efavirenz [Ligand Id: 11287] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL223228 (DMP-266, (-)-efavirenz, Efavirenz, Efavirenz teva, Efavirenzum, L-743726, NSC-742403, Stocrin, Sustiva, Sustiva 600, Viraday)
  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
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  • Envelope glycoprotein gp160 in Human immunodeficiency virus 1 [ChEMBL: CHEMBL1293311] [UniProtKB: Q6QLK5]
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  • Human immunodeficiency virus type 1 reverse transcriptase in Human immunodeficiency virus 1 [ChEMBL: CHEMBL247] [UniProtKB: Q72547]
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  • CYP3A4 in Human [GtoPdb: 1337] [UniProtKB: P08684]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
ChEMBL 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 B 4.69 pIC50 20600 nM IC50 Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322]
CYP46A1/Cholesterol 24-hydroxylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523510] [GtoPdb: 1373] [UniProtKB: Q9Y6A2]
ChEMBL 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 B 4.99 pKd 10200 nM Kd J Med Chem (2020) 63: 6477-6488 [PMID:31617715]
ChEMBL 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 B 5.3 pKd 5000 nM Kd J Med Chem (2020) 63: 6477-6488 [PMID:31617715]
ChEMBL 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 B 6.1 pKd 800 nM Kd J Med Chem (2020) 63: 6477-6488 [PMID:31617715]
Envelope glycoprotein gp160 in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293311] [UniProtKB: Q6QLK5]
ChEMBL Binding affinity to HIV1 cYTA48P envelope glycoprotein gp120 infected in human TZM-b1 cells assessed as induction of conformational changes measured after 48 hrs B 8.46 pIC50 3.5 nM IC50 Bioorg Med Chem Lett (2019) 29: 719-723 [PMID:30665681]
Human immunodeficiency virus type 1 reverse transcriptase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL247] [UniProtKB: Q72547]
ChEMBL Inhibition of HIV1 reverse transcriptase K103N mutant B 5.52 pKi 3000 nM Ki J Med Chem (2007) 50: 5412-5424 [PMID:17910429]
ChEMBL Inhibition of HIV1 recombinant reverse transcriptase K103N mutant-DNA binary complex expressed in Escherichia coli BL21 B 5.8 pKi 1600 nM Ki J Med Chem (2009) 52: 840-851 [PMID:19140683]
ChEMBL Inhibition of HIV1 recombinant free reverse transcriptase K103N mutant expressed in Escherichia coli BL21 B 5.82 pKi 1500 nM Ki J Med Chem (2009) 52: 840-851 [PMID:19140683]
ChEMBL 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 B 6.14 pKi 730 nM Ki Bioorg Med Chem (2011) 19: 5794-5802 [PMID:21903401]
ChEMBL 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 B 6.24 pKi 580 nM Ki Bioorg Med Chem (2011) 19: 5794-5802 [PMID:21903401]
ChEMBL Inhibition of HIV1 reverse transcriptase p66/p51 K103N mutant after 30 mins by liquid scintillation counting B 6.24 pKi 580 nM Ki Bioorg Med Chem (2013) 21: 1150-1158 [PMID:23357038]
ChEMBL Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution Y188L B 6.52 pKi 300 nM Ki J Med Chem (2001) 44: 305-315 [PMID:11462972]
ChEMBL Inhibition of HIV1 recombinant reverse transcriptase K103N mutant-DNA-dNTP ternary complex expressed in Escherichia coli BL21 B 6.7 pKi 200 nM Ki J Med Chem (2009) 52: 840-851 [PMID:19140683]
ChEMBL Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution K103N B 6.8 pKi 160 nM Ki J Med Chem (2001) 44: 305-315 [PMID:11462972]
ChEMBL Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 K103N mutant expressed in Escherichia coli JM109 B 6.8 pKi 160 nM Ki J Med Chem (2009) 52: 1224-1228 [PMID:19170521]
ChEMBL Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 Y181I mutant expressed in Escherichia coli JM109 B 6.82 pKi 150 nM Ki J Med Chem (2009) 52: 1224-1228 [PMID:19170521]
ChEMBL Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution Y181I B 6.82 pKi 150 nM Ki J Med Chem (2001) 44: 305-315 [PMID:11462972]
ChEMBL Inhibition of HIV1 reverse transcriptase p66/p51 K103N/Y181C mutant after 30 mins by liquid scintillation counting B 6.85 pKi 140 nM Ki Bioorg Med Chem (2013) 21: 1150-1158 [PMID:23357038]
ChEMBL Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 L100I mutant expressed in Escherichia coli JM109 B 6.92 pKi 120 nM Ki J Med Chem (2009) 52: 1224-1228 [PMID:19170521]
ChEMBL Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution L1001 B 6.92 pKi 120 nM Ki J Med Chem (2001) 44: 305-315 [PMID:11462972]
ChEMBL Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant after 30 mins by liquid scintillation counting B 7.1 pKi 80 nM Ki Bioorg Med Chem (2013) 21: 1150-1158 [PMID:23357038]
ChEMBL 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 B 7.1 pKi 80 nM Ki Bioorg Med Chem (2011) 19: 5794-5802 [PMID:21903401]
ChEMBL Inhibition of HIV1 reverse transcriptase p66/p51 V106A mutant after 30 mins by liquid scintillation counting B 7.3 pKi 50 nM Ki Bioorg Med Chem (2013) 21: 1150-1158 [PMID:23357038]
ChEMBL Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution V106A B 7.4 pKi 40 nM Ki J Med Chem (2001) 44: 305-315 [PMID:11462972]
ChEMBL Inhibition of HIV-1 wild-type RT B 7.52 pKi 30 nM Ki J Med Chem (2001) 44: 305-315 [PMID:11462972]
ChEMBL Inhibition of wild type HIV1 3B reverse transcriptase B 7.52 pKi 30 nM Ki J Med Chem (2007) 50: 5412-5424 [PMID:17910429]
ChEMBL Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 expressed in Escherichia coli JM109 B 7.52 pKi 30 nM Ki J Med Chem (2009) 52: 1224-1228 [PMID:19170521]
ChEMBL Inhibition of wild type HIV1 free reverse transcriptase B 7.52 pKi 30 nM Ki J Med Chem (2009) 52: 840-851 [PMID:19140683]
ChEMBL Inhibition of wild type HIV1 reverse transcriptase-DNA binary complex B 7.52 pKi 30 nM Ki J Med Chem (2009) 52: 840-851 [PMID:19140683]
