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)
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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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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
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  • Reverse transcriptase in Human immunodeficiency virus 1 [ChEMBL: CHEMBL2366516] [UniProtKB: Q9WKE8]
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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
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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 HIV1 RT L100I mutant B 6.92 pIC50 120 nM IC50 J Med Chem (2005) 48: 7153-7165 [PMID:16279773]
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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 enzyme B 7.32 pIC50 48 nM IC50 Bioorg Med Chem Lett (1999) 9: 2805-2810 [PMID:10522695]
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 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 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 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 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 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 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 HIV1 reverse transcriptase Y181C mutant B 7.4 pIC50 40 nM IC50 J Med Chem (2009) 52: 1219-1223 [PMID:19175319]
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 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 J Med Chem (2019) 62: 4851-4883 [PMID:30516990]
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 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 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 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 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 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 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 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 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 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 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 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 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 virion-associated reverse transcriptase B 7.7 pIC50 20 nM IC50 Bioorg Med Chem (2008) 16: 6353-6363 [PMID:18502646]
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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856]
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]
Reverse transcriptase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366516] [UniProtKB: Q9WKE8]
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 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 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 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 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 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 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 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 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 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 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 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 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 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 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]
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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]