1 reverse transcriptase G190A mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Searching for novel N |
AID1163232 | Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
AID698301 | Antiviral activity against HIV1 containing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID302261 | Inhibition of HIV1 reverse transcriptase L100I mutant | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID446254 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with F227L mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
AID518736 | Selectivity ratio of IC50 for RNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant to IC50 for RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID557050 | Antiviral activity against HIV1 clade H harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID279478 | Antiviral activity against HIV1 isolate with RT 106L, 188L mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID519022 | Antiviral activity against Human immunodeficiency virus 1 NL432 infected in human MT-4 cells assessed as decrease in the integrated viral DNA | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
| The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral. |
AID583848 | Antiviral activity against HIV1 NL4-3 infected in human SupT1 cells derived from 11 viral passages assessed as inhibition of viral replication after 21 days relative to drug sensitive HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID588996 | Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, MRP2 | 2010 | Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
| Membrane transporters in drug development. |
AID1729160 | Antiviral activity against HIV1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID82464 | Antiviral activity against K103N/Y181C strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
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. |
AID279409 | Antiviral activity against HIV1 isolate with RT 101P, 103N mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1485965 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Searching for novel N |
AID1483284 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase E138K mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID166688 | Antiviral activity of Protein Binding of compound was evaluated for RF virus expressed plasma; value ranges from 92-220 | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID141358 | Potency of second-generation NNRTIs against Mutant HIV-1 sV179D/L100I/Y181C | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID1754645 | Antiviral activity against HIV1 harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
AID1446872 | Inhibition of recombinant HIV-1 group M subtype B RT-RNase H activity expressed in Escherichia coli M15 using 18-nucleotide 3'-fluorescein-labeled RNA annealed to a complementary 18-nucleotide 5'-dabsyl-labeled DNA as substrate measured after 1 hr | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Natural product-inspired esters and amides of ferulic and caffeic acid as dual inhibitors of HIV-1 reverse transcriptase. |
AID685330 | Antiviral activity against HIV-1 RES056 harboring RT K103N/Y181C mutant gene infected human MT4 cells assessed as inhibition in viral syncytium formation by MTT assay | 2012 | Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors. |
AID279389 | Antiviral activity against HIV1 isolate with RT 103N mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside 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. |
AID82475 | Antiviral activity against Y188C strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1888705 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT RES056 mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
AID1457074 | Neuroprotective activity against glutamate-induced excitotoxicity in C57BL/6 mouse BV2 cells assessed as increase in cell viability at 1000 nM preincubated for 30 mins followed by reincubation in conditioned culture media for 18 hrs in presence of glutama | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID508652 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101P, K103N, V108I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1435515 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase Y188L mutant | | | |
AID1391087 | Antiviral activity against HIV1 harboring reverse transcriptase RES056 double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID1157603 | Antiviral activity against HIV1 MP411 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID279497 | Antiviral activity against HIV1 isolate with RT K103N-K101Q-P225H mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID298060 | Antiviral activity against HIV1 RF in human CEM-SS cells by XTT assay | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability. |
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. |
AID248882 | Inhibitory concentration against human immunodeficiency virus type 1 (with V108I/Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2. |
AID347611 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 101E mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID519882 | Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID557023 | Antiviral activity against HIV1 clade A harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1161105 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors. |
AID1574375 | Antiviral activity against HIV 1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID330488 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID457959 | Inhibition of HIV1 reverse transcriptase L100I mutant by RNA-dependent DNA polymerase activity assay | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
| Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID492279 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy. |
AID302252 | Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT IRLL98 mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID1141970 | Ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID293181 | Selectivity index, ratio of CC50 for MT4 cells to IC50 for HIV1 LAI | 2007 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
| Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity. |
AID1637401 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring Y181C mutant infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID1275548 | Antiviral activity against HIV1 3B expressing reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID197931 | HIV-1 reverse transcriptase inhibitory activity against Asn103 mutant using (poly)rC600*(oligo)dGT as template primer. | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
| Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues. |
AID366521 | Resistance index, ratio of EC50 for drug-resistant HIV1 isolate with reverse transcriptase K103N mutation to EC50 for wild type HIV1 NL4-3 | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID576035 | Cmax in healthy human plasma at 400 mg, po measured on day 1 post dose by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID82608 | The effect of protein binding on the antiviral activity versus wild type virus strain K103N was tested in the presence of human serum in HeLa MAGI assay | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1357800 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase L100I mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
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. |
AID1822277 | Antiviral activity against HIV-1 harboring K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID1275545 | Antiviral activity against HIV1 3B expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID1815399 | Inhibition of HIV1 reverse transcriptase Y181C mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID622055 | Ratio of Ki for HIV1 RT p66/p66 homodimer Y181C mutant to Ki for wild-type HIV1 RT p66/p66 homodimer | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID247502 | Inhibitory activity against HIV-1 mutant strain 188L | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
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. |
AID635301 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
AID779529 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
AID1212917 | Drug metabolism in microsomes expressing CYP2B6.6 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by HPLC/UV system in absence of Cyt b5 coexpression | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID1077219 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
AID541135 | Selectivity ratio of EC50 for antiviral activity against PI-resistant HIV1 harboring RTG48V, V82A and L90M mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID650549 | Resistance ratio of EC50 for HIV 1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID1191403 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
| Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID509270 | Inhibition of HIV1 protease assessed as substrate cleavage by cell free assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Antiviral efficacy of the novel compound BIT225 against HIV-1 release from human macrophages. |
AID508767 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230L mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1884491 | Antiviral activity against drug-resistant HIV-1 Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID519960 | Selectivity ratio of EC50 for 0.01 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by MTS assay to EC50 for 0.01 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID246340 | Effective concentration against human immunodeficiency virus type 1 K103N and Y181C mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). |
AID248492 | In vitro inhibitory concentration against HIV K101E and K103N mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID293180 | Antiviral activity against HIV1 RT 103N/181C mutant assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method | 2007 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
| Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity. |
AID1391083 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID1335208 | Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/Y181C double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID1185991 | Cytotoxicity against HEK293T cells at 10 uM after 48 hrs | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID440671 | Antiviral activity against NNRTI-resistant HIV1 A17 with reverse transcriptase K103N, Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
| Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants. |
AID82607 | The effect of protein binding on the antiviral activity versus wild type virus strain K103N was tested in the presence of both acid glycoprotein and human serum in HeLa MAGI assay | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1743636 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID1357794 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase L100I mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID1761011 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID1261340 | Antiviral activity against HSV1 | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
AID1653623 | Binding affinity to recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli in presence of substrate by UV-spectrophotometric method | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID562702 | Antiviral activity against HIV1 harboring capsid I201V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation. |
AID361921 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase P236L mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1391084 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID1811046 | Selectivity index, ratio of CC50 for mock infected human MT4 cells to IC50 for HIV1 IIIB infected human MT4 cells | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID492276 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy. |
AID717256 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs. |
AID1884492 | Antiviral activity against drug-resistant HIV-1 Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID1220361 | Total blood plasma concentration in human | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
| Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid. |
AID586365 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase L101I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID717844 | Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation at 20 uM after 45 mins by spectrophotometric analysis relative to control | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
| Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2. |
AID279506 | Antiviral activity against HIV1 isolate with RT V106I mutation in Hela-JC-53 cells | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID650692 | Inhibition of HIV 1 reverse transcriptase Y188L mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT) | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID518739 | Selectivity ratio of IC50 for DNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant to IC50 for DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID1653624 | Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase and L-Glu by gas chromatography | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID1220362 | Total seminal plasma concentration in human | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
| Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid. |
AID541172 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V and V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID279529 | Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells in the presence of 50% human serum after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID473116 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
| Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV. |
AID443681 | Antiviral activity against HIV with reverse transcriptase G190A mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID1156484 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors. |
AID663296 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID1163231 | Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei rhodesiense STIB-900 assessed as reduction in parasite growth after 72 hrs | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
AID246266 | Effective concentration against human immunodeficiency virus type 1 K103N mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). |
AID1077220 | Cytotoxicity against human MT4 cells assessed as growth inhibition after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
AID1520066 | Inhibition of recombinant wild type HIV-1 His-tagged reverse transcriptase p66/p51 expressed in Escherichia coli JM109 using poly(rA)/oligo(dT)16 as template/primer incubated for 40 mins by pico-green based spectrofluorometric analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID247526 | Inhibitory activity against wild type HIV-1 LAI cell line | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID735082 | Antiviral activity against wild type HIV by cell based assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
| Synthesis and biological evaluation of phosphonate analogues of nevirapine. |
AID1773454 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring Y188L mutant infected in human MT4 cells | | | |
AID279429 | Antiviral activity against HIV1 isolate with RT 103N, 106M mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID299028 | Antiviral activity against HIV1 with reverse transcriptase K103N mutation in CEM cells assessed as inhibition of virus-induced giant cell formation | 2007 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
| Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains. |
AID1352316 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID371899 | Antiviral activity against HIV1 NL4-3 with L100I mutant in human MT4 cells assessed as inhibition of virus-induced cytopathicity after 5 days by multiple round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID663298 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID541150 | Selectivity ratio of EC50 for antiviral activity against 3TC-resistant HIV1 selected after 4 passages to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1249719 | Antiviral activity against HIV1 expressing reverse transcriptase K103N mutant | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID496629 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K20R, V35T, E36D, T39N, V60I, D123N, I135V, S162A, K173T, Q174K, D177E, T200A, Q207E, R211K mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID1352168 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 48 to 96 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Quinoxaline derivatives as new inhibitors of coxsackievirus B5. |
AID279432 | Antiviral activity against HIV1 isolate with RT 181I mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID279510 | Antiviral activity against HIV1 isolate with RT T369I mutation in Hela-JC-53 cells | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID496631 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I,Y181C/V35T, T39M, P119S, D123E, S162A, E169D, K173T, Q174K, D177E, T200A, Q207E, K219N, V245Q, E248D mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID1141966 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1249720 | Antiviral activity against HIV1 expressing reverse transcriptase E138K mutant | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID391225 | Antiviral activity against HIV1 with reverse transcriptase K103N mutant infected in human MT4 cells after 72 hrs in presence of 10% fetal bovine serum | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
| Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses. |
AID348905 | Antiviral activity against drug-resistant HIV1 with reverse transcriptase K103N mutant infected in human MT4 cells assessed as virus-induced cell death by MTT method | 2008 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
| Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies. |
AID541161 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring T66I mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1171592 | Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase K103N-Y181C mutant to EC50 for wild type HIV1 NL4-3 | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID366531 | Inhibition of RNA dependent DNA polymerase activity of HIV1 reverse transcriptase L100I mutant | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID430057 | Selectivity index, CC50 for human MT4 cells to EC50 for HIV1 3B | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
| Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents. |
AID265467 | Antiviral activity against HIV1 3B in MT4 cell line | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide. |
AID366520 | Antiviral activity against HIV1 isolates with reverse transcriptase K103N mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID282735 | Inhibition of HIV1 RT | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity. |
AID576033 | Tmax in healthy human plasma at 400 mg, po measured on day 1 post dose by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID614141 | Antiviral activity against wild type Human immunodeficiency virus 1 3B bearing reverse transcriptase K103N and Y181C double mutation infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17
| Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs. |
AID1155811 | Fold resistance, ratio of EC50 for HIV-1 harboring NNTRI-resistant reverse transcriptase Y181C mutant infected in human MT4 cells to EC50 for wild type HIV-1 NL4-3 infected in human MT4 cells | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID248259 | In vitro inhibitory concentration against HIV K101E mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID1483272 | Inhibition of HIV1 3B reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID104448 | Concentration required to protect the cell against HIV-1 strain IIIB viral cytopathogenicity by 50% in MT-4 cells | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
| 5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series. |