ChEMBL Inhibition of HIV1 reverse transcriptase p66/p51 Y181C mutant after 30 mins by liquid scintillation counting B 7.52 pKi 30 nM Ki Bioorg Med Chem (2013) 21: 1150-1158 [PMID:23357038]
ChEMBL Binding affinity towards L100I mutant HIV-1 reverse transcriptase (as per ref 10 in the article) B 7.6 pKi 25 nM Ki Bioorg Med Chem Lett (2001) 11: 2799-2802 [PMID:11597403]
ChEMBL Binding affinity towards L100I mutant HIV-1 reverse transcriptase (as per ref 10 in the article) B 7.77 pKi 17 nM Ki Bioorg Med Chem Lett (2001) 11: 2799-2802 [PMID:11597403]
ChEMBL Non-competitive inhibition of wild type HIV1 reverse transcriptase p66/p51 after 30 mins by liquid scintillation counting B 8 pKi 10 nM Ki Bioorg Med Chem (2013) 21: 1150-1158 [PMID:23357038]
ChEMBL Inhibition of HIV1 reverse transcriptase K103N mutant by SPA assay B 8.07 pKi 8.5 nM Ki Bioorg Med Chem Lett (2010) 20: 4328-4332 [PMID:20609585]
ChEMBL Inhibition of wild type HIV1 reverse transcriptase-DNA-dNTP ternary complex B 8.4 pKi 4 nM Ki J Med Chem (2009) 52: 840-851 [PMID:19140683]
ChEMBL Binding affinity towards wild type HIV-1 reverse transcriptase (as per ref 10 in the article) B 8.52 pKi 3 nM Ki Bioorg Med Chem Lett (2001) 11: 2799-2802 [PMID:11597403]
ChEMBL Binding affinity towards wild type HIV-1 reverse transcriptase (as per ref 10 in the article) B 8.52 pKi 3 nM Ki Bioorg Med Chem Lett (2001) 11: 2799-2802 [PMID:11597403]
ChEMBL Inhibition of HIV1 reverse transcriptase B 8.53 pKi 2.93 nM Ki J Med Chem (2019) 62: 4851-4883 [PMID:30516990]
ChEMBL Inhibition of wild type HIV1 reverse transcriptase by SPA assay B 9.4 pKi 0.4 nM Ki Bioorg Med Chem Lett (2010) 20: 4328-4332 [PMID:20609585]
ChEMBL Inhibition of HIV1 reverse transcriptase Y181C mutant by SPA assay B 9.52 pKi 0.3 nM Ki Bioorg Med Chem Lett (2010) 20: 4328-4332 [PMID:20609585]
ChEMBL Inhibition of ribonuclease H activity of wild type Human immunodeficiency virus 1 reverse transcriptase B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2012) 50: 216-229 [PMID:22361685]
ChEMBL Inhibition of wild type HIV1 reverse transcriptase K103N mutant assessed as reduction in enzyme activity B 4.7 pIC50 >20000 nM IC50 J Med Chem (2014) 57: 9945-9957 [PMID:25418038]
ChEMBL Inhibition of HIV1 wild-type reverse transcriptase K103N mutant using [3H]dTTP by scintillation counting B 4.7 pIC50 >20000 nM IC50 Eur J Med Chem (2014) 80: 101-111 [PMID:24769348]
ChEMBL 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 counting method B 4.7 pIC50 >20000 nM IC50 Eur J Med Chem (2020) 208: 112696-112696 [PMID:32883642]
ChEMBL 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 analysis B 4.7 pIC50 >20000 nM IC50 J Med Chem (2017) 60: 6528-6547 [PMID:28628334]
ChEMBL Inhibitory concentration against HIV-1 mutant reverse transcriptase (K103R) B 5.68 pIC50 2100 nM IC50 J Med Chem (2005) 48: 3858-3873 [PMID:15916438]
ChEMBL Inhibition of wild type HIV1 reverse transcriptase B 5.82 pIC50 1520 nM IC50 Bioorg Med Chem (2011) 19: 5924-5934 [PMID:21930388]
ChEMBL 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 B 5.85 pIC50 1420 nM IC50 J Med Chem (2016) 59: 7991-8007 [PMID:27541578]
ChEMBL 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 B 5.92 pIC50 1200 nM IC50 Bioorg Med Chem (2017) 25: 3861-3870 [PMID:28559060]
ChEMBL Inhibition of HIV1 3B reverse transcriptase p66/p51 K103N/Y181C mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry B 5.92 pIC50 1200 nM IC50 Bioorg Med Chem (2016) 24: 2476-2485 [PMID:27112451]
ChEMBL Inhibition of DNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by gel-based primer extension assay B 6.04 pIC50 910 nM IC50 Antimicrob Agents Chemother (2010) 54: 2401-2408 [PMID:20308384]
ChEMBL Inhibition of HIV1 reverse transcriptase B 6.1 pIC50 800 nM IC50 Bioorg Med Chem Lett (2006) 16: 3430-3433 [PMID:16632349]
ChEMBL Inhibition of RNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by filter-based filtration assay B 6.13 pIC50 740 nM IC50 Antimicrob Agents Chemother (2010) 54: 2401-2408 [PMID:20308384]
ChEMBL 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 B 6.13 pIC50 740 nM IC50 Bioorg Med Chem (2016) 24: 3006-3022 [PMID:27234889]
ChEMBL Inhibition of HIV1 reverse transcriptase p66/p51 K103N mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry B 6.14 pIC50 730 nM IC50 Bioorg Med Chem (2016) 24: 2476-2485 [PMID:27112451]
ChEMBL Inhibition of RNA-dependent DNA polymerase activity of Human immunodeficiency virus 1 reverse transcriptase Lys103Asn mutant B 6.17 pIC50 680 nM IC50 Eur J Med Chem (2012) 50: 216-229 [PMID:22361685]
ChEMBL Inhibition of HIV1 reverse transcriptase Tyr181Cys mutant-associated RNA-dependent DNA polymerase activity after 30 mins B 6.17 pIC50 680 nM IC50 Eur J Med Chem (2015) 93: 452-460 [PMID:25728026]
ChEMBL 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 B 6.2 pIC50 630 nM IC50 Bioorg Med Chem (2017) 25: 3861-3870 [PMID:28559060]
ChEMBL Inhibition of HIV1 Reverse transcriptase p51/p66 K103N mutant after 30 mins using alpha-[32P]dATP by liquid scintillation counting B 6.24 pIC50 580 nM IC50 Medchemcomm (2013) 4: 1443-1451
ChEMBL Inhibition of HIV1 reverse transcriptase K103N mutant expressed in Escherichia coli BL21 (DE3) using [alpha-32P]dATP after 30 mins by liquid scintillation counting B 6.24 pIC50 580 nM IC50 Medchemcomm (2013) 4: 741-748
ChEMBL Inhibition of HIV1 reverse transcriptase Y181I mutant by RNA-dependent DNA polymerase activity assay B 6.3 pIC50 500 nM IC50 Bioorg Med Chem (2010) 18: 1702-1710 [PMID:20097079]
ChEMBL Inhibitory concentration against HIV-1 mutant reverse transcriptase (K103N+Y181C) B 6.3 pIC50 500 nM IC50 J Med Chem (2005) 48: 3858-3873 [PMID:15916438]
ChEMBL 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 B 6.32 pIC50 480 nM IC50 Eur J Med Chem (2022) 238: 114471-114471 [PMID:35640327]
