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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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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]