AID1558858 | Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID1574379 | Resistance index, ratio of EC50 for HIV-1 IRLL98 harboring reverse transcriptase M41L, D67N, Y181C, M184V, R211K, and T215Y mutants to EC50 for wild type HIV-1 NL4-3 | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID572181 | Antiviral activity against HIV-1 SM007 harboring NNTRI 103N mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID166708 | Inhibitory activity against RNA | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| Synthesis and biological activities of potential metabolites of the non-nucleoside reverse transcriptase inhibitor efavirenz. |
AID1456308 | Inhibition of HIV1 RES056 reverse transcriptase 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 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. |
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. |
AID1815383 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1653626 | Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) F405A mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID586359 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T66A mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vir | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID222294 | Effect of human plasma protein binding on antiviral efficacy. | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID650540 | Antiviral activity against wild type HIV 1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID443679 | Antiviral activity against HIV with reverse transcriptase Y181C mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID231368 | Ratio of wild type IIIB to that of Y181C HIV-1 induced cytopathogenicity | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
| Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C varia |
AID361904 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/L100I mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID736041 | Inhibition of HIV1 reverse transcriptase p66/p51 V106A mutant after 30 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | | | |
AID1191671 | Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 pre-incubated with compound before enzyme addition using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
| Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs. |
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. |
AID622047 | Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer K103N mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID583864 | Ratio of IC50 for HIV1 HXB2 reverse transcriptase K103N mutant to IC50 for wild type HIV1 reverse transcriptase | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID1316343 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID571984 | Antiviral activity against HIV-1 subtype C V022816 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1304408 | Antiviral activity against HIV-1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID1750720 | Inhibition of HIV-1 p66/p51 reverse transcriptase Y188L mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | | | |
AID247725 | Inhibitory concentration against 181C mutant was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity. |
AID1609103 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 4 days by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID279469 | Antiviral activity against HIV1 isolate with RT 238N mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID88371 | Antiviral activity against P236L mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1773836 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies. |
AID1743635 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID1163233 | Antiviral activity against HIV1 infected in human TZM-bl cells assessed as viral inhibition pre-incubated for 30 mins prior to infection measured after 48 hrs by | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
AID361911 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase L100I mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID347616 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 179D mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID104450 | Concentration required to protect the cell against HIV-2 strain ROD viral cytopathogenicity by 50% in MT-4 cells; NA denotes not active | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
| 5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series. |
AID279413 | Antiviral activity against HIV1 isolate with RT 106A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1750727 | Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase E138K mutant | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID279400 | Antiviral activity against HIV1 isolate with RT 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1186003 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/G190A double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay r | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID1204078 | Antiviral activity against HIV1 infected in human MT4 cells assessed as protection against viral-induced cytopathogenecity after 4 days by MTT method | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
| N-((1,3-Diphenyl-1H-pyrazol-4-yl)methyl)anilines: A novel class of anti-RSV agents. |
AID1873200 | Inhibition of human ABCG2 expressed in dog MDCK-II-BCRP cells mediated pheophorbide A efflux preincubated with PhA followed by compound addition and measured after 60 mins by flow cytometry | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators. |
AID1155808 | Antiviral activity against HIV-1 harboring NNTRI-resistant reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID573981 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for Human immunodeficiency virus 2 EHO | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID632801 | Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT4 cells assessed as inhibition of viral infection | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents. |
AID1212881 | Drug metabolism in microsomes expressing CYP2B6.1 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by HPLC/UV system in presence of Cyt b5 coexpression | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID586909 | Induction of MRP3 activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Interaction potential of etravirine with drug transporters assessed in vitro. |
AID96290 | In vitro antiviral activity against HIV-1 (L100I). | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID1304407 | Inhibition of HIV-1 BH10 recombinant reverse transcriptase K103N mutant expressed in Escherichia coli assessed as incorporation of [32P]GTP into poly(rA)/oligo(dT) as template primer | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID1316333 | Cytotoxicity against human mock-infected MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID269793 | Antiviral activity against HIV1 | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269793 | Antiviral activity against HIV1 | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269793 | Antiviral activity against HIV1 | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID522369 | Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106A mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID663299 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | | | |
AID246299 | Effective concentration of the compound to inhibit HIV-1 mutant L100I replication in HIV-infected MT-4 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1264543 | Cytotoxicity against human CD4-positive T cells | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
| Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance. |
AID1316330 | Antiviral activity against wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID576045 | Fraction unbound in healthy human plasma at 400 mg, po measured on day 1 post dose by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID404606 | Antiviral activity against HIV1 with reverse transcriptase Y181C mutation | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
| Parallel one-pot synthesis and structure-activity relationship study of symmetric formimidoester disulfides as a novel class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID523345 | Antiviral activity against HIV1 with RT connection domain T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID635345 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
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. |
AID1246228 | Cytotoxicity against human MT4 cells | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, cytotoxicity and antimicrobial activity of thiourea derivatives incorporating 3-(trifluoromethyl)phenyl moiety. |
AID650547 | Resistance ratio of EC50 for HIV 1 harboring reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID576044 | Drug concentration in PBMCs of healthy human at 400 mg, po ad for 14 days measured after 24 hrs post last dose by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID82459 | Antiviral activity against K103N strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID586377 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Q148K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID279457 | Antiviral activity against HIV1 isolate with RT 98G, 101E, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1811044 | Antiviral activity against HIV1 IIIB infected human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID1231488 | Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action. |
AID1822280 | Antiviral activity against HIV-1 harboring E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID446257 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with K101E mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
AID1171414 | Cytotoxicity against human MT2 cells assessed as reduction in cell viability by MTT assay | 2014 | ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
| Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers. |
AID83549 | Potency evaluated against NNRTI-Resistant HIV-1 strain Leu100Ile | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
| Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian |
AID586388 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T66K/L74M mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficienc | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1261311 | Cytotoxicity against african green monkey Vero 76 cells assessed as cell viability after 48 to 96 hrs by crystal violet staining method | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
AID330485 | Antiviral activity against HIV1 3B infected in MT4 cells by MTT | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID541163 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92Q mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
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. |
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. |
AID464764 | Antiviral activity against wild type HIV1 infected in human MT2 cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1163254 | Antileishmanial activity against Leishmania infantum MHOM/MA (BE)/67 infected in primary peritoneal mouse macrophages assessed as reduction in parasite burdun | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
AID279463 | Antiviral activity against HIV1 isolate with RT 108I, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID492280 | Selectivity index, CC50 for human MT4 cells to EC50 for wild type HIV1 3B | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy. |
AID279401 | Antiviral activity against HIV1 isolate with RT 181C, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID508795 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V090I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID464766 | Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT2 cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID492284 | Antiviral activity against HIV1 with reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy. |
AID347087 | Inhibition of RNA-dependent DNA polymerase activity of HIV1 reverse transcriptase Y181C mutant | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays. |
AID1316345 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1520060 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID1741395 | Inhibition of reverse transcriptase Y181C mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID279521 | Antiviral activity against wild type HIV1 NL4-3 in Hela-JC53 cells in the presence of 40% human serum after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID279467 | Antiviral activity against HIV1 isolate with RT 106A, 181C mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID302621 | Cytotoxicity against human MT2 cells by MTT assay | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| From docking false-positive to active anti-HIV agent. |
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. |
AID1773828 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies. |
AID1272058 | Half life in human administered as single dose | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry. |
AID366526 | Inhibition of RNA dependent DNA polymerase activity of wild-type HIV1 reverse transcriptase | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID738332 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for wild type HIV1 3B | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs. |
AID440085 | Antiviral activity against HIV1 HXB2 harboring 101E and K103N mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID1171598 | Inhibition of wild type HIV1 reverse transcriptase Y181I mutant assessed as reduction in enzyme activity | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1754638 | Cytotoxicity against mock-infected human MT4 cells incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
AID279459 | Antiviral activity against HIV1 isolate with RT 101H mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID246392 | Effective concentration against human immunodeficiency virus type 1 mutated at 100I+103N | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID556526 | Antiviral activity against Human immunodeficiency virus 1 clone Q9016 harboring K122E, Q145M, I202V, F214L mutation in reverse transcriptase by phenosense assay relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility. |
AID779528 | Antiviral activity against HIV-1 RESO56 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
AID267855 | Antiviral activity against HIV1 IRLL98 in MT4 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
AID508780 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138S mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID88379 | Antiviral activity against V108I mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID557024 | Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase L100I mutant relative to drug-sensitive HIV1 CNDO | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID571969 | Antiviral activity against HIV-1 subtype CRF02_AG V022826 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID576042 | Drug concentration in PBMCs of healthy human at 400 mg, po ad for 14 days measured after 5 hrs post last dose by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID508833 | Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93MW959 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1693801 | Antiviral activity against HIV2 ROD infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C. |
AID1729158 | Antiviral activity against HIV1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID571973 | Antiviral activity against HIV-1 subtype CRF01_AE V022822 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1410397 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site. |
AID508622 | Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG024 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID361923 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/G190A mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4
| DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
AID1705192 | Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID1457064 | Inhibition of HIV1 reverse transcriptase p66 K103N mutant associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintillation counting | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID279494 | Antiviral activity against HIV1 isolate with RT G190A mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1731746 | Inhibition of reverse transcriptase L100I mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID571968 | Antiviral activity against HIV-1 subtype CRF02_AG V022825 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1743630 | Antiviral activity against HIV1 harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID1520061 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B harbouring NNRTI K103N mutant infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID1141972 | Ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID441309 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with K103N mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 1: design and initial optimisation of a novel template. |
AID441315 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with P236L mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 1: design and initial optimisation of a novel template. |
AID508829 | Antiviral activity against Human immunodeficiency virus 1 subtype B isolate JR-CSF infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID541168 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID443701 | Antiviral activity against HIV with reverse transcriptase K103N/Y181C double mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID519888 | Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID1126510 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to IC50 for HIV1 3B infected in human MT4 cells | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
| Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1069708 | Cytotoxicity against human MT4 cells assessed as cell viability | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
| Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID571987 | Antiviral activity against HIV-1 subtype C V022831 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID448403 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with P236L mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 3: optimisation of physicochemical properties. |
AID457961 | Inhibition of HIV1 reverse transcriptase K103N mutant by RNA-dependent DNA polymerase activity assay | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
| Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID573987 | Antiviral activity against Protease inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID508633 | Cytotoxicity against human MT4 cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID519870 | Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID1390710 | Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
| First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain. |
AID1773457 | Resistance factor, ratio of EC50 for HIV1 harboring L1001 mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells | | | |
AID282740 | Inhibition of HIV1 RT Y188L mutant | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity. |
AID572186 | Antiviral activity against HIV-1 SM034 harboring NNTRI 188L mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID443689 | Antiviral activity against HIV with reverse transcriptase K101E/Y181C/G190A mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID105324 | Inhibition of Efavirenz resistant HIV-1 (K103N-Y181C) induced cytopathicity in MT-4 cells. | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations. |
AID519856 | Antiviral activity against pseudotype HIV1 NL-RLuc infected in human MT2 cells measured on day 5 postinfection by luciferase reporter gene assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID541175 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring G140S and Q148H mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID440083 | Antiviral activity against HIV1 HXB2 harboring 227C mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID576034 | Tmax in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID1155815 | Inhibition of HIV-1 recombinant NNTRI-resistant reverse transcriptase Y181I mutant assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:1 | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID517497 | Antiviral activity against HIV1 harboring reverse transcriptase V106A mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses. |