ChEMBL Inhibition of HIV1 HXB2 reverse transcriptase K103N mutant activity by primer extension assay B 6.38 pIC50 414 nM IC50 Antimicrob Agents Chemother (2010) 54: 4451-4463 [PMID:20660667]
ChEMBL Inhibition of wild type HIV1 reverse transcriptase Y181I mutant assessed as reduction in enzyme activity B 6.4 pIC50 400 nM IC50 J Med Chem (2014) 57: 9945-9957 [PMID:25418038]
ChEMBL 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 analysis B 6.4 pIC50 400 nM IC50 J Med Chem (2017) 60: 6528-6547 [PMID:28628334]
ChEMBL Inhibition of HIV1 reverse transcriptase K103N mutant RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate B 6.4 pIC50 400 nM IC50 J Med Chem (2012) 55: 6634-6638 [PMID:22712652]
ChEMBL Inhibition of HIV1 wild-type reverse transcriptase Y181I/Y181C mutant using [3H]dTTP by scintillation counting B 6.4 pIC50 400 nM IC50 Eur J Med Chem (2014) 80: 101-111 [PMID:24769348]
ChEMBL Inhibition of wild type HIV1 reverse transcriptase Y181I/Y181C mutant assessed as reduction in enzyme activity B 6.4 pIC50 400 nM IC50 J Med Chem (2014) 57: 9945-9957 [PMID:25418038]
ChEMBL Inhibition of HIV1 RT Y188L mutant B 6.42 pIC50 380 nM IC50 J Med Chem (2005) 48: 7153-7165 [PMID:16279773]
ChEMBL Inhibition of RNA-dependent DNA polymerase activity of HIV1 reverse transcriptase K103N mutant B 6.44 pIC50 364 nM IC50 J Med Chem (2009) 52: 1219-1223 [PMID:19175319]
ChEMBL 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 B 6.44 pIC50 360 nM IC50 Bioorg Med Chem (2018) 26: 2051-2060 [PMID:29559197]
ChEMBL Inhibition of HIV1 reverse transcriptase Lys103Asn mutant-associated RNA-dependent DNA polymerase activity after 30 mins B 6.55 pIC50 280 nM IC50 Eur J Med Chem (2015) 93: 452-460 [PMID:25728026]
ChEMBL 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 B 6.57 pIC50 270 nM IC50 Bioorg Med Chem (2017) 25: 3861-3870 [PMID:28559060]
ChEMBL 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 B 6.59 pIC50 260 nM IC50 Eur J Med Chem (2020) 185: 111874-111874 [PMID:31735575]
ChEMBL Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry B 6.6 pIC50 250 nM IC50 Bioorg Med Chem (2016) 24: 2476-2485 [PMID:27112451]
ChEMBL 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 B 6.67 pIC50 216 nM IC50 Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127]
ChEMBL Inhibition of HIV1 reverse transcriptase K103N mutant by RNA-dependent DNA polymerase activity assay B 6.7 pIC50 200 nM IC50 Bioorg Med Chem (2010) 18: 1702-1710 [PMID:20097079]
ChEMBL 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 B 6.74 pIC50 180 nM IC50 Bioorg Med Chem (2021) 30: 115927-115927 [PMID:33352387]
ChEMBL Inhibition of HIV1 reverse transcriptase K103N mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis B 6.77 pIC50 170 nM IC50 Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311]
ChEMBL Inhibition of HIV1 RT K103N mutant B 6.8 pIC50 160 nM IC50 J Med Chem (2005) 48: 7153-7165 [PMID:16279773]
ChEMBL Inhibition of HIV1 RT Y181I mutant B 6.82 pIC50 150 nM IC50 J Med Chem (2005) 48: 7153-7165 [PMID:16279773]
ChEMBL Inhibition of HIV1 reverse transcriptase K103N/Y181C mutant expressed in Escherichia coli BL21 (DE3) using [alpha-32P]dATP after 30 mins by liquid scintillation counting B 6.85 pIC50 140 nM IC50 Medchemcomm (2013) 4: 741-748
ChEMBL Inhibition of HIV1 Reverse transcriptase p51/p66 K103N/Y181C mutant after 30 mins using alpha-[32P]dATP by liquid scintillation counting B 6.85 pIC50 140 nM IC50 Medchemcomm (2013) 4: 1443-1451
ChEMBL Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay B 6.9 pIC50 126 nM IC50 Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127]
ChEMBL 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 B 6.92 pIC50 120 nM IC50 Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311]
ChEMBL Inhibition of HIV1 RT L100I mutant B 6.92 pIC50 120 nM IC50 J Med Chem (2005) 48: 7153-7165 [PMID:16279773]
ChEMBL Inhibition of wild type HIV1 reverse transcriptase L100I mutant assessed as reduction in enzyme activity B 6.92 pIC50 120 nM IC50 J Med Chem (2014) 57: 9945-9957 [PMID:25418038]
ChEMBL Inhibition of recombinant HIV1 reverse transcriptase using poly rA:dT as template/primer after 1 hr by ELISA B 6.92 pIC50 120 nM IC50 Bioorg Med Chem Lett (2013) 23: 6593-6597 [PMID:24239481]
ChEMBL Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay B 6.95 pIC50 112 nM IC50 Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127]
ChEMBL Inhibition of HIV-1 NL4-3 reverse transcriptase by RT-PCR analysis B 6.96 pIC50 110 nM IC50 Eur J Med Chem (2023) 246: 114981-114981 [PMID:36481598]
ChEMBL Inhibition of HIV1 reverse transcriptase Y188L mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis B 7 pIC50 100 nM IC50 Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311]
ChEMBL 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 B 7 pIC50 100 nM IC50 Bioorg Med Chem (2017) 25: 3861-3870 [PMID:28559060]
ChEMBL Inhibition of RNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase by filter-based filtration assay B 7.03 pIC50 93 nM IC50 Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127]
ChEMBL 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 scintillation counting method B 7.1 pIC50 80 nM IC50 Eur J Med Chem (2020) 208: 112696-112696 [PMID:32883642]
ChEMBL Inhibition of wild type HIV1 reverse transcriptase RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate B 7.1 pIC50 80 nM IC50 J Med Chem (2012) 55: 6634-6638 [PMID:22712652]
ChEMBL Inhibition of HIV1 wild-type reverse transcriptase using [3H]dTTP by scintillation counting B 7.1 pIC50 80 nM IC50 Eur J Med Chem (2014) 80: 101-111 [PMID:24769348]
ChEMBL Inhibition of HIV1 reverse transcriptase L100I mutant expressed in Escherichia coli BL21 (DE3) using [alpha-32P]dATP after 30 mins by liquid scintillation counting B 7.1 pIC50 80 nM IC50 Medchemcomm (2013) 4: 741-748
ChEMBL Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in enzyme activity B 7.1 pIC50 80 nM IC50 J Med Chem (2014) 57: 9945-9957 [PMID:25418038]
ChEMBL Inhibition of HIV1 Reverse transcriptase p51/p66 L100I mutant after 30 mins using alpha-[32P]dATP by liquid scintillation counting B 7.1 pIC50 80 nM IC50 Medchemcomm (2013) 4: 1443-1451
ChEMBL 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 counting analysis B 7.1 pIC50 80 nM IC50 J Med Chem (2017) 60: 6528-6547 [PMID:28628334]
ChEMBL Inhibition of HIV1 reverse transcriptase p66/p51 Y181C mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry B 7.15 pIC50 70 nM IC50 Bioorg Med Chem (2016) 24: 2476-2485 [PMID:27112451]
ChEMBL HIV-1 reverse transcriptase inhibitory activity against Asn103 mutant using (poly)rC600*(oligo)dGT as template primer. B 7.21 pIC50 61 nM IC50 J Med Chem (1999) 42: 4150-4160 [PMID:10514285]
ChEMBL Inhibition of reverse transcriptase activity in HIV1 NL4-3 infected MT4 cells after dialysis B 7.22 pIC50 60 nM IC50 Antimicrob Agents Chemother (2007) 51: 638-644 [PMID:17116672]
ChEMBL Inhibition of HIV1 reverse transcriptase G190A mutant expressed in Escherichia coli BL21 (DE3) using [alpha-32P]dATP after 30 mins by liquid scintillation counting B 7.22 pIC50 60 nM IC50 Medchemcomm (2013) 4: 741-748
ChEMBL 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 B 7.24 pIC50 57 nM IC50 Bioorg Med Chem (2017) 25: 3861-3870 [PMID:28559060]
ChEMBL Inhibition of DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by gel-based primer extension assay B 7.24 pIC50 57 nM IC50 Antimicrob Agents Chemother (2010) 54: 2401-2408 [PMID:20308384]
ChEMBL Inhibition of HIV1 reverse transcriptase K103N mutant in 293T cells B 7.27 pIC50 54 nM IC50 Bioorg Med Chem Lett (2006) 16: 3034-3038 [PMID:16527484]
ChEMBL Inhibition of HIV1 reverse transcriptase L100I mutant by RNA-dependent DNA polymerase activity assay B 7.3 pIC50 50 nM IC50 Bioorg Med Chem (2010) 18: 1702-1710 [PMID:20097079]
ChEMBL Inhibition of HIV1 reverse transcriptase V106A mutant expressed in Escherichia coli BL21 (DE3) using [alpha-32P]dATP after 30 mins by liquid scintillation counting B 7.3 pIC50 50 nM IC50 Medchemcomm (2013) 4: 741-748
ChEMBL Inhibition of HIV1 reverse transcriptase p66/p51 V106A mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry B 7.3 pIC50 50 nM IC50 Bioorg Med Chem (2016) 24: 2476-2485 [PMID:27112451]
ChEMBL HIV-1 reverse transcriptase inhibitory activity against Ile 100 mutant using (poly)rC600*(oligo)dGT as template primer. B 7.3 pIC50 50 nM IC50 J Med Chem (1999) 42: 4150-4160 [PMID:10514285]
ChEMBL Inhibition of HIV1 Reverse transcriptase p51/p66 V106A mutant after 30 mins using alpha-[32P]dATP by liquid scintillation counting B 7.3 pIC50 50 nM IC50 Medchemcomm (2013) 4: 1443-1451
ChEMBL Inhibition of recombinant wild type HIV1 RT using poly(rA)/oligo(dT)16 as template after 40 mins by spectrofluorometric analysis B 7.32 pIC50 48 nM IC50 Eur J Med Chem (2013) 65: 134-143 [PMID:23707918]
ChEMBL Inhibitory activity against HIV-1 reverse transcriptase enzyme B 7.32 pIC50 48 nM IC50 Bioorg Med Chem Lett (1999) 9: 2805-2810 [PMID:10522695]
ChEMBL Inhibitory concentration for 50% inhibition of HIV-1 reverse transcriptase B 7.32 pIC50 48 nM IC50 Bioorg Med Chem Lett (2000) 10: 1729-1731 [PMID:10937734]
ChEMBL Inhibitory activity against HIV-1 reverse transcriptase B 7.32 pIC50 48 nM IC50 Bioorg Med Chem Lett (1999) 9: 3221-3224 [PMID:10576692]
ChEMBL Inhibition of HIV-1 reverse transcriptase. B 7.32 pIC50 48 nM IC50 Bioorg Med Chem Lett (2001) 11: 1943-1945 [PMID:11459666]
ChEMBL Inhibitory activity against HIV-1 reverse transcriptase B 7.33 pIC50 47 nM IC50 Bioorg Med Chem Lett (2001) 11: 619-622 [PMID:11266155]
ChEMBL Compound was evaluated for the inhibition of HIV-1 Reverse transcriptase F 7.33 pIC50 47 nM IC50 J Med Chem (2000) 43: 2019-2030 [PMID:10821714]
ChEMBL The compound was evaluated for the inhibition of HIV-1 reverse transcriptase B 7.33 pIC50 47 nM IC50 Bioorg Med Chem Lett (2000) 10: 193-195 [PMID:10673109]
ChEMBL Tested for inhibitory concentration against HIV-1 non-nucleoside reverse transcriptase B 7.33 pIC50 47 nM IC50 Bioorg Med Chem Lett (2001) 11: 211-214 [PMID:11206461]
ChEMBL Inhibition of the NNRTI HIV-1 enzyme by 50% using enzyme assay. B 7.33 pIC50 47 nM IC50 Bioorg Med Chem Lett (2001) 11: 309-312 [PMID:11212098]
ChEMBL 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 B 7.36 pIC50 44 nM IC50 Eur J Med Chem (2015) 97: 1-9 [PMID:25935383]
ChEMBL Inhibition of reverse transcriptase activity in HIV1 NL4-3 infected MT4 cells before dialysis B 7.38 pIC50 42 nM IC50 Antimicrob Agents Chemother (2007) 51: 638-644 [PMID:17116672]
ChEMBL Inhibition of RNA-dependent DNA polymerase activity of HIV1 reverse transcriptase Y181C mutant B 7.4 pIC50 40 nM IC50 J Med Chem (2009) 52: 1219-1223 [PMID:19175319]
ChEMBL Inhibition of HIV1 RT V106A mutant B 7.4 pIC50 40 nM IC50 J Med Chem (2005) 48: 7153-7165 [PMID:16279773]
ChEMBL Inhibition of RNA-dependent DNA polymerase activity of Human immunodeficiency virus 1 recombinant reverse transcriptase expressed in Escherichia coli using poly(rA)oligo(dT) template primer after 30 min B 7.4 pIC50 40 nM IC50 Med Chem Res (2006) 15: 492-510
ChEMBL 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 B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2017) 140: 383-391 [PMID:28987601]
ChEMBL Inhibition of recombinant wild type HIV1 p66/p51 using poly(rA) template/oligo(dT)16 primer after 40 mins by PicoGreen-based spectrofluorometric method B 7.42 pIC50 38 nM IC50 Eur J Med Chem (2016) 121: 352-363 [PMID:27267005]