AID490370 | Antiviral activity against HIV1 expressing reverse transcriptase K103N/L100I double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses. |
AID523478 | Antiviral activity against HIV1 with RT connection domain G190A/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID1773837 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies. |
AID1171584 | Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 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. |
AID1261317 | Antiviral activity against Human poliovirus 1 Sabin infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity by plaque reduction assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
AID1316329 | Inhibition of recombinant wild type HIV1 reverse transcriptase using DIG-dUTP/biotin-dUTP/dTTP assessed as suppression of biotin-dUTP incorporation after 1 hr by ELISA | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID519883 | Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID1884220 | Antiviral activity against HIV-1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID279476 | Antiviral activity against HIV1 isolate with RT 101N, 103N mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID82469 | Antiviral activity against V106A/Y181C strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1126509 | Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
| Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1574373 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID263515 | Antiviral activity against HIV1 I135T mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2. |
AID508775 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1457072 | Effect on fizz mRNA levels in C57BL/6 mouse BV2 cells at 1000 nM after 24 hrs by RT-PCR assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID584029 | Inhibition of HIV1 histidine-tagged reverse transcriptase E233V mutant activity by primer extension assay | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID1191669 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
| Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs. |
AID573988 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for Reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID738335 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs. |
AID571970 | Antiviral activity against HIV-1 subtype CRF02_AG V022830 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID443692 | Antiviral activity against HIV with reverse transcriptase MDRC4 mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID726437 | Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase K103N and Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
| Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency. |
AID519865 | Antiviral activity against HIV1 subtype B-NL4-3 infected in 3 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID541153 | Selectivity ratio of EC50 for antiviral activity against EFV-resistant HIV1 selected after 7 passages to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID541151 | Selectivity ratio of EC50 for antiviral activity against 3TC-resistant HIV1 selected after 8 passages to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1552563 | Antiviral activity against HIV1 V13-03413B infected in human LC5 cells expressing DsRed1 reporter gene assessed as inhibition of viral infection measured after 48 hrs post infection by reporter gene based luminescence assay | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
| Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline. |
AID571980 | Antiviral activity against HIV-1 subtype B V022812 harboring NNRTI V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID519892 | Selectivity ratio of EC50 for 0.05 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.05 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID750863 | Antiviral activity against HIV1 infected in human 293T cells assessed as inhibition of viral replication incubated for 15 mins prior to infection measured after 48 hrs by luciferase reporter gene assay | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6
| Diterpenoids with diverse skeletons from the roots of Euphorbia micractina. |
AID1171596 | Inhibition of wild type HIV1 reverse transcriptase L100I mutant assessed as reduction in enzyme activity | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1069124 | Antiviral activity against HIV harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
| Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses. |
AID392513 | Antiviral activity against HIV1 | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
| Unified QSAR approach to antimicrobials. 4. Multi-target QSAR modeling and comparative multi-distance study of the giant components of antiviral drug-drug complex networks. |
AID371904 | Antiviral activity against HIV1 NL4-3 with K103N/L100I double mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID368555 | Inhibition of wild type HIV1 reverse transcriptase-mediated RNA-dependent DNA polymerase activity assessed as [3H]dTTP incorporation by cell free-based scintillation counting | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID246349 | Effective concentration against human immunodeficiency virus type 1 mutated at 103N | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID1212916 | Drug metabolism in microsomes expressing CYP2B6.1 (unknown origin) assessed as intrinsic clearance for enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in absence of Cyt b5 coexpression | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID663311 | Resistance ratio of ID50 for HIV1 reverse transcriptase K103N mutant to ID50 HIV1 wild type reverse transcriptase | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID735080 | Ratio of EC50 for HIV harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
| Synthesis and biological evaluation of phosphonate analogues of nevirapine. |
AID1155804 | Antiviral activity against wild type HIV-1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID1220376 | Drug metabolism in human liver microsomes assessed as formation of metabolites with retention time of 1.92 mins at 20 uM by UPLC-MS/MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
| Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid. |
AID573257 | Antiviral activity against HIV1 infected in children assessed as decrease in viral burden at 14.4 mg/kg once daily measured after 3 months | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID279321 | Inhibition of reverse transcriptase activity in HIV1 infected HeLa-MAGI cells at 37 deg C after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification. |
AID541130 | Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RTM184V mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID151310 | percentage in tissue culture medium | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID586472 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E138K/Q148H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID253495 | Dose required to inhibit HIV-1 reverse transcriptase activity ( L100I mutant) by 50% | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
| Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation. |
AID576030 | Volume of distribution in healthy human plasma at 400 mg, po measured on day 1 post dose by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID248841 | Inhibitory concentration against human immunodeficiency virus type 1 (with G190A resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2. |
AID1761009 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID279500 | Antiviral activity against HIV1 isolate with RT V106I mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID81628 | Antiviral activity was evaluated against wild-type HIV-1 virus | 2001 | Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9
| Synthesis and evaluation of efavirenz (Sustiva) analogues as HIV-1 reverse transcriptase inhibitors: replacement of the cyclopropylacetylene side chain. |
AID328841 | Inhibition of human MRP1 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence by CMFDA assay | 2007 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
| Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors. |
AID572183 | Antiviral activity against HIV-1 SM024 harboring NNTRI 190A mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1443663 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID508786 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V108I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID572187 | Antiviral activity against HIV-1 SM051 harboring NNTRI 100I and 103N mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1435513 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase K103N mutant | | | |
AID1152373 | Cytotoxicity against human MT4 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
| Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1171583 | Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID573986 | Antiviral activity against non nucleoside reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID1435514 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase Y181C mutant | | | |
AID523486 | Antiviral activity against HIV1 with RT connection domain L100I/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID263514 | Antiviral activity against HIV1 V106A mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2. |
AID1443669 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID366522 | Antiviral activity against HIV1 isolates with reverse transcriptase Y181C mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID586480 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Q148R/N155H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID105707 | Anti-HIV-1 activity against Y188L strain was determined in MT-4 cells by the MTT method | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
| 3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1653627 | Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) K358A mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID1815388 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID572184 | Antiviral activity against HIV-1 SM026 harboring NNTRI 103N and 181C mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1884540 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID1077222 | Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
AID1572523 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
AID557046 | Antiviral activity against HIV1 clade C harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1773829 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies. |
AID586484 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase V72I/F121Y/T125K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunode | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID605183 | Antiviral activity against HIV1 R8 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as concentration required to inhibit >95% viral spread in presence of 10% FBS | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif. |
AID632797 | Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT2 cells assessed as inhibition of viral infection | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents. |
AID246203 | Concentration required to achieve 50% protection of infected MT-4 cells from Y181C-HIV-1 strain | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives. |
AID446238 | Antiviral activity against HIV RF infected in human SupT1 cells | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
AID1141967 | Antiviral activity against HIV1 harboring reverse transcriptase L1001 mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1455949 | Antiviral activity against VSV pseudotyped HIV1 infected in SupT1 cells after 48 hrs by luciferase reporter gene assay | 2017 | Journal of natural products, 02-24, Volume: 80, Issue:2
| Griseofulvin Derivative and Indole Alkaloids from Penicillium griseofulvum CPCC 400528. |
AID1754640 | Antiviral activity against wild type HIV-2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured after 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
AID279392 | Antiviral activity against HIV1 isolate with RT 100I, 103N mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID576046 | Fraction unbound in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID446408 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with V108I mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
AID1736358 | Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase L100I/K103N double mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hr | | | |
AID269688 | Antiviral activity against HIV1 NNTRI resistant K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269688 | Antiviral activity against HIV1 NNTRI resistant K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269688 | Antiviral activity against HIV1 NNTRI resistant K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID518737 | Inhibition of DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by gel-based primer extension assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID247726 | Inhibitory concentration against 188L mutant was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity. |
AID473114 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
| Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV. |
AID267856 | Antiviral activity against HIV1 K103N mutant in MT4 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
AID735083 | Inhibition of HIV reverse transcriptase | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
| Synthesis and biological evaluation of phosphonate analogues of nevirapine. |
AID492281 | Antiviral activity against wild type HIV1 LAI infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy. |
AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID519893 | Selectivity ratio of EC50 for 0.005 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by MTS assay to EC50 for 0.005 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID82458 | Antiviral activity against K101E strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1773460 | Resistance factor, ratio of EC50 for HIV1 harboring Y188L mutant mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells | | | |
AID465419 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID269796 | Antiviral activity against HIV1 F227L mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269796 | Antiviral activity against HIV1 F227L mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269796 | Antiviral activity against HIV1 F227L mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1705183 | Antiviral activity against HIV-1 NL4-3 infected in human MT-4 cells assessed as virus induced cytopathic effect by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID573256 | Apparent oral clearance in HIV-1 infected children at 14.4 mg/kg, po administered once daily by HPLC | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID508765 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M236L mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID541160 | Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 9 passages to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID517494 | Selectivity ratio of IC50 for wild type HIV1 in presence of 40% human serum to IC50 for wild type HIV1 in presence of 10% FBS | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses. |
AID1736347 | Inhibition of HIV-1 reverse transcriptase RNA-dependent DNA polymerase activity assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT) as template/primer incubated for 1 hr followed by transferring into streptavidin plate for 1 hr by absorba | | | |
AID360704 | Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA/DNAM duplex primed substrate by scintillation proximity assay | 2007 | The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
| HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro. |
AID517496 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses. |
AID1520057 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID1443668 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID368560 | Antiviral activity against HIV1 reverse transcriptase Y181C mutant infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID1705185 | Selectivity ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV-1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID1596756 | Inhibition of recombinant wild-type HIV1 3B reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(rA)/oligo(dT)16 as template primer incubated for 1 hr followed by the addition of (DIG)-dUTP and biotin-labeled dNTPs by ELISA | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains. |
AID263519 | Antiviral activity against HIV1 Y181C mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2. |
AID1446873 | Inhibition of wild-type HIV1 RT associated RNA dependent DNA polymerase activity using poly(A) template/oligo(dT) primer after 30 mins by picogreen staining based method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Natural product-inspired esters and amides of ferulic and caffeic acid as dual inhibitors of HIV-1 reverse transcriptase. |
AID523355 | Antiviral activity against HIV1 with RT connection domain Y181C/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID361925 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/Y181C mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1503175 | Antiviral activity against VSV-G pseudotyped HIV1 infected in human SupT1 cells at 100 uM after 48 hrs by luciferase reporter gene assay relative to control | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10
| Metabolites from the Plant Endophytic Fungus Aspergillus sp. CPCC 400735 and Their Anti-HIV Activities. |
AID586380 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase S153F mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1191400 | Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
| Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1410481 | Inhibition of wild-type HIV1 3B reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
AID584239 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase Y181C, V179V/D mutant derived from 17 days viral passages with lersivirine infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID1815386 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID248012 | In vitro inhibitory concentration against HIV LAI cell line | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID1761007 | Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability measured after 1 day by CytoTox-Glo assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID232750 | Selectivity index is the ratio between CC50 for MT-4 cells and IC50 against HIV-1 infection | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
| 5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series. |
AID293174 | Antiviral activity against HIV1 LAI assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method | 2007 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
| Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity. |
AID557042 | Antiviral activity against HIV1 isolate R8 harboring wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID527375 | Antiviral activity against wild type HIV1 NL4-3 infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID222921 | percentage in human serum; value ranges from -0.2-0.5 | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID94447 | Inhibitory concentration against wild-type virus K103N and HIV-1 RT mutant in a whole cell antiviral assay | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
| 3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors. |
AID313194 | Antiviral activity against HIV1 K103N/Y181C mutant | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Synthesis and antiviral activity of new dimeric inhibitors against HIV-1. |
AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1
| Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID1261310 | Cytotoxicity against BHK cells assessed as cell viability after 48 to 96 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
AID1552554 | Antiviral activity against HIV1 HXB2 pseudovirus infected in human TZM-bl cells assessed as inhibition of viral infection incubated for 20 mins prior to infection and measured after 48 hrs by bright Glo-luciferase reporter gene assay | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
| Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline. |
AID431622 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
| Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID622057 | Ratio of Ki for HIV1 RT p66/p66 homodimer G190A mutant to Ki for wild-type HIV1 RT p66/p66 homodimer | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID440078 | Antiviral activity against HIV1 HXB2 harboring 106A mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID1407647 | Therapeutic index, ratio of CC50 for human CEM-GFP cells to IC50 for HIV-1 NL4-3 infected in human CEM-GFP cells | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors. |
AID663309 | Inhibition of HIV1 recombinant reverse transcriptase V106A mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT) | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID1335218 | Antiviral activity against wild-type HIV-1 NL4-3 harboring vesicular stomatitis virus glycoprotein infected in HEK293T cells pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID279445 | Antiviral activity against HIV1 isolate with RT 101E, 103N mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1185997 | Antiviral activity against HIV1 harboring reverse transcriptase L1001/K103N double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay r | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID1376906 | Antiviral activity against VSV-G pseudotyped HIV1 infected in human SupT1 cells after 48 hrs by firefly luciferase reporter gene assay | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6
| Stachybotrysins A-G, Phenylspirodrimane Derivatives from the Fungus Stachybotrys chartarum. |
AID1335206 | Ratio of IC50 for HIV-1 NL4-3 harboring RT-Y181C mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID1435506 | Antiviral activity against HIV1 expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | | | |
AID508638 | Antiviral activity against Human immunodeficiency virus 1 subtype F1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID441303 | Inhibition of wild type HIV reverse transcriptase in presence of poly(rA) 300 template, (dT) 16 primer | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 1: design and initial optimisation of a novel template. |
AID1888702 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
AID279512 | Antiviral activity against HIV1 isolate with RT V106I, Y181C, F227L mutation in Hela-JC-53 cells | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID94443 | Potency of second-generation NNRTIs against Mutant HIV-1 K103N | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID279420 | Antiviral activity against HIV1 isolate with RT 190S mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1249718 | Antiviral activity against HIV1 expressing reverse transcriptase L100I mutant | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID519885 | Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID622054 | Ratio of Ki for HIV1 RT p66/p66 homodimer K103N mutant to Ki for wild-type HIV1 RT p66/p66 homodimer | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID1596753 | Antiviral activity against HIV-1 3B harboring reverse transcriptase RES056 mutant infected in MT4 cells measured after 5 days by MTT assay | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains. |
AID586471 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E138A/Q148R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1483278 | Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID1410484 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B reverse transcriptase infected in human MT4 cells | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
AID1574389 | Resistance index, ratio of ID50 for recombinant HIV-1 His-tagged reverse transcriptase p66/p51 Y181I mutant to ID50 for recombinant wild type HIV-1 reverse transcriptase His-tagged p66/p51 | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID1741400 | Inhibition of recombinant HIV-1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye based fluorescence assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID490371 | Antiviral activity against HIV1 expressing reverse transcriptase G190A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses. |
AID508627 | Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR019 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1741393 | Inhibition of reverse transcriptase L100I mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID1761017 | Antiviral activity against HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID779525 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
AID83551 | Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr181Cys | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
| Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian |
AID1535526 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells | 2019 | Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
| Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs. |
AID106057 | Inhibitory activity against 103N strain and 181C strain of HIV-I in MT-4 cells | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. |
AID347613 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 103N mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID430056 | Cytotoxicity against human MT4 cells after 5 days | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
| Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents. |
AID198399 | Tested for inhibitory concentration against HIV-1 non-nucleoside reverse transcriptase | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
| 3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors. |
AID1822276 | Antiviral activity against HIV-1 harboring RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID1705191 | Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID266345 | Inhibition of wild type HIV1 reverse transcriptase in 293T cells | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity. |
AID1443662 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID1171590 | Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4-3 | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID347609 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 190S mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID650544 | Antiviral activity against HIV 1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID1761016 | Antiviral activity against HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID588211 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1
| Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID1407642 | Inhibition of recombinant HIV-1 reverse transcriptase RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)16 as template/primer preincubated for 5 to 10 mins followed by template/primer addition and measured after 16 hrs by colorimetric assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors. |
AID586476 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase G140S/Q148H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1373160 | Inhibition of reverse transcriptase Y188L mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Structural optimization of N |
AID584241 | Ratio of EC50 for wild type HIV1 NL4-3 to EC50 for HIV1 NL4-3 harboring reverse transcriptase V179V/D mutant | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID299031 | Antiviral activity against HIV1 with reverse transcriptase Y188H mutation in CEM cells assessed as inhibition of virus-induced giant cell formation | 2007 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
| Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains. |
AID1157585 | Antiviral activity against zidovudine-resistant HIV1 harboring RT 67N, 70R, 215F, 219Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID279484 | Antiviral activity against HIV1 isolate with RT K103N-P225H mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID757623 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1186327 | Cytotoxicity against mock-infected human MT4 cells after 96 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
| Antiviral activity of benzimidazole derivatives. III. Novel anti-CVB-5, anti-RSV and anti-Sb-1 agents. |
AID1060630 | Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs. |
AID232055 | Selectivity index (Ratio of CC50/EC50). | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations. |
AID198912 | Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution L1001 | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. |
AID586902 | Activity at MRP2 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Interaction potential of etravirine with drug transporters assessed in vitro. |
AID105905 | Effective dose required to achieve protection of MT-4 cells from Y181C HIV-1 induced cytopathogenicity | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
| Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C varia |
AID347621 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 181C mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID1171580 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1155818 | Fold resistance, ratio of ID50 for HIV-1 recombinant NNTRI-resistant reverse transcriptase Y181I mutant to ID50 for wild type HIV-1 recombinant reverse transcriptase | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID572185 | Antiviral activity against HIV-1 SM030 harboring NNTRI 100I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1503177 | Cytotoxicity against human SupT1 cells assessed as decrease in cell viability after 48 hrs by CCK-8 assay | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10
| Metabolites from the Plant Endophytic Fungus Aspergillus sp. CPCC 400735 and Their Anti-HIV Activities. |
AID267645 | Antiviral activity against wild type HIV1 virus | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID293555 | Antiviral activity against wild type HIV1 LAI infected in MT4 cells by EGFP based replication assay | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5
| Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains. |
AID1741394 | Inhibition of reverse transcriptase K103N mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID293562 | Antiviral activity against HIV1 LAI with RT F227C mutation in MT4 cells by EGFP based replication assay | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5
| Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains. |
AID248881 | Inhibitory concentration against human immunodeficiency virus type 1 (with V106A/Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2. |
AID685333 | Cytotoxicity against mock-infected human MT4 cells by MTT assay | 2012 | Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors. |
AID1059142 | Inhibition of recombinant HIV1 reverse transcriptase using poly rA:dT as template/primer after 1 hr by ELISA | 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. |
AID1705195 | Inhibition of RNA-dependent DNA polymerase activity of recombinant HIV-1 p66/p51 reverse transcriptase K103N mutant assessed as inhibition of [3H]dTTP incorporation using poly(rA)/oligo(dT) as templates incubated for 15 mins by MicroBeta scintillation cou | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID1637398 | Antiviral activity against human HIV-1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID1057037 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B infected in MT4 cells | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
| Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs. |
AID226250 | Y181C/WTIIIB ratio of the compound | 2001 | Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
| Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1574384 | Inhibition of recombinant wild type HIV-1 His-tagged reverse transcriptase p66/p51 expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysis | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID246350 | Effective concentration against human immunodeficiency virus type 1 mutated at 181C | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID94313 | Antiviral activity toward K103N mutant HIV-1 virus as protein binding adjusted (PB adj). | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID313191 | Antiviral activity against HIV1 HTLV-3B | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Synthesis and antiviral activity of new dimeric inhibitors against HIV-1. |
AID576050 | Effect on P-gp activity in PBMCs isolated from healthy human receiving compound dose at 400 mg, po qd for 14 days by rhodamine -123 efflux assay | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID1773444 | Selectivity ratio of CC50 for human MT4 cells to IC50 for HIV1 RES056 infected in MT4 cells | | | |
AID527563 | Antiviral activity against HIV1 NL4-3 containing reverse transcriptase Y181C mutation infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1335207 | Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID1754646 | Antiviral activity against HIV1 harboring RT F227L/V106A mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
AID440075 | Antiviral activity against HIV1 HXB2 harboring Y188L mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID1705187 | Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID586470 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase F121Y/T125K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID541129 | Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RTK65R mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
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. |
AID1880376 | Antiviral activity against HIV-1 IIIB harboring reverse transcriptase L1001 mutant infected in human MT4 cells by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Structure-Based Discovery of Novel NH |
AID1304399 | Inhibition of HIV-1 BH10 recombinant reverse transcriptase expressed in Escherichia coli assessed as incorporation of [32P]GTP into poly(rC)/oligo(dG) as template primer | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID779526 | Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
AID622056 | Ratio of Ki for HIV1 RT p66/p66 homodimer Y188L mutant to Ki for wild-type HIV1 RT p66/p66 homodimer | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID1880377 | Antiviral activity against HIV-1 IIIB harboring reverse transcriptase K103N mutant infected in human MT4 cells by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Structure-Based Discovery of Novel NH |
AID371907 | Antiviral activity against HIV1 NL4-3 with Y181L mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID448400 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with V106A mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 3: optimisation of physicochemical properties. |
AID1261341 | Antiviral activity against VSV | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
AID1352320 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID371908 | Antiviral activity against HIV1 NL4-3 with V108I mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID518738 | Inhibition of DNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by gel-based primer extension assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID1572521 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | | | |
AID1248224 | Selectivity index, ratio of CC50 for uninfected human MT4 cells to EC50 for wild type HIV 1 3B infected in human MT4 cells | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
| A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities. |
AID1298248 | Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
AID1264542 | Aqueous solubility of compound | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
| Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance. |
AID1304404 | Selectivity index, ratio of CC50 for cytotoxicity against mock-infected human CEM-SS cells to EC50 for antiviral activity against HIV-1 RF | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID248878 | Inhibitory concentration against human immunodeficiency virus type 1 (with K103N/G190A resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2. |
AID1155817 | Fold resistance, ratio of ID50 for HIV-1 recombinant NNTRI-resistant reverse transcriptase K103N mutant to ID50 for wild type HIV-1 recombinant reverse transcriptase | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID717260 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs. |
AID1410486 | Inhibition of wild-type HIV1 reverse transcriptase infected in human MT4 cells assessed as reduction in biotin-dUTP incorporation | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
AID605175 | Antiviral activity against HIV1 R8 harboring wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral spread in presence of 10% fetal bovine serum | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif. |
AID642208 | Cytotoxicity against human MT4 cells after 96 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Quinoline tricyclic derivatives. Design, synthesis and evaluation of the antiviral activity of three new classes of RNA-dependent RNA polymerase inhibitors. |
AID1186004 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/V108I double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID361916 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V108I mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1583019 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
| Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel. |
AID1653631 | Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) K358L mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID246352 | Effective concentration against human immunodeficiency virus type 1 mutated at 227C | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID457960 | Inhibition of HIV1 reverse transcriptase Y181I mutant by RNA-dependent DNA polymerase activity assay | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
| Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID248493 | In vitro inhibitory concentration value against HIV K103N and Y181C mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID632800 | Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral infection | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents. |
AID518735 | Inhibition of RNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by filter-based filtration assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID1357799 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase F227L/V106A mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID496634 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I,A98G/V35T, E36D, T39K, S48A, I50V, V60I, S68G, I135V, S162A, K173T, Q174K, D177E, G196E, T200A, E203G, Q207D, R211K, Q222P mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID1171581 | Antiviral activity against HIV1 3B infected in human CEM cells assessed as protection against virus-induced cytopathicity by giant cell formation assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID293179 | Antiviral activity against HIV1 RT 100I/103N mutant assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method | 2007 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
| Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity. |
AID198230 | Inhibitory activity against wild-type HIV-1 reverse transcriptase | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase. |
AID541155 | Selectivity ratio of EC50 for antiviral activity against APV-resistant HIV1 selected after 4 passages to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID440664 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
| Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants. |
AID492283 | Antiviral activity against HIV1 with reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy. |
AID347620 | Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 188H mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. |