ChEMBL Compound was evaluated for its ability to inhibit HIV-1 Reverse Transcriptase in an in vitro enzyme assay B 7.42 pIC50 38 nM IC50 Bioorg Med Chem Lett (2001) 11: 1389-1392 [PMID:11378361]
ChEMBL Inhibition of HIV1 reverse transcriptase B 7.42 pIC50 38 nM IC50 Eur J Med Chem (2016) 108: 455-465 [PMID:26708112]
ChEMBL Inhibition of wild-type HIV1 reverse transcriptase p66/p51 after 40 mins by spectrophotometry B 7.42 pIC50 38 nM IC50 Bioorg Med Chem (2014) 22: 2535-2541 [PMID:24680058]
ChEMBL Inhibition of HIV1 reverse transcriptase B 7.42 pIC50 38 nM IC50 J Med Chem (2019) 62: 4851-4883 [PMID:30516990]
ChEMBL Inhibition of HIV-1 wild type recombinant reverse transcriptase p66/p51 assessed as RNA-DNA heteroduplex formation using poly(rA) template/oligo(dT)16 primer incubated prior to enzyme addition by spectrofluorometer analysis B 7.43 pIC50 37 nM IC50 Medchemcomm (2014) 5: 468-473
ChEMBL 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 B 7.43 pIC50 37 nM IC50 Bioorg Med Chem (2013) 21: 6477-6483 [PMID:24055077]
ChEMBL 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 B 7.44 pIC50 36 nM IC50 Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127]
ChEMBL 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 B 7.46 pIC50 35 nM IC50 Eur J Med Chem (2015) 102: 215-222 [PMID:26276435]
ChEMBL 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 B 7.46 pIC50 35 nM IC50 J Med Chem (2021) 64: 8579-8598 [PMID:34106711]
ChEMBL 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 B 7.49 pIC50 32 nM IC50 Bioorg Med Chem (2014) 22: 1459-1467 [PMID:24457088]
ChEMBL Inhibition of recombinant wild type HIV-1 reverse transcriptase using DNA/RNA as substrate incubated for 40 mins by Pico-green dye based spectrofluorometric analysis B 7.52 pIC50 30 nM IC50 J Med Chem (2023) 66: 4755-4767 [PMID:36996328]
ChEMBL Inhibition of RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by filter-based filtration assay B 7.52 pIC50 30 nM IC50 Antimicrob Agents Chemother (2010) 54: 2401-2408 [PMID:20308384]
ChEMBL Inhibition of HIV1 reverse transcriptase Y181C mutant expressed in Escherichia coli BL21 (DE3) using [alpha-32P]dATP after 30 mins by liquid scintillation counting B 7.52 pIC50 30 nM IC50 Medchemcomm (2013) 4: 741-748
ChEMBL Inhibition of HIV1 Reverse transcriptase p51/p66 Y181C mutant after 30 mins using alpha-[32P]dATP by liquid scintillation counting B 7.52 pIC50 30 nM IC50 Medchemcomm (2013) 4: 1443-1451
ChEMBL 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 B 7.52 pIC50 30 nM IC50 Bioorg Med Chem (2017) 25: 3861-3870 [PMID:28559060]
ChEMBL 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 B 7.52 pIC50 30 nM IC50 Bioorg Med Chem (2017) 25: 3861-3870 [PMID:28559060]
ChEMBL 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 B 7.52 pIC50 30 nM IC50 ACS Med Chem Lett (2018) 9: 334-338 [PMID:29670696]
ChEMBL Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye-based spectrofluorometric analysis B 7.52 pIC50 30 nM IC50 J Med Chem (2019) 62: 11430-11436 [PMID:31714780]
ChEMBL Inhibition of recombinant HIV-1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye based spectrofluorometric assay B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2019) 182: 111603-111603 [PMID:31421633]
ChEMBL Inhibition of HIV1 Reverse transcriptase incubated for 30 mins by fluorescence based analysis B 7.52 pIC50 30 nM IC50 J Med Chem (2023) 66: 6193-6217 [PMID:37130343]
ChEMBL Inhibition of wild type HIV1 p66/p51 reverse transcriptase by spectrofluorometry B 7.62 pIC50 24 nM IC50 Bioorg Med Chem (2015) 23: 624-631 [PMID:25537532]
ChEMBL 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 B 7.66 pIC50 22 nM IC50 Bioorg Med Chem (2015) 23: 1069-1081 [PMID:25638501]
ChEMBL Inhibition of recombinant HIV1 Reverse transcriptase p66/p51 using poly (rA)-oligo (dT) as template primer after 40 mins by spectrofluorometric analysis B 7.66 pIC50 22 nM IC50 Bioorg Med Chem (2015) 23: 6587-6593 [PMID:26385446]
ChEMBL 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 B 7.66 pIC50 22 nM IC50 Bioorg Med Chem (2015) 23: 4248-4255 [PMID:26162497]
ChEMBL Inhibition of wild-type HIV1 Reverse transcriptase p66/p51 assessed as relative fluorescence signal after 40 mins B 7.66 pIC50 22 nM IC50 Bioorg Med Chem (2015) 23: 3860-3868 [PMID:25907370]
ChEMBL Inhibitory concentration against HIV-1 mutant reverse transcriptase (Y181C) B 7.7 pIC50 20 nM IC50 J Med Chem (2005) 48: 3858-3873 [PMID:15916438]
ChEMBL 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 B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2014) 87: 52-62 [PMID:25240095]
ChEMBL 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 B 7.7 pIC50 20 nM IC50 Bioorg Med Chem (2018) 26: 2051-2060 [PMID:29559197]
ChEMBL Inhibition of HIV1 virion-associated reverse transcriptase B 7.7 pIC50 20 nM IC50 Bioorg Med Chem (2008) 16: 6353-6363 [PMID:18502646]
ChEMBL 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 B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311]
ChEMBL Inhibition of HIV1 reverse transcriptase L100I mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311]
ChEMBL 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 PicoGreen dye based spectrofluorometric analysis B 7.72 pIC50 19 nM IC50 Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935]
ChEMBL 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 PicoGreen dye based spectrofluorometric analysis B 7.72 pIC50 19 nM IC50 Bioorg Med Chem (2017) 25: 3861-3870 [PMID:28559060]
ChEMBL Inhibition of HIV1 RT polymerase K103N mutant by SPA B 7.72 pIC50 18.9 nM IC50 J Med Chem (2008) 51: 6503-6511 [PMID:18826204]
ChEMBL Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase DNA-dependent DNA polymerase activity by gel-based primer extension assay B 7.74 pIC50 18 nM IC50 Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127]
ChEMBL Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA PPT primed substrate by scintillation proximity assay B 7.77 pIC50 17 nM IC50 J Biol Chem (2007) 282: 8005-8010 [PMID:17172472]
ChEMBL Inhibition of wild type HIV-1 reverse transcriptase assessed as assessed as inhibition of biotin deoxyuridine triphosphate incorporation into protein B 7.8 pIC50 16 nM IC50 Eur J Med Chem (2023) 247: 115042-115042 [PMID:36577220]
ChEMBL Inhibitory concentration against HIV-1 wild type reverse transcriptase (IIIB) B 7.85 pIC50 14 nM IC50 J Med Chem (2005) 48: 3858-3873 [PMID:15916438]
ChEMBL Inhibition of RNA-dependent DNA polymerase activity of wild type HIV1 reverse transcriptase B 7.85 pIC50 14 nM IC50 J Med Chem (2009) 52: 1219-1223 [PMID:19175319]
ChEMBL Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into template incubated for 1 hr by ELISA B 7.85 pIC50 14 nM IC50 Eur J Med Chem (2019) 182: 111619-111619 [PMID:31434039]
ChEMBL Inhibition of HIV1 recombinant wild type reverse transcriptase B 7.85 pIC50 14 nM IC50 Bioorg Med Chem (2008) 16: 4173-4185 [PMID:18226533]
ChEMBL Inhibition of wild type recombinant HIV-1 reverse transcriptase assessed as reduction of biotin-dUTP incorporation into protein using ABTS as substrate incubated for 1 hrs by ELISA analysis B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2023) 247: 115045-115045 [PMID:36577216]
ChEMBL Inhibition of HIV1 reverse transcriptase-associated RNA-dependent DNA polymerase activity after 30 mins B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2015) 93: 452-460 [PMID:25728026]
ChEMBL 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 B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2023) 246: 114957-114957 [PMID:36446205]
ChEMBL Inhibition of recombinant wild-type p66/p51 HIV-1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2022) 238: 114512-114512 [PMID:35679690]
ChEMBL Inhibition of HIV-1 reverse transcriptase using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorometric analysis B 7.96 pIC50 11 nM IC50 J Med Chem (2022) 65: 8478-8492 [PMID:35649164]
ChEMBL Inhibition of HIV1 isolate R8 reverse transcriptase K103N mutant after 90 mins by electrochemiluminescence analysis B 7.99 pIC50 10.2 nM IC50 Antimicrob Agents Chemother (2009) 53: 2424-2431 [PMID:19289522]
ChEMBL Inhibition of wild type HIV1 reverse transcriptase using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis B 8 pIC50 10 nM IC50 Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311]
ChEMBL Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis B 8 pIC50 10 nM IC50 J Med Chem (2022) 65: 2122-2138 [PMID:35073089]
ChEMBL Inhibition of HIV1 reverse transcriptase Y181C mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis B 8 pIC50 10 nM IC50 Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311]
ChEMBL Inhibition of HIV1 wild type reverse transcriptase p66/p51 using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry B 8 pIC50 10 nM IC50 Bioorg Med Chem (2016) 24: 2476-2485 [PMID:27112451]
ChEMBL Inhibition of HIV1 reverse transcriptase E138K mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis B 8 pIC50 10 nM IC50 Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311]
ChEMBL Inhibition of HIV1 wild type reverse transcriptase expressed in Escherichia coli BL21 (DE3) using [alpha-32P]dATP after 30 mins by liquid scintillation counting B 8 pIC50 10 nM IC50 Medchemcomm (2013) 4: 741-748
ChEMBL Inhibition of wild-type HIV1 Reverse transcriptase p51/p66 after 30 mins using alpha-[32P]dATP by liquid scintillation counting B 8 pIC50 10 nM IC50 Medchemcomm (2013) 4: 1443-1451
ChEMBL Inhibition of HIV-1 reverse transcriptase assessed as assessed as reduction of biotin-dUTP incorporation into protein incubated for 1 hrs by ELISA analysis B 8 pIC50 10 nM IC50 J Med Chem (2023) 66: 8643-8665 [PMID:37255025]
ChEMBL 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 B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2016) 26: 4101-4105 [PMID:27390064]
ChEMBL Inhibition of reverse transcriptase activity in HIV1 infected HeLa-MAGI cells at 37 deg C after 48 hrs B 8 pIC50 10 nM IC50 Antimicrob Agents Chemother (2007) 51: 638-644 [PMID:17116672]
ChEMBL Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis B 8 pIC50 10 nM IC50 J Med Chem (2021) 64: 5067-5081 [PMID:33851529]
ChEMBL Inhibition of HIV-1 reverse transcriptase using [2,8-3H]dGTP as substrate by fluorescence based assay B 8 pIC50 10 nM IC50 Eur J Med Chem (2023) 248: 115114-115114 [PMID:36640458]
ChEMBL 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 B 8 pIC50 10 nM IC50 J Med Chem (2021) 64: 10297-10311 [PMID:34197708]
ChEMBL Inhibition of HIV1 reverse transcriptase Y188C mutant in 293T cells B 8.02 pIC50 9.5 nM IC50 Bioorg Med Chem Lett (2006) 16: 3034-3038 [PMID:16527484]
ChEMBL Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into template incubated for 1 hr by ELISA B 8.09 pIC50 8.13 nM IC50 Eur J Med Chem (2021) 213: 113051-113051 [PMID:33279288]
ChEMBL Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into template incubated for 1 hr by ELISA B 8.09 pIC50 8.1 nM IC50 Eur J Med Chem (2021) 213: 113051-113051 [PMID:33279288]
ChEMBL Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into wild type RT measured after 1 hr by ELISA B 8.1 pIC50 8 nM IC50 Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378]
ChEMBL Inhibition of HIV1 RT polymerase Y181C mutant by SPA B 8.14 pIC50 7.2 nM IC50 J Med Chem (2008) 51: 6503-6511 [PMID:18826204]
ChEMBL Inhibition of HIV1 reverse transcriptase activity by primer extension assay B 8.14 pIC50 7.2 nM IC50 Antimicrob Agents Chemother (2010) 54: 4451-4463 [PMID:20660667]
ChEMBL 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 B 8.15 pIC50 7.08 nM IC50 J Med Chem (2019) 62: 2083-2098 [PMID:30721060]
ChEMBL 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 B 8.15 pIC50 7 nM IC50 Bioorg Med Chem (2019) 27: 447-456 [PMID:30606670]
ChEMBL 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 B 8.15 pIC50 7 nM IC50 J Med Chem (2019) 62: 2083-2098 [PMID:30721060]
ChEMBL Inhibition of wild-type HIV1 reverse transcriptase infected in human MT4 cells assessed as reduction in biotin-dUTP incorporation B 8.22 pIC50 6 nM IC50 ACS Med Chem Lett (2018) 9: 370-375 [PMID:29670703]
ChEMBL Inhibition of HIV1 reverse transcriptase Y181C mutant in 293T cells B 8.22 pIC50 6 nM IC50 Bioorg Med Chem Lett (2006) 16: 3034-3038 [PMID:16527484]
ChEMBL 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 B 8.22 pIC50 6 nM IC50 Eur J Med Chem (2019) 176: 11-20 [PMID:31091477]
ChEMBL HIV-1 reverse transcriptase inhibitory activity against Cys181 mutant using (poly)rC600*(oligo)dGT as template primer. B 8.22 pIC50 6 nM IC50 J Med Chem (1999) 42: 4150-4160 [PMID:10514285]
ChEMBL Inhibition of HIV1 reverse transcriptase RNA-dependent DNA polymerase activity assessed as incorporation of radioactive dTTP into poly(rA)/oligo(DT) B 8.4 pIC50 4 nM IC50 Bioorg Med Chem (2008) 16: 7429-7435 [PMID:18585918]
ChEMBL 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 mins by PicoGreen dye based spectrofluorometric analysis B 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2018) 28: 3491-3495 [PMID:30318436]
ChEMBL HIV-1 reverse transcriptase inhibitory activity against Wild Type Reverse transcriptase using (poly)rC600*(oligo)dGT as template primer. B 8.4 pIC50 4 nM IC50 J Med Chem (1999) 42: 4150-4160 [PMID:10514285]
ChEMBL Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase B 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2007) 17: 1956-1960 [PMID:17276064]
ChEMBL Inhibition of HIV1 recombinant RNA-dependent DNA polymerase activity of reverse transcriptase assessed as incorporation of radioactive dTTP into poly(rA)/oligo(dT) B 8.4 pIC50 4 nM IC50 Bioorg Med Chem (2009) 17: 5962-5967 [PMID:19616956]
ChEMBL Inhibition of RNA-dependent DNA polymerase activity of HIV1 reverse transcriptase using poly(rA)/pligo(dT) template B 8.4 pIC50 4 nM IC50 Bioorg Med Chem (2010) 18: 1702-1710 [PMID:20097079]
ChEMBL Concentration required to protect the cell against HIV-1 strain IIIB viral cytopathogenicity by 50% in MT-4 cells F 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2004) 14: 3173-3176 [PMID:15149669]
ChEMBL Inhibition of RNA-dependent DNA polymerase activity of wild type Human immunodeficiency virus 1 reverse transcriptase B 8.52 pIC50 3 nM IC50 Eur J Med Chem (2012) 50: 216-229 [PMID:22361685]
ChEMBL 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 B 8.7 pIC50 2 nM IC50 Eur J Med Chem (2018) 145: 726-734 [PMID:29353724]
ChEMBL Inhibition of wild-type HIV1 reverse transcriptase B 8.89 pIC50 1.3 nM IC50 Eur J Med Chem (2009) 44: 2190-2201 [PMID:19058881]
ChEMBL Inhibition of wild type Human immunodeficiency virus 1 reverse transcriptase after 30 min by fluorescence microplate reader analysis B 8.89 pIC50 1.3 nM IC50 Med Chem Res (2010) 19: 311-336
ChEMBL Inhibition of wild type HIV1 RT polymerase by SPA B 9 pIC50 1 nM IC50 J Med Chem (2008) 51: 6503-6511 [PMID:18826204]
ChEMBL Inhibition of wild type HIV1 reverse transcriptase in 293T cells B 9.1 pIC50 0.8 nM IC50 Bioorg Med Chem Lett (2006) 16: 3034-3038 [PMID:16527484]
ChEMBL Inhibitory concentration against wild-type reverse transcriptase of HIV-1 B 9.12 pIC50 0.75 nM IC50 J Med Chem (2004) 47: 1175-1182 [PMID:14971897]
ChEMBL Inhibition of HIV1 isolate R8 reverse transcriptase after 90 mins B 9.38 pIC50 0.42 nM IC50 Antimicrob Agents Chemother (2009) 53: 2424-2431 [PMID:19289522]
ChEMBL Inhibition of HIV1 isolate R8 reverse transcriptase Y181C mutant after 90 mins by electrochemiluminescence analysis B 9.51 pIC50 0.31 nM IC50 Antimicrob Agents Chemother (2009) 53: 2424-2431 [PMID:19289522]
ChEMBL Inhibition of HIV1 recombinant reverse transcriptase assessed as incorporation of [32P]GTP into poly(rC).oligo(dG) template primer B 9.78 pIC50 0.17 nM IC50 Medchemcomm (2014) 5: 1685-1692
ChEMBL Inhibition of HIV-1BH10 reverse transcriptase expressed in Escherichia coli assessed as polymerization by real time FRET assay B 10.04 pIC50 0.09 nM IC50 Eur J Med Chem (2020) 186: 111900-111900 [PMID:31771827]
ChEMBL 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 B 10.04 pIC50 0.09 nM IC50 Eur J Med Chem (2021) 220: 113498-113498 [PMID:33933756]
ChEMBL 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 B 6.29 pEC50 514 nM EC50 J Med Chem (2017) 60: 4424-4443 [PMID:28481112]
ChEMBL 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 B 6.42 pEC50 380 nM EC50 Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378]
ChEMBL 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 B 6.46 pEC50 348 nM EC50 J Med Chem (2017) 60: 4424-4443 [PMID:28481112]
ChEMBL 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 B 6.51 pEC50 308 nM EC50 J Med Chem (2017) 60: 4424-4443 [PMID:28481112]
ChEMBL Antiviral activity against HIV1 Y188L mutant in MT4 cells by MTT assay F 6.52 pEC50 300 nM EC50 Bioorg Med Chem Lett (2006) 16: 3541-3544 [PMID:16621553]
ChEMBL 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 B 6.59 pEC50 260 nM EC50 Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378]
ChEMBL 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 B 6.65 pEC50 224 nM EC50 ACS Med Chem Lett (2018) 9: 370-375 [PMID:29670703]
ChEMBL Antiviral activity against HIV1 IRLL98 in MT4 cells by MTT assay F 6.7 pEC50 200 nM EC50 Bioorg Med Chem Lett (2006) 16: 3541-3544 [PMID:16621553]
ChEMBL 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 B 6.77 pEC50 171.1 nM EC50 Eur J Med Chem (2020) 202: 112549-112549 [PMID:32712537]
ChEMBL 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 B 6.8 pEC50 160 nM EC50 Bioorg Med Chem (2017) 25: 2491-2497 [PMID:28314514]
ChEMBL 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 B 6.81 pEC50 156.17 nM EC50 Eur J Med Chem (2018) 157: 310-319 [PMID:30099253]
ChEMBL 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 B 6.94 pEC50 115 nM EC50 J Med Chem (2017) 60: 4424-4443 [PMID:28481112]
ChEMBL 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 B 7 pEC50 101 nM EC50 Eur J Med Chem (2016) 122: 185-195 [PMID:27371922]
ChEMBL Inhibition of HIV-1 p66/p51 reverse transcriptase K103N mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis B 7.04 pEC50 91.5 nM EC50 J Med Chem (2021) 64: 5067-5081 [PMID:33851529]
ChEMBL 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 B 7.1 pEC50 80.1 nM EC50 J Med Chem (2017) 60: 4424-4443 [PMID:28481112]
ChEMBL 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 B 7.12 pEC50 76 nM EC50 Eur J Med Chem (2020) 202: 112549-112549 [PMID:32712537]
ChEMBL 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 B 7.15 pEC50 71 nM EC50 Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378]
ChEMBL Antiviral activity against HIV1 K103N mutant in MT4 cells by MTT assay F 7.24 pEC50 57 nM EC50 Bioorg Med Chem Lett (2006) 16: 3541-3544 [PMID:16621553]
ChEMBL 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 B 7.24 pEC50 57 nM EC50 Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935]
ChEMBL 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 B 7.32 pEC50 47.5 nM EC50 Eur J Med Chem (2020) 202: 112549-112549 [PMID:32712537]
ChEMBL Inhibition of HIV-1 p66/p51 reverse transcriptase L100I mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis B 7.35 pEC50 44.7 nM EC50 J Med Chem (2021) 64: 5067-5081 [PMID:33851529]
ChEMBL 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 B 7.36 pEC50 44 nM EC50 Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935]
ChEMBL 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 B 7.42 pEC50 38 nM EC50 Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935]
ChEMBL Inhibition of HIV1 reverse transcriptase K103N mutant by scintillation counting assay B 7.47 pEC50 34 nM EC50 Bioorg Med Chem Lett (2008) 18: 4352-4354 [PMID:18632268]
ChEMBL 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 B 7.51 pEC50 31 nM EC50 Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378]
ChEMBL 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 B 7.54 pEC50 29 nM EC50 Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935]
ChEMBL 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 B 7.8 pEC50 16 nM EC50 Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935]
ChEMBL 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 B 8.09 pEC50 8.2 nM EC50 J Med Chem (2017) 60: 4424-4443 [PMID:28481112]
ChEMBL 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 B 8.15 pEC50 7 nM EC50 Eur J Med Chem (2020) 202: 112549-112549 [PMID:32712537]
ChEMBL Inhibition of HIV-1 p66/p51 reverse transcriptase Y181C mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis B 8.27 pEC50 5.4 nM EC50 J Med Chem (2021) 64: 5067-5081 [PMID:33851529]
ChEMBL 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 B 8.28 pEC50 5.2 nM EC50 Bioorg Med Chem (2017) 25: 2491-2497 [PMID:28314514]
ChEMBL 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 B 8.28 pEC50 5.19 nM EC50 J Med Chem (2017) 60: 4424-4443 [PMID:28481112]
ChEMBL 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 B 8.3 pEC50 5 nM EC50 Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935]
ChEMBL 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 B 8.3 pEC50 5 nM EC50 Eur J Med Chem (2016) 122: 185-195 [PMID:27371922]
ChEMBL 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 B 8.3 pEC50 5 nM EC50 Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378]
ChEMBL 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 B 8.32 pEC50 4.8 nM EC50 Eur J Med Chem (2020) 202: 112549-112549 [PMID:32712537]
ChEMBL 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 B 8.4 pEC50 4 nM EC50 Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935]
ChEMBL Concentration required to inhibit HIV-1 reverse transcriptase activity (wild-type) by 50% B 8.4 pEC50 4 nM EC50 J Med Chem (2005) 48: 4378-4388 [PMID:15974590]
ChEMBL 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 B 8.52 pEC50 3 nM EC50 Eur J Med Chem (2018) 158: 371-392 [PMID:30223123]
ChEMBL Inhibition of wild-type HIV1 3B reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay B 8.55 pEC50 2.85 nM EC50 ACS Med Chem Lett (2018) 9: 370-375 [PMID:29670703]
ChEMBL Inhibition of HIV1 reverse transcriptase Y181C mutant by scintillation counting assay B 8.7 pEC50 2 nM EC50 Bioorg Med Chem Lett (2008) 18: 4352-4354 [PMID:18632268]
ChEMBL Inhibition of HIV1 wild-type reverse transcriptase by scintillation counting assay B 9 pEC50 1 nM EC50 Bioorg Med Chem Lett (2008) 18: 4352-4354 [PMID:18632268]
ChEMBL Antiviral activity against wild type HIV1 NL4-3 in MT4 cells by MTT assay F 9 pEC50 1 nM EC50 Bioorg Med Chem Lett (2006) 16: 3541-3544 [PMID:16621553]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O positive erythrocyte assessed as reduction in parasitemia after 72 hrs F 4.36 pIC50 43820 nM IC50 Bioorg Med Chem (2014) 22: 5241-5248 [PMID:25199582]
CYP3A4 in Human [GtoPdb: 1337] [UniProtKB: P08684]
GtoPdb Inhibition of CYP3A-mediated conversion of triazolam to 4-OH-triazolam in human liver microsomes. - 4.76 pIC50 17500 nM IC50 J Clin Pharmacol (2001) 41: 85-91 [PMID:11225565]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]