AID446258 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with P236L mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
AID88384 | Antiviral activity against wild-type HIV-1 in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1357783 | Antiviral activity against wild-type HIV-1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID1161103 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors. |
AID584238 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase K103N, V108V/I mutant derived from 10 days viral passages with lersivirine infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID279416 | Antiviral activity against HIV1 isolate with RT 179A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1552578 | Selectivity ratio of IC50 for HIV1 V13-03413B infected in human LC5 cells to IC50 for HIV1 LAI infected in human LC5 cells | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
| Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline. |
AID441312 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with V106A mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 1: design and initial optimisation of a novel template. |
AID279501 | Antiviral activity against HIV1 isolate with RT Y181C mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1077218 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
AID1503176 | Antiviral activity against VSV-G pseudotyped HIV1 infected in human SupT1 cells after 48 hrs by luciferase reporter gene assay | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10
| Metabolites from the Plant Endophytic Fungus Aspergillus sp. CPCC 400735 and Their Anti-HIV Activities. |
AID248844 | Inhibitory concentration against human immunodeficiency virus type 1 (with V108I resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2. |
AID583849 | Inhibition of HIV1 reverse transcriptase activity by primer extension assay | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1231489 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action. |
AID1435518 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase mutant | | | |
AID572188 | Antiviral activity against HIV-1 SM052 harboring NNTRI 101E and 103N mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1773440 | Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | | | |
AID302265 | Inhibition of HIV1 reverse transcriptase Y188L mutant | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID1754643 | Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
AID522372 | Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106A/V179D mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID1731750 | Inhibition of reverse transcriptase E138K mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID1191670 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
| Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs. |
AID586908 | Induction of MRP1 activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Interaction potential of etravirine with drug transporters assessed in vitro. |
AID519887 | Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID1335202 | Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/G190A double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID1326647 | Inhibition of reverse transcriptase Y181C mutant in HIV-1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by cell titer glo based luciferase reporter gene assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1. |
AID1275543 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID1888701 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
AID82468 | Antiviral activity against V106A strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1391088 | Inhibition of HIV1 reverse transcriptase K103N/Y181C double mutant using poly (A)/oligo (dT)15 as template/primer assessed as decrease in biotin-dUTP incorporation after 1 hr by ELISA | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID557067 | Plasma protein binding in HIV1 infected patient | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1594858 | Half life in human serum at 600 mg, qd | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic. |
AID248260 | In vitro inhibitory concentration against HIV K103N mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID736439 | Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant after 30 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID397178 | Ratio of EC50 for HIV1 3B expressing reverse transcriptase Y181C mutant to EC50 for HIV1 3B | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5
| Parallel synthesis, molecular modelling and further structure-activity relationship studies of new acylthiocarbamates as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1572527 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
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. |
AID586468 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T97A/N155H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficien | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID361908 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID105906 | Effective dose required to achieve protection of MT-4 cells from wild type IIIB HIV-1 induced cytopathogenicity | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
| Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C varia |
AID541173 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E138K and Q148K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID583842 | Ratio of IC50 for HIV1 reverse transcriptase Y181I, Y188L mutant to IC50 for wild type HIV1 reverse transcriptase | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID496628 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K20R, V35T, E36A, T39D, V60I, I135V, T139I, K173A, Q174K, T200E, Q207A, R211K, F214L mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID508828 | Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92RW020 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1520058 | Antiviral activity against HIV1 3B harbouring NNRTI K103N mutant infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID1357788 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID371910 | Antiviral activity against HIV1 NL4-3 with K103N mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID779527 | Antiviral activity against HIV-2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
AID523352 | Antiviral activity against HIV1 with RT connection domain K103N/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID1763899 | Antiviral activity against HIV-1 IIIB harboring RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID1185994 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID246786 | Concentration required to reduce the amount of p24 by 90% in C8166 cells infected with an efavirenz-resistant strain EFVR | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives. |
AID1572524 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
AID492285 | Antiviral activity against HIV1 with reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy. |
AID299024 | Cytotoxicity against MT4 cells assessed as reduction of cell viability | 2007 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
| Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains. |
AID199102 | Inhibitory concentration against wild-type reverse transcriptase of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1636927 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against viral infection by MTT method | 2016 | Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
| Computer-aided discovery of anti-HIV agents. |
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. |
AID298088 | Inhibition of HIV1 RT K103N mutant | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. |
AID1565100 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID279514 | Antiviral activity against HIV1 isolate with RT V106I, D123G, Y181C, F227L mutation in Hela-JC-53 cells | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID586906 | Inhibition of BCRP activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Interaction potential of etravirine with drug transporters assessed in vitro. |
AID1212886 | Drug metabolism in microsomes expressing CYP2B6.6 (unknown origin) assessed as intrinsic clearance for enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in presence of Cyt b5 coexpression | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID1884541 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID1882469 | Antiviral activity against HIV-1 harboring Y181C mutant infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors. |
AID279492 | Antiviral activity against HIV1 isolate with RT K103N-F227L mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID766432 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
| Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility. |
AID576043 | Drug concentration in PBMCs of healthy human at 400 mg, po measured after 24 hrs on day 1 post dose by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID443687 | Antiviral activity against HIV with reverse transcriptase K103N/P225H double mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID443693 | Antiviral activity against HIV with reverse transcriptase CNDO mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID698305 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1373156 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Structural optimization of N |
AID663310 | Inhibition of HIV1 recombinant reverse transcriptase Y188L mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT) | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID267863 | Inhibition of HIV1 reverse transcriptase Y181I mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
AID416431 | Antiviral activity against HIV1 bearing VSV envelope infected in human HeLa CD4 cells coexpressing LTR/beta-Gal gene assessed as reduction in virus-induced beta-galactosidase reporter gene activity after 72 hrs by single-cycle infection assay | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Identification and characterization of UK-201844, a novel inhibitor that interferes with human immunodeficiency virus type 1 gp160 processing. |
AID573252 | AUC (0 to t) in HIV-1 infected children at 10 to 15 mg/kg, po administered once daily by HPLC | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID360705 | Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA PPT primed substrate by scintillation proximity assay | 2007 | The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
| HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro. |
AID269795 | Antiviral activity against HIV1 E138K mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269795 | Antiviral activity against HIV1 E138K mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269795 | Antiviral activity against HIV1 E138K mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID623217 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID1348215 | Antiviral activity against HIV1 NL4-3 infected in human MT2 cells measured after 72 hrs post infection by fluorAce beta-galactosidase reporter gene assay | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12
| Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities. |
AID1198748 | Inhibition of HIV1 reverse transcriptase-associated DNA polymerase-independent RNase H activity after 1 hr | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase. |
AID508657 | Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF02 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1357786 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID573255 | Apparent oral clearance in HIV-1 infected children at 13.3 mg/kg, po administered once daily by HPLC | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID738331 | Cytotoxicity against mock-infected human MT4 cells assessed as cell viability after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs. |
AID523480 | Antiviral activity against HIV1 with RT connection domain G190S/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID416756 | Antiviral activity against HIV1 with reverse transcriptase K103N mutation in human CEM cells assessed as protection against virus-induced cytopathicity | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus. |
AID476470 | Antiviral activity against HIV1 reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral replication by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
| Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives. |
AID1811036 | Anti-viral activity against HIV1 harboring RT Y181C mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID246348 | Effective concentration against human immunodeficiency virus type 1 mutated at 100I | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID267858 | Antiviral activity against HIV1 Y188L mutant in MT4 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
AID279406 | Antiviral activity against HIV1 isolate with RT 103N, 238T mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1275544 | Antiviral activity against HIV1 3B expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID572175 | Antiviral activity against HIV-1 subtype F V029522 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID96293 | Potency of second-generation NNRTIs against Mutant HIV-1 sL100I | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID248843 | Inhibitory concentration against human immunodeficiency virus type 1 (with V106A resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2. |
AID523351 | Antiviral activity against HIV1 with RT connection domain K103N/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID605182 | Antiviral activity against HIV1 R8 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral spread in presence of 10% fetal bovine serum | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif. |
AID1157597 | Antiviral activity against HIV1 MP582 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID279396 | Antiviral activity against HIV1 isolate with RT 103N, 225H mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1152372 | Antiviral activity against HIV1 RES056 harboring RT K103N,Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
| Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1882470 | Antiviral activity against HIV-1 harboring K103N/Y181C mutant infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors. |
AID1352169 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 3 to 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Quinoxaline derivatives as new inhibitors of coxsackievirus B5. |
AID1743628 | Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID1185990 | Antiviral activity against wild type HIV1 infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID573476 | Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5512 by cell based assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID293177 | Antiviral activity against HIV1 RT 188L mutant assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method | 2007 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
| Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity. |
AID361907 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase Y181C mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1286669 | Antiviral activity against HIV1 BH10 harboring wild type reverse transcriptase infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor. |
AID279415 | Antiviral activity against HIV1 isolate with RT 101E, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1767120 | Antiviral activity against HIV1 NL4-3 VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of early stage viral production at 10 uM measured after 48 hrs by luciferase assay relative to control | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase. |
AID586364 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E92V mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vir | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
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. |
AID1483274 | Inhibition of HIV1 3B reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID246556 | Concentration required for 50% protection of infected MT-4 cells from wtIIIB-HIV-1-induced cytopathogenicity was determined by the MTT method | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives. |
AID586907 | Induction of ABCB1 activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Interaction potential of etravirine with drug transporters assessed in vitro. |
AID508778 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179E mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1357791 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID517499 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/L100I double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses. |
AID313192 | Antiviral activity against efavirenz-resistant HIV1 | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Synthesis and antiviral activity of new dimeric inhibitors against HIV-1. |
AID519966 | Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells by phenosense assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | | | |
AID726439 | Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
| Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency. |
AID370729 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 V179D mutant expressed in Escherichia coli JM109 | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
AID443697 | Antiviral activity against HIV with reverse transcriptase Y188L mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID1705196 | Inhibition of RNA-dependent DNA polymerase activity of recombinant HIV-1 p66/p51 reverse transcriptase Y188L mutant assessed as inhibition of [3H]dTTP incorporation using poly(rA)/oligo(dT) as templates incubated for 15 mins by MicroBeta scintillation cou | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID1326645 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B reverse transcriptase infected in human MT4 cells | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1. |
AID1822274 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID592539 | Selectivity index, CC50 for human CEM cells to IC50 for HIV1 3B | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide. |
AID1888690 | Antiviral activity against HIV1 3B infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
AID1637400 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring K103N mutant infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID649490 | Inhibition of ribonuclease H activity of Human immunodeficiency virus 1 reverse transcriptase Tyr181Cys mutant | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach. |
AID1705184 | Cytotoxicity against human MT-4 cells assessed as reduction in cell viability by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID269805 | Antiviral activity against HIV1 Y181S mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269805 | Antiviral activity against HIV1 Y181S mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269805 | Antiviral activity against HIV1 Y181S mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1435507 | Antiviral activity against HIV1 expressing reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | | | |
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. |
AID1249724 | Inhibition of HIV1 reverse transcriptase p66/p51 assessed as inhibition of biotin-dUTP incorporation using poly (rA)/oligo(dT)16 as template/primer incubated for 40 mins | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID522371 | Antiviral activity against recombinant HIV1 harboring reverse transcriptase V179D mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID1212901 | Drug metabolism in human liver microsomes harboring CYP2B6*6/*6 genotype assessed as intrinsic clearance for CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation measured per mg protein after 15 mins by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID1155806 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 NL4-3 infected in human MT4 cells | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID257163 | Inhibition of wild type HIV1 reverse transcriptase by [3H]dTTP poly(rA)/oligo(dT) incorporation | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
| Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity. |
AID557051 | Antiviral activity against PI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID583846 | Ratio of IC50 for HIV1 reverse transcriptase V106A, F227L mutant to IC50 for wild type HIV1 reverse transcriptase | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID1060632 | Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as inhibition of viral cytopathicity after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs. |
AID1157583 | Antiviral activity against N119-sensitive HIV1 harboring Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID1275554 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV2 ROD infected in human MT4 cells | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID279483 | Antiviral activity against HIV1 isolate with RT K103N-Y181C mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID650689 | Inhibition of HIV 1 reverse transcriptase K103N mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT) | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID508646 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, Y188L mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1691439 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 RES056 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP. |
AID279495 | Antiviral activity against HIV1 isolate with RT K103N-Y188L mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID663303 | Resistance ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4-3 | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID586911 | Induction of SLCO1B1 activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Interaction potential of etravirine with drug transporters assessed in vitro. |
AID440672 | Antiviral activity against HIV1 EFV with reverse transcriptase K103R, V179D, P225H mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
| Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants. |
AID572172 | Antiviral activity against HIV-1 subtype CRF05_DF V022823 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID584240 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase Y181C, V108V/I, V179V/D mutant derived from 17 days viral passages with lersivirine infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to w | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID1373154 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Structural optimization of N |
AID1882473 | Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytopathicity by MTT assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors. |
AID446252 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with K103N mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
AID1264538 | Antiviral activity against HIV-1 X4 expressing wild-type reverse transcriptase infected in human CD4+ T cells for 3 days by FACS analysis | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
| Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance. |
AID1457068 | Antineuroinflammatory activity in C57BL/6 mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production at 1 to 10 uM after 24 hrs by Griess assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID443696 | Antiviral activity against HIV with reverse transcriptase Y181C mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID391223 | Inhibition of HIV1 RT polymerase Y181C mutant by SPA | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
| Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses. |
AID82473 | Antiviral activity against V108I/Y181C strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1249721 | Antiviral activity against HIV1 expressing reverse transcriptase Y181C mutant | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID605177 | Inhibition of HIV1 reverse transcriptase K103N mutant by SPA assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif. |
AID523348 | Antiviral activity against HIV1 with RT connection domain T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID448404 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with V108I mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 3: optimisation of physicochemical properties. |
AID508789 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103S mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID586368 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T124A mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID366525 | Resistance index, ratio of EC50 for drug-resistant HIV1 isolate with reverse transcriptase Y188L mutation to EC50 for wild type HIV1 NL4-3 | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID1457059 | Ratio of EC50 for HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID685331 | Antiviral activity against HIV-1 3B infected human MT4 cells assessed as inhibition in viral syncytium formation by MTT assay | 2012 | Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors. |
AID1185999 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay relative HIV1 | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID267654 | Selectivity for wild type HIV1 virus over HIV1 K103N/L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID446253 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with Y181C mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
AID586375 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Q146R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1636928 | Cytotoxicity against human MT2 cells assessed as growth inhibition by MTT method | 2016 | Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
| Computer-aided discovery of anti-HIV agents. |
AID586904 | Activity at BCRP | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Interaction potential of etravirine with drug transporters assessed in vitro. |
AID1888689 | Antiviral activity against HIV1 with RT F227L + V106A mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
AID1693800 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C. |
AID1304402 | Cytotoxicity against mock-infected human CEM-SS cells | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID562870 | Selectivity ratio of EC50 for HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells to EC50 for wild type HIV1 infected in human HeLa cells | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation. |
AID663302 | Resistance ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4-3 | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID269803 | Antiviral activity against HIV1 V179E mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. |
AID269803 | Antiviral activity against HIV1 V179E mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269803 | Antiviral activity against HIV1 V179E mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
| Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID496621 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase K101E/V35T, E36D, K49R, V60I, K122P, I135R, S162A, E169R, K173T, Q174E,D177E, V189I, T200A, I202V, Q207E, R211K, V245Q mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID663307 | Inhibition of HIV1 recombinant reverse transcriptase L100I mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT) | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID298064 | Cytotoxicity against human MT4 cells by MTT assay | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability. |
AID1485974 | Inhibition of HIV-1 reverse transcriptase Y188L mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Searching for novel N |
AID282739 | Inhibition of HIV1 RT Y181I mutant | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity. |
AID1183080 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction in proliferation after 96 hrs by MTT method | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis and antiviral activity of new phenylimidazopyridines and N-benzylidenequinolinamines derived by molecular simplification of phenylimidazo[4,5-g]quinolines. |
AID279487 | Antiviral activity against HIV1 isolate with RT K103N-L100I mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1731744 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | | | |
AID1897020 | Antiviral activity against HIV-1 KP-5mvcR infected in human TZM-bl cells assessed as inhibition of viral entry by measuring reduction in RLU by single round assay | 2022 | Bioorganic & medicinal chemistry, 12-15, Volume: 76 | Hybrids of small CD4 mimics and gp41-related peptides as dual-target HIV entry inhibitors. |
AID519872 | Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID1487425 | Aqueous solubility of the compound in buffer at pH 6.4 after 48 hrs UV spectroscopy based shake flask method | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
| Discovery of novel dengue virus entry inhibitors via a structure-based approach. |
AID1636929 | Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against viral infection by MTT method | 2016 | Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
| Computer-aided discovery of anti-HIV agents. |
AID1272059 | Half life in human administered as multiple doses | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry. |
AID348908 | Ratio of ED50 for drug resistant HIV1 with reverse transcriptase Y181C mutant to wild type HIV1 NL4-3 | 2008 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
| Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies. |
AID267644 | Inhibition of HIV1 reverse transcriptase | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID1882474 | Antiviral activity against HIV-1 harboring E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathicity by MTT assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors. |
AID698298 | Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-3 | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1693805 | Inhibition of recombinant HIV-1 BH10 reverse transcriptase Y181C mutant using D38/[32P]25PGA as template-primer incubated for 60 mins in absence of DTT followed by dTTP addition and measured after 15 to 30 sec by nucleotide incorporation assay | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C. |
AID1736368 | Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase V108I/K103N double mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cel | | | |
AID1060631 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of viral cytopathicity after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs. |
AID492282 | Antiviral activity against HIV1 with reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy. |
AID1882471 | Cytotoxicity against human MT2 cells assessed as cell viability by MTT assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors. |
AID1141961 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4.3 infected in human MT4 cells | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1141962 | Antiviral activity against HIV1 3B infected in human CEM cells assessed as protection of cells monitored by giant cell formation by microscopy | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID248879 | Inhibitory concentration against human immunodeficiency virus type 1 (with K103N/V108I resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2. |
AID1888700 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
AID523485 | Antiviral activity against HIV1 with RT connection domain L100I/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID1888698 | Antiviral activity against HIV1 with RT E138K mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
AID1754642 | Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
AID443700 | Antiviral activity against HIV with reverse transcriptase L100I/K103N double mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID1152371 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
| Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID266348 | Inhibition of HIV1 reverse transcriptase Y188C mutant in 293T cells | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity. |
AID1653630 | Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) K358R mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID1884227 | Antiviral activity against HIV-1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID1410410 | Fold resistance, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site. |
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. |
AID370725 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 L100I mutant expressed in Escherichia coli JM109 | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
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. |
AID519862 | Antiviral activity against HIV1 subtype B-LAI infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID1565092 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | | | |
AID571974 | Antiviral activity against HIV-1 subtype CRF01_AE V029521 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID342721 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors. |
AID1483275 | Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID571971 | Antiviral activity against HIV-1 subtype CRF01_AE V022820 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID611888 | Antiviral activity against Human immunodeficiency virus 1 assessed as inhibition of viral replication at 0.001 uM | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Bioactive neolignans and lignans from the bark of Machilus robusta. |
AID298077 | Cytotoxicity against lymphocytes | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. |
AID541158 | Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 6 passages to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1741391 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID1141977 | Inhibition of HIV1 wild-type reverse transcriptase Y181I/Y181C mutant using [3H]dTTP by scintillation counting | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1743622 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 RES056 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID246298 | Effective concentration of the compound to inhibit HIV-1 mutant K103N replication in HIV-infected MT-4 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID263522 | Antiviral activity against HIV1 F227L mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2. |
AID1157600 | Antiviral activity against HIV1 CRF01 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID248262 | In vitro inhibitory concentration against HIV V106A mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID1171591 | Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase L100I mutant to EC50 for wild type HIV1 NL4-3 | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1373159 | Inhibition of reverse transcriptase K103N mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Structural optimization of N |
AID279516 | Antiviral activity against wild type HIV1 NL4-3 in Hela-JC53 cells after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID299023 | Antiviral activity against HIV1 assessed as reduction of virus-induced cytopathic effect in MT4 cells | 2007 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
| Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains. |
AID279405 | Antiviral activity against HIV1 isolate with RT 101E, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID519864 | Antiviral activity against HIV1 subtype B-NL4-3 infected in 2 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID366528 | Resistance index, ratio of ID50 for reverse transcriptase K103N mutant to IC50 for wild-type HIV1 sreverse transcriptase | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile. |
AID279390 | Antiviral activity against HIV1 isolate with RT 103N, 181C mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID371896 | Antiviral activity against wild type HIV1 NL4-3 in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
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. |
AID576036 | Cmax in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID586469 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase L101I/S153F mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID586362 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E92I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vir | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID519021 | Antiviral activity against Human immunodeficiency virus 1 NL432 infected in human MT-4 cells assessed as effect on total viral DNA | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
| The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral. |
AID1572519 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
AID508794 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID391227 | Antiviral activity against wild type HIV1 infected in human MT4 cells after 72 hrs in presence of 50% normal human serum | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
| Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses. |
AID1390713 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
| First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain. |
AID586487 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase V72I/F121Y/T125K/I151V mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human im | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1407646 | Antiviral activity against Human immunodeficiency virus 1 NL4-3 infected in human CEM-GFP cells after 7 days by p24 ELISA | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors. |
AID584082 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase L100I, K103Q, H221H/Y mutant infected in human SupT1 cells derived from 11 viral passages with efavirenz assessed as inhibition of viral replication after 21 days relative to drug sensi | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID1754641 | Antiviral activity against HIV1 harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
AID302249 | Antiviral activity against HIV1 NL43 in MT4 cells assessed as inhibition of viral induced cytopathic effect after 4 days by MTT method | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID279519 | Antiviral activity against wild type HIV1 NL4-3 in Hela-JC53 cells in the presence of 20% human serum after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1736356 | Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase Y181C mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hrs post-infect | | | |
AID1246230 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity by MTT assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, cytotoxicity and antimicrobial activity of thiourea derivatives incorporating 3-(trifluoromethyl)phenyl moiety. |
AID441310 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with Y181C mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 1: design and initial optimisation of a novel template. |
AID1357801 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase K103N mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID496619 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase A98G/V35T, V60I, I135L, S162A, K173A, Q174K, D177E, I178M, T200A,Q207E, R211K, V245Q, D250E mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID263521 | Antiviral activity against HIV1 F227C mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2. |
AID263520 | Antiviral activity against HIV1 Y188L mutant | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
| Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2. |
AID583871 | Inhibition of HIV1 histidine-tagged reverse transcriptase Y181C mutant activity by primer extension assay | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID198577 | Inhibitory concentration for 90% inhibition of HIV-1 reverse transcriptase, whole cell based antiviral assay | 2000 | Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
| Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors. |
AID573467 | Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase G190A-81C mutant by filter-based filtration assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID508632 | Antiviral activity against Human immunodeficiency virus 1 subtype G isolate RU132 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
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. |
AID1815401 | Inhibition of HIV1 reverse transcriptase E138K mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID361909 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106A mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1815391 | Inhibition of HIV1 reverse transcriptase K103N/Y181C double mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID573465 | Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1847042 | Antiviral activity against HIV 1 infected in human HeLa-MAGI cells assessed as inhibition of viral replication measured 24 hrs post infection by fluorescence based analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
| Quinolinonyl Non-Diketo Acid Derivatives as Inhibitors of HIV-1 Ribonuclease H and Polymerase Functions of Reverse Transcriptase. |
AID105695 | Anti-HIV-1 activity against K103N strain in MT-4 cells by the MTT method | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
| 3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1155810 | Fold resistance, ratio of EC50 for HIV-1 harboring NNTRI-resistant reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for wild type HIV-1 NL4-3 infected in human MT4 cells | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes. |
AID492047 | Antiviral activity against HIV1 bearing reverse transcriptase K103N and Y181C double mutation infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors. |
AID1249713 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by MTT method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID508654 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181C, F227C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | | | |
AID279421 | Antiviral activity against HIV1 isolate with RT 101E, 190S mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1443661 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID573999 | Ratio of EC50 for Human immunodeficiency virus in presence of 10% FCS to EC50 for Human immunodeficiency virus in presence of 50% human serum | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID709869 | Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID658572 | Antiviral activity against wild type Human immunodeficiency virus 1 NL4-3 pseudotyped with HIV envelope infected in human HeLa-SxR5 cells assessed as inhibition of viral replication at 65 nM after 3 days by beta-galactosidase assay | 2012 | Journal of natural products, Mar-23, Volume: 75, Issue:3
| Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium. |
AID279434 | Antiviral activity against HIV1 isolate with RT 101E, 181C, 190S mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1275547 | Antiviral activity against HIV1 3B expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID557052 | Antiviral activity against NRTI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1884221 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID279524 | Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells in the presence of 5% human serum after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1069125 | Inhibition of HIV wild-type reverse transcriptase by electrochemiluminescence assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
| Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses. |
AID361922 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase Y188C mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID588997 | Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, MPR3 | 2010 | Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
| Membrane transporters in drug development. |
AID257169 | Antiviral activity against HIV1 Y188L mutant strain infected MT4 cells by MTT method | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
| Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity. |
AID717261 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs. |
AID1693804 | Inhibition of recombinant HIV-1 BH10 reverse transcriptase Y181C mutant using D38/[32P]25PGA as template-primer incubated for 5 mins in presence of DTT followed by dTTP addition and measured after 15 to 30 sec by nucleotide incorporation assay | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C. |
AID663904 | Cytotoxicity against human MT4 cells after 96 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 5-acetyl-2-arylbenzimidazoles as antiviral agents. Part 4. |
AID416432 | Antiviral activity against HIV1 bearing HIV1 NL4-3 envelope infected in human HeLa CD4 cells coexpressing LTR/beta-Gal gene assessed as reduction in virus-induced beta-galactosidase reporter gene activity after 72 hrs by single-cycle infection assay | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Identification and characterization of UK-201844, a novel inhibitor that interferes with human immunodeficiency virus type 1 gp160 processing. |
AID1815395 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID522370 | Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106I mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID302260 | Inhibition of HIV1 reverse transcriptase K103N mutant | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID302248 | Cytotoxicity against MT4 cells after 4 days by MTT method | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID496617 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, E36D, T39K, I50V, V60I, S68G, I135V, S162A, K173V, Q174K,D177E, T200A, E203Q, Q207D, R211K mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID397179 | Antiviral activity against HIV1 3B expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5
| Parallel synthesis, molecular modelling and further structure-activity relationship studies of new acylthiocarbamates as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID508761 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, F227L mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID508779 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179D mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID573250 | Cmax in HIV-1 infected children at 14.4 mg/kg, po administered once daily by HPLC | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID82466 | Antiviral activity against P225H strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID573470 | Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | | | |
AID1357793 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID279485 | Antiviral activity against HIV1 isolate with RT K103N-V108I mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1609109 | Antiviral activity against HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1060627 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs. |
AID665271 | Antiviral activity against HIV1 3B harboring wild type RT infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID443694 | Antiviral activity against HIV with reverse transcriptase L100I mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID1888699 | Antiviral activity against HIV1 with RT RES056 mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
AID279408 | Antiviral activity against HIV1 isolate with RT 101Q, 103N mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1298250 | Inhibition of HIV1 reverse transcriptase p66/p51 V106A mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
AID1750714 | Antiviral activity against HIV-1 infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID246779 | Concentration required to reduce the amount of p24 by 90% in wtIIIB-HIV-1-infected C8166 cells | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives. |
AID443708 | Antiviral activity against HIV with reverse transcriptase V106A/G190A/F227L mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID1773462 | Resistance factor, ratio of EC50 for HIV1 harboring F227L/V106A double mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells | | | |
AID197934 | HIV-1 reverse transcriptase inhibitory activity against Wild Type Reverse transcriptase using (poly)rC600*(oligo)dGT as template primer. | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
| Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues. |
AID1609106 | Antiviral activity against HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1249717 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID1882475 | Antiviral activity against HIV-1 harboring K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathicity by MTT assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors. |
AID361917 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106I mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1348216 | Antiviral activity against wild-type VSV-G pseudotyped MLV infected in HEK293 cells pretreated for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene assay | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12
| Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities. |
AID1248222 | Antiviral activity against wild type HIV 1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
| A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities. |
AID265472 | Activity against HIV-112 assessed by inhibition of p24 production in human lymphocytes | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide. |
AID279441 | Antiviral activity against HIV1 isolate with RT 101Q, 190S mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID573471 | Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase G190A-81C mutant by filter-based filtration assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID279442 | Antiviral activity against HIV1 isolate with RT 98G, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1773448 | Antiviral activity against wild type HIV1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | | | |
AID1264544 | Ratio of EC50 for HIV-1 expressing reverse transcriptase K101P mutant to EC50 for HIV-1 X4 expressing wild-type reverse transcriptase | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
| Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance. |
AID248255 | In vitro inhibitory concentration against HIV E138K mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID279428 | Antiviral activity against HIV1 isolate with RT 101E, 181C mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID586903 | Activity at MRP3 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Interaction potential of etravirine with drug transporters assessed in vitro. |
AID143393 | Inhibition of the NNRTI HIV-1 enzyme by 50% using enzyme assay. | 2001 | Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
| Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase. |
AID248842 | Inhibitory concentration against human immunodeficiency virus type 1 (with K103N resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2. |
AID302262 | Inhibition of HIV1 reverse transcriptase V106A mutant | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID1141965 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID302251 | Antiviral activity against HIV1 with reverse transcriptase IRLL98 mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID1561722 | Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-[4-[2-cyanovinyl]-2,6-dimethylphenoxy]thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonam | | | |
AID1637394 | Antiviral activity against human HIV-1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID519886 | Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID457958 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
| Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID257918 | Antiviral activity against HIV1 V106A mutant using HeLa MAGI assay | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor. |
AID1761006 | Antiviral activity against wild type HIV1 NL4-3 infected in human TZM-bl cells assessed as reduction in viral infection measured after 1 day by luciferase reporter gene assay based luminiscence assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | | | |
AID293561 | Antiviral activity against HIV1 LAI with RT Y181C mutation in MT4 cells by EGFP based replication assay | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5
| Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains. |
AID391222 | Inhibition of HIV1 RT polymerase K103N mutant by SPA | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
| Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses. |
AID141363 | Inhibitory activity against mutant L1001 HIV-1 Reverse transcriptase | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
| Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors. |
AID1572528 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
AID246300 | Effective concentration of the compound to inhibit HIV-1 mutant Y181C replication in HIV-infected MT-4 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1811039 | Anti-viral activity against HIV1 harboring RT L100I mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID271414 | Antiviral activity against HIV1 K103N-Y181C mutant in HeLa-JC53 cells | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
| Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase. |
AID1248227 | Inhibition of recombinant HIV1 Reverse transcriptase p66/p51 using poly (rA)-oligo (dT) as template primer after 40 mins by spectrofluorometric analysis | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
| A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities. |
AID371905 | Antiviral activity against HIV1 NL4-3 with K103N/Y181C double mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID518740 | Antiviral activity against HIV 1 subtype B harboring wild type reverse transcriptase infected in human TZM-bl cells assessed as inhibition of viral growth by luciferase reporter gene assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID1212899 | Drug metabolism in human liver microsomes harboring CYP2B6*1/*1 genotype assessed as intrinsic clearance for CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation measured per mg protein after 15 mins by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID279520 | Antiviral activity against wild type HIV1 NL4-3 in Hela-JC53 cells in the presence of 30% human serum after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID248264 | In vitro inhibitory concentration against HIV Y188L mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID246323 | Effective concentration against human immunodeficiency virus type 1 Y181C mutant was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). |
AID298065 | Metabolic stability in rat plasma | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability. |
AID443423 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus induced cytopathogenicity after 4 days by MTT assay | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
| Synthesis, pharmacological and antiviral activity of 1,3-thiazepine derivatives. |
AID622052 | Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer K103N/Y181C mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID698304 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID623212 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID1373153 | Inhibition of recombinant wild-type HIV-1 3B reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli JM109 assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Structural optimization of N |
AID440071 | Antiviral activity against HIV-1 LAI harboring wild type reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID576049 | Reduction in ABCC2 mRNA expression in healthy human at 400 mg, po qd for 14 days by RT-PCR | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID449491 | Cytotoxicity against human MT4 cells as reduction in cell viability after 5 days by MTT assay | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
| Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID282736 | Inhibition of HIV1 RT L100I mutant | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity. |
AID1485972 | Inhibition of HIV-1 reverse transcriptase E138K mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Searching for novel N |
AID279486 | Antiviral activity against HIV1 isolate with RT K103N-K101Q mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID522376 | Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V179D mutant clone to EC50 for wild type HIV1 | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID246269 | Effective concentration against human immunodeficiency virus type 1 Y188L mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). |
AID1171594 | Inhibition of wild type HIV1 reverse transcriptase K103N mutant assessed as reduction in enzyme activity | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID556527 | Antiviral activity against Human immunodeficiency virus 1 clone 14682 harboring 122E, 135V, Q145V, 200A mutation in reverse transcriptase by phenosense assay relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility. |
AID541124 | Antiviral activity against HIV1 3B infected in SupT1 cells assessed as fold decrease in viral 2-LTR circles accumulation after 3 hrs postinfection by TaqMan real-time PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1391081 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID519869 | Antiviral activity against HIV1 subtype B-ASM 044 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID736040 | Inhibition of HIV1 reverse transcriptase p66/p51 Y181C mutant after 30 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1435510 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay | | | |
AID427967 | Antiviral activity against HIV1 infected in human HeLa cells expressing CD4-LTR assessed as inhibition of viral entry-related beta galactosidase expression treated for 2 hrs followed by drug wash out measured after 48 hrs by MAGI assay | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
| Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2. |
AID443690 | Antiviral activity against HIV with reverse transcriptase K103N/Y181C/G190A mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID557053 | Antiviral activity against NRTI-, PI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID736438 | Inhibition of HIV1 reverse transcriptase p66/p51 K103N mutant after 30 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID82472 | Antiviral activity against V108I strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID508643 | Antiviral activity against Human immunodeficiency virus 1 subtype A1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID440080 | Antiviral activity against HIV1 HXB2 harboring 179E mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
AID83553 | Potency evaluated against NNRTI-Resistant HIV-1 strain Val106Ala | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
| Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian |
AID622051 | Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer G190A mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID279475 | Antiviral activity against HIV1 isolate with RT 101E, 103N, 190A mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID248845 | Inhibitory concentration against human immunodeficiency virus type 1 (with Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2. |
AID305057 | Antiviral activity against HIV in HEK293T cells after 48 hrs | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
| 4-Aminopyrimidines as novel HIV-1 inhibitors. |
AID257168 | Antiviral activity against HIV1 K103N mutant strain infected MT4 cells by MTT method | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
| Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity. |
AID573244 | Cmin in HIV-1 infected children at 12 mg/kg, po administered once daily by HPLC | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID1335215 | Antiviral activity against HIV-1 NL4-3 harboring RT-Y181C mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5. |
AID1435512 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase L100I mutant | | | |
AID198915 | Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution Y181I | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. |
AID279403 | Antiviral activity against HIV1 isolate with RT 108I mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID1352321 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103 N/Y181C double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID279394 | Antiviral activity against HIV1 isolate with RT 98G mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID198578 | Inhibitory concentration against HIV-1 reverse transcriptase | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
| 3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors. |
AID389380 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
| 1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1574387 | Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 L100I mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID1773827 | Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies. |
AID82471 | Antiviral activity against V106I/Y181C strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID279425 | Antiviral activity against HIV1 isolate with RT 179G mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID649485 | Inhibition of RNA-dependent DNA polymerase activity of wild type Human immunodeficiency virus 1 reverse transcriptase | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach. |
AID1157584 | Antiviral activity against A17-sensitive HIV1 harboring 103N, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID246301 | Effective concentration of the compound to inhibit HIV-1 mutant Y188L replication in HIV-infected MT-4 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1884538 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 L100I mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID614142 | Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17
| Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs. |
AID1157594 | Antiviral activity against TMC120-resistant HIV1 harboring RT 100I, 138G mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID1884224 | Antiviral activity against HIV-1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID573251 | AUC (0 to t) in HIV-1 infected children at 12 mg/kg, po administered once daily by HPLC | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
| Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children? |
AID1391082 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID496623 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/G18V, Q23P, V35T, E40D, V60I, S68G, D123E, I135V, S162A, K173T, Q174N, T200A, Q207E, R211K, F214L mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID1304403 | Cytotoxicity against mock-infected human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
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. |
AID1286672 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C/K103N double mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor. |
AID431621 | Cytotoxicity against human MT4 cells by MTT assay | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
| Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID663305 | Inhibition of HIV1 wild type recombinant reverse transcriptase assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT) | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID44798 | In vitro concentration required to reduce the amount of p24 by 90% in WTIIIB infected C8166 cells | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations. |
AID1185998 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID248256 | In vitro inhibitory concentration against HIV F227C mutant strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. |
AID576047 | Reduction in ABCB1 mRNA expression in healthy human at 400 mg, po qd for 14 days by RT-PCR | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID1249716 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 4 days by MTT assay | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID368564 | Inhibition of wild type HIV1 free reverse transcriptase | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID1687685 | Antiviral activity against HIV-2 ROD strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID650687 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV 1 NL4-3 | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID490369 | Antiviral activity against wild type HIV1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect in presence of 40 % human serum | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses. |
AID1152374 | Selectivity index, ratio CC50 for human MT4 cells to EC50 for HIV 1 3B | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
| Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID198099 | Inhibitory activity against HIV-1 reverse transcriptase enzyme | 1999 | Bioorganic & medicinal chemistry letters, Oct-04, Volume: 9, Issue:19
| Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors. |
AID518742 | Selectivity ratio of EC50 for antiviral activity against HIV 1 subtype B harboring reverse transcriptase M230L mutant to EC50 for antiviral activity against HIV 1 subtype B harboring wild type reverse transcriptase | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
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. |
AID541128 | Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of integrated junction products after 48 hrs by Alu-PCR assay | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID368568 | Inhibition of HIV1 recombinant reverse transcriptase K103N mutant-DNA binary complex expressed in Escherichia coli BL21 | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID1583020 | Antiviral activity against NNRTI-resistant HIV1 RES056 containing reverse transcriptase K103N+Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
| Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel. |
AID557036 | Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1212883 | Drug metabolism in microsomes expressing CYP2B6.1 (unknown origin) assessed as intrinsic clearance for enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in presence of Cyt b5 coexpression | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
| Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo. |
AID508776 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179T mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID557045 | Antiviral activity against HIV1 CRF17_BF harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID557020 | Antiviral activity against HIV1 clade B harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1561716 | Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in absence of test compound assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID279449 | Antiviral activity against HIV1 isolate with RT 98G, 188L mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID541109 | Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID197933 | HIV-1 reverse transcriptase inhibitory activity against Ile 100 mutant using (poly)rC600*(oligo)dGT as template primer. | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
| Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues. |
AID371900 | Antiviral activity against HIV1 NL4-3 with K103N mutant in human MT4 cells assessed as inhibition of virus-induced cytopathicity after 5 days by multiple round replication assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID246463 | Compound concentration required to achieve 50% protection of infected MT-4 cells from Y181C strain was determined by the MTT method | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives. |
AID571976 | Antiviral activity against HIV-1 subtype B V022807 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID267649 | Antiviral activity against HIV1 L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID508625 | Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 93TH073 infected in human PBMC cells by cell based assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
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. |
AID94444 | Potency of second-generation NNRTIs against Mutant HIV-1 K103N free drug | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID572177 | Antiviral activity against HIV-1 subtype H V022828 harboring NNRTI K101Q and V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID1390714 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
| First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain. |
AID1456311 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B wild type reverse transcriptase infected in human MT4 cells | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. |
AID1206939 | Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 assessed as reduction in biotin-labeled dUTP incorporation into DNA using polyr(A) x oligo(dT)16 template/primer hybrid | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID246153 | Concentration required to achieve 50% protection of infected MT-4 cells from K103N-Y181C | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives. |
AID330487 | Cytotoxicity against human MT4 cells | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID541165 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E138K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1609104 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID586900 | Activity at ABCB1 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Interaction potential of etravirine with drug transporters assessed in vitro. |
AID1261342 | Antiviral activity against Vaccinia virus | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5. |
AID1157604 | Antiviral activity against HIV1 MP1033 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID88365 | Antiviral activity against G190A mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
| 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID247723 | Inhibitory concentration against 100I mutant was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity. |
AID1520059 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID1390712 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
| First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain. |
AID247496 | Inhibitory activity against HIV-1 mutant strain 101E | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| 4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains. |
AID1485970 | Inhibition of HIV-1 reverse transcriptase K103N mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Searching for novel N |
AID508751 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, F227C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID104411 | Antiviral activity of Protein Binding of compound was evaluated for RF virus expressed MT-2 by RNA | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID586366 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase G118S mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1815396 | Inhibition of wild type HIV1 reverse transcriptase using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID586905 | Inhibition of ABCB1 activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Interaction potential of etravirine with drug transporters assessed in vitro. |
AID576051 | Ratio of drug concentration in PBMCs to plasma of healthy human administered at 400 mg, po qd for 14 days measured after 24 hrs post last dose | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. |
AID1298246 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
AID1743639 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT F227L/V106A mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID584030 | Inhibition of HIV1 histidine-tagged reverse transcriptase L234I mutant activity by primer extension assay | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID1687688 | Antiviral activity against wild type HIV1 assessed as inhibitory effect on virus producing cells at 10 uM by cell based inhibition assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Rational design and Structure-Activity relationship of coumarin derivatives effective on HIV-1 protease and partially on HIV-1 reverse transcriptase. |
AID361905 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/P225H mutant in HeLa cells by MAGI assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1357789 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID443707 | Antiviral activity against HIV with reverse transcriptase K103N/Y181C/G190A mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID1637388 | Antiviral activity against human HIV-1 3B infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID1443664 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID1743621 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID573995 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for L-708,906-resistant Human immunodeficiency virus harboring T66I, L74M and S230R mutations in integrase | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
AID1443666 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID1743627 | Antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID1565096 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
AID571985 | Antiviral activity against HIV-1 subtype C V022817 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. |
AID464770 | Half life in Beagle dog at 0.5 mg/kg, iv or 0.5 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID279496 | Antiviral activity against HIV1 isolate with RT K103N-G190A mutation | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID386490 | Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in human MT4 cells assessed as reduction of virus-induced cytopathogenicity by MTT assay | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Parallel synthesis, molecular modelling and structure-activity relationship studies on O-[2-(hetero)arylethyl]-N-phenylthiocarbamates. |
AID104409 | Antiviral activity of Protein Binding of compound was evaluated for E virus expressed MT-2 by yield | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. |
AID1729152 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV 3B infected in human MT4 cells | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID448397 | Fold resistance, ratio of IC50 for HIV reverse transcriptase with K103N mutant to IC50 for HIV wild type reverse transcriptase | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| Pyrazole NNRTIs 3: optimisation of physicochemical properties. |
AID302264 | Inhibition of HIV1 reverse transcriptase Y1811 mutant | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID1653629 | Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) Y427A mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID562120 | Apparent oral volume of distribution in patient with HIV infection at 600 mg/kg QD | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
| Influence of the cytochrome P450 2B6 genotype on population pharmacokinetics of efavirenz in human immunodeficiency virus patients. |
AID1574385 | Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 K103N mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID1410485 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
AID443685 | Antiviral activity against HIV with reverse transcriptase K103N/G190A double mutant assessed as inhibition of viral replication | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID519971 | Selectivity ratio of EC50 for 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT to EC50 for 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID1687680 | Antiviral activity against wild type HIV-1 strain 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID1627028 | Cytotoxicity against HIV1 infected African green monkey Vero cells assessed as reduction in cell viability after 7 days by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1596752 | Antiviral activity against HIV-1 3B harboring reverse transcriptase E138K mutant infected in MT4 cells measured after 5 days by MTT assay | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains. |
AID1815377 | Anti-HIV activity against HIV-1 IIIB infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1157602 | Antiviral activity against HIV1 MP634 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID1357802 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase E138K mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID1773441 | Antiviral activity against wild type HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | | | |
AID757626 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID368566 | Inhibition of wild type HIV1 reverse transcriptase-DNA-dNTP ternary complex | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID1485971 | Inhibition of HIV-1 reverse transcriptase V106A mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Searching for novel N |
AID443698 | Antiviral activity against HIV with reverse transcriptase G190A mutant assessed as inhibition of viral replication relative to wild type | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
| Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses. |
AID757621 | Inhibition of recombinant wild type HIV1 RT using poly(rA)/oligo(dT)16 as template after 40 mins by spectrofluorometric analysis | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1761008 | Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID519889 | Selectivity ratio of EC50 for 0.005 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.005 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
AID508760 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, V108I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID523358 | Antiviral activity against HIV1 with RT connection domain G190A/N348Ib mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
AID508759 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1163253 | Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
AID586381 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase S153Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1653633 | Binding affinity to recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli at 15 to 30 uM in absence of substrate by UV-spectrophotometric method | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. |
AID1558849 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells incubated for 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID663297 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies. |
AID370733 | Therapeutic index, ratio of IC50 for HIV1 3B to TC50 for human C8166 cells | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
AID1373152 | Inhibition of reverse transcriptase Y181C mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Structural optimization of N |
AID330490 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES053 | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID279456 | Antiviral activity against HIV1 isolate with RT 188H mutation relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors. |
AID302266 | Resistance index, ratio of Ki for HIV1 RT K103N mutant to Ki for wild type HIV1 3B reverse transcriptase | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains. |
AID586361 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T66K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vir | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID366548 | Inhibition of HIV1 wild-type reverse transcriptase by scintillation counting assay | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID621982 | Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer L100I mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
| 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID1822275 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV-1 IIIB infected in human MT4 cells | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID586372 | Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Y143H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi | 2011 | Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
| In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. |
AID1275546 | Antiviral activity against HIV1 3B expressing reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID81766 | Compound was evaluated for its ability to inhibit the wild type RF strain of HIV-1 | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
| 4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | | | |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6
| A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | | | |
AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6
| A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2002 | European journal of biochemistry, Mar, Volume: 269, Issue:6
| Structural basis for the inhibitory efficacy of efavirenz (DMP-266), MSC194 and PNU142721 towards the HIV-1 RT K103N mutant. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | | | |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
| Